KR101624752B1 - Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄 - Google Patents

Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄 Download PDF

Info

Publication number
KR101624752B1
KR101624752B1 KR1020107017573A KR20107017573A KR101624752B1 KR 101624752 B1 KR101624752 B1 KR 101624752B1 KR 1020107017573 A KR1020107017573 A KR 1020107017573A KR 20107017573 A KR20107017573 A KR 20107017573A KR 101624752 B1 KR101624752 B1 KR 101624752B1
Authority
KR
South Korea
Prior art keywords
mmol
compound
compounds
akt
tert
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.)
Expired - Fee Related
Application number
KR1020107017573A
Other languages
English (en)
Korean (ko)
Other versions
KR20100103865A (ko
Inventor
요셉 벤크식
제임스 에프. 블레이크
니콜라스 씨. 칼란
이안 에스. 미첼
케이트 엘. 스펜서
뎅밍 시아오
루이 슈
크리스틴 샤봇
스티븐 도
준 리앙
브라이언 사피나
비롱 장
제임스 그레이햄
Original Assignee
어레이 바이오파마 인크.
제넨테크, 인크.
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 어레이 바이오파마 인크., 제넨테크, 인크. filed Critical 어레이 바이오파마 인크.
Publication of KR20100103865A publication Critical patent/KR20100103865A/ko
Application granted granted Critical
Publication of KR101624752B1 publication Critical patent/KR101624752B1/ko
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • 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
    • 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
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
KR1020107017573A 2008-01-09 2009-01-09 Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄 Expired - Fee Related KR101624752B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US2008708P 2008-01-09 2008-01-09
US61/020,087 2008-01-09

Publications (2)

Publication Number Publication Date
KR20100103865A KR20100103865A (ko) 2010-09-28
KR101624752B1 true KR101624752B1 (ko) 2016-05-26

Family

ID=40386151

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020107017573A Expired - Fee Related KR101624752B1 (ko) 2008-01-09 2009-01-09 Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄

Country Status (19)

Country Link
US (1) US8853216B2 (enExample)
EP (1) EP2240455B1 (enExample)
JP (1) JP5539225B2 (enExample)
KR (1) KR101624752B1 (enExample)
CN (1) CN101932565B (enExample)
AU (1) AU2009204019B2 (enExample)
BR (1) BRPI0907372A2 (enExample)
CA (1) CA2711692A1 (enExample)
CO (1) CO6280510A2 (enExample)
CR (1) CR11591A (enExample)
EC (1) ECSP10010392A (enExample)
ES (1) ES2401685T3 (enExample)
IL (1) IL206607A0 (enExample)
MA (1) MA32343B1 (enExample)
MX (1) MX2010007546A (enExample)
NZ (1) NZ586720A (enExample)
RU (1) RU2520735C2 (enExample)
UA (1) UA100544C2 (enExample)
WO (1) WO2009089453A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
NZ582692A (en) * 2007-07-05 2012-05-25 Array Biopharma Inc Pyrimidyl cyclopentanes as akt protein kinase inhibitors
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
EP2242755B1 (en) 2008-01-08 2012-09-12 Array Biopharma, Inc. Pyrrolopyridines as kinase inhibitors
EP2242757B1 (en) 2008-01-09 2012-08-01 Array Biopharma, Inc. Pyrazolopyridines as kinase inhibitors
WO2009089462A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors
EP2850200A1 (en) * 2012-05-17 2015-03-25 Genentech, Inc. Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof
MX385726B (es) * 2013-11-15 2025-03-18 Hoffmann La Roche Procesos para la preparación de compuestos de pirimidinilciclopentano.
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment

Family Cites Families (87)

* 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
US7067664B1 (en) 1995-06-06 2006-06-27 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
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
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
JP2002511092A (ja) 1997-07-01 2002-04-09 ワーナー−ランバート・コンパニー 4−ブロモまたは4−ヨードフェニルアミノベンズヒドロキサム酸誘導体およびそのmek阻害剤としての使用
AU756586C (en) 1997-07-01 2004-01-29 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
CA2358438A1 (en) 1999-01-07 2000-07-13 David Thomas Dudley Antiviral method using mek inhibitors
DE69924641D1 (de) 1999-01-07 2005-05-12 Warner Lambert Company Llc Mor Behandlung von asthma anhand von mek-inhibitoren
AU2203700A (en) 1999-01-13 2000-08-01 Warner-Lambert Company Benzoheterocycles and their use as mek inhibitors
WO2000042002A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors
WO2000042003A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Benzenesulfonamide derivatives and their use as mek inhibitors
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
WO2000042029A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company 1-heterocycle substituted diarylamines
JP2002534446A (ja) 1999-01-13 2002-10-15 ワーナー−ランバート・カンパニー 4′ヘテロアリールジアリールアミン
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
TR200200205T2 (tr) 1999-07-16 2002-06-21 Warner-Lambert Company MEK inhibitörleri kullanılarak kronik ağrının tedavi edilmesi
IL147617A0 (en) 1999-07-16 2002-08-14 Warner Lambert Co 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
KR20020015376A (ko) 1999-07-16 2002-02-27 로즈 암스트롱, 크리스틴 에이. 트러트웨인 Mek 억제제를 사용한 만성 통증의 치료 방법
MXPA02008103A (es) 2000-03-15 2002-11-29 Warner Lambert Co Diarilaminas sustituidas con 5-amida como inhibidores mek.
US6960614B2 (en) 2000-07-19 2005-11-01 Warner-Lambert Company Oxygenated esters of 4-lodo phenylamino benzhydroxamic acids
MXPA03001654A (es) 2000-08-25 2004-09-10 Warner Lambert Co Proceso para la elaboracion del acido n-aril-antranilico y sus derivados.
JP2004514718A (ja) 2000-11-02 2004-05-20 アストラゼネカ アクチボラグ 抗癌剤としての置換キノリン類
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
AR033295A1 (es) 2001-04-30 2003-12-10 Glaxo Group Ltd Compuestos biciclicos de pirimidina, proceso para su obtencion, uso de los mismos para la preparacion de una composicion farmaceutica y dicha composicion farmaceutica
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
MXPA04008893A (es) 2002-03-13 2005-06-20 Array Biopharma Inc Derivados de bencimidazol n3 alquilados como inhibidores de mek.
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
JP2005526076A (ja) 2002-03-13 2005-09-02 アレイ バイオファーマ、インコーポレイテッド Mek阻害剤としてのn3アルキル化ベンズイミダゾール誘導体
AU2003223467B2 (en) 2002-04-08 2007-10-04 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
CA2481229C (en) 2002-04-08 2010-09-21 Merck & Co., Inc. Substituted pyrazine inhibitors of akt
CA2481241C (en) 2002-04-08 2010-07-27 Merck & Co., Inc. Fused quinoxaline derivatives as inhibitors of akt activity
JP4451136B2 (ja) 2002-04-08 2010-04-14 メルク エンド カムパニー インコーポレーテッド Akt活性阻害薬
MXPA04011093A (es) 2002-05-10 2005-02-14 Neurocrine Biosciences Inc Piperazina sustituida como ligandos de receptores de melanocortina.
DE60336576D1 (de) 2002-10-30 2011-05-12 Merck Sharp & Dohme Hemmer der akt aktivität
US20040102360A1 (en) 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
US20040099681A1 (en) * 2002-11-21 2004-05-27 Nice-Pak Products, Inc. Non-planar dispenser for articles
GB0308208D0 (en) 2003-04-09 2003-05-14 Glaxo Group Ltd Chemical compounds
JP2006524254A (ja) 2003-04-24 2006-10-26 メルク エンド カムパニー インコーポレーテッド Akt活性の阻害剤
ATE440825T1 (de) 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
KR20060118398A (ko) 2003-08-05 2006-11-23 버텍스 파마슈티칼스 인코포레이티드 전압 개폐 이온 채널 억제제로서의 축합 피라미딘 화합물
CA2534785A1 (en) 2003-08-12 2005-02-17 Robin Douglas Clark Tetrahydroquinazoline derivatives as cfr antagonists
KR20060072142A (ko) 2003-09-09 2006-06-27 오노 야꾸힝 고교 가부시키가이샤 Crf 길항제 및 이환식 복소환 화합물
US20050182061A1 (en) 2003-10-02 2005-08-18 Jeremy Green Phthalimide compounds useful as protein kinase inhibitors
CN102786482A (zh) * 2003-11-21 2012-11-21 阿雷生物药品公司 Akt蛋白激酶抑制剂
US8076338B2 (en) 2004-04-23 2011-12-13 Exelixis, Inc. Kinase modulators and methods of use
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
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
EP1858902A1 (en) 2005-02-24 2007-11-28 Pfizer Products Incorporated Bicyclic heteroaromatic derivatives useful as anticancer agents
US8921376B2 (en) 2005-05-20 2014-12-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
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
EA200800664A1 (ru) 2005-10-13 2009-02-27 Глаксо Груп Лимитед Производные пирролопиримидина в качестве ингибиторов syk
CA2635541A1 (en) 2005-12-28 2007-07-12 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds and their use as mineralocorticoid receptor ligands
WO2007125320A1 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical compounds
RU2008152171A (ru) 2006-07-05 2010-08-10 Интермьюн, Инк. (Us) Новые ингибиторы вирусной репликации гепатита с
ATE493418T1 (de) * 2006-07-06 2011-01-15 Array Biopharma Inc Dihydrofuropyrimidine als akt- proteinkinaseinhibitoren
JP5231411B2 (ja) * 2006-07-06 2013-07-10 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阻害剤としてのジヒドロチエノピリミジン
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
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
TW200808325A (en) 2006-07-06 2008-02-16 Astrazeneca Ab Novel compounds
US7910747B2 (en) 2006-07-06 2011-03-22 Bristol-Myers Squibb Company Phosphonate and phosphinate pyrazolylamide glucokinase activators
GB0613518D0 (en) 2006-07-06 2006-08-16 Phytopharm Plc Chemical compounds
PL2049478T3 (pl) 2006-07-06 2012-09-28 Glaxo Group Ltd Podstawione N-fenylometylo 5-okso-prolino-2-amidy jako antagoniści receptora P2X7 oraz sposoby ich zastosowania
ES2372955T3 (es) 2006-07-06 2012-01-30 Array Biopharma, Inc. Ciclopenta[d]pirimidinas como inhibidores de la proteína cinasa akt.
ES2393932T3 (es) 2006-07-14 2013-01-02 Novartis Ag Derivados de Pirimidina como inhibidores de ALK-5
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
NZ582692A (en) 2007-07-05 2012-05-25 Array Biopharma Inc Pyrimidyl cyclopentanes as akt protein kinase inhibitors
US8377937B2 (en) 2007-07-05 2013-02-19 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors

Also Published As

Publication number Publication date
AU2009204019B2 (en) 2014-02-20
CN101932565A (zh) 2010-12-29
JP2011509306A (ja) 2011-03-24
MX2010007546A (es) 2010-09-30
WO2009089453A1 (en) 2009-07-16
EP2240455B1 (en) 2012-12-26
CO6280510A2 (es) 2011-05-20
NZ586720A (en) 2012-11-30
BRPI0907372A2 (pt) 2015-07-14
HK1149269A1 (en) 2011-09-30
CA2711692A1 (en) 2009-07-16
ECSP10010392A (es) 2010-09-30
ES2401685T3 (es) 2013-04-23
ES2401685T8 (es) 2014-11-06
WO2009089453A9 (en) 2009-11-05
CR11591A (es) 2010-11-30
CN101932565B (zh) 2013-06-12
US8853216B2 (en) 2014-10-07
US20100292244A1 (en) 2010-11-18
MA32343B1 (fr) 2011-06-01
KR20100103865A (ko) 2010-09-28
RU2520735C2 (ru) 2014-06-27
AU2009204019A1 (en) 2009-07-16
IL206607A0 (en) 2010-12-30
UA100544C2 (ru) 2013-01-10
EP2240455A1 (en) 2010-10-20
JP5539225B2 (ja) 2014-07-02
RU2010132912A (ru) 2012-02-20

Similar Documents

Publication Publication Date Title
KR101624752B1 (ko) Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄
KR101624753B1 (ko) Akt 단백질 키나제 저해물질로서의 수산화된 피리미딜 시클로펜탄
KR101578877B1 (ko) AKT 단백질 키나제 억제제로서의 히드록실화 및 메톡실화 시클로펜타[d]피리미딘
US9359340B2 (en) Hydroxylated and methoxylated pyrimidyl cyclopentanes as Akt protein kinase inhibitors
TWI428335B (zh) 作為akt蛋白質激酶抑制劑之嘧啶環戊烷
AU2008272832B2 (en) Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8329701B2 (en) Dihydrofuro pyrimidines as AKT protein kinase inhibitors
US20130065908A1 (en) Dihydrofuro pyrimidines as akt protein kinase inhibitors
US20150051217A1 (en) Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
US20160152574A9 (en) Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
HK1149269B (en) Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
HK1150201B (en) Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
HK1150201A (en) Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

R15-X000 Change to inventor requested

St.27 status event code: A-3-3-R10-R15-oth-X000

R16-X000 Change to inventor recorded

St.27 status event code: A-3-3-R10-R16-oth-X000

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

FPAY Annual fee payment

Payment date: 20190327

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

PN2301 Change of applicant

St.27 status event code: A-5-5-R10-R13-asn-PN2301

St.27 status event code: A-5-5-R10-R11-asn-PN2301

PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20210521

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20210521