JP5628028B2 - Aktプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン - Google Patents

Aktプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン Download PDF

Info

Publication number
JP5628028B2
JP5628028B2 JP2010515269A JP2010515269A JP5628028B2 JP 5628028 B2 JP5628028 B2 JP 5628028B2 JP 2010515269 A JP2010515269 A JP 2010515269A JP 2010515269 A JP2010515269 A JP 2010515269A JP 5628028 B2 JP5628028 B2 JP 5628028B2
Authority
JP
Japan
Prior art keywords
methyl
dihydro
cyclopenta
pyrimidin
piperazin
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2010515269A
Other languages
English (en)
Japanese (ja)
Other versions
JP2010532386A (ja
JP2010532386A5 (cg-RX-API-DMAC7.html
Inventor
ジョセフ ベンクシク,
ジョセフ ベンクシク,
ジェイムス エフ. ブレーク,
ジェイムス エフ. ブレーク,
ジェイムス エム. グラハム,
ジェイムス エム. グラハム,
マーティン エフ. ヘンテマン,
マーティン エフ. ヘンテマン,
ニコラス シー. カラン,
ニコラス シー. カラン,
イアン エス. ミッチェル,
イアン エス. ミッチェル,
スティーブン ティー. シェラクター,
スティーブン ティー. シェラクター,
キース エル. スペンサー,
キース エル. スペンサー,
デンミン シャオ,
デンミン シャオ,
ルイ スー,
ルイ スー,
マイク ウェルチ,
マイク ウェルチ,
ユン リャン,
ユン リャン,
ブライアン エス. サフィーナ,
ブライアン エス. サフィーナ,
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
Original Assignee
Genentech 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 Genentech Inc filed Critical Genentech Inc
Publication of JP2010532386A publication Critical patent/JP2010532386A/ja
Publication of JP2010532386A5 publication Critical patent/JP2010532386A5/ja
Application granted granted Critical
Publication of JP5628028B2 publication Critical patent/JP5628028B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Ophthalmology & Optometry (AREA)
JP2010515269A 2007-07-05 2008-07-03 Aktプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン Active JP5628028B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US94813807P 2007-07-05 2007-07-05
US60/948,138 2007-07-05
US2008808P 2008-01-09 2008-01-09
US61/020,088 2008-01-09
PCT/US2008/069144 WO2009006567A2 (en) 2007-07-05 2008-07-03 Pyrimidyl cyclopentanes as akt protein kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2013207007A Division JP2014028842A (ja) 2007-07-05 2013-10-02 Aktプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン

Publications (3)

Publication Number Publication Date
JP2010532386A JP2010532386A (ja) 2010-10-07
JP2010532386A5 JP2010532386A5 (cg-RX-API-DMAC7.html) 2012-07-26
JP5628028B2 true JP5628028B2 (ja) 2014-11-19

Family

ID=40076864

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2010515269A Active JP5628028B2 (ja) 2007-07-05 2008-07-03 Aktプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン
JP2013207007A Withdrawn JP2014028842A (ja) 2007-07-05 2013-10-02 Aktプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2013207007A Withdrawn JP2014028842A (ja) 2007-07-05 2013-10-02 Aktプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン

Country Status (19)

Country Link
US (1) US8618097B2 (cg-RX-API-DMAC7.html)
EP (1) EP2170863B1 (cg-RX-API-DMAC7.html)
JP (2) JP5628028B2 (cg-RX-API-DMAC7.html)
KR (2) KR20150089099A (cg-RX-API-DMAC7.html)
CN (2) CN101801955B (cg-RX-API-DMAC7.html)
AR (1) AR067413A1 (cg-RX-API-DMAC7.html)
AU (1) AU2008272830B8 (cg-RX-API-DMAC7.html)
BR (1) BRPI0813999A2 (cg-RX-API-DMAC7.html)
CA (1) CA2692502C (cg-RX-API-DMAC7.html)
CO (1) CO6251283A2 (cg-RX-API-DMAC7.html)
CR (1) CR11229A (cg-RX-API-DMAC7.html)
EC (1) ECSP109937A (cg-RX-API-DMAC7.html)
ES (1) ES2551352T3 (cg-RX-API-DMAC7.html)
MA (1) MA31679B1 (cg-RX-API-DMAC7.html)
NZ (1) NZ582692A (cg-RX-API-DMAC7.html)
RU (1) RU2486181C2 (cg-RX-API-DMAC7.html)
SG (1) SG185274A1 (cg-RX-API-DMAC7.html)
TW (1) TWI450720B (cg-RX-API-DMAC7.html)
WO (1) WO2009006567A2 (cg-RX-API-DMAC7.html)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2068878B1 (en) 2006-09-20 2019-04-10 Aerie Pharmaceuticals, Inc. Rho kinase inhibitors
US8455513B2 (en) 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
WO2009089352A1 (en) 2008-01-08 2009-07-16 Array Biopharma Inc. Pyrrolopyridines as kinase inhibitors
US8372842B2 (en) 2008-01-09 2013-02-12 Array Biopharma Inc. Pyrazolopyridines as kinase inhibitors
CL2009000035A1 (es) 2008-01-09 2009-11-27 Array Biopharma Inc Compuestos derivados 3-espiro-heterociclo-1il-5h-ciclopentan[d]pirimidin-indol, util para inhibir la actividad de akt quinasa; composicion farmaceutica que comprende dichos compuestos; y uso en el tratamiento de enfermedades tal como cancer, fibrosis quistica, diabetes, enfermedad de alzheimer, entre otras.
JP5539225B2 (ja) 2008-01-09 2014-07-02 アレイ バイオファーマ、インコーポレイテッド Aktタンパク質キナーゼ阻害剤としての水酸化されたピリミジルシクロペンタン
CN101932564B (zh) 2008-01-09 2012-12-26 阵列生物制药公司 作为akt蛋白激酶抑制剂的羟基化嘧啶基环戊烷类
JP5635910B2 (ja) 2008-01-09 2014-12-03 アレイ バイオファーマ、インコーポレイテッド AKTタンパク質キナーゼ阻害剤としての5H−シクロペンタ[d]ピリミジン
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
CA2929545C (en) 2009-05-01 2019-04-09 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
CA2793892A1 (en) 2010-04-16 2011-10-20 Elizabeth Punnoose Foxo3a as predictive biomarker for pi3k/akt kinase pathway inhibitor efficacy
CN103858007B (zh) 2011-04-01 2017-03-29 基因泰克公司 用于预测对癌症治疗的敏感性的生物标记
BR112014028593A2 (pt) 2012-05-17 2017-12-19 Genentech Inc forma amorfa de um composto de pirimidinil-ciclopentano inibidor de akt, composições e métodos dos mesmos"
US9452990B2 (en) 2012-06-20 2016-09-27 Novartis Ag Complement pathway modulators and uses thereof
EP2959014B1 (en) 2013-02-25 2019-11-13 Genentech, Inc. Methods and compositions for detecting and treating drug resistant akt mutant
ES2852377T3 (es) 2013-03-15 2021-09-13 Aerie Pharmaceuticals Inc Sales dimesilato de 4-(3-amino-1-(isoquinolin-6-ilamino)-1-oxopropan-2-il)bencilo, sus combinaciones con prostaglandinas y el uso de las mismas en el tratamiento de trastornos oculares
US10550087B2 (en) 2015-11-17 2020-02-04 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
US9643927B1 (en) 2015-11-17 2017-05-09 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
CN109640966A (zh) 2016-08-31 2019-04-16 爱瑞制药公司 眼用组合物
SG10202104386UA (en) 2016-10-28 2021-05-28 Icahn School Med Mount Sinai Compositions and methods for treating ezh2-mediated cancer
EP3609871A4 (en) 2017-03-31 2021-01-06 Aerie Pharmaceuticals, Inc. ARYL CYCLOPROPYL-AMINO-ISOQUINOLINYL AMIDE COMPOUNDS
CA3092677A1 (en) * 2018-03-06 2019-09-12 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (akt) degradation / disruption compounds and methods of use
BR112020020307A2 (pt) * 2018-04-04 2021-01-12 Arvinas Operations, Inc. Moduladores de proteólise e métodos de uso associados
CN112996518A (zh) 2018-06-21 2021-06-18 西奈山伊坎医学院 Wd40重复结构域蛋白5(wdr5)降解/破坏化合物和使用方法
WO2020056345A1 (en) 2018-09-14 2020-03-19 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
US20220185796A1 (en) * 2019-03-27 2022-06-16 St. Jude Children's Research Hospital Small molecule modulators of pank
EP3965824B1 (en) 2019-05-06 2025-01-08 Icahn School of Medicine at Mount Sinai Heterobifunctional compounds as degraders of hpk1
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
WO2023109540A1 (zh) * 2021-12-17 2023-06-22 中国医药研究开发中心有限公司 具有akt激酶抑制活性的杂环化合物及其制备方法和医药用途
KR20250151412A (ko) 2023-01-26 2025-10-21 아비나스 오퍼레이션스, 인코포레이티드 세레블론계 kras 분해 단백질 및 이와 관련된 용도

Family Cites Families (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3885035A (en) 1972-04-05 1975-05-20 Sandoz Ag Method for treating arrhythmia by using 1,4-bis(4 quinazolinyl) piperazines
US3956495A (en) 1973-10-30 1976-05-11 Eli Lilly And Company 2,4-Diaminoquinazolines as antithrombotic agents
US3966936A (en) 1974-02-21 1976-06-29 Pfizer Inc. Piperazino quinazoline bronchodilators
US4060615A (en) 1976-02-18 1977-11-29 Mead Johnson & Company 2-Piperazinyl-6,7-dimethoxyquinazolines
JPS562968A (en) 1979-06-21 1981-01-13 Mitsubishi Yuka Yakuhin Kk Novel pyrimidine derivative
JPS6270A (ja) 1985-03-07 1987-01-06 Sankyo Co Ltd シクロペンタ〔d〕ピリミジン誘導体
WO1990007926A1 (en) 1989-01-20 1990-07-26 Pfizer Inc. 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines
KR100262254B1 (ko) 1992-10-05 2000-07-15 나카히로 마오미 피리미딘 화합물
EP0710654A4 (en) 1993-07-23 1996-08-28 Green Cross Corp TRIAZOLE DERIVATIVE AND ITS PHARMACEUTICAL USE
GB9416189D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
RU2129549C1 (ru) 1994-08-13 1999-04-27 Юхан Корпорейшн Производные пиримидина и способы их получения
US5525625A (en) 1995-01-24 1996-06-11 Warner-Lambert Company 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders
US7125880B1 (en) 1995-06-06 2006-10-24 Pfizer Inc. Corticotropin releasing factor antagonists
ZA979961B (en) 1996-11-15 1999-05-05 Lilly Co Eli 5-HT1F agonists
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
US6821963B2 (en) 1997-07-01 2004-11-23 Warner-Lambert Company 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors
US6506798B1 (en) 1997-07-01 2003-01-14 Warner-Lambert Company 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors
BR9810366A (pt) 1997-07-01 2000-08-29 Warner Lambert Co Derivados de ácido 4-bromo ou 4-iodo fenilamino benzidroxîmico e seu uso como inibidores de mek
NZ501277A (en) 1997-07-01 2002-12-20 Warner Lambert Co -2(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors
US6310060B1 (en) 1998-06-24 2001-10-30 Warner-Lambert Company 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors
WO1999051582A1 (en) 1998-03-31 1999-10-14 Kyowa Hakko Kogyo Co., Ltd. Nitrogenous heterocyclic compounds
DE19853278A1 (de) 1998-11-19 2000-05-25 Aventis Pharma Gmbh Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
HUP0104933A3 (en) 1999-01-07 2003-12-29 Warner Lambert Co Antiviral method using mek inhibitors
ATE292462T1 (de) 1999-01-07 2005-04-15 Warner Lambert Co Behandlung von asthma anhand von mek-inhibitoren
IL144215A0 (en) 1999-01-13 2002-05-23 Warner Lambert Co 1-heterocycle substituted diarylamines
ATE311363T1 (de) 1999-01-13 2005-12-15 Warner Lambert Co Sulfohydroxamsäure and sulfohydroxamate und ihre verwendung als mek-inhibitoren
ES2252996T3 (es) 1999-01-13 2006-05-16 Warner-Lambert Company Llc Derivados de bencenosulfonamida y su uso como inhibidores de mek.
IL144214A0 (en) 1999-01-13 2002-05-23 Warner Lambert Co Benzoheterocycles and their use as mek inhibitors
BR9916857A (pt) 1999-01-13 2001-12-04 Warner Lambert Co 4 heteroaril diarilaminas
CA2348236A1 (en) 1999-01-13 2000-07-20 Stephen Douglas Barrett 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
HUP0202180A3 (en) 1999-07-16 2004-10-28 Warner Lambert Co Method for treating chronic pain using mek inhibitors
AU5785900A (en) 1999-07-16 2001-02-05 Warner-Lambert Company Method for treating chronic pain using mek inhibitors
EP1202726A2 (en) 1999-07-16 2002-05-08 Warner-Lambert Company Llc Method for treating chronic pain using mek inhibitors
PL352835A1 (en) 1999-07-16 2003-09-08 Warner-Lambert Company Method for treating chronic pain using mek inhibitors
BR0109188A (pt) 2000-03-15 2003-03-18 Warner Lambert Co Diarilaminas 5-amida substituìdas como inibidores de mex
YU2503A (sh) 2000-07-19 2006-05-25 Warner-Lambert Company Oksigenovani estri 4-jodo fenilamino benzhidroksamskih kiselina
JP2004507518A (ja) 2000-08-25 2004-03-11 ワーナー−ランバート・カンパニー・エルエルシー N−アリール−アントラニル酸及びその誘導体の製造法
JP2004509115A (ja) 2000-09-15 2004-03-25 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとして有用なピラゾール化合物
AU2002210714A1 (en) 2000-11-02 2002-06-11 Astrazeneca Ab Substituted quinolines as antitumor agents
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
ATE386727T1 (de) 2001-04-30 2008-03-15 Glaxo Group Ltd Kondensierte pyrimidine als antagonisten des corticotropin releasing factor (crf)
US7115741B2 (en) 2001-09-06 2006-10-03 Levy Daniel E 4-thieno[2,3-D]pyrimidin-4-YL piperazine compounds
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
TW200306819A (en) * 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
CA2478534A1 (en) 2002-03-13 2003-09-25 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as mek inhibitors
TWI350285B (en) 2002-03-13 2011-10-11 Array Biopharma Inc N3 alkylated benzimidazole derivatives as mek inhibitors
AU2003226250B2 (en) 2002-04-08 2007-08-16 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
CA2480880C (en) 2002-04-08 2011-03-22 Merck & Co., Inc. Inhibitors of akt activity
AU2003226271B2 (en) 2002-04-08 2007-10-18 Merck Sharp & Dohme Corp. Fused quinoxaline derivatives as inhibitors of Akt activity
EP1496896A4 (en) 2002-04-08 2007-10-31 Merck & Co Inc AKT INHIBITORS EFFECT
MXPA04011093A (es) 2002-05-10 2005-02-14 Neurocrine Biosciences Inc Piperazina sustituida como ligandos de receptores de melanocortina.
AU2003284981B2 (en) 2002-10-30 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
US20040102360A1 (en) 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
GB0308208D0 (en) 2003-04-09 2003-05-14 Glaxo Group Ltd Chemical compounds
EP1620095A4 (en) 2003-04-24 2009-04-01 Merck & Co Inc HEMMER OF ACT ACTIVITY
WO2004111014A1 (en) 2003-06-06 2004-12-23 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
EP1663994B1 (en) 2003-08-05 2012-03-07 Vertex Pharmaceuticals Incorporated Tetrahydroquinazoline compounds as inhibitors of voltage-gated ion channels
DE602004009200T2 (de) 2003-08-12 2008-07-10 F. Hoffmann-La Roche Ag Tetrahydrochinazolinderivate als cfr-antagonisten
BRPI0414238A (pt) 2003-09-09 2006-10-31 Ono Pharmaceutical Co antagonistas de crf e compostos heterobicìclicos
WO2005039564A1 (en) 2003-10-02 2005-05-06 Vertex Pharmaceuticals Incorporated Phthalimide compounds useful as protein kinase inhibitors
JP2007512364A (ja) * 2003-11-21 2007-05-17 アレイ バイオファーマ、インコーポレイテッド Aktプロテインキナーゼインヒビター
JP5213229B2 (ja) 2004-04-23 2013-06-19 エグゼリクシス, インコーポレイテッド キナーゼ調節因子および使用方法
WO2005113762A1 (en) 2004-05-18 2005-12-01 Pfizer Products Inc. CRYSTAL STRUCTURE OF PROTEIN KINASE B-α (AKT-1) AND USES THEREOF
US20060025074A1 (en) 2004-07-30 2006-02-02 Chih-Ming Liang Bluetooth-based headset
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
TWM266655U (en) 2004-09-23 2005-06-01 Blueexpert Technology Corp Bluetooth earphone device capable of wirelessly receiving and transmitting stereo sound signal and digital information signal
TW200621257A (en) * 2004-10-20 2006-07-01 Astellas Pharma Inc Pyrimidine derivative fused with nonaromatic ring
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
CA2590961C (en) * 2004-12-28 2013-11-26 Exelixis, Inc. [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases
JP2008531542A (ja) 2005-02-24 2008-08-14 ファイザー・プロダクツ・インク 抗癌剤として有用な二環式複素芳香族誘導体
JP2008539277A (ja) * 2005-04-28 2008-11-13 スーパージェン, インコーポレイテッド プロテインキナーゼインヒビター
WO2006127587A1 (en) 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
KR100959771B1 (ko) 2005-06-10 2010-05-28 머크 샤프 앤드 돔 코포레이션 Akt 활성의 억제제
AR054485A1 (es) 2005-06-21 2007-06-27 Cancer Rec Tech Ltd ARIL-ALQUILAMINAS Y HETEROARIL-ALQUILAMINAS COMO INHIBIDORES DE PROTEINA QUINASA A Y B, UN PROCESO PARA SU PREPARACION, COMPOSICIONES FARMACEUTICAS QUE LAS CONTIENEN Y SU USO EN LA FABRICACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO O PROFILAXIS DE ENFERMEDADES ORIGINADAS EN EL CRECIMIENTO ANORMAL DE LA
EP1948658A1 (en) 2005-10-13 2008-07-30 Glaxo Group Limited Pyrrolopyrimidine derivatives as syk inhibitors
AR056893A1 (es) 2005-12-28 2007-10-31 Takeda Pharmaceutical Compuestos heterociclicos fusionados y no fusionados, antagonistas de receptores mineralocorticoides
JP2009534454A (ja) 2006-04-25 2009-09-24 アステックス、セラピューティックス、リミテッド 医薬化合物
RU2008152171A (ru) 2006-07-05 2010-08-10 Интермьюн, Инк. (Us) Новые ингибиторы вирусной репликации гепатита с
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US7910747B2 (en) 2006-07-06 2011-03-22 Bristol-Myers Squibb Company Phosphonate and phosphinate pyrazolylamide glucokinase activators
UA95641C2 (xx) 2006-07-06 2011-08-25 Эррей Биофарма Инк. Гідроксильовані піримідильні циклопентани як інгібітори акт протеїнкінази$гидроксилированные пиримидильные циклопентаны как ингибиторы акт протеинкиназы
SI2049500T1 (sl) 2006-07-06 2012-01-31 Array Biopharma Inc Ciklopenta (d) pirimidini kot AKT protein kinazni inhibitorji
BRPI0714062A2 (pt) 2006-07-06 2012-12-18 Glaxo Group Ltd n-fenil-metil-5-oxo-prolina-2-amidas substituìdas como antagonistas do receptor da p2x, e os seus métodos de uso
GB0613518D0 (en) 2006-07-06 2006-08-16 Phytopharm Plc Chemical compounds
CN101511842B (zh) 2006-07-06 2012-10-31 阵列生物制药公司 作为akt蛋白激酶抑制剂的二氢呋喃并嘧啶
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
US7659270B2 (en) * 2006-08-11 2010-02-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8329159B2 (en) * 2006-08-11 2012-12-11 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US20100190815A1 (en) * 2006-09-08 2010-07-29 Kyowa Hakko Bio Co., Ltd. Hypertension-ameliorating agent
US7741347B2 (en) * 2007-05-17 2010-06-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8377937B2 (en) 2007-07-05 2013-02-19 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8629171B2 (en) * 2007-08-08 2014-01-14 Bristol-Myers Squibb Company Crystalline form of methyl ((1S)-1-((25)-2-(5-(4'-(2-((25)-1((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt
CN101932564B (zh) 2008-01-09 2012-12-26 阵列生物制药公司 作为akt蛋白激酶抑制剂的羟基化嘧啶基环戊烷类
JP5539225B2 (ja) 2008-01-09 2014-07-02 アレイ バイオファーマ、インコーポレイテッド Aktタンパク質キナーゼ阻害剤としての水酸化されたピリミジルシクロペンタン
JP5635910B2 (ja) 2008-01-09 2014-12-03 アレイ バイオファーマ、インコーポレイテッド AKTタンパク質キナーゼ阻害剤としての5H−シクロペンタ[d]ピリミジン
US7704992B2 (en) * 2008-02-13 2010-04-27 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7906655B2 (en) * 2008-08-07 2011-03-15 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2010096462A1 (en) * 2009-02-17 2010-08-26 Enanta Pharmaceuticals, Inc Linked diimidazole derivatives
KR20180028070A (ko) * 2009-05-13 2018-03-15 길리애드 파마셋 엘엘씨 항바이러스 화합물

Also Published As

Publication number Publication date
JP2010532386A (ja) 2010-10-07
KR20150089099A (ko) 2015-08-04
MA31679B1 (fr) 2010-09-01
WO2009006567A3 (en) 2009-03-19
US20110015204A1 (en) 2011-01-20
AU2008272830B8 (en) 2013-12-12
CA2692502A1 (en) 2009-01-08
TW200902013A (en) 2009-01-16
BRPI0813999A2 (pt) 2019-10-01
RU2486181C2 (ru) 2013-06-27
AU2008272830B2 (en) 2013-12-05
WO2009006567A2 (en) 2009-01-08
KR20100044819A (ko) 2010-04-30
US8618097B2 (en) 2013-12-31
CN101801955A (zh) 2010-08-11
ES2551352T3 (es) 2015-11-18
EP2170863A2 (en) 2010-04-07
EP2170863B1 (en) 2015-09-02
CA2692502C (en) 2016-03-01
SG185274A1 (en) 2012-11-29
NZ582692A (en) 2012-05-25
CN103396409A (zh) 2013-11-20
KR101650956B1 (ko) 2016-08-24
TWI450720B (zh) 2014-09-01
HK1147255A1 (en) 2011-08-05
CN101801955B (zh) 2013-05-08
CN103396409B (zh) 2015-03-11
JP2014028842A (ja) 2014-02-13
AU2008272830A1 (en) 2009-01-08
CO6251283A2 (es) 2011-02-21
CR11229A (es) 2010-02-09
RU2010103813A (ru) 2011-08-10
AR067413A1 (es) 2009-10-07
ECSP109937A (es) 2010-03-31

Similar Documents

Publication Publication Date Title
JP5628028B2 (ja) Aktプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン
KR101527232B1 (ko) Akt 단백질 키나제 억제제로서의 시클로펜타〔d〕피리미딘
JP5836294B2 (ja) Aktプロテインキナーゼ阻害剤としてのヒドロキシル化およびメトキシル化されたシクロペンタ[d]ピリミジン
JP5542282B2 (ja) Aktプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン
US9409886B2 (en) Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
HK1147255B (en) Pyrimidyl cyclopentanes as akt protein kinase inhibitors
HK1185873A (en) Cyclopenta [d] pyrimidines as akt protein kinase inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110613

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20110613

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120531

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20130530

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130604

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130903

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130910

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20131002

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20140121

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140521

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20140704

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140722

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140807

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140912

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20141001

R150 Certificate of patent or registration of utility model

Ref document number: 5628028

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250