CN101511842B - 作为akt蛋白激酶抑制剂的二氢呋喃并嘧啶 - Google Patents

作为akt蛋白激酶抑制剂的二氢呋喃并嘧啶 Download PDF

Info

Publication number
CN101511842B
CN101511842B CN2007800330476A CN200780033047A CN101511842B CN 101511842 B CN101511842 B CN 101511842B CN 2007800330476 A CN2007800330476 A CN 2007800330476A CN 200780033047 A CN200780033047 A CN 200780033047A CN 101511842 B CN101511842 B CN 101511842B
Authority
CN
China
Prior art keywords
compound
methyl
dihydrofuro
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.)
Expired - Fee Related
Application number
CN2007800330476A
Other languages
English (en)
Chinese (zh)
Other versions
CN101511842A (zh
Inventor
伊恩·S·米切尔
詹姆斯·F·布莱克
徐睿
尼古拉斯·C·卡兰
校登明
基思·L·斯潘塞
约瑟夫·R·本克西克
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.)
Array Biopharma Inc
Original Assignee
Array Biopharma 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 Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of CN101511842A publication Critical patent/CN101511842A/zh
Application granted granted Critical
Publication of CN101511842B publication Critical patent/CN101511842B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed 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
    • 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
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychology (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
CN2007800330476A 2006-07-06 2007-07-05 作为akt蛋白激酶抑制剂的二氢呋喃并嘧啶 Expired - Fee Related CN101511842B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US81880706P 2006-07-06 2006-07-06
US60/818,807 2006-07-06
PCT/US2007/072863 WO2008006025A1 (en) 2006-07-06 2007-07-05 Dihydrofuro pyrimidines as akt protein kinase inhibitors

Publications (2)

Publication Number Publication Date
CN101511842A CN101511842A (zh) 2009-08-19
CN101511842B true CN101511842B (zh) 2012-10-31

Family

ID=38603508

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2007800330476A Expired - Fee Related CN101511842B (zh) 2006-07-06 2007-07-05 作为akt蛋白激酶抑制剂的二氢呋喃并嘧啶

Country Status (8)

Country Link
US (1) US8329701B2 (https=)
EP (1) EP2049546B1 (https=)
JP (1) JP5231410B2 (https=)
CN (1) CN101511842B (https=)
AT (1) ATE493418T1 (https=)
CA (1) CA2656566C (https=)
DE (1) DE602007011628D1 (https=)
WO (1) WO2008006025A1 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
ATE532789T1 (de) 2006-07-06 2011-11-15 Array Biopharma Inc Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren
US8846683B2 (en) 2007-07-05 2014-09-30 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
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
CA2711614A1 (en) 2008-01-08 2009-07-16 Array Biopharma Inc. Pyrrolopyridines as kinase inhibitors
CA2711741A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. Pyrazolopyridines as kinase inhibitors
EP2240455B1 (en) 2008-01-09 2012-12-26 Array Biopharma, Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
CN101970415A (zh) 2008-01-09 2011-02-09 阵列生物制药公司 作为AKT蛋白激酶抑制剂的5H-环戊二烯并[d]嘧啶
CA2729045A1 (en) 2008-07-31 2010-02-04 Philippe Bergeron Pyrimidine compounds, compositions and methods of use
EP2499143B1 (en) 2009-11-12 2016-03-16 F.Hoffmann-La Roche Ag N7-substituted purine and pyrazolopyrimidine compounds, compositions and methods of use
JP5579864B2 (ja) 2009-11-12 2014-08-27 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト N−9−置換プリン化合物、組成物及び使用の方法
CN112472699A (zh) 2013-07-26 2021-03-12 种族肿瘤学公司 改善比生群及衍生物的治疗益处的组合方法
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
AU2020214258B2 (en) 2019-01-29 2025-08-28 Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. AKT inhibitor
CN115485276B (zh) * 2020-05-15 2024-05-31 南京正大天晴制药有限公司 氘代akt激酶抑制剂
US20230321108A1 (en) * 2020-07-22 2023-10-12 Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. Unit dosage composition of akt inhibitor
US20230286979A1 (en) 2020-07-22 2023-09-14 Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. Salt of dihydropyrido[2,3-d]pyrimidinone derivative, preparation method therefor, and use thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004041162A2 (en) * 2002-10-30 2004-05-21 Merck & Co., Inc. Inhibitors of akt activity
WO2006027346A2 (en) * 2004-09-06 2006-03-16 Altana Pharma Ag Novel pyrazolopyrimidines

Family Cites Families (85)

* 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
WO1987004928A1 (fr) * 1986-02-24 1987-08-27 Mitsui Petrochemical Industries, Ltd. Agents therapeutiques de la neuropathie
MX19185A (es) 1989-01-20 1993-12-01 Pfizer Procedimiento para preparar 3-(1,2,5,6-tretrahidropiridil)-pirrolopiridinas.
KR100262254B1 (ko) 1992-10-05 2000-07-15 나카히로 마오미 피리미딘 화합물
US5750545A (en) 1993-07-23 1998-05-12 The Green Cross Corporation Triazole derivative and pharmaceutical use thereof
GB9416189D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
JP2896532B2 (ja) 1994-08-13 1999-05-31 ユーハン コーポレーション 新規なピリミジン誘導体およびその製造方法
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
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
BR9810385A (pt) 1997-07-01 2000-09-05 Warner Lambert Co Derivados de ácido benzóico 2-(4-bromo ou 4-iodo fenilamino) e sua utilização como inibidores de mek
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
NZ501276A (en) 1997-07-01 2000-10-27 Warner Lambert Co 4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors in treating proliferative disorders
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
EP1067123B1 (en) 1998-03-31 2011-01-19 Kyowa Hakko Kirin 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
WO2000040237A1 (en) 1999-01-07 2000-07-13 Warner-Lambert Company Antiviral method using mek inhibitors
EP1140062B1 (en) 1999-01-07 2005-04-06 Warner-Lambert Company LLC Treatment of asthma with 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
ATE311363T1 (de) 1999-01-13 2005-12-15 Warner Lambert Co Sulfohydroxamsäure and sulfohydroxamate und ihre verwendung als mek-inhibitoren
CA2349832A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Benzenesulfonamide derivatives and their use as mek inhibitors
CA2349180A1 (en) 1999-01-13 2000-07-20 Stephen Douglas Barrett Anthranilic acid derivatives
DE69926914T2 (de) 1999-01-13 2006-06-29 Warner-Lambert Co. Llc 1-heterozyklus-substituierte diarylaminen
IL144214A0 (en) 1999-01-13 2002-05-23 Warner Lambert Co Benzoheterocycles and their use as mek inhibitors
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.
HUP0202381A3 (en) 1999-07-16 2004-12-28 Warner Lambert Co Method for treating chronic pain using mek inhibitors
KR20020012315A (ko) 1999-07-16 2002-02-15 로즈 암스트롱, 크리스틴 에이. 트러트웨인 Mek 저해제를 사용한 만성 통증의 치료 방법
PL352835A1 (en) 1999-07-16 2003-09-08 Warner-Lambert Company Method for treating chronic pain using mek inhibitors
MXPA02008103A (es) 2000-03-15 2002-11-29 Warner Lambert Co Diarilaminas sustituidas con 5-amida como inhibidores mek.
JP3811775B2 (ja) 2000-07-19 2006-08-23 ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー 4−ヨードフェニルアミノベンズヒドロキサム酸の酸素化エステル
SK2072003A3 (en) 2000-08-25 2004-01-08 Warner Lambert Co Process for making N-aryl-anthranilic acids and their derivatives
US7067532B2 (en) 2000-11-02 2006-06-27 Astrazeneca Substituted quinolines as antitumor agents
CA2438272A1 (en) * 2001-03-02 2002-10-10 John Macor Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
DE60225127T2 (de) 2001-04-30 2009-02-19 Glaxo Group Ltd., Greenford Kondensierte pyrimidine als antagonisten des corticotropin releasing factor (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
KR100984595B1 (ko) 2002-03-13 2010-09-30 어레이 바이오파마 인크. Mek 억제제로서의 n3 알킬화 벤즈이미다졸 유도체
EP1482944A4 (en) 2002-03-13 2006-04-19 Array Biopharma Inc NZ ALKYL BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
US7273869B2 (en) 2002-04-08 2007-09-25 Merck & Co., Inc. Inhibitors of Akt activity
JP4394959B2 (ja) 2002-04-08 2010-01-06 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
EP1496906A4 (en) 2002-04-08 2006-05-03 Merck & Co Inc HEMMER OF ACT ACTIVITY
US7223738B2 (en) 2002-04-08 2007-05-29 Merck & Co., Inc. Inhibitors of Akt activity
AU2003230367A1 (en) 2002-05-10 2003-11-11 Neurocrine Biosciences, Inc. Substituted piperazine as melanocortin receptors ligands
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
EP1646615B1 (en) 2003-06-06 2009-08-26 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
CN1894222A (zh) 2003-08-05 2007-01-10 沃泰克斯药物股份有限公司 作为电压门控离子通道抑制剂的稠合嘧啶化合物
ES2293317T3 (es) 2003-08-12 2008-03-16 F. Hoffmann-La Roche Ag Derivados de tetrahidroquinazolina com antagonistas de cfr.
AU2004272437A1 (en) 2003-09-09 2005-03-24 Ono Pharmaceutical Co., Ltd. CRF antagonists and heterobicyclic compounds
WO2005039564A1 (en) 2003-10-02 2005-05-06 Vertex Pharmaceuticals Incorporated Phthalimide compounds useful as protein kinase inhibitors
NZ590160A (en) 2003-11-21 2012-07-27 Array Biopharma Inc AKT protein kinase inhibitors
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
US20060025074A1 (en) 2004-07-30 2006-02-02 Chih-Ming Liang Bluetooth-based headset
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
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
US20090111805A1 (en) 2005-02-24 2009-04-30 Pfizer Inc. Bicyclic heteroaromatic derivatives useful as anticancer agents
EP2354140A1 (en) 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
UY29610A1 (es) 2005-06-21 2007-01-31 Cancer Rec Tech Ltd Aril-alquilaminas y heteroaril-alquilaminas como inhibidores de la quinasa proteínica
KR100670171B1 (ko) * 2005-06-25 2007-01-17 한국과학기술연구원 신규 퓨로[2,3-d]피리미딘계 Akt1 키나아제 저해제,그 제조 중간체 및 이들의 제조 방법
JP2009511528A (ja) 2005-10-13 2009-03-19 グラクソ グループ リミテッド Syk阻害物質としてのピロロピリミジン誘導体群
CA2635541A1 (en) 2005-12-28 2007-07-12 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds and their use as mineralocorticoid receptor ligands
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
KR20090024834A (ko) 2006-07-05 2009-03-09 인터뮨, 인크. C형 간염 바이러스 복제의 신규 억제제
ATE523499T1 (de) 2006-07-06 2011-09-15 Array Biopharma Inc Cyclopenta [d]-pyrimidine als akt-proteinkinasehemmer
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
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
MX2009000117A (es) 2006-07-06 2009-01-23 Glaxo Group Ltd N-fenilmetil-5-oxo-prolin-2-amidas sustituidas como antagonistas de receptores p2x7 y sus metodos de uso.
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004041162A2 (en) * 2002-10-30 2004-05-21 Merck & Co., Inc. Inhibitors of akt activity
WO2006027346A2 (en) * 2004-09-06 2006-03-16 Altana Pharma Ag Novel pyrazolopyrimidines

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Gui-Dong Zhu, et al..Discovery and SAR of oxindole–pyridine-based protein kinase B/Akt inhibitors for treating cancers.《Bioorganic & Medicinal Chemistry Letters》.2006,第16卷3424-3429. *
Sheela A. Thomas, et al..Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.《Bioorganic & Medicinal Chemistry Letters》.2006,第16卷3740-3744. *

Also Published As

Publication number Publication date
EP2049546A1 (en) 2009-04-22
US8329701B2 (en) 2012-12-11
JP2009542720A (ja) 2009-12-03
DE602007011628D1 (de) 2011-02-10
WO2008006025A1 (en) 2008-01-10
CA2656566C (en) 2014-06-17
JP5231410B2 (ja) 2013-07-10
US20110269773A1 (en) 2011-11-03
EP2049546B1 (en) 2010-12-29
ATE493418T1 (de) 2011-01-15
CA2656566A1 (en) 2008-01-10
CN101511842A (zh) 2009-08-19

Similar Documents

Publication Publication Date Title
CN101511842B (zh) 作为akt蛋白激酶抑制剂的二氢呋喃并嘧啶
CN101578273B (zh) 作为akt蛋白激酶抑制剂的羟基化和甲氧基化的环戊二烯并[d]嘧啶
TWI428335B (zh) 作為akt蛋白質激酶抑制劑之嘧啶環戊烷
JP5231411B2 (ja) 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
US20220226326A1 (en) Hydroxylated and methoxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
US20130065908A1 (en) Dihydrofuro pyrimidines as akt protein kinase inhibitors
HK1176072A (en) Hydroxylated and methoxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors
HK1185873A (en) Cyclopenta [d] pyrimidines as akt protein kinase inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20121031

Termination date: 20200705

CF01 Termination of patent right due to non-payment of annual fee