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    Renin inhibiting compounds
    1.
    发明授权
    Renin inhibiting compounds 失效
    肾素抑制化合物

    公开(公告)号：US4826815A

    公开(公告)日：1989-05-02

    申请号：US946881

    申请日：1987-01-09

    申请人： Jay R. Luly ,  Joseph Dellaria ,  Anthony K. L. Fung ,  Dale J. Kempf ,  Jacob J. Plattner ,  Saul H. Rosenberg ,  Hing L. Sham

    发明人： Jay R. Luly ,  Joseph Dellaria ,  Anthony K. L. Fung ,  Dale J. Kempf ,  Jacob J. Plattner ,  Saul H. Rosenberg ,  Hing L. Sham

    IPC分类号： A61K38/00 ,  C07D207/12 ,  C07D231/12 ,  C07D233/54 ,  C07D263/20 ,  C07D295/185 ,  C07D317/28 ,  C07D319/06 ,  C07D339/06 ,  C07D339/08 ,  C07D405/06 ,  C07D409/06 ,  C07K5/02 ,  C07K5/065 ,  A61K37/02 ,  C07K5/08

    CPC分类号： C07D231/12 ,  C07D207/12 ,  C07D233/64 ,  C07D263/20 ,  C07D295/185 ,  C07D317/28 ,  C07D319/06 ,  C07D339/06 ,  C07D339/08 ,  C07D405/06 ,  C07D409/06 ,  C07K5/02 ,  C07K5/0227 ,  C07K5/06078 ,  A61K38/00 ,  Y02P20/55 ,  Y10S530/80 ,  Y10S530/86

    摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; Or.sub.10 wherein R.sub.10 is hydrogen or loweralkyl; NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen and loweralkyl; or R.sub.13 --CO--B wherein B is NH, O, CH.sub.2, HNCH.sub.2 and R.sub.13 is loweralkyl, alkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, aminoalkyl, N-protected aminoalkyl, hydroxylated dialkylamino, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic, carboxyalkyl, or lower alkyl carboxyalkyl esters; W is N or CH: U,V may be the following combinations H,OH; OH,H; H,H; or when taken together as O represents a carbonyl with the provisos that if U,V.dbd.H,OH, then W=CH, and if U,V.dbd.O then W.dbd.N; R.sub.1 , R.sub.3 and R.sub.5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R.sub.2, R.sub.4, R.sub.7, R.sub.8 and R.sub.9 are hydrogen or loweralkyl and may be the same or different; X is NH, O, S, SO, SO.sub.2, or CH.sub.2 ; and R.sub.6 is loweralkyl cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group, with the proviso that R.sub.6 may be an N-protecting group when X is NH.

    摘要翻译： 本发明涉及下式的肾素抑制化合物：其中A是氢; 低级烷基 芳烷基 其中R 10是氢或低级烷基; NR11R12其中R11和R12独立地选自氢和低级烷基; 或R13-CO-B，其中B是NH，O，CH2，HNCH2和R13是低级烷基，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，氨基烷基，N-保护的氨基烷基，羟基化二烷基氨基，（杂环）烷基或取代 或未取代的杂环，羧基烷基或低级烷基羧烷基酯; W是N或CH：U，V可以是以下组合：H，OH; OH，H; H，H; 或者当O代表羰基时，条件是如果U，V = H，OH，则W = CH，并且如果U，V = O，则W = N; R 1，R 3和R 5是低级烷基或亲水性，亲油性或芳族氨基酸侧链，可以相同或不同; R2，R4，R7，R8和R9是氢或低级烷基，可以相同或不同; X是NH，O，S，SO，SO 2或CH 2; 并且R 6是低级烷基环烷基，环烷基烷基，芳基，芳烷基或N-保护基，条件是当X是NH时，R6可以是N-保护基。

    Angiotensinogen analogs
    2.
    发明授权
    Angiotensinogen analogs 失效

    公开(公告)号：US4857507A

    公开(公告)日：1989-08-15

    申请号：US946883

    申请日：1987-01-09

    申请人： Saul H. Rosenberg ,  Joseph Dellaria ,  Anthony K, L. Fung ,  Dale J. Kempf ,  Jay R. Luly ,  Jacob J. Plattner

    发明人： Saul H. Rosenberg ,  Joseph Dellaria ,  Anthony K, L. Fung ,  Dale J. Kempf ,  Jay R. Luly ,  Jacob J. Plattner

    IPC分类号： A61K38/00 ,  C07D207/12 ,  C07D231/12 ,  C07D233/54 ,  C07D263/20 ,  C07D295/185 ,  C07D317/28 ,  C07D319/06 ,  C07D339/06 ,  C07D339/08 ,  C07D405/06 ,  C07D409/06 ,  C07K5/02 ,  C07K5/065

    CPC分类号： C07D231/12 ,  C07D207/12 ,  C07D233/64 ,  C07D263/20 ,  C07D295/185 ,  C07D317/28 ,  C07D319/06 ,  C07D339/06 ,  C07D339/08 ,  C07D405/06 ,  C07D409/06 ,  C07K5/02 ,  C07K5/0227 ,  C07K5/06078 ,  A61K38/00 ,  Y02P20/55 ,  Y10S530/86

    摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; OR.sub.10 or SR.sub.10 wherein R.sub.10 is hydrogen, loweralkyl or aminoalkyl; NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.13 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, aminoalkyl, alkoxycarbonylalkyl, carboxyalkyl, N-protected aminoalkyl, alkylaminoalkyl, (N-protected)(alkyl)aminoalkyl, dialkylaminoalkyl, (heterocyclic) alkyl or a substituted or unsubstituted heterocyclic; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloaklylmethyl, benzyl, .alpha.,.alpha.-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)-methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R.sub.1 is phenoxy, thiophenoxy or anilino, B is CH.sub.2 or CHOH or A is hydrogen, R.sub.3 is loweralkyl, vinylloweralkyl, benzyl or heterocyclic ring substituted methyl, R.sub.5 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.2 and R.sub.4 are independently selected from hydrogen and loweralkyl; R.sub.6 is CHOH or CO; R.sub.7 is CH.sub.2, CF.sub.2 or CF with the proviso that when R.sub.6 is CO, R.sub.7 is CF.sub.2 ; R.sub.8 is CH.sub.2, CHR.sub.14 wherein R.sub.14 is lower-alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or R.sub.7 and R.sub.8 taken together can be ##STR3## with the proviso that when R.sub.7 is CF.sub.2, R.sub.8 is CH.sub.2 ; E is O, S, SO, SO.sub.2, NR.sub.15 wherein R.sub.15 is hydrogen or loweralkyl or NR.sub.16 CO wherein R.sub.16 is hydrogen or loweralkyl; R.sub.9 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protected group, or E and R.sub.9 taken together can be N.sub.3, with the proviso that when E is NH, R.sub.9 is an N-protecting group; and pharmaceutically acceptable salts thereof.

    Functionalized peptidyl aminodiols and -triols
    5.
    发明授权
    Functionalized peptidyl aminodiols and -triols 失效
    官能化肽基氨基二醇和三醇

    公开(公告)号：US4837204A

    公开(公告)日：1989-06-06

    申请号：US191714

    申请日：1988-05-09

    申请人： Saul H. Rosenberg ,  Jay R. Luly ,  Jacob J. Plattner

    发明人： Saul H. Rosenberg ,  Jay R. Luly ,  Jacob J. Plattner

    IPC分类号： A61K38/00 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/083

    CPC分类号： C07D233/64 ,  C07K5/0227 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/0806 ,  A61K38/00 ,  Y10S530/86

    摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; aryalkyl; OR.sub.8 or SR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or aminoalkyl; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.11 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; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, .alpha.-methylbenzyl, .alpha.,.alpha.-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)-methyl, (2-naphthyl)methyl, (4-imidazolyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R.sub.1 is henoxy, thiophenoxy or anilino, B is CH.sub.2 or CHOH or A is hydrogen; R.sub.3 is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R.sub.4 is loweralkyl, cycloalkyl- methyl or benzyl; R.sub.2, R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl; X is O, NH or S; R.sub.7 is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl ##STR3## wherein R.sub.12 and R.sub.13 are independently hydrogen or loweralkyl, n is 0-2 and R.sub.14 is substituted or unsubstituted phenyl or heterocyclic; or XR.sub.7 together are loweralkylsulfonyl, N.sub.3 or Cl, and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及下式的肾素抑制化合物：其中A是氢; 低级烷基 烷基 OR 8或SR 8，其中R 8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， 噻吩氧基或苯胺基; 如果R1是苯氧基，苯氧基或苯胺基，B是CH2或CHOH或A是氢; R3是低级烷基，苄基或杂环取代的甲基; R4是低级烷基，环烷基 - 甲基或苄基; R2，R5和R6独立地是氢或低级烷基; X是O，NH或S; R 7为氢，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为取代或未取代的苯基或杂环基; 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。

    Functionalized peptidyl aminodiols and -triols 4-amino-5-cyclohexyl-3-hydroxy-1,2-oxopentane and derivatives thereof
    6.
    发明授权
    Functionalized peptidyl aminodiols and -triols 4-amino-5-cyclohexyl-3-hydroxy-1,2-oxopentane and derivatives thereof 失效
    官能化肽基氨基二醇和三醇4-氨基-5-环己基-3-羟基-1,2-氧代戊烷及其衍生物

    公开(公告)号：US4977277A

    公开(公告)日：1990-12-11

    申请号：US361522

    申请日：1989-06-05

    申请人： Saul H. Rosenberg ,  Jay R. Luly ,  Jacob J. Plattner

    发明人： Saul H. Rosenberg ,  Jay R. Luly ,  Jacob J. Plattner

    IPC分类号： A61K38/00 ,  C07C271/16 ,  C07C271/20 ,  C07D231/38 ,  C07D295/215 ,  C07D303/36 ,  C07F7/18 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065

    CPC分类号： C07D231/38 ,  C07C271/16 ,  C07C271/20 ,  C07D295/215 ,  C07D303/36 ,  C07F7/1856 ,  C07K5/0227 ,  C07K5/06043 ,  C07K5/06078 ,  A61K38/00 ,  C07C2101/14 ,  Y10S530/86

    摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; OR.sub.8 or SR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or aminoalkyl; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.11 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; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, .alpha.-methylbenzyl, .alpha., .alpha.-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)-methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R.sub.1 is phenoxy, thiophenoxy or anilino, B is CH.sub.2 or CHOH or A is hydrogen; R.sub.3 is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R.sub.4 is lower-alkyl, cycloalkyl- methyl or benzyl; R.sub.2, R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl; X is O, NH or S; R.sub.7 is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl ##STR3## wherein R.sub.12 and R.sub.13 are independently hydrogen or loweralkyl, n is 0-2 and R.sub.14 is substituted or unsubstituted phenyl or heterocyclic; or XR.sub.7 together are loweralkylsulfonyl, N.sub.3 or Cl, and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及下式的肾素抑制化合物：其中A是氢; 低级烷基 芳烷基 OR 8或SR 8，其中R 8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， 噻吩氧基或苯胺基; 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为氢，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为取代或未取代的苯基或杂环基; 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。

    Heterocyclic renin inhibitors
    7.
    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

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

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

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

    CPC分类号： C07D233/64 ,  C07D405/12 ,  C07D417/12 ,  C07K5/0207 ,  C07K5/06139 ,  A61K38/00

    摘要： 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.

    摘要翻译： 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。