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EA201170680A1 - Ингибиторы акт и p70 s6-киназы - Google Patents

Ингибиторы акт и p70 s6-киназы

Info

Publication number
EA201170680A1
EA201170680A1 EA201170680A EA201170680A EA201170680A1 EA 201170680 A1 EA201170680 A1 EA 201170680A1 EA 201170680 A EA201170680 A EA 201170680A EA 201170680 A EA201170680 A EA 201170680A EA 201170680 A1 EA201170680 A1 EA 201170680A1
Authority
EA
Eurasian Patent Office
Prior art keywords
kinase inhibitors
active
formula
compounds
present
Prior art date
Application number
EA201170680A
Other languages
English (en)
Other versions
EA018947B1 (ru
Inventor
Роберт Дин Дэлли
Саджан Джозеф
Тимоти Алан Шеферд
Original Assignee
Эли Лилли Энд Компани
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 Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA201170680A1 publication Critical patent/EA201170680A1/ru
Publication of EA018947B1 publication Critical patent/EA018947B1/ru

Links

Classifications

    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

В настоящем изобретении предложены ингибиторы АКТ и р70 S6-киназы формулы:В настоящем изобретении также предложены фармацевтические композиции, содержащие соединения формулы I, применение соединений формулы I и способы применения соединений формулы I.
EA201170680A 2008-11-11 2009-11-03 Ингибиторы акт и p70 s6-киназы EA018947B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11327308P 2008-11-11 2008-11-11
PCT/US2009/063020 WO2010056563A1 (en) 2008-11-11 2009-11-03 Akt and p70 s6 kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201170680A1 true EA201170680A1 (ru) 2011-12-30
EA018947B1 EA018947B1 (ru) 2013-11-29

Family

ID=41402451

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170680A EA018947B1 (ru) 2008-11-11 2009-11-03 Ингибиторы акт и p70 s6-киназы

Country Status (37)

Country Link
US (1) US8148387B2 (ru)
EP (1) EP2358710B1 (ru)
JP (1) JP5432275B2 (ru)
KR (1) KR101334460B1 (ru)
CN (1) CN102216302B (ru)
AR (1) AR074072A1 (ru)
AU (1) AU2009314324B2 (ru)
BR (1) BRPI0921916A2 (ru)
CA (1) CA2743019C (ru)
CO (1) CO6382114A2 (ru)
CR (1) CR20110240A (ru)
CY (1) CY1113409T1 (ru)
DK (1) DK2358710T3 (ru)
DO (1) DOP2011000129A (ru)
EA (1) EA018947B1 (ru)
EC (1) ECSP11011048A (ru)
ES (1) ES2391704T3 (ru)
HK (1) HK1158203A1 (ru)
HN (1) HN2011001247A (ru)
HR (1) HRP20120738T1 (ru)
IL (1) IL211940A (ru)
JO (1) JO2822B1 (ru)
MA (1) MA32776B1 (ru)
MX (1) MX2011005000A (ru)
MY (1) MY161461A (ru)
NZ (1) NZ592062A (ru)
PA (1) PA8846901A1 (ru)
PE (1) PE20110807A1 (ru)
PL (1) PL2358710T3 (ru)
PT (1) PT2358710E (ru)
RS (1) RS52520B (ru)
SI (1) SI2358710T1 (ru)
TN (1) TN2011000207A1 (ru)
TW (1) TWI422587B (ru)
UA (1) UA100190C2 (ru)
WO (1) WO2010056563A1 (ru)
ZA (1) ZA201102549B (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2690679C2 (ru) * 2014-02-11 2019-06-05 Мерк Патент Гмбх Новые пиримидинимидазоламины в качестве модуляторов активности киназы

Families Citing this family (14)

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Publication number Priority date Publication date Assignee Title
SI2448927T1 (sl) 2009-07-02 2014-06-30 Sanofi Novi (6-okso-1,6-dihidro-pirimidin-2-il)-amidni derivati, njihova priprava in njihova farmacevtska uporaba kot AKT fosforilacijski inhibitorji
CN102574852B (zh) * 2009-10-23 2014-06-25 伊莱利利公司 Akt抑制剂
AP3597A (en) 2011-04-07 2016-02-19 Bayer Ip Gmbh Imidazopyridazines as akt kinase inhibitors
JP5695800B2 (ja) * 2011-07-09 2015-04-08 山東軒竹医薬科技有限公司 ジペプチジルペプチダーゼ−ｉｖ阻害剤の塩の結晶形ｉ、及びその製造方法並びにその応用
SI2755965T1 (sl) * 2011-09-12 2017-12-29 Merck Patent Gmbh Novi imidazolni amidi kot modulatorji kinazne aktivnosti
HUE034979T2 (en) 2011-09-12 2018-05-02 Merck Patent Gmbh Aminopyrimidine derivatives for use as modulators of kinase activity
AU2013344552B2 (en) * 2012-11-16 2018-03-15 Xiaoling Chen Novel heterocyclic derivatives as modulators of kinase activity
US9315517B2 (en) * 2012-11-16 2016-04-19 Merck Patent Gmbh Imidazol-piperidinyl derivatives as modulators of kinase activity
ES2746756T3 (es) 2013-03-11 2020-03-06 Merck Patent Gmbh Derivados de 6-[4-(1H-imidazol-2-il)piperidin-1-il]pirimidin-4-amina como moduladores de la actividad cinasa
TW201718574A (zh) 2015-08-12 2017-06-01 美國禮來大藥廠 Ｃｇｒｐ受體拮抗劑
TWI679202B (zh) * 2016-05-20 2019-12-11 日商大鵬藥品工業股份有限公司 新穎5H-吡咯并[2, 3-d]嘧啶-6(7H)-酮衍生物
CN115397815B (zh) * 2020-03-17 2024-06-14 江苏恒瑞医药股份有限公司 稠合二环类衍生物、其制备方法及其在医药上的应用
CN113444110B (zh) * 2020-03-25 2023-05-12 江苏恒瑞医药股份有限公司 四氢吡咯并吡唑类衍生物、其制备方法及其在医药上的应用
TW202328138A (zh) 2021-09-17 2023-07-16 大陸商江蘇恒瑞醫藥股份有限公司 稠合二環類衍生物的可藥用鹽、晶型及其製備方法

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AU2005249380C1 (en) 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
ATE543821T1 (de) 2004-12-28 2012-02-15 Exelixis Inc Ä1h-pyrazoloä3,4-düpyrimidin-4-ylü-piperidin- oder piperazinverbindungen als serin-threonin- kinasemodulatoren (p70s6k, atk1 und atk2) zur behandlung von immunologischen, entzündlichen und proliferativen erkrankungen
WO2006091450A1 (en) * 2005-02-18 2006-08-31 Lexicon Genetics Incorporated 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine compounds
EP1907383A1 (en) 2005-06-30 2008-04-09 Prosidion Limited Gpcr agonists
EP2043655A2 (en) 2006-04-25 2009-04-08 Astex Therapeutics Limited Purine and deazapurine derivatives as pharmaceutical compounds
JP2009536620A (ja) 2006-04-25 2009-10-15 アステックス、セラピューティックス、リミテッド 医薬組み合わせ物
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
AR064416A1 (es) * 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas.
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2690679C2 (ru) * 2014-02-11 2019-06-05 Мерк Патент Гмбх Новые пиримидинимидазоламины в качестве модуляторов активности киназы

Also Published As

Publication number Publication date
JO2822B1 (en) 2014-09-15
TW201022268A (en) 2010-06-16
IL211940A (en) 2014-01-30
DOP2011000129A (es) 2016-02-29
NZ592062A (en) 2013-03-28
AR074072A1 (es) 2010-12-22
MX2011005000A (es) 2011-05-25
HK1158203A1 (en) 2012-07-13
CR20110240A (es) 2011-06-09
ES2391704T3 (es) 2012-11-29
RS52520B (en) 2013-04-30
PA8846901A1 (es) 2010-06-28
KR101334460B1 (ko) 2013-12-02
CN102216302A (zh) 2011-10-12
EA018947B1 (ru) 2013-11-29
CN102216302B (zh) 2013-08-21
ECSP11011048A (es) 2011-06-30
US8148387B2 (en) 2012-04-03
UA100190C2 (en) 2012-11-26
PT2358710E (pt) 2012-10-01
MA32776B1 (fr) 2011-11-01
DK2358710T3 (da) 2012-09-03
CY1113409T1 (el) 2016-06-22
AU2009314324B2 (en) 2013-06-20
MY161461A (en) 2017-04-14
US20100120801A1 (en) 2010-05-13
PL2358710T3 (pl) 2012-12-31
KR20110074578A (ko) 2011-06-30
CO6382114A2 (es) 2012-02-15
WO2010056563A1 (en) 2010-05-20
ZA201102549B (en) 2012-09-26
JP5432275B2 (ja) 2014-03-05
TN2011000207A1 (en) 2012-12-17
JP2012508274A (ja) 2012-04-05
PE20110807A1 (es) 2011-10-31
HRP20120738T1 (hr) 2012-10-31
IL211940A0 (en) 2011-06-30
BRPI0921916A2 (pt) 2015-12-29
HN2011001247A (es) 2013-05-20
EP2358710B1 (en) 2012-08-15
AU2009314324A1 (en) 2010-05-20
EP2358710A1 (en) 2011-08-24
CA2743019A1 (en) 2010-05-20
SI2358710T1 (sl) 2012-11-30
CA2743019C (en) 2013-08-13
TWI422587B (zh) 2014-01-11

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