RU2021102805A - 4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ - Google Patents
4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ Download PDFInfo
- Publication number
- RU2021102805A RU2021102805A RU2021102805A RU2021102805A RU2021102805A RU 2021102805 A RU2021102805 A RU 2021102805A RU 2021102805 A RU2021102805 A RU 2021102805A RU 2021102805 A RU2021102805 A RU 2021102805A RU 2021102805 A RU2021102805 A RU 2021102805A
- Authority
- RU
- Russia
- Prior art keywords
- pyrazines
- inhibitors
- janus kinase
- substituted pyrazolo
- pyrazol
- Prior art date
Links
- 102000015617 Janus Kinases Human genes 0.000 title 1
- 108010024121 Janus Kinases Proteins 0.000 title 1
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- JTBCMVGGBDUBFT-QGZVFWFLSA-N (2R)-3-[4-[4-(1-pentan-3-ylpyrazol-4-yl)pyrazolo[1,5-a]pyrazin-6-yl]pyrazol-1-yl]propane-1,2-diol Chemical compound CCC(CC)N1N=CC(=C1)C=1C=2N(C=C(N=1)C=1C=NN(C=1)C[C@H](CO)O)N=CC=2 JTBCMVGGBDUBFT-QGZVFWFLSA-N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
Classifications
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
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- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Child & Adolescent Psychology (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Transplantation (AREA)
- Emergency Medicine (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
Claims (4)
1. (R)-3-(4-(4-(1-(пентан-3-ил)-1H-пиразол-4-ил)пиразоло[1,5-a]пиразин-6-ил)-1H-пиразол-1-ил)пропан-1,2-диол или его фармацевтически приемлемая соль.
2. Соединение, имеющее формулу:
3. Применение (R)-3-(4-(4-(1-(пентан-3-ил)-1H-пиразол-4-ил)пиразоло[1,5-a]пиразин-6-ил)-1H-пиразол-1-ил)пропан-1,2-диола или его фармацевтически приемлемой соли для изготовления лекарственного среддства дл лечения заболевания или расстройства, связанного с киназой JAK.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462088068P | 2014-12-05 | 2014-12-05 | |
| US62/088,068 | 2014-12-05 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017123387A Division RU2742938C2 (ru) | 2014-12-05 | 2015-12-04 | 4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2021102805A true RU2021102805A (ru) | 2021-02-12 |
Family
ID=55069089
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017123387A RU2742938C2 (ru) | 2014-12-05 | 2015-12-04 | 4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ |
| RU2021102805A RU2021102805A (ru) | 2014-12-05 | 2015-12-04 | 4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017123387A RU2742938C2 (ru) | 2014-12-05 | 2015-12-04 | 4,6-ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US10189845B2 (ru) |
| EP (2) | EP3227297B1 (ru) |
| JP (2) | JP6641373B2 (ru) |
| KR (1) | KR20170090476A (ru) |
| CN (1) | CN107278203B (ru) |
| AU (1) | AU2015357585B2 (ru) |
| BR (1) | BR112017011798A2 (ru) |
| CA (1) | CA2969709A1 (ru) |
| CL (1) | CL2017001422A1 (ru) |
| CO (1) | CO2017006674A2 (ru) |
| CR (1) | CR20170309A (ru) |
| DK (1) | DK3227297T3 (ru) |
| ES (1) | ES2865483T3 (ru) |
| HR (1) | HRP20210501T1 (ru) |
| HU (1) | HUE054371T2 (ru) |
| IL (1) | IL252656A0 (ru) |
| MX (1) | MX2017007284A (ru) |
| MY (1) | MY191016A (ru) |
| PH (1) | PH12017501032A1 (ru) |
| PL (1) | PL3227297T3 (ru) |
| PT (1) | PT3227297T (ru) |
| RS (1) | RS61693B1 (ru) |
| RU (2) | RU2742938C2 (ru) |
| SG (1) | SG11201704542SA (ru) |
| SI (1) | SI3227297T1 (ru) |
| TW (1) | TWI725004B (ru) |
| UA (1) | UA120065C2 (ru) |
| WO (1) | WO2016090285A1 (ru) |
| ZA (1) | ZA201704494B (ru) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY191016A (en) | 2014-12-05 | 2022-05-28 | Array Biopharma Inc | 4,6-substituted-pyrazolo[1,5-a]pyrazines as janus kinase inhibitors |
| WO2017144995A1 (en) * | 2016-02-24 | 2017-08-31 | Pfizer Inc. | Pyrazolo[1,5-a]pyrazin-4-yl derivatives as jak-inhibitors |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| 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 |
| JP6888101B2 (ja) * | 2017-01-18 | 2021-06-16 | 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ラゾロ［１，５−ａ］ピラジン化合物 |
| US20200157081A1 (en) * | 2017-05-24 | 2020-05-21 | 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 |
| WO2019143991A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
| CN111971286B (zh) | 2018-01-18 | 2023-04-14 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物 |
| CA3111984A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| CA3136468A1 (en) * | 2019-04-12 | 2020-10-15 | Primegene (Beijing) Co., Ltd. | Pyrazolopyrazine derived compounds and pharmaceutical compositions used as jak inhibitors |
| KR20230031981A (ko) | 2019-05-14 | 2023-03-07 | 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 |
| CN115715194A (zh) | 2020-04-04 | 2023-02-24 | 辉瑞公司 | 治疗冠状病毒疾病2019的方法 |
| KR20230092863A (ko) | 2020-06-11 | 2023-06-26 | 프로벤션 바이오, 인코포레이티드 | 제1형 당뇨병을 예방하기 위한 방법 및 조성물 |
| CN118317960A (zh) * | 2021-11-12 | 2024-07-09 | 海南康哲美丽科技有限公司 | 吡唑并环化合物及其应用 |
| 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 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA01001893A (es) | 1998-08-21 | 2002-04-24 | Parker Hughes Inst | Derivados de quinazolina. |
| DE102007032349A1 (de) | 2007-07-11 | 2009-01-15 | Bayer Healthcare Ag | Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung |
| GEP20156243B (en) * | 2009-12-23 | 2015-02-10 | 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 |
| NZ603446A (en) * | 2010-04-14 | 2014-05-30 | Array Biopharma Inc | 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases |
| JP2014528475A (ja) * | 2011-10-12 | 2014-10-27 | アレイ バイオファーマ、インコーポレイテッド | ５，７置換イミダゾ［１，２−ｃ］ピリミジン |
| EA027416B1 (ru) * | 2012-03-28 | 2017-07-31 | Мерк Патент Гмбх | Бициклические пиразиноновые производные |
| MY191016A (en) | 2014-12-05 | 2022-05-28 | Array Biopharma Inc | 4,6-substituted-pyrazolo[1,5-a]pyrazines as janus kinase inhibitors |
-
2015
- 2015-12-04 MY MYPI2017702034A patent/MY191016A/en unknown
- 2015-12-04 EP EP15819933.1A patent/EP3227297B1/en active Active
- 2015-12-04 WO PCT/US2015/064062 patent/WO2016090285A1/en active Application Filing
- 2015-12-04 TW TW104140878A patent/TWI725004B/zh not_active IP Right Cessation
- 2015-12-04 HU HUE15819933A patent/HUE054371T2/hu unknown
- 2015-12-04 US US15/532,937 patent/US10189845B2/en active Active
- 2015-12-04 RU RU2017123387A patent/RU2742938C2/ru active
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