SUBSTITUTED FUSED HETEROARYL COMPOUND SERVING AS A KINASE INHIBITOR, AND APPLICATIONS THEREOF
申请人:Impact Therapeutics (Shanghai), Inc
公开号:EP3567041A9
公开(公告)日:2022-04-20
The disclosure relates to substituted fused heteroaromatic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I:
or a pharmaceutically acceptable salt or prodrug thereof, wherein A1-A4, B1-B3, D1-D4 and R1-R3 are defined herein. Compounds having Formula I are kinalse inhibitors. Therefore, compounds of the disclosure may be used to treat clinical conditions caused by DDR functional defects, such as cancer.
This invention relates to a taxane derivative represented by the following formula (1):
wherein at least one of X and Y represents a group -CO-A-B in which A represents a single bond, an alkylenecarbonyl group or the like and B represents a substituted or unsubstituted piperidino group or the like, the other represents a tert-butoxycarbonyl group or the like, and Z represents a hydrogen atom or a triethylenesilyl group, and also to a drug containing the same.
This compound has high solubility in water and also has excellent antitumor activities.
本发明涉及下式(1)所代表的一种紫杉烷衍生物:
其中 X 和 Y 至少有一个代表基团-CO-A-B,其中 A 代表单键、烷基羰基或类似基团,B 代表取代或未取代的哌啶基或类似基团,另一个代表叔丁氧羰基或类似基团,Z 代表氢原子或三乙烯基硅烷基。
这种化合物在水中的溶解度很高,而且具有很好的抗肿瘤活性。
TAXANE DERIVATIVES
申请人:Kabushiki Kaisha Yakult Honsha
公开号:EP1044971A1
公开(公告)日:2000-10-18
Taxane derivatives represented by general formula (1) or salts thereof and drugs containing the same as the active ingredient wherein A1 represents (a) (wherein R1 represents H or optionally substituted alkyl) or (b) (wherein R2 represents amino, mono- or dialkylamino, piperidino, pyrrolidino or morpholino); X represents H, alkoxycarbonyl or benzoyl; Y represents H or trialkylsilyl; A2 represents furyl, alkylfuryl, alkyl or fluorophenyl; Ac represents acetyl; and Bz represents benzoyl. These compounds are excellent in solubility in water and antitumor activity.
由通式(1)代表的紫杉烷衍生物或其盐类以及含有通式(1)作为活性成分的药物 其中 A1 代表(a)(其中 R1 代表 H 或任选取代的烷基)或(b)(其中 R2 代表氨基、单烷基或二烷基氨基、哌啶基、吡咯烷基或吗啉基);X 代表 H、烷氧羰基或苯甲酰基;Y 代表 H 或三烷基硅基;A2 代表呋喃基、烷基呋喃基、烷基或氟苯基;Ac 代表乙酰基;Bz 代表苯甲酰基。这些化合物具有优异的水溶性和抗肿瘤活性。
Substituted fused heteroaromatic compounds as kinase inhibitors and the use thereof
申请人:IMPACT THERAPEUTICS, INC.
公开号:US10874670B2
公开(公告)日:2020-12-29
The disclosure relates to substituted fused heteroaromatic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I:
or a pharmaceutically acceptable salt or prodrug thereof, wherein A1-A4, B1-B3, D1-D4 and R1-R3 are defined herein. Compounds having Formula I are kinalse inhibitors. Therefore, compounds of the disclosure may be used to treat clinical conditions caused by DDR functional defects, such as cancer.
本公开涉及取代的融合杂芳香族化合物及其用途。具体地说,本公开提供了如下式 I 的化合物:
或其药学上可接受的盐或原药,其中 A1-A4、B1-B3、D1-D4 和 R1-R3 在本文中定义。具有式 I 的化合物是 Kinalse 抑制剂。因此,本公开的化合物可用于治疗由 DDR 功能缺陷引起的临床病症,如癌症。