发明名称 UREA DERIVATIVES AND THEIR USE AS FATTY-ACID BINDING PROTEIN (FABP) INHIBITORS
摘要 The invention provides novel compounds having the general formula (I);;wherein R1, R2, R3, R4, W, A and B are as described herein, compositions including the compounds and methods of using the compounds.
申请公布号 US2016002152(A1) 申请公布日期 2016.01.07
申请号 US201514857007 申请日期 2015.09.17
申请人 HOFFMANN-LA ROCHE INC. 发明人 BUETTELMANN BERND;CECCARELLI SIMONA M.;CONTE AURELIA;KUEHNE HOLGER;KUHN BERND;NEIDHART WERNER;OBST SANDER ULRIKE;RICHTER HANS
分类号 C07C275/28;C07C273/18 主分类号 C07C275/28
代理机构 代理人
主权项 1. Compounds of formula (I) wherein R1 and R2 together with the carbon they are attached to form a cycloalkyl; R3 is H, alkyl or cycloalkyl; R4 is H, alkyl or cycloalkyl; W is a bond, —O—, —S—, —NR5—, —C(O)—, —S(O)2—, —C(O)—NR5— or —CR6R7—; R5 is H, alkyl or cycloalkyl; R6 and R7 are independently selected from H, alkyl or cycloalkyl; A is substituted phenyl, substituted thiophenyl, substituted benzothiophenyl, substituted thienopyridinyl, wherein substituted phenyl, substituted thiophenyl, substituted benzothiophenyl and substituted thienopyridinyl are substituted with R8, R9 and R10; B is substituted cycloalkyl, substituted cycloalkenyl, substituted pyridinyl, substituted phenyl, substituted thiophenyl, substituted benzothiophenyl, substituted thienopyridinyl, wherein substituted cycloalkyl, substituted cycloalkenyl, substituted pyridinyl, substituted phenyl, substituted thiophenyl, substituted benzothiophenyl and substituted thienopyridinyl are substituted with R11, R12 and R13; R8, R9, R10 are independently selected from H, alkyl, alkenyl, alkinyl, hydroxyalkyl, haloalkyl, hydroxyhaloalkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, cycloalkylalkoxy, cycloalkoxy, cycloalkoxyalkyl, cycloalkylalkoxyalkyl, alkoxy, alkoxyalkyl, haloalkoxy, haloalkoxyalkyl, alkoxyalkoxy, alkoxyalkoxyalkyl, phenyl, substituted phenyl, pyridinyl, substituted pyridinyl, halogen, hydroxy, cyano, substituted aminosulfonyl, substituted aminocarbonyl, substituted amino and substituted aminoalkyl, wherein substituted aminosulfonyl, substituted aminocarbonyl, substituted amino and substituted aminoalkyl are substituted on the nitrogen atom with one to two substituents independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl and cycloalkylcarbonyl and wherein substituted phenyl and substituted pyridinyl are substituted with one to three substituent selected from alkyl, hydroxyalkyl, haloalkyl, cycloalkyl, alkoxy, haloalkoxy, halogen, hydroxy and cyano; R11, R12 and R13 are independently selected from H, alkyl, alkenyl, alkinyl, hydroxyalkyl, haloalkyl, hydroxyhaloalkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, cycloalkylalkoxy, cycloalkoxy, cycloalkoxyalkyl, cycloalkylalkoxyalkyl, alkoxy, alkoxyalkyl, haloalkoxy, haloalkoxyalkyl, alkoxyalkoxy, alkoxyalkoxyalkyl, phenyl, substituted phenyl, pyridinyl, substituted pyridinyl, halogen, hydroxy, cyano, substituted aminosulfonyl, substituted aminocarbonyl, substituted amino and substituted aminoalkyl, wherein substituted aminosulfonyl, substituted aminocarbonyl, substituted amino and substituted aminoalkyl are substituted on the nitrogen atom with one to two substituents independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl and cycloalkylcarbonyl and wherein substituted phenyl and substituted pyridinyl are substituted with one to three substituent selected from alkyl, hydroxyalkyl, haloalkyl, cycloalkyl, alkoxy, haloalkoxy, halogen, hydroxy and cyano; or pharmaceutically acceptable salts;
地址 Little Falls NJ US