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。

公开(公告)号：US20040087660A1

公开(公告)日：2004-05-06

申请号：US10643941

申请日：2003-08-20

Applicant: Sepracor Inc.

Inventor： Chris Hugh Senanayake ,  Zhengxu Han ,  Dhileepkumar Krishnamurthy ,  Derek Pflum

IPC: A61K031/137

CPC classification number: C07C209/60 ,  C07C313/06 ,  C07C2601/04 ,  C07C211/29

Abstract: This invention encompasses novel methods of preparing sibutramine and sibutramine derivatives, and stereomerically pure sibutramine derivatives in particular. Examples of sibutramine derivatives include, but are not limited to, sibutramine metabolites such as desmethylsibutramine and didesmethylsibutramine. The invention further encompasses novel compounds useful in the synthesis of sibutramine derivatives.

Abstract translation: 本发明包括制备西布曲明和西布曲明衍生物的新方法，特别是立体异构纯的西布曲明衍生物。 西布曲明衍生物的实例包括但不限于西布曲明代谢物如脱甲基西布曲明和二甲基西布曲明。 本发明还包括可用于合成西布曲明衍生物的新化合物。