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    Functionalized peptidyl aminodiols and -triols
    1.
    发明公开
    Functionalized peptidyl aminodiols and -triols 失效
    功能性磷酸二肽和 -

    公开(公告)号：EP0230266A3

    公开(公告)日：1990-01-17

    申请号：EP87100422.2

    申请日：1987-01-15

    申请人： ABBOTT LABORATORIES

    发明人： Rosenberg, Saul Howard ,  Plattner, Jacob John ,  Luly, Jay Richard

    IPC分类号： C07K5/06 ,  C07K5/02 ,  C07K5/08 ,  C07D233/64 ,  A61K31/415 ,  A61K37/02 ,  A61K37/64

    CPC分类号： C07D233/64 ,  A61K38/00 ,  C07K5/0227 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/0806

    摘要： The invention relates to renin inhibiting compounds of the formula
    wherein A is hydrogen; loweralkyl; arylalkyl; OR₈ or SR₈ wherein R₈ is hydrogen, loweralkyl or aminoalkyl; NR₉R₁₀ wherein R₉ and R₁₀ are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl;
    wherein B is NH, alkylamino, S, O, CH₂ or CHOH and R₁₁ is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxy­alkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected)­ alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R₁ is loweralkyl, cycloalkylmethyl, benzyl, α-methylbenzyl, α, α-di­methylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)­methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R₁ is phenoxy, thiophenoxy or anilino, B is CH₂ or CHOH or A is hydrogen; R₃ is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R₄ is lower­alkyl, cycloalkyl- methyl or benzyl; R₂, R₅ and R₆ are independently hydrogen or loweralkyl; X is O, NH or S; R₇ is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl.
    wherein R₁₂ and R₁₃ are independently hydrogen or loweralkyl, n is 0-2 and R₁₄ is substituted or unsubstituted penyl or heterocyclic; or XR₇ together are loweralkylsulfonyl, N₃ or Cl, and pharmaceutically acceptable salts thereof.

    Peptidylaminodiols
    2.
    发明公开
    Peptidylaminodiols 失效
    PEPTIDYLAMINODIOLS

    公开(公告)号：EP0229667A3

    公开(公告)日：1991-03-13

    申请号：EP87100424.8

    申请日：1987-01-15

    申请人： ABBOTT LABORATORIES

    发明人： Luly, Jay Richard ,  Kempf, Dale John ,  Plattner, Jacob John

    IPC分类号： C07K5/06 ,  C07K5/08 ,  C07K5/02 ,  C07D233/64 ,  C07C237/12 ,  A61K31/415 ,  A61K37/02 ,  A61K37/64 ,  A61K31/16

    CPC分类号： C07D233/64 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0227 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0821 ,  C07K5/0823 ,  Y02P20/55

    摘要： A renin inhibiting compound of the formula:
    wherein A is a substituent; W is C=O or CHOH; U is CH₂ or NR₂, provided that when W is CHOH then U is CH₂; R₁ is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, α, α -dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R₂ is hydrogen or loweralkyl; R₃ is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R₄ is loweralkyl, cycloalkylmethyl or benzyl; R₅ is vinyl, formyl, hydroxymethyl or hydrogen; R₇ is hydrogen or loweralkyl; R₈ and R₉ are independently selected from OH and NH₂; and R₆ is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R₅ and R₇ are both hydrogen and R₈ and R₉ are OH, the carbon bearing R₅ is of the "R" configuration and the carbon bearing R₆ 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.

    Functionalized peptidyl aminodiols and -triols
    6.
    发明公开
    Functionalized peptidyl aminodiols and -triols 失效
    磷脂酰胺和三聚氰胺。

    公开(公告)号：EP0230266A2

    公开(公告)日：1987-07-29

    申请号：EP87100422.2

    申请日：1987-01-15

    申请人： ABBOTT LABORATORIES

    发明人： Rosenberg, Saul Howard ,  Plattner, Jacob John ,  Luly, Jay Richard

    IPC分类号： C07K5/06 ,  C07K5/02 ,  C07K5/08 ,  C07D233/64 ,  A61K31/415 ,  A61K37/02 ,  A61K37/64

    CPC分类号： C07D233/64 ,  A61K38/00 ,  C07K5/0227 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/0806

    摘要： The invention relates to renin inhibiting compounds of the formula
    wherein A is hydrogen; loweralkyl; arylalkyl; OR₈ or SR₈ wherein R₈ is hydrogen, loweralkyl or aminoalkyl; NR₉R₁₀ wherein R₉ and R₁₀ are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl;
    wherein B is NH, alkylamino, S, O, CH₂ or CHOH and R₁₁ is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxy­alkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected)­ alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R₁ is loweralkyl, cycloalkylmethyl, benzyl, α-methylbenzyl, α, α-di­methylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)­methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R₁ is phenoxy, thiophenoxy or anilino, B is CH₂ or CHOH or A is hydrogen; R₃ is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R₄ is lower­alkyl, cycloalkyl- methyl or benzyl; R₂, R₅ and R₆ are independently hydrogen or loweralkyl; X is O, NH or S; R₇ is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl.
    wherein R₁₂ and R₁₃ are independently hydrogen or loweralkyl, n is 0-2 and R₁₄ is substituted or unsubstituted penyl or heterocyclic; or XR₇ together are loweralkylsulfonyl, N₃ or Cl, and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及式：CHEM的肾素抑制化合物，其中A是氢; 低级烷基; 芳; OR8或SR8，其中R8是氢，低级烷基或氨基烷基; NR 9 R 10，其中R 9和R 10独立地选自氢，低级烷基，氨基烷基，氰基烷基和羟烷基; 其中B是NH，烷基氨基，S，O，CH 2或CHOH，R 11是低级烷基，环烷基，芳基，芳基烷基，烷氧基，烯氧基，羟基烷氧基，二羟基烷氧基，芳基烷氧基，芳基烷氧基烷基，氨基，烷基氨基，二烷基氨基，（羟基烷基） 烷基）氨基，（二羟基烷基）（烷基）氨基，羧酸取代的烷基，烷氧基羰基烷基，氨基烷基，N-保护的氨基烷基，烷基氨基烷基，二烷基氨基烷基，（N-保护的）烷基）氨基烷基，（杂环）烷基或取代或未取代的杂环 ; R1是低级烷基，环烷基甲基，苄基，α-甲基苄基，α，α-二甲基苄基，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，苯乙基，苯氧基， 或anilino; 如果R1是苯氧基，硫代苯氧基或苯胺基，B是CH 2或CHOH或A是氢; R3是低级烷基，苄基或杂环环取代的甲基; R4是低级烷基，环烷基 - 甲基或苄基; R2，R5和R6独立地是氢或低级烷基; X是O，NH或S; R 7是氢，低级烷基，烷酰基，烷基磺酰基。 其中R 12和R 13独立地为氢或低级烷基，n为0-2，R 14为取代或未取代的吡啶基或杂环基; 或XR7一起是低级烷基磺酰基，N 3或Cl，及其药学上可接受的盐。

    Benzisoxazole carboxylic acids
    7.
    发明公开
    Benzisoxazole carboxylic acids 失效
    苯并恶唑羧酸

    公开(公告)号：EP0119294A1

    公开(公告)日：1984-09-26

    申请号：EP83106498.5

    申请日：1983-07-04

    申请人： ABBOTT LABORATORIES

    发明人： Plattner, Jacob John ,  Fung, Anthony K.

    IPC分类号： C07D498/04 ,  A61K31/42

    CPC分类号： C07D413/04 ,  C07C45/00 ,  C07C45/46 ,  C07C45/513 ,  C07C45/673 ,  C07C45/68 ,  C07C49/84 ,  C07D307/85 ,  C07C47/575 ,  C07C49/83 ,  C07C49/835

    摘要： Described are compounds of the formula
    wherein X is hydrogen, loweralkyl, halo, loweralkoxy or trifluoromethyl, and Z is hydrogen, loweralkyl, halo, hydroxy or alkoxy, or compounds of the formula
    wherein X' and Y' may be the same or different and are selected from hydrogen, loweralkyl, or halo, and Z' is hydrogen, loweralkyl, halo, hydroxy or loweralkoxy, or pharmaceutically acceptable salts thereof.
    The compounds possess diuretic activity.

    摘要翻译： 描述了下式化合物，其中X是氢，低级烷基，卤素，低级烷氧基或三氟甲基，Z是氢，低级烷基，卤素，羟基或烷氧基，或下式化合物其中X'和Y'可以相同或不同， 选自氢，低级烷基或卤素，Z'为氢，低级烷基，卤素，羟基或低级烷氧基，或其药学上可接受的盐。 这些化合物具有利尿活性。

    Peptidylaminodiols
    9.
    发明公开
    Peptidylaminodiols 失效

    公开(公告)号：EP0229667A2

    公开(公告)日：1987-07-22

    申请号：EP87100424.8

    申请日：1987-01-15

    申请人： ABBOTT LABORATORIES

    发明人： Luly, Jay Richard ,  Kempf, Dale John ,  Plattner, Jacob John

    IPC分类号： C07K5/06 ,  C07K5/08 ,  C07K5/02 ,  C07D233/64 ,  C07C237/12 ,  A61K31/415 ,  A61K37/02 ,  A61K37/64 ,  A61K31/16

    CPC分类号： C07D233/64 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0227 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0821 ,  C07K5/0823 ,  Y02P20/55

    摘要： A renin inhibiting compound of the formula:
    wherein A is a substituent; W is C=O or CHOH; U is CH₂ or NR₂, provided that when W is CHOH then U is CH₂; R₁ is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, α, α -dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R₂ is hydrogen or loweralkyl; R₃ is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R₄ is loweralkyl, cycloalkylmethyl or benzyl; R₅ is vinyl, formyl, hydroxymethyl or hydrogen; R₇ is hydrogen or loweralkyl; R₈ and R₉ are independently selected from OH and NH₂; and R₆ is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R₅ and R₇ are both hydrogen and R₈ and R₉ are OH, the carbon bearing R₅ is of the "R" configuration and the carbon bearing R₆ 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.

    摘要翻译： 一种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，则U是CH 2; （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（低级烷基） 或苯胺基; R 2是氢或低级烷基; R 3是低级烷基，[（烷氧基）烷氧基]烷基，（硫代烷氧基）烷基，低级链烯基，苄基或杂环取代的甲基; R 4是低级烷基，环烷基甲基或苄基; R 5是乙烯基，甲酰基，羟甲基或氢; R 7是氢或低级烷基; R 7和R 7独立地选自OH和NH 2; 和R 6是氢，低级烷基，乙烯基或芳基烷基; 条件是当R 5和R 7都是氢而R 7和R 7是OH时，带有R 5的碳是“R”构型，带有R 6的碳是“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和中间体用于制备肾素抑制化合物的方法。