KR20220029690A - HPK1 저해제로서의 피롤로[2,3-b]피라진 및 이의 용도 - Google Patents
HPK1 저해제로서의 피롤로[2,3-b]피라진 및 이의 용도 Download PDFInfo
- Publication number
- KR20220029690A KR20220029690A KR1020227002739A KR20227002739A KR20220029690A KR 20220029690 A KR20220029690 A KR 20220029690A KR 1020227002739 A KR1020227002739 A KR 1020227002739A KR 20227002739 A KR20227002739 A KR 20227002739A KR 20220029690 A KR20220029690 A KR 20220029690A
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- methyl
- heterocyclyl
- cycloalkyl
- conr
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
Links
Classifications
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- 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
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019094749 | 2019-07-04 | ||
| CNPCT/CN2019/094749 | 2019-07-04 | ||
| CNPCT/CN2019/123268 | 2019-12-05 | ||
| CN2019123268 | 2019-12-05 | ||
| CNPCT/CN2020/089498 | 2020-05-09 | ||
| CN2020089498 | 2020-05-09 | ||
| PCT/CN2020/100037 WO2021000925A1 (en) | 2019-07-04 | 2020-07-03 | PYRROLO [2, 3-b] PYRAZINES AS HPK1 INHIBITOR AND THE USE THEREOF |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20220029690A true KR20220029690A (ko) | 2022-03-08 |
Family
ID=74100904
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020227002739A Ceased KR20220029690A (ko) | 2019-07-04 | 2020-07-03 | HPK1 저해제로서의 피롤로[2,3-b]피라진 및 이의 용도 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US12454534B2 (https=) |
| EP (1) | EP3994136A4 (https=) |
| JP (1) | JP7579816B2 (https=) |
| KR (1) | KR20220029690A (https=) |
| CN (3) | CN114096536A (https=) |
| AU (1) | AU2020299892A1 (https=) |
| BR (1) | BR112022000019A2 (https=) |
| CA (1) | CA3145751A1 (https=) |
| CO (1) | CO2022001094A2 (https=) |
| IL (1) | IL289553A (https=) |
| MX (1) | MX2022000244A (https=) |
| TW (1) | TWI848141B (https=) |
| WO (1) | WO2021000925A1 (https=) |
| ZA (1) | ZA202110732B (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11203591B2 (en) | 2018-10-31 | 2021-12-21 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds |
| WO2020092528A1 (en) | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity |
| EP3972695A1 (en) | 2019-05-23 | 2022-03-30 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
| TWI848141B (zh) | 2019-07-04 | 2024-07-11 | 英屬開曼群島商百濟神州有限公司 | 及其用途 |
| US12459958B2 (en) | 2019-07-17 | 2025-11-04 | Beone Medicines I Gmbh | Tricyclic compounds as HPK1 inhibitor and the use thereof |
| CN114685490B (zh) * | 2020-12-31 | 2025-03-28 | 南京再明医药有限公司 | 吡咯并吡啶类化合物及其应用 |
| WO2022184152A1 (zh) * | 2021-03-03 | 2022-09-09 | 劲方医药科技(上海)有限公司 | 稠环取代的六元杂环化合物及其制法和用途 |
| CN115073472A (zh) * | 2021-03-16 | 2022-09-20 | 江苏恒瑞医药股份有限公司 | 稠合二环类化合物、其制备方法及其在医药上的应用 |
| WO2022199676A1 (zh) * | 2021-03-26 | 2022-09-29 | 江苏恒瑞医药股份有限公司 | 稠合四环类化合物、其制备方法及其在医药上的应用 |
| EP4341261A1 (en) * | 2021-05-21 | 2024-03-27 | Arcus Biosciences, Inc. | Axl compounds |
| WO2022246179A1 (en) * | 2021-05-21 | 2022-11-24 | Arcus Biosciences, Inc. | Axl inhibitor compounds |
| TW202321239A (zh) | 2021-07-20 | 2023-06-01 | 瑞典商阿斯特捷利康公司 | 作為hpk1抑制劑用於治療癌症之經取代的吡𠯤—2—甲醯胺 |
| JP2024528722A (ja) * | 2021-07-30 | 2024-07-30 | ベイジーン リミテッド | HPK1分解誘導薬としてのピロロ[2,3-b]ピラジン系の二官能性化合物及びその使用 |
| WO2023151559A1 (zh) * | 2022-02-08 | 2023-08-17 | 和径医药科技(上海)有限公司 | 杂环化合物、包含其的药物组合物及其抗肿瘤应用 |
| CN116731029B (zh) * | 2022-03-11 | 2026-01-02 | 石药集团中奇制药技术(石家庄)有限公司 | 一类并环化合物及其制备和应用 |
| CN116925082A (zh) * | 2022-04-24 | 2023-10-24 | 百济神州(苏州)生物科技有限公司 | 5H-吡咯并[2,3-b]吡嗪衍生物的多晶型形式,制备方法及其用途 |
| WO2023207911A1 (zh) * | 2022-04-24 | 2023-11-02 | 上海医药集团股份有限公司 | 一种双环杂环化合物、药物组合物和应用 |
| WO2023207894A1 (en) * | 2022-04-24 | 2023-11-02 | Beigene , Ltd. | POLYMORPH FORMS OF A 5H-PYRROLO [2, 3-b] PYRAZINE DERIVATIVE, METHODS OF PREPARATION, AND USES THEREFORE |
| AR129722A1 (es) | 2022-06-28 | 2024-09-18 | Arcus Biosciences Inc | Compuestos inhibidores de axl |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5942532A (en) | 1997-09-05 | 1999-08-24 | Ortho Pharmaceutical Corporation | 2-substituted phenyl-benzimidazole antibacterial agents |
| TWI339206B (en) | 2003-09-04 | 2011-03-21 | Vertex Pharma | Compositions useful as inhibitors of protein kinases |
| WO2006015123A1 (en) | 2004-07-27 | 2006-02-09 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| CA2573573A1 (en) * | 2004-07-27 | 2006-02-09 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| US7709645B2 (en) | 2004-07-27 | 2010-05-04 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| WO2006058120A1 (en) | 2004-11-22 | 2006-06-01 | Vertex Pharmaceuticals Incorporated | Bicyclic inhibitors or rho kinase |
| US20070087988A1 (en) | 2005-09-30 | 2007-04-19 | New York University | Hematopoietic progenitor kinase 1 for modulation of an immune response |
| WO2010049173A1 (en) | 2008-10-31 | 2010-05-06 | Cenix Bioscience Gmbh | Use of inhibitors of host kinases for the treatment of infectious diseases |
| JP6086326B2 (ja) | 2010-05-24 | 2017-03-01 | ユニヴァーシティー オブ ロチェスター | 二環式ヘテロアリールキナーゼ阻害剤および使用方法 |
| CN101851237B (zh) | 2010-06-18 | 2012-10-17 | 南方医科大学 | 一种螺环化合物及其制备方法和应用 |
| JP2012012332A (ja) | 2010-06-30 | 2012-01-19 | Dainippon Sumitomo Pharma Co Ltd | 新規アザインドール誘導体 |
| SG11201408816QA (en) | 2012-07-03 | 2015-03-30 | Aurigene Discovery Tech Ltd | 3-(PYRAZOLYL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS |
| CN104884059B (zh) | 2012-11-30 | 2018-08-10 | 罗切斯特大学 | 用于hiv/aids治疗的混合谱系激酶抑制剂 |
| US9260426B2 (en) | 2012-12-14 | 2016-02-16 | Arrien Pharmaceuticals Llc | Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors |
| CN104513253A (zh) | 2013-10-01 | 2015-04-15 | 南京波尔泰药业科技有限公司 | 用于治疗增殖性疾病的大环化合物 |
| CN105777756B (zh) | 2014-07-02 | 2019-03-01 | 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 |
| KR101660863B1 (ko) | 2015-04-03 | 2016-09-28 | 주식회사 녹십자 | IKKε 및 TBK1 억제제로서의 7-아자인돌 또는 4,7-다이아자인돌 유도체 및 이를 포함하는 약학적 조성물 |
| WO2016164641A1 (en) * | 2015-04-08 | 2016-10-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| MA42456B1 (fr) | 2015-06-25 | 2021-06-30 | Univ Health Network | Inhibiteurs de hpk1 et leurs procédés d'utilisation |
| CN106336413B (zh) * | 2015-07-09 | 2021-04-20 | 广东东阳光药业有限公司 | 作为jak抑制剂的化合物及其用途 |
| CN106432246B (zh) | 2015-08-05 | 2020-07-07 | 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 |
| GB201517263D0 (en) | 2015-09-30 | 2015-11-11 | Ucb Biopharma Sprl And Katholieke Universiteit Leuven | Therapeutic agents |
| CN115819417A (zh) | 2016-09-09 | 2023-03-21 | 因赛特公司 | 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途 |
| US10280164B2 (en) | 2016-09-09 | 2019-05-07 | Incyte Corporation | Pyrazolopyridone compounds and uses thereof |
| US20180072741A1 (en) * | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyrimidine compounds and uses thereof |
| WO2018049214A1 (en) * | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer |
| CN110402248B (zh) | 2017-03-15 | 2023-01-06 | 豪夫迈·罗氏有限公司 | 作为hpk1抑制剂的氮杂吲哚类 |
| AU2018244935A1 (en) | 2017-03-30 | 2019-08-15 | F. Hoffmann-La Roche Ag | Naphthyridines as inhibitors of HPK1 |
| EP3601259B1 (en) | 2017-03-30 | 2022-02-23 | F. Hoffmann-La Roche AG | Isoquinolines as inhibitors of hpk1 |
| US10654825B2 (en) | 2017-03-30 | 2020-05-19 | Corvus Pharmaceuticals, Inc. | Processes for making triazolo[4,5D] pyramidine derivatives and intermediates thereof |
| IL276232B2 (en) | 2018-03-02 | 2024-04-01 | Otsuka Pharma Co Ltd | Pyrazine derivatives, pharmaceutical compositions comprising them and their use for treating diseases |
| CN108440532A (zh) | 2018-03-27 | 2018-08-24 | 上海道亦化工科技有限公司 | 一种苯并吡嗪化合物及其用途和发光器件 |
| MX2020012679A (es) | 2018-05-25 | 2021-02-09 | Silverback Therapeutics Inc | Compuestos de amino-pirazincarboxamida, conjugados, y usos de los mismos. |
| CN112243439A (zh) | 2018-06-13 | 2021-01-19 | 百济神州有限公司 | 作为hpk1抑制剂的吡咯并[2,3-b]吡啶或吡咯并[2,3-b]吡嗪及其用途 |
| WO2020103896A1 (en) | 2018-11-22 | 2020-05-28 | Beigene, Ltd. | Pyrrolo[2,3-b]pyridines as hpk1 inhibitor and uses thereof |
| JP7503851B2 (ja) * | 2019-05-06 | 2024-06-21 | アイカーン スクール オブ メディスン アット マウント シナイ | Hpk1の分解剤としてのヘテロ二官能性化合物 |
| TWI848141B (zh) | 2019-07-04 | 2024-07-11 | 英屬開曼群島商百濟神州有限公司 | 及其用途 |
| US12459958B2 (en) | 2019-07-17 | 2025-11-04 | Beone Medicines I Gmbh | Tricyclic compounds as HPK1 inhibitor and the use thereof |
| WO2021032148A1 (en) | 2019-08-21 | 2021-02-25 | Beigene, Ltd. | Aminopyrazine compounds as hpk1 inhibitor and the use thereof |
| CN112552293A (zh) * | 2019-09-25 | 2021-03-26 | 珠海宇繁生物科技有限责任公司 | 一种protac小分子化合物及其应用 |
-
2020
- 2020-07-01 TW TW109122260A patent/TWI848141B/zh active
- 2020-07-03 CN CN202080045779.2A patent/CN114096536A/zh active Pending
- 2020-07-03 MX MX2022000244A patent/MX2022000244A/es unknown
- 2020-07-03 EP EP20834932.4A patent/EP3994136A4/en active Pending
- 2020-07-03 AU AU2020299892A patent/AU2020299892A1/en not_active Abandoned
- 2020-07-03 JP JP2021575442A patent/JP7579816B2/ja active Active
- 2020-07-03 BR BR112022000019A patent/BR112022000019A2/pt unknown
- 2020-07-03 CN CN202210690804.3A patent/CN115028639A/zh active Pending
- 2020-07-03 CN CN202210690828.9A patent/CN115073474B/zh active Active
- 2020-07-03 US US17/623,732 patent/US12454534B2/en active Active
- 2020-07-03 KR KR1020227002739A patent/KR20220029690A/ko not_active Ceased
- 2020-07-03 CA CA3145751A patent/CA3145751A1/en active Pending
- 2020-07-03 WO PCT/CN2020/100037 patent/WO2021000925A1/en not_active Ceased
-
2021
- 2021-12-21 ZA ZA2021/10732A patent/ZA202110732B/en unknown
-
2022
- 2022-01-02 IL IL289553A patent/IL289553A/en unknown
- 2022-02-02 CO CONC2022/0001094A patent/CO2022001094A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN115073474B (zh) | 2024-10-18 |
| EP3994136A4 (en) | 2023-06-28 |
| US20220267333A1 (en) | 2022-08-25 |
| AU2020299892A1 (en) | 2022-01-27 |
| TWI848141B (zh) | 2024-07-11 |
| CN114096536A (zh) | 2022-02-25 |
| EP3994136A1 (en) | 2022-05-11 |
| CN115028639A (zh) | 2022-09-09 |
| JP2022538019A (ja) | 2022-08-31 |
| CA3145751A1 (en) | 2021-01-07 |
| IL289553A (en) | 2022-03-01 |
| CO2022001094A2 (es) | 2022-04-29 |
| TW202116773A (zh) | 2021-05-01 |
| JP7579816B2 (ja) | 2024-11-08 |
| MX2022000244A (es) | 2022-02-03 |
| WO2021000925A1 (en) | 2021-01-07 |
| CN115073474A (zh) | 2022-09-20 |
| ZA202110732B (en) | 2022-09-28 |
| BR112022000019A2 (pt) | 2022-02-22 |
| US12454534B2 (en) | 2025-10-28 |
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