申请人:Janssen Pharmaceutica N.V.
公开号:US06576640B1
公开(公告)日:2003-06-10
The present invention concerns compounds of formula (I)
the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C5-12alkanediyl; n is 1 or 2; p is 1 and q is 2; or p is 2 and q is 1; X is —O—, —S—, —S(═O)—, —S(═O)2— or NR2; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; R2 is hydrogen, C1-6alkyl, aryl or C1-6alkyl substituted with aryl; aryl is phenyl or phenyl substituted with a halogen or C1-6alkyl; D is an optionally substituted benzophenone or 3-benzisoxazolyl; having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.
本发明涉及化合物(I)的N-氧化物形式,其药学上可接受的加合物盐和立体化学异构体形式,其中Alk为C5-12烷基二元醇;n为1或2;p为1且q为2;或p为2且q为1;X为—O—、—S—、—S(═O)—、—S(═O)2—或NR2;每个R1独立地为氢、卤素、C1-6烷基、硝基、羟基或C1-4烷氧基;R2为氢、C1-6烷基、芳基或C1-6烷基取代的芳基;芳基为苯基或取代有卤素或C1-6烷基的苯基;D为可选取代的苯基酮或3-苯并异噁唑基;具有中央&agr;2-肾上腺素受体拮抗活性。本发明还涉及它们的制备、药学用途和组合物。