发明名称 Substituted pteridines
摘要 The invention relates to new pteridines which are suitable for treating respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system and cancers. This invention also relates to pharmaceutical compositions containing these compounds.
申请公布号 US8877756(B2) 申请公布日期 2014.11.04
申请号 US201012689273 申请日期 2010.01.19
申请人 Boehringer Ingelheim International GmbH 发明人 Dollinger Horst;Martyres Domnic;Mack Juergen;Goeggel Rolf;Jung Birgit;Nickolaus Peter
分类号 A61K31/5025;C07D519/00;C07D475/08;A61P29/00;A61P1/00;A61P35/00 主分类号 A61K31/5025
代理机构 代理人 Morris Michael P.;Witkowski Timothy X.
主权项 1. A method of treating chronic obstructive pulmonary disease (COPD) or asthma, the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula 1,wherein: R1 is pyrrolidinyl; R2 is piperazinyl; and R3 is NHR3.1 or OR3.1, wherein R3.1 is H or a group selected from branched or unbranched alkyl with 1 to 6 carbon atoms substituted by one or more hydroxyl groups, C1-6-haloalkyl, C1-6-alkylene-O—C1-2-alkyl, a mono- or bicyclic, saturated or partially unsaturated C3-10-cycloalkyl, mono- or bicyclic, saturated or partially saturated, four-to ten-membered heterocyclic group with 1 to 3 heteroatoms selected from S, N, or O, and a mono- or bicyclic, five- to ten-membered heteroaromatic group with 1 to 4 heteroatoms selected from S, N, or O, which may optionally be substituted by one or more groups selected from among OH, halogen, C1-6-alkyl, branched or unbranched alkyl with 1 to 6 carbon atoms substituted by one or more hydroxyl groups, C1-6-haloalkyl, COOR3.3, O—C1-6-alkyl, C6-10-aryl, C3-10-cycloalkyl, four- to ten-membered heterocyclic group, five- to ten-membered heteroaromatic group, and O—C1-4-alkyl-henyl, wherein this group is optionally substituted by one or more groups selected from halogen, OH, C1-3-alkyl, and C1-3-haloalkyl, and wherein R3.3 is H, C1-6-alkyl, or branched or unbranched alkyl with 1 to 6 carbon atoms substituted by one or more hydroxyl groups, or R3 is a saturated or partially saturated, bi- or polycyclic seven-, eight-, nine-, or ten-membered heterocyclic group containing a nitrogen atom and optionally containing one, two, or three other atoms selected from S, N, and O and which are optionally substituted by one or more groups selected from OH, halogen, C1-6-alkyl, branched or unbranched alkyl with 1 to 6 carbon atoms substituted by one or more hydroxyl groups, C14-alkyl-O—C1-3-alkyl, C6-10-aryl, C3-10-cycloalkyl, five- to ten-membered heteroaryl, four- to ten-membered heterocyclic group, C1-2-alkylene-C5-10-heteroaryl, and C1-2-alkylene-C4-10 heterocycle, each of which are optionally substituted by one or more groups selected from methyl, ethyl, O-methyl, Cl, F, and OH,and the pharmacologically acceptable salts, diastereomers, enantiomers, and racemates thereof.
地址 Ingelheim am Rhein DE