[EN] PHENYL SULFONYL DERIVATIVES AND THEIR USE AS HISTAMINE H3 ANTAGONISTS<br/>[FR] DÉRIVÉS PHÉNYLSULFONYLE ET LEUR UTILISATION COMME ANTAGONISTES DE L'HISTAMINE H3
申请人:TAKEDA PHARMACEUTICAL
公开号:WO2011121309A1
公开(公告)日:2011-10-06
A compound having the formula (1) wherein W represents N or CH; R1 represents H or C1-3 alkyl; R2 represents a N-containing heterocyclyl ring or a -C1-3 alkylene-N-containing heterocyclyl group; in which any N-containing heterocyclyl comprising or present on R2 may be optionally substituted; or, when W represents N, R1 and R2 and the N atom to which they are attached may join to form an optionally substituted azacyclic ring, wherein the azacylic ring may be optionally substituted; R3 represents H or C1-3 alkyl; R4 represents optionally substituted C3-6 cycloalkyl, heteroaryl or heterocyclyl; or R3 and R4 and the N atom to which they are attached may join to form an optionally substituted heterocyclyl ring; or a pharmaceutically acceptable salt thereof. The compounds of the invention have been found to modulate the histamine H3 receptor.
具有以下式子(1)的化合物:其中W代表N或CH; R1代表H或C1-3烷基; R2代表一个含氮杂环环或-C1-3烷基-含氮杂环基团;其中R2上包含或存在的任何含氮杂环均可选择性地被取代;或者,当W代表N时,R1和R2以及它们附着的N原子可以连接形成一个可选择性取代的氮杂环环,其中该氮杂环环可以选择性地被取代; R3代表H或C1-3烷基; R4代表可选择性取代的C3-6环烷基,杂环芳基或杂环基;或R3和R4以及它们附着的N原子可以连接形成一个可选择性取代的杂环基环;或其药学上可接受的盐。该发明的化合物已被发现可以调节组胺H3受体。