CA2687966A1 - Thiazoles and pyrazoles useful as kinase inhibitors - Google Patents
Thiazoles and pyrazoles useful as kinase inhibitors Download PDFInfo
- Publication number
- CA2687966A1 CA2687966A1 CA002687966A CA2687966A CA2687966A1 CA 2687966 A1 CA2687966 A1 CA 2687966A1 CA 002687966 A CA002687966 A CA 002687966A CA 2687966 A CA2687966 A CA 2687966A CA 2687966 A1 CA2687966 A1 CA 2687966A1
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- Prior art keywords
- compound
- ring
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- membered
- Prior art date
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- 229940043355 kinase inhibitor Drugs 0.000 title description 7
- 239000003757 phosphotransferase inhibitor Substances 0.000 title description 7
- 150000003217 pyrazoles Chemical class 0.000 title description 2
- 150000003557 thiazoles Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 157
- 239000000203 mixture Substances 0.000 claims abstract description 43
- 238000000034 method Methods 0.000 claims abstract description 38
- 239000003112 inhibitor Substances 0.000 claims abstract description 21
- 239000005441 aurora Substances 0.000 claims abstract description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 16
- 102000001253 Protein Kinase Human genes 0.000 claims abstract description 5
- 108060006633 protein kinase Proteins 0.000 claims abstract description 5
- -1 -OR Chemical group 0.000 claims description 63
- 229910052757 nitrogen Inorganic materials 0.000 claims description 42
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 37
- 125000005842 heteroatom Chemical group 0.000 claims description 32
- 125000000623 heterocyclic group Chemical group 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 28
- 125000001931 aliphatic group Chemical group 0.000 claims description 23
- 125000001072 heteroaryl group Chemical group 0.000 claims description 23
- 206010028980 Neoplasm Diseases 0.000 claims description 22
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- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 16
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 15
- 230000000694 effects Effects 0.000 claims description 12
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 12
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- 125000003118 aryl group Chemical group 0.000 claims description 11
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- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 10
- 239000001301 oxygen Chemical group 0.000 claims description 10
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 10
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- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims description 5
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- FKNJHZBBRHMVJO-INIZCTEOSA-N n-[4-[4-[(3s)-3-fluoropyrrolidin-1-yl]-6-[(5-methyl-1h-pyrazol-3-yl)amino]pyridin-2-yl]sulfanylphenyl]cyclopropanecarboxamide Chemical compound N1N=C(C)C=C1NC1=CC(N2C[C@@H](F)CC2)=CC(SC=2C=CC(NC(=O)C3CC3)=CC=2)=N1 FKNJHZBBRHMVJO-INIZCTEOSA-N 0.000 claims description 5
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US93987607P | 2007-05-24 | 2007-05-24 | |
| US60/939,876 | 2007-05-24 | ||
| PCT/US2008/062331 WO2008147626A2 (en) | 2007-05-24 | 2008-05-02 | Thiazoles and pyrazoles useful as kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2687966A1 true CA2687966A1 (en) | 2008-12-04 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002687966A Abandoned CA2687966A1 (en) | 2007-05-24 | 2008-05-02 | Thiazoles and pyrazoles useful as kinase inhibitors |
Country Status (8)
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|---|---|
| US (1) | US20110060013A1 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2164842A2 (cg-RX-API-DMAC7.html) |
| JP (2) | JP2010528021A (cg-RX-API-DMAC7.html) |
| CN (1) | CN101687852A (cg-RX-API-DMAC7.html) |
| AU (1) | AU2008257044A1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2687966A1 (cg-RX-API-DMAC7.html) |
| MX (1) | MX2009012719A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2008147626A2 (cg-RX-API-DMAC7.html) |
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| NZ594385A (en) | 2005-11-03 | 2013-02-22 | Vertex Pharma | Aminopyrimidines useful as kinase inhibitors |
| DE602007004750D1 (de) | 2006-11-02 | 2010-03-25 | Vertex Pharma | Als inhibitoren von proteinkinasen geeignete aminopyridine und aminopyrimidine |
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| AU2008226466B2 (en) | 2007-03-09 | 2013-06-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
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| EP2152694A2 (en) | 2007-05-02 | 2010-02-17 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| CN101801959A (zh) | 2007-05-02 | 2010-08-11 | 沃泰克斯药物股份有限公司 | 可用作激酶抑制剂的氨基嘧啶类化合物 |
| NZ582879A (en) | 2007-07-31 | 2012-03-30 | Vertex Pharma | Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof |
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| EP2748159A1 (en) | 2011-08-25 | 2014-07-02 | F.Hoffmann-La Roche Ag | Serine/threonine pak1 inhibitors |
| JP2015504876A (ja) | 2011-12-22 | 2015-02-16 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | セリン／トレオニンキナーゼ阻害剤としての２，４−ジアミン−ピリミジン誘導体 |
| LT2841428T (lt) | 2012-04-24 | 2018-12-10 | Vertex Pharmaceuticals Incorporated | Dnr-pk inhibitoriai |
| WO2017156493A1 (en) | 2016-03-11 | 2017-09-14 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
| CN105246883B (zh) | 2013-03-12 | 2017-07-21 | 沃泰克斯药物股份有限公司 | Dna‑pk抑制剂 |
| KR102411227B1 (ko) | 2013-10-17 | 2022-06-21 | 버텍스 파마슈티칼스 인코포레이티드 | Dna-pk 억제제로서 (s)-n-메틸-8-(1-((2'-메틸-[4,5'-비피리미딘]-6-일)아미노)프로판-2-일)퀴놀린-4-카복스아미드 및 이의 듀테로화된 유도체의 공결정 |
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| WO2017087905A1 (en) | 2015-11-20 | 2017-05-26 | Denali Therapeutics Inc. | Compound, compositions, and methods |
| SG10201912632YA (en) | 2016-06-16 | 2020-02-27 | Denali Therapeutics Inc | Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders |
| TW201815418A (zh) | 2016-09-27 | 2018-05-01 | Vertex Pharma | 使用dna破壞劑及dna-pk抑制劑之組合治療癌症的方法 |
| EP4090426B1 (en) | 2020-01-13 | 2025-12-31 | Verge Analytics, Inc. | Substitutes for pyrazolos and pyrimidines and their uses |
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-
2008
- 2008-05-02 AU AU2008257044A patent/AU2008257044A1/en not_active Abandoned
- 2008-05-02 CN CN200880022823A patent/CN101687852A/zh active Pending
- 2008-05-02 WO PCT/US2008/062331 patent/WO2008147626A2/en not_active Ceased
- 2008-05-02 EP EP08747433A patent/EP2164842A2/en not_active Withdrawn
- 2008-05-02 MX MX2009012719A patent/MX2009012719A/es not_active Application Discontinuation
- 2008-05-02 JP JP2010509424A patent/JP2010528021A/ja active Pending
- 2008-05-02 CA CA002687966A patent/CA2687966A1/en not_active Abandoned
-
2009
- 2009-11-20 US US12/601,026 patent/US20110060013A1/en not_active Abandoned
-
2014
- 2014-05-09 JP JP2014097421A patent/JP2014141529A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| AU2008257044A1 (en) | 2008-12-04 |
| JP2014141529A (ja) | 2014-08-07 |
| JP2010528021A (ja) | 2010-08-19 |
| WO2008147626A2 (en) | 2008-12-04 |
| EP2164842A2 (en) | 2010-03-24 |
| MX2009012719A (es) | 2010-02-04 |
| US20110060013A1 (en) | 2011-03-10 |
| CN101687852A (zh) | 2010-03-31 |
| WO2008147626A3 (en) | 2009-03-19 |
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| FZDE | Discontinued |
Effective date: 20140502 |