AU2008237660B2 - 3-amido-pyrrolo [3, 4-C] pyrazole-5 (1H, 4H, 6H) carbaldehyde derivatives as inhibitors of protein kinase C - Google Patents

3-amido-pyrrolo [3, 4-C] pyrazole-5 (1H, 4H, 6H) carbaldehyde derivatives as inhibitors of protein kinase C Download PDF

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Publication number
AU2008237660B2
AU2008237660B2 AU2008237660A AU2008237660A AU2008237660B2 AU 2008237660 B2 AU2008237660 B2 AU 2008237660B2 AU 2008237660 A AU2008237660 A AU 2008237660A AU 2008237660 A AU2008237660 A AU 2008237660A AU 2008237660 B2 AU2008237660 B2 AU 2008237660B2
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AU
Australia
Prior art keywords
dimethyl
carbonyl
tetrahydropyrrolo
pyrazol
nmr
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Ceased
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AU2008237660A
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AU2008237660A1 (en
Inventor
Iriny Botrous
Yufeng Hong
Hui Li
Kevin Kun-Chin Liu
Seiji Nukui
Min Teng
Eileen Valenzuela Tompkins
Chunfeng Yin
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Pfizer Inc
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Pfizer Inc
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    • 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
    • C07D487/04—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
    • 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
    • A61P25/28—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
    • A61P35/00—Antineoplastic 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
    • 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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • 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)
AU2008237660A 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 Ceased AU2008237660B2 (en)

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

Publications (2)

Publication Number Publication Date
AU2008237660A1 AU2008237660A1 (en) 2008-10-23
AU2008237660B2 true AU2008237660B2 (en) 2011-12-22

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AU2008237660A Ceased AU2008237660B2 (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

Country Status (11)

Country Link
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)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
UA102336C2 (uk) * 2009-11-10 2013-06-25 Пфайзер Інк. N1-ПІРАЗОЛСПІРОКЕТОНИ ЯК ІНГІБІТОРИ АЦЕТИЛ-СоА-КАРБОКСИЛАЗ
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
DK2621493T3 (en) 2010-09-30 2016-10-24 Pfizer N1 PYRAZOLOSPIROKETON-ACETYL-CoA carboxylase INHIBITORS
CN103189377B (zh) 2010-10-29 2015-02-25 辉瑞大药厂 N1/n2-内酰胺乙酰辅酶a羧化酶抑制剂
US8841463B2 (en) 2011-02-11 2014-09-23 Glaxosmithkline Intellectual Property Development Limited Cathepsin C inhibitors
EA022375B1 (ru) 2011-04-22 2015-12-30 Пфайзер Инк. ПРОИЗВОДНЫЕ ПИРАЗОЛОСПИРОКЕТОНОВ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ АЦЕТИЛ-КоА-КАРБОКСИЛАЗ
US8846712B2 (en) 2011-09-12 2014-09-30 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
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
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
US9814716B2 (en) 2014-05-23 2017-11-14 Mingsight Pharmaceuticals, Inc. Treatment of autoimmune disease
US10131679B2 (en) * 2014-10-31 2018-11-20 Ube Industries, Ltd. Substituted dihydropyrrolopyrazole compound
JP2017531684A (ja) * 2014-11-21 2017-10-26 イーライ リリー アンド カンパニー 腎障害の治療のための１，２−ベンゾチアゾール化合物
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
AU2016281225B2 (en) * 2015-06-15 2020-10-15 Ube Corporation Substituted dihydropyrrolopyrazole derivative
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
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
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
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. CYCLIN DEPENDENT KINASE 7 INHIBITORS AND USES THEREOF
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004056827A2 (en) * 2002-12-19 2004-07-08 Pharmacia Italia Spa Substituted pyrrolo-pyrazole derivatives as kinase inhibitors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2416527C (en) 2000-08-10 2009-12-22 Pharmacia Italia S.P.A. Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
BRPI0408486A (pt) * 2003-03-11 2006-04-04 Pharmacia Italia Spa derivados de biciclopirazol ativos como inibidores da cinase, processo para a sua preparação e composições farmacêuticas compreendendo-os
WO2005030776A1 (en) * 2003-09-23 2005-04-07 Vertex Pharmaceuticals Incorporated Pyrazolopyrrole derivatives as protein kinase inhibitors
CA2593428C (en) * 2005-01-10 2012-04-17 Pfizer Inc. Pyrrolopyrazoles, potent kinase inhibitors
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004056827A2 (en) * 2002-12-19 2004-07-08 Pharmacia Italia Spa Substituted pyrrolo-pyrazole derivatives as kinase inhibitors

Also Published As

Publication number Publication date
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
CN101675052A (zh) 2010-03-17
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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