发明名称 Cyclohexyl amide derivatives as CRF receptor antagonists
摘要 There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).;
申请公布号 US8835444(B2) 申请公布日期 2014.09.16
申请号 US201113576040 申请日期 2011.01.31
申请人 Novartis AG 发明人 Beattie David;Bruce Ian;Colson Anny-Odile;Culshaw Andrew James;Sharp Thomas
分类号 C07C233/79;C07D213/82;C07D231/12;C07D231/38;C07D249/08;C07D401/12;C07D231/16;C07D473/00;C07D231/54;C07D231/14;C07D405/04;C07D491/052;C07D231/20;C07D231/56;C07D401/04;C07D471/04;C07D401/14 主分类号 C07C233/79
代理机构 代理人 Roth Joshua
主权项 1. A compound of formula I; in which R1 is a group: wherein X1 is haloalkyl C1 to 10; X2 is halogen; R4 together with R5 and the nitrogen to which they are attached forms a group of formula III; R5 together with R4 and the nitrogen to which they are attached forms a group of formula III; X5 is O or —CH2—; X6 is O or —CH2—; R12 is hydrogen, alkyl C1 to 6, alkoxy C1 to 6, hydroxyalkyl C1 to 6, —CO2R11 or phenyl optionally substituted by fluoro; R11 is alkyl C1 to 6; R13 is hydrogen, alkyl C1 to 6 or chloro; R14 is hydrogen, alkyl C1 to 6, methoxy, hydroxyalkyl C1 to 6, ethoxycarbonyl, pyridyl, benzo[1,3]dioxo-5-yl or phenyl, optionally substituted by fluoro, alkoxy C1 to 6; R15 is hydrogen or methyl; R16, R17, R18, R19, R20, which may be the same or different, are each hydrogen or alkyl C1 to 6; and stereoisomers thereof; in free form or in salt form; provided that the compound of formula I is not: trans-2-chloro-N-[4-(3,5-dimethyl-pyrazol-1-ylmethyl)-cyclohexyl]-5-trifluoromethyl-benzamide; trans-2-chloro-N-[4-(3,5-di-(d3)-methyl-pyrazol-1-ylmethyl)-cyclohexyl]-5-trifluoromethyl-benzamide; trans-2-chloro-N-[4-(5-methyl-pyrazol-1-ylmethyl)-cyclohexyl]-5-trifluoromethyl-benzamide; trans-2-chloro-N-[4-(3-methyl-pyrazol-1-ylmethyl)-cyclohexyl]-5-trifluoromethyl-benzamide; trans-2-chloro-N-{4-[3-(4-methoxy-phenyl)-pyrazol-1-ylmethyl]-cyclohexyl}-5-trifluoromethyl-benzamide; 2-chloro-N-[4-(4-chloro-3,5-dimethyl-pyrazol-1-ylmethyl)-cyclohexyl]-5-trifluoromethyl-benzamide; 2-chloro-5-trifluoromethyl-N-[4-(3,4,5-trimethyl-pyrazol-1-ylmethyl)-cyclohexyl]-benzamide; 2-chloro-N-[4-(3-phenyl-pyrazol-1-ylmethyl)-cyclohexyl]-5-trifluoromethyl-benzamide.
地址 Basel CH