发明名称 2,3-disubstituted pyrazinesulfonamides as CRTH2 inhibitors
摘要 The present invention is related to the use of 2,3 substituted pyrazine sulfonamides of formula (I); for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity.
申请公布号 US8796280(B2) 申请公布日期 2014.08.05
申请号 US200611918294 申请日期 2006.04.20
申请人 Merck Serono, S.A. 发明人 Page Patrick;Schwarz Matthias;Sebille Eric;Cleva Christophe;Merlot Cedric;Maio Maurizio
分类号 A61K31/4965;C07D409/12;C07D401/10;C07D241/22;C07D413/10;C07D405/12;C07D403/10;C07D401/12 主分类号 A61K31/4965
代理机构 EMD Serono Research and Development Institute 代理人 EMD Serono Research and Development Institute ;Brown Thomas W.
主权项 1. A pharmaceutical composition which inhibits chemoattractant receptor-homologous molecule expressed on T-helper 2 cell activity comprising a pharmaceutically acceptable carrier, diluent or excipient and a compound according to Formula (I), or stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein: A is selected from the group consisting of: where n is 0, 1, 2, 3 or 4; m is 2; B is selected from the group consisting of phenyl or piperazinyl; R1 is hydrogen; R2 is phenyl, wherein R2 is optionally substituted with one or more substituents selected from the group consisting of halogen, cyano, C1-C6-alkyl; R3 is selected from the group consisting of C1-C6-alkyl, aryl, heteroaryl, C1-C6-alkylaryl, C1-C6-alkylheteroaryl, C3-C8-cycloalkyl and C3-C8-heterocycloalkyl wherein each of said C1-C6-alkyl, aryl, heteroaryl, C1-C6-alkylaryl, C1-C6-alkylheteroaryl, C3-C8-cycloalkyl and C3-C8-heterocycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halogen, cyano, C1-C6-alkyl, C1-C6-alkoxy, heteroaryl, aryl, thioalkoxy and thioalkyl, or wherein said aryl, heteroaryl, C1-C6-alkylaryl, C1-C6-alkylheteroaryl, C3-C8-cycloalkyl or C3-C8-heterocycloalkyl may be fused to one or more aryl, heteroaryl, C3-C8-cycloalkyl or C3-C8-heterocycloalkyl groups and may be substituted with one or more substituents selected of the group consisting of C1-C6-alkyl, alkoxy, aryl, heteroaryl, carboxyl, cyano, halogen, hydroxy, amino, aminocarbonyl, nitro, sulfoxy, sulfonyl, sulfonamide and trihaloalkyl; R7 is selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, heteroaryl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, carboxy, cyano, amino and hydroxy; the aryl is selected from phenyl or naphthyl; and the heteroaryl is selected from pyridyl, indolyl, benzimidazolyl and quinolyl.
地址 Coinsins, Vaud CH