公开(公告)号：NZ231053A

公开(公告)日：1991-02-26

申请号：NZ23105389

申请日：1989-10-18

Applicant: ABBOTT LAB

Inventor： BISWANATH D E ,  DELLARIA JOSEPH F ,  BAKER WILLIAM R ,  ROSENBERG SAUL H ,  ZYDOWSKY THOMAS M ,  JAE HWAN SOO

IPC: C07D253/06 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/42 ,  A61K31/421 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/54 ,  A61K38/00 ,  A61P9/04 ,  A61P9/12 ,  A61P31/12 ,  A61P43/00 ,  C07D211/14 ,  C07D211/76 ,  C07D211/84 ,  C07D211/86 ,  C07D211/88 ,  C07D213/74 ,  C07D233/30 ,  C07D233/54 ,  C07D239/42 ,  C07D241/04 ,  C07D241/08 ,  C07D243/08 ,  C07D263/04 ,  C07D263/06 ,  C07D263/10 ,  C07D263/18 ,  C07D263/22 ,  C07D263/24 ,  C07D263/26 ,  C07D265/32 ,  C07D277/20 ,  C07D277/32 ,  C07D295/15 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07K5/078 ,  C07D403/14 ,  C07D401/12 ,  C07D405/14 ,  C07D417/14 ,  C07D295/00 ,  C07D243/04 ,  C07C103/19 ,  C07K5/06

Abstract: A renin inhibiting compound of the formula: wherein X is N, O or CH; R1 is absent or a functional group; A and L are independently selected from absent, C=O, SO2 and CH2; D is C=O, SO2 or CH2; Y is N or CH; R2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.

公开(公告)号：NZ226002A

公开(公告)日：1990-06-26

申请号：NZ22600288

申请日：1988-08-31

Applicant: ABBOTT LAB

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

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 ,  C07D277/04 ,  C07D307/14 ,  A61K31/425 ,  A61K31/495 ,  A61K37/02

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：DK514688A

公开(公告)日：1989-03-17

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.