Nothing Special   »   [go: up one dir, main page]

PL3630761T3 - Inhibitory KRAS G12C i sposoby ich zastosowania - Google Patents

Inhibitory KRAS G12C i sposoby ich zastosowania

Info

Publication number
PL3630761T3
PL3630761T3 PL18731624T PL18731624T PL3630761T3 PL 3630761 T3 PL3630761 T3 PL 3630761T3 PL 18731624 T PL18731624 T PL 18731624T PL 18731624 T PL18731624 T PL 18731624T PL 3630761 T3 PL3630761 T3 PL 3630761T3
Authority
PL
Poland
Prior art keywords
kras
inhibitors
methods
same
Prior art date
Application number
PL18731624T
Other languages
English (en)
Inventor
Brian Alan Lanman
Jian Chen
Anthony B. Reed
Victor J. Cee
Longbin Liu
David John Kopecky
Patricia Lopez
Ryan Paul Wurz
Thomas T. Nguyen
Shon Booker
Nobuko Nishimura
Youngsook Shin
Nuria A. Tamayo
John Gordon Allen
Jennifer Rebecca Allen
Original Assignee
Amgen Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Amgen Inc. filed Critical Amgen Inc.
Publication of PL3630761T3 publication Critical patent/PL3630761T3/pl

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/34—Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
PL18731624T 2017-05-22 2018-05-21 Inhibitory KRAS G12C i sposoby ich zastosowania PL3630761T3 (pl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762509629P 2017-05-22 2017-05-22
EP18731624.5A EP3630761B1 (en) 2017-05-22 2018-05-21 Kras g12c inhibitors and methods of using the same
PCT/US2018/033714 WO2018217651A1 (en) 2017-05-22 2018-05-21 Kras g12c inhibitors and methods of using the same

Publications (1)

Publication Number Publication Date
PL3630761T3 true PL3630761T3 (pl) 2022-04-11

Family

ID=62620997

Family Applications (1)

Application Number Title Priority Date Filing Date
PL18731624T PL3630761T3 (pl) 2017-05-22 2018-05-21 Inhibitory KRAS G12C i sposoby ich zastosowania

Country Status (37)

Country Link
US (4) US10519146B2 (pl)
EP (2) EP3630761B1 (pl)
JP (4) JP6785819B2 (pl)
KR (4) KR102300499B1 (pl)
CN (2) CN110997668B (pl)
AR (9) AR111882A1 (pl)
AU (3) AU2018273356B2 (pl)
BR (1) BR112019024525B1 (pl)
CA (1) CA3063469C (pl)
CL (2) CL2019003394A1 (pl)
CO (1) CO2019013010A2 (pl)
CR (2) CR20190534A (pl)
CY (1) CY1125289T1 (pl)
DK (1) DK3630761T3 (pl)
EA (1) EA201992781A1 (pl)
ES (1) ES2905676T3 (pl)
HR (1) HRP20212017T1 (pl)
HU (1) HUE057632T2 (pl)
IL (2) IL270490B (pl)
JO (1) JOP20190272A1 (pl)
LT (1) LT3630761T (pl)
MA (1) MA48772B1 (pl)
MX (2) MX2019013858A (pl)
NZ (1) NZ758786A (pl)
PE (1) PE20200733A1 (pl)
PH (1) PH12019502579A1 (pl)
PL (1) PL3630761T3 (pl)
PT (1) PT3630761T (pl)
RS (1) RS62800B1 (pl)
SA (2) SA522432081B1 (pl)
SG (1) SG10201913195RA (pl)
SI (1) SI3630761T1 (pl)
TW (2) TWI834294B (pl)
UA (1) UA127968C2 (pl)
UY (1) UY37744A (pl)
WO (1) WO2018217651A1 (pl)
ZA (3) ZA201907651B (pl)

Families Citing this family (175)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201913491PA (en) 2016-12-22 2020-03-30 Amgen Inc Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer
JOP20190272A1 (ar) * 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3679040B1 (en) 2017-09-08 2022-08-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
AU2019249231B2 (en) 2018-04-04 2022-04-21 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
AU2019262599B2 (en) 2018-05-04 2023-10-12 Amgen Inc. KRAS G12C inhibitors and methods of using the same
CA3098574A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
CA3099045A1 (en) * 2018-05-10 2019-11-14 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
MX2020012731A (es) 2018-06-01 2021-02-22 Amgen Inc Inhibidores de kras g12c y metodos para su uso.
WO2019241157A1 (en) * 2018-06-11 2019-12-19 Amgen Inc. Kras g12c inhibitors for treating cancer
JP7369719B2 (ja) 2018-06-12 2023-10-26 アムジエン・インコーポレーテツド ＫＲａｓ Ｇ１２Ｃ阻害剤及びそれを使用する方法
FI3814347T3 (fi) 2018-06-27 2023-06-12 Bristol Myers Squibb Co Naftyridinoniyhdisteitä, jotka ovat käyttökelpoisia t-solun aktivoijina
BR112020026681A2 (pt) 2018-06-27 2021-04-06 Bristol-Myers Squibb Company Compostos naftiridinona substituídos úteis como ativadores de célula t
WO2020085504A1 (ja) 2018-10-26 2020-04-30 大鵬薬品工業株式会社 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法
JP7516029B2 (ja) * 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
MA55136A (fr) 2018-11-19 2022-02-23 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
JP7377679B2 (ja) * 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
KR20210103498A (ko) 2018-12-10 2021-08-23 아이디어야 바이오사이언시스 인코포레이티드 메티오닌 아데노실트랜스퍼라제 2a 억제제로서 2-옥소퀴나졸린 유도체
US20220064141A1 (en) * 2019-01-29 2022-03-03 Brightgene Bio-Medical Technology Co., Ltd. Benzopyridone heterocyclic compound and use thereof
CN113382774A (zh) 2019-02-12 2021-09-10 诺华股份有限公司 包含tno155和krasg12c抑制剂的药物组合
JP2022529523A (ja) * 2019-04-22 2022-06-22 ユニバーシティ オブ ピッツバーグ －オブ ザ コモンウェルス システム オブ ハイヤー エデュケイション 小児対象において神経膠腫を治療するためのｔｇ０２の使用
KR20220012255A (ko) * 2019-04-28 2022-02-03 젠플리트 테라퓨틱스 (상하이) 아이엔씨. 옥사아자퀴나졸린-7(8h)-케톤 화합물, 이의 제조 방법 및 이의 약학적 응용
EP3738593A1 (en) * 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
EP3972972A1 (en) 2019-05-21 2022-03-30 Amgen Inc. Solid state forms
PE20220504A1 (es) 2019-05-21 2022-04-07 Amgen Inc Formas en estado solido
CN112585129B (zh) 2019-05-21 2022-03-01 益方生物科技(上海)股份有限公司 杂环化合物，其制备方法和用途
US20220213100A1 (en) * 2019-05-29 2022-07-07 Shanghai Hansoh Biomedical Co., Ltd. Nitrogen-containing heterocyclic derivative regulator, preparation method therefor and application thereof
CN112552294B (zh) * 2019-09-10 2023-12-19 上海翰森生物医药科技有限公司 含哌嗪杂环类衍生物抑制剂、其制备方法和应用
CN113396147B (zh) * 2019-05-31 2024-06-18 上海翰森生物医药科技有限公司 芳香杂环类衍生物调节剂、其制备方法和应用
JP2022539341A (ja) * 2019-06-24 2022-09-08 クヮントン ニューオップ バイオファーマシューティカルズ カンパニー， リミテッド Ｋｒａｓ ｇ１２ｃの阻害剤としての複素環式化合物
CN113993860B (zh) * 2019-06-25 2023-08-01 正大天晴药业集团股份有限公司 作为kras g12c突变蛋白抑制剂的七元杂环类衍生物
CN110256421A (zh) * 2019-06-26 2019-09-20 微境生物医药科技(上海)有限公司 Kras-g12c抑制剂
WO2021000885A1 (zh) * 2019-07-01 2021-01-07 江苏恒瑞医药股份有限公司 喹唑啉酮类衍生物、其制备方法及其在医药上的应用
CN112300194B (zh) * 2019-07-30 2022-01-14 上海凌达生物医药有限公司 一类稠环吡啶酮类化合物、制备方法和用途
CA3149403A1 (en) * 2019-08-02 2021-02-11 Shanghai Jemincare Pharmaceuticals Co., Ltd Tetracyclic compound, preparation method and use thereof
WO2021023247A1 (en) * 2019-08-07 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitor
CN112390788A (zh) * 2019-08-13 2021-02-23 苏州闻天医药科技有限公司 一种用于抑制krasg12c突变蛋白的化合物及其制备方法和用途
CN112390797A (zh) * 2019-08-15 2021-02-23 微境生物医药科技(上海)有限公司 新型螺环类K-Ras G12C抑制剂
CN112390796B (zh) * 2019-08-19 2023-06-27 贝达药业股份有限公司 Kras g12c抑制剂及其在医药上的应用
AR119821A1 (es) 2019-08-28 2022-01-12 Bristol Myers Squibb Co Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t
WO2021047603A1 (zh) 2019-09-11 2021-03-18 凯瑞斯德生化(苏州)有限公司 一种应用于kras抑制剂类药物杂环中间体的合成方法
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
CA3155066A1 (en) * 2019-09-20 2021-03-25 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
EP4034123A4 (en) * 2019-09-24 2023-11-01 Mirati Therapeutics, Inc. COMBINATION THERAPIES
EP4045047A1 (en) 2019-10-15 2022-08-24 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
US20240190862A1 (en) 2019-10-24 2024-06-13 Amgen Inc. Epoxyamides as kras g12c and kras g12d inhibitors and methods of using the same
CN112225734B (zh) * 2019-10-25 2021-12-07 南京瑞捷医药科技有限公司 Kras g12c抑制剂及其用途
MX2022005053A (es) * 2019-10-28 2022-05-18 Merck Sharp & Dohme Llc Inhibidores de peque?as moleculas de mutante g12c de kras.
JP2023502891A (ja) * 2019-10-30 2023-01-26 ▲勁▼方医▲薬▼科技（上海）有限公司 置換された複素環－環系化合物、その調製方法及び医薬への応用
CR20220243A (es) 2019-11-04 2022-08-04 Revolution Medicines Inc Inhibidores de ras
MX2022005357A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
PE20221278A1 (es) 2019-11-04 2022-09-05 Revolution Medicines Inc Inhibidores de ras
AR120456A1 (es) 2019-11-14 2022-02-16 Amgen Inc Síntesis mejorada del compuesto inhibidor de g12c de kras
EP4058453A1 (en) 2019-11-14 2022-09-21 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
CN114630832A (zh) * 2019-11-15 2022-06-14 四川海思科制药有限公司 一种嘧啶并环衍生物及其在医药上的应用
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
BR112022010278A2 (pt) 2019-11-27 2022-10-04 Turning Point Therapeutics Inc Terapia combinada que envolve compostos macrocíclicos de diarila
CN111377918B (zh) * 2019-11-29 2021-03-02 苏州信诺维医药科技有限公司 一种kras抑制剂化合物
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
WO2021104431A1 (zh) * 2019-11-29 2021-06-03 苏州信诺维医药科技股份有限公司 Kras g12c抑制剂化合物及其用途
WO2021113595A1 (en) * 2019-12-06 2021-06-10 Beta Pharma, Inc. Phosphorus derivatives as kras inhibitors
AU2020401223A1 (en) * 2019-12-10 2022-06-23 The Board Of Regents Of The University Of Texas System Compositions and methods for substituted 7-(piperazin-1-yl)pyrazolo[1,5-a]pyrimidine analogs as inhibitors of KRAS
WO2021126816A1 (en) 2019-12-16 2021-06-24 Amgen Inc. Dosing regimen of a kras g12c inhibitor
WO2021120045A1 (en) * 2019-12-18 2021-06-24 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
WO2021121367A1 (en) * 2019-12-19 2021-06-24 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
AR120823A1 (es) 2019-12-23 2022-03-23 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos útiles como activadores de células t
WO2021139678A1 (zh) * 2020-01-07 2021-07-15 广州百霆医药科技有限公司 吡啶并嘧啶类kras g12c突变蛋白抑制剂
WO2021139748A1 (en) 2020-01-08 2021-07-15 Ascentage Pharma (Suzhou) Co., Ltd. Spirocyclic tetrahydroquinazolines
CN111205286B (zh) * 2020-01-13 2022-12-13 中科苏州药物研究院 作为kras g12c突变蛋白抑制剂的腈甲基哌嗪类衍生物及其应用
CN114671866A (zh) * 2020-12-25 2022-06-28 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
WO2021150613A1 (en) 2020-01-20 2021-07-29 Incyte Corporation Spiro compounds as inhibitors of kras
WO2021147967A1 (zh) * 2020-01-21 2021-07-29 南京明德新药研发有限公司 作为kras抑制剂的大环类化合物
GB202001344D0 (en) 2020-01-31 2020-03-18 Redx Pharma Plc Ras Inhibitors
CN112159405B (zh) * 2020-02-04 2021-09-14 广州必贝特医药技术有限公司 吡啶并嘧啶酮类化合物及其应用
US11618751B1 (en) 2022-03-25 2023-04-04 Ventus Therapeutics U.S., Inc. Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives
CN113248521B (zh) * 2020-02-11 2023-07-18 上海和誉生物医药科技有限公司 一种k-ras g12c抑制剂及其制备方法和应用
US20230143751A1 (en) 2020-02-24 2023-05-11 Shanghai Zheye Biotechnology Co. Ltd. Aromatic Compound And Use Thereof In Preparing Antineoplastic Drugs
WO2021175199A1 (zh) * 2020-03-02 2021-09-10 上海喆邺生物科技有限公司 一类芳香杂环类化合物及其在药物中的应用
TW202144345A (zh) 2020-03-17 2021-12-01 大陸商北京加科思新藥研發有限公司 Ｋｒａｓ突變蛋白抑制劑
AU2021248363B2 (en) * 2020-04-03 2024-02-15 Medshine Discovery Inc. Octahydropyrazinodiazanaphthyridine dione compounds
WO2021218939A1 (zh) * 2020-04-28 2021-11-04 贝达药业股份有限公司 稠环化合物及其在医药上的应用
WO2021231526A1 (en) 2020-05-13 2021-11-18 Incyte Corporation Fused pyrimidine compounds as kras inhibitors
US20230241073A1 (en) 2020-05-18 2023-08-03 Wellmarker Bio Co., Ltd. Pharmaceutical composition for preventing or treating non-small cell lung cancer associated with ron mutantation, and method using same
WO2021236920A1 (en) * 2020-05-20 2021-11-25 Teva Pharmaceuticals International Gmbh Solid state forms of amg-510 and process for preparation thereof
CN112574199B (zh) * 2020-05-20 2021-05-18 首药控股(北京)股份有限公司 Kras-G12C抑制剂杂环化合物
CN114585624A (zh) * 2020-06-02 2022-06-03 上海喆邺生物科技有限公司 一种手性中间体及其制备方法
CR20220614A (es) 2020-06-02 2023-05-08 Univ Vanderbilt 2-amino-3-cianotiofenos anulados y derivados para el tratamiento del cáncer
WO2021249563A1 (zh) * 2020-06-12 2021-12-16 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
CA3183032A1 (en) 2020-06-18 2021-12-23 Mallika Singh Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
EP4171570A1 (en) 2020-06-24 2023-05-03 Boehringer Ingelheim International GmbH Anticancer combination therapy comprising a sos1 inhibitor and a kras g12c inhibitor
BR112022026186A2 (pt) * 2020-06-25 2023-01-17 Tolremo Therapeutics Ag Combinação de um inibidor de bromodomínio cbp/p300 e um inibidor de kras
CN113929676A (zh) * 2020-07-14 2022-01-14 浙江海正药业股份有限公司 吡啶并杂环类衍生物及其制备方法和用途
CN113980032B (zh) * 2020-07-27 2023-06-16 江苏恒瑞医药股份有限公司 稠合四环类衍生物、其制备方法及其在医药上的应用
CN115052870B (zh) 2020-08-02 2024-02-20 上海喆邺生物科技有限公司 一种芳香类化合物及其在抗肿瘤药物中的应用
WO2022037560A1 (zh) * 2020-08-21 2022-02-24 广东东阳光药业有限公司 嘧啶酮衍生物及其在药物中的应用
US20230295163A1 (en) * 2020-08-21 2023-09-21 Zhejiang Hisun Pharmaceutical Co., Ltd. Tetracyclic derivative, method for preparing same and use thereof in medicine
WO2022047093A1 (en) * 2020-08-28 2022-03-03 Incyte Corporation Vinyl imidazole compounds as inhibitors of kras
AU2021344830A1 (en) 2020-09-03 2023-04-06 Revolution Medicines, Inc. Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
JP2023541916A (ja) 2020-09-15 2023-10-04 レボリューション メディシンズ インコーポレイテッド がんの治療における、ｒａｓ阻害剤としてのインドール誘導体
US11767320B2 (en) 2020-10-02 2023-09-26 Incyte Corporation Bicyclic dione compounds as inhibitors of KRAS
CN116323611A (zh) 2020-10-07 2023-06-23 美国安进公司 使7-氯-6-氟-1-(2-异丙基-4-甲基吡啶-3-基)吡啶并[2,3-d]嘧啶-2,4(1h,3h)-二酮的阻转异构体外消旋和分离的方法
US20230406860A1 (en) 2020-10-27 2023-12-21 Amgen Inc. Heterocyclic spiro compounds and methods of use
AU2021377810A1 (en) * 2020-11-13 2023-05-11 Genentech, Inc. Methods and compositions comprising a krasg12c inhibitor and a vegf inhibitor for treating solid tumors
WO2022109242A1 (en) * 2020-11-20 2022-05-27 Amgen Inc. Process for preparing 7-chloro-6-fluoro-1-(2-isopropyl-4-methylpyridin-3- yl)pyridof[2,3-d]pyrimidine-2,4(1h,3h)-dione
TW202227412A (zh) * 2020-11-24 2022-07-16 大陸商杭州多域生物技術有限公司 一種芳香化合物、其製備方法及應用
CN116390919A (zh) * 2020-11-24 2023-07-04 杭州多域生物技术有限公司 一种芳香化合物、其制备方法及应用
CA3200164A1 (en) * 2020-11-26 2022-06-02 Qingxin Liu Salt and crystal form of nitrogen-containing heterocyclic derivative, preparation method therefor and application thereof
WO2022121839A1 (zh) * 2020-12-08 2022-06-16 上海和誉生物医药科技有限公司 吡啶并[2,3-d]嘧啶-2(1H)-酮衍生物及其制备方法和应用
KR20230151981A (ko) * 2020-12-11 2023-11-02 에라스카, 아이엔씨. 암 치료를 위한 병용 요법
WO2022127847A1 (zh) * 2020-12-17 2022-06-23 广东东阳光药业有限公司 嘧啶酮衍生物及其在药物中的应用
CN116529249A (zh) * 2020-12-18 2023-08-01 正大天晴药业集团股份有限公司 吡啶并嘧啶酮类化合物
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
CN114685502A (zh) * 2020-12-25 2022-07-01 由理生物医药（上海）有限公司 作为kras-g12c抑制剂的螺环类化合物
US20240091230A1 (en) 2021-01-08 2024-03-21 Amgen Inc. Use of kras g12c inhibitor in treating cancers
AU2022234388A1 (en) * 2021-03-10 2023-10-26 Beta Pharma, Inc. Pyridopyrimidine derivatives as kras inhibitors
WO2022188849A1 (en) * 2021-03-11 2022-09-15 InventisBio Co., Ltd. Solid dispersions
CN113018415B (zh) * 2021-03-17 2022-07-01 遵义医科大学 一种药物组合及其应用
WO2022204112A1 (en) 2021-03-22 2022-09-29 Incyte Corporation Imidazole and triazole kras inhibitors
JP2024514127A (ja) 2021-04-09 2024-03-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 抗がん剤療法
EP4329749A1 (en) * 2021-04-27 2024-03-06 Merck Sharp & Dohme LLC Small molecule inhibitors of kras g12c mutant
EP4329888A1 (en) 2021-04-29 2024-03-06 Amgen Inc. 2-aminobenzothiazole compounds and methods of use thereof
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
AU2022270116A1 (en) 2021-05-05 2023-12-21 Revolution Medicines, Inc. Ras inhibitors
JP2024519845A (ja) * 2021-05-19 2024-05-21 ジェネンテック， インコーポレイテッド 併用療法
US20240254122A1 (en) 2021-05-19 2024-08-01 Teva Pharmaceuticals International Gmbh Process for preparation of sotorasib and solid state form thereof
TW202313633A (zh) * 2021-05-25 2023-04-01 美商伊瑞斯卡公司 含硫雜芳族三環ｋｒａｓ抑制劑
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
WO2022262797A1 (en) * 2021-06-18 2022-12-22 Shanghai Antengene Corporation Limited Combination of an erk inhibitor and a kras inhibitor and uses thereof
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途
WO2022269008A1 (en) 2021-06-24 2022-12-29 Sandoz Ag Crystalline form of sotorasib
EP4227305A1 (en) 2022-02-10 2023-08-16 Sandoz AG Crystalline form of sotorasib
EP4384177A1 (en) * 2021-08-10 2024-06-19 Amgen Inc. Heterocyclic compounds and methods of use
KR20240055778A (ko) 2021-09-01 2024-04-29 노파르티스 아게 Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도
EP4389751A1 (en) 2021-09-03 2024-06-26 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
CN114605406B (zh) * 2021-09-18 2023-05-26 都创(上海)医药开发有限公司 Amg510化合物的晶型及其制备方法和用途
US12030883B2 (en) 2021-09-21 2024-07-09 Incyte Corporation Hetero-tricyclic compounds as inhibitors of KRAS
US12030884B2 (en) 2021-10-01 2024-07-09 Incyte Corporation Pyrazoloquinoline KRAS inhibitors
AU2022356286B2 (en) 2021-10-01 2024-10-10 Xinthera, Inc. Azetidine and pyrrolidine parp1 inhibitors and uses thereof
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
KR20240101561A (ko) 2021-10-14 2024-07-02 인사이트 코포레이션 Kras의 저해제로서의 퀴놀린 화합물
EP4421076A1 (en) 2021-10-22 2024-08-28 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Nitrogen-containing tetracyclic compound, preparation method therefor, and medical use thereof
CA3237199A1 (en) 2021-11-02 2023-05-11 Flare Therapeutics Inc. Pparg inverse agonists and uses thereof
CN118139861A (zh) * 2021-11-05 2024-06-04 苏州信诺维医药科技股份有限公司 Kras突变体抑制剂的晶型、其制备方法及其应用
US12110276B2 (en) 2021-11-24 2024-10-08 Genentech, Inc. Pyrazolo compounds and methods of use thereof
US20230203062A1 (en) 2021-11-24 2023-06-29 Genentech, Inc. Therapeutic compounds and methods of use
CA3240980A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023122662A1 (en) 2021-12-22 2023-06-29 The Regents Of The University Of California Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase
EP4452964A1 (en) 2021-12-22 2024-10-30 Boehringer Ingelheim International GmbH Heteroaromatic compounds for the treatment of cancer
AU2023209820B2 (en) 2022-01-21 2024-10-10 Xinthera, Inc. Parp1 inhibitors and uses thereof
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
MX2024010045A (es) 2022-02-16 2024-08-26 Amgen Inc Compuestos de quinazolina y uso de los mismos como inhibidores de proteinas mutantes kras.
WO2023159087A1 (en) 2022-02-16 2023-08-24 Amgen Inc. Quinazoline compounds and use thereof as inhibtors of mutant kras proteins
WO2023172858A1 (en) 2022-03-07 2023-09-14 Amgen Inc. A process for preparing 4-methyl-2-propan-2-yl-pyridine-3-carbonitrile
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023190748A1 (ja) 2022-03-31 2023-10-05 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療用医薬組成物
WO2023194310A1 (en) 2022-04-04 2023-10-12 Sanofi Therapeutic combination of kras g12c inhibitor and tead inhibitor
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
AU2023259236A1 (en) 2022-04-28 2024-10-24 Xinthera, Inc. Tricyclic parp1 inhibitors and uses thereof
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024031088A1 (en) 2022-08-05 2024-02-08 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2024040131A1 (en) 2022-08-17 2024-02-22 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
GB202212641D0 (en) 2022-08-31 2022-10-12 Jazz Pharmaceuticals Ireland Ltd Novel compounds
CN115368358A (zh) * 2022-09-01 2022-11-22 浙江九洲药业股份有限公司 一种Sotorasib新晶型及其制备方法与应用
WO2024081674A1 (en) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Combination therapies for the treatment of cancer
WO2024102421A2 (en) 2022-11-09 2024-05-16 Revolution Medicines, Inc. Compounds, complexes, and methods for their preparation and of their use
WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024216048A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024216016A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor

Family Cites Families (235)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4232027A (en) 1979-01-29 1980-11-04 E. R. Squibb & Sons, Inc. 1,2-Dihydro-2-oxo-4-phenyl-3-quinolinecarbonitrile derivatives
EP0090505B1 (en) 1982-03-03 1990-08-08 Genentech, Inc. Human antithrombin iii, dna sequences therefor, expression vehicles and cloning vectors containing such sequences and cell cultures transformed thereby, a process for expressing human antithrombin iii, and pharmaceutical compositions comprising it
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
JP2762522B2 (ja) 1989-03-06 1998-06-04 藤沢薬品工業株式会社 血管新生阻害剤
GB8912336D0 (en) 1989-05-30 1989-07-12 Smithkline Beckman Intercredit Compounds
US5112946A (en) 1989-07-06 1992-05-12 Repligen Corporation Modified pf4 compositions and methods of use
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5892112A (en) 1990-11-21 1999-04-06 Glycomed Incorporated Process for preparing synthetic matrix metalloprotease inhibitors
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
CA2066898A1 (en) 1991-04-29 1992-10-30 Chuan Shih Pharmaceutical compounds
CA2102780C (en) 1991-05-10 2007-01-09 Alfred P. Spada Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
ES2279508T3 (es) 1992-11-13 2007-08-16 Immunex Corporation Ligando elk, una citoquina.
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
EP0672035A1 (en) 1993-10-01 1995-09-20 Novartis AG Pyrimidineamine derivatives and processes for the preparation thereof
US5656643A (en) 1993-11-08 1997-08-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
WO1995014023A1 (en) 1993-11-19 1995-05-26 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
JP3745772B2 (ja) 1993-12-17 2006-02-15 ノバルティス アクチエンゲゼルシャフト 免疫抑制剤として有用なラパマイシン誘導体
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
AU2096895A (en) 1994-03-07 1995-09-25 Sugen, Incorporated Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
AU702522B2 (en) 1994-04-15 1999-02-25 Amgen, Inc. HEK5, HEK7, HEK8, HEK11, new EPH-like receptor protein tyrosine kinases
EP0682027B1 (de) 1994-05-03 1997-10-15 Novartis AG Pyrrolopyrimidinderivate mit antiproliferativer Wirkung
US6303769B1 (en) 1994-07-08 2001-10-16 Immunex Corporation Lerk-5 dna
US5919905A (en) 1994-10-05 1999-07-06 Immunex Corporation Cytokine designated LERK-6
US6057124A (en) 1995-01-27 2000-05-02 Amgen Inc. Nucleic acids encoding ligands for HEK4 receptors
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
EP3103799B1 (en) 1995-03-30 2018-06-06 OSI Pharmaceuticals, LLC Quinazoline derivatives
NZ304859A (en) 1995-04-03 2000-01-28 Novartis Ag 4-amino-1H-pyrazolo[3,4-d]pyrimidine derivatives, medicaments and processes for the preparation thereof
ATE198326T1 (de) 1995-04-20 2001-01-15 Pfizer Arylsulfonamido-substituierte hydroxamsäure derivate als inhibitoren von mmp und tnf
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
DK0833828T3 (da) 1995-06-09 2003-03-17 Novartis Ag Rapamycinderivater
NZ312665A (en) 1995-07-06 1999-08-30 Novartis Ag Rrolopyrimidines(7h-pyrrolo[2,3-d]pyrimidine and preparation of these
DE19534177A1 (de) 1995-09-15 1997-03-20 Merck Patent Gmbh Cyclische Adhäsionsinhibitoren
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
PT780386E (pt) 1995-12-20 2003-02-28 Hoffmann La Roche Inibidores de metaloprotease de matriz
WO1997027199A1 (en) 1996-01-23 1997-07-31 Novartis Ag Pyrrolopyrimidines and processes for their preparation
JP3406763B2 (ja) 1996-01-30 2003-05-12 東レ・ダウコーニング・シリコーン株式会社 シリコーンゴム組成物
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
DE19608588A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19629652A1 (de) 1996-03-06 1998-01-29 Thomae Gmbh Dr K 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
BR9709443B1 (pt) 1996-03-15 2009-05-05 n-7-heterociclil-pirrol[2,3-d]pirimidinas, bem como composições farmacêuticas compreendendo as mesmas.
CN100503580C (zh) 1996-04-12 2009-06-24 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
CA2258548C (en) 1996-06-24 2005-07-26 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
AU735648B2 (en) 1996-07-12 2001-07-12 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
CZ8799A3 (cs) 1996-07-13 1999-06-16 Glaxo Group Limited Bicyklické heteroaromatické sloučeniny, způsob jejich výroby a farmaceutický prostředek
PT912559E (pt) 1996-07-13 2003-03-31 Glaxo Group Ltd Compostos heterociclicos fundidos como inibidores de proteina tirosina quinase
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
EP0923585B1 (en) 1996-07-18 2002-05-08 Pfizer Inc. Phosphinate based inhibitors of matrix metalloproteases
JP4440344B2 (ja) 1996-08-16 2010-03-24 シェーリング コーポレイション 哺乳動物細胞表面抗原；関連試薬
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
PL331895A1 (en) 1996-08-23 1999-08-16 Pfizer Arylosulphonylamino derivatives of hydroxamic acid
AU720429B2 (en) 1996-08-23 2000-06-01 Novartis Ag Substituted pyrrolopyrimidines and processes for their preparation
WO1998014449A1 (en) 1996-10-02 1998-04-09 Novartis Ag Fused pyrazole derivatives and processes for their preparation
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
DE69732780T2 (de) 1996-10-02 2006-04-06 Novartis Ag Pyrimiderivate und verfahren zu ihrer herstellung
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
ATE272640T1 (de) 1997-01-06 2004-08-15 Pfizer Cyclische sulfonderivate
SK283963B6 (sk) 1997-02-03 2004-06-08 Pfizer Products Inc. Deriváty arylsulfonylaminohydroxamovej kyseliny, farmaceutický prostriedok, spôsob inhibície matričných metaloproteináz alebo produkcie faktora nekrózy nádorov
DE69839338T2 (de) 1997-02-05 2008-07-10 Warner-Lambert Company Llc Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation
AU5493598A (en) 1997-02-07 1998-08-26 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
ID22809A (id) 1997-02-11 1999-12-09 Pfizer Turunan-turunan asam arilsulfonil hidroksamat
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
US6329375B1 (en) 1997-08-05 2001-12-11 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
EA002490B1 (ru) 1997-08-08 2002-06-27 Пфайзер Продактс Инк. Производные арилоксиарилсульфониламиногидроксамовой кислоты
AU1102399A (en) 1997-10-21 1999-05-10 Human Genome Sciences, Inc. Human tumor necrosis factor receptor-like proteins tr11, tr11sv1, and tr11sv2
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
CA2319236A1 (en) 1998-02-09 1999-08-12 Genentech, Inc. Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same
EP1066286B1 (en) 1998-03-04 2009-04-29 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
US6395734B1 (en) 1998-05-29 2002-05-28 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
CA2336848A1 (en) 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
CA2341409A1 (en) 1998-08-31 2000-03-09 Merck And Co., Inc. Novel angiogenesis inhibitors
PT1004578E (pt) 1998-11-05 2004-06-30 Pfizer Prod Inc Derivados hidroxamida do acido 5-oxo-pirrolidino-2-carboxilico
ES2377847T3 (es) 1999-01-13 2012-04-02 Bayer Healthcare Llc Difenil ureas sustituidas con omega-carboxi arilo como agentes inhibidores de la cinasa p38
ATE329596T1 (de) 1999-03-30 2006-07-15 Novartis Pharma Gmbh Phthalazinderivate zur behandlung von entzündlicher erkrankungen
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
PT1187918E (pt) 1999-06-07 2006-08-31 Immunex Corp Antagonistas de tek
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
JP2003504343A (ja) 1999-07-12 2003-02-04 ジェネンテック・インコーポレーテッド 腫瘍壊死因子リガンド／レセプター相同体による血管形成及び心血管形成の促進と抑制
ES2219388T3 (es) 1999-08-24 2004-12-01 Ariad Gene Therapeutics, Inc. 28-epi-rapalogos.
EP1244647B1 (en) 1999-11-05 2006-06-21 AstraZeneca AB Quinazoline derivatives as vegf inhibitors
DK1233943T3 (da) 1999-11-24 2011-08-15 Sugen Inc Ioniserbare indolinon derivater og anvendelse deraf som PTK ligander
US6515004B1 (en) 1999-12-15 2003-02-04 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
AU2001247219B2 (en) 2000-02-25 2007-01-04 Immunex Corporation Integrin antagonists
KR100773621B1 (ko) 2000-07-19 2007-11-05 워너-램버트 캄파니 엘엘씨 4-요오도 페닐아미노 벤즈히드록삼산의 산소화 에스테르
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
PT1343782E (pt) 2000-12-21 2009-06-29 Smithkline Beecham Corp Pirimidinoaminas como moduladores de angiogénese
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
JP2002233610A (ja) 2002-02-18 2002-08-20 Olympia:Kk スロットマシン
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
US20050009849A1 (en) 2003-01-03 2005-01-13 Veach Darren R. Pyridopyrimidine kinase inhibitors
JP4638876B2 (ja) 2003-05-23 2011-02-23 ワイス Ｇｉｔｒリガンド及びｇｉｔｒリガンド関連分子及び抗体及びその使用
DE602004017736D1 (de) 2003-07-08 2008-12-24 Novartis Ag Verwendung von rapamycin und dessen derivaten zur behandlung von knochenverlust
WO2005016252A2 (en) 2003-07-11 2005-02-24 Ariad Gene Therapeutics, Inc. Phosphorus-containing macrocycles
WO2005007190A1 (en) 2003-07-11 2005-01-27 Schering Corporation Agonists or antagonists of the clucocorticoid-induced tumour necrosis factor receptor (gitr) or its ligand for the treatment of immune disorders, infections and cancer
TW200523262A (en) 2003-07-29 2005-07-16 Smithkline Beecham Corp Inhibitors of AKT activity
EP1656376A1 (en) 2003-08-22 2006-05-17 Avanir Pharmaceuticals Substituted naphthyridine derivatives as inhibitors of macrophage migration inhibitory factor and their use in the treatment of human diseases
EP1692318A4 (en) 2003-12-02 2008-04-02 Genzyme Corp COMPOSITIONS AND METHODS FOR DIAGNOSIS AND TREATMENT OF LUNG CANCER
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
EP1765402A2 (en) 2004-06-04 2007-03-28 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
EP1786785B9 (en) 2004-08-26 2013-05-22 Pfizer Inc. Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
MX2007004489A (es) 2004-10-13 2007-09-21 Wyeth Corp Analogos de 17-hidroxiwortamina como inhibidores pi3k.
WO2006044860A2 (en) 2004-10-18 2006-04-27 Amgen, Inc. Thiadiazole compounds and methods of use
EP2343320B1 (en) 2005-03-25 2017-10-25 GITR, Inc. Anti-gitr antibodies and uses thereof
EP2439272A3 (en) 2005-05-09 2013-07-31 Ono Pharmaceutical Co., Ltd. Human monoclonal antibodies to programmed death 1(PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapeutics
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
WO2007034327A1 (en) 2005-09-20 2007-03-29 Pfizer Products Inc. Dosage forms and methods of treatment using a tyrosine kinase inhibitor
EP1981884B1 (en) 2006-01-18 2012-06-13 Amgen, Inc Thiazole compounds as protein kinase b (pkb) inhibitors
WO2007133822A1 (en) 2006-01-19 2007-11-22 Genzyme Corporation Gitr antibodies for the treatment of cancer
WO2008070740A1 (en) 2006-12-07 2008-06-12 F.Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use
WO2008118454A2 (en) 2007-03-23 2008-10-02 Amgen Inc. Derivatives of quinoline or benzopyrazine and their uses for the treatment of (inter alia) inflammatory diseases, autoimmune diseases or various kinds of cancer
DK2137186T3 (en) 2007-03-23 2016-04-18 Amgen Inc Heterocyclic compounds and their uses
ES2446417T3 (es) 2007-03-23 2014-03-07 Amgen Inc. Derivados de quinolina o quinoxalina sustituidos en 3 y su uso como inhibidores de fosfatidilinositol 3-cinasa (PI3K)
WO2008153947A2 (en) 2007-06-07 2008-12-18 Amgen Inc. Heterocyclic compounds as raf kinase modulators
US8591886B2 (en) 2007-07-12 2013-11-26 Gitr, Inc. Combination therapies employing GITR binding molecules
WO2009011871A2 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
WO2009011880A2 (en) 2007-07-17 2009-01-22 Amgen Inc. Heterocyclic modulators of pkb
ES2401557T3 (es) 2007-08-02 2013-04-22 Amgen, Inc Moduladores de Pl3 cinasas y métodos de uso
BRPI0816769A2 (pt) 2007-09-12 2016-11-29 Hoffmann La Roche combinações de compostos inibidores de fosfoinositida 3-cinase e agentes quimioterapêuticos, e métodos de uso
ES2439705T3 (es) 2007-10-25 2014-01-24 Genentech, Inc. Proceso para la preparación de compuestos de tienopirimidina
JP5520831B2 (ja) 2007-12-19 2014-06-11 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
CN101945867A (zh) 2007-12-19 2011-01-12 安姆根有限公司 作为细胞周期抑制剂的稠合吡啶、嘧啶和三嗪化合物
WO2009126584A1 (en) 2008-04-07 2009-10-15 Amgen Inc. Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors
AU2009260447B2 (en) 2008-05-30 2012-03-29 Amgen Inc. Inhibitors of PI3 kinase
JP2011526794A (ja) 2008-07-02 2011-10-20 エマージェント プロダクト デベロップメント シアトル， エルエルシー ＴＧＦ−βアンタゴニスト多重標的結合性分子
JPWO2010030002A1 (ja) 2008-09-12 2012-02-02 国立大学法人三重大学 外来性ｇｉｔｒリガンド発現細胞
WO2010083246A1 (en) 2009-01-15 2010-07-22 Amgen Inc. Fluoroisoquinoline substituted thiazole compounds and methods of use
MX2011008674A (es) 2009-02-18 2011-11-04 Amgen Inc Compuestos de indol/bencimidazol como inhibidores de quinasa mtor.
WO2010108074A2 (en) 2009-03-20 2010-09-23 Amgen Inc. Inhibitors of pi3 kinase
UY32582A (es) 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
US20120190666A1 (en) 2009-05-13 2012-07-26 Amgen Inc. Heteroaryl Compounds as PIKK Inhibitors
MX2011013901A (es) 2009-06-25 2012-05-08 Amgen Inc Derivados de 4h-pirido [1,2-a] pirimidin-4-ona como inhibidores de pi3k.
KR20140015121A (ko) 2009-06-25 2014-02-06 암젠 인크 헤테로사이클릭 화합물 및 이의 용도
US8765940B2 (en) 2009-06-25 2014-07-01 Amgen Inc. Heterocyclic compounds and their uses
US20100331306A1 (en) 2009-06-25 2010-12-30 Amgen Inc. Heterocyclic compounds and their uses
EP2266984A1 (en) * 2009-06-26 2010-12-29 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Pyrido[2,3-d]pyrimidines as Wnt antagonists for treatment of cancer and arthritis
EP2473531A4 (en) 2009-09-03 2013-05-01 Merck Sharp & Dohme ANTI-GITRANT ANTIBODIES
SG179102A1 (en) 2009-09-11 2012-04-27 Amgen Inc N-4 ( - ( ( 3- ( 2 -amino-4 pyrimidinyl) -2 -pyridinyl) oxy) phenyl) -4- (4-methyl-2-thienyl) -1-phthalazinamine for use in the treatment of antimitotic agent resistant cancer
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
WO2011075747A1 (en) * 2009-12-18 2011-06-23 Glaxosmithkline Llc Therapeutic compounds
KR20120125611A (ko) 2009-12-29 2012-11-16 이머전트 프로덕트 디벨롭먼트 시애틀, 엘엘씨 이종이량체 결합 단백질 및 이의 용도
WO2012142498A2 (en) 2011-04-13 2012-10-18 Innovimmune Biotherapeutics, Inc. Mif inhibitors and their uses
US20130108641A1 (en) 2011-09-14 2013-05-02 Sanofi Anti-gitr antibodies
US20150087628A1 (en) 2012-04-10 2015-03-26 The Regents Of The University Of California Compositions and methods for treating cancer
ES2618004T3 (es) 2012-08-07 2017-06-20 Merck Patent Gmbh Derivados de piridopirimidina como inhibidores de proteínas quinasas
WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
JP6473133B2 (ja) 2013-03-15 2019-02-20 アラクセス ファーマ エルエルシー Ｋｒａｓｇ１２ｃの共有結合性阻害剤
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
GB201312059D0 (en) 2013-07-05 2013-08-21 Univ Leuven Kath Novel GAK modulators
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
EP3636639A1 (en) * 2013-10-10 2020-04-15 Araxes Pharma LLC Inhibitors of kras g12c
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
WO2015109285A1 (en) 2014-01-20 2015-07-23 Cleave Biosciences, Inc. FUSED PYRIMIDINES AS INHIBITORS OF p97 COMPLEX
WO2016035008A1 (en) 2014-09-04 2016-03-10 Lupin Limited Pyridopyrimidine derivatives as mek inhibitors
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
WO2016049524A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2016161361A1 (en) 2015-04-03 2016-10-06 Nantbioscience, Inc. Compositions and methods of targeting mutant k-ras
TW201702232A (zh) 2015-04-10 2017-01-16 亞瑞克西斯製藥公司 經取代之喹唑啉化合物及其使用方法
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
WO2017015562A1 (en) 2015-07-22 2017-01-26 Araxes Pharma Llc Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
CN108779097A (zh) 2015-11-16 2018-11-09 亚瑞克西斯制药公司 包含取代的杂环基的2-取代的喹唑啉化合物及其使用方法
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
WO2017201161A1 (en) * 2016-05-18 2017-11-23 Mirati Therapeutics, Inc. Kras g12c inhibitors
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
CN110036010A (zh) 2016-09-29 2019-07-19 亚瑞克西斯制药公司 Kras g12c突变蛋白的抑制剂
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
SG10201913491PA (en) 2016-12-22 2020-03-30 Amgen Inc Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer
US20200385364A1 (en) 2017-01-26 2020-12-10 Araxes Pharma Llc Fused n-heterocyclic compounds and methods of use thereof
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
EP3679040B1 (en) 2017-09-08 2022-08-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
AU2019262599B2 (en) 2018-05-04 2023-10-12 Amgen Inc. KRAS G12C inhibitors and methods of using the same
CA3098574A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
CA3099045A1 (en) 2018-05-10 2019-11-14 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
MX2020012731A (es) 2018-06-01 2021-02-22 Amgen Inc Inhibidores de kras g12c y metodos para su uso.
WO2019241157A1 (en) 2018-06-11 2019-12-19 Amgen Inc. Kras g12c inhibitors for treating cancer
JP7369719B2 (ja) 2018-06-12 2023-10-26 アムジエン・インコーポレーテツド ＫＲａｓ Ｇ１２Ｃ阻害剤及びそれを使用する方法
MA52942A (fr) 2018-06-21 2021-04-28 Janssen Pharmaceutica Nv Composés inhibiteurs d'oga
AU2019291099A1 (en) 2018-06-21 2021-01-07 Janssen Pharmaceutica Nv Oga inhibitor compounds
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
MA55136A (fr) 2018-11-19 2022-02-23 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
PE20220504A1 (es) 2019-05-21 2022-04-07 Amgen Inc Formas en estado solido
EP3972972A1 (en) 2019-05-21 2022-03-30 Amgen Inc. Solid state forms
US20240190862A1 (en) 2019-10-24 2024-06-13 Amgen Inc. Epoxyamides as kras g12c and kras g12d inhibitors and methods of using the same
EP4058453A1 (en) 2019-11-14 2022-09-21 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
AR120456A1 (es) 2019-11-14 2022-02-16 Amgen Inc Síntesis mejorada del compuesto inhibidor de g12c de kras
WO2021126816A1 (en) 2019-12-16 2021-06-24 Amgen Inc. Dosing regimen of a kras g12c inhibitor

Also Published As

Publication number Publication date
ZA201907651B (en) 2024-01-31
KR102690360B1 (ko) 2024-08-05
SA522432081B1 (ar) 2023-02-19
AU2018273356A1 (en) 2019-11-21
CL2020002405A1 (es) 2020-12-28
KR20240119348A (ko) 2024-08-06
CN110997668A (zh) 2020-04-10
AR122784A2 (es) 2022-10-05
AR122786A2 (es) 2022-10-05
AR111882A1 (es) 2019-08-28
EP3974429A1 (en) 2022-03-30
AR122790A2 (es) 2022-10-05
ZA202202559B (en) 2024-02-28
AR122785A2 (es) 2022-10-05
CY1125289T1 (el) 2024-02-16
CN115626923A (zh) 2023-01-20
AU2023263502A1 (en) 2023-11-30
US20240174660A1 (en) 2024-05-30
TWI780154B (zh) 2022-10-11
SA519410622B1 (ar) 2022-07-16
US11905281B2 (en) 2024-02-20
US20200055845A1 (en) 2020-02-20
CR20240126A (es) 2024-05-07
KR102573230B1 (ko) 2023-08-31
LT3630761T (lt) 2022-01-10
AU2018273356B2 (en) 2021-09-16
KR102300499B1 (ko) 2021-09-13
IL290399B1 (en) 2023-03-01
PT3630761T (pt) 2022-02-02
US20180334454A1 (en) 2018-11-22
AR122788A2 (es) 2022-10-05
CR20190534A (es) 2020-03-20
AR122783A2 (es) 2022-10-05
UA127968C2 (uk) 2024-02-28
KR20210111900A (ko) 2021-09-13
IL290399A (en) 2022-04-01
BR112019024525A2 (pt) 2020-06-09
AR122789A2 (es) 2022-10-05
JP2024109775A (ja) 2024-08-14
US20210009577A1 (en) 2021-01-14
JP2022126763A (ja) 2022-08-30
AU2021245150A1 (en) 2021-11-04
AU2021245150B2 (en) 2023-11-23
HRP20212017T1 (hr) 2022-04-01
CN115626923B (zh) 2024-08-02
JP2019031476A (ja) 2019-02-28
UY37744A (es) 2019-01-02
CA3063469C (en) 2022-03-22
MA48772B1 (fr) 2022-02-28
AR122787A2 (es) 2022-10-05
PH12019502579A1 (en) 2020-07-13
EA201992781A1 (ru) 2020-04-01
JP6785819B2 (ja) 2020-11-18
SG10201913195RA (en) 2020-02-27
JP2021020948A (ja) 2021-02-18
TW202323252A (zh) 2023-06-16
CA3063469A1 (en) 2018-11-29
HUE057632T2 (hu) 2022-05-28
ES2905676T3 (es) 2022-04-11
WO2018217651A1 (en) 2018-11-29
MX2019013858A (es) 2020-01-20
JP7495444B2 (ja) 2024-06-04
PE20200733A1 (es) 2020-07-23
KR20200010384A (ko) 2020-01-30
IL270490B (en) 2022-03-01
NZ758786A (en) 2023-03-31
US10519146B2 (en) 2019-12-31
CO2019013010A2 (es) 2020-04-01
ZA202100644B (en) 2023-03-29
MX2021011115A (es) 2021-10-13
EP3630761A1 (en) 2020-04-08
JOP20190272A1 (ar) 2019-11-21
CL2019003394A1 (es) 2020-04-13
DK3630761T3 (da) 2022-02-07
EP3630761B1 (en) 2021-11-24
SI3630761T1 (sl) 2022-02-28
RS62800B1 (sr) 2022-02-28
TW201906821A (zh) 2019-02-16
MA48772A (fr) 2020-04-08
BR112019024525B1 (pt) 2021-08-10
JP7095052B2 (ja) 2022-07-04
CN110997668B (zh) 2022-11-01
TWI834294B (zh) 2024-03-01
IL290399B2 (en) 2023-07-01
KR20230128589A (ko) 2023-09-05

Similar Documents

Publication Publication Date Title
IL290399A (en) kras g12c inhibitors and methods of using them
IL287223A (en) kras g12c inhibitors and methods of using them
IL272512A (en) KRAS G12C inhibitors and methods of using them
HUS2400019I1 (hu) KRas G12C inhibotorok
IL288200A (en) kras g12c inhibitors and their use
HK1249513A1 (zh) Kras的稠合三環抑制劑及其使用方法
IL262867B (en) kras g12c inhibitors
HK1259232A1 (zh) Menin-mll的取代抑制劑及其使用方法
IL271025A (en) Multibiotic substances and methods of using them
EP3700527A4 (en) PAPD5 INHIBITORS AND THEIR METHODS OF USE
EP3684361A4 (en) MENINE-MLL SUBSTITUTE INHIBITORS AND METHODS OF USE
IL276095A (en) gcn2 inhibitors and their uses
EP3368538A4 (en) WEE-1 KINASE INHIBITORS AND METHOD FOR THE PRODUCTION AND USE THEREOF
IL267291A (en) Actonucleotidase inhibitors and methods of using them
IL279475A (en) Actonucleotidase inhibitors and methods of using them
IL274504A (en) 2ACSS inhibitors and methods of their use
IL268619B (en) Piperidine-converted mnk inhibitors and related methods
IL286485A (en) pi4-kinase inhibitors and methods of using them
EP3793552C0 (en) ABHD12 INHIBITORS AND METHODS OF MANUFACTURE AND USE THEREOF