JP2010520886A5 - - Google Patents
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- JP2010520886A5 JP2010520886A5 JP2009552927A JP2009552927A JP2010520886A5 JP 2010520886 A5 JP2010520886 A5 JP 2010520886A5 JP 2009552927 A JP2009552927 A JP 2009552927A JP 2009552927 A JP2009552927 A JP 2009552927A JP 2010520886 A5 JP2010520886 A5 JP 2010520886A5
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- Prior art keywords
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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 69
- 125000000217 alkyl group Chemical group 0.000 claims description 40
- 239000003814 drug Substances 0.000 claims description 40
- 239000000203 mixture Substances 0.000 claims description 30
- 229940079593 drug Drugs 0.000 claims description 29
- 125000005843 halogen group Chemical group 0.000 claims description 28
- 239000003795 chemical substances by application Substances 0.000 claims description 26
- 201000010099 disease Diseases 0.000 claims description 23
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 23
- 125000000623 heterocyclic group Chemical group 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 20
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 11
- 229940124597 therapeutic agent Drugs 0.000 claims description 11
- 125000005842 heteroatom Chemical group 0.000 claims description 10
- 201000006417 multiple sclerosis Diseases 0.000 claims description 10
- 206010012601 diabetes mellitus Diseases 0.000 claims description 9
- 229910052757 nitrogen Inorganic materials 0.000 claims description 9
- 125000002723 alicyclic group Chemical group 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 210000002569 neuron Anatomy 0.000 claims description 8
- 208000020925 Bipolar disease Diseases 0.000 claims description 7
- 201000002364 leukopenia Diseases 0.000 claims description 7
- 231100001022 leukopenia Toxicity 0.000 claims description 7
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- 201000000980 schizophrenia Diseases 0.000 claims description 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 208000024827 Alzheimer disease Diseases 0.000 claims description 5
- 208000023105 Huntington disease Diseases 0.000 claims description 5
- 208000001132 Osteoporosis Diseases 0.000 claims description 5
- 208000018737 Parkinson disease Diseases 0.000 claims description 5
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 5
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims description 4
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 4
- 208000006011 Stroke Diseases 0.000 claims description 4
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 4
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 208000020431 spinal cord injury Diseases 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 230000009529 traumatic brain injury Effects 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 3
- 238000000338 in vitro Methods 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 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
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 230000033115 angiogenesis Effects 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
- 239000012472 biological sample Substances 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 230000000973 chemotherapeutic effect Effects 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 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
- 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
- 208000033065 inborn errors of immunity Diseases 0.000 claims description 2
- 208000028867 ischemia Diseases 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 230000004766 neurogenesis Effects 0.000 claims description 2
- 239000003900 neurotrophic factor Substances 0.000 claims description 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 2
- 238000000554 physical therapy Methods 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 208000028529 primary immunodeficiency disease Diseases 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 238000011084 recovery Methods 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 208000030507 AIDS Diseases 0.000 claims 3
- 206010012289 Dementia Diseases 0.000 claims 3
- 210000003050 axon Anatomy 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 210000001787 dendrite Anatomy 0.000 claims 1
- -1 fluoro compound Chemical class 0.000 claims 1
- 210000004027 cell Anatomy 0.000 description 4
- 108091000080 Phosphotransferase Proteins 0.000 description 3
- 102000020233 phosphotransferase Human genes 0.000 description 3
- 206010065040 AIDS dementia complex Diseases 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 230000003376 axonal effect Effects 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 208000032839 leukemia Diseases 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
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90608607P | 2007-03-09 | 2007-03-09 | |
| US60/906,086 | 2007-03-09 | ||
| US95302007P | 2007-07-31 | 2007-07-31 | |
| US60/953,020 | 2007-07-31 | ||
| PCT/US2008/056423 WO2008112642A1 (en) | 2007-03-09 | 2008-03-10 | Aminopyrimidines useful as inhibitors of protein kinases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010520886A JP2010520886A (ja) | 2010-06-17 |
| JP2010520886A5 true JP2010520886A5 (enExample) | 2012-04-05 |
| JP5520057B2 JP5520057B2 (ja) | 2014-06-11 |
Family
ID=39472801
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009552927A Expired - Fee Related JP5520057B2 (ja) | 2007-03-09 | 2008-03-10 | 蛋白キナーゼの阻害剤として有用なアミノピリミジン |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US8664219B2 (enExample) |
| EP (1) | EP2134707B1 (enExample) |
| JP (1) | JP5520057B2 (enExample) |
| CN (1) | CN101663295B (enExample) |
| AU (2) | AU2008226457B2 (enExample) |
| CA (1) | CA2679884A1 (enExample) |
| ES (1) | ES2435997T3 (enExample) |
| MX (1) | MX2009009590A (enExample) |
| NZ (1) | NZ579446A (enExample) |
| WO (1) | WO2008112642A1 (enExample) |
Families Citing this family (36)
| 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 |
| DK1318997T3 (da) | 2000-09-15 | 2006-09-25 | Vertex Pharma | Pyrazolforbindelser der er nyttige som proteinkinase-inhibitorer |
| WO2004072029A2 (en) | 2003-02-06 | 2004-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridazines useful as inhibitors of protein kinases |
| TW200734327A (en) | 2005-11-03 | 2007-09-16 | Vertex Pharma | Aminopyrimidines useful as kinase inhibitors |
| WO2008057940A1 (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 |
| US8247421B2 (en) | 2006-12-21 | 2012-08-21 | Vertex Pharmaceuticals Incorporated | 5-cyano-4-(pyrrolo [2,3B] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors |
| WO2008112642A1 (en) | 2007-03-09 | 2008-09-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| EP2137183B1 (en) | 2007-03-09 | 2011-09-28 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| EP2134709A1 (en) | 2007-03-09 | 2009-12-23 | Vertex Pharmaceuticals, Inc. | Aminopyridines useful as inhibitors of protein kinases |
| JP2010523700A (ja) | 2007-04-13 | 2010-07-15 | 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 | キナーゼインヒビターとして有用なアミノピリミジン |
| CN101679378A (zh) | 2007-05-02 | 2010-03-24 | 沃泰克斯药物股份有限公司 | 用作激酶抑制剂的噻唑和吡唑 |
| 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 |
| AR067762A1 (es) | 2007-07-31 | 2009-10-21 | Vertex Pharma | Proceso para preparar 5-fluoro-1h-pirazolo (3,4-b) piridin-3-amina y derivados de la misma |
| EP2262498A2 (en) * | 2008-03-10 | 2010-12-22 | Vertex Pharmceuticals Incorporated | Pyrimidines and pyridines useful as inhibitors of protein kinases |
| CN101768110B (zh) * | 2009-01-07 | 2012-09-12 | 上海开拓者化学研究管理有限公司 | 一种2-氯-5-氟吡啶-3-甲酸的制备方法 |
| GEAP202213376A (en) | 2009-06-17 | 2022-02-25 | Vertex Pharmaceuticals Incorporated Us | Inhibitors of influenza viruses replication |
| EP2305274A1 (en) * | 2009-09-21 | 2011-04-06 | Centre National de la Recherche Scientifique (CNRS) | Use of WNT stimulators for treating demyelinating diseases |
| 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 |
| 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 |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| CN103492381A (zh) | 2010-12-16 | 2014-01-01 | 沃泰克斯药物股份有限公司 | 流感病毒复制的抑制剂 |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| 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 |
| IN2014KN02601A (enExample) | 2012-04-24 | 2015-05-08 | Vertex Pharma | |
| SMT202100687T1 (it) | 2013-03-12 | 2022-01-10 | Vertex Pharma | Inibitori della dna-pk |
| ES2705342T3 (es) | 2013-10-17 | 2019-03-22 | Vertex Pharma | Co-cristales de (S)-N-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propan-2-il)quinolin-4-carboxamida y derivados deuterados de la misma como inhibidores de DNA-PK |
| HUE052178T2 (hu) | 2013-11-13 | 2021-04-28 | Vertex Pharma | Eljárások influenzavírus-replikáció inhibitorainak elõállítására |
| LT3068776T (lt) | 2013-11-13 | 2019-08-12 | Vertex Pharmaceuticals Incorporated | Gripo virusų replikacijos inhibitoriai |
| JP6857617B2 (ja) | 2015-05-13 | 2021-04-14 | 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | インフルエンザウイルスの複製の阻害剤 |
| WO2016183116A1 (en) | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
| EP3518931A4 (en) | 2016-09-27 | 2020-05-13 | Vertex Pharmaceuticals Incorporated | METHOD FOR TREATING CANCER WITH A COMBINATION OF DNA-DAMAGING SUBSTANCES AND DNA-PK INHIBITORS |
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| KR20060123164A (ko) | 2003-10-17 | 2006-12-01 | 아스트라제네카 아베 | 암 치료에 사용하기 위한 4-(피라졸-3-일아미노)피리미딘유도체 |
| EP1697375A2 (en) * | 2003-12-02 | 2006-09-06 | Vertex Pharmaceuticals Incorporated | Heterocyclic protein kinase inhibitors and uses thereof |
| AU2006279376B2 (en) | 2005-08-18 | 2011-04-14 | Vertex Pharmaceuticals Incoporated | Pyrazine kinase inhibitors |
| WO2007023382A2 (en) * | 2005-08-25 | 2007-03-01 | Pfizer Inc. | Pyrimidine amino pyrazole compounds, potent kinase inhibitors |
| CA2622352C (en) | 2005-09-30 | 2014-05-27 | Miikana Therapeutics, Inc. | Substituted pyrazole compounds |
| TW200734327A (en) | 2005-11-03 | 2007-09-16 | Vertex Pharma | Aminopyrimidines useful as kinase inhibitors |
| EP1951716B1 (en) | 2005-11-16 | 2011-05-04 | Vertex Pharmaceuticals, Inc. | Aminopyrimidines useful as kinase inhibitors |
| WO2008057940A1 (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 |
| WO2008112642A1 (en) | 2007-03-09 | 2008-09-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| EP2137183B1 (en) | 2007-03-09 | 2011-09-28 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| EP2134709A1 (en) | 2007-03-09 | 2009-12-23 | Vertex Pharmaceuticals, Inc. | Aminopyridines useful as inhibitors of protein kinases |
| CN101675041A (zh) | 2007-03-20 | 2010-03-17 | 沃泰克斯药物股份有限公司 | 用作激酶抑制剂的氨基嘧啶类化合物 |
| WO2008131103A2 (en) | 2007-04-17 | 2008-10-30 | Vertex Pharmaceuticals Incorporated | Drug discovery methods for aurora kinase inhibitors |
| AU2008247595A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| CN101679378A (zh) | 2007-05-02 | 2010-03-24 | 沃泰克斯药物股份有限公司 | 用作激酶抑制剂的噻唑和吡唑 |
| 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 |
| AU2008257044A1 (en) | 2007-05-24 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| AR067762A1 (es) * | 2007-07-31 | 2009-10-21 | Vertex Pharma | Proceso para preparar 5-fluoro-1h-pirazolo (3,4-b) piridin-3-amina y derivados de la misma |
| MX384179B (es) | 2009-03-20 | 2025-03-14 | Vertex Pharma | Proceso para producir moduladores del regulador de conductancia transmembrana de fibrosis quística. |
-
2008
- 2008-03-10 WO PCT/US2008/056423 patent/WO2008112642A1/en not_active Ceased
- 2008-03-10 MX MX2009009590A patent/MX2009009590A/es active IP Right Grant
- 2008-03-10 EP EP08731830.9A patent/EP2134707B1/en not_active Not-in-force
- 2008-03-10 JP JP2009552927A patent/JP5520057B2/ja not_active Expired - Fee Related
- 2008-03-10 AU AU2008226457A patent/AU2008226457B2/en not_active Ceased
- 2008-03-10 CA CA002679884A patent/CA2679884A1/en not_active Abandoned
- 2008-03-10 CN CN200880012693.9A patent/CN101663295B/zh not_active Expired - Fee Related
- 2008-03-10 ES ES08731830T patent/ES2435997T3/es active Active
- 2008-03-10 NZ NZ579446A patent/NZ579446A/en not_active IP Right Cessation
-
2010
- 2010-06-02 US US12/791,976 patent/US8664219B2/en not_active Expired - Fee Related
-
2014
- 2014-01-15 US US14/155,624 patent/US20140194444A1/en not_active Abandoned
- 2014-06-18 AU AU2014203289A patent/AU2014203289A1/en not_active Abandoned
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