JP2010509231A5 - - Google Patents
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- JP2010509231A5 JP2010509231A5 JP2009535466A JP2009535466A JP2010509231A5 JP 2010509231 A5 JP2010509231 A5 JP 2010509231A5 JP 2009535466 A JP2009535466 A JP 2009535466A JP 2009535466 A JP2009535466 A JP 2009535466A JP 2010509231 A5 JP2010509231 A5 JP 2010509231A5
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- JP
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- Prior art keywords
- ring
- aliphatic
- compound according
- optionally substituted
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- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 73
- 125000001931 aliphatic group Chemical group 0.000 claims description 52
- 239000003814 drug Substances 0.000 claims description 40
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 32
- 229940079593 drugs Drugs 0.000 claims description 29
- 229910052757 nitrogen Inorganic materials 0.000 claims description 27
- 125000000623 heterocyclic group Chemical group 0.000 claims description 26
- 229910052739 hydrogen Inorganic materials 0.000 claims description 26
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 24
- 125000001072 heteroaryl group Chemical group 0.000 claims description 24
- 239000001257 hydrogen Substances 0.000 claims description 24
- 125000004429 atoms Chemical group 0.000 claims description 22
- 239000000203 mixture Substances 0.000 claims description 21
- 125000005843 halogen group Chemical group 0.000 claims description 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
- 125000001475 halogen functional group Chemical group 0.000 claims description 16
- 201000002674 obstructive nephropathy Diseases 0.000 claims description 16
- 201000010099 disease Diseases 0.000 claims description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 14
- 239000003795 chemical substances by application Substances 0.000 claims description 13
- 206010012601 Diabetes mellitus Diseases 0.000 claims description 12
- 125000004043 oxo group Chemical group O=* 0.000 claims description 12
- 229910052760 oxygen Inorganic materials 0.000 claims description 12
- 206010002026 Amyotrophic lateral sclerosis Diseases 0.000 claims description 10
- 125000005842 heteroatoms Chemical group 0.000 claims description 10
- 239000001301 oxygen Chemical group 0.000 claims description 10
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical group O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims description 10
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 201000002364 leukopenia Diseases 0.000 claims description 8
- 231100001022 leukopenia Toxicity 0.000 claims description 8
- 201000006417 multiple sclerosis Diseases 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 239000000126 substance Substances 0.000 claims description 8
- NINIDFKCEFEMDL-UHFFFAOYSA-N sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 8
- 229910052717 sulfur Chemical group 0.000 claims description 8
- 239000011593 sulfur Chemical group 0.000 claims description 8
- 206010004938 Bipolar disease Diseases 0.000 claims description 6
- 125000001118 alkylidene group Chemical group 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000005605 benzo group Chemical group 0.000 claims description 6
- 150000002829 nitrogen Chemical group 0.000 claims description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
- NGVDGCNFYWLIFO-UHFFFAOYSA-N pyridoxal 5'-phosphate Chemical group CC1=NC=C(COP(O)(O)=O)C(C=O)=C1O NGVDGCNFYWLIFO-UHFFFAOYSA-N 0.000 claims description 6
- 201000000980 schizophrenia Diseases 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- -1 -OR Chemical group 0.000 claims description 4
- 206010065040 AIDS dementia complex Diseases 0.000 claims description 4
- 206010001897 Alzheimer's disease Diseases 0.000 claims description 4
- 201000001971 Huntington's disease Diseases 0.000 claims description 4
- 206010020880 Hypertrophy Diseases 0.000 claims description 4
- 210000004413 Myocytes, Cardiac Anatomy 0.000 claims description 4
- 208000001132 Osteoporosis Diseases 0.000 claims description 4
- 206010061536 Parkinson's disease Diseases 0.000 claims description 4
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 210000002317 cardiac myocyte Anatomy 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 4
- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 238000000338 in vitro Methods 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 4
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 4
- 238000011084 recovery Methods 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 125000004530 1,2,4-triazinyl group Chemical group N1=NC(=NC=C1)* 0.000 claims description 2
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims description 2
- 229940116904 ANTIINFLAMMATORY THERAPEUTIC RADIOPHARMACEUTICALS Drugs 0.000 claims description 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 2
- 208000008787 Cardiovascular Disease Diseases 0.000 claims description 2
- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 claims description 2
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 claims description 2
- 229960003444 IMMUNOSUPPRESSANTS Drugs 0.000 claims description 2
- UXGVMFHEKMGWMA-UHFFFAOYSA-N Isobenzofuran Chemical compound C1=CC=CC2=COC=C21 UXGVMFHEKMGWMA-UHFFFAOYSA-N 0.000 claims description 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims description 2
- 108010008267 Nerve Growth Factors Proteins 0.000 claims description 2
- 229940074726 OPHTHALMOLOGIC ANTIINFLAMMATORY AGENTS Drugs 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 230000000240 adjuvant Effects 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 230000001028 anti-proliferant Effects 0.000 claims description 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 2
- 230000000973 chemotherapeutic Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000006161 haloaliphatic group Chemical group 0.000 claims description 2
- 150000002367 halogens Chemical class 0.000 claims description 2
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 239000002955 immunomodulating agent Substances 0.000 claims description 2
- 230000002584 immunomodulator Effects 0.000 claims description 2
- 229940121354 immunomodulators Drugs 0.000 claims description 2
- 230000001861 immunosuppresant Effects 0.000 claims description 2
- 239000003018 immunosuppressive agent Substances 0.000 claims description 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 201000010901 lateral sclerosis Diseases 0.000 claims description 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 239000003900 neurotrophic factor Substances 0.000 claims description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 2
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 239000011780 sodium chloride Substances 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- HONIICLYMWZJFZ-UHFFFAOYSA-N Azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 206010052739 Immunodeficiency disorder Diseases 0.000 claims 1
- 102000030951 Phosphotransferases Human genes 0.000 description 2
- 108091000081 Phosphotransferases Proteins 0.000 description 2
- 208000006011 Stroke Diseases 0.000 description 2
- 150000001539 azetidines Chemical class 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 230000001404 mediated Effects 0.000 description 1
- 230000001575 pathological Effects 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 201000002367 primary immunodeficiency disease Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85613506P | 2006-11-02 | 2006-11-02 | |
| US95302507P | 2007-07-31 | 2007-07-31 | |
| PCT/US2007/083334 WO2008057940A1 (en) | 2006-11-02 | 2007-11-01 | Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010509231A JP2010509231A (ja) | 2010-03-25 |
| JP2010509231A5 true JP2010509231A5 (US07585860-20090908-C00112.png) | 2010-12-16 |
Family
ID=39092661
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009535466A Pending JP2010509231A (ja) | 2006-11-02 | 2007-11-01 | プロテインキナーゼの阻害剤として有用なアミノピリジンおよびアミノピリミジン |
Country Status (10)
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6638926B2 (en) | 2000-09-15 | 2003-10-28 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| WO2004072029A2 (en) | 2003-02-06 | 2004-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridazines useful as inhibitors of protein kinases |
| AU2006311830B2 (en) | 2005-11-03 | 2013-03-14 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| AU2007317435A1 (en) | 2006-11-02 | 2008-05-15 | Vertex Pharmaceuticals Incorporated | Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases |
| WO2008077086A1 (en) | 2006-12-19 | 2008-06-26 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| JP5520057B2 (ja) | 2007-03-09 | 2014-06-11 | バーテックス ファーマシューティカルズ インコーポレイテッド | 蛋白キナーゼの阻害剤として有用なアミノピリミジン |
| NZ579483A (en) | 2007-03-09 | 2012-07-27 | Vertex Pharma | Aminopyridines useful as inhibitors of protein kinases |
| JP5393489B2 (ja) | 2007-03-09 | 2014-01-22 | バーテックス ファーマシューティカルズ インコーポレイテッド | 蛋白キナーゼの阻害剤として有用なアミノピリミジン |
| MX2009011059A (es) | 2007-04-13 | 2009-11-26 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de cinasas. |
| WO2008137621A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| CA2685876A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| CA2694499A1 (en) * | 2007-07-31 | 2009-02-05 | Vertex Pharmaceuticals Incorporated | Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| WO2010091808A1 (en) | 2009-02-13 | 2010-08-19 | Bayer Schering Pharma Aktiengesellschaft | Fused pyrimidines |
| 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 |
| 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 |
| 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 |
| RS61664B1 (sr) | 2012-04-24 | 2021-04-29 | Vertex Pharma | Inhibitori dna-pk |
| RS58374B1 (sr) | 2013-03-12 | 2019-03-29 | Vertex Pharma | Inhibitori dnk-pk |
| EP3057953B1 (en) | 2013-10-17 | 2018-08-15 | Vertex Pharmaceuticals Incorporated | Co-crystals of (s)-n-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide and deuterated derivatives thereof as dna-pk inhibitors |
| KR101731624B1 (ko) * | 2014-07-01 | 2017-05-04 | 광주과학기술원 | 세포 리프로그래밍 유도용 조성물 |
| WO2016197009A1 (en) | 2015-06-05 | 2016-12-08 | Vertex Pharmaceuticals Incorporated | Triazoles for the treatment of demyelinating diseases |
| 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 |
| WO2018106641A1 (en) * | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Pyrazoles for the treatment of demyelinating diseases |
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2007
- 2007-11-01 AU AU2007317435A patent/AU2007317435A1/en not_active Abandoned
- 2007-11-01 WO PCT/US2007/083334 patent/WO2008057940A1/en active Application Filing
- 2007-11-01 MX MX2009004807A patent/MX2009004807A/es active IP Right Grant
- 2007-11-01 AT AT07844798T patent/ATE457311T1/de not_active IP Right Cessation
- 2007-11-01 JP JP2009535466A patent/JP2010509231A/ja active Pending
- 2007-11-01 NZ NZ576750A patent/NZ576750A/en not_active IP Right Cessation
- 2007-11-01 EP EP07844798A patent/EP2086965B1/en active Active
- 2007-11-01 CA CA002668429A patent/CA2668429A1/en not_active Abandoned
- 2007-11-01 DE DE602007004750T patent/DE602007004750D1/de active Active
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2009
- 2009-05-01 US US12/433,998 patent/US8372850B2/en not_active Expired - Fee Related
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2013
- 2013-01-09 US US13/736,988 patent/US20140187781A1/en not_active Abandoned
