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

AR086008A1 - Compuestos de benceno sustituidos con arilo o heteroarilo - Google Patents

Compuestos de benceno sustituidos con arilo o heteroarilo

Info

Publication number
AR086008A1
AR086008A1 ARP120101288A ARP120101288A AR086008A1 AR 086008 A1 AR086008 A1 AR 086008A1 AR P120101288 A ARP120101288 A AR P120101288A AR P120101288 A ARP120101288 A AR P120101288A AR 086008 A1 AR086008 A1 AR 086008A1
Authority
AR
Argentina
Prior art keywords
alkyl
halo
cyano
amino
cycloalkyl
Prior art date
Application number
ARP120101288A
Other languages
English (en)
Inventor
Natalie Warholic
Kenneth W Duncan
Kevin W Kuntz
Richard Chesworth
Heike-Klaus C Keilhack
Original Assignee
Epizyme 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46045109&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR086008(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Epizyme Inc filed Critical Epizyme Inc
Publication of AR086008A1 publication Critical patent/AR086008A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • 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
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

La presente se refiere a compuestos de benceno sustituidos con arilo o heteroarilo. La presente también se refiere a composiciones farmacéuticas que contienen estos compuestos y métodos de tratamiento de cáncer por administración de estos compuestos y composiciones farmacéuticas a sujetos que lo necesitan. La presente también se refiere al uso de tales compuestos para investigación u otros fines no terapéuticos.Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales farmacéuticamente aceptables, en donde: X1 es N o CR11; X2 es N o CR13; Z es NR7R8, OR7, S(O)nR7 o CR7R8R14, en donde n es 0, 1 ó 2; cada uno de R1, R5, R9 y R10, de modo independiente, es H o alquilo C1-6 opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, hidroxilo, COOH, C(O)O-alquilo C1-6, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros; cada uno de R2, R3 y R4, de modo independiente, es -Q1-T1, en donde Q1 es un enlace o ligador de alquilo C1-3 opcionalmente sustituido con halo, ciano, hidroxilo o alcoxi C1-6 y T1 es H, halo, hidroxilo, COOH, ciano o RS1, en donde RS1 es alquilo C1-3, alquenilo C2-6, alquinilo C2-6, alcoxilo C1-6, C(O)O-alquilo C1-6, cicloalquilo C3-8, arilo C6-10, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, heterocicloalquilo de 4 a 12 miembros o heteroarilo de 5 ó 6 miembros y RS1 está opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, hidroxilo, oxo, COOH, C(O)O-alquilo C1-6, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros; R6 es arilo C6-10 o heteroarilo de 5 ó 6 miembros, cada uno de los cuales está opcionalmente sustituido con uno o varios -Q2-T2, en donde Q2 es un enlace o ligador de alquilo C1-3 opcionalmente sustituido con halo, ciano, hidroxilo o alcoxi C1-6 y T2 es H, halo, ciano, -ORa, -NRaRb, -(NRaRbRc)+A-, -C(O)Ra, -C(O)ORa, -C(O)NRaRb, -NRbC(O)Ra, -NRbC(O)ORa, -S(O)2Ra, -S(O)2NRaRb o RS2, en donde cada uno de Ra, Rb y Rc, de modo independiente es H o RS3, A- es un anión farmacéuticamente aceptable, cada uno de RS2 y RS3, de modo independiente, es alquilo C1-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros o heteroarilo de 5 ó 6 miembros o Ra y Rb, junto con el átomo de N al que están unidos, forman un anillo heterocicloalquilo de 4 a 12 miembros con 0 ó 1 heteroátomos adicionales y cada uno de RS2, RS3 y el anillo heterocicloalquilo de 4 a 12 miembros formado por Ra y Rb, está opcionalmente sustituido con uno o varios -Q3-T3, en donde Q3 es un enlace o ligador de alquilo C1-3 cada uno opcionalmente sustituido con halo, ciano, hidroxilo o alcoxi C1-6 y T3 está seleccionado del grupo que consiste en halo, ciano, alquilo C1-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros, heteroarilo de 5 ó 6 miembros, ORd, COORd, -S(O)2Rd, -NRdRe y -C(O)NRdRe, siendo cada uno de Rd y Re de modo independiente H o alquilo C1-6 o -Q3-T3 es oxo; o dos -Q2-T2 vecinos, junto con los átomos a los que están unidos, forman un anillo de 5 ó 6 miembros que opcionalmente contiene 1 - 4 heteroátomos seleccionados de N, O y S y opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, hidroxilo, COOH, C(O)O-alquilo C1-6, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros; R7 es -Q4-T4, en donde Q4 es un enlace, ligador de alquilo C1-4 o ligador de alquenilo C2-4, cada ligador opcionalmente sustituido con halo, ciano, hidroxilo o alcoxi C1-4 y T4 es H, halo, ciano, NRfRg, -ORf, -C(O)Rf, -C(O)ORf, -C(O)NRfRg, -C(O)NRfORg, -NRfC(O)Rg, -S(O)2Rf o RS4, en donde cada uno de Rf y Rg, de modo independiente es H o RS5, cada uno de RS4 y RS5, de modo independiente, es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros o heteroarilo de 5 ó 6 miembros y cada uno de RS4 y RS5 está opcionalmente sustituido con uno o varios -Q5-T5, en donde Q5 es un enlace, C(O), C(O)NRk, NRkC(O), S(O)2 o ligador de alquilo C1-3, siendo Rk H o alquilo C1-6 y T5 es H, halo, alquilo C1-6, hidroxilo, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros, heteroarilo de 5 ó 6 miembros o S(O)qRq, en donde q es 0, 1 ó 2 y Rq es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros o heteroarilo de 5 ó 6 miembros y T5 está opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, alquilo C1-6, hidroxilo, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros excepto cuando T5 es H, halo, hidroxilo o ciano; o -Q5-T5 es oxo; cada uno de R8, R11, R12 y R13, de modo independiente, es H, halo, hidroxilo, COOH, ciano, RS6, ORS6 o COORS6, en donde RS6 es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, heterocicloalquilo de 4 a 12 miembros, amino, mono-alquil C1-6-amino o di-alquil C1-6-amino y RS6 está opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, hidroxilo, COOH, C(O)O-alquilo C1-6, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino y di-alquil C1-6-amino; o R7 y R8, junto con el átomo de N al que están unidos, forman un anillo heterocicloalquilo de 4 a 11 miembros que tiene 0 a 2 heteroátomos adicionales o R7 y R8, junto con el átomo de C al que están unidos, forman cicloalquilo C3-8 o un anillo heterocicloalquilo de 4 a 11 miembros que tiene 1 a 3 heteroátomos y cada uno de los anillos heterocicloalquilo de 4 a 11 miembros o cicloalquilo C3-8 formado por R7 y R8 está opcionalmente sustituido con uno o varios -Q6-T6, en donde Q6 es un enlace, C(O), C(O)NRm, NRmC(O), S(O)2 o ligador de alquilo C1-3, siendo Rm H o alquilo C1-6 y T6 es H, halo, alquilo C1-6, hidroxilo, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros, heteroarilo de 5 ó 6 miembros o S(O)pRp en donde p es 0, 1 ó 2 y Rp es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros o heteroarilo de 5 ó 6 miembros y T6 está opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, alquilo C1-6, hidroxilo, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros excepto cuando T6 es H, halo, hidroxilo o ciano; o -Q6-T6 es oxo; y R14 está ausente, H o alquilo C1-6 opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo que consiste en halo, hidroxilo, COOH, C(O)O-alquilo C1-6, ciano, alcoxilo C1-6, amino, mono-alquil C1-6-amino, di-alquil C1-6-amino, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo de 4 a 12 miembros y heteroarilo de 5 ó 6 miembros.
ARP120101288A 2011-04-13 2012-04-13 Compuestos de benceno sustituidos con arilo o heteroarilo AR086008A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161474821P 2011-04-13 2011-04-13
US201161499595P 2011-06-21 2011-06-21

Publications (1)

Publication Number Publication Date
AR086008A1 true AR086008A1 (es) 2013-11-13

Family

ID=46045109

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120101288A AR086008A1 (es) 2011-04-13 2012-04-13 Compuestos de benceno sustituidos con arilo o heteroarilo

Country Status (36)

Country Link
US (14) US8410088B2 (es)
EP (5) EP3486234B1 (es)
JP (6) JP5933686B2 (es)
KR (7) KR102154946B1 (es)
CN (2) CN107311921B (es)
AR (1) AR086008A1 (es)
AU (1) AU2012242595B2 (es)
BR (2) BR112013026324B1 (es)
CA (2) CA3086473A1 (es)
CL (1) CL2013002898A1 (es)
CY (3) CY1117986T1 (es)
DK (4) DK2697199T3 (es)
ES (4) ES2973868T3 (es)
FI (1) FI3943485T3 (es)
HK (1) HK1193804A1 (es)
HR (3) HRP20211297T8 (es)
HU (4) HUE056552T2 (es)
IL (3) IL228745A (es)
JO (2) JO3438B1 (es)
LT (4) LT3943485T (es)
ME (1) ME02500B (es)
MX (2) MX343685B (es)
MY (1) MY166171A (es)
NZ (3) NZ717119A (es)
PE (1) PE20140863A1 (es)
PH (1) PH12016502132A1 (es)
PL (4) PL3943485T3 (es)
PT (4) PT3943485T (es)
RS (3) RS62279B1 (es)
RU (1) RU2632193C2 (es)
SG (1) SG194447A1 (es)
SI (4) SI3486234T1 (es)
SM (1) SMT201600308B (es)
TW (1) TWI529162B (es)
WO (1) WO2012142504A1 (es)
ZA (1) ZA201307539B (es)

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011160206A1 (en) 2010-06-23 2011-12-29 Morin Ryan D Biomarkers for non-hodgkin lymphomas and uses thereof
AU2011298987B2 (en) 2010-09-10 2017-09-28 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
JO3438B1 (ar) * 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TWI598336B (zh) 2011-04-13 2017-09-11 雅酶股份有限公司 經取代之苯化合物
CA2850570A1 (en) * 2011-09-30 2013-04-04 Glaxosmithkline Llc Methods of treating cancer
EP2780013A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
CA2862289C (en) 2012-02-10 2019-11-26 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
RU2704445C2 (ru) * 2012-03-12 2019-10-28 Эпизайм, Инк. Ингибиторы ezh2 человека и способы их применения
RU2699546C2 (ru) * 2012-04-13 2019-09-06 Эпизайм, Инк. Комбинированная терапия для лечения рака
DK2836491T3 (en) 2012-04-13 2017-03-06 Epizyme Inc SALT FORM OF A HUMAN HISTONMETHYL TRANSFERASE EZH2 INHIBITOR
US9562041B2 (en) 2012-05-16 2017-02-07 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
WO2014049488A1 (en) * 2012-09-28 2014-04-03 Pfizer Inc. Benzamide and heterobenzamide compounds
CN110898067A (zh) * 2012-10-15 2020-03-24 Epizyme股份有限公司 癌症治疗方法
UA115074C2 (uk) * 2012-10-15 2017-09-11 Епізайм, Інк. Бензольні сполуки, що містять замісники
CN104968646B (zh) 2012-12-13 2017-09-05 葛兰素史密斯克莱有限责任公司 Zeste同源物增强子2的抑制剂
WO2014100080A1 (en) * 2012-12-19 2014-06-26 Glaxosmithkline Llc Combination
AU2013361060B2 (en) * 2012-12-21 2018-04-19 Epizyme, Inc. 1,4-pyridone compounds
US9701666B2 (en) 2012-12-21 2017-07-11 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
SI2953941T1 (sl) * 2013-02-11 2017-08-31 Constellation Pharmaceuticals, Inc. Modulatorji metil-modificirajočih encimov, sestavki in uporabe le-teh
US9394258B2 (en) 2013-03-14 2016-07-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9045455B2 (en) 2013-03-14 2015-06-02 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
KR102158756B1 (ko) 2013-03-14 2020-09-23 에피자임, 인코포레이티드 아르기닌 메틸기 전이효소 억제제 및 이의 용도
US9023883B2 (en) 2013-03-14 2015-05-05 Epizyme, Inc. PRMT1 inhibitors and uses thereof
EP3363434A1 (en) 2013-03-14 2018-08-22 Epizyme Inc Arginine methyltransferase inhibitors and uses thereof
US9776972B2 (en) 2013-03-14 2017-10-03 Epizyme Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US20160039767A1 (en) 2013-03-14 2016-02-11 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
WO2014153172A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
WO2014153214A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyl transferase inhibtors and uses thereof
RU2015139054A (ru) 2013-03-14 2017-04-19 Дженентек, Инк. Способы лечения рака и профилактики лекарственной резистентности рака
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9243001B2 (en) 2013-03-15 2016-01-26 Epizyme, Inc. Substituted benzene compounds
WO2014151142A1 (en) 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
AU2014254392B2 (en) 2013-03-15 2018-05-24 Epizyme, Inc. Substituted benzene compounds
CN105308038B (zh) 2013-04-30 2018-05-29 葛兰素史密斯克莱知识产权（第2 号）有限公司 Zeste增强子同源物2的抑制剂
JP2016520645A (ja) * 2013-06-06 2016-07-14 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｎｏ．２ Ｌｉｍｉｔｅｄ Ｚｅｓｔｅホモログ２エンハンサー阻害剤
WO2015004618A1 (en) * 2013-07-10 2015-01-15 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
WO2015010049A1 (en) * 2013-07-19 2015-01-22 Epizyme, Inc. Substituted benzene compounds
US9624205B2 (en) 2013-07-19 2017-04-18 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2015023915A1 (en) 2013-08-15 2015-02-19 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
PT3057962T (pt) * 2013-10-16 2023-11-07 Epizyme Inc Forma de sal cloridrato para inibição de ezh2
WO2015077193A1 (en) 2013-11-19 2015-05-28 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
WO2015077194A1 (en) * 2013-11-22 2015-05-28 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
EP3888659A1 (en) 2013-12-06 2021-10-06 Epizyme Inc Combination therapy for treating cancer
CN105037360B (zh) * 2014-04-28 2016-08-17 四川大学 吡啶酮衍生物及其制备方法和用途
IL285201B2 (en) 2014-06-17 2024-05-01 Epizyme Inc EZH2 inhibitors for the treatment of lymphoma
CR20160574A (es) 2014-06-17 2017-02-23 Pfizer Compuestos de dihidroisoquinolinona sustituida
WO2015200650A1 (en) 2014-06-25 2015-12-30 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
KR102397720B1 (ko) 2014-10-16 2022-05-13 에피자임, 인코포레이티드 암을 치료하기 위한 방법
WO2016066697A1 (en) * 2014-10-28 2016-05-06 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
CA2964629A1 (en) 2014-11-06 2016-05-12 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
DK3220916T3 (da) 2014-11-17 2023-06-26 Epizyme Inc Fremgangsmåde til behandling af cancer med n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamid
AR102767A1 (es) 2014-12-05 2017-03-22 Lilly Co Eli Inhibidores de ezh2
CN108135908A (zh) * 2015-04-20 2018-06-08 Epizyme股份有限公司 用于治疗癌症的组合疗法
CN107635965A (zh) 2015-06-10 2018-01-26 Epizyme股份有限公司 用于治疗淋巴瘤的ezh2抑制剂
TW201708210A (zh) * 2015-06-30 2017-03-01 葛蘭素史克智慧財產（第二）有限公司 Ｚｅｓｔｅ同源物２增強子之抑制劑
KR20180042356A (ko) 2015-08-24 2018-04-25 에피자임, 인코포레이티드 암 치료 방법
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ｅｚｈ２抑制劑
WO2017040190A1 (en) 2015-08-28 2017-03-09 Constellation Pharmaceuticals, Inc. Crystalline forms of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide
US20190083504A1 (en) 2015-10-06 2019-03-21 Epizyme, Inc. Method of treating medulloblastoma with an ezh2 inhibitor
EP3370725A4 (en) * 2015-11-06 2019-07-03 Epizyme, Inc. PEDIATRIC DOSAGE FOR THE TREATMENT OF CANCER WITH AN EZH2 INHIBITOR
JP6828229B2 (ja) 2015-11-19 2021-02-10 ジエンス ヘンルイ メデイシンカンパニー リミテッドＪｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．，Ｌｔｄ． ベンゾフラン誘導体、その製造方法および医薬におけるその使用
CN105440023A (zh) * 2015-12-10 2016-03-30 江苏理工学院 Epz-6438的合成方法
TWI773657B (zh) 2015-12-18 2022-08-11 美商亞德利克斯公司 作爲非全身ｔｇｒ５促效劑之經取代之4-苯基吡啶化合物
US12084472B2 (en) 2015-12-18 2024-09-10 Ardelyx, Inc. Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists
JP2019503391A (ja) * 2016-01-29 2019-02-07 エピザイム，インコーポレイティド 癌を処置するための併用療法
IL261721B (en) 2016-03-15 2022-07-01 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
WO2017174023A1 (zh) * 2016-04-08 2017-10-12 南京明德新药研发股份有限公司 作为ezh2抑制剂的联苯化合物
EP3445365A4 (en) * 2016-04-22 2019-10-16 Dana-Farber Cancer Institute, Inc. EZH2 INHIBITORS AND USES THEREOF
US10987353B2 (en) 2016-05-04 2021-04-27 The Wistar Institute Of Anatomy And Biology Methods of treating cancers overexpressing CARM1 with EZH2 inhibitors and platinum-based antineoplastic drugs
BR112018072740A2 (pt) 2016-05-05 2019-02-19 Glaxosmithkline Intellectual Property (No. realçador de inibidores de homólogo 2 de zeste
JP7121660B2 (ja) 2016-06-01 2022-08-18 エピザイム，インコーポレイティド 癌を処置するためのｅｚｈ２阻害剤の使用
JP2019521988A (ja) 2016-06-17 2019-08-08 エピザイム，インコーポレイティド 癌を処置するためのｅｚｈ２阻害剤
CA3039059A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
WO2018102687A2 (en) 2016-12-02 2018-06-07 Epizyme, Inc. Combination therapy for treating cancer
US11191741B2 (en) * 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
CN108314677B (zh) * 2017-01-17 2020-06-30 安徽中科拓苒药物科学研究有限公司 一种ezh2抑制剂及其用途
CN110191722B (zh) * 2017-01-19 2022-03-01 第一三共株式会社 用于治疗htlv-1相关性脊髓病的药物组合物
US11214561B2 (en) 2017-01-25 2022-01-04 Ancureall Pharmaceutical (Shanghai) Co., Ltd. Histone methyltransferase EZH2 inhibitor, preparation method and pharmaceutical use thereof
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
US11642346B2 (en) 2017-03-31 2023-05-09 Epizyme, Inc. Combination therapy for treating cancer
CN110621316B (zh) * 2017-04-21 2024-01-26 Epizyme股份有限公司 用ehmt2抑制剂进行的组合疗法
AU2018269268B2 (en) 2017-05-18 2022-01-06 Jiangsu Hengrui Medicine Co., Ltd. Crystal of benzofuran derivative free base and preparation method
CN110944628A (zh) 2017-06-02 2020-03-31 Epizyme股份有限公司 使用ezh2抑制剂治疗癌症
US20230201212A1 (en) 2017-06-13 2023-06-29 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
CN111093660A (zh) 2017-09-05 2020-05-01 Epizyme股份有限公司 用于治疗癌症的组合疗法
KR20200088386A (ko) 2017-11-14 2020-07-22 화이자 인코포레이티드 Ezh2 억제제 병용 요법
JP7025556B2 (ja) 2018-01-31 2022-02-24 ミラティ セラピューティクス， インコーポレイテッド Ｐｒｃ２阻害剤
CN108640842B (zh) * 2018-04-04 2021-06-04 大连九信精细化工有限公司 一种2-溴-5-氟硝基苯的合成方法
BR112020024822B1 (pt) * 2018-06-07 2024-03-12 Merck Sharp & Dohme Llc Processos para a preparação de sugammadex
EP3823671B1 (en) 2018-07-09 2024-02-07 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
KR20210040077A (ko) * 2018-07-27 2021-04-12 쑤저우 시노벤트 파마슈티칼즈 씨오., 엘티디. 다치환 벤젠화합물 및 이의 제조방법
KR102689665B1 (ko) 2019-02-19 2024-07-31 한미약품 주식회사 신규한 헤테로트리시클릭 유도체 화합물 및 이의 용도
JP7395807B2 (ja) * 2019-03-25 2023-12-12 上海華匯拓医薬科技有限公司 アミド類化合物の調製方法及びその医薬分野の使用
EP4017527A1 (en) 2019-08-22 2022-06-29 Juno Therapeutics, Inc. Combination therapy of a t cell therapy and an enhancer of zeste homolog 2 (ezh2) inhibitor and related methods
WO2021249305A1 (zh) * 2020-06-08 2021-12-16 南京明德新药研发有限公司 联苯类化合物
CN116348459A (zh) * 2020-10-13 2023-06-27 苏州信诺维医药科技股份有限公司 多取代苯环化合物马来酸盐的晶型、其制备方法及其应用
CN114907299B (zh) * 2021-02-08 2024-06-25 上海医药工业研究院 他泽司他关键中间体的盐型、其制备方法及其中间体
CN114907300B (zh) * 2021-02-08 2024-05-28 上海医药工业研究院 他泽司他关键中间体的制备方法及其中间体
CN113292489B (zh) * 2021-06-16 2022-08-30 泓博智源(开原)药业有限公司 二氯代二烷基烟腈的制备方法
CN113527275A (zh) * 2021-07-20 2021-10-22 成都师范学院 一种sklb1039化合物及其制备方法和应用
CN113582863B (zh) * 2021-08-19 2023-05-26 沈阳农业大学 一种氨乙基联苯类化合物及其制备方法和用途
KR20230081459A (ko) 2021-11-30 2023-06-07 엘젠테라퓨틱스 주식회사 헤테로사이클릭이 치환된 신규한 3-페닐피리딘과 4-페닐피리딘 유도체 및 이의 용도
WO2023111810A1 (en) 2021-12-14 2023-06-22 Pfizer Inc. Combination therapies and uses for treating cancer
AU2023262308A1 (en) 2022-04-27 2024-10-03 Astrazeneca Uk Limited Combination of antibody-drug conjugate with ezh1 and/or ezh2 inhibitor
WO2023244918A1 (en) 2022-06-13 2023-12-21 Treeline Biosciences, Inc. Quinolone bcl6 bifunctional degraders
WO2023244917A1 (en) 2022-06-13 2023-12-21 Treeline Biosciences, Inc. 1,8-naphthyridin-2-one heterobifunctional bcl6 degraders
CN115197202B (zh) * 2022-07-15 2024-01-26 四川大学 一种ezh2共价抑制剂及其制备方法和应用

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
JPH0733729A (ja) 1993-07-26 1995-02-03 Kirin Brewery Co Ltd Ｎ−シアノ−ｎ′−置換−アリールカルボキシイミダミド化合物の製造法
HUT74450A (en) * 1993-12-27 1996-12-30 Eisai Co Ltd Anthranilic acid derivative and pharmaceutical compns. contg. such compds.
DE19516776A1 (de) 1995-05-10 1996-11-14 Boehringer Ingelheim Int Chromatin-Regulatorgene
US5741819A (en) 1995-06-07 1998-04-21 3-Dimensional Pharmaceuticals, Inc. Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
JP3906935B2 (ja) 1995-12-18 2007-04-18 杏林製薬株式会社 Ｎ−置換ジオキソチアゾリジルベンズアミド誘導体及びその製造法
AU6060099A (en) 1998-09-30 2000-04-17 Procter & Gamble Company, The 2-substituted ketoamides
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
BR0116539A (pt) 2000-12-28 2003-09-23 Shionogi & Co Derivados de piridona tendo uma atividade de ligação para o receptor 2 do tipo canabinóide
US20040102455A1 (en) * 2001-01-30 2004-05-27 Burns Christopher John Method of inhibiting kinases
US7700293B2 (en) 2001-08-02 2010-04-20 The Regents Of The University Of Michigan Expression profile of prostate cancer
EP1465869B1 (en) * 2001-12-21 2013-05-15 Exelixis Patent Company LLC Modulators of lxr
DE60329981D1 (de) 2002-02-19 2009-12-24 Shionogi & Co Antipruriginosa
TW200306155A (en) 2002-03-19 2003-11-16 Du Pont Benzamides and advantageous compositions thereof for use as fungicides
EP2281564A3 (en) 2002-12-27 2012-09-05 Sucampo AG Derivatives of prostaglandins for treating abdominal discomfort
MEP52808A (en) 2003-02-26 2011-05-10 Sugen Inc Aminoheteroaryl compounds as protein kinase inhibitors
US7405295B2 (en) * 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US7442685B2 (en) 2003-06-13 2008-10-28 The University Of North Carolina At Chapel Hill DOT1 histone methyltransferases as a target for identifying therapeutic agents for leukemia
EP1633740B1 (en) 2003-06-19 2011-11-09 GlaxoSmithKline LLC 5-(acylamino)indazole derivatives as kinase inhibitors
RS52625B (en) * 2003-07-23 2013-06-28 Bayer Healthcare Llc FLUORO SUBSTITUTED OMEGA-CARBOXYARYL DIPHENYL UREA FOR TREATMENT AND PREVENTION OF DISEASES AND DISEASES
AU2004266169B9 (en) 2003-08-26 2007-05-10 Merck Hdac Research, Llc Method of treating cancer with HDAC inhibitors
US20050059682A1 (en) 2003-09-12 2005-03-17 Supergen, Inc., A Delaware Corporation Compositions and methods for treatment of cancer
JP4861976B2 (ja) 2004-03-11 2012-01-25 アクテリオン ファーマシューティカルズ リミテッド インドール−１−イル酢酸誘導体
CN1286973C (zh) 2004-04-12 2006-11-29 上海第二医科大学附属瑞金医院 一种组蛋白甲基转移酶及其制备方法
JP5160885B2 (ja) 2004-06-01 2013-03-13 ザ・ユニヴァーシティ・オヴ・ノース・キャロライナ・アト・チャペル・ヒル 再構成ヒストンメチルトランスフェラーゼ複合体及びそのモジュレーターの識別方法
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
ATE494548T1 (de) 2005-06-02 2011-01-15 Univ North Carolina Reinigung, charakterisierung und wiederherstellung einer ubiquitin-e3-ligase
FR2889526B1 (fr) 2005-08-04 2012-02-17 Aventis Pharma Sa 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation
PT1940821E (pt) 2005-10-19 2013-05-29 Gruenenthal Gmbh Novos ligandos do receptor de vanilóide e seu uso para a produção de medicamentos
EP1951672B1 (en) 2005-10-21 2011-05-25 Merck Sharp & Dohme Corp. Potassium channel inhibitors
US20090203057A1 (en) 2005-10-28 2009-08-13 Yi Zhang Protein demethylases comprising a jmjc domain
CA2631236C (en) 2005-12-01 2019-10-29 Medical Prognosis Institute Methods and devices for identifying biomarkers of treatment response and use thereof to predict treatment efficacy
WO2007070818A1 (en) 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
EP2730661A1 (en) 2006-01-20 2014-05-14 The University of North Carolina at Chapel Hill Diagnostic and therapeutic targets for leukemia
CN101443007A (zh) 2006-05-15 2009-05-27 Irm责任有限公司 Terephthalamate化合物和组合物及其作为hiv整合酶抑制剂的用途
WO2007136592A2 (en) 2006-05-18 2007-11-29 Amphora Discovery Corporation 2-0x0-l,2-dihydr0quin0line derivatives, compositions, and uses thereof as antiproliferative agents
EP2086318A4 (en) 2006-10-10 2009-12-23 Burnham Inst Medical Research NEUROPROTEKTIVE COMPOSITIONS AND METHOD
AU2008219166B2 (en) 2007-02-16 2013-05-16 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors
US8338437B2 (en) 2007-02-28 2012-12-25 Methylgene Inc. Amines as small molecule inhibitors
WO2008109534A1 (en) * 2007-03-02 2008-09-12 Mdrna, Inc. Nucleic acid compounds for inhibiting ezh2 gene expression and uses thereof
WO2008113006A1 (en) 2007-03-14 2008-09-18 Xenon Pharmaceuticals Inc. Methods of using quinolinone compounds in treating sodium channel-mediated diseases or conditions
DE102007017884A1 (de) 2007-04-13 2008-10-16 Grünethal GmbH Neue Vanilloid-Rezeptor Liganden und ihre Verwendung zur Herstellung von Arzneimitteln
US20090012031A1 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan EZH2 Cancer Markers
CN101754955A (zh) 2007-07-16 2010-06-23 雅培制药有限公司 作为蛋白激酶抑制剂的吲唑、苯并异*唑和苯并异噻唑化合物
CA2703909A1 (en) * 2007-10-31 2009-05-07 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
MX2010006739A (es) 2007-12-19 2010-10-08 Cancer Rec Tech Ltd Compuestos pirido[2,3-b]pirazina-8-sustituidos y su uso.
EP2235001B1 (en) * 2008-01-23 2014-12-24 Bristol-Myers Squibb Company Process for preparing pyridinone compounds
WO2009124137A2 (en) 2008-04-01 2009-10-08 Mount Sinai School Of Medicine Of New York University Method of suppressing gene transcription through histone lysine methylation
US20100113415A1 (en) 2008-05-29 2010-05-06 Rajapakse Hemaka A Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer
UY31982A (es) * 2008-07-16 2010-02-26 Boehringer Ingelheim Int Derivados de 1,2-dihidropiridin-3-carboxamidas n-sustituidas
WO2010017355A2 (en) 2008-08-08 2010-02-11 New York Blood Center Small molecule inhibitors of retroviral assembly and maturation
FR2934995B1 (fr) 2008-08-14 2010-08-27 Sanofi Aventis Composes d'azetidines polysubstitues, leur preparation et leur application en therapeutique
SG174903A1 (en) * 2009-03-24 2011-11-28 Sanofi Sa 9h-pyrrolo[2,3-b: 5,4-c'] dipyridine azacarboline derivatives, preparation thereof, and therapeutic use thereof
EP2411007A4 (en) 2009-03-27 2012-12-05 Uab Research Foundation MODULATION OF IRES-MEDIATED TRANSLATION
WO2011011366A2 (en) 2009-07-20 2011-01-27 Constellation Pharmaceuticals Agents for stimulating activity of methyl modifying enzymes and methods of use thereof
WO2011082044A1 (en) 2009-12-30 2011-07-07 Avon Products, Inc. Topical lightening composition and uses thereof
JP5864546B2 (ja) * 2010-05-07 2016-02-17 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ インダゾール
WO2012005805A1 (en) * 2010-05-07 2012-01-12 Glaxosmithkline Llc Azaindazoles
PT2566327T (pt) * 2010-05-07 2017-05-26 Glaxosmithkline Llc Indoles
WO2011160206A1 (en) 2010-06-23 2011-12-29 Morin Ryan D Biomarkers for non-hodgkin lymphomas and uses thereof
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
AU2011298987B2 (en) 2010-09-10 2017-09-28 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
US20130310379A1 (en) 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
JP5908493B2 (ja) 2010-12-01 2016-04-26 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ インドール
CN103339139A (zh) 2010-12-03 2013-10-02 Epizyme股份有限公司 组蛋白甲基转移酶的7-氮杂嘌呤调节剂及其使用方法
EP2681216B1 (en) 2011-02-28 2017-09-27 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TWI598336B (zh) 2011-04-13 2017-09-11 雅酶股份有限公司 經取代之苯化合物
CA2850570A1 (en) 2011-09-30 2013-04-04 Glaxosmithkline Llc Methods of treating cancer
RU2704445C2 (ru) * 2012-03-12 2019-10-28 Эпизайм, Инк. Ингибиторы ezh2 человека и способы их применения
RU2699546C2 (ru) 2012-04-13 2019-09-06 Эпизайм, Инк. Комбинированная терапия для лечения рака
DK2836491T3 (en) 2012-04-13 2017-03-06 Epizyme Inc SALT FORM OF A HUMAN HISTONMETHYL TRANSFERASE EZH2 INHIBITOR
US9562041B2 (en) 2012-05-16 2017-02-07 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
UA115074C2 (uk) 2012-10-15 2017-09-11 Епізайм, Інк. Бензольні сполуки, що містять замісники
CN110898067A (zh) 2012-10-15 2020-03-24 Epizyme股份有限公司 癌症治疗方法

Also Published As

Publication number Publication date
US20240277723A1 (en) 2024-08-22
PT2697199T (pt) 2016-09-05
PL2697199T3 (pl) 2016-12-30
JP5933686B2 (ja) 2016-06-15
SMT201600308B (it) 2016-11-10
ZA201307539B (en) 2014-06-25
KR20180120275A (ko) 2018-11-05
CN107311921A (zh) 2017-11-03
RS62279B1 (sr) 2021-09-30
MY166171A (en) 2018-06-07
JP2019014732A (ja) 2019-01-31
SI3150580T1 (sl) 2019-03-29
HRP20211297T8 (hr) 2022-02-18
CN107311921B (zh) 2021-02-12
IL266418A (en) 2019-06-30
CN104080769A (zh) 2014-10-01
EP4360712A2 (en) 2024-05-01
CL2013002898A1 (es) 2014-08-22
EP2697199A1 (en) 2014-02-19
KR102154946B1 (ko) 2020-09-10
WO2012142504A1 (en) 2012-10-18
HRP20211297T1 (hr) 2021-12-10
ME02500B (me) 2017-02-20
MX2013011921A (es) 2014-03-27
NZ717119A (en) 2017-10-27
JOP20180104A1 (ar) 2019-01-30
CA2832843C (en) 2020-09-29
CY1124617T1 (el) 2022-07-22
DK2697199T3 (en) 2016-09-12
BR112013026324A2 (pt) 2016-10-11
JP6778226B2 (ja) 2020-10-28
KR102032303B1 (ko) 2019-10-15
NZ734744A (en) 2019-03-29
HRP20161115T1 (hr) 2016-11-18
EP3943485B1 (en) 2023-12-27
KR20190121386A (ko) 2019-10-25
US20120264734A1 (en) 2012-10-18
AU2012242595A1 (en) 2013-05-02
US9522152B2 (en) 2016-12-20
US20130123234A1 (en) 2013-05-16
SG194447A1 (en) 2013-12-30
EP4360712A3 (en) 2024-07-31
RS55113B1 (sr) 2016-12-30
KR20230134128A (ko) 2023-09-20
US20170119780A1 (en) 2017-05-04
KR20190025055A (ko) 2019-03-08
US20160022693A1 (en) 2016-01-28
US10155002B2 (en) 2018-12-18
CN104080769B (zh) 2017-06-20
PT3486234T (pt) 2021-09-07
KR101914321B1 (ko) 2018-11-02
CY1117986T1 (el) 2017-05-17
US20170252349A1 (en) 2017-09-07
TWI529162B (zh) 2016-04-11
KR102566864B1 (ko) 2023-08-11
US20150353494A1 (en) 2015-12-10
RU2013150345A (ru) 2015-05-20
CY1121120T1 (el) 2019-12-11
PL3943485T3 (pl) 2024-05-20
HRP20190074T1 (hr) 2019-03-08
US20240245697A1 (en) 2024-07-25
EP3150580A1 (en) 2017-04-05
US20240245698A1 (en) 2024-07-25
CA3086473A1 (en) 2012-10-18
KR20210118968A (ko) 2021-10-01
KR101955871B1 (ko) 2019-03-08
US20140288041A1 (en) 2014-09-25
US8410088B2 (en) 2013-04-02
PL3150580T3 (pl) 2019-04-30
MX343685B (es) 2016-11-17
US20210379076A1 (en) 2021-12-09
IL249273B (en) 2019-05-30
KR102308488B1 (ko) 2021-10-06
EP3486234A1 (en) 2019-05-22
FI3943485T3 (fi) 2024-01-29
AU2012242595B2 (en) 2014-05-15
JO3438B1 (ar) 2019-10-20
LT3943485T (lt) 2024-02-12
EP2697199B1 (en) 2016-06-08
MX2020012695A (es) 2021-04-12
PL3486234T3 (pl) 2021-11-29
IL228745A (en) 2016-12-29
JP2021042243A (ja) 2021-03-18
HUE066461T2 (hu) 2024-08-28
SI2697199T1 (sl) 2016-10-28
HUE056552T2 (hu) 2022-02-28
SI3943485T1 (sl) 2024-04-30
JO3363B1 (ar) 2019-03-13
US9549931B2 (en) 2017-01-24
ES2886099T3 (es) 2021-12-16
US20180318309A1 (en) 2018-11-08
JP2023011933A (ja) 2023-01-24
BR122020006541B1 (pt) 2022-05-10
US9855275B2 (en) 2018-01-02
ES2973868T3 (es) 2024-06-24
JP2018104450A (ja) 2018-07-05
LT3150580T (lt) 2019-02-11
SI3486234T1 (sl) 2021-12-31
US20190192526A1 (en) 2019-06-27
US10420775B2 (en) 2019-09-24
EP3486234B1 (en) 2021-06-02
US8765732B2 (en) 2014-07-01
BR112013026324A8 (pt) 2018-01-30
EP3943485A1 (en) 2022-01-26
KR20140029442A (ko) 2014-03-10
HUE042788T2 (hu) 2019-07-29
PT3150580T (pt) 2019-01-28
PE20140863A1 (es) 2014-07-19
DK3486234T3 (da) 2021-08-16
IL249273A0 (en) 2017-01-31
HK1193804A1 (zh) 2014-10-03
PH12016502132A1 (en) 2017-05-22
JP2016147886A (ja) 2016-08-18
BR112013026324B1 (pt) 2020-12-08
CA2832843A1 (en) 2012-10-18
ES2589555T3 (es) 2016-11-15
RU2017132054A (ru) 2019-02-06
PT3943485T (pt) 2024-03-06
NZ616298A (en) 2016-03-31
RU2017132054A3 (es) 2021-05-14
RU2632193C2 (ru) 2017-10-03
US20200155562A1 (en) 2020-05-21
KR20200105543A (ko) 2020-09-07
IL228745A0 (en) 2013-12-31
US11052093B2 (en) 2021-07-06
US9090562B2 (en) 2015-07-28
TW201302704A (zh) 2013-01-16
JP2014516931A (ja) 2014-07-17
RS58226B1 (sr) 2019-03-29
DK3150580T3 (en) 2019-02-04
HUE028837T2 (en) 2017-01-30
LT3486234T (lt) 2021-09-10
EP3150580B1 (en) 2018-10-17
ES2706951T3 (es) 2019-04-01
LT2697199T (lt) 2016-09-26
DK3943485T3 (da) 2024-01-22

Similar Documents

Publication Publication Date Title
AR086008A1 (es) Compuestos de benceno sustituidos con arilo o heteroarilo
AR121661A2 (es) Esteroides neuroactivos, composiciones y usos de los mismos
AR103833A1 (es) Compuestos bicíclicos de sulfonamida cetona
ES2432821T3 (es) Compuestos de pirimidina, composiciones y métodos de utilización
AR086839A1 (es) Derivados de piridin-2-ona con actividad inhibitoria de ezh2
AR100438A1 (es) Pirazolopiridinas y pirazolopirimidinas
AR115296A1 (es) Heterocíclicos inhibidores de mat2a y métodos de uso para el tratamiento del cáncer
AR109709A1 (es) Inhibidores de la fosfatidilinositol 3-quinasa
AR103297A1 (es) Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina
AR084553A1 (es) DERIVADOS IMIDAZOLICOS HETEROCICLICOS INHIBIDORES DE b-SECRETASA, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y USO DE LOS MISMOS PARA TRATAR ENFERMEDADES NEURODEGENERATIVAS, EN PARTICULAR ALZHEIMER
AR082886A1 (es) Compuestos y composiciones farmaceuticas que los contienen
AR091193A1 (es) HETEROCICLOS DE 5 MIEMBROS QUE CONTIENEN NITROGENO SUSTITUIDO POR CARBOXAMIDA O SULFONAMIDA COMO MODULADORES PARA EL RECEPTOR NUCLEAR HUERFANO RORg
AR099363A1 (es) Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil y pirrolo[2,3-d]piridinil acrilamidas
AR104720A1 (es) Moduladores de ccr2
AR052948A1 (es) DERIVADOS DE ACETILENIL-PIRAZOLO-PIRIMIDINA COMO ANTAGONISTAS DE MGLUR2, METODOS PARA SU PREPARACION, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y SU EMPLEO EN LA FABRICACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE ENFERMEDADES DEL SNC
AR094299A1 (es) Derivados de ftalazin-1(2h)-ona sustituidos
AR091424A1 (es) Compuestos triciclicos sustituidos como inhibidores de receptores del factor de crecimiento del fibroplasto (fgfr)
AR086357A1 (es) Derivados de indazol sustituidos activos como inhibidores de quinasas
AR092108A1 (es) Piridazina 1,4 disustituida, analogos de la misma y metodos para tratar las enfermedades relacionadas con deficiencia del smn
AR085958A1 (es) 8-etil-6-(aril)pirido[2,3-d]pirimidin-7(8h)-onas para el tratamiento de trastornos del cns y cancer
AR094410A1 (es) Compuestos terapéuticos
TR201809990T4 (en) NEW COMPOSITIONS, USES AND METHODS FOR THEIR MAKING.
AR111983A1 (es) ANILLOS 6 - 5 FUSIONADOS COMO INHIBIDORES DE C5a
AR090955A1 (es) Aminas biciclicas c-17 de triterpenoides con actividad inhibidora de la maduracion del vih
AR099498A1 (es) Compuestos de triazina y su uso farmacéutico

Legal Events

Date Code Title Description
FG Grant, registration