发明名称 BICYCLIC HETEROAROMATIC COMPOUNDS USEFUL AS LH AGONISTS
摘要 The invention relates to a bicyclic heteroaromatic derivative compound according to general formula (I), (see formula I) or a pharmaceutically acceptable salt thereof, wherein R1 is NR5R6, OR5, SR5 or R7 ; R5 and R6 are independently selected from H, (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, alkyl(1-8C)carbonyl, (6-14C)arylcarbonyl, (6-14C)aryl or (4-13C)heteroaryl, or R5 and R6 together are joined in a (2-7C)heterocycloalkyl ring; R7 is (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl or (4-13C) heteroaryl, R2 is (1-8C) alkyl, (2-8C) alkenyl, (2- 8C)alkynyl, or (6-14C)aryl or (4-13C)heteroaryl, both optionally substituted with one or more substituents selected from (1-8C)alkyl, (l-8C)alkylthio, (1-8C)(di)alkylamino, (1- 8C)alkoxy, (2-8C)alkenyl, or (2-8C)alkynyl; R3 is (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, or (6-14C)aryl or (4-13C)heteroaryl, both optionally substituted with one or more substituents selected from (1-8C)alkyl, (1-8C)(di)alkylamino or (1-8C) alkoxy; X is S, O or N(R4); R4 is H, (1-8C) alkyl, (1-8C)alkylcarbonyl, (6-14C)arylcarbonyl or (6-14C)aryl(1-8C)alkyl; Y is CH or N; Z is NH2 or OH; A is S, N(H), N(R9), O or a bond; R9 can be selected from the same groups as described for R2 and B is N(H), O or a bond. The compounds of the invention have LH receptor activating activity and can be used in fertility regulating therapies.
申请公布号 CA2368834(C) 申请公布日期 2009.11.03
申请号 CA20002368834 申请日期 2000.04.03
申请人 AKZO NOBEL N.V. 发明人 GERRITSMA, GERRILDINA GEZIENA;ADANG, ANTON EGBERT PETER;VAN STRATEN, NICOLE CORINE RENEE
分类号 C07D495/04;A61K31/4365;A61K31/44;A61K31/505;A61K31/519;A61P5/06;A61P5/24;A61P15/00;C07D207/00;C07D239/00;C07D333/02;C07D487/04 主分类号 C07D495/04
代理机构 代理人
主权项
地址