EP0189203A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Peptidylaminodiols
Assignee: Abbott Laboratories
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Filing: 1986-01-23
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Granted: —
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Expires: 2006-01-23
Abstract
Abstract The invention relates to renin inhibiting compounds of the formula: wherein R 10 is A is hydrogen or an N-protecting group; w is 0 or 1; B is hydrogen, hydroxy, NH, N-alkyl, loweralkyl or arylalkyl; with the proviso that when w is 1, B is NH and when w is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R 1 is loweralkyl or lipophilic or aromatic or hydrophilic amino acid side chains; m is 1-3; n is 1-3; p is 1-3; q is 1-3; s is 1-3; t is 0-2; R 2 is hydrogen or loweralkyl; R 3 and R 4 are independently selected from loweralkyl, lipophilic or aromatic amino acid side chains; R 5 and R 7 are independently selected from hydrogen or loweralkyl; and R 6 is hydrogen, loweralkyl, vinyl, arylalkyl or wherein R 8 is hydrogen or loweralkyl, X is O, NH or S and R 9 is hydrogen, loweralkyl or alkanoyl or XR 9 together can be loweralkylsulfonyl, N 3 or Cl.
Inventors
- 👤 Jay Richard Luly
- 👤 John Jacob Plattner
- 👤 Saul Howard Rosenberg
- 👤 Anthony K.L. Fung
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-08 13:14
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06078; C07K5/02; C07K5/0227; C07K5/06017; C07K5/06139; A; A61; A61K; A61K38/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
168 words
A renin inhibiting compound of the formula wherein R 10 is A is hydrogen or an N-protecting group; w is 0 or 1; B is hydrogen, hydroxy, NH, N-alkyl, loweralkyl or arylalkyl; with the proviso that when w is 1, B is NH and when w is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R 1 is loweralkyl or lipophilic or aromatic or hydrophilic amino acid side chains; m is 1-3; n is 1-3; p is 1-3; q is 1-3; s is 1-3; t is 0-2; R 2 is hydrogen or loweralkyl; R 3 and R 4 are independently selected from loweralkyl, lipophilic or aromatic amino acid side chains; R 5 and R 7 are independently selected from hydrogen or loweralkyl; and R 6 is hydrogen, loweralkyl, vinyl, arylalkyl or wherein R 8 is hydrogen or loweralkyl, X is 0, NH or S and R 9 is hydrogen, loweralkyl or alkanoyl or XR 9 together can be loweralkylsulfonyl, N 3 or Cl and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
168 words
A renin inhibiting compound of the formula wherein R 10 is A is hydrogen or an N-protecting group; w is 0 or 1; B is hydrogen, hydroxy, NH, N-alkyl, loweralkyl or arylalkyl; with the proviso that when w is 1, B is NH and when w is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R 1 is loweralkyl or lipophilic or aromatic or hydrophilic amino acid side chains; m is 1-3; n is 1-3; p is 1-3; q is 1-3; s is 1-3; t is 0-2; R 2 is hydrogen or loweralkyl; R 3 and R 4 are independently selected from loweralkyl, lipophilic or aromatic amino acid side chains; R 5 and R 7 are independently selected from hydrogen or loweralkyl; and R 6 is hydrogen, loweralkyl, vinyl, arylalkyl or wherein R 8 is hydrogen or loweralkyl, X is 0, NH or S and R 9 is hydrogen, loweralkyl or alkanoyl or XR 9 together can be loweralkylsulfonyl, N 3 or Cl and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
17 words
The renin inhibiting compounds of Claim 1 wherein R 10 is is hydrogen; and R 6 is
Claim 4
Dependent Claim
43 words
The renin inhibiting compound of Claim 2 wherein w is 1; B is NH, R 1 is benzyl, 4-methoxybenzyl or isobutyl; R 2 is hydrogen; R 3 is loweralkyl, (4-imidazoyl)methyl or (3-pyrazoyl)methyl; R 4 is loweralkyl or cycloalkylmethyl; and R 5 is hydrogen.
Claim 5
Dependent Claim
20 words
The renin inhibiting compounds of Claim 1 wherein R 10 is and R 6 is hydrogen, loweralkyl, vinyl or arylalkyl.
Claim 6
Dependent Claim
72 words
The renin inhibiting compounds of Claim 4 wherein A is t-butyloxycarbonyl, t-butylacetyl or ethoxycarbonyl; w is 1; B is NH; R 1 is benzyl, cyclohexylmethyl, (4-methox)ybenzyl, (1-naphthyl)methyl or isobutyl; R 2 is hydrogen or methyl; R 3 is methyl, (4-imidazoyl)methyl, benzyl, (3-pyrazoyl)methyl, (methylmercapto)methyl or isobutyl; R 4 is isobutyl or cyclohexylmethyl; R 5 is hydrogen or isopentyl; R 6 is hydrogen, loweralkyl, vinyl or benzyl; and R 7 is hydrogen or ethyl.
Claim 7
Dependent Claim
39 words
The renin inhibiting compounds of Claim 5 wherein A is ethoxycarbonyl; R 1 is (4-methoxy)benzyl; R 2 is hydrogen; R 3 is (4-imidazoyl)methyl; R 4 is cyclohexylmethyl; R 5 and R 7 are hydrogen; and R 6 is isobutyl.
Claim 8
Dependent Claim
38 words
The renin inhibiting compounds of Claim 5 wherein A is ethoxycarbonyl; R 1 is benzyl; R 2 , R 5 and R 7 are hydrogen; R 3 is (4-imidazoyl)methyl; R 4 is cyclohexylmethyl; and R 6 is isobutyl.
Claim 9
Dependent Claim
37 words
The renin inhibiting compounds of Claim 5 wherein A is ethoxycarbonyl; R 1 is benzyl; R 2 , R 5 and R 7 are hydrogen; R 3 and R 6 are isobutyl and R 4 is cyclohexylmethyl.
Claim 10
Dependent Claim
27 words
The renin inhibiting compounds of Claim 1 wherein R 10 is R 4 is cyclohexylmethyl; R 5 and R 7 are hydrogen; and R 6 is loweralkyl.
Claim 11
Dependent Claim
21 words
The renin inhibiting compound of Claim 9 wherein R 10 is A is ethoxycarbonyl; n is 1; and m is 2.
Claim 12
Dependent Claim
19 words
The renin inhibiting compound of Claim 9 wherein R 10 is A is hydrogen; and R 1 is methyl.
Claim 13
Dependent Claim
22 words
A pharmaceutical composition for treating renin-associated hypertension, comprising a pharmaceutical carrier and a therapeutically effective amount of the compound of Claim 1.
Claim 14
Dependent Claim
25 words
A method of treating hypertension comprising administering to a host in need of such treatment a therapeutically effective amount of a compound of Claim 1.
References Cited (Backward Citations)
No citation records indexed.
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