PE20190811A1 - Derivados de pirazolopirimidinas como inhibidor de quinasa - Google Patents
Derivados de pirazolopirimidinas como inhibidor de quinasaInfo
- Publication number
- PE20190811A1 PE20190811A1 PE2018003174A PE2018003174A PE20190811A1 PE 20190811 A1 PE20190811 A1 PE 20190811A1 PE 2018003174 A PE2018003174 A PE 2018003174A PE 2018003174 A PE2018003174 A PE 2018003174A PE 20190811 A1 PE20190811 A1 PE 20190811A1
- Authority
- PE
- Peru
- Prior art keywords
- pyrazolopyrimidines
- derivatives
- kinase inhibitor
- compound
- halogen
- Prior art date
Links
Classifications
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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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Referido a un compuesto derivado de pirazolopirimidina de formula I, en donde R1 es arilo C6-C10; o heteroarilo C2-10 que contiene de uno a tres de N, O o S; R2 es H, alquilo C1-4 o halogeno; R3 es alquilo C1-4 no sustituido o sustituido con ciano o halogeno, entre otros; X1 es CR4 o N; X2 es CR5 o N; X3 es NR6, O o S; X4 es CH o N; X5 es un enlace, o NH. Un compuesto seleccionado es (R)-1-(3-(2-(4-(4-metilpiperazin-1-il)fenilamino)-7H-pirrolo[2,3-d]pirimidin-4-ilamino)piperidin-1-il)prop-2-en-1-ona. Dicho compuesto tiene actividad inhibidora de quinasas. Tambien se refiere a un procedimiento para la preparacion del mismo y a una composicion farmaceutica para el tratamiento de enfermedad inflamatoria, autoinmunitaria, proliferativa, entre otros.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20160083050 | 2016-06-30 | ||
| PCT/KR2017/006980 WO2018004306A1 (en) | 2016-06-30 | 2017-06-30 | Pyrazolopyrimidine derivatives as kinase inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20190811A1 true PE20190811A1 (es) | 2019-06-13 |
Family
ID=60785389
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018003174A PE20190811A1 (es) | 2016-06-30 | 2017-06-30 | Derivados de pirazolopirimidinas como inhibidor de quinasa |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US10961247B2 (es) |
| EP (3) | EP3478687B1 (es) |
| JP (2) | JP2019519579A (es) |
| KR (1) | KR102329162B1 (es) |
| CN (2) | CN109311896B (es) |
| AU (1) | AU2017287762C1 (es) |
| BR (1) | BR112018074621B1 (es) |
| CA (1) | CA3025636C (es) |
| CL (1) | CL2018003511A1 (es) |
| CO (1) | CO2018013293A2 (es) |
| DO (1) | DOP2018000275A (es) |
| EC (1) | ECSP18093777A (es) |
| ES (1) | ES2977557T3 (es) |
| IL (1) | IL263306B (es) |
| MX (2) | MX393499B (es) |
| MY (1) | MY191110A (es) |
| PE (1) | PE20190811A1 (es) |
| PH (1) | PH12018502507B1 (es) |
| RU (1) | RU2714206C1 (es) |
| SA (2) | SA518400547B1 (es) |
| SG (1) | SG11201811470PA (es) |
| WO (1) | WO2018004306A1 (es) |
| ZA (1) | ZA201808431B (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112020002265A2 (pt) | 2017-08-01 | 2020-07-28 | Theravance Biopharma R&D Ip, Llc | compostos pirazólicos e triazólicos bicíclicos como inibidores de jak quiinase |
| KR102577241B1 (ko) * | 2017-12-28 | 2023-09-11 | 주식회사 대웅제약 | 카이네이즈 저해제로서의 아미노-플루오로피페리딘 유도체 |
| MA51431B1 (fr) * | 2017-12-28 | 2022-08-31 | Daewoong Pharmaceutical Co Ltd | Dérivés d'oxy-fluoropipéridine utilisés en tant qu'inhibiteur de kinase |
| KR102577242B1 (ko) | 2017-12-28 | 2023-09-11 | 주식회사 대웅제약 | 카이네이즈 저해제로서의 아미노-메틸피페리딘 유도체 |
| CN108586341B (zh) * | 2018-05-25 | 2020-05-08 | 天津商业大学 | 酰胺类化合物和其药用盐及其制备方法和药物用途 |
| BR112021002479A2 (pt) * | 2018-08-10 | 2021-07-27 | Aclaris Therapeutics, Inc. | composto, composição farmacêutica, método para inibir a atividade de itk ou jak3 em uma população de células, método para tratar um distúrbio mediado por itk ou jak3 em um indivíduo necessitando do mesmo e uso de um composto |
| WO2020154350A1 (en) | 2019-01-23 | 2020-07-30 | Theravance Biopharma R&D Ip, Llc | Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors |
| EP3851438A4 (en) * | 2019-03-18 | 2021-11-10 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd | BTK INHIBITOR, PHARMACEUTICALLY ACCEPTABLE SALT, POLYMORPHIC AND APPLICATION OF THE SAME |
| CN110317176A (zh) * | 2019-07-04 | 2019-10-11 | 沈阳药科大学 | 2-氨基嘧啶类化合物及其用途 |
| CN114901659A (zh) | 2019-11-26 | 2022-08-12 | 施万生物制药研发Ip有限责任公司 | 作为jak抑制剂的稠合嘧啶吡啶酮化合物 |
| WO2021147952A1 (zh) * | 2020-01-21 | 2021-07-29 | 江苏先声药业有限公司 | 嘧啶并吡咯类化合物 |
| CN115244055B (zh) * | 2020-01-21 | 2024-09-03 | 江苏先声药业有限公司 | 嘧啶并五元环类衍生物及其应用 |
| CN113214265B (zh) * | 2020-01-21 | 2023-07-07 | 江苏先声药业有限公司 | 嘧啶并五元环类化合物 |
| CN111620878A (zh) * | 2020-06-10 | 2020-09-04 | 中国药科大学 | 吡咯并嘧啶类衍生物作为蛋白激酶抑制剂及其应用 |
| TW202202498A (zh) * | 2020-07-01 | 2022-01-16 | 大陸商四川海思科製藥有限公司 | 一種並環雜環衍生物及其在醫藥上的應用 |
| WO2022062601A1 (zh) * | 2020-09-22 | 2022-03-31 | 江苏先声药业有限公司 | 嘧啶并吡咯类化合物 |
| CN114315838B (zh) * | 2020-09-30 | 2024-09-03 | 江苏先声药业有限公司 | 嘧啶并吡咯类化合物 |
| WO2022140246A1 (en) | 2020-12-21 | 2022-06-30 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| CN114907357A (zh) * | 2021-02-07 | 2022-08-16 | 江苏先声药业有限公司 | 嘧啶并吡咯类化合物 |
| JP2025525347A (ja) * | 2022-06-16 | 2025-08-05 | アンフィスタ セラピューティクス リミテッド | 標的タンパク質分解のための新規の二官能性分子 |
| CN115368366A (zh) * | 2022-08-02 | 2022-11-22 | 江苏省中医药研究院 | 嘧啶并吡唑类化合物及其应用 |
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| WO2024228580A1 (ko) * | 2023-05-04 | 2024-11-07 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| WO2025121899A1 (ko) * | 2023-12-05 | 2025-06-12 | 주식회사 대웅제약 | 1-((3s,4r)-3-((2-((1-에틸-1h-피라졸-4-일)아미노)-7h-피롤로[2,3-d]피리미딘-4-일)옥시)-4-플루오로피페리딘-1-일)프로프-2-엔-1-온의 제조 방법, 및 이의 중간체 화합물 |
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| CN105732637B (zh) | 2014-12-30 | 2020-04-21 | 广东东阳光药业有限公司 | 杂芳化合物及其在药物中的应用 |
| CA2976109A1 (en) | 2015-02-13 | 2016-08-18 | Dana-Farber Cancer Institute, Inc. | Substituted pyrrolopyrimidine, pyrazolopyrimidine and purine derivatives and use thereof as lrrk2 inhibitors |
-
2017
- 2017-06-30 MY MYPI2018002167A patent/MY191110A/en unknown
- 2017-06-30 EP EP17820582.9A patent/EP3478687B1/en active Active
- 2017-06-30 JP JP2018568407A patent/JP2019519579A/ja active Pending
- 2017-06-30 WO PCT/KR2017/006980 patent/WO2018004306A1/en not_active Ceased
- 2017-06-30 SG SG11201811470PA patent/SG11201811470PA/en unknown
- 2017-06-30 AU AU2017287762A patent/AU2017287762C1/en active Active
- 2017-06-30 CN CN201780039336.0A patent/CN109311896B/zh active Active
- 2017-06-30 PH PH1/2018/502507A patent/PH12018502507B1/en unknown
- 2017-06-30 CA CA3025636A patent/CA3025636C/en active Active
- 2017-06-30 EP EP25207256.6A patent/EP4656249A2/en active Pending
- 2017-06-30 KR KR1020170083259A patent/KR102329162B1/ko active Active
- 2017-06-30 CN CN202110351304.2A patent/CN113135920A/zh active Pending
- 2017-06-30 MX MX2021009378A patent/MX393499B/es unknown
- 2017-06-30 RU RU2019102376A patent/RU2714206C1/ru active
- 2017-06-30 US US16/304,798 patent/US10961247B2/en active Active
- 2017-06-30 MX MX2018016287A patent/MX388591B/es unknown
- 2017-06-30 PE PE2018003174A patent/PE20190811A1/es unknown
- 2017-06-30 EP EP21190933.8A patent/EP3950691A1/en active Pending
- 2017-06-30 ES ES17820582T patent/ES2977557T3/es active Active
- 2017-06-30 BR BR112018074621-5A patent/BR112018074621B1/pt active IP Right Grant
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2018
- 2018-11-27 IL IL263306A patent/IL263306B/en active IP Right Grant
- 2018-11-28 SA SA518400547A patent/SA518400547B1/ar unknown
- 2018-11-28 SA SA521430937A patent/SA521430937B1/ar unknown
- 2018-12-07 CO CONC2018/0013293A patent/CO2018013293A2/es unknown
- 2018-12-07 CL CL2018003511A patent/CL2018003511A1/es unknown
- 2018-12-10 DO DO2018000275A patent/DOP2018000275A/es unknown
- 2018-12-13 ZA ZA2018/08431A patent/ZA201808431B/en unknown
- 2018-12-18 EC ECSENADI201893777A patent/ECSP18093777A/es unknown
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2020
- 2020-06-04 JP JP2020097918A patent/JP7084961B2/ja active Active
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