发明名称 Oxazole pyridine derivatives useful as S1P1 receptor agonists
摘要 The present invention provides oxadiazole pyridine derivatives of Formula (I), their use as medicaments and their use for treating multiple sclerosis and other diseases.
申请公布号 US8791142(B2) 申请公布日期 2014.07.29
申请号 US201013203044 申请日期 2010.03.02
申请人 Merck Serono S.A. 发明人 Quattropani Anna;Gerber Patrick;Dorbais Jerome
分类号 A61K31/443;C07D413/04 主分类号 A61K31/443
代理机构 Saliwanchik, Lloyd & Eisenschenk 代理人 Saliwanchik, Lloyd & Eisenschenk
主权项 1. A compound of formula (I): wherein: R1 denotes —CO2R3, —CON(H)2-p(A)p, —N(H)(CH2)nCO2R3, —N(R3)(CH2)nCO2R3, —NH—CO-A, Hal, —CF3, —OCF3, —OH, —OA, —CN, or —NO2, —(CH2)sN(H)2-p(A)p, —CH(CH3)(CH2)nN(H)2-p(A)p, —CH(R3)(CH2)nN(H)2-p(A)p, —(CH2)sN(R3)(CH2)nCO2R3, —(CH2)sNH—CO-A, —(CH2)nN(R3)2, —CH(CH3)(CH2)nN(R3)CH(CH3)(CH2)nCO2R3, or —CH(R3)(CH2)nN(R3)CH(R3)(CH2)nCO2R3, or when in position meta or para to the oxadiazole ring, R1 also denotes —N(H)2-p(A)p or A, R2 is H, Hal, —CN, —NO2, —OH, OA, —CO2R3, —CON(H)2-p(A)p, —N(H)(CH2)nCO2R3, —NH—CO-A, —CF3, or —OCF3, or when in position meta or para to the oxadiazole ring, R2 also denotes —N(H)2-p(A)p or A, Ra and Rb are independently from each other A, —CF3, Hal, —CH2—OR3, OR3, —OCF3, (C1-C7)alkyl, —(CH2)nO(CH2)nOMe or CH(CH3)OCH3, W, Y are independently from each other CH, Z denotes Ar, A is branched or linear alkyl having 1 to 12 C-atoms, wherein one or more H-atoms are optionally substituted Hal, OR3, CN, CO2R3 or N(R3)2 and wherein one or more non-adjacent CH2-groups are optionally substituted by O, NR3 or S and/or by —CH═CH— or —C≡C— groups, or A denotes a cycloalkyl or cycloalkylalkylene having 3-7 ring C atoms, Ar denotes a monocyclic or bicyclic, aromatic carbocyclic ring having 6 carbon atoms, which is unsubstituted, monosubstituted, disubstituted or trisubstituted by Hal, —CF3, —OCF3, —NO2, —CN, perfluoroalkyl, A, OA, —OH, —NH2, —COH, —COOR3, —CONH2, —CON(H)2-qAq, —NR3(CH2)nCOA, —NR3(CH2)nCOOA, —NR3(CH2)nCOR3, —N(H)2-qAq, —NHSO2A, —NHSO2—N(H)2-m(A)m, —N(H)1-qAqCOA, —N(H)1-qAqSO2—N(H)2-m(A)m, —N(H)1-qAqCON(H)2-m(A)m, —COOA, —SO2A, —SO2N(H)2-m(A)m, or —(CH2)nOR3, Hal is F, Cl, Br or I, R3 is H or A, m is 0, 1 or 2, p is 0, 1 or 2, q is 0 or 1, s is 1, 2, 3, 4 or 5, n is 0, 1, 2, 3, 4 or 5, and pharmaceutically acceptable salts thereof.
地址 Coinsins, Vaud CH