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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- A61P37/00—Drugs for immunological or allergic disorders
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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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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
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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 |
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| ES2865483T3 true ES2865483T3 (es) | 2021-10-15 |
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| CN107278203B (zh) | 2014-12-05 | 2020-05-19 | 阵列生物制药公司 | 作为JANUS激酶抑制剂的4,6-取代的吡唑并[1,5-a]吡嗪 |
| CN109071546B (zh) * | 2016-02-24 | 2021-03-02 | 辉瑞大药厂 | 作为jak抑制剂的吡唑并[1,5-a]吡嗪-4-基衍生物 |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| SMT202100699T1 (it) | 2016-06-16 | 2022-01-10 | Denali Therapeutics Inc | Pirimidin-2-ilammino-1h-pirazoli come inibitori di lrrk2 per l'uso nel trattamento di disturbi neurodegenerativi |
| GB201617758D0 (en) * | 2016-10-20 | 2016-12-07 | Almac Discovery Limited | Pharmaceutical compounds |
| WO2018136661A1 (en) * | 2017-01-18 | 2018-07-26 | Andrews Steven W | 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 |
| WO2019034973A1 (en) | 2017-08-14 | 2019-02-21 | Pfizer Inc. | PYRAZOLO [1,5-A] PYRAZIN-4-YL AND RELATED DERIVATIVES |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| JP7060694B2 (ja) | 2018-01-18 | 2022-04-26 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピロロ［２，３－ｄ］ピリミジン化合物 |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine 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 |
| US12404275B2 (en) | 2019-04-12 | 2025-09-02 | Primegene (Beijing) Co., Ltd. | Pyrazolopyrazine derived compounds, pharmaceutical composition and use thereof |
| WO2020232247A1 (en) | 2019-05-14 | 2020-11-19 | Provention Bio, Inc. | Methods and compositions for preventing type 1 diabetes |
| 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 |
| IL297050A (en) | 2020-04-04 | 2022-12-01 | Pfizer | Methods of treating the 2019 corona virus disease |
| IL298999A (en) | 2020-06-11 | 2023-02-01 | Provention Bio Inc | Methods and compositions for the prevention of type 1 diabetes |
| JP2024520444A (ja) | 2021-05-24 | 2024-05-24 | プロヴェンション・バイオ・インコーポレイテッド | １型糖尿病を治療するための方法 |
| KR20240103022A (ko) * | 2021-11-12 | 2024-07-03 | 소테르 바이오파마 피티이. 리미티드 | 피라졸로 융합 고리 화합물 및 이의 용도 |
| EP4711367A1 (en) * | 2023-05-12 | 2026-03-18 | CMS Research & Development Pte. Ltd. | Pyrazolopyrazine compound and method for preparing crystal form thereof |
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| DE102007032349A1 (de) * | 2007-07-11 | 2009-01-15 | Bayer Healthcare Ag | Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung |
| NZ601267A (en) | 2009-12-23 | 2014-03-28 | Takeda Pharmaceutical | Fused heteroaromatic pyrrolidinones as syk inhibitors |
| US9073927B2 (en) * | 2010-01-22 | 2015-07-07 | Fundacion Centro Nacional De Investigaciones Oncologicas 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 |
| KR20130094710A (ko) | 2010-04-14 | 2013-08-26 | 어레이 바이오파마 인크. | Ｊａｋ 키나아제의 억제제로서 5,7-치환된-이미다조［1,2-ｃ］피리미딘 |
| 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 |
| CA2868620C (en) * | 2012-03-28 | 2020-02-25 | Dieter Dorsch | Bicyclic pyrazinone derivatives |
| CN107278203B (zh) | 2014-12-05 | 2020-05-19 | 阵列生物制药公司 | 作为JANUS激酶抑制剂的4,6-取代的吡唑并[1,5-a]吡嗪 |
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