发明名称 Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation
摘要 The present invention relates to compounds defined by formula I; wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
申请公布号 US9029544(B2) 申请公布日期 2015.05.12
申请号 US201113029697 申请日期 2011.02.17
申请人 Boehringer Ingelheim International GmbH 发明人 Wagner Holger;Berta Daniela;Fuchs Klaus;Giovannini Riccardo;Hamprecht Dieter Wolfgang;Konetzki Ingo;Streicher Ruediger;Trieselmann Thomas
分类号 C07D491/20;A61K31/506;C07D491/048;C07D491/04;C07D215/56 主分类号 C07D491/20
代理机构 代理人 Morris Michael P.;Kershner David L.;Patel Usha R.
主权项 1. A compound of formula I wherein R1 is a mono- or bicyclic 5- to 10-membered aryl or heteroaryl group, which heteroaryl contains 1 to 4 heteroatoms selected from the group consisting of N, O and S, and which aryl or heteroaryl may optionally be substituted by R9, R10 and/or R11, in which R9 is hydrogen, halogen, cyano, 1-4C-alkyl, 2-4C-alkenyl, 3-6C-cycloalkyl, 1-4C-alkoxy, completely or partially fluorine-substituted 1-4C-alkyl, completely or partially fluorine-substituted 1-4C-alkoxy, pentafluorosulfanyl, cyano-1-4C-alkyl, 1-2C-alkyl-3-6C-cycloalkyl, cyano-3-6C-cycloalkyl, 1-2C-alkoxy-1-4C-alkyl, hydroxy-1-4C-alkyl or 3-(1-2C-alkyl)-oxetan-3-yl, R10 is hydrogen, halogen, cyano, 1-4C-alkyl, 2-4C-alkenyl, 3-6C-cycloalkyl, 1-4C-alkoxy, completely or partially fluorine-substituted 1-4C-alkyl, completely or partially fluorine-substituted 1-4C-alkoxy, cyano-1-4C-alkyl, methyl-3-6C-cycloalkyl, cyano-3-6C-cycloalkyl, methoxy-1-4C-alkyl, hydroxy-1-4C-alkyl or 3-(1-2C-alkyl)-oxetan-3-yl, R11 is hydrogen or halogen, or R9 and R10 together and with inclusion of the carbon atoms, to which they are attached, form a 5-6C-cycloalkane ring wherein one methylene group may optionally be replaced by oxygen, which ring, for the case of 6-membered ring system, may optionally contain a double bond, and/orwhich ring may optionally be mono- or disubstituted by methyl, wherein, for the case that both methyl groups are connected to the same carbon, the methyl groups together with the carbon to which they are connected, may optionally form a cyclopropyl ring, R2 is 1-6C-alkyl, 1-3C-perfluoroalkyl, 1-4C-alkoxy-1-4C-alkyl, or 4-7C-cycloalkyl, which 4-7C-cycloalkyl may optionally be mono- or disubstituted by fluorine, hydroxy, methoxy and/or 1-2C-alkyl and in which, for the case of 5-7C-cycloalkyl systems, one methylene group may optionally be replaced by oxygen, R3 is hydrogen or 1-4C-alkyl, R4 is hydrogen or 1-4C-alkyl, or R3 and R4 together and with inclusion of the carbon atom, to which they are attached, form a 4-7C-cycloalkane ring, R5 is hydrogen or 1-4C-alkyl, R6 is 1-4C-alkyl, R7 is hydrogen or 1-4C-alkyl, or R6 and R7 together and with inclusion of the carbon atom, to which they are attached, form a 5-7C-cycloalkane ring wherein one methylene group may optionally be replaced by oxygen,which ring may optionally contain one double bond, and/orwhich ring may optionally be mono- or disubstituted by fluorine, hydroxyl, 1-2C-alkoxy and/or 1-2C-alkyl, R8 is hydrogen, acetoxy, propionyloxy, methoxy or hydroxy, or a tautomer thereof, a stereoisomer thereof, a mixture thereof or a salt thereof.
地址 Ingelheim am Rhein DE