ES2865483T3 - Pirazolo[1,5-a]pirazinas sustituidas en 4,6 como inhibidores de Janus cinasa - Google Patents
Pirazolo[1,5-a]pirazinas sustituidas en 4,6 como inhibidores de Janus cinasa Download PDFInfo
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- ES2865483T3 ES2865483T3 ES15819933T ES15819933T ES2865483T3 ES 2865483 T3 ES2865483 T3 ES 2865483T3 ES 15819933 T ES15819933 T ES 15819933T ES 15819933 T ES15819933 T ES 15819933T ES 2865483 T3 ES2865483 T3 ES 2865483T3
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- alkyl
- pyrazol
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- 150000003216 pyrazines Chemical class 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 287
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- -1 hetCyc4 Chemical group 0.000 claims abstract description 152
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims abstract description 97
- 150000003839 salts Chemical class 0.000 claims abstract description 90
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims abstract description 75
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 73
- 239000012453 solvate Substances 0.000 claims abstract description 70
- 125000001424 substituent group Chemical group 0.000 claims abstract description 54
- 125000003545 alkoxy group Chemical group 0.000 claims abstract description 46
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 43
- 229910052736 halogen Inorganic materials 0.000 claims abstract description 40
- 229920006395 saturated elastomer Polymers 0.000 claims abstract description 40
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract description 38
- 150000002367 halogens Chemical class 0.000 claims abstract description 38
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- 125000004990 dihydroxyalkyl group Chemical group 0.000 claims abstract description 27
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 27
- 125000004950 trifluoroalkyl group Chemical group 0.000 claims abstract description 27
- 229910052799 carbon Inorganic materials 0.000 claims abstract description 25
- 125000005842 heteroatom Chemical group 0.000 claims abstract description 25
- 239000001257 hydrogen Substances 0.000 claims abstract description 24
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 22
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract description 19
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- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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| US201462088068P | 2014-12-05 | 2014-12-05 | |
| PCT/US2015/064062 WO2016090285A1 (en) | 2014-12-05 | 2015-12-04 | 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS |
Publications (1)
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| ES2865483T3 true ES2865483T3 (es) | 2021-10-15 |
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| WO2017156493A1 (en) | 2016-03-11 | 2017-09-14 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
| PL3227297T3 (pl) | 2014-12-05 | 2021-10-25 | Array Biopharma, Inc. | 4,6 podstawione-pyrazolo[1,5-a]pirazyny jako inhibitory kinaz janusowych |
| RU2718902C2 (ru) * | 2016-02-24 | 2020-04-15 | Пфайзер Инк. | Производные пиразоло[1,5-а]пиразин-4-ила в качестве jak-ингибиторов |
| PE20190395A1 (es) | 2016-06-16 | 2019-03-13 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos |
| GB201617758D0 (en) * | 2016-10-20 | 2016-12-07 | Almac Discovery Limited | Pharmaceutical compounds |
| CA3049136C (en) | 2017-01-18 | 2022-06-14 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| WO2018217946A1 (en) * | 2017-05-24 | 2018-11-29 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| EP3668858A1 (en) | 2017-08-14 | 2020-06-24 | Pfizer Inc | Pyrazolo[1,5-a]pyrazin-4-yl and related derivatives |
| CA3087354C (en) | 2018-01-18 | 2023-01-03 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CA3087578C (en) | 2018-01-18 | 2023-08-08 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| JP7256291B2 (ja) * | 2019-04-12 | 2023-04-11 | プライムジーン（ベイジン）カンパニー リミテッド | ピラゾロピラジン誘導の化合物、医薬組成物およびその使用 |
| KR102503349B1 (ko) | 2019-05-14 | 2023-02-23 | 프로벤션 바이오, 인코포레이티드 | 제1형 당뇨병을 예방하기 위한 방법 및 조성물 |
| CN113150012B (zh) * | 2020-01-22 | 2023-03-24 | 浙江海正药业股份有限公司 | 吡唑并[1,5-a]吡嗪类衍生物及其制备方法和用途 |
| WO2021198980A1 (en) | 2020-04-04 | 2021-10-07 | Pfizer Inc. | Methods of treating coronavirus disease 2019 |
| US12006366B2 (en) | 2020-06-11 | 2024-06-11 | Provention Bio, Inc. | Methods and compositions for preventing type 1 diabetes |
| IL312782A (en) * | 2021-11-12 | 2024-07-01 | Soter Biopharma Pte Ltd | Pyrazolo fused ring compound and use thereof |
| WO2024235167A1 (zh) * | 2023-05-12 | 2024-11-21 | 海南康哲美丽科技有限公司 | 一种吡唑并吡嗪类化合物及其晶型的制备方法 |
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| KR20010089171A (ko) | 1998-08-21 | 2001-09-29 | 추후제출 | 퀴나졸린 유도체 |
| DE102007032349A1 (de) * | 2007-07-11 | 2009-01-15 | Bayer Healthcare Ag | Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung |
| KR101790255B1 (ko) * | 2009-12-23 | 2017-10-26 | 다케다 야쿠힌 고교 가부시키가이샤 | Ｓｙｋ 억제제로서의 융합된 헤테로방향족 피롤리디논 |
| EP2526102B1 (en) * | 2010-01-22 | 2017-03-08 | Fundación Centro Nacional de Investigaciones Oncológicas Carlos III | Inhibitors of PI3 kinase |
| UY33213A (es) * | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| US20110241987A1 (en) * | 2010-04-01 | 2011-10-06 | Smart Technologies Ulc | Interactive input system and information input method therefor |
| NZ603446A (en) * | 2010-04-14 | 2014-05-30 | Array Biopharma Inc | 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases |
| CN103987713A (zh) * | 2011-10-12 | 2014-08-13 | 阵列生物制药公司 | 5,7-取代的咪唑并[1,2-c]嘧啶 |
| WO2013143663A1 (en) * | 2012-03-28 | 2013-10-03 | Merck Patent Gmbh | Bicyclic pyrazinone derivatives |
| PL3227297T3 (pl) | 2014-12-05 | 2021-10-25 | Array Biopharma, Inc. | 4,6 podstawione-pyrazolo[1,5-a]pirazyny jako inhibitory kinaz janusowych |
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2019
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