公开(公告)号：AU6759887A

公开(公告)日：1987-07-23

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 ,  C07C143/78 ,  C07C103/46 ,  C07C121/68 ,  C07C101/08 ,  C07C101/04 ,  C07C125/065 ,  C07C91/15 ,  C07C125/073 ,  C07C143/72 ,  C07C149/273 ,  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：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：CA1340948C

公开(公告)日：2000-04-04

申请号：CA615759

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

Abstract: A renin inhibiting compound of the formula: or parmaceutically 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：IE63602B1

公开(公告)日：1995-05-17

申请号：IE7987

申请日：1987-01-13

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 ,  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：DE3750184T2

公开(公告)日：1994-11-10

申请号：DE3750184

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：DE3750184D1

公开(公告)日：1994-08-18

申请号：DE3750184

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：AT108456T

公开(公告)日：1994-07-15

申请号：AT87100424

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：AU599581B2

公开(公告)日：1990-07-26

申请号：AU5274386

申请日：1986-01-28

Applicant: ABBOTT LAB

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

IPC: A61K31/16 ,  A61K31/165 ,  A61K31/47 ,  A61K31/55 ,  A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07C103/50 ,  C07C103/737 ,  C07C103/78 ,  C07C125/065

公开(公告)号：ES2004274A6

公开(公告)日：1988-12-16

申请号：ES8700881

申请日：1987-03-27

Applicant: ABBOTT LAB

Inventor： DELLARIA JOSEPH ,  KEMPF DALE JOHN ,  PLATTNER JACOB JOHN ,  SHAM HING LEUNG ,  FUNG ANTHONY K L ,  LULY JAY RICHARD ,  ROSENBERG SAUL HOWARD

IPC: A61K37/64

Abstract: COMPRENDE LA REACCION DE UN COMPUESTO DE FORMULA (I) CON UN COMPUESTO DE FORMULA (II), (III), (IV) O (V) PARA PROPORCIONAR UN COMPUESTO DE FORMULA (VI), EN LAS QUE LOS DIFERENTES SIMBOLOS REPRESENTAN RADICALES ORGANICOS.LOS COMPUESTOS DE FORMULA (VI) SON UTILES EN EL TRATAMIENTO DE LA HIPERTENSION CAUSADA POR RENINA.

公开(公告)号：GR870511B

公开(公告)日：1987-07-30

申请号：GR870100511

申请日：1987-03-30

Applicant: ABBOTT LAB

Inventor： DELLARIA JOSEPH ,  FUNG ANTHONY K L ,  KEMPF DALE JOHN ,  LULY JAY RICHARD ,  PLATTNER JACOB JOHN ,  ROSENBERG SAUL HOWARD ,  SHAM HING LEUNG