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 US2016237045(A1) 申请公布日期 2016.08.18
申请号 US201415024939 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 C07D257/04;C07D401/12;C07D249/08;C07D405/12 主分类号 C07D257/04
代理机构 代理人
主权项 1. A compound of the formula in which R1 represents a group of the formula where # is the point of attachment to the nitrogen atom,R5 represents 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 independently of one another selected from the group consisting ofhydroxy, 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 hydroxy, amino, hydroxycarbonyl and methoxy, and in which alkyl is additionally substituted by 1 to 6 fluorine substituents,R6 represents hydrogen, fluorine or chlorine,R7 and R8 together with the carbon atoms to which they are attached form a 5-membered heterocycle, where the heterocycle may be substituted by 1 to 2 substituents independently of one another selected 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 independently of one another selected from the group consisting of hydroxy, 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 hydroxy, amino, hydroxycarbonyl and methoxy, and in which alkyl is additionally substituted by 1 to 6 fluorine substituents,R9 represents hydrogen, fluorine or chlorine, R2 represents hydrogen, fluorine, chlorine, methyl or methoxy, R3a represents hydrogen, fluorine, chlorine, C1-C4-alkyl, methoxy or trifluoromethyl, R3b represents hydrogen or fluorine, R4 represents amino, cyano, hydroxymethyl, methyl, C1-C3-alkoxy, C1-C3-alkylamino, C1-C3-alkoxycarbonyl, —S(O)2NR10R11, —C(O)NR12R13 or —NR14(CO)R15, where alkoxy is substituted by 1 to 2 substituents independently of one another selected from the group consisting of fluorine, hydroxy, amino, hydroxycarbonyl, C1-C3-alkylamino, difluoromethyl, trifluoromethyl, —(OCH2CH2)n—OCH3, —(OCH2CH2)m—OH, morpholinyl, piperidinyl and pyrrolidinyl, in which n is a number from 1 to 6,in which m is a number from 1 to 6, andwhere methyl is substituted by 5- or 6-membered heterocyclyl which is attached via a nitrogen atom, andwhere R10 represents hydrogen, C1-C3-alkyl, C3-C6-cycloalkyl, benzyl or 4- to 8-membered heterocyclyl which is attached via a carbon atom,R11 represents hydrogen or C1-C3-alkyl, orR10 and R11 together with the nitrogen atom to which they are attached form a 4- to 7-membered heterocycle,in which 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,R12 represents hydrogen, C1-C3-alkyl, C1-C3-alkoxy, C3-C6-cycloalkyl, benzyl or 4- to 8-membered heterocyclyl which is attached via a carbon atom, in which alkyl may be substituted by 1 to 2 substituents independently of one another selected from the group consisting of fluorine, hydroxy, amino, hydroxycarbonyl, C1-C3-alkylamino, difluoromethyl, trifluoromethyl, —(OCH2CH2)n—OCH3, —(OCH2CH2)m—OH, morpholinyl, piperidinyl and pyrrolidinyl, in which n is a number from 1 to 6, in which m is a number from 1 to 6, andin which cycloalkyl may be substituted by 1 to 2 substituents independently of one another selected from the group consisting of oxo, fluorine, hydroxy, amino, C1-C4-alkyl and C1-C3-alkylamino, in which alkyl and alkylamino for their part may be substituted by 1 to 5 fluorine substituents, andin which heterocyclyl may be substituted by 1 to 2 substituents independently of one another selected from the group consisting of oxo, fluorine, hydroxy, amino, hydroxycarbonyl, C1-C4-alkyl, C1-C3-alkylamino, C1-C4-alkoxycarbonyl, aminocarbonyl and C1-C3-alkylaminocarbonyl, in which alkyl and alkylamino for their part may be substituted by 1 to 5 fluorine substituents, andin which heterocyclyl may additionally be substituted by 1 to 4 substituents independently of one another selected from the group consisting of fluorine and methyl,R13 represents hydrogen or C1-C3-alkyl, orR12 and R13 together with the nitrogen atom to which they are attached form a 4- to 7-membered heterocycle, in which 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, in which alkyl for its part may be substituted by a hydroxy substituent,R14 represents hydrogen or C1-C3-alkyl,R15 represents C1-C4-alkyl, C3-C6-cycloalkyl, phenyl or 5- to 7-membered heterocyclyl, in which alkyl may be substituted by a substituent selected from the group consisting of C1-C3-alkylamino and —NH(CO)CH2NH(CO)CH2NH2, or one of the salts thereof, solvates thereof or solvates of the salts thereof.
地址 Berlin DE