CN101675052A - 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物 - Google Patents

作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物 Download PDF

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CN101675052A
CN101675052A CN200880014779A CN200880014779A CN101675052A CN 101675052 A CN101675052 A CN 101675052A CN 200880014779 A CN200880014779 A CN 200880014779A CN 200880014779 A CN200880014779 A CN 200880014779A CN 101675052 A CN101675052 A CN 101675052A
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dimethyl
compound
pharmaceutically acceptable
tetrahydro
carbonyl
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I·伯特鲁斯
洪玉峰
李辉
K·K-C·刘
贯井齐治
滕敏
E·V·汤普金斯
尹春风
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Pfizer Inc
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    • 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
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    • 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
    • A61P25/28—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
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    • A—HUMAN NECESSITIES
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    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • General Health & Medical Sciences (AREA)
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  • Obesity (AREA)
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  • Oncology (AREA)
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  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN200880014779A 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物 Pending CN101675052A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201410533053.XA CN104370914B (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US91146207P 2007-04-12 2007-04-12
US60/911,462 2007-04-12
US3551908P 2008-03-11 2008-03-11
US61/035,519 2008-03-11
US4011508P 2008-03-27 2008-03-27
US61/040,115 2008-03-27
PCT/IB2008/000862 WO2008125945A2 (en) 2007-04-12 2008-04-10 3-amido-pyrrolo [3, 4-c] pyrazole-5 (1h, 4h, 6h) carbaldehyde derivatives as inhibitors of protein kinase c

Related Child Applications (2)

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CN201410533054.4A Division CN104356136A (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
CN201410533053.XA Division CN104370914B (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物

Publications (1)

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CN101675052A true CN101675052A (zh) 2010-03-17

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CN200880014779A Pending CN101675052A (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
CN201410533053.XA Expired - Fee Related CN104370914B (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
CN201410533054.4A Pending CN104356136A (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物

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CN201410533053.XA Expired - Fee Related CN104370914B (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
CN201410533054.4A Pending CN104356136A (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物

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US (2) US8114871B2 (cg-RX-API-DMAC10.html)
EP (1) EP2195321B1 (cg-RX-API-DMAC10.html)
JP (1) JP5404601B2 (cg-RX-API-DMAC10.html)
KR (1) KR101113387B1 (cg-RX-API-DMAC10.html)
CN (3) CN101675052A (cg-RX-API-DMAC10.html)
AU (1) AU2008237660B2 (cg-RX-API-DMAC10.html)
CA (1) CA2683695C (cg-RX-API-DMAC10.html)
HK (1) HK1207067A1 (cg-RX-API-DMAC10.html)
IL (1) IL201104A (cg-RX-API-DMAC10.html)
MX (1) MX2009010951A (cg-RX-API-DMAC10.html)
WO (1) WO2008125945A2 (cg-RX-API-DMAC10.html)

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CN103491777A (zh) * 2011-02-11 2014-01-01 葛兰素史密斯克莱知识产权发展有限公司 组织蛋白酶c抑制剂
CN105377852A (zh) * 2014-05-23 2016-03-02 深圳明赛瑞霖药业有限公司 自身免疫疾病的治疗
CN107074887A (zh) * 2014-10-31 2017-08-18 宇部兴产株式会社 取代二氢吡咯并吡唑化合物
CN107074842A (zh) * 2014-11-21 2017-08-18 伊莱利利公司 用于治疗肾病的1,2‑苯并噻唑化合物
CN107735401A (zh) * 2015-06-15 2018-02-23 宇部兴产株式会社 取代二氢吡咯并吡唑衍生物

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CN101675052A (zh) 2007-04-12 2010-03-17 辉瑞大药厂 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
JP5435592B2 (ja) 2008-05-28 2014-03-05 ファイザー・インク ピラゾロスピロケトンアセチルＣｏＡカルボキシラーゼ阻害剤
WO2011044264A2 (en) * 2009-10-06 2011-04-14 Afraxis, Inc. Pyrrolopyrazoles for treating cns disorders
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EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
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JP6165733B2 (ja) * 2011-09-16 2017-07-19 ノバルティス アーゲー Ｎ−置換ヘテロシクリルカルボキサミド類
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
JP6106685B2 (ja) 2011-11-17 2017-04-05 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド Ｃ−ｊｕｎ−ｎ−末端キナーゼ（ｊｎｋ）の阻害剤
EP2847191B1 (en) 2012-05-09 2016-06-15 Sanofi Substituted 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US10154988B2 (en) 2012-11-14 2018-12-18 The Johns Hopkins University Methods and compositions for treating schizophrenia
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WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
WO2017044858A2 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
CA3005723A1 (en) 2015-11-20 2017-05-26 Mingsight Pharmaceuticals, Inc. Treatment of autoimmune disease
EP3484477B1 (en) 2016-07-14 2023-09-13 Mingsight Pharmaceuticals, Inc. Treatment of cancer
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JP7530297B2 (ja) 2018-11-14 2024-08-07 Ｕｂｅ株式会社 ジヒドロピロロピラゾール誘導体
CN113164477A (zh) 2018-12-14 2021-07-23 达纳-法伯癌症研究所股份有限公司 C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途
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CN119684220A (zh) * 2024-12-13 2025-03-25 江苏宝众宝达药业股份有限公司 一种(2r,5r)-1,2,5-三甲基哌嗪的制备方法

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Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103491777A (zh) * 2011-02-11 2014-01-01 葛兰素史密斯克莱知识产权发展有限公司 组织蛋白酶c抑制剂
CN103491777B (zh) * 2011-02-11 2015-05-06 葛兰素史密斯克莱知识产权发展有限公司 组织蛋白酶c抑制剂
CN105377852A (zh) * 2014-05-23 2016-03-02 深圳明赛瑞霖药业有限公司 自身免疫疾病的治疗
US9814716B2 (en) 2014-05-23 2017-11-14 Mingsight Pharmaceuticals, Inc. Treatment of autoimmune disease
US9980965B2 (en) 2014-05-23 2018-05-29 Mingsight Pharmaceuticals, Inc. Treatment of autoimmune disease
CN107074887A (zh) * 2014-10-31 2017-08-18 宇部兴产株式会社 取代二氢吡咯并吡唑化合物
CN107074887B (zh) * 2014-10-31 2020-12-22 宇部兴产株式会社 取代二氢吡咯并吡唑化合物
US10968238B2 (en) 2014-10-31 2021-04-06 Ube Industries, Ltd. Substituted dihydropyrrolopyrazole compound
CN107074842A (zh) * 2014-11-21 2017-08-18 伊莱利利公司 用于治疗肾病的1,2‑苯并噻唑化合物
CN107735401A (zh) * 2015-06-15 2018-02-23 宇部兴产株式会社 取代二氢吡咯并吡唑衍生物
CN107735401B (zh) * 2015-06-15 2021-08-31 宇部兴产株式会社 取代二氢吡咯并吡唑衍生物

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AU2008237660B2 (en) 2011-12-22
AU2008237660A1 (en) 2008-10-23
IL201104A (en) 2017-09-28
EP2195321B1 (en) 2016-10-19
JP5404601B2 (ja) 2014-02-05
WO2008125945A2 (en) 2008-10-23
CA2683695A1 (en) 2008-10-23
MX2009010951A (es) 2009-10-29
KR20090130039A (ko) 2009-12-17
WO2008125945A3 (en) 2009-03-12
US20120108588A1 (en) 2012-05-03
US8999981B2 (en) 2015-04-07
CN104370914A (zh) 2015-02-25
CN104356136A (zh) 2015-02-18
EP2195321A2 (en) 2010-06-16
HK1207068A1 (en) 2016-01-22
US20100249128A1 (en) 2010-09-30
JP2010523643A (ja) 2010-07-15
CN104370914B (zh) 2018-09-07
IL201104A0 (en) 2010-05-17
CA2683695C (en) 2013-06-18
KR101113387B1 (ko) 2012-04-23
HK1207067A1 (en) 2016-01-22
US8114871B2 (en) 2012-02-14

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