MD3419978T2 - Derivaţi de pirazolo[1,5-a]pirazin-4-il - Google Patents
Derivaţi de pirazolo[1,5-a]pirazin-4-ilInfo
- Publication number
- MD3419978T2 MD3419978T2 MDE20190031T MDE20190031T MD3419978T2 MD 3419978 T2 MD3419978 T2 MD 3419978T2 MD E20190031 T MDE20190031 T MD E20190031T MD E20190031 T MDE20190031 T MD E20190031T MD 3419978 T2 MD3419978 T2 MD 3419978T2
- Authority
- MD
- Moldova
- Prior art keywords
- alkyl
- hydroxy
- cycloalkyl
- independently represent
- halo
- Prior art date
Links
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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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
-
- 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
- A61P37/02—Immunomodulators
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
Abstract
Se propune un compus având structura (I) sau o sare farmaceutic acceptabilă a acestuia, sau un solvat farmaceutic acceptabil al compusului menţionat sau o sare farmaceutic acceptabilă, în care: A, A' şi A'' independent reprezintă O, C=O, C- R' sau N-R», în care R' şi R» independent pot reprezenta H, amino, -NR7COR6, COR6, -CONR7R8, C1-C6 alchil sau hidroxi(C1-C6 alchil) şi R» poate fi prezent sau absent, şi este prezent acolo unde regulile de valenţă permit şi unde nu mai mult de unul dintre A, A' şi A» reprezintă O sau C=O; Ro şi R independent reprezintă H, Br, CI, F sau C1-C6 alchil; R1 reprezintă H, C1-C6 alchil sau hidroxi(C1-C6 alchil); R2 se selectează din grupa constând din H, C1-C6 alchil, C1-C6 alcoxi, hidroxi(C1-C6 alchil), fenil(C1-C6 alchil), formil, heteroaril, heterociclic, -COR6, -OCOR6, -COOR6, -NR7COR6, -CONR7R8 şi -(CH2)n-W, în care W reprezintă cian, hidroxi, C3-C8 cicloalchil, -SO2NR7R8 şi -SO2-R9, în care R9 reprezintă C1-C6 alchil, C3-C8 cicloalchil, heteroaril sau heterociclic; în care fiecare dintre alchil, cicloalchil, heterociclic sau heteroaril menţionat poate fi substituit sau nesubstituit cu halo, cian, hidroxi sau C1-C6 alchil; X reprezintă C-R3 sau N, în care R3 poate fi H sau C1-C6 alchil; R4 şi R5 independent reprezintă H, amino, C1-C6 alchil sau hidroxi(C1-C6 alchil); R6, R7 şi R8 fiecare independent reprezintă H, C1-C6 alchil, C1-C4 alcoxi(C1-C6 alchil) sau C3-C8 cicloalchil, C1-C6 alchil menţionat este substituit opţional cu halo, CN sau hidroxi; sau R7 şi R8 împreună cu atomul legat de acesta formează un inel cu 5- sau 6- membri, inelul menţionat fiind opţional substituit cu halo, hidroxi, CN sau C1-C6 alchil; şi n este 0, 1, 2 sau 3. Sunt propuse, de asemenea, metode de tratament în calitate de inhibitori ai kinazei Janus şi compoziţii farmaceutice care conţin compuşii invenţiei şi combinaţii ale acestora cu alţi agenţi terapeutici.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662299130P | 2016-02-24 | 2016-02-24 | |
| PCT/IB2017/050748 WO2017144995A1 (en) | 2016-02-24 | 2017-02-10 | Pyrazolo[1,5-a]pyrazin-4-yl derivatives as jak-inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MD3419978T2 true MD3419978T2 (ro) | 2020-07-31 |
Family
ID=58054385
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDE20190031T MD3419978T2 (ro) | 2016-02-24 | 2017-02-10 | Derivaţi de pirazolo[1,5-a]pirazin-4-il |
Country Status (45)
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CO2018008799A2 (es) | 2016-02-24 | 2018-09-20 | Pfizer | Derivados de pirazolo[1,5-a]pirazin-4-ilo como inhibidores de jak |
| PE20211001A1 (es) | 2018-02-27 | 2021-06-01 | Incyte Corp | Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b |
| AR117398A1 (es) * | 2018-03-12 | 2021-08-04 | Abbvie Inc | Inhibidores de la señalización mediada por tirosina cinasa 2 |
| US20220324865A1 (en) | 2018-05-17 | 2022-10-13 | Bayer Aktiengesellschaft | Substituted dihydropyrazolo pyrazine carboxamide derivatives |
| JP7391046B2 (ja) | 2018-05-18 | 2023-12-04 | インサイト・コーポレイション | Ａ２ａ／ａ２ｂ阻害剤としての縮合ピリミジン誘導体 |
| TW202033198A (zh) | 2018-10-17 | 2020-09-16 | 美商美國禮來大藥廠 | 以巴瑞克替尼(baricitinib)治療原發性膽汁性膽管炎及原發性硬化性膽管炎 |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及***并吡啶 |
| 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 |
| IL287665A (en) | 2019-04-30 | 2022-07-01 | Celgene Corp | Combined treatments including apremilaste and tyk2 inhibitors |
| AU2020347561A1 (en) * | 2019-09-11 | 2022-04-14 | Pfizer Inc. | Treatment of hidradenitis with JAK inhibitors |
| TW202135816A (zh) * | 2019-12-18 | 2021-10-01 | 美商輝瑞股份有限公司 | 以激酶抑制劑治療潰瘍性結腸炎 |
| CA3177852A1 (en) | 2020-04-04 | 2021-10-07 | Pfizer Inc. | Methods of treating coronavirus disease 2019 |
| US20230159539A1 (en) * | 2020-04-08 | 2023-05-25 | Pfizer Inc. | Crystalline forms of 3-cyano-1-[4-[6-(1-methyl-1h-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]-1h-pyrazol-1-yl]cyclobutaneacetonitrile, and use thereof |
| WO2022056196A1 (en) * | 2020-09-11 | 2022-03-17 | Pulmosim Therapeutics Llc | Compositions and methods for treating or preventing pulmonary hypertension |
| CN112592345A (zh) * | 2020-12-07 | 2021-04-02 | 嘉兴特科罗生物科技有限公司 | 一种三氮唑并吡嗪类化合物及其用途 |
| EP4284802A1 (en) * | 2021-02-01 | 2023-12-06 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
| JP2022155540A (ja) | 2021-03-30 | 2022-10-13 | ファイザー・インク | 白斑を処置するための方法 |
| WO2023076161A1 (en) | 2021-10-25 | 2023-05-04 | Kymera Therapeutics, Inc. | Tyk2 degraders and uses thereof |
| WO2023083200A1 (zh) * | 2021-11-12 | 2023-05-19 | 南京明德新药研发有限公司 | 吡唑并环化合物及其应用 |
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| US8895745B2 (en) | 2006-12-22 | 2014-11-25 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as FGFR inhibitors |
| AR066879A1 (es) * | 2007-06-08 | 2009-09-16 | Novartis Ag | Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus |
| CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| PE20140407A1 (es) | 2008-06-10 | 2014-04-25 | Abbott Lab | Nuevos compuestos triciclicos |
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| EP2397482A1 (en) | 2010-06-15 | 2011-12-21 | Almirall, S.A. | Heteroaryl imidazolone derivatives as jak inhibitors |
| KR20140076619A (ko) | 2011-10-12 | 2014-06-20 | 어레이 바이오파마 인크. | 5,7-치환된-이미다조[1,2-c]피리미딘 |
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| EP3394066A2 (en) | 2015-12-22 | 2018-10-31 | H. Hoffnabb-La Roche Ag | PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS |
| CO2018008799A2 (es) | 2016-02-24 | 2018-09-20 | Pfizer | Derivados de pirazolo[1,5-a]pirazin-4-ilo como inhibidores de jak |
| AU2017395023B2 (en) | 2016-12-23 | 2022-04-07 | Plexxikon Inc. | Compounds and methods for CDK8 modulation and indications therefor |
| WO2018136661A1 (en) | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
| WO2018234342A1 (en) | 2017-06-21 | 2018-12-27 | F. Hoffmann-La Roche Ag | ISOINDOLINONE DERIVATIVES AS MODULATORS OF IRAK4 |
| US11254668B2 (en) | 2017-08-14 | 2022-02-22 | Pfizer Inc. | Pyrazolo[1,5-A]pyrazin-4-yl and related derivatives |
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2017
- 2017-02-10 CO CONC2018/0008799A patent/CO2018008799A2/es unknown
- 2017-02-10 CU CU2018000078A patent/CU24511B1/es unknown
- 2017-02-10 WO PCT/IB2017/050748 patent/WO2017144995A1/en active Application Filing
- 2017-02-10 PT PT177057056T patent/PT3419978T/pt unknown
- 2017-02-10 SI SI201730289T patent/SI3419978T1/sl unknown
- 2017-02-10 RS RS20200584A patent/RS60261B1/sr unknown
- 2017-02-10 EP EP20168877.7A patent/EP3712153B1/en active Active
- 2017-02-10 DK DK17705705.6T patent/DK3419978T3/da active
- 2017-02-10 KR KR1020187024431A patent/KR102128671B1/ko active IP Right Grant
- 2017-02-10 MD MDE20190031T patent/MD3419978T2/ro unknown
- 2017-02-10 CN CN201780013165.4A patent/CN109071546B/zh active Active
- 2017-02-10 NZ NZ744349A patent/NZ744349A/en unknown
- 2017-02-10 CR CR20180372A patent/CR20180372A/es unknown
- 2017-02-10 JP JP2018544300A patent/JP6505956B2/ja active Active
- 2017-02-10 LT LTEP17705705.6T patent/LT3419978T/lt unknown
- 2017-02-10 GE GEAP201714864A patent/GEP20217242B/en unknown
- 2017-02-10 EA EA201891463A patent/EA035036B1/ru unknown
- 2017-02-10 RU RU2018130547A patent/RU2718902C2/ru active
- 2017-02-10 UA UAA201808148A patent/UA119835C2/uk unknown
- 2017-02-10 ME MEP-2020-97A patent/ME03743B/me unknown
- 2017-02-10 ES ES17705705T patent/ES2794779T3/es active Active
- 2017-02-10 EP EP17705705.6A patent/EP3419978B1/en active Active
- 2017-02-10 MX MX2018010236A patent/MX2018010236A/es unknown
- 2017-02-10 MY MYPI2018702937A patent/MY189118A/en unknown
- 2017-02-10 MA MA43668A patent/MA43668B1/fr unknown
- 2017-02-10 TN TNP/2018/000295A patent/TN2018000295A1/en unknown
- 2017-02-10 AU AU2017222417A patent/AU2017222417B2/en active Active
- 2017-02-10 PL PL17705705T patent/PL3419978T3/pl unknown
- 2017-02-10 HU HUE17705705A patent/HUE049305T2/hu unknown
- 2017-02-10 MA MA052987A patent/MA52987A/fr unknown
- 2017-02-10 SG SG11201806307YA patent/SG11201806307YA/en unknown
- 2017-02-21 US US15/437,618 patent/US10144738B2/en active Active
- 2017-02-21 CA CA2958490A patent/CA2958490C/en active Active
- 2017-02-21 TW TW106105777A patent/TWI665201B/zh active
- 2017-02-22 UY UY0001037133A patent/UY37133A/es unknown
- 2017-02-23 AR ARP170100462A patent/AR107714A1/es unknown
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2018
- 2018-07-18 SV SV2018005726A patent/SV2018005726A/es unknown
- 2018-07-24 ZA ZA2018/04972A patent/ZA201804972B/en unknown
- 2018-08-01 IL IL260923A patent/IL260923B/en unknown
- 2018-08-03 NI NI201800080A patent/NI201800080A/es unknown
- 2018-08-17 CL CL2018002358A patent/CL2018002358A1/es unknown
- 2018-08-23 PH PH12018501788A patent/PH12018501788A1/en unknown
- 2018-08-24 DO DO2018000187A patent/DOP2018000187A/es unknown
- 2018-09-24 EC ECSENADI201872109A patent/ECSP18072109A/es unknown
- 2018-11-06 US US16/181,596 patent/US10822341B2/en active Active
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2019
- 2019-01-14 HK HK19100512.8A patent/HK1258157A1/zh unknown
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2020
- 2020-05-13 HR HRP20200781TT patent/HRP20200781T1/hr unknown
- 2020-05-15 CY CY20201100470T patent/CY1122949T1/el unknown
- 2020-09-08 US US17/014,533 patent/US11472809B2/en active Active
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2022
- 2022-09-07 US US17/939,375 patent/US20230045252A1/en active Pending
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