发明名称 SUBSTITUTED PHENYLALANINE DERIVATIVES
摘要 The invention relates to substituted phenylalanine derivatives and to processes for preparation thereof, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and/or severe perioperative blood loss.
申请公布号 US2016222056(A1) 申请公布日期 2016.08.04
申请号 US201415024974 申请日期 2014.09.24
申请人 BAYER PHARMA AKTIENGESELLSCHAFT 发明人 RÖHN Ulrike;ELLERMANN Manuel;STRASSBURGER Julia;WENDT Astrid;RÖHRIG Susanne;WEBSTER Robert Alan;SCHMIDT Martina Victoria;TERSTEEGEN Adrian;BEYER Kristin;SCHÄFER Martina;BUCHMÜLLER Anja;GERDES Christoph;SPERZEL Michael;SANDMANN Steffen;HEITMEIER Stefan;HILLISCH Alexander;ACKERSTAFF Jens;TERJUNG Carsten
分类号 C07K5/065 主分类号 C07K5/065
代理机构 代理人
主权项 1. A compound of the formula in which R1 is a group of the formula where # is the attachment site to the nitrogen atom,R6 is 5-membered heteroaryl, where heteroaryl may be substituted by a substituent selected from the group consisting of oxo, chlorine, cyano, hydroxyl and C1-C3-alkyl, in which alkyl may be substituted by 1 to 3 substituents selected independently from the group consisting of hydroxyl, amino, hydroxycarbonyl and methoxy, orin which alkyl may be substituted by 1 to 7 fluorine substituents, orin which alkyl is substituted by a substituent selected from the group consisting of hydroxyl, amino, hydroxycarbonyl and methoxy, and in which alkyl is additionally substituted by 1 to 6 fluorine substituents,R7 is hydrogen, fluorine or chlorine,R8 and R9 together with the carbon atoms to which they are bonded form a 5-membered heterocycle, where the heterocycle may be substituted by 1 to 2 substituents selected independently from the group consisting of oxo, chlorine, cyano, hydroxyl, C1-C3-alkyl, pyrazolyl and pyridyl, in which alkyl may be substituted by 1 to 3 substituents selected independently from the group consisting of hydroxyl, amino, hydroxycarbonyl and methoxy, orin which alkyl may be substituted by 1 to 7 fluorine substituents, orin which alkyl is substituted by a substituent selected from the group consisting of hydroxyl, amino, hydroxycarbonyl and methoxy, and in which alkyl is additionally substituted by 1 to 6 fluorine substituents,R10 is hydrogen, fluorine or chlorine, R2 is hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl, 4- to 9-membered heterocyclyl bonded via a carbon atom or 5- or 6-membered heteroaryl, where alkyl may be substituted by 1 to 2 substituents selected independently from the group consisting of fluorine, hydroxyl, amino, hydroxycarbonyl, C1-C3-alkylamino, difluoromethyl, trifluoromethyl, —(OCH2CH2)n—OCH3, —(OCH2CH2)m—OH, trimethylaminium and pyrrolidinyl, in which n is a number from 1 to 6,in which m is a number from 1 to 6, andwhere cycloalkyl may be substituted by 1 to 2 substituents selected independently from the group consisting of oxo, fluorine, hydroxyl, amino, C1-C4-alkyl, C1-C3-alkylamino and morpholinyl, in which alkyl and alkylamino may be substituted by 1 to 5 fluorine substituents, andwhere heterocyclyl may be substituted by 1 to 2 substituents selected independently from the group consisting of oxo, fluorine, hydroxyl, amino, hydroxycarbonyl, C1-C4-alkyl, C1-C3-alkylamino, difluoromethyl, trifluoromethyl, 2,2,2-trifluoroeth-1-yl, C1-C4-alkoxycarbonyl, aminocarbonyl and C1-C3-alkylaminocarbonyl, where alkyl and alkylamino may be substituted by 1 to 5 substituents selected independently from the group consisting of hydroxyl and fluorine, andwhere heterocyclyl may additionally be substituted by 1 to 4 substituents selected independently from the group consisting of fluorine and methyl, andwhere heteroaryl may be substituted by 1 to 2 substituents selected independently from the group consisting of oxo, chlorine, cyano, hydroxyl and C1-C3-alkyl, R3 is hydrogen or C1-C3-alkyl, or R2 and R3 together with the nitrogen atom to which they are bonded form a 4- to 7-membered heterocycle, where the heterocycle may be substituted by 1 to 2 substituents selected independently from the group consisting of oxo, fluorine, hydroxyl, amino, hydroxycarbonyl, C1-C4-alkyl, C1-C3-alkylamino, difluoromethyl, trifluoromethyl, 2,2,2-trifluoroeth-1-yl, C1-C4-alkoxycarbonyl, aminocarbonyl and C1-C3-alkylaminocarbonyl, R4 is hydrogen, fluorine, chlorine, methyl or methoxy, R5 is hydrogen, fluorine, chlorine, C1-C4-alkyl, methoxy or trifluoromethyl, or one of the salts thereof, solvates thereof or solvates of the salts thereof.
地址 Berlin DE