公开(公告)号：EP0757677B1

公开(公告)日：2003-06-18

申请号：EP95916449.2

申请日：1995-04-25

申请人： Syntex (U.S.A.) LLC

发明人： MARTINEZ, Gregory, R. ,  REPKE, David, B. ,  TEITELBAUM, Philip, J. ,  WALKER, Keith, A., M. ,  GOODING, Owen, W. ,  WHITING, Roger, L. ,  BANSAL, Rekha, P. ,  MUEHLDORF, Alexander, V. ,  O'YANG, Counde

IPC分类号： C07D233/84 ,  A61K31/415 ,  A61K31/41 ,  C07D233/88 ,  C07D233/90 ,  C07D249/12 ,  C07D249/14 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10

CPC分类号： C07D403/04 ,  C07D233/28 ,  C07D233/32 ,  C07D233/36 ,  C07D233/42 ,  C07D233/84 ,  C07D249/12 ,  C07D403/10 ,  C07D405/12 ,  Y02P20/582

摘要： The present invention relates to novel benzocycloalkylazolethione compounds of formula (I) in which n is 0, 1 or 2; t is 0, 1, 2 or 3; R1 is independently halo, hydroxy or (C¿1-4?)alkyloxy; and R?2¿ is attached to the α, β or η-position and is a group selected from formulae (a), (b) and (c) which are dopamine β-hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from indanyl, 1,2,3,4-tetrahydronaphthalenyl and 6,7,8,9-tetrahydro-5H-benzocycloheptenyl (in which the benzo is optionally substituted with one to three substituents) and the azolethione portion of the compound is selected from 2-thioxo-2,3-dihydro-1H-imidazol-3-yl, 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-4-yl and 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-1-yl (each optionally substituted with one to three substituents); and the prodrugs, pharmaceutically acceptable salts, individual isomers and mixtures of isomers and the methods of using and preparing such benzocycloalkylazolethione compounds.

摘要翻译： 本发明涉及式（I）的新型苯并环烷基唑硫酮化合物，其中n是0,1或2; t是0,1,2或3; R1独立地为卤素，羟基或（C1-4）烷氧基; R 2'与α，β或η-位连接，并且是选自式（a），（b）和（c）的基团，它们是多巴胺β-羟化酶抑制剂，其中化合物的苯并环烷基部分是 选自2,3-二氢化茚基，1,2,3,4-四氢萘基和6,7,8,9-四氢-5H-苯并环庚烯基（其中苯并任选被1-3个取代基取代）并且选择该化合物的偶氮唑硫酮部分 从2-硫代-2,3-二氢-1H-咪唑-3-基，5-硫代-4,5-二氢-1H- [1,2,4]三唑-4-基和5-硫代-4,5-二氢-1H- 5-二氢-1H- [1,2,4]三唑-1-基（各自任选被1至3个取代基取代）; 以及前药，药学上可接受的盐，单独的异构体和异构体的混合物以及使用和制备此类苯并环烷基唑硫酮化合物的方法。