CN102015708B - 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 - Google Patents

作为akt蛋白激酶抑制剂的嘧啶基环戊烷 Download PDF

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CN102015708B
CN102015708B CN200980108322.5A CN200980108322A CN102015708B CN 102015708 B CN102015708 B CN 102015708B CN 200980108322 A CN200980108322 A CN 200980108322A CN 102015708 B CN102015708 B CN 102015708B
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methyl
dihydro
indoline
pyrimidin
spiro
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CN102015708A (zh
Inventor
安娜·班卡
约瑟夫·R·本西克
詹姆斯·F·布拉克
方建朝
马丁·F·亨特曼
伊恩·S·米切尔
道格拉斯·M·萨蒙德
托尼·P·唐
伊莱·M·华莱士
徐睿
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Array Biopharma Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
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  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
CN200980108322.5A 2008-01-09 2009-01-09 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 Active CN102015708B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US2012508P 2008-01-09 2008-01-09
US61/020,125 2008-01-09
PCT/US2009/030603 WO2009089454A1 (en) 2008-01-09 2009-01-09 Pyrimidyl cyclopentanes as akt protein kinase inhibitors

Publications (2)

Publication Number Publication Date
CN102015708A CN102015708A (zh) 2011-04-13
CN102015708B true CN102015708B (zh) 2014-03-26

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CN200980108322.5A Active CN102015708B (zh) 2008-01-09 2009-01-09 作为akt蛋白激酶抑制剂的嘧啶基环戊烷

Country Status (11)

Country Link
US (2) US8324221B2 (enExample)
EP (1) EP2240483B8 (enExample)
JP (1) JP5512545B2 (enExample)
CN (1) CN102015708B (enExample)
AR (1) AR070136A1 (enExample)
CA (1) CA2714888C (enExample)
CL (1) CL2009000035A1 (enExample)
ES (1) ES2403284T3 (enExample)
PE (1) PE20091315A1 (enExample)
TW (1) TW200940542A (enExample)
WO (1) WO2009089454A1 (enExample)

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EP2285808B1 (en) 2008-04-29 2013-11-20 Novartis AG Spiro-indole derivatives for the treatment of parasitic diseases
EP2393827B1 (en) 2009-02-05 2015-10-07 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
TWI466885B (zh) 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
US8921576B2 (en) 2011-10-19 2014-12-30 Kowa Company, Ltd. Spiroindoline compound, and medicinal agent comprising same
PL2841075T3 (pl) 2012-04-26 2020-09-21 The General Hospital Corporation Środki i sposoby leczenia i zapobiegania rogowaceniu łojotokowemu
CA2904170A1 (en) 2013-03-14 2014-09-25 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
WO2014186663A2 (en) * 2013-05-17 2014-11-20 The General Hospital Corporation Methods for detecting and treating variants of seborrheic keratoses
KR20160058774A (ko) 2013-08-12 2016-05-25 토카이 파마슈티컬, 아이엔씨. 안드로겐-표적 치료제를 이용하는 종양 질환 치료를 위한 바이오마커
WO2016126726A1 (en) 2015-02-02 2016-08-11 Forma Therapeutics, Inc. Bicyclic [4,6,0] hydroxamic acids as hdac6 inhibitors
TW201629026A (zh) 2015-02-02 2016-08-16 佛瑪治療公司 作為ｈｄａｃ抑制劑的３－烷基雙環［４，５，０］異羥肟酸
US9745253B2 (en) 2015-03-13 2017-08-29 Forma Therapeutics, Inc. Alpha-cinnamide compounds and compositions as HDAC8 inhibitors
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TWI830733B (zh) * 2018-05-11 2024-02-01 中國大陸商迪哲（江蘇）醫藥有限公司 環戊烷化合物
CN114981298B (zh) 2019-12-12 2024-08-20 听治疗有限责任公司 用于预防和治疗听力损失的组合物和方法
WO2022109360A1 (en) 2020-11-23 2022-05-27 Enanta Pharmaceuticals, Inc. Novel spiropyrrolidine derived antiviral agents
US12540141B2 (en) 2020-11-23 2026-02-03 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
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CN114751852B (zh) * 2022-05-23 2023-09-15 山西库邦生物医药科技有限公司 一种西咯多辛关键中间体的制备方法
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Also Published As

Publication number Publication date
EP2240483B1 (en) 2013-02-27
CN102015708A (zh) 2011-04-13
EP2240483A1 (en) 2010-10-20
ES2403284T3 (es) 2013-05-17
CL2009000035A1 (es) 2009-11-27
TW200940542A (en) 2009-10-01
AR070136A1 (es) 2010-03-17
JP5512545B2 (ja) 2014-06-04
PE20091315A1 (es) 2009-09-21
WO2009089454A1 (en) 2009-07-16
US20110053959A1 (en) 2011-03-03
HK1149270A1 (en) 2011-09-30
US9346805B2 (en) 2016-05-24
US8324221B2 (en) 2012-12-04
EP2240483B8 (en) 2013-04-03
US20130072500A1 (en) 2013-03-21
CA2714888A1 (en) 2009-07-16
CA2714888C (en) 2017-03-14
JP2011509307A (ja) 2011-03-24

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