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 PDFInfo
- 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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- Australia
- Prior art keywords
- dimethyl
- carbonyl
- tetrahydropyrrolo
- pyrazol
- nmr
- 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.)
- Ceased
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- 102000003923 Protein Kinase C Human genes 0.000 title description 32
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- 125000005958 tetrahydrothienyl group Chemical group 0.000 description 1
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- 125000005505 thiomorpholino group Chemical group 0.000 description 1
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- 125000005503 thioxanyl group Chemical group 0.000 description 1
- 238000003354 tissue distribution assay Methods 0.000 description 1
- 229960005371 tolbutamide Drugs 0.000 description 1
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- 125000004306 triazinyl group Chemical group 0.000 description 1
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- 238000000825 ultraviolet detection Methods 0.000 description 1
- 238000011144 upstream manufacturing Methods 0.000 description 1
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Classifications
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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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
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- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
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- Hospice & Palliative Care (AREA)
- Psychiatry (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)
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)
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| AU2008237660A1 AU2008237660A1 (en) | 2008-10-23 |
| AU2008237660B2 true AU2008237660B2 (en) | 2011-12-22 |
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| Country | Link |
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| US (2) | US8114871B2 (enExample) |
| EP (1) | EP2195321B1 (enExample) |
| JP (1) | JP5404601B2 (enExample) |
| KR (1) | KR101113387B1 (enExample) |
| CN (3) | CN101675052A (enExample) |
| AU (1) | AU2008237660B2 (enExample) |
| CA (1) | CA2683695C (enExample) |
| HK (1) | HK1207067A1 (enExample) |
| IL (1) | IL201104A (enExample) |
| MX (1) | MX2009010951A (enExample) |
| WO (1) | WO2008125945A2 (enExample) |
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| WO2008125945A2 (en) | 2007-04-12 | 2008-10-23 | Pfizer Inc. | 3-amido-pyrrolo [3, 4-c] pyrazole-5 (1h, 4h, 6h) carbaldehyde derivatives as inhibitors of protein kinase c |
| US8318762B2 (en) | 2008-05-28 | 2012-11-27 | Pfizer Inc. | Pyrazolospiroketone acetyl-CoA carboxylase inhibitors |
| EP2485727A4 (en) * | 2009-10-06 | 2013-05-01 | Afraxis Inc | PYRROLOPYRAZOLE FOR THE TREATMENT OF CNS DISEASES |
| CU24077B1 (es) * | 2009-11-10 | 2015-03-30 | Pfizer | DERIVADOS DE N1-PIRAZOLOESPIROCETONA ÚTILES COMO INHIBIDORES DE ACETIL-CoA CARBOXILASA |
| EP2519517B1 (en) | 2009-12-29 | 2015-03-25 | 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 |
| US8933024B2 (en) | 2010-06-18 | 2015-01-13 | Sanofi | Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases |
| 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 |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| 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 |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| HRP20161178T1 (hr) | 2010-09-30 | 2016-11-04 | Pfizer Inc. | N1-PIRAZOLOSPIROKETONSKI INHIBITORI ACETIL-CoA-KARBOKSILAZE |
| CA2815169C (en) | 2010-10-29 | 2015-10-06 | Pfizer Inc. | N1/n2-lactam acetyl-coa carboxylase inhibitors |
| EA023168B1 (ru) | 2011-02-11 | 2016-04-29 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Ингибитор катепсина с |
| ME02312B (me) | 2011-04-22 | 2016-06-20 | Pfizer | DERIVATI PIRAZOLOSPIROKETONA, NAMIJENJENI UPOTREBI KAO INHIBITORI ACETIL-CoA-KARBOKSILAZE |
| 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 |
| 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 |
| 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 |
| EP2755652B1 (en) * | 2011-09-16 | 2021-06-02 | Novartis AG | N-substituted heterocyclyl carboxamides |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | 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 |
| WO2013167403A1 (en) | 2012-05-09 | 2013-11-14 | Sanofi | Substituted 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors |
| US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| JP6440625B2 (ja) | 2012-11-14 | 2018-12-19 | ザ・ジョンズ・ホプキンス・ユニバーシティー | 精神分裂病を処置するための方法および組成物 |
| AU2014337044A1 (en) | 2013-10-18 | 2016-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
| AU2014337122B2 (en) | 2013-10-18 | 2019-01-03 | Dana-Farber Cancer Institute, Inc. | Heteroaromatic compounds useful for the treatment of proliferative diseases |
| WO2015179847A1 (en) * | 2014-05-23 | 2015-11-26 | Mingsight Pharmaceuticals, Inc. | Treatment of autoimmune disease |
| EP3214086B1 (en) * | 2014-10-31 | 2021-09-22 | Ube Industries, Ltd. | Substituted dihydropyrrolopyrazole compound |
| US20170246166A1 (en) * | 2014-11-21 | 2017-08-31 | Eli Lilly And Company | 1,2-benzothiazole compounds for the treatment of kidney disorders |
| JP6854762B2 (ja) * | 2014-12-23 | 2021-04-07 | 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 | サイクリン依存性キナーゼ７（ｃｄｋ７）の阻害剤 |
| AU2016243529B2 (en) | 2015-03-27 | 2021-03-25 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| KR102588426B1 (ko) | 2015-06-15 | 2023-10-13 | 유비이 가부시키가이샤 | 치환 디히드로피롤로피라졸 유도체 |
| JP7028766B2 (ja) | 2015-09-09 | 2022-03-02 | 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 | サイクリン依存性キナーゼの阻害剤 |
| SG11201804210XA (en) | 2015-11-20 | 2018-06-28 | Mingsight Pharmaceuticals Inc | Treatment of autoimmune disease |
| CN109715166A (zh) | 2016-07-14 | 2019-05-03 | 深圳明赛瑞霖药业有限公司 | 癌症的治疗 |
| EP3810132A4 (en) | 2018-06-25 | 2022-06-22 | Dana-Farber Cancer Institute, Inc. | TAIRE FAMILY KINASE INHIBITORS AND RELATED USES |
| US12304913B2 (en) | 2018-11-14 | 2025-05-20 | Ube Industries, Ltd. | Dihydropyrrolopyrazole derivative |
| AU2019413694B2 (en) | 2018-12-28 | 2025-03-20 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 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)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2004056827A2 (en) * | 2002-12-19 | 2004-07-08 | Pharmacia Italia Spa | Substituted pyrrolo-pyrazole derivatives as kinase inhibitors |
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| CN102060857A (zh) * | 2000-08-10 | 2011-05-18 | 辉瑞意大利有限公司 | 具有激酶抑制剂活性的二环吡唑类、其制备方法和包含它们的药物组合物 |
| 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 |
| CA2539549A1 (en) * | 2003-09-23 | 2005-04-07 | Vertex Pharmaceuticals Incorporated | Pyrazolopyrrole derivatives as protein kinase inhibitors |
| KR100919343B1 (ko) | 2005-01-10 | 2009-09-25 | 화이자 인코포레이티드 | 키네이스 억제제로서 피롤로피라졸 |
| WO2008125945A2 (en) | 2007-04-12 | 2008-10-23 | Pfizer Inc. | 3-amido-pyrrolo [3, 4-c] pyrazole-5 (1h, 4h, 6h) carbaldehyde derivatives as inhibitors of protein kinase c |
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| WO2004056827A2 (en) * | 2002-12-19 | 2004-07-08 | Pharmacia Italia Spa | Substituted pyrrolo-pyrazole derivatives as kinase inhibitors |
Also Published As
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| CN101675052A (zh) | 2010-03-17 |
| US8114871B2 (en) | 2012-02-14 |
| JP5404601B2 (ja) | 2014-02-05 |
| CN104370914B (zh) | 2018-09-07 |
| IL201104A0 (en) | 2010-05-17 |
| WO2008125945A3 (en) | 2009-03-12 |
| US8999981B2 (en) | 2015-04-07 |
| WO2008125945A2 (en) | 2008-10-23 |
| EP2195321B1 (en) | 2016-10-19 |
| CN104356136A (zh) | 2015-02-18 |
| AU2008237660A1 (en) | 2008-10-23 |
| HK1207068A1 (en) | 2016-01-22 |
| KR101113387B1 (ko) | 2012-04-23 |
| US20120108588A1 (en) | 2012-05-03 |
| IL201104A (en) | 2017-09-28 |
| US20100249128A1 (en) | 2010-09-30 |
| CA2683695A1 (en) | 2008-10-23 |
| HK1207067A1 (en) | 2016-01-22 |
| EP2195321A2 (en) | 2010-06-16 |
| JP2010523643A (ja) | 2010-07-15 |
| KR20090130039A (ko) | 2009-12-17 |
| MX2009010951A (es) | 2009-10-29 |
| CA2683695C (en) | 2013-06-18 |
| CN104370914A (zh) | 2015-02-25 |
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