Chromonyl/chromonylalkyl-N-terminal amino hydroxy
    4.
    发明授权
    Chromonyl/chromonylalkyl-N-terminal amino hydroxy 失效
    色酮基/染色体烷基-N-末端氨基羟基

    公开(公告)号:US5210095A

    公开(公告)日:1993-05-11

    申请号:US736866

    申请日:1991-07-29

    摘要: Non-peptidyl compounds characterized generally as chromonyl/chromonylalkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein Q is oxygen atom; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; and wherein R.sub.7 is isobutyl or ethyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译: 通常作为染色体/染色体烷基-N-末端氨基羟基β-氨基酸衍生物表征的非肽基化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物具有式“IMAGE”,其中R 1选自,其中Y和Z各自独立地选自氢,氯,氟,甲氧基和二甲基氨基; 其中Q是氧原子; 其中n是选自0至4的数字,包括端值; 其中R2和R4各自独立地选自氢和甲基; 其中R3是甲基或乙基; 其中R5是环己基甲基; 其中R6是羟基; 并且其中R 7是异丁基或乙基; 或其药学可接受的盐。

    Quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal amino
hydroxy .beta.-amino acid derivatives
    6.
    发明授权
    Quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives 失效
    喹啉基/喹啉基烷基-N-端环烷氧基-C末端氨基羟基β-氨基酸衍生物

    公开(公告)号:US5223514A

    公开(公告)日:1993-06-29

    申请号:US889865

    申请日:1992-05-28

    摘要: Non-peptidyl compounds characterized generally as quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.7 are taken together to form a partially saturated or fully saturated heterocyclic ring containing five to eight ring members with one or two ring members being oxygen atoms and the remaining ring members being carbon atoms, and which heterocyclic ring may be optionally substituted with lower alkyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译: 通常以喹啉基/喹啉基烷基-N-端环烷氧基-C末端氨基羟基β-氨基酸衍生物为特征的非肽基化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物具有式“IMAGE”,其中R 1选自,其中Y和Z各自独立地选自氢,氯,氟,甲氧基和二甲基氨基; 其中n是选自0至4的数字,包括端值; 其中R2和R4各自独立地选自氢和甲基; 其中R3是甲基或乙基; 其中R5是环己基甲基; 其中R6和R7一起形成含有5-8个环成员的部分饱和或完全饱和的杂环,其中一个或两个环成员是氧原子,其余的环成员是碳原子,并且该杂环可以任选地被 低级烷基 或其药学上可接受的盐。

    Cycloalkyl/cycloalkylalkyl-N-terminal cycloalkoxy-C-terminal amino
hydroxy .beta.-amino acid derivatives
    7.
    发明授权
    Cycloalkyl/cycloalkylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives 失效
    环烷基/环烷基烷基-N-端环烷氧基-C末端氨基羟基β-氨基酸衍生物

    公开(公告)号:US5217991A

    公开(公告)日:1993-06-08

    申请号:US889738

    申请日:1992-05-28

    摘要: Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from cycloalkyl and cycloalkylalkyl groups, wherein said cycloalkyl group contains three to about eight carbon atoms and the acyclic alkyl portion of said cycloalkylalkyl group contains one to about eight carbon atoms; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl: wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.7 are taken together to form a partially saturated or fully saturated heterocyclic ring containing five to eight ring members with one or two ring members being oxygen atoms and the remaining ring members being carbon atoms, and which heterocyclic ring may be optionally substituted with lower alkyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译: 通常以环烷基/环烷基烷基-N-端环烷氧基-C末端氨基羟基β-氨基酸衍生物表征的非肽基化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物具有下式:其中R 1选自环烷基和环烷基烷基,其中所述环烷基含有3至约8个碳原子,所述环烷基烷基的无环烷基部分含有1至约8个碳原子; 其中R2和R4各自独立地选自氢和甲基; 其中R 3是甲基或乙基:其中R 5是环己基甲基; 其中R6和R7一起形成含有5-8个环成员的部分饱和或完全饱和的杂环,其中一个或两个环成员是氧原子,其余的环成员是碳原子,并且该杂环可以任选地被 低级烷基 或其药学上可接受的盐。

    Aralkyl-N-terminal amino hydroxy
    8.
    发明授权
    Aralkyl-N-terminal amino hydroxy 失效
    芳烷基-N-末端氨基羟基

    公开(公告)号:US5180744A

    公开(公告)日:1993-01-19

    申请号:US736869

    申请日:1991-07-29

    摘要: Non-peptidyl compounds characterized generally as aralkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; wherein R.sub.7 is isobutyl or ethyl; and wherein each of R.sub.8 and R.sub.9 is hydrido; or a pharmaceutically-acceptable salt thereof. g

    摘要翻译: 通常为芳烷基-N-端氨基羟基β-氨基酸衍生物的非肽基化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物具有式“IMAGE”,其中R 1选自,其中Y和Z各自独立地选自氢,氯,氟,甲氧基和二甲基氨基; 其中n是选自0至4的数字,包括端值; 其中R2和R4各自独立地选自氢和甲基; 其中R3是甲基或乙基; 其中R5是环己基甲基; 其中R6是羟基; 其中R 7是异丁基或乙基; 并且其中R8和R9各自是氢的; 或其药学上可接受的盐。

    Chromonyl/chromonylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy
.beta.-amino derivatives
    10.
    发明授权
    Chromonyl/chromonylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino derivatives 失效
    色酮基/色酮基烷基-N-端环烷氧基-C末端氨基羟基β-氨基衍生物

    公开(公告)号:US5223532A

    公开(公告)日:1993-06-29

    申请号:US889872

    申请日:1992-05-28

    摘要: Non-peptidyl compounds characterized generally as chromonyl/chromonylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.7 are taken together to form a partially saturated or fully saturated heterocyclic ring containing five to eight ring members with one or two ring members being oxygen atoms and the remaining ring members being carbon atoms, and which heterocyclic ring may be optionally substituted with lower alkyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译: 特别是作为染色体/染色体烷基-N-端环烷氧基-C末端氨基羟基β-氨基酸衍生物的非肽基化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物具有式“IMAGE”,其中R 1选自,其中Y和Z各自独立地选自氢,氯,氟,甲氧基和二甲基氨基; 其中n是选自0至4的数字,包括端值; 其中R2和R4各自独立地选自氢和甲基; 其中R3是甲基或乙基; 其中R5是环己基甲基; 其中R6和R7一起形成含有5-8个环成员的部分饱和或完全饱和的杂环,其中一个或两个环成员是氧原子,其余的环成员是碳原子,并且该杂环可以任选地被 低级烷基 或其药学可接受的盐。