CN116113633A - 一种作为可透脑的btk或her2抑制剂的化合物及其制备方法与用途 - Google Patents
一种作为可透脑的btk或her2抑制剂的化合物及其制备方法与用途 Download PDFInfo
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Abstract
一种作为BTK抑制剂或HER2抑制剂的化合物及其制备方法与用途，所述化合物具有式II所示结构或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体或其混合物形式、药学上可接受的水合物、溶剂化物或盐。本发明的BTK蛋白质激酶抑制剂对野生型BTK和突变的BTK(C481S)都有很强的抑制活性，部分化合物具有很高的透脑率；本发明的HER2抑制剂具有较好的HER2激酶抑制活性、很高的血脑屏障透过率；且本发明化合物具有良好的药代动力学性质，有很好的应用前景。
Description
PCT国内申请，说明书已公开。
Claims (10)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010679776 | 2020-07-15 | ||
| CN2020106797766 | 2020-07-15 | ||
| CN2020113370229 | 2020-11-25 | ||
| CN202011337022.9A CN113943294A (zh) | 2020-07-15 | 2020-11-25 | 一种作为btk抑制剂的化合物及其制备方法与用途 |
| PCT/CN2021/105960 WO2022012509A1 (zh) | 2020-07-15 | 2021-07-13 | 一种作为可透脑的btk或her2抑制剂的化合物及其制备方法与用途 |
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| CN116113633A true CN116113633A (zh) | 2023-05-12 |
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| CN202180037167.3A Pending CN115989231A (zh) | 2020-07-15 | 2021-07-13 | 一种作为btk抑制剂的化合物及其制备方法与用途 |
| CN202180037168.8A Pending CN116113633A (zh) | 2020-07-15 | 2021-07-13 | 一种作为可透脑的btk或her2抑制剂的化合物及其制备方法与用途 |
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| CN202180037167.3A Pending CN115989231A (zh) | 2020-07-15 | 2021-07-13 | 一种作为btk抑制剂的化合物及其制备方法与用途 |
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| WO2021136219A1 (en) * | 2020-01-02 | 2021-07-08 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. | Btk inhibitors |
| US20230145305A1 (en) * | 2020-03-12 | 2023-05-11 | Fochon Biosciences, Ltd. | Compounds useful as kinase inhibitors |
| CN114920745A (zh) * | 2022-03-28 | 2022-08-19 | 深圳海博为药业有限公司 | 一种咪唑并吡嗪类化合物及其作为igf1r抑制剂的应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| GB9414974D0 (en) * | 1994-07-26 | 1994-09-14 | Bnfl Fluorchem Ltd | Selectively fluorinated organic compounds |
| JP2011520970A (ja) * | 2008-05-19 | 2011-07-21 | オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド | 置換されたイミダゾピラジン類およびイミダゾトリアジン類 |
| US7718662B1 (en) * | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
| SG10201900025UA (en) * | 2013-07-31 | 2019-02-27 | Merck Patent Gmbh | Pyridines, pyrimidines, and pyrazines, as btk inhibitors and uses thereof |
| CN105017256A (zh) * | 2014-04-29 | 2015-11-04 | 浙江导明医药科技有限公司 | 多氟化合物作为布鲁顿酪氨酸激酶抑制剂 |
| WO2016106652A1 (en) * | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Biarylether imidazopyrazine btk inhibitors |
| WO2016106624A1 (en) * | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Tertiary alcohol imidazopyrazine btk inhibitors |
| WO2016106627A1 (en) * | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| CN106146511A (zh) * | 2015-04-03 | 2016-11-23 | 安润医药科技（苏州）有限公司 | 吡唑并嘧啶衍生物、制备方法、药物组合物及用途 |
| KR102327917B1 (ko) * | 2016-07-07 | 2021-11-17 | 주식회사 대웅제약 | 신규한 4-아미노피라졸로[3,4-d]피리미디닐아자바이사이클로 유도체 및 이를 포함하는 약학 조성물 |
| CN106243133A (zh) * | 2016-07-28 | 2016-12-21 | 天津师范大学 | 具有氢气吸附性质的蒽环双三唑锌配合物单晶与应用 |
| JP2022517280A (ja) * | 2019-01-18 | 2022-03-07 | シービン リィアォ | ブルトン型チロシンキナーゼ阻害剤 |
| CN111454268B (zh) * | 2019-01-18 | 2023-09-08 | 明慧医药（上海）有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
| WO2021136219A1 (en) * | 2020-01-02 | 2021-07-08 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. | Btk inhibitors |
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| CA3185574A1 (en) | 2022-01-20 |
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| CN113943294A (zh) | 2022-01-18 |
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| TWI826819B (zh) | 2023-12-21 |
| EP4186905A1 (en) | 2023-05-31 |
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