发明名称 Piperidine derivatives, pharmaceutical compositions and uses thereof
摘要 The invention relates to new piperidine derivatives of the formula I; to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
申请公布号 US8759528(B2) 申请公布日期 2014.06.24
申请号 US201213691971 申请日期 2012.12.03
申请人 Boehringer Ingelheim International GmbH 发明人 Roth Gerald Juergen;Fleck Martin;Lehmann-Lintz Thorsten;Nosse Bernd
分类号 C07D211/20;C07D211/26;C07D211/68;C07D213/02;A01N43/40;A61K31/445;C07D413/14;C07D211/22;C07D211/34;C07D401/04 主分类号 C07D211/20
代理机构 代理人 Morris Michael P.;Stempel Alan R.
主权项 1. A compound of the formula Iwherein either X is N and Y is CH, or X is CH and Y is N; Ar1 is selected from the group consisting of: phenylene, pyridinylene and pyrimidinylene,wherein each of the beforementioned groups may be substituted with a substituent RA; RA is selected from the group consisting of: H, F, Cl, Br, I, CN, OH, —NO2, C1-4-alkyl, C2-4-alkenyl, C1-4-alkyl-O—, C1-4-alkyl-C(═O)—, H2N—, H2N—C(═O)—, H2N—S(═O)2—, HO—C(═O)—, C1-4-alkyl-O—C(═O)—, phenyl and phenyl-C1-3-alkyl, wherein in each NH2-group, one or both hydrogen atoms may independently be replaced by C1-4-alkyl; R1 is selected from the group consisting of: OH, C1-4-alkyl-O—, C3-7-cycloalkyl-O—, C3-7-cycloalkyl-C1-3-alkyl-O—, H2N—, (C1-4-alkyl)NH—, (C1-4-alkyl)2N—, C3-7-cycloalkyl-NH—, C3-7-cycloalkyl-N(C1-4-alkyl)-, C1-4-alkyl-C(═O)—, C1-4-alkyl-S(═O)2-, HO—C(═O)—, C1-4-alkyl-O —C(═O)—, H2N—C(═O)—, (C1-4-alkyl)HN—C(═O)— and (C1-4-alkyl)2N—C(═O)—, wherein each alkyl or cycloalkyl may be optionally substituted with one or more substituents selected from F and OH; Ar2 is selected from the group consisting of: phenylene and a 5- or 6-membered monocyclic aromatic ring containing 1, 2 or 3 heteroatoms selected from N, O, or S, R2 is selected from the group consisting of: H and C1-alkyl; R3 is selected from the group consisting of: H and methyl; R4 is selected from the group consisting of: H, C1-4-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-3-alkyl, phenyl, and phenyl-C1-3-alkyl, wherein each alkyl and cycloalkyl may be optionally substituted with one or more groups independently selected from the group consisting of: F, Cl, Br, CN, OH and —O—(C1-4-alkyl), andwherein each phenyl group may be optionally substituted with one or more substituents L; or R3 and R4 may be connected with each other and together with the N-atom to which they are attached form a group selected from the group consisting of: azetidinyl, pyrrolidinyl, piperidinyl and azepanyl, wherein in each of these groups one or two CH2-groups may be independently replaced by N, O, S, C(═O) or SO2, and/orwherein each of these groups may be substituted by one or more C1-4-alkyl; and L is selected from the group consisting of: F, Cl, Br, CN, OH, C1-alkyl-, C1-4-alkyl-O—, C1-4-alkyl-S—, C1-4-alkyl-S(═O)2-, H2N—, (C1-4-alkyl)NH—, (C1-4-alkyl)2N— and heterocyclyl,wherein each alkyl may be optionally substituted with one or more F-atoms and/ or with a substituent selected from OH, C1-3-alkyl-O— and CN; andwherein two substituents L attached to an aryl or heteroaryl group may be linked to each other and form a C2-5-alkylene bridging group in which 1 or 2 —CH2-groups may be replaced by a group independently of each other selected from O, S, NH and N(C1-4-alkyl)-, wherein the C2-5-alkylene bridging group is optionally be substituted by 1 or 2 C1-3-alkyl groups; or a pharmaceutically acceptable salt thereof.
地址 Ingelheim am Rhein DE