发明名称 N-PROP-2-YNYL CARBOXAMIDE DERIVATIVES AND THEIR USE AS TRPA1 ANTAGONISTS
摘要 Compounds of formula I, wherein A, B, X, Z and R1-R6, are as defined in the claims, exhibit TRPA 1 activity and are thus useful as TRPA1 modulators.;
申请公布号 US2015376130(A1) 申请公布日期 2015.12.31
申请号 US201314674940 申请日期 2013.09.30
申请人 ORION CORPORATION 发明人 ARVELA Riina;HEIKKINEN Terhi;HOLM Patrik;PRUSIS Peteris;ROSLUND Mattias;SALO Harri
分类号 C07D213/82;C07C237/30;A61K31/166;C07D319/18;A61K31/357;C07D239/42;A61K31/505;C07C255/60;A61K31/277;C07D401/12;A61K31/444;C07D417/12;A61K31/4439;C07D217/02;A61K31/472;A61K31/5377;A61K31/455 主分类号 C07D213/82
代理机构 代理人
主权项 1. A compound of Formula I, wherein A and B form, together with the atoms to which they are attached, wherein the atoms marked with * and *′ are bonded to the parent molecular moiety; X is CR5 or N; Y is CR6 or N; Z is CR4 or N, provided that when Y or X is N, then Z is not N; R1 is (C1-C6)alkyl, cyclo(C3-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkyl, halo(C1-C6)alkoxy(C1-C6)alkyl, (C1-C6)alkyl-S—(C1-C6)alkyl, heterocyclyl, heterocyclyl(C1-C3)alkyl, phenyl, phenyl(C1-C3)alkyl, or phenoxy(C1-C6)alkyl, wherein said cyclo(C3-C6)alkyl, heterocyclyl, or phenyl is unsubstituted or substituted with 1 or 2 substituent(s) each independently being halogen, (C1-C5)alkyl, halo(C1-C5)alkyl, (C1-C5)alkoxy, cyclo(C3-C6)alkyl, CN, halo(C1-C5)alkoxy, (C1-C5)alkyl-S—, (C1-C5)alkyl-(S═O)—, (C1-C5)alkyl-(O═S═O)—, (C1-C3)alkylamino or di(C1-C3)alkylamino; R2 is (C1-C6)alkyl; R3 is (C1-C6)alkyl; R4 is H, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, halo(C1-C6)alkoxy, (C1-C6)alkoxy(C1-C6)alkoxy, (C1-C6)alkyl-S—, (C1-C6)alkylamino, halo(C1-C5)alkylamino, (C1-C6)alkyl(C═O), CN, or heterocyclyl; R5 is H, halogen, (C1-C6)alkyl, cyclo(C3-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkyl, halo(C1-C6)alkoxy, (C1-C6)alkoxy(C1-C6)alkoxy, (C1-C6)alkyl-S—, (C1-C6)alkyl-(S═O)—, (C1-C6)alkyl-(O═S═O)—, halo(C1-C6)alkyl-S—, halo(C1-C6)alkylamino, (C1-C6)alkyl(C═O), or CN; and R6 is H, halogen, (C1-C6)alkyl, or halo(C1-C6)alkyl; or R1 and R6 form, together with the atoms to which they are attached, a condensed 5 or 6 membered saturated or unsaturated heterocyclic ring containing, in addition to the nitrogen atom to which R1 is attached, 0 or 1 further heteroatom selected from N, O, and S, wherein said heterocyclic ring is unsubstituted or substituted with 1 or 2 substituent(s) each independently being (C1-C2)alkyl or halogen; or R4 and R5 form, together with the carbon ring atoms to which they are attached, a condensed 5, 6 or 7 membered saturated or unsaturated carbocyclic ring or a condensed 5, 6, or 7 membered saturated or unsaturated heterocyclic ring containing 1 or 2 heteroatom(s) selected from N, O, and S, wherein said carbocyclic or heterocyclic ring is unsubstituted or substituted with 1 or 2 substituent(s) each independently being (C1-C2)alkyl or halogen; or a pharmaceutically acceptable salt or ester thereof; with the proviso that the compound is not 2-(methylamino)-N-(2-methylbut-3-yn-2-yl)benzamide or N-(2-methylbut-3-yn-2-yl)-2-(propylamino)benzamide.
地址 Espoo FI