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    Peptidylaminodiols
    2.
    发明授权
    Peptidylaminodiols 失效
    肽基氨基二醇

    公开(公告)号：US5214129A

    公开(公告)日：1993-05-25

    申请号：US793773

    申请日：1991-11-18

    申请人： Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    发明人： Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    IPC分类号： A61K38/00 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097

    CPC分类号： C07D233/64 ,  C07K5/0202 ,  C07K5/0227 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/0802 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0821 ,  C07K5/0823 ,  A61K38/00

    摘要： 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.sub.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, loweralkenyl, 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.

    摘要翻译： 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; （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anilino; 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，低级烯基，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。

    Peptidylaminodiols
    3.
    发明授权
    Peptidylaminodiols 失效
    肽基氨基二醇

    公开(公告)号：US4845079A

    公开(公告)日：1989-07-04

    申请号：US217106

    申请日：1988-07-11

    申请人： Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    发明人： Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    IPC分类号： A61K38/00 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097

    CPC分类号： C07D233/64 ,  C07K5/0227 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/0802 ,  C07K5/0808 ,  C07K5/0823 ,  A61K38/00 ,  Y10S530/86

    摘要： 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.sub.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-napththyl)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, loweralkenyl, 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.

    摘要翻译： 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-萘乙基）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， 或anilino; 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，低级烯基，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。

    Angiotensinogen analogs
    4.
    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。

    Renin inhibiting compounds
    6.
    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。

    Peptidylaminodiols
    8.
    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

    申请人： Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

    发明人： Jay R. Luly ,  Jacob J. Plattner ,  Dale J. Kempf

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

    CPC分类号： C07K5/0227 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06139 ,  A61K38/00

    摘要： 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.

    摘要翻译： 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。

    Functionalized peptidyl aminodiols and -triols 4-amino-5-cyclohexyl-3-hydroxy-1,2-oxopentane and derivatives thereof
    10.
    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。