MD4735B1 - Derivaţi ai pirolo[2,3-d]pirimidinei ca inhibitori de Kinaze Janus-asociate (JAK) - Google Patents
Derivaţi ai pirolo[2,3-d]pirimidinei ca inhibitori de Kinaze Janus-asociate (JAK) Download PDFInfo
- Publication number
- MD4735B1 MD4735B1 MDA20150073A MD20150073A MD4735B1 MD 4735 B1 MD4735 B1 MD 4735B1 MD A20150073 A MDA20150073 A MD A20150073A MD 20150073 A MD20150073 A MD 20150073A MD 4735 B1 MD4735 B1 MD 4735B1
- Authority
- MD
- Moldova
- Prior art keywords
- pyrimidine derivatives
- jak
- pyrrolo
- inhibitors
- janus
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000004943 pyrrolo[2,3-d]pyrimidines Chemical class 0.000 title abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- 102000015617 Janus Kinases Human genes 0.000 abstract 2
- 108010024121 Janus Kinases Proteins 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 0.000 abstract 1
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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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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- 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
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
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- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
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Abstract
Invenţia se referă la derivaţi ai pirolo[2,3-d]pirimidinei farmaceutic activi. Conform invenţiei, se revendică derivaţi ai pirolo[2,3-d]pirimidinei cu formula IA: De asemenea, se revendică utilizarea lor în calitate de inhibitori de Kinaze Janus (JAK) şi compoziţii farmaceutice care îi conţin.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361767947P | 2013-02-22 | 2013-02-22 | |
| PCT/IB2014/058889 WO2014128591A1 (en) | 2013-02-22 | 2014-02-11 | Pyrrolo [2, 3 -d]pyrimidine derivatives as inhibitors of janus- related kinases (jak) |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| MD20150073A2 MD20150073A2 (ro) | 2016-01-31 |
| MD4735B1 true MD4735B1 (ro) | 2020-12-31 |
| MD4735C1 MD4735C1 (ro) | 2021-07-31 |
Family
ID=50151346
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDA20150073A MD4735C1 (ro) | 2013-02-22 | 2014-02-11 | Derivaţi ai pirolo[2,3-d]pirimidinei ca inhibitori de Kinaze Janus-asociate (JAK) |
Country Status (47)
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2605652T3 (pl) | 2010-08-18 | 2018-04-30 | Samumed, Llc | Diketony i hydroksyketony jako aktywatory szlaku sygnalizacji kateninowej |
| AU2014209141B2 (en) | 2013-01-24 | 2018-05-10 | Palvella Therapeutics, Inc. | Compositions for transdermal delivery of mTOR inhibitors |
| PE20151721A1 (es) | 2013-02-22 | 2015-12-07 | Samumed Llc | Y-dicetonas como activadores de la ruta de senalizacion de wnt/b-catenina |
| EP3290421B1 (en) * | 2013-02-22 | 2019-01-02 | Pfizer Inc | Combination of pyrrolo [2, 3 -d]pyrimidine derivatives with one or more additional agents as inhibitors of janus- related kinases (jak) |
| JP6585158B2 (ja) | 2014-08-12 | 2019-10-02 | ファイザー・インク | ヤヌスキナーゼの阻害に有用なピロロ［２，３−ｄ］ピリミジン誘導体 |
| KR102165385B1 (ko) | 2014-08-20 | 2020-10-15 | 사뮤메드, 엘엘씨 | 피부 노화 및 주름의 치료 및 예방을 위한 감마-디케톤 |
| WO2016192563A1 (zh) * | 2015-05-29 | 2016-12-08 | 南京明德新药研发股份有限公司 | Janus激酶抑制剂 |
| US12365689B2 (en) | 2015-10-16 | 2025-07-22 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US10550126B2 (en) | 2015-10-16 | 2020-02-04 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| CA3251507A1 (en) | 2015-10-16 | 2025-05-21 | Abbvie Inc | Use of a solid dosage form comprising (3s,4r)-3-ethyl-4-(3h-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide for treating rheumatoid arthritis |
| US11780848B2 (en) | 2015-10-16 | 2023-10-10 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1- carboxamide and solid state forms thereof |
| US11365198B2 (en) | 2015-10-16 | 2022-06-21 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| CN106831779B (zh) * | 2015-11-28 | 2019-07-19 | 南昌弘益药业有限公司 | 一类jak激酶抑制剂的新化合物 |
| WO2017143014A1 (en) * | 2016-02-16 | 2017-08-24 | Brian Kim | Jak inhibitors and uses thereof |
| JP7108631B2 (ja) | 2017-01-06 | 2022-07-28 | パルヴェラ セラピューティクス、インク． | ｍＴＯＲ阻害剤の無水組成物およびその使用方法 |
| CN108794480A (zh) * | 2017-04-28 | 2018-11-13 | 天津药物研究院有限公司 | 吡咯并嘧啶类化合物、其制备方法和用途 |
| PT3762368T (pt) | 2018-03-08 | 2022-05-06 | Incyte Corp | Compostos de aminopirazina diol como inibidores de pi3k-y |
| WO2020010003A1 (en) | 2018-07-02 | 2020-01-09 | Incyte Corporation | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS |
| JP2021530463A (ja) | 2018-07-02 | 2021-11-11 | パルヴェラ セラピューティクス、インク． | ｍＴＯＲ阻害剤の無水組成物および使用方法 |
| IL279926B2 (en) * | 2018-07-06 | 2023-12-01 | Pfizer | Manufacturing process and intermediates for a pyrrolo[2,3- d]pyrimidine compound and use thereof |
| MX2021005334A (es) * | 2018-11-05 | 2021-06-23 | Avista Pharma Solutions Inc | Compuestos quimicos. |
| CN111499641B (zh) * | 2019-01-30 | 2021-06-04 | 格格巫（珠海）生物科技有限公司 | 一种jak抑制剂及其制备方法 |
| KR102820235B1 (ko) | 2019-02-15 | 2025-06-16 | 화이자 인코포레이티드 | 결정질 피리미디닐-3,8-다이아자바이사이클로[3.2.1]옥타닐메타논 화합물 및 이의 용도 |
| WO2020182159A1 (zh) | 2019-03-14 | 2020-09-17 | 上海华汇拓医药科技有限公司 | Jak激酶抑制剂及其制备方法和在医药领域的应用 |
| WO2020261041A1 (en) * | 2019-06-27 | 2020-12-30 | Glenmark Life Sciences Limited | Process for preparation of abrocitinib |
| ES3019413T3 (en) * | 2019-09-11 | 2025-05-20 | Pfizer | Treatment of hidradenitis suppurativa with a jak inhibitor |
| KR20220088699A (ko) | 2019-09-27 | 2022-06-28 | 디스크 메디슨, 인크. | 골수섬유증 및 관련 상태의 치료 방법 |
| WO2021198980A1 (en) | 2020-04-04 | 2021-10-07 | Pfizer Inc. | Methods of treating coronavirus disease 2019 |
| CN113637018A (zh) | 2020-04-27 | 2021-11-12 | 苏州晶云药物科技股份有限公司 | 磺酰胺类化合物的晶型及其制备方法 |
| KR20230012539A (ko) | 2020-05-13 | 2023-01-26 | 디스크 메디슨, 인크. | 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체 |
| US20230219963A1 (en) * | 2020-05-28 | 2023-07-13 | Pfizer Inc. | Pyrrolo[2,3-d]pyrimidine derivatives |
| TW202227434A (zh) * | 2020-09-08 | 2022-07-16 | 瑞士商葛德瑪控股公司 | 新穎jak抑制劑化合物、其合成方法及其用途 |
| CA3191598A1 (en) * | 2020-09-11 | 2022-03-17 | Gilles Ouvry | Novel jak inhibitor compounds, method for synthesizing same and use thereof |
| CN116847850A (zh) | 2021-02-02 | 2023-10-03 | 辉瑞公司 | 治疗慢性手部湿疹的给药方案 |
| KR20230019801A (ko) * | 2021-08-02 | 2023-02-09 | 한국화학연구원 | 신규한 피롤로 피리미딘 유도체 화합물, 이의 제조방법, 및 이를 유효성분으로 포함하는 대사성 간질환의 예방 또는 치료용 약학적 조성물 |
| CN118255769A (zh) * | 2022-12-28 | 2024-06-28 | 格格巫（珠海）生物科技有限公司 | 一种立体异构体的制备方法及中间体 |
| ES2993658B2 (es) * | 2023-06-27 | 2025-07-02 | Moehs Iberica Sl | (3-(metil(7h-pirrolo[2,3-d]pirimidin-4-il)amino)ciclobutilo)carbamato de bencilo o una sal del mismo, procedimiento para su preparacion y su uso en la sintesis de abrocitinib |
| WO2025008772A2 (en) | 2023-07-06 | 2025-01-09 | Pfizer Ireland Pharmaceuticals | Improved manufacturing process and intermediates for a pyrrolo[2,3-d]pyrimidine compound and use thereof |
| ES3040374A1 (es) | 2024-04-30 | 2025-10-30 | Moehs Iberica Sl | Cocristales de N-{cis-3-[metil(7H-pirrolo[2,3-d]pirimidin-4-il)amino]ciclobutil}propano-1-sulfonamida |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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