MX2010005950A - 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors. - Google Patents
2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors.Info
- Publication number
- MX2010005950A MX2010005950A MX2010005950A MX2010005950A MX2010005950A MX 2010005950 A MX2010005950 A MX 2010005950A MX 2010005950 A MX2010005950 A MX 2010005950A MX 2010005950 A MX2010005950 A MX 2010005950A MX 2010005950 A MX2010005950 A MX 2010005950A
- Authority
- MX
- Mexico
- Prior art keywords
- inhibitors
- methods
- fluoropyrazolo
- pyrimidines
- protein kinase
- Prior art date
Links
- NGNRRQCRTQANMW-UHFFFAOYSA-N 2-fluoropyrazolo[1,5-a]pyrimidine Chemical class FC1=NN2C=CC=NC2=C1 NGNRRQCRTQANMW-UHFFFAOYSA-N 0.000 title 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 239000003909 protein kinase inhibitor Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 abstract 7
- 201000010099 disease Diseases 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 239000000203 mixture Substances 0.000 abstract 3
- 101150050673 CHK1 gene Proteins 0.000 abstract 2
- 101100439046 Caenorhabditis elegans cdk-2 gene Proteins 0.000 abstract 2
- 208000024891 symptom Diseases 0.000 abstract 2
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- LDIJKUBTLZTFRG-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine Chemical compound N1=CC=CN2N=CC=C21 LDIJKUBTLZTFRG-UHFFFAOYSA-N 0.000 abstract 1
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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- 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
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- 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
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Pyrazolo[1,5-a]pyrimidine-based inhibitors of various kinase, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions that contain such inhibitors are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 or CHK-1 inhibitor compounds, methods of inhibiting CDK-2 or CHK-1, and methods for treating disease or disease symptoms.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US99073607P | 2007-11-28 | 2007-11-28 | |
| PCT/US2008/084643 WO2009070567A1 (en) | 2007-11-28 | 2008-11-25 | 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2010005950A true MX2010005950A (en) | 2010-06-17 |
Family
ID=40343608
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2010005950A MX2010005950A (en) | 2007-11-28 | 2008-11-25 | 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors. |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP2225247A1 (en) |
| JP (1) | JP2011504931A (en) |
| CN (1) | CN101970440A (en) |
| CA (1) | CA2706946A1 (en) |
| MX (1) | MX2010005950A (en) |
| WO (1) | WO2009070567A1 (en) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101853026B1 (en) | 2008-10-22 | 2018-04-27 | 어레이 바이오파마 인크. | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS |
| AR077468A1 (en) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | PIRAZOLO COMPOUNDS (1,5-A) PYRIMIDINE SUBSTITUTED AS TRK-QUINASA INHIBITORS |
| CN105693720B (en) | 2010-05-20 | 2019-01-18 | 阵列生物制药公司 | Macrocyclic compound as TRK kinase inhibitor |
| EP2723746A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| BR112015012454B1 (en) | 2012-12-07 | 2022-07-05 | Vertex Pharmaceuticals Incorporated | ATR KINASE INHIBITOR COMPOUNDS, THEIR USE AND PHARMACEUTICAL COMPOSITION COMPRISING THEM |
| WO2014143241A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2014143242A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2014143240A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| ES2768678T3 (en) | 2013-12-06 | 2020-06-23 | Vertex Pharma | 2-Amino-6-fluoro-N- [5-fluoro-pyridin-3-yl] pyrazolo [1,5-a] pyrimidin-3-carboxamide compound useful as an ATR kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
| WO2015097121A1 (en) | 2013-12-23 | 2015-07-02 | Norgine B.V. | Compounds useful as ccr9 modulators |
| ES2777608T3 (en) | 2014-06-05 | 2020-08-05 | Vertex Pharma | Radiolabeled derivatives of a 2-amino-6-fluoro-N- [5-fluoro-pyridin-3-yl] -pyrazolo [1,5-a] pyrimidine-3-carboxamide compound useful as ATR kinase inhibitors, the preparation of said compound and different solid forms of it |
| KR20170016498A (en) | 2014-06-17 | 2017-02-13 | 버텍스 파마슈티칼스 인코포레이티드 | Method for treating cancer using a combination of chk1 and atr inhibitors |
| PE20170920A1 (en) | 2014-11-03 | 2017-07-12 | Bayer Pharma AG | PIPERIDINYLpyrazolOPYRIMIDINONES AND THE USE OF THEM |
| CA2966581A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| DK3215511T3 (en) | 2014-11-06 | 2024-05-13 | Bial R&D Invest S A | SUBSTITUTED PYRAZOLO(1,5-A)PYRIMIDINES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| ES2958391T3 (en) | 2014-11-06 | 2024-02-08 | Bial R&D Invest S A | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| TWI746426B (en) | 2014-11-16 | 2021-11-21 | 美商亞雷生物製藥股份有限公司 | Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| CN107108633B (en) * | 2014-12-19 | 2020-05-12 | 詹森药业有限公司 | Heterocyclyl-linked imidazopyridazine derivatives as PI3K β inhibitors |
| KR102678021B1 (en) | 2015-09-30 | 2024-06-26 | 버텍스 파마슈티칼스 인코포레이티드 | Pharmaceutical composition for cancer treatment comprising an ATR inhibitor, used in combination with a DNA damaging agent |
| TN2018000138A1 (en) | 2015-10-26 | 2019-10-04 | Array Biopharma Inc | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| HUE068971T2 (en) | 2016-04-04 | 2025-02-28 | Loxo Oncology Inc | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| WO2017176962A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics, Inc. | Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| JP7046827B2 (en) | 2016-04-06 | 2022-04-04 | リソソーマル・セラピューティクス・インコーポレイテッド | Imidazo [1,5-a] pyrimidinylcarboxamide compounds and their use in the treatment of medical disorders |
| WO2017176960A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| US11345698B2 (en) | 2016-05-05 | 2022-05-31 | Bial—R&D Investments, S.A. | Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders |
| BR112018072552A8 (en) | 2016-05-05 | 2023-03-14 | Lysosomal Therapeutics Inc | IMIDAZO [1,2-B]PYRIDAZINE COMPOUNDS AND SUBSTITUTED IMIDAZO [1,5-B] PYRIDAZINE, PHARMACEUTICAL COMPOSITION INCLUDING THEM AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| SI3458456T1 (en) | 2016-05-18 | 2021-04-30 | Loxo Oncology, Inc. | Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| TW201825499A (en) | 2016-09-19 | 2018-07-16 | 德商拜耳作物科學股份有限公司 | Fused bicyclic heterocyclic derivative as insecticide |
| JOP20190092A1 (en) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | PROCESS FOR THE PREPARATION OF PYRAZOLO[1,5-a]PYRIMIDINES AND SALTS THEREOF |
| JOP20190213A1 (en) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | Macrocyclic compounds as ros1 kinase inhibitors |
| EP4069224A4 (en) * | 2019-12-20 | 2023-12-20 | Recurium IP Holdings, LLC | Combinations |
| CN115209952B (en) | 2020-01-13 | 2025-05-30 | 维基分析有限公司 | Substituted pyrazolopyrimidines and their uses |
| EP4114528A1 (en) * | 2020-03-06 | 2023-01-11 | Bayer Aktiengesellschaft | Imidazotriazines acting on cancer via inhibition of cdk12 |
| WO2021246095A1 (en) * | 2020-06-01 | 2021-12-09 | ユニマテック株式会社 | Fluorine-containing fused ring pyrimidine compound and method for producing same |
| GB202016710D0 (en) * | 2020-10-21 | 2020-12-02 | Univ Birmingham | Treatment of eye conditions |
| CA3204146A1 (en) * | 2021-01-27 | 2022-08-04 | Peng Li | Salt crystals |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004052315A2 (en) * | 2002-12-11 | 2004-06-24 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| MXPA05008955A (en) * | 2003-02-28 | 2006-02-22 | Teijin Pharma Ltd | Pyrazolo[1,5-a]pyrimidine derivatives. |
| JP2008531656A (en) * | 2005-03-02 | 2008-08-14 | ビーエーエスエフ ソシエタス・ヨーロピア | 2-substituted 7-aminoazolopyrimidines, methods for their preparation and their use in controlling pathogenic fungi, and agents containing the compounds |
-
2008
- 2008-11-25 CA CA2706946A patent/CA2706946A1/en not_active Abandoned
- 2008-11-25 EP EP08854702A patent/EP2225247A1/en not_active Withdrawn
- 2008-11-25 JP JP2010536116A patent/JP2011504931A/en not_active Withdrawn
- 2008-11-25 WO PCT/US2008/084643 patent/WO2009070567A1/en not_active Ceased
- 2008-11-25 MX MX2010005950A patent/MX2010005950A/en not_active Application Discontinuation
- 2008-11-25 CN CN2008801257650A patent/CN101970440A/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CA2706946A1 (en) | 2009-06-04 |
| EP2225247A1 (en) | 2010-09-08 |
| WO2009070567A1 (en) | 2009-06-04 |
| CN101970440A (en) | 2011-02-09 |
| JP2011504931A (en) | 2011-02-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |