公开(公告)号：EP0295294A4

公开(公告)日：1990-04-10

申请号：EP88900918

申请日：1987-12-22

Applicant: ABBOTT LAB ,  FUNG ANTHONY K L ,  KEMPF DALE JOHN ,  LULY JAY RICHARD ,  ROSENBERG SAUL HOWARD ,  PLATTNER JACOB JOHN

Inventor： FUNG ANTHONY K L ,  KEMPF DALE JOHN ,  LULY JAY RICHARD ,  ROSENBERG SAUL HOWARD ,  PLATTNER JACOB JOHN

IPC: C12N9/99 ,  A61K31/165 ,  A61K31/44 ,  A61K31/4406 ,  A61K38/00 ,  A61P9/12 ,  C07C67/00 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07C237/20 ,  C07C237/22 ,  C07C239/00 ,  C07C271/20 ,  C07C271/24 ,  C07C313/00 ,  C07C317/44 ,  C07C323/60 ,  C07C325/00 ,  C07C327/20 ,  C07C333/02 ,  C07D213/00 ,  C07D213/71 ,  C07D213/78 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097 ,  C07K14/81

CPC classification number: C07D233/64 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0227 ,  C07K5/06026 ,  C07K5/06078 ,  C07K5/0802 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0821 ,  C07K5/0823

公开(公告)号：AU1158088A

公开(公告)日：1988-07-27

申请号：AU1158088

申请日：1987-12-22

Applicant: ABBOTT LAB

Inventor： PLATTNER JACOB JOHN ,  ROSENBERG SAUL HOWARD ,  LULY JAY RICHARD ,  KEMPF DALE JOHN ,  FUNG ANTHONY K L

IPC: C12N9/99 ,  A61K31/165 ,  A61K31/44 ,  A61K31/4406 ,  A61K38/00 ,  A61P9/12 ,  C07C67/00 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07C237/20 ,  C07C237/22 ,  C07C239/00 ,  C07C271/20 ,  C07C271/24 ,  C07C313/00 ,  C07C317/44 ,  C07C323/60 ,  C07C325/00 ,  C07C327/20 ,  C07C333/02 ,  C07D213/00 ,  C07D213/71 ,  C07D213/78 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097 ,  C07K14/81 ,  C07K5/10 ,  A61K37/43

Abstract: 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, (alpha,alpha)-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R2 is hydrogen or loweralkyl; R3 is loweralkenyl, [(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.

公开(公告)号：AU6759987A

公开(公告)日：1987-07-23

申请号：AU6759987

申请日：1987-01-15

Applicant: ABBOTT LAB

Inventor： LULY JAY RICHARD ,  PLATTNER JACOB JOHN ,  KEMPF DALE JOHN

IPC: C07C215/10 ,  A61K31/16 ,  A61K31/165 ,  A61K31/18 ,  A61K31/215 ,  A61K31/22 ,  A61K31/255 ,  A61K31/33 ,  A61K31/535 ,  A61K31/5375 ,  A61K38/00 ,  A61P9/12 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C215/20 ,  C07C215/26 ,  C07C215/28 ,  C07C217/44 ,  C07C231/00 ,  C07C231/12 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C235/74 ,  C07C237/08 ,  C07C237/10 ,  C07C237/22 ,  C07C239/00 ,  C07C269/00 ,  C07C271/16 ,  C07C273/10 ,  C07C301/00 ,  C07C303/30 ,  C07C303/40 ,  C07C309/63 ,  C07C311/00 ,  C07C313/00 ,  C07C323/60 ,  C07D233/54 ,  C07D233/64 ,  C07D241/24 ,  C07D295/18 ,  C07D521/00 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/083 ,  C07K5/097 ,  C07K14/81 ,  C12N9/99 ,  C07K5/08 ,  C07C143/78 ,  C07C101/46 ,  C07C125/065

Abstract: 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, alpha , alpha -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.

公开(公告)号：DK20987D0

公开(公告)日：1987-01-15

申请号：DK20987

申请日：1987-01-15

Applicant: ABBOTT LAB

Inventor： LULY JAY RICHARD ,  PLATTNER JACOB JOHN ,  KEMPF DALE JOHN

IPC: C07C215/10 ,  A61K31/16 ,  A61K31/165 ,  A61K31/18 ,  A61K31/215 ,  A61K31/22 ,  A61K31/255 ,  A61K31/33 ,  A61K31/535 ,  A61K31/5375 ,  A61K38/00 ,  A61P9/12 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C215/20 ,  C07C215/26 ,  C07C215/28 ,  C07C217/44 ,  C07C231/00 ,  C07C231/12 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C235/74 ,  C07C237/08 ,  C07C237/10 ,  C07C237/22 ,  C07C239/00 ,  C07C269/00 ,  C07C271/16 ,  C07C273/10 ,  C07C301/00 ,  C07C303/30 ,  C07C303/40 ,  C07C309/63 ,  C07C311/00 ,  C07C313/00 ,  C07C323/60 ,  C07D233/54 ,  C07D233/64 ,  C07D241/24 ,  C07D295/18 ,  C07D521/00 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/083 ,  C07K5/097 ,  C07K14/81 ,  C12N9/99 ,  C07C103/44

Abstract: 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, alpha , alpha -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.

公开(公告)号：CA1340984C

公开(公告)日：2000-05-02

申请号：CA616530

申请日：1992-11-27

Applicant: ABBOTT LAB

Inventor： LULY JAY RICHARD ,  KEMPF DALE JOHN ,  PLATTNER JACOB JOHN

IPC: C07C215/10 ,  A61K31/16 ,  A61K31/165 ,  A61K31/18 ,  A61K31/215 ,  A61K31/22 ,  A61K31/255 ,  A61K31/33 ,  A61K31/535 ,  A61K31/5375 ,  A61K38/00 ,  A61P9/12 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C215/20 ,  C07C215/26 ,  C07C215/28 ,  C07C217/44 ,  C07C231/00 ,  C07C231/12 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C235/74 ,  C07C237/08 ,  C07C237/10 ,  C07C237/22 ,  C07C239/00 ,  C07C269/00 ,  C07C271/16 ,  C07C273/10 ,  C07C301/00 ,  C07C303/30 ,  C07C303/40 ,  C07C309/63 ,  C07C311/00 ,  C07C313/00 ,  C07C323/60 ,  C07D233/54 ,  C07D233/64 ,  C07D241/24 ,  C07D295/18 ,  C07D521/00 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/083 ,  C07K5/097 ,  C07K14/81 ,  C12N9/99

Abstract: 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, alpha , alpha -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.

公开(公告)号：CA1340940C

公开(公告)日：2000-04-04

申请号：CA527514

申请日：1987-01-16

Applicant: ABBOTT LAB

Inventor： PLATTNER JACOB JOHN ,  LULY JAY RICHARD ,  KEMPF DALE JOHN

IPC: C07C215/10 ,  A61K31/16 ,  A61K31/165 ,  A61K31/18 ,  A61K31/215 ,  A61K31/22 ,  A61K31/255 ,  A61K31/33 ,  A61K31/535 ,  A61K31/5375 ,  A61K38/00 ,  A61P9/12 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C215/20 ,  C07C215/26 ,  C07C215/28 ,  C07C217/44 ,  C07C231/00 ,  C07C231/12 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C235/74 ,  C07C237/08 ,  C07C237/10 ,  C07C237/22 ,  C07C239/00 ,  C07C269/00 ,  C07C271/16 ,  C07C273/10 ,  C07C301/00 ,  C07C303/30 ,  C07C303/40 ,  C07C309/63 ,  C07C311/00 ,  C07C313/00 ,  C07C323/60 ,  C07D233/54 ,  C07D233/64 ,  C07D241/24 ,  C07D295/18 ,  C07D521/00 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/083 ,  C07K5/097 ,  C07K14/81 ,  C12N9/99 ,  C07D295/20 ,  A61K38/05 ,  A61K38/06 ,  C07K5/08 ,  A61K31/395

Abstract: A renin inhibiting compound of the formula: (see formula I) ~ 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. .alpha.,.alpha.-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R2 is hydrogen or loweralkyl; R3 is loweralkyl, ¢(alkoxy)alkoxy!alkyl, (thioalkoxy)alkyl, loweralkenyl, 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.

公开(公告)号：ES2059313T3

公开(公告)日：1994-11-16

申请号：ES87100424

申请日：1987-01-15

Applicant: ABBOTT LAB

Inventor： LULY JAY RICHARD ,  KEMPF DALE JOHN ,  PLATTNER JACOB JOHN

IPC: C07C215/10 ,  A61K31/16 ,  A61K31/165 ,  A61K31/18 ,  A61K31/215 ,  A61K31/22 ,  A61K31/255 ,  A61K31/33 ,  A61K31/535 ,  A61K31/5375 ,  A61K38/00 ,  A61P9/12 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C215/20 ,  C07C215/26 ,  C07C215/28 ,  C07C217/44 ,  C07C231/00 ,  C07C231/12 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C235/74 ,  C07C237/08 ,  C07C237/10 ,  C07C237/22 ,  C07C239/00 ,  C07C269/00 ,  C07C271/16 ,  C07C273/10 ,  C07C301/00 ,  C07C303/30 ,  C07C303/40 ,  C07C309/63 ,  C07C311/00 ,  C07C313/00 ,  C07C323/60 ,  C07D233/54 ,  C07D233/64 ,  C07D241/24 ,  C07D295/18 ,  C07D521/00 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/083 ,  C07K5/097 ,  C07K14/81 ,  C12N9/99 ,  C07K5/08 ,  C07C237/12 ,  A61K31/415 ,  A61K37/02 ,  A61K37/64

Abstract: 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, alpha , alpha -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.

公开(公告)号：AU609774B2

公开(公告)日：1991-05-09

申请号：AU1158088

申请日：1987-12-22

Applicant: ABBOTT LAB

Inventor： PLATTNER JACOB JOHN ,  ROSENBERG SAUL HOWARD ,  LULY JAY RICHARD ,  KEMPF DALE JOHN ,  FUNG ANTHONY K L

IPC: C12N9/99 ,  A61K31/165 ,  A61K31/44 ,  A61K31/4406 ,  A61K38/00 ,  A61P9/12 ,  C07C67/00 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07C237/20 ,  C07C237/22 ,  C07C239/00 ,  C07C271/20 ,  C07C271/24 ,  C07C313/00 ,  C07C317/44 ,  C07C323/60 ,  C07C325/00 ,  C07C327/20 ,  C07C333/02 ,  C07D213/00 ,  C07D213/71 ,  C07D213/78 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097 ,  C07K14/81 ,  C07K5/10 ,  A61K37/43

Abstract: 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, (alpha,alpha)-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R2 is hydrogen or loweralkyl; R3 is loweralkenyl, [(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.

公开(公告)号：AU603080B2

公开(公告)日：1990-11-08

申请号：AU6759987

申请日：1987-01-15

Applicant: ABBOTT LAB

Inventor： LULY JAY RICHARD ,  PLATTNER JACOB JOHN ,  KEMPF DALE JOHN

IPC: C07C215/10 ,  A61K31/16 ,  A61K31/165 ,  A61K31/18 ,  A61K31/215 ,  A61K31/22 ,  A61K31/255 ,  A61K31/33 ,  A61K31/535 ,  A61K31/5375 ,  A61K38/00 ,  A61P9/12 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C215/20 ,  C07C215/26 ,  C07C215/28 ,  C07C217/44 ,  C07C231/00 ,  C07C231/12 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C235/74 ,  C07C237/08 ,  C07C237/10 ,  C07C237/22 ,  C07C239/00 ,  C07C269/00 ,  C07C271/16 ,  C07C273/10 ,  C07C301/00 ,  C07C303/30 ,  C07C303/40 ,  C07C309/63 ,  C07C311/00 ,  C07C313/00 ,  C07C323/60 ,  C07D233/54 ,  C07D233/64 ,  C07D241/24 ,  C07D295/18 ,  C07D521/00 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/083 ,  C07K5/097 ,  C07K14/81 ,  C12N9/99 ,  C07K5/08 ,  C07C143/78 ,  C07C101/46 ,  C07C125/065

Abstract: 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, alpha , alpha -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.

公开(公告)号：NZ223096A

公开(公告)日：1990-09-26

申请号：NZ22309688

申请日：1988-01-06

Applicant: ABBOTT LAB

Inventor： FUNG ANTHONY K L ,  KEMPF DALE JOHN ,  LULY JAY RICHARD ,  ROSENBERG SAUL HOWARD ,  PLATTNER JACOB JOHN

IPC: C12N9/99 ,  A61K31/165 ,  A61K31/44 ,  A61K31/4406 ,  A61K38/00 ,  A61P9/12 ,  C07C67/00 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07C237/20 ,  C07C237/22 ,  C07C239/00 ,  C07C271/20 ,  C07C271/24 ,  C07C313/00 ,  C07C317/44 ,  C07C323/60 ,  C07C325/00 ,  C07C327/20 ,  C07C333/02 ,  C07D213/00 ,  C07D213/71 ,  C07D213/78 ,  C07D233/54 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097 ,  C07K14/81 ,  A61K37/02 ,  A61K37/43

Abstract: 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, (alpha,alpha)-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R2 is hydrogen or loweralkyl; R3 is loweralkenyl, [(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.