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

Ａｋｔ 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄 Download PDF

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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
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mmol
compound
compounds
akt
tert
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KR20100103865A (ko
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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
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어레이 바이오파마 인크.
제넨테크, 인크.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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

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  • Ophthalmology & Optometry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hospice & Palliative Care (AREA)
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KR1020107017573A 2008-01-09 2009-01-09 Ａｋｔ 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄 Expired - Fee Related KR101624752B1 (ko)

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US2008708P 2008-01-09 2008-01-09
US61/020,087 2008-01-09

Publications (2)

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

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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
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
WO2009006567A2 (en) * 2007-07-05 2009-01-08 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
EP2242757B1 (en) 2008-01-09 2012-08-01 Array Biopharma, Inc. Pyrazolopyridines as kinase inhibitors
US8329709B2 (en) 2008-01-09 2012-12-11 Genentech, Inc. 5H-cyclopenta[D]pyrimidines as AKT protein kinase inhibitors
CA2873661C (en) * 2012-05-17 2020-07-21 Genentech, Inc. Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof
CN112898210B (zh) * 2013-11-15 2025-02-21 豪夫迈·罗氏有限公司 用于制备嘧啶基环戊烷化合物的方法
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
US4749704A (en) 1985-03-07 1988-06-07 Sankyo Company Limited Cyclopenta[d]pyrimidine derivatives and use as antidepressants
WO1990007926A1 (en) 1989-01-20 1990-07-26 Pfizer Inc. 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines
PT664291E (pt) 1992-10-05 2000-11-30 Ube Industries Composto de pirimidina
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
CN1102144C (zh) 1994-08-13 2003-02-26 株式会社柳韩洋行 新的嘧啶衍生物及其制备方法
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
CA2290506C (en) 1997-07-01 2005-12-27 Warner-Lambert Company 4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as mek inhibitors
DE69836378T2 (de) 1997-07-01 2007-10-11 Warner-Lambert Co. Llc Benzoesäure- und Benzamid-Derivate von Anthranilsäure und ihre Anwendung als MEK-Inhibitoren
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
CA2326324C (en) 1998-03-31 2010-05-11 Kyowa Hakko Kogyo Co., Ltd. Nitrogen-containing heterocyclic compound
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
BR9916785A (pt) 1999-01-07 2001-10-23 Warner Lambert Co Tratamento de asma com inibidores mek
DE69926914T2 (de) 1999-01-13 2006-06-29 Warner-Lambert Co. Llc 1-heterozyklus-substituierte diarylaminen
YU49401A (sh) 1999-01-13 2004-07-15 Warner-Lambert Company Benzoheterocikli i njihova upotreba kao inhibitori mek
ATE309205T1 (de) 1999-01-13 2005-11-15 Warner Lambert Co Benzenesulfonamid-derivative und ihre verwendung als mek-inhibitoren
BR9916894A (pt) 1999-01-13 2001-11-20 Warner Lambert Co ácidos sulfohidroxâmicos e sulfohidroxamatos eseu uso como inibidores de mek
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
AU2483400A (en) 1999-01-13 2000-08-01 Warner-Lambert Company 4'heteroaryl diarylamines
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
ES2208364T3 (es) 1999-07-16 2004-06-16 Warner-Lambert Company Llc Procedimiento para tratar dolor cronico usando inhibidores de mek.
IL147150A0 (en) 1999-07-16 2002-08-14 Warner Lambert Co Method for treating chronic pain using mek inhibitors
CA2377100A1 (en) 1999-07-16 2001-01-25 Warner-Lambert Company Method for treating chronic pain using mek inhibitors
PL352684A1 (pl) 1999-07-16 2003-09-08 Warner-Lambert Company Sposób leczenia chronicznego bólu z użyciem inhibitorów MEK
CA2403017A1 (en) 2000-03-15 2001-09-20 Warner-Lambert Company 5-amide substituted diarylamines as mex inhibitors
NZ524120A (en) 2000-07-19 2005-08-26 Warner Lambert Co Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids
BR0113520A (pt) 2000-08-25 2003-06-24 Warner Lambert Co Processo de preparação de ácidos n-aril-antranìlicos e seus derivados
WO2002044166A1 (en) 2000-11-02 2002-06-06 Astrazeneca Ab Substituted quinolines as antitumor agents
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
ES2301633T3 (es) 2001-04-30 2008-07-01 Glaxo Group Limited Pirimidinas condensadas como antagonistas del factor de liberacion de corticotropina (crf).
WO2003022214A2 (en) 2001-09-06 2003-03-20 Millennium Pharmaceuticals, Inc. Piperazine and homopiperazine 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
PL401638A1 (pl) 2002-03-13 2013-05-27 Array Biopharma Inc. N3 alkilowane pochodne benzimidazolu jako inhibitory MEK
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
CA2481229C (en) 2002-04-08 2010-09-21 Merck & Co., Inc. Substituted pyrazine inhibitors of akt
US7273869B2 (en) 2002-04-08 2007-09-25 Merck & Co., Inc. Inhibitors of Akt activity
AU2003223467B2 (en) 2002-04-08 2007-10-04 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
WO2003086403A1 (en) 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
EP1503761A1 (en) 2002-05-10 2005-02-09 Neurocrine Biosciences, Inc. Substituted piperazines as melanocortin receptor ligands
CA2501365C (en) 2002-10-30 2011-05-31 Merck & Co., Inc. Inhibitors of akt activity
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
EP1620095A4 (en) 2003-04-24 2009-04-01 Merck & Co Inc HEMMER OF ACT ACTIVITY
EP1646615B1 (en) 2003-06-06 2009-08-26 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
ATE374190T1 (de) 2003-08-12 2007-10-15 Hoffmann La Roche Tetrahydrochinazolinderivate als cfr-antagonisten
EP1666468A4 (en) 2003-09-09 2007-03-21 Ono Pharmaceutical Co CRF ANTAGONISTS AND HETEROBICYCLIC COMPOUNDS
WO2005039564A1 (en) 2003-10-02 2005-05-06 Vertex Pharmaceuticals Incorporated Phthalimide compounds useful as protein kinase inhibitors
NZ547327A (en) * 2003-11-21 2009-08-28 Array Biopharma Inc AKT protein kinase inhibitors
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
JP5274842B2 (ja) 2004-12-28 2013-08-28 エグゼリクシス， インコーポレイテッド 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター（ｐ７０Ｓ６Ｋ、Ａｋｔ−１およびＡｋｔ−２）としての［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジンまたは［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジン化合物
EP1858902A1 (en) 2005-02-24 2007-11-28 Pfizer Products Incorporated Bicyclic heteroaromatic derivatives useful as anticancer agents
NZ564065A (en) 2005-05-20 2011-03-31 Vertex Pharma 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
BRPI0617241A2 (pt) 2005-10-13 2016-11-08 Glaxo Group Ltd composto ou um sal ou solvato do mesmo, composição farmacêutica, método para tratar uma doença ou condição mediada por atividade syk inadequada em um mamífero, e, uso de um composto ou um sal ou solvato farmaceuticamente aceitável do mesmo
PE20071164A1 (es) 2005-12-28 2008-01-11 Takeda Pharmaceutical Compuestos heterociclico fusionado como antagonista del receptor mineralocorticoide
US20090124610A1 (en) 2006-04-25 2009-05-14 Gordon Saxty Pharmaceutical compounds
RU2008152171A (ru) 2006-07-05 2010-08-10 Интермьюн, Инк. (Us) Новые ингибиторы вирусной репликации гепатита с
CA2656618C (en) 2006-07-06 2014-08-26 Array Biopharma Inc. Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
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
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
ATE532789T1 (de) 2006-07-06 2011-11-15 Array Biopharma Inc Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren
TW200808325A (en) 2006-07-06 2008-02-16 Astrazeneca Ab Novel compounds
GB0613518D0 (en) 2006-07-06 2006-08-16 Phytopharm Plc Chemical compounds
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
SI2049478T1 (sl) 2006-07-06 2012-08-31 Glaxo Group Ltd Substituirani N-fenilmetil-5-okso-prolin-2-amidi kot antagonisti receptorja P2X7 in postopki za njihovo uporabo
AR061974A1 (es) 2006-07-14 2008-08-10 Novartis Ag Derivados de pirimidina como inhibidores de alk, composiciones farmaceuticas y procesos de obtencion
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
SI2173723T1 (sl) 2007-07-05 2011-12-30 Array Biopharma Inc Pirimidil ciklopentani kot inhibitorji AKT-protein-kinaze
WO2009006567A2 (en) * 2007-07-05 2009-01-08 Array Biopharma Inc. Pyrimidyl cyclopentanes as akt protein kinase inhibitors

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

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