公开(公告)号：US20030171440A1

公开(公告)日：2003-09-11

申请号：US10308878

申请日：2002-12-02

Applicant: SEPRACOR INC.

Inventor： Chris Hugh Senanayake ,  Thomas P. Jerussi ,  Paul T. Grover ,  Qun Kevin Fang ,  Mark Currie

IPC: A61K031/137 ,  A61K031/704 ,  A61K031/277 ,  C07D211/22 ,  A61K031/445 ,  A61K031/40

CPC classification number: C07C217/74 ,  C07C217/52 ,  C07C255/59 ,  C07C2601/02 ,  C07C2601/14

Abstract: Compounds of formula I are effective in treating disorders modulated by opiate receptor activity and/or monoamine activity. 1 In formula I, R1 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl; R2 is selected from hydrogen, hydroxy, cyano, haloalkyl, glycosyl, SO2R5, and OR5; R3 and R4 are independently selected from hydrogen and lower alkyl, or R3 and R4 taken together with nitrogen form a five- or six-membered heterocyclic or substituted heterocyclic ring; and R5 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl.

Abstract translation: 式I的化合物在治疗由阿片剂受体活性和/或单胺活性调节的病症中是有效的。 在式I中，R 1选自烷基，芳基，烷基芳基，取代的烷基，取代的芳基和取代的烷基芳基; R 2选自氢，羟基，氰基，卤代烷基，糖基，SO 2 R 5和OR 5; R 3和R 4独立地选自氢和低级烷基，或R 3和R 4与氮一起形成五元或六元杂环或取代的杂环; R 5选自烷基，芳基，烷基芳基，取代的烷基，取代的芳基和取代的烷基芳基。