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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- Prior art keywords
- ring
- aliphatic
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- optionally substituted
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- 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.)
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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 drug 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 atom Chemical group 0.000 claims description 18
- 125000005843 halogen group Chemical group 0.000 claims description 18
- 239000000203 mixture Substances 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
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 14
- 201000010099 disease Diseases 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 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
- 229910052760 oxygen Inorganic materials 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 11
- 229940124597 therapeutic agent Drugs 0.000 claims description 11
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 10
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 10
- 125000005842 heteroatom Chemical group 0.000 claims description 10
- 239000001301 oxygen Chemical group 0.000 claims description 10
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 8
- 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
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 239000000126 substance Substances 0.000 claims description 8
- 229910052717 sulfur Chemical group 0.000 claims description 8
- 239000011593 sulfur Chemical group 0.000 claims description 8
- 208000006011 Stroke Diseases 0.000 claims description 7
- 208000020925 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
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-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
- 208000024827 Alzheimer disease Diseases 0.000 claims description 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 208000023105 Huntington disease Diseases 0.000 claims description 4
- 206010020880 Hypertrophy Diseases 0.000 claims description 4
- 208000001132 Osteoporosis Diseases 0.000 claims description 4
- 208000018737 Parkinson disease 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
- 210000004413 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
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 4
- 125000006413 ring segment Chemical group 0.000 claims description 4
- 229920006395 saturated elastomer Polymers 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
- UXGVMFHEKMGWMA-UHFFFAOYSA-N 2-benzofuran Chemical compound C1=CC=CC2=COC=C21 UXGVMFHEKMGWMA-UHFFFAOYSA-N 0.000 claims description 2
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims description 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 2
- 208000024172 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
- 108010025020 Nerve Growth Factor Proteins 0.000 claims description 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 2
- 230000001028 anti-proliverative effect 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 effect 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 atom 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
- 229940121354 immunomodulator Drugs 0.000 claims description 2
- 229960003444 immunosuppressant agent Drugs 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
- 208000005264 motor neuron disease Diseases 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
- 125000004043 oxo group Chemical group O=* 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
- 239000003981 vehicle Substances 0.000 claims description 2
- 208000029462 Immunodeficiency disease Diseases 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- 150000001539 azetidines Chemical class 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 208000033065 inborn errors of immunity Diseases 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 208000028529 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 (OSRAM) | 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)
| Country | Link |
|---|---|
| US (2) | US8372850B2 (OSRAM) |
| EP (1) | EP2086965B1 (OSRAM) |
| JP (1) | JP2010509231A (OSRAM) |
| AT (1) | ATE457311T1 (OSRAM) |
| AU (1) | AU2007317435A1 (OSRAM) |
| CA (1) | CA2668429A1 (OSRAM) |
| DE (1) | DE602007004750D1 (OSRAM) |
| MX (1) | MX2009004807A (OSRAM) |
| NZ (1) | NZ576750A (OSRAM) |
| WO (1) | WO2008057940A1 (OSRAM) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| ATE346064T1 (de) | 2000-09-15 | 2006-12-15 | Vertex Pharma | Pyrazolverbindungen als protein-kinasehemmer |
| WO2004072029A2 (en) | 2003-02-06 | 2004-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridazines useful as inhibitors of protein kinases |
| JP5249770B2 (ja) | 2005-11-03 | 2013-07-31 | 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 | キナーゼインヒビターとして有用なアミノピリジン |
| EP2086965B1 (en) | 2006-11-02 | 2010-02-10 | Vertex Pharmaceuticals, Inc. | Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases |
| DE602007007985D1 (de) * | 2006-12-19 | 2010-09-02 | Vertex Pharma | Als inhibitoren von proteinkinasen geeignete aminopyrimidine |
| MX2009009592A (es) | 2007-03-09 | 2009-11-10 | Vertex Pharma | Aminopiridinas utiles como inhibidores de proteinas cinasas. |
| KR20090120510A (ko) * | 2007-03-09 | 2009-11-24 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제 억제제로서 유용한 아미노피리미딘 |
| CA2679884A1 (en) | 2007-03-09 | 2008-09-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| CA2683785A1 (en) | 2007-04-13 | 2008-10-23 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| JP5389786B2 (ja) | 2007-05-02 | 2014-01-15 | 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 | キナーゼ阻害として有用なアミノピリミジン |
| AU2008247592A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| AU2008282156B2 (en) | 2007-07-31 | 2014-07-17 | 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 |
| MX2011008583A (es) * | 2009-02-13 | 2011-12-12 | Bayer Pharma AG | Pirimidinas fusionadas. |
| 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 |
| 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 |
| RS61664B1 (sr) | 2012-04-24 | 2021-04-29 | Vertex Pharma | Inhibitori dna-pk |
| SI3527563T1 (sl) | 2013-03-12 | 2022-01-31 | Vertex Pharmaceuticals Incorporated | Inhibitorji DNA-PK |
| SI3424920T1 (sl) | 2013-10-17 | 2020-08-31 | Vertex Pharmaceuticals Incorporated | Kokristali (s)-n-metil-8-(1-((2'-metil-(4,5'-bipirimidin)-6-il)amino)propan-2-il) kinolin-4-karboksamida in devterirani derivati le-teh kot inhibitorji dna-pk |
| 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 |
| KR20190062485A (ko) | 2016-09-27 | 2019-06-05 | 버텍스 파마슈티칼스 인코포레이티드 | Dna-손상제 및 dna-pk 저해제의 조합을 사용한 암 치료 방법 |
| WO2018106641A1 (en) * | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Pyrazoles for the treatment of demyelinating diseases |
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| CN1319968C (zh) * | 2002-08-02 | 2007-06-06 | 沃泰克斯药物股份有限公司 | 用作gsk－3的抑制剂的吡唑组合物 |
| KR20060123164A (ko) | 2003-10-17 | 2006-12-01 | 아스트라제네카 아베 | 암 치료에 사용하기 위한 4-(피라졸-3-일아미노)피리미딘유도체 |
| CA2619517A1 (en) | 2005-08-18 | 2007-02-22 | Michael Mortimore | Pyrazine kinase inhibitors |
| WO2007023382A2 (en) | 2005-08-25 | 2007-03-01 | Pfizer Inc. | Pyrimidine amino pyrazole compounds, potent kinase inhibitors |
| WO2007041358A2 (en) | 2005-09-30 | 2007-04-12 | Miikana Therapeutics, Inc. | Substituted pyrazole compounds |
| JP5249770B2 (ja) | 2005-11-03 | 2013-07-31 | 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 | キナーゼインヒビターとして有用なアミノピリジン |
| CA2629781A1 (en) | 2005-11-16 | 2007-05-24 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| EP2086965B1 (en) | 2006-11-02 | 2010-02-10 | Vertex Pharmaceuticals, Inc. | Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases |
| DE602007007985D1 (de) | 2006-12-19 | 2010-09-02 | Vertex Pharma | Als inhibitoren von proteinkinasen geeignete aminopyrimidine |
| KR20090120510A (ko) | 2007-03-09 | 2009-11-24 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제 억제제로서 유용한 아미노피리미딘 |
| MX2009009592A (es) | 2007-03-09 | 2009-11-10 | Vertex Pharma | Aminopiridinas utiles como inhibidores de proteinas cinasas. |
| CA2679884A1 (en) | 2007-03-09 | 2008-09-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| CA2682195A1 (en) | 2007-03-20 | 2008-09-25 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| WO2008131103A2 (en) | 2007-04-17 | 2008-10-30 | Vertex Pharmaceuticals Incorporated | Drug discovery methods for aurora kinase inhibitors |
| MX2009011811A (es) | 2007-05-02 | 2010-01-14 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de cinasa. |
| JP5389786B2 (ja) | 2007-05-02 | 2014-01-15 | 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 | キナーゼ阻害として有用なアミノピリミジン |
| AU2008247592A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| CN101687852A (zh) | 2007-05-24 | 2010-03-31 | 沃泰克斯药物股份有限公司 | 可用作激酶抑制剂的噻唑类和吡唑类化合物 |
-
2007
- 2007-11-01 EP EP07844798A patent/EP2086965B1/en active Active
- 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 DE DE602007004750T patent/DE602007004750D1/de active Active
- 2007-11-01 AU AU2007317435A patent/AU2007317435A1/en not_active Abandoned
- 2007-11-01 MX MX2009004807A patent/MX2009004807A/es active IP Right Grant
- 2007-11-01 NZ NZ576750A patent/NZ576750A/en not_active IP Right Cessation
- 2007-11-01 CA CA002668429A patent/CA2668429A1/en not_active Abandoned
- 2007-11-01 WO PCT/US2007/083334 patent/WO2008057940A1/en not_active Ceased
-
2009
- 2009-05-01 US US12/433,998 patent/US8372850B2/en not_active Expired - Fee Related
-
2013
- 2013-01-09 US US13/736,988 patent/US20140187781A1/en not_active Abandoned
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