US 5,643,879 A · Amino-substituted heterocycles as renin inhibitors

Abstract

The invention concerns novel renin-inhibitory compounds which contain an amino-substituted heterocycle at the P.sub.2 position. These are useful for treating renin-associated hypertension, congestive heart failure, glaucoma, hyperaldosteronism, and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the compounds, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, or hyperaldosteronism.

Claims24

Dependent claims

A compound of the formula ##STR25## or a pharmaceutically acceptable acid addition salt thereof wherein A is BOC, BBSP, Z, ##STR26## wherein R and R.sub.1 are each independently hydrogen or straight or branched chain lower alkyl which is unsubstituted or substituted by one or two hydroxy, one or two amino groups, or ##STR27## wherein this is a saturated ring containing two to five carbon atoms wherein Q is CH.sub.2, O, S, or NR wherein R is as above;

B is absent, PHE, TYR, or TYR(OME) with the proviso that when A is BBSP, B is absent;
C is CST, FCS, FCO, CD is DH, or STA;
D is absent, OH, or NR.sub.2 R.sub.3 wherein R.sub.2 and R.sub.3 are each independently hydrogen or straight or branched lower alkyl or when R.sub.2 is hydrogen, R.sub.3 can also be --(CH.sub.2).sub.m X wherein m is an integer of from zero to eight and X is --OH, ##STR28## as defined above, OR.sub.4, NR.sub.5 R.sub.6 wherein R.sub.4, R.sub.5, and R.sub.6 are each independently hydrogen, straight or branched chain lower alkyl substituted or unsubstituted by one or two hydroxy or amino groups with the proviso that when C is CAD, D is absent;
E is hydrogen, Z, BOC, TROC, or lower alkanoyl,
n is an integer of from 0 to 2;
X and Y are each independently O, S, N or NH and at least one of X and Y must be N;
X and
Y cannot both be N.

5 more elements

Dependencies are inferred from the claim text.

Facts

Application

08/440,585Filed 15 May 1995 · division

Priority

26 May 1989

Granted

1 Jul 1997

Term ends

Not estimatedThe source records don’t support an estimate.

Classification15 codes

C07K 5/06191
Dipeptides: containing heteroatoms different from O, S, or N
A61P 5/38
Drugs for disorders of the endocrine system: of the suprarenal hormones
A61P 9/00
Drugs for disorders of the cardiovascular system
A61P 9/12
Drugs for disorders of the cardiovascular system: antihypertensives

Family

Serial357,561Parent of this continuation-in-part · filed 26 May 1989

Serial511,271Parent of this division · filed 25 Apr 1990

Serial38,728Parent of this division · filed 26 Mar 1993

US 5,453,488 AParent of this division

US 5,238,923 AParent of this division

US 5,643,879 AThis patent

From the US filing history. Foreign family members aren’t listed.

Abstract

Claims24

Dependent claims

B is absent, PHE, TYR, or TYR(OME) with the proviso that when A is BBSP, B is absent;
C is CST, FCS, FCO, CD is DH, or STA;
D is absent, OH, or NR.sub.2 R.sub.3 wherein R.sub.2 and R.sub.3 are each independently hydrogen or straight or branched lower alkyl or when R.sub.2 is hydrogen, R.sub.3 can also be --(CH.sub.2).sub.m X wherein m is an integer of from zero to eight and X is --OH, ##STR28## as defined above, OR.sub.4, NR.sub.5 R.sub.6 wherein R.sub.4, R.sub.5, and R.sub.6 are each independently hydrogen, straight or branched chain lower alkyl substituted or unsubstituted by one or two hydroxy or amino groups with the proviso that when C is CAD, D is absent;
E is hydrogen, Z, BOC, TROC, or lower alkanoyl,
n is an integer of from 0 to 2;
X and Y are each independently O, S, N or NH and at least one of X and Y must be N;
X and
Y cannot both be N.

5 more elements

Dependencies are inferred from the claim text.

Amino-substituted heterocycles as renin inhibitors

Life of this patent

Abstract

Claims24

Amino-substituted heterocycles as renin inhibitors

Life of this patent

Abstract

Claims24