CN110267959B - 作为PI3Kδ抑制剂的咪唑并[1,5-A]吡嗪衍生物 - Google Patents
作为PI3Kδ抑制剂的咪唑并[1,5-A]吡嗪衍生物 Download PDFInfo
- Publication number
- CN110267959B CN110267959B CN201780076039.3A CN201780076039A CN110267959B CN 110267959 B CN110267959 B CN 110267959B CN 201780076039 A CN201780076039 A CN 201780076039A CN 110267959 B CN110267959 B CN 110267959B
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- Prior art keywords
- compound
- chloro
- phenyl
- ethyl
- alkyl
- 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.)
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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
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202210507333.8A CN114805366A (zh) | 2016-12-07 | 2017-12-07 | 作为PI3Kδ抑制剂的咪唑并[1,5-A]吡嗪衍生物 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2016108897 | 2016-12-07 | ||
| CNPCT/CN2016/108897 | 2016-12-07 | ||
| PCT/CN2017/114970 WO2018103688A1 (en) | 2016-12-07 | 2017-12-07 | IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3Kdelta INHIBITORS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202210507333.8A Division CN114805366A (zh) | 2016-12-07 | 2017-12-07 | 作为PI3Kδ抑制剂的咪唑并[1,5-A]吡嗪衍生物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN110267959A CN110267959A (zh) | 2019-09-20 |
| CN110267959B true CN110267959B (zh) | 2022-05-27 |
Family
ID=62491736
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780076039.3A Expired - Fee Related CN110267959B (zh) | 2016-12-07 | 2017-12-07 | 作为PI3Kδ抑制剂的咪唑并[1,5-A]吡嗪衍生物 |
| CN202210507333.8A Pending CN114805366A (zh) | 2016-12-07 | 2017-12-07 | 作为PI3Kδ抑制剂的咪唑并[1,5-A]吡嗪衍生物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202210507333.8A Pending CN114805366A (zh) | 2016-12-07 | 2017-12-07 | 作为PI3Kδ抑制剂的咪唑并[1,5-A]吡嗪衍生物 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US11136323B2 (https=) |
| EP (1) | EP3551630A4 (https=) |
| JP (2) | JP7064495B2 (https=) |
| KR (1) | KR20190091339A (https=) |
| CN (2) | CN110267959B (https=) |
| AU (2) | AU2017372377B2 (https=) |
| BR (1) | BR112019011847A2 (https=) |
| CA (1) | CA3045959A1 (https=) |
| EA (1) | EA201991355A1 (https=) |
| IL (2) | IL266986B (https=) |
| MX (1) | MX394882B (https=) |
| NZ (1) | NZ754944A (https=) |
| SG (1) | SG10201912192RA (https=) |
| TW (2) | TW202233190A (https=) |
| WO (1) | WO2018103688A1 (https=) |
| ZA (1) | ZA201903286B (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202233190A (zh) * | 2016-12-07 | 2022-09-01 | 英屬開曼群島商百濟神州有限公司 | 作為PI3Kδ抑制劑的咪唑並[1,5-A]吡衍生物 |
| TWI817956B (zh) | 2017-09-08 | 2023-10-11 | 英屬開曼群島商百濟神州有限公司 | 咪唑並[1,5-A]吡嗪衍生物作爲PI3Kδ 抑制劑 |
| JP2023503230A (ja) * | 2019-11-21 | 2023-01-27 | ベイジーン リミテッド | Pi3キナーゼデルタ阻害剤との組合せで抗ox40抗体を用いる癌治療の方法 |
| KR102344185B1 (ko) * | 2020-02-26 | 2021-12-27 | 계명대학교 산학협력단 | 신규한 Pim 키나아제 억제제 및 이의 용도 |
| JP2024521763A (ja) * | 2021-05-27 | 2024-06-04 | ベイジーン スウィッツァーランド ゲーエムベーハー | Pi3kデルタ阻害剤の塩、その結晶形態、調製方法、及び使用 |
| KR20240060647A (ko) * | 2021-09-14 | 2024-05-08 | 베이진 엘티디 | Btk 저해제와 pi3 키나제 저해제의 조합물을 이용하는 암 치료 방법 |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1898240A (zh) * | 2003-10-15 | 2007-01-17 | Osi制药公司 | 咪唑并吡嗪类酪氨酸激酶抑制剂 |
| CN102428087A (zh) * | 2009-04-16 | 2012-04-25 | 西班牙国家癌症研究中心 | 用作激酶抑制剂的咪唑并吡嗪类化合物 |
| WO2012107465A1 (en) * | 2011-02-09 | 2012-08-16 | F. Hoffmann-La Roche Ag | Heterocyclic compounds as pi3 kinase inhibitors |
| CN104066735A (zh) * | 2012-01-10 | 2014-09-24 | 拜耳知识产权有限责任公司 | 作为akt激酶抑制剂的取代的咪唑并吡嗪 |
| WO2015058084A1 (en) * | 2013-10-18 | 2015-04-23 | Medivation Technologies, Inc. | Heterocyclic compounds and methods of use |
| CN105682658A (zh) * | 2013-05-30 | 2016-06-15 | 无限药品公司 | 使用pi3激酶亚型调节剂的癌症疗法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2914296B2 (en) | 2012-11-01 | 2021-09-29 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| MA40596B1 (fr) | 2014-08-11 | 2021-12-31 | Acerta Pharma Bv | Combinaisons thérapeutiques d'un inhibiteur de btk et d'un inhibiteur de bcl-2 |
| TW202233190A (zh) * | 2016-12-07 | 2022-09-01 | 英屬開曼群島商百濟神州有限公司 | 作為PI3Kδ抑制劑的咪唑並[1,5-A]吡衍生物 |
| TWI817956B (zh) | 2017-09-08 | 2023-10-11 | 英屬開曼群島商百濟神州有限公司 | 咪唑並[1,5-A]吡嗪衍生物作爲PI3Kδ 抑制劑 |
-
2017
- 2017-12-07 TW TW111114434A patent/TW202233190A/zh unknown
- 2017-12-07 SG SG10201912192RA patent/SG10201912192RA/en unknown
- 2017-12-07 CN CN201780076039.3A patent/CN110267959B/zh not_active Expired - Fee Related
- 2017-12-07 EP EP17877406.3A patent/EP3551630A4/en not_active Withdrawn
- 2017-12-07 TW TW106143023A patent/TWI762534B/zh not_active IP Right Cessation
- 2017-12-07 CA CA3045959A patent/CA3045959A1/en active Pending
- 2017-12-07 MX MX2019006612A patent/MX394882B/es unknown
- 2017-12-07 KR KR1020197019710A patent/KR20190091339A/ko not_active Ceased
- 2017-12-07 EA EA201991355A patent/EA201991355A1/ru unknown
- 2017-12-07 CN CN202210507333.8A patent/CN114805366A/zh active Pending
- 2017-12-07 AU AU2017372377A patent/AU2017372377B2/en not_active Ceased
- 2017-12-07 NZ NZ754944A patent/NZ754944A/en not_active IP Right Cessation
- 2017-12-07 US US16/466,621 patent/US11136323B2/en active Active
- 2017-12-07 BR BR112019011847-0A patent/BR112019011847A2/pt not_active IP Right Cessation
- 2017-12-07 WO PCT/CN2017/114970 patent/WO2018103688A1/en not_active Ceased
- 2017-12-07 JP JP2019530790A patent/JP7064495B2/ja not_active Expired - Fee Related
-
2019
- 2019-05-24 ZA ZA2019/03286A patent/ZA201903286B/en unknown
- 2019-05-29 IL IL266986A patent/IL266986B/en unknown
-
2021
- 2021-07-08 US US17/370,728 patent/US11725012B2/en active Active
-
2022
- 2022-02-07 IL IL290419A patent/IL290419B2/en unknown
- 2022-04-22 JP JP2022070763A patent/JP2022090051A/ja active Pending
- 2022-05-31 AU AU2022203737A patent/AU2022203737A1/en not_active Abandoned
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1898240A (zh) * | 2003-10-15 | 2007-01-17 | Osi制药公司 | 咪唑并吡嗪类酪氨酸激酶抑制剂 |
| CN102428087A (zh) * | 2009-04-16 | 2012-04-25 | 西班牙国家癌症研究中心 | 用作激酶抑制剂的咪唑并吡嗪类化合物 |
| WO2012107465A1 (en) * | 2011-02-09 | 2012-08-16 | F. Hoffmann-La Roche Ag | Heterocyclic compounds as pi3 kinase inhibitors |
| CN104066735A (zh) * | 2012-01-10 | 2014-09-24 | 拜耳知识产权有限责任公司 | 作为akt激酶抑制剂的取代的咪唑并吡嗪 |
| CN105682658A (zh) * | 2013-05-30 | 2016-06-15 | 无限药品公司 | 使用pi3激酶亚型调节剂的癌症疗法 |
| WO2015058084A1 (en) * | 2013-10-18 | 2015-04-23 | Medivation Technologies, Inc. | Heterocyclic compounds and methods of use |
Also Published As
| Publication number | Publication date |
|---|---|
| US20220098202A1 (en) | 2022-03-31 |
| TW202233190A (zh) | 2022-09-01 |
| EA201991355A1 (ru) | 2019-11-29 |
| US20190367523A1 (en) | 2019-12-05 |
| TWI762534B (zh) | 2022-05-01 |
| EP3551630A4 (en) | 2020-07-15 |
| EP3551630A1 (en) | 2019-10-16 |
| AU2022203737A1 (en) | 2022-06-23 |
| CN114805366A (zh) | 2022-07-29 |
| IL290419B2 (en) | 2023-02-01 |
| US11136323B2 (en) | 2021-10-05 |
| KR20190091339A (ko) | 2019-08-05 |
| WO2018103688A1 (en) | 2018-06-14 |
| IL266986A (en) | 2019-07-31 |
| ZA201903286B (en) | 2021-01-27 |
| JP2022090051A (ja) | 2022-06-16 |
| CA3045959A1 (en) | 2018-06-14 |
| SG10201912192RA (en) | 2020-02-27 |
| BR112019011847A2 (pt) | 2019-10-29 |
| MX394882B (es) | 2025-03-24 |
| IL290419A (en) | 2022-04-01 |
| IL290419B (en) | 2022-10-01 |
| US11725012B2 (en) | 2023-08-15 |
| MX2019006612A (es) | 2019-08-01 |
| IL266986B (en) | 2022-03-01 |
| CN110267959A (zh) | 2019-09-20 |
| AU2017372377A1 (en) | 2019-07-18 |
| JP7064495B2 (ja) | 2022-05-10 |
| NZ754944A (en) | 2023-02-24 |
| AU2017372377B2 (en) | 2022-03-03 |
| JP2020500909A (ja) | 2020-01-16 |
| TW201833113A (zh) | 2018-09-16 |
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