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    • 8. 发明申请
    • N-(ACYLAMINOMETHYL)GLUTARYL AMINO ACIDS AND THEIR USE AS DUAL INHIBITORS OF NEUTRAL ENDOPEPTIDASE AND ANGIOTENSIN CONVERTING ENZYME
    • N-(ACYLAMINOMETHYL)GLUTARYL氨基酸及其作为中性内切酶和血管紧张素转换酶的双重抑制剂的用途
    • WO1994006756A1
    • 1994-03-31
    • PCT/US1993008706
    • 1993-09-21
    • SCHERING CORPORATION
    • SCHERING CORPORATIONNEUSTADT, Bernard, R.
    • C07C271/22
    • C07D295/215C07C237/24C07C271/22C07C275/14C07C307/06C07C311/05C07C2601/08
    • Novel glutarylamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of formula (I) wherein: R1 and R3 are independently hydroxy, lower alkoxy, aryllower alkoxy, amino, lower alkylamino and di-(lower alkyl)amino; R2 is H or hydroxy; R4 is aryl, substituted aryl, heteroaryl or substituted heteroaryl; R6 is H or R7-(CH2)3-, wherein R7 is amino or (aryllower alkoxy)carbonylamino; Q is -C(O)- or -SO2; Y is lower alkyl, lower alkoxy, aryllower alkoxy, amino, lower alkylamino, di-(lower alkyl)amino, or a group of formula (a), wherein A is a bond, -N(R5)-, or -O-; and R5 is H or lower alkyl; B is H or Z-(CH2)m-; Z is amino, lower alkylamino, di-(lower alkyl)amino, (aryllower alkoxy)carbonylamino, 1-pyrrolidino or 1-piperidino; m = 1, 2, 3, 4 or 5; and n = 1, 2 or 3; or a pharmaceutically acceptable addition salt thereof; useful in the treatment of cardiovascular disorders, are disclosed.
    • 式(I)的中性内肽酶和血管紧张素转换酶的新型戊二酰氨基酸衍生物双重抑制剂,其中:R1和R3独立地是羟基,低级烷氧基,芳基低级烷氧基,氨基,低级烷基氨基和二 - (低级烷基)氨基; R2是H或羟基; R4是芳基,取代的芳基,杂芳基或取代的杂芳基; R6是H或R7-(CH2)3-,其中R7是氨基或(芳基低级烷氧基)羰基氨基; Q是-C(O) - 或-SO 2; Y是低级烷基,低级烷氧基,芳基低级烷氧基,氨基,低级烷基氨基,二(低级烷基)氨基或式(a)的基团,其中A是键,-N(R5) - 或-O- ; R5为H或低级烷基; B是H或Z-(CH 2)m - ; Z是氨基,低级烷基氨基,二(低级烷基)氨基,(芳基低级烷氧基)羰基氨基,1-吡咯烷子基或1-哌啶子基; m = 1,2,3,4或5; 和n = 1,2或3; 或其药学上可接受的加成盐; 可用于治疗心血管疾病。