发明名称 Tetraaza-cyclopenta[a]indenyl and their use as Positive Allosteric Modulators
摘要 The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.;
申请公布号 US2015018343(A1) 申请公布日期 2015.01.15
申请号 US201214366901 申请日期 2012.11.30
申请人 Merck Patent GmbH 发明人 Swinnen Dominique;Montagne Cyril;Pomel Vincent;Quattropani Anna;Molette Jerome;Gerber Patrick
分类号 C07D487/14;A61K31/519;A61K31/5513 主分类号 C07D487/14
代理机构 代理人
主权项 1. A compound of Formula (I) wherein R1, R2, R3 are each independently H, linear or branched C1-C6-alkyl, linear or branched C1-C6-alkoxy, Hal, or hydroxyl; Ra, Rb are each independently H, Hal, hydroxy or A; Q denotes a 6-membered aromatic group or a 5-6-membered heteroaromatic group having 1 to 4 heteroatoms independently selected from N, O and S; R4 denotes G, OG, SG, OCHF2, OCF2CHF2, NR5G, —COOG, or OCOG; each R5 is independently H or a linear or branched alkyl having 1 to 6 carbon atoms; each G is independently —CH3, —CF3, —CH2-A, Het, Cyc, Ar, —CH2-Het, —CH2-Cyc, —CH2—Ar, Hal, or hydroxy; each Hal is independently F, Cl, Br or I; each A is independently a linear or branched carbon chain having 1 to 6 carbon atoms, wherein 1 to 3 non adjacent —CH2-groups may be independently from each other substituted by a group selected from O, NR5, S, SO, SO2, CO, and wherein 1 to 5 hydrogen atoms may be independently from each other substituted by Het, Cyc, Ar, or Hal; each Het is independently a saturated, unsaturated or aromatic ring, each of which is monocyclic, bicyclic, or fused-bicyclic, and having 3- to 8-members and containing 1 to 4 heteroatoms independently selected from N, NR5, O, S, CO, SO or SO2, each of which may be substituted by 1 to 3 substituents independently selected from A, Hal, OH and Het1; Het1 denotes a 4, 5 or 6 membered carbocyclic ring wherein 1 or 2 carbon atom are replaced by Oxygen atoms. each Ar is independently a 6-membered carbocyclic aromatic ring or a fused or non fused byclic aromatic ring, and optionally substituted by 1 to 3 substituents independently selected from A or Hal; each Cyc is independently a saturated or unsaturated carbocyclic ring having from 3 to 8 carbon atoms and optionally substituted by 1 to 3 substituents independently selected from A or Hal; and/or pharmaceutically acceptable derivatives, tautomers, salts, solvates and stereoisomers thereof.
地址 Darmstadt DE