MX2017007284A - Pirazolo [1,5-a] pirazinas 4,6-sustituidas como inhibidores de janus cinasas. - Google Patents
Pirazolo [1,5-a] pirazinas 4,6-sustituidas como inhibidores de janus cinasas.Info
- Publication number
- MX2017007284A MX2017007284A MX2017007284A MX2017007284A MX2017007284A MX 2017007284 A MX2017007284 A MX 2017007284A MX 2017007284 A MX2017007284 A MX 2017007284A MX 2017007284 A MX2017007284 A MX 2017007284A MX 2017007284 A MX2017007284 A MX 2017007284A
- Authority
- MX
- Mexico
- Prior art keywords
- pyrazines
- pyrazolo
- substituted
- kinase inhibitors
- janus kinase
- Prior art date
Links
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 title 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 102000042838 JAK family Human genes 0.000 abstract 1
- 102000015617 Janus Kinases Human genes 0.000 abstract 1
- 108010024121 Janus Kinases Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 208000014951 hematologic disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 210000000056 organ Anatomy 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 238000002054 transplantation Methods 0.000 abstract 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
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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
- A61K31/535—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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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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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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
- A61P37/02—Immunomodulators
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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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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
Abstract
Compuestos de Fórmula I: y estereoisómeros y sales solvatos farmacéuticamente aceptables de estos en los que R1, R2, R3 y R4 tienen los significados dados en la memoria descriptiva, son inhibidores de una o más JAK cinasas y son útiles en el tratamiento de enfermedades y trastornos relacionados con la JAK cinasa, tales como enfermedades autoinmunitarias, rechazo del trasplante de órganos, tejidos y células, así como también neoplasias y trastornos hematológicos y sus comorbilidades.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 (2)
| Publication Number | Publication Date |
|---|---|
| MX2017007284A true MX2017007284A (es) | 2017-08-25 |
| MX386316B MX386316B (es) | 2025-03-18 |
Family
ID=55069089
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017007284A MX386316B (es) | 2014-12-05 | 2015-12-04 | Pirazolo [1,5-a] pirazinas 4,6-sustituidas como inhibidores de janus cinasas. |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US10189845B2 (es) |
| EP (2) | EP3878451A1 (es) |
| JP (2) | JP6641373B2 (es) |
| KR (1) | KR20170090476A (es) |
| CN (1) | CN107278203B (es) |
| AU (1) | AU2015357585B2 (es) |
| BR (1) | BR112017011798A2 (es) |
| CA (1) | CA2969709A1 (es) |
| CL (1) | CL2017001422A1 (es) |
| CO (1) | CO2017006674A2 (es) |
| CR (1) | CR20170309A (es) |
| DK (1) | DK3227297T3 (es) |
| ES (1) | ES2865483T3 (es) |
| HR (1) | HRP20210501T1 (es) |
| HU (1) | HUE054371T2 (es) |
| IL (1) | IL252656A0 (es) |
| MX (1) | MX386316B (es) |
| MY (1) | MY191016A (es) |
| PH (1) | PH12017501032A1 (es) |
| PL (1) | PL3227297T3 (es) |
| PT (1) | PT3227297T (es) |
| RS (1) | RS61693B1 (es) |
| RU (2) | RU2742938C2 (es) |
| SG (1) | SG11201704542SA (es) |
| SI (1) | SI3227297T1 (es) |
| TW (1) | TWI725004B (es) |
| UA (1) | UA120065C2 (es) |
| WO (1) | WO2016090285A1 (es) |
| ZA (1) | ZA201704494B (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016090285A1 (en) | 2014-12-05 | 2016-06-09 | Array Biopharma Inc. | 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS |
| CR20180372A (es) * | 2016-02-24 | 2018-09-19 | Pfizer | Derivados de pirazolo [1,5-a] pirazin-4-ilo |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| PE20240221A1 (es) | 2016-06-16 | 2024-02-16 | 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 |
| CN110267960B (zh) * | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
| WO2018217946A1 (en) * | 2017-05-24 | 2018-11-29 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| US11254668B2 (en) | 2017-08-14 | 2022-02-22 | Pfizer Inc. | Pyrazolo[1,5-A]pyrazin-4-yl and related derivatives |
| US11603374B2 (en) | 2018-01-18 | 2023-03-14 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CA3087972C (en) | 2018-01-18 | 2023-01-10 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | 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 |
| AU2020256720B2 (en) * | 2019-04-12 | 2022-09-01 | PrimeGene (Beijing) Co. Ltd. | Pyrazolopyrazine derived compounds, pharmaceutical composition and use thereof |
| 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 |
| AU2021248720A1 (en) | 2020-04-04 | 2022-11-03 | 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 |
| US20250011332A1 (en) * | 2021-11-12 | 2025-01-09 | 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 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6313129B1 (en) | 1998-08-21 | 2001-11-06 | Hughes Institute | Therapeutic compounds |
| DE102007032349A1 (de) * | 2007-07-11 | 2009-01-15 | Bayer Healthcare Ag | Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung |
| US8440689B2 (en) * | 2009-12-23 | 2013-05-14 | Takeda Pharmaceutical Company Limited | Fused heteroaromatic pyrrolidinones |
| 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 |
| CA2796388A1 (en) * | 2010-04-14 | 2011-10-20 | Array Biopharma Inc. | 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases |
| BR112014008865A2 (pt) * | 2011-10-12 | 2017-04-25 | Array Biopharma Inc | imidazo[1,2-c]pirimidinas 5,7-substituídas |
| EA027416B1 (ru) * | 2012-03-28 | 2017-07-31 | Мерк Патент Гмбх | Бициклические пиразиноновые производные |
| WO2016090285A1 (en) | 2014-12-05 | 2016-06-09 | Array Biopharma Inc. | 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS |
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2015
- 2015-12-04 WO PCT/US2015/064062 patent/WO2016090285A1/en not_active Ceased
- 2015-12-04 ES ES15819933T patent/ES2865483T3/es active Active
- 2015-12-04 MX MX2017007284A patent/MX386316B/es unknown
- 2015-12-04 HR HRP20210501TT patent/HRP20210501T1/hr unknown
- 2015-12-04 JP JP2017529681A patent/JP6641373B2/ja not_active Expired - Fee Related
- 2015-12-04 EP EP21152373.3A patent/EP3878451A1/en not_active Withdrawn
- 2015-12-04 HU HUE15819933A patent/HUE054371T2/hu unknown
- 2015-12-04 AU AU2015357585A patent/AU2015357585B2/en not_active Ceased
- 2015-12-04 CN CN201580066136.5A patent/CN107278203B/zh not_active Expired - Fee Related
- 2015-12-04 SG SG11201704542SA patent/SG11201704542SA/en unknown
- 2015-12-04 UA UAA201707008A patent/UA120065C2/uk unknown
- 2015-12-04 SI SI201531544T patent/SI3227297T1/sl unknown
- 2015-12-04 US US15/532,937 patent/US10189845B2/en active Active
- 2015-12-04 CR CR20170309A patent/CR20170309A/es unknown
- 2015-12-04 CA CA2969709A patent/CA2969709A1/en not_active Abandoned
- 2015-12-04 BR BR112017011798A patent/BR112017011798A2/pt not_active IP Right Cessation
- 2015-12-04 DK DK15819933.1T patent/DK3227297T3/da active
- 2015-12-04 KR KR1020177018122A patent/KR20170090476A/ko not_active Withdrawn
- 2015-12-04 MY MYPI2017702034A patent/MY191016A/en unknown
- 2015-12-04 EP EP15819933.1A patent/EP3227297B1/en active Active
- 2015-12-04 RS RS20210415A patent/RS61693B1/sr unknown
- 2015-12-04 RU RU2017123387A patent/RU2742938C2/ru active
- 2015-12-04 RU RU2021102805A patent/RU2021102805A/ru unknown
- 2015-12-04 PL PL15819933T patent/PL3227297T3/pl unknown
- 2015-12-04 TW TW104140878A patent/TWI725004B/zh not_active IP Right Cessation
- 2015-12-04 PT PT158199331T patent/PT3227297T/pt unknown
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2017
- 2017-06-02 PH PH12017501032A patent/PH12017501032A1/en unknown
- 2017-06-04 IL IL252656A patent/IL252656A0/en active IP Right Grant
- 2017-06-05 CL CL2017001422A patent/CL2017001422A1/es unknown
- 2017-06-30 CO CONC2017/0006674A patent/CO2017006674A2/es unknown
- 2017-07-03 ZA ZA2017/04494A patent/ZA201704494B/en unknown
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2018
- 2018-12-06 US US16/212,493 patent/US10730880B2/en active Active
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2019
- 2019-12-11 JP JP2019223760A patent/JP2020055859A/ja active Pending
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2020
- 2020-06-02 US US16/890,663 patent/US11028093B2/en active Active
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| EA202192822A1 (ru) | Нафтиридиновые соединения в качестве ингибиторов jak киназы |