MERCK SHARP & DOHME B.V.;ORGANON BIOSCIENCES NEDERLAND B.V.;AKZO NOBEL N V;MSD OSS B.V.;N.V. ORGANON
发明人:
ANTON EGBERT PETER ADANG,GERRITDINA GEZIENA GERRITSMA,NICOLE CORINE RENÉE VAN STRATEN
申请号：
BR0009558
公开号：
BRPI0009558B1
申请日:
2000.04.03
申请国别(地区):
BR
年份:
2016
代理人:
摘要：
"heteroaromatic bicyclic derivative compound, pharmaceutical composition, and use of heteroaromatic bicyclic derivative compounds". The invention relates to a heteroaromatic bicyclic derivative compound according to the general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 1 is nr ^ 5 ^ nr ^ 5 ^, or ^ 5 ^ or sr ^ 5 ^ or R ^ 7 ^； R 7 and R 6 are independently selected from h, (1-8c) alkyl, (2-8c) alkenyl, (2-8c) alkynyl, (3-8c) cycloalkyl), (2-7c) heterocycloalkyl, (1-8c) alkylcarbonyl, (6-14c) arylcarbonyl, (6-14c) aryl or (4-13c) heteroaryl, or R ^5 ^ and R ^6 ^ together are attached in a (2-7c) ring heterocycloalkyl； R ^7 ^ is (3-8c) cycloalkyl, (2-7c) heterocycloalkyl, (6-14c) aryl or (4-13c) heteroaryl, r ^2 ^ is (1-8c) alkyl, (2-8c) alkenyl, (2-8c) alkynyl, or (6-14c) aryl or (4-13c) heteroaryl, both optionally substituted by one or more substituents selected from (1-8c) alkyl, (1-8c) 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 by one or more substituents chosen from (1-8c) (alkyl), (1-8c) (di) alkylamino or (1-8c) alkoxy； x is s, o or n (r ^ 4 ^)； 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 (w), o or a bond； w may be chosen from the same groups described for r 2 and b is n (h), o or a bond. The compounds of the invention have 1h receptor activation activity and may be used in fertility control therapies."composto derivado bicíclico heteroaromático, composição farmacêutica, e, uso de compostos derivados bicíclicos heteroaromáticos". a invenção se refere a um composto derivado biciclico heteroaromático de acordo com a fórmula geral (i) ou um sal farmacêuticamente aceitável do mesmo, em que r^ 1^ é nr^ 5^ nr^ 5^, or^ 5^ ou sr^ 5^ ou r^ 7^； r
