MA43668B1 - Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jak - Google Patents
Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jakInfo
- Publication number
- MA43668B1 MA43668B1 MA43668A MA43668A MA43668B1 MA 43668 B1 MA43668 B1 MA 43668B1 MA 43668 A MA43668 A MA 43668A MA 43668 A MA43668 A MA 43668A MA 43668 B1 MA43668 B1 MA 43668B1
- Authority
- MA
- Morocco
- Prior art keywords
- alkyl
- group
- hydroxy
- independently
- cycloalkyl
- 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
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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
- A61P17/06—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
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- 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
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- 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
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- 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]
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- 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
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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
- A61P37/02—Immunomodulators
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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
- A61P37/02—Immunomodulators
- 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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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Gastroenterology & Hepatology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Transplantation (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La présente invention concerne un composé de structure (i) ou son sel pharmaceutiquement acceptable, ou un solvate pharmaceutiquement acceptable dudit composé ou sel pharmaceutiquement acceptable, a, a' et a'' étant indépendamment o, c=o, c-r' ou n-r'', où r' et r'' peuvent indépendamment être h, un groupe amino, -nr7cor6, cor6, -conr7r8, un groupe alkyle en c1 à c6, ou un groupe hydroxy(alkyle en c1 à c6), et r'' peut être présent ou absent, et est présent où les règles de valence le permettent, et où pas plus d'un de a, a' et a'' est o ou un groupe c=o ; r0 et r sont indépendamment h, br, cl, f, ou un groupe alkyle en c1 à c6 ; r1 est h, un groupe alkyle en c1 à c6, ou un groupe hydroxy(alkyle en c1 à c6) ; r2 est sélectionné dans le groupe constitué de h, du groupe alkyle en c1 à c6, alcoxy en c1 à c6, hydroxy(alkyle en c1 à c6), phényl(alkyle en c1 à c6), formyle, hétéroaryle, hétérocyclique, -cor6, -ocor6, -coor6, -nr7cor6, -conr7r8, et -(ch2)n-w, où w est un groupe cyano, hydroxy, cycloalkyle en c3 à c8, -so2nr7r8, et -so2-r9, où r9 est un groupe alkyle en c1 à c6, cycloalkyle en c3 à c8, hétéroaryle, ou hétérocyclique ; où chacun dudit groupe alkyle, cycloalkyle, hétérocyclique, ou hétéroaryle peut être non substitué ou substitué par un groupe halogéno, cyano, hydroxy, ou alkyle en c1 à c6 ; x est un groupe c-r3 ou n, où r3 peut être h ou un groupe alkyle en c1 à c6 ; r4 et r5 sont indépendamment h, un groupe amino, alkyle en c1 à c6, ou hydroxy(alkyle en c1 à c6) ; r6, r7 et r8 sont chacun indépendamment h, un groupe alkyle en c1 à c6, alcoxy en c1 à c4(alkyle en c1 à c6), ou cycloalkyle en c3 à c8, ledit groupe alkyle en c1 à c6 est éventuellement substitué par un groupe halogéno, cn ou hydroxy ; où, r7 et r8 conjointement à l'atome lié à celui-ci forment un cycle à 5 ou 6 chaînons, ledit cycle étant éventuellement substitué par un groupe halogéno, hydroxy, cn, ou alkyle en c1 à c6 ; et, n à la valeur de 0, 1, 2 ou 3. Sont également décrits des procédés de traitement comme inhibiteurs de janus kinases et des compositions pharmaceutiques contenant les composés de l'invention et leurs combinaisons avec d'autres agents thérapeutiques.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662299130P | 2016-02-24 | 2016-02-24 | |
| PCT/IB2017/050748 WO2017144995A1 (fr) | 2016-02-24 | 2017-02-10 | Dérivés pyrazolo[1,5-a]pyrazin-4-yle comme inhibiteurs jac |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MA43668B1 true MA43668B1 (fr) | 2020-05-29 |
Family
ID=58054385
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA43668A MA43668B1 (fr) | 2016-02-24 | 2017-02-10 | Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jak |
| MA052987A MA52987A (fr) | 2016-02-24 | 2017-02-10 | Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jak |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA052987A MA52987A (fr) | 2016-02-24 | 2017-02-10 | Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jak |
Country Status (45)
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6505956B2 (ja) | 2016-02-24 | 2019-04-24 | ファイザー・インク | ＪＡＫ阻害剤としてのピラゾロ［１，５−ａ］ピラジン−４−イル誘導体 |
| US20190292188A1 (en) | 2018-02-27 | 2019-09-26 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors |
| UY38144A (es) | 2018-03-12 | 2019-10-31 | Abbvie Inc | Inhibidores de la señalización mediada por tirosina cinasa |
| MX2020012201A (es) | 2018-05-17 | 2021-01-29 | Bayer Ag | Derivados sustituidos de la carboxamida dihidropirazolo pirazina. |
| CA3100731A1 (fr) | 2018-05-18 | 2019-11-21 | Incyte Corporation | Derives de pyrimidine fusionnes utilises en tant qu'inhibiteurs de a2a/a2b |
| CA3105721A1 (fr) | 2018-07-05 | 2020-01-09 | Incyte Corporation | Derives de pyrazine fusionnes en tant qu'inhibiteurs d'a2a/a2b |
| 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三唑并吡啶 |
| CN113924301A (zh) * | 2019-04-12 | 2022-01-11 | 北京普祺医药科技有限公司 | 一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途 |
| BR112021021809A2 (pt) | 2019-04-30 | 2022-01-04 | Celgene Corp | Terapias de combinação compreendendo os inibidores de apremilast e tyk2 |
| EP4028007A1 (fr) | 2019-09-11 | 2022-07-20 | Pfizer Inc. | Traitement de l'hidradénite avec des inhibiteurs de jak |
| WO2021124095A1 (fr) * | 2019-12-18 | 2021-06-24 | Pfizer Inc. | Traitement de la rectocolite hémorragique avec des inhibiteurs de kinase |
| CA3177852A1 (fr) | 2020-04-04 | 2021-10-07 | Pfizer Inc. | Procedes de traitement de la maladie a coronavirus 2019 |
| AU2021252213A1 (en) * | 2020-04-08 | 2022-11-03 | 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 |
| EP4210684A1 (fr) * | 2020-09-11 | 2023-07-19 | Pulmosim Therapeutics LLC | Compositions et méthodes de traitement ou de prévention de l'hypertension pulmonaire |
| 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 |
| WO2022165530A1 (fr) * | 2021-02-01 | 2022-08-04 | Janssen Biotech, Inc. | Inhibiteurs à petites molécules de kinases inductibles par le sel |
| WO2022208315A1 (fr) | 2021-03-30 | 2022-10-06 | Pfizer Inc. | Méthodes de traitement du vitiligo |
| CA3236262A1 (fr) | 2021-10-25 | 2023-05-04 | Isaac Marx | Agents de degradation de tyk2 et leurs utilisations |
| WO2023083200A1 (fr) * | 2021-11-12 | 2023-05-19 | 南京明德新药研发有限公司 | Composé à cycle condensé pyrazole et son utilisation |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
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| AU2007337886C1 (en) | 2006-12-22 | 2014-10-16 | 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. |
| KR20110017431A (ko) | 2008-06-10 | 2011-02-21 | 아보트 러보러터리즈 | 신규한 트리사이클릭 화합물 |
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| UY33213A (es) * | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
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| EP2397482A1 (fr) | 2010-06-15 | 2011-12-21 | Almirall, S.A. | Dérivés d'imidazolone d'hétéroaryle en tant qu'inhibiteurs de JAK |
| RU2014118954A (ru) * | 2011-10-12 | 2015-11-20 | Эррэй Биофарма Инк. | 5,7-ЗАМЕЩЕННЫЕ-ИМИДАЗО[1,2-c]ПИРИМИДИНЫ |
| US9120805B2 (en) | 2012-03-28 | 2015-09-01 | Merck Patent Gmbh | Substituted pyrrolo[1,2-A]pyrazin-1-ones and pyrazolo[1,5-A]pyrazin-4-ones as inhibitors of tankyrase and poly(ADP-ribose)polymerase activity |
| EP2832734A4 (fr) * | 2012-03-28 | 2015-08-26 | Takeda Pharmaceutical | Composé hétérocyclique |
| MX2016001427A (es) | 2013-07-31 | 2016-08-03 | Gilead Sciences Inc | Inhibidores de syk. |
| WO2015086693A1 (fr) | 2013-12-11 | 2015-06-18 | Almirall, S.A. | Dérivés de pyrazolopyrimidin-2-yle utilisés comme inhibiteurs de jak |
| WO2015166370A1 (fr) * | 2014-04-28 | 2015-11-05 | Pfizer Inc. | Composés hétéroaromatiques et leur utilisation en tant que ligands de la dopamine d1 |
| WO2016009028A1 (fr) | 2014-07-17 | 2016-01-21 | Valeo Systèmes d'Essuyage | Balai plat caréné d'essuie-glace |
| TWI725004B (zh) * | 2014-12-05 | 2021-04-21 | 美商亞雷生物製藥股份有限公司 | 4,6-經取代之吡唑并［1,5-ａ］吡 |
| WO2016119707A1 (fr) | 2015-01-29 | 2016-08-04 | Hutchison Medipharma Limited | Nouveaux composés hétéroaryliques et hétérocycliques, compositions et procédés |
| WO2016130920A2 (fr) | 2015-02-13 | 2016-08-18 | Dana-Farber Cancer Institute, Inc. | Inhibiteurs de lrrk2 et leurs méthodes de production et d'utilisation |
| GB201504565D0 (en) | 2015-03-18 | 2015-05-06 | Takeda Pharmaceutical | Novel compounds |
| MX370933B (es) | 2015-04-29 | 2020-01-09 | Wuxi Fortune Pharmaceuticals Co Ltd | Inhibidores jak. |
| CN108473498B (zh) | 2015-12-22 | 2021-11-02 | 豪夫迈·罗氏有限公司 | 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物 |
| JP6505956B2 (ja) | 2016-02-24 | 2019-04-24 | ファイザー・インク | ＪＡＫ阻害剤としてのピラゾロ［１，５−ａ］ピラジン−４−イル誘導体 |
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| JP2020524663A (ja) | 2017-06-21 | 2020-08-20 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｉｒａｋ４調節因子としてのイソインドリノン誘導体 |
| EP3668858A1 (fr) | 2017-08-14 | 2020-06-24 | Pfizer Inc | Pyrazolo[1,5-a]pyrazin-4-yl et dérivés associés |
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2017
- 2017-02-10 JP JP2018544300A patent/JP6505956B2/ja active Active
- 2017-02-10 MX MX2018010236A patent/MX2018010236A/es unknown
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- 2017-02-10 CU CU2018000078A patent/CU24511B1/es unknown
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- 2017-02-10 MA MA052987A patent/MA52987A/fr unknown
- 2017-02-10 HU HUE17705705A patent/HUE049305T2/hu unknown
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2018
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2019
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