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    Peptidylaminodiols
    56.
    发明授权
    Peptidylaminodiols 失效
    肽基氨基二醇

    公开(公告)号：US5091575A

    公开(公告)日：1992-02-25

    申请号：US713644

    申请日：1991-06-10

    Applicant: Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    Inventor： Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    IPC: A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078

    CPC classification number: C07K5/0227 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06139 ,  A61K38/00

    Abstract: A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sup.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, .alpha.,.alpha.-dimethylbenzyl, 1-benzyloxyethyl; phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl; lowerakenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.6 is of the "S" configuration; or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.

    Abstract translation: 下式的肾素抑制化合物：其中A是取代基; W是C = O或CHOH; U是CH 2或NR 2，条件是当W是CHOH时，U是CH 2; R1是低级烷基，环烷基甲基，苄基，4-甲氧基苄基，卤代苄基，（1-萘基）甲基，（2-萘基）甲基，（4-咪唑基）甲基，α，α-二甲基苄基，1-苄氧基乙基; 苯乙基，苯氧基，硫代苯氧基或苯胺基; R2是氢或低级烷基; R3是低级烷基，[（烷氧基）烷氧基]烷基，（硫代烷氧基）烷基; 苄基或杂环取代的甲基; R4是低级烷基，环烷基甲基或苄基; R5是乙烯基，甲酰基，羟甲基或氢; R7是氢或低级烷基; R8和R9独立地选自OH和NH2; 和R6是氢，低级烷基，乙烯基或芳基烷基; 条件是当R 5和R 7均为氢且R 8和R 9为OH时，碳原子的R 5为“R”构型，碳原子的R 6为“S”构型; 或其药学上可接受的盐或酯。 还公开了肾素抑制组合物，治疗高血压的方法，制备肾素抑制化合物的方法和可用于制备肾素抑制化合物的中间体。

    Heterocyclic renin inhibitors
    58.
    发明授权
    Heterocyclic renin inhibitors 失效
    杂环肾素抑制剂

    公开(公告)号：US4994477A

    公开(公告)日：1991-02-19

    申请号：US173382

    申请日：1988-03-24

    Applicant: Dale J. Kempf ,  Saul H. Rosenberg ,  Jacob J. Plattner ,  Hing L. Shan ,  Biswanath De

    Inventor： Dale J. Kempf ,  Saul H. Rosenberg ,  Jacob J. Plattner ,  Hing L. Shan ,  Biswanath De

    IPC: A61K38/00 ,  C07D233/54 ,  C07D405/12 ,  C07D417/12 ,  C07K5/02 ,  C07K5/078

    CPC classification number: C07D233/64 ,  C07D405/12 ,  C07D417/12 ,  C07K5/0207 ,  C07K5/06139 ,  A61K38/00

    Abstract: A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; R.sub.1 is loweralkyl, loweralkenyl, alkoxyalkyl, [(alkoxy)alkoxy]alkyl, alkoxycarbonylalkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; R.sub.2 is hydrogen, loweralkyl, cycloalkylmethyl or benzyl; D is a substituent; or pharmaceutically acceptable salts or esters thereof.Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.

    Abstract translation: 下式的肾素抑制化合物：其中A是取代基; R1是低级烷基，低级烯基，烷氧基烷基，[（烷氧基）烷氧基]烷基，烷氧基羰基烷基，羧基烷基，（硫代烷氧基）烷基，苄基或杂环取代的甲基; R2是氢，低级烷基，环烷基甲基或苄基; D是取代基; 或其药学上可接受的盐或酯。 还公开了肾素抑制组合物，治疗高血压的方法，制备肾素抑制化合物的方法和可用于制备肾素抑制化合物的中间体。

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