公开(公告)号：JPS62234053A

公开(公告)日：1987-10-14

申请号：JP627987

申请日：1987-01-16

Applicant: ABBOTT LAB

Inventor： ROSENBERG SAUL HOWARD ,  LULY JAY RICHARD ,  PLATTNER JACOB JOHN

IPC: C07K14/81 ,  A61K31/16 ,  A61K31/165 ,  A61K31/18 ,  A61K31/215 ,  A61K31/22 ,  A61K31/255 ,  A61K31/27 ,  A61K31/33 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/655 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07C67/00 ,  C07C231/00 ,  C07C237/08 ,  C07C237/10 ,  C07C237/22 ,  C07C239/00 ,  C07C253/00 ,  C07C255/24 ,  C07C269/00 ,  C07C273/10 ,  C07C301/00 ,  C07C309/63 ,  C07C311/00 ,  C07C313/00 ,  C07C317/28 ,  C07C323/41 ,  C07C323/60 ,  C07D231/12 ,  C07D233/64 ,  C07D263/22 ,  C07D295/18 ,  C07D521/00 ,  C07K5/06 ,  C12N9/99

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：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.

公开(公告)号：AU583971B2

公开(公告)日：1989-05-11

申请号：AU6759887

申请日：1987-01-15

Applicant: ABBOTT LAB

Inventor： ROSENBERG SAUL HOWARD ,  LULY JAY RICHARD ,  PLATTNER JACOB JOHN

IPC: A61K38/00 ,  C07D233/54 ,  C07K20060101 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/083 ,  C07C103/46 ,  C07C121/68 ,  C07C101/08 ,  C07C101/04 ,  C07C125/065 ,  C07C91/15 ,  C07C125/073 ,  C07C143/72 ,  C07C149/273 ,  C07C143/78 ,  C07C101/19 ,  C07C101/18 ,  C07C101/30 ,  C07D233/64

Abstract: 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, alpha -methylbenzyl, alpha , alpha -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.

公开(公告)号：FR2459226A1

公开(公告)日：1981-01-09

申请号：FR8013218

申请日：1980-06-13

Applicant: ABBOTT LAB

Inventor： ALI AKHTAR ,  PLATTNER JACOB JOHN

IPC: C07K5/02 ,  C07K5/083 ,  C07C103/52 ,  G01N33/68

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：DK20887A

公开(公告)日：1988-07-17

申请号：DK20887

申请日：1987-01-15

Applicant: ABBOTT LAB

Inventor： ROSENBERG SAUL HOWARD ,  LULY JAY RICHARD ,  PLATTNER JACOB JOHN

IPC: A61K38/00 ,  C07D233/54 ,  C07K20060101 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/083 ,  C07C103/44 ,  C07K5/04

Abstract: 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, alpha -methylbenzyl, alpha , alpha -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.

公开(公告)号：AU570642B2

公开(公告)日：1988-03-24

申请号：AU1778883

申请日：1983-07-05

Applicant: ABBOTT LAB

Inventor： PLATTNER JACOB JOHN ,  FUNG ANTHONY KEI LUN

IPC: C07D498/00 ,  C07C45/00 ,  C07C45/46 ,  C07C45/51 ,  C07C45/67 ,  C07C45/68 ,  C07C49/84 ,  C07D307/85 ,  C07D413/04 ,  C07D498/04 ,  C07D413/10

Abstract: 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 min and Y min may be the same or different and are selected from hydrogen, loweralkyl, or halo, and Z min is hydrogen, loweralkyl, halo, hydroxy or loweralkoxy, or pharmaceutically acceptable salts thereof. The compounds possess diuretic activity.