发明名称 MACROCYCLIC PYRIDAZINONE DERIVATIVES
摘要 The present invention relates to compounds of formula (I) Wherein R1, R2, R3, R4, L and Z have the meaning given in claim 1, and their use in the prophylaxis and treatment of diseases.;
申请公布号 US2015376206(A1) 申请公布日期 2015.12.31
申请号 US201414766291 申请日期 2014.02.07
申请人 MERCK PATENT GMBH 发明人 JORAND-LEBRUN Catherine;KULKARNI Santosh;CHRISTMANN-FRANCK Serge
分类号 C07D498/18;C07D487/22;A61K45/06;C07D471/22;C07D487/18;A61K31/504 主分类号 C07D498/18
代理机构 代理人
主权项 1: A compound of formula (I) wherein R1, R3 denote each, independently of one another H, (CH2)pCON(R5)2, OA, Hal, COOH, COOA, (CH2)pNHCOA, (CH2)pHet1, (CH2)pNR2R5, or OH; R2 denotes H or linear or branched alkyl with 1, 2 or 3 C atoms, wherein one or two H atoms of the alkyl group are optionally replaced by OR6, NR5R6, NHCOR5, CONR5R6; R4 denotes H or A; R5 denotes H or linear or branched alkyl with 1, 2 or 3 C atoms; R6 denotes H or linear or branched alkyl with 1, 2 or 3 C atoms; Z is absent or denotes Ar-diyl or Het-diyl; L denotes (CH2)n wherein one or two CH2 groups are optionally replaced by O and/or a CH═CH-group, and/or wherein one or two H atoms are optionally replaced by OR2, NR2R5 or Het1; Ar-diyl denotes 1,2-, 1,3- or 1,4-phenylen optionally substituted with from 1 to 5 groups independently selected from the group consisting of Hal, CN, —CF3, —OCF3, OH, O-A, SO2-A, COOH, COOA, —CO-A, O-phenyl, SO2-phenyl, SO2—CF3, Het2 and A; Het-diyl denotes an unsaturated, saturated or aromatic 5- or 6-membered heterocycle comprising 1 to 2 N, O and/or S atoms, which are optionally unsubstituted or mono-, di- or trisubstituted by Hal, CN, —CF3, —OCF3, O-A, SO2-A, COOH, COOA, —CO-A, O-phenyl, SO2-phenyl, SO2—CF3, Het2 and/or A; A denotes an unbranched or branched alkyl comprising 1 to 10 C atoms, in which 1 to 5 H atoms are optionally replaced by F and/or in which one or two non-adjacent CH2 groups are optionally replaced by O; Het1 denotes morpholinyl, piperidinyl or pyrrolidinyl; Het2 denotes morpholinyl, piperidinyl or pyrrolidinyl; Hal denotes F, Cl, Br, I; n denotes 1, 2, 3, 4, 5 or 6; p denotes 0, 1 or 2; including pharmaceutically acceptable solvates, hydrates, and salts thereof.
地址 Darmstadt DE