发明名称 Thiazole compounds, methods for preparation and use thereof
摘要 The present invention relates to thiazole compounds of formula I, the method for preparation and use thereof. More specifically, the present invention relates to novel derivatives of natural product largazole, the method for preparing them and their uses for treatments against tumor and multiple sclerosis as inhibitors of histone deacetylase.;
申请公布号 US9216962(B2) 申请公布日期 2015.12.22
申请号 US201214116944 申请日期 2012.05.07
申请人 Shanghai Puyi Chemical Co., Ltd. 发明人 Nan Fajun;Chen Fei;Zhang Yangming;Li Jia;Zhou Yubo;Su Mingbo;Ding Jian;Meng Linghua;Xie Xin;Wang Shixian
分类号 C07D417/00;C07D277/56;C07D277/58;C07D277/60;C07D417/14;C07D417/04 主分类号 C07D417/00
代理机构 Blue Filament Law 代理人 Goldstein Avery N.;Blue Filament Law
主权项 1. A thiazole compound of general formula I, wherein,R1 is one of R1a, R1b, or R1c: In which, R4a and R5a are in each occurrence independently one of: C1-C6 alkyl, tert-butoxycarbonylamino, hydrogen, halogen, hydroxyl, nitro, C3-C6 cycloalkyl, C1-C6 alkoxyl; where the C1-C6 alkoxyl can be substituted with C6-C10 aryl, amino, C1-C6 alkylamino; where the C1-C6 alkylamino can be substituted with C6-C10 aryl, or C1-C6 alkyl; where the C1-C6 alkyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkenyl; where the C2-C6 alkenyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkynyl; where the C2-C6 alkynyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or 5 to 7-membered aromatic heterocycle containing 1-3 heteroatoms selected from N, O and S; R4b and R5b are in each occurrence independently one of: hydrogen, halogen, hydroxyl, nitro, C3-C6 cycloalkyl, C1-C6 alkoxyl; where the C1-C6 alkoxyl can be substituted with C6-C10 aryl, amino, C1-C6 alkylamino; where the C1-C6 alkylamino can be substituted with C6-C10 aryl, or C1-C6 alkyl; where the C1-C6 alkyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkenyl; where the C2-C6 alkenyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkynyl; where the C2-C6 alkynyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or 5 to 7-membered aromatic heterocycle containing 1-3 heteroatoms selected from N, O and S; or, R4b and R5b together with a carbon atom to which R4b and R5b are both attached form a 3 to 10-membered cyclic hydrocarbon, or a 3 to 10-membered heterocycle containing 1 to 3 heteroatoms selected from N, O and S; R4c, R5c and R6 are in each occurrence independently one of: hydrogen, halogen, hydroxyl, nitro, C3-C6 cycloalkyl, C1-C6 alkoxyl; where the C1-C6 alkoxyl can be substituted with C6-C10 aryl, amino, or C1-C6 alkylamino; where the C1-C6 alkylamino can be substituted with C6-C10 aryl, or C1-C6 alkyl; where the C1-C6 alkyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkenyl; where the C2-C6 alkenyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkynyl; where the C2-C6 alkynyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or 5 to 7-membered aromatic heterocycle containing 1-3 heteroatoms selected from N, O and S; R2 is hydrogen, halogen, hydroxyl, C1-C6 alkoxyl, C1-C8 alkoxyl which can be substituted with C6-C10 aryl, amino, or C1-C6 alkylamino, where the C1-C6 alkylamino can be substituted with C6-C10 aryl, C1-C6 alkyl, or C3-C6 cycloalkyl; where the C3-C6 cycloalkyl can be substituted with C1-C6 alkyl; where the C1-C6 alkyl can be substituted by one or more substituent groups independently selected from hydroxyl, C1-C4 alkoxyl, halogen, benzyloxyl, C6-C10 aryl, or C2-C6 alkenyl; where the C2-C6 alkenyl group can be substituted by one or more substituent groups independently selected from hydroxyl, C1-C4 alkoxyl, halogen, C6-C10 aryl, or C2-C6 alkynyl; where the C2-C6 alkynyl that can be substituted by one or more substituent groups independently selected from hydroxyl, C1-C4 alkoxyl, halogen, C6-C10 aryl, C6-C10 aryl; where the C6-C10 aryl can be substituted by halogen or nitro, or 5-7 membered aromatic heterocycle containing 1 to 3 heteroatoms selected from N, O and S; n is 0, 1 or 2; X is —N(R7)— orwherein R7 is hydrogen or C1-C6 alkyl; conditional component Y is one of: —(C1-C10 alkyl)-, —(C2-C9 alkenyl)-, —(C6-C10 aryl)-, —(C1-C6 alkyl)-(C6-C10 aryl)-, —(C6-C10 aryl)-(C2-C6 alkenyl)-, —(C3-C6 cycloalkyl)-, —(C1-C5 alkyl)-C(O)—NH—(C1-C5 alkyl)-, —(C1-C5 alkyl)-C(O)—O—(C1-C5 alkyl)- or —(C1-C5 alkyl)-C(O)—O—(C2-C9 alkenyl)-; R3 is one of R3a, R3c, R3d, or R3e: R8 is hydrogen or C1-C6 alkylcarbonyl; and R9 is hydrogen or C1-C10 alkylcarbonyl.
地址 Shanghai CN