公开(公告)号：BRPI0719563A2

公开(公告)日：2013-12-10

申请号：BRPI0719563

申请日：2007-12-04

Applicant: ABBOTT LAB

Inventor： ANDERSON MARK GERALD ,  KROEGER PAUL E ,  ROSENBERG SAUL HOWARD ,  TAHIR STEPHEN KENNETH ,  TSE CHRISTIN ,  WASS JOHN A

IPC: C12Q1/68

Abstract: Methods for identifying cancer patients eligible to receive Bcl-2 family inhibitor therapy and for monitoring patient response to Bcl-2 family inhibitor therapy comprise assessment of the expression levels of the biomarker combinations set out in TABLES 1, 2, 3, 4, 5 or 6 in a patient tissue sample. The methods of the invention allow more effective identification of patients to receive Bcl-2 family inhibitor therapy and of determination of patient response to the therapy.

公开(公告)号：AU613956B2

公开(公告)日：1991-08-15

申请号：AU2222388

申请日：1988-09-14

Applicant: ABBOTT LAB

Inventor： BAKER WILLIAM R ,  KEMPF DALE J ,  SHAM HING LEUNG ,  DELLARIA JOSEPH F ,  ROSENBERG SAUL HOWARD

IPC: C07C271/10 ,  A61K31/395 ,  A61K31/415 ,  A61K31/42 ,  A61K31/421 ,  A61K31/535 ,  A61K31/536 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/54 ,  A61K38/00 ,  A61P9/12 ,  C07C67/00 ,  C07C69/24 ,  C07C213/00 ,  C07C215/10 ,  C07C215/20 ,  C07C215/28 ,  C07C217/08 ,  C07C217/28 ,  C07C229/22 ,  C07C229/26 ,  C07C229/30 ,  C07C229/32 ,  C07C229/34 ,  C07C229/36 ,  C07C231/00 ,  C07C231/02 ,  C07C233/11 ,  C07C233/22 ,  C07C233/40 ,  C07C233/47 ,  C07C233/51 ,  C07C235/20 ,  C07C237/12 ,  C07C237/20 ,  C07C239/20 ,  C07C255/46 ,  C07C265/02 ,  C07C265/04 ,  C07C271/16 ,  C07C271/20 ,  C07C271/22 ,  C07C275/24 ,  C07C317/28 ,  C07C317/44 ,  C07C317/48 ,  C07C323/24 ,  C07C323/41 ,  C07C323/56 ,  C07C323/59 ,  C07C323/60 ,  C07D207/12 ,  C07D211/76 ,  C07D213/40 ,  C07D233/32 ,  C07D233/61 ,  C07D263/04 ,  C07D263/06 ,  C07D263/16 ,  C07D263/22 ,  C07D263/24 ,  C07D263/28 ,  C07D265/10 ,  C07D273/04 ,  C07D277/24 ,  C07D285/10 ,  C07D295/12 ,  C07D295/13 ,  C07D295/185 ,  C07D295/205 ,  C07D295/215 ,  C07D295/22 ,  C07D309/14 ,  C07D319/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D521/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/08 ,  C07D263/08 ,  C07D317/38 ,  C07D233/34 ,  C07D239/10 ,  A61K37/64

Abstract: A renin inhibiting compound of the formula: wherein A is a substituent; W is C=O, CHOH or NR2 wherein R2 is hydrogen or loweralkyl; U is C=O, CH2 or NR2 wherein R2 is hydrogen or loweralkyl, with the proviso that when W is CHOH then U is CH2 and with the proviso that U is C=O or CH2 when W is NR2; V is CH, C(OH) or C(halogen) with the proviso that V is CH when U is NR2; R1 is loweralkyl, cycloalkylalkyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, 4-hydroxybenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (unsubstituted heterocyclic)methyl, (substituted heterocyclic)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino, provided that B is CH2 or CHOH or A is hydrogen when R1 is phenoxy, thiophenoxy or anilino; R3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, azidoalkyl, aminoalkyl, (alkyl)aminoalkyl, dialkylaminoalkyl, (alkoxy)(alkyl)aminoalkyl, (alkoxy)aminoalkyl, benzyl or heterocyclic ring substituted methyl; R4 is loweralkyl, cycloalkylmethyl or benzyl; R5 is OH or NH2; and Z is a substituent. Also disclosed are compositions for and 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：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：DK20887D0

公开(公告)日：1987-01-15

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：AU2007329458A1

公开(公告)日：2008-06-12

申请号：AU2007329458

申请日：2007-12-04

Applicant: ABBOTT LAB

Inventor： ROSENBERG SAUL HOWARD ,  KROEGER PAUL E ,  WASS JOHN A ,  TSE CHRISTIN ,  ANDERSON MARK GERALD ,  TAHIR STEPHEN KENNETH

IPC: C12Q1/68

Abstract: Methods for identifying cancer patients eligible to receive Bcl-2 family inhibitor therapy and for monitoring patient response to Bcl-2 family inhibitor therapy comprise assessment of the expression levels of the biomarker combinations set out in TABLES 1, 2, 3, 4, 5 or 6 in a patient tissue sample. The methods of the invention allow more effective identification of patients to receive Bcl-2 family inhibitor therapy and of determination of patient response to the therapy.

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：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：DK514688D0

公开(公告)日：1988-09-15

申请号：DK514688

申请日：1988-09-15

Applicant: ABBOTT LAB

Inventor： ROSENBERG SAUL HOWARD ,  SHAM HING LEUNG ,  BAKER WILLIAM R ,  DELLARIA JR JOSEPH F ,  KEMPF DALE J

IPC: C07C271/10 ,  A61K31/395 ,  A61K31/415 ,  A61K31/42 ,  A61K31/421 ,  A61K31/535 ,  A61K31/536 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/54 ,  A61K38/00 ,  A61P9/12 ,  C07C67/00 ,  C07C69/24 ,  C07C213/00 ,  C07C215/10 ,  C07C215/20 ,  C07C215/28 ,  C07C217/08 ,  C07C217/28 ,  C07C229/22 ,  C07C229/26 ,  C07C229/30 ,  C07C229/32 ,  C07C229/34 ,  C07C229/36 ,  C07C231/00 ,  C07C231/02 ,  C07C233/11 ,  C07C233/22 ,  C07C233/40 ,  C07C233/47 ,  C07C233/51 ,  C07C235/20 ,  C07C237/12 ,  C07C237/20 ,  C07C239/20 ,  C07C255/46 ,  C07C265/02 ,  C07C265/04 ,  C07C271/16 ,  C07C271/20 ,  C07C271/22 ,  C07C275/24 ,  C07C317/28 ,  C07C317/44 ,  C07C317/48 ,  C07C323/24 ,  C07C323/41 ,  C07C323/56 ,  C07C323/59 ,  C07C323/60 ,  C07D207/12 ,  C07D211/76 ,  C07D213/40 ,  C07D233/32 ,  C07D233/61 ,  C07D263/04 ,  C07D263/06 ,  C07D263/16 ,  C07D263/22 ,  C07D263/24 ,  C07D263/28 ,  C07D265/10 ,  C07D273/04 ,  C07D277/24 ,  C07D285/10 ,  C07D295/12 ,  C07D295/13 ,  C07D295/185 ,  C07D295/205 ,  C07D295/215 ,  C07D295/22 ,  C07D309/14 ,  C07D319/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D521/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/08 ,  C07C125/063 ,  C07C91/02 ,  C07C101/04 ,  C07C103/34 ,  C07C147/06 ,  C07C149/273 ,  C07D207/04 ,  C07D231/12 ,  C07D233/64 ,  C07D239/10 ,  C07D241/02 ,  C07D263/18 ,  C07D265/30 ,  C07D277/30 ,  C07D291/04 ,  C07K5/04

Abstract: A renin inhibiting compound of the formula: wherein A is a substituent; W is C=O, CHOH or NR2 wherein R2 is hydrogen or loweralkyl; U is C=O, CH2 or NR2 wherein R2 is hydrogen or loweralkyl, with the proviso that when W is CHOH then U is CH2 and with the proviso that U is C=O or CH2 when W is NR2; V is CH, C(OH) or C(halogen) with the proviso that V is CH when U is NR2; R1 is loweralkyl, cycloalkylalkyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, 4-hydroxybenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (unsubstituted heterocyclic)methyl, (substituted heterocyclic)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino, provided that B is CH2 or CHOH or A is hydrogen when R1 is phenoxy, thiophenoxy or anilino; R3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, azidoalkyl, aminoalkyl, (alkyl)aminoalkyl, dialkylaminoalkyl, (alkoxy)(alkyl)aminoalkyl, (alkoxy)aminoalkyl, benzyl or heterocyclic ring substituted methyl; R4 is loweralkyl, cycloalkylmethyl or benzyl; R5 is OH or NH2; and Z is a substituent. Also disclosed are compositions for and a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.