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    Enzyme inhibiting peptide derivatives
    2.
    发明授权
    Enzyme inhibiting peptide derivatives 失效
    酶抑制肽衍生物

    公开(公告)号：US5126326A

    公开(公告)日：1992-06-30

    申请号：US361895

    申请日：1989-06-06

    申请人： Paul C. Anderson ,  Yvan Guindon ,  Christiane Yoakim

    发明人： Paul C. Anderson ,  Yvan Guindon ,  Christiane Yoakim

    IPC分类号： C12N9/99 ,  A61K38/55 ,  A61P9/00 ,  A61P9/12 ,  A61P43/00 ,  C07K1/06 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81

    CPC分类号： C07K5/0227

    摘要： Disclosed herein are peptide derivatives which inhibit the activities of human immunodeficiency virus (HIV) protease and renin. The peptide derivatives can be represented by general formula R.sup.1 --R.sup.2 --Y--R.sup.3 --R.sup.4 wherein R.sup.1 is a derived amino acid based on an O.sup.4 -(carboxymethyl)-tyrosyl residue, R.sup.2 and are amino acid or analogous amino acid residues (R.sup.3 may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R.sup.4 is [--NR.sup.17 CHR.sup.18 --C(O)].sub.p --Z wherein R.sup.17 is hydrogen or lower alkyl, R.sup.18 is an amino acid or analogous amino acid side chain, p is zero or one and Z is a terminal group (e.g. hydroxy or amino), or R.sup.4 is --NR.sup.17 CR.sup.18 (R.sup.21)CH.sub.2 OH wherein R.sup.17 and R.sup.18 are as noted hereinabove and R.sup.21 is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives are useful as agents for combatting HIV infections and for treating renin-associated hypertension and congestive heart failure.

    摘要翻译： 本文公开了抑制人免疫缺陷病毒（HIV）蛋白酶和肾素的活性的肽衍生物。 肽衍生物可以由通式R 1 -R 2 -Y-R 3 -R 4表示，其中R 1是基于O 4 - （羧甲基） - 酪氨酰残基R2的衍生氨基酸，并且是氨基酸或类似氨基酸残基（R3可以 任选地不存在），Y是非肽连接单元，例如 辛基，R4是[-NR17CHR18-C（O）] pZ，其中R17是氢或低级烷基，R18是氨基酸或类似的氨基酸侧链，p是0或1，Z是末端基团（例如羟基或 氨基），或R 4是-NR 17 CR 18（R 21）CH 2 OH，其中R 17和R 18如上所述，R 21是氢，低级烷基或羟基（低级）烷基。 该衍生物可用作抗艾滋病毒感染和治疗肾素相关性高血压和充血性心力衰竭的药剂。

    Enzyme inhibitors
    3.
    发明授权
    Enzyme inhibitors 失效
    酶抑制剂

    公开(公告)号：US5212157A

    公开(公告)日：1993-05-18

    申请号：US362171

    申请日：1989-06-06

    申请人： Paul C. Anderson ,  Yvan Guindon ,  Christiane Yoakim

    发明人： Paul C. Anderson ,  Yvan Guindon ,  Christiane Yoakim

    IPC分类号： C12N9/99 ,  A61K38/00 ,  A61K38/55 ,  A61P9/00 ,  A61P9/12 ,  A61P31/12 ,  A61P31/18 ,  A61P43/00 ,  C07D217/26 ,  C07K1/06 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  C07K14/81

    CPC分类号： C07K5/0205 ,  C07D217/26 ,  C07K5/0207 ,  A61K38/00

    摘要： Disclosed herein are peptide derivatives which inhibit the activity of human immunodeficiency virus (HIV) protease. The peptide derivatives can be represented by general formula R.sup.1 --R.sup.2 --Y--R.sup.3 --R.sup.4 wherein R.sup.1 is an optionally substituted 3-(1,2,3,4-tetrahydroisoquinolyl)carbonyl residue, R.sup.2 and R.sup.3 are amino acid or analogous amino acid residues (R.sup.3 may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R.sup.4 is [--NR.sup.17 CH(R.sup.18)C(O)].sub.p --Z wherein R.sup.17 is hydrogen or lower alkyl, R.sup.18 is an amino acid or analogous amino acid side chain, p is zero or 1 and Z is a terminal group (e.g. hydroxy or amino), or R.sup.4 is --NR.sup.17 CR.sup.18 (R.sup.21)CH.sub.2 --OH wherein R.sup.17 and R.sup.18 are as noted hereinabove and R.sup.21 is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives also inhibit renin activity. Accordingly, the derivatives can be used for combating HIV infections or for treating hypertension or congestive heart failure.

    Renin inhibiting polyhydroxy-monoamides
    10.
    发明授权
    Renin inhibiting polyhydroxy-monoamides 失效
    肾素抑制多羟基 - 单酰胺

    公开(公告)号：US5354767A

    公开(公告)日：1994-10-11

    申请号：US990779

    申请日：1992-12-10

    申请人： Paul C. Anderson ,  Gary W. Bantle ,  Grace L. Jung ,  Pierre Lavallee ,  Bruno Simoneau

    发明人： Paul C. Anderson ,  Gary W. Bantle ,  Grace L. Jung ,  Pierre Lavallee ,  Bruno Simoneau

    IPC分类号： C07C235/08 ,  C07C235/26 ,  C07C235/34 ,  C07D233/54 ,  C07D233/88 ,  C07D277/36 ,  C07D307/58 ,  A61K31/16

    CPC分类号： C07D233/64 ,  C07C235/08 ,  C07C235/26 ,  C07C235/34 ,  C07D233/88 ,  C07D277/36 ,  C07D307/58 ,  C07C2101/02 ,  C07C2101/08 ,  C07C2101/14

    摘要： Disclosed herein are compounds of the formula:R.sup.1 CH.sub.2 CH(X)CH(Y)CH(Z)CHR.sup.2 C(O)NHCHR.sup.3 CH(OH)CH(OH)R.sup.4wherein R.sup.1 is a terminal unit, for example lower cycloalkyl or phenyl; R.sup.2 is, for example, an optionally substituted alkyl, cycloalkylmethyl, benzyl, 4-imidazolylmethyl, 2-thienylmethyl or 4-thiazolylmethyl; R.sup.3 is alkyl, cycloalkylmethyl or an optionally substituted benzyl; R.sup.4 is alkyl or cycloalkyl; and X and Y each is hydroxy and Z is hydrogen, or X and Z each is hydroxy and Y is hydrogen; with the provisos that (a) the carbon atom bearing R.sup.2 has the "R" configuration except when R.sup.2 is 2-thienylmethyl or 2-thiazolylmethyl, X and Y each is hydroxy and Z is hydrogen, then the carbon atom bearing R.sup.2 has the "S" configuration; (b) the carbon atoms bearing R.sup.3 and R.sup.4 each has the "S" configuration; and (c) the carbon atom located between the last-said two carbon atoms has the "R" configuration. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.

    摘要翻译： 本文公开的是下式的化合物：R1CH2CH（X）CH（Y）CH（Z）CHR2C（O）NHCHR3CH（OH）CH（OH）R4其中R1是末端单元，例如低级环烷基或苯基; R2是例如任选取代的烷基，环烷基甲基，苄基，4-咪唑基甲基，2-噻吩基甲基或4-噻唑基甲基; R3是烷基，环烷基甲基或任选取代的苄基; R4是烷基或环烷基; X和Y各自为羟基，Z为氢，或X和Z各自为羟基，Y为氢; 条件是（a）带有R2的碳原子具有“R”构型，除非R2是2-噻吩基甲基或2-噻唑基甲基，X和Y各自为羟基，Z为氢，则带有R2的碳原子具有“ S“配置; （b）含有R 3和R 4的碳原子各自具有“S”构型; 和（c）位于最后所述两个碳原子之间的碳原子具有“R”构型。 该化合物抑制肾素活性，并被指示用于治疗高血压和充血性心力衰竭。