发明名称 Substituted fused imidazoles and pyrazoles and use thereof
摘要 The present application relates to novel substituted fused imidazoles and pyrazoles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof producing medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
申请公布号 US9023849(B2) 申请公布日期 2015.05.05
申请号 US201313736692 申请日期 2013.01.08
申请人 Bayer Intellectual Property GmbH 发明人 Follmann Markus;Stasch Johannes-Peter;Redlich Gorden;Griebenow Nils;Lang Dieter;Wunder Frank;Paulsen Holger;Hübsch Walter;Vakalopoulos Alexandros;Tersteegen Adrian
分类号 A61K31/5365;C07D253/00;C07D487/04;C07D519/00;A61K31/519;A61K31/53;A61K45/06 主分类号 A61K31/5365
代理机构 Buchanan Ingersoll & Rooney PC 代理人 Buchanan Ingersoll & Rooney PC
主权项 1. A compound of formula (I) wherein A is nitrogen or CR3 whereR3 is hydrogen, fluorine, difluoromethyl, trifluoromethyl, methyl, ethyl, cyclopropyl or cyclobutyl, L is a #-CR4AR4B—(CR5AR5B)m-## group where# is the attachment site to the carbonyl group,## is the attachment site to the pyrimidine or triazine ring,m is a number 0,R4A is hydrogen, fluorine, methyl, ethyl, hydroxyl or amino,R4B is hydrogen, fluorine, difluoromethyl, trifluoromethyl, methyl, ethyl, cyclopropyl, cyclobutyl, cyclopentyl or a group of the formula -M-R6, in which methyl and ethyl may each be substituted by 1 to 3 substituents selected independently from the group of fluorine, cyano, trifluoromethyl, cyclopropyl, cyclobutyl, difluoromethoxy and trifluoromethoxy,where R4B is hydrogen, difluoromethyl, trifluoromethyl, methyl, ethyl, cyclopropyl, cyclobutyl, cyclopentyl or a group of the formula -M-R6 when R4A is hydroxyl,and in whichM is a bond,R6 is —(C═O)r—NR7R8, phenyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl or pyrimidinyl, in whichr is the number 1,R7 and R8 are each independently hydrogen, or cyclopropyl,andin which phenyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl and pyrimidinyl may each in turn be substituted by 1 or 2 substituents selected independently from the group of fluorine, difluoromethyl, trifluoromethyl, methyl, ethyl, isopropyl, 2,2,2-trifluoroethyl, 1,1,2,2,2-pentafluoroethyl, cyclopropyl, cyclobutyl, cyclopropylmethyl and cyclobutylmethyl,orR4A and R4B together with the carbon atom to which they are bonded form a cyclopropyl, cyclobutyl, cyclopentyl, azetidinyl, tetrahydrofuranyl, pyrrolidinyl or tetrahydropyranyl ring, in which the cyclopropyl, cyclobutyl, cyclopentyl, azetidinyl, tetrahydrofuranyl, pyrrolidinyl and tetrahydropyranyl ring may each be substituted by 1 or 2 substituents selected independently from the group of fluorine and methyl, the ring Q is a group of the formula where * is the attachment site to —CH2—R2, ** is the attachment site to the pyrimidine or triazine ring, A1 is N or CH, R1a is hydrogen or methyl, R1b is hydrogen, fluorine or chlorine when A1 is CH, R1b is hydrogen when A1 is N, R1c is hydrogen or fluorine, R1d is hydrogen or chlorine, R2 is 3,3,3-trifluoroprop-1-yl, 2,2,3,3-tetrafluoroprop-1-yl, pentafluoroprop-1-yl, phenyl or pyridyl, where phenyl is substituted by 1 to 3 fluorine substituents,andwhere pyridyl may be substituted by 1 fluorine substituent, or a salt thereof.
地址 Monheim DE