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US4645759A
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Renin inhibiting compounds
Assignee: Abbott Laboratories
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Filing: 1985-05-17
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Granted: 1987-02-24
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Expires: 2005-05-17
Abstract
Abstract The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is an N-protecting group; n is 0 or 1; B is hydrogen, hydroxy, NH, loweralkyl or arylalkyl; with the proviso that when A is an N-protecting group, B is NH and when n is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R 1 , R 3 and R 5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R 2 , R 4 , R 7 , R 8 and R 9 are hydrogen or loweralkyl and may be the same or different; X is NH, O, S, SO or SO 2 ; and R 6 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group, with the proviso that R 6 may be an N-protecting group when X is NH.
Inventors
- 👤 Jay R. Luly
- 👤 John J. Plattner
- 👤 Joseph F. Dellaria
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 21:13
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06078; C07K5/02; C07K5/0227; A; A61; A61K; A61K38/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55; Y10; Y10S; Y10S530/00; Y10S530/86
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
82 words
A renin inhibiting compound of the formula: ##STR3## wherein A is a N-protecting group; R 1 is arylalkyl; R 3 is loweralkyl, arylalkyl, hydroxyloweralkyl, hydroxyarylalkyl, or imidazole-4-yl-loweralkyl; R 5 is loweralkyl, arylalkyl or cycloalkylalkyl; R 2 , R 4 , R 7 , R 8 and R 9 are independently selected from hydrogen and loweralkyl; X is NH, O, S, SO or SO 2 ; and R 6 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group when X is NH.
Claim 2
Dependent Claim
82 words
A renin inhibiting compound of the formula: ##STR3## wherein A is a N-protecting group; R 1 is arylalkyl; R 3 is loweralkyl, arylalkyl, hydroxyloweralkyl, hydroxyarylalkyl, or imidazole-4-yl-loweralkyl; R 5 is loweralkyl, arylalkyl or cycloalkylalkyl; R 2 , R 4 , R 7 , R 8 and R 9 are independently selected from hydrogen and loweralkyl; X is NH, O, S, SO or SO 2 ; and R 6 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group when X is NH.
Claim 3
Dependent Claim
24 words
The renin inhibiting compounds of claim 1 wherein R 2 , R 4 , R 7 , R 8 and R 9 are hydrogen.
Claim 4
Dependent Claim
31 words
The renin inhibiting compound of claim 2 wherein A is Boc, R 1 is benzyl, R 3 is methyl, R 5 is isobutyl, X is SO and R 6 is cyclohexyl.
Claim 5
Dependent Claim
16 words
The renin inhibiting compounds of claim 2 wherein R 1 is benzyl or α- or β-naphthyl.
Claim 6
Dependent Claim
12 words
The renin inhibiting compounds of claim 4 wherein R 3 is methyl.
Claim 7
Dependent Claim
12 words
The renin inhibiting compounds of claim 4 wherein R 3 is imidazole-4-yl-methyl.
Claim 8
Dependent Claim
12 words
The renin inhibiting comounds of claim 4 wherein R 5 is isobutyl.
Claim 9
Dependent Claim
12 words
The renin inhibiting compounds of claim 4 wherein R 5 is cyclohexylmethyl.
Claim 10
Dependent Claim
15 words
The renin inhibiting compounds of claim 4 wherein X is S or SO 2 .
Claim 11
Dependent Claim
14 words
The renin inhibiting compounds of claim 4 wherein R 6 is cyclohexyl or isopropyl.
Claim 12
Dependent Claim
11 words
The renin inhibiting compounds of claim 4 wherein X is oxygen.
Claim 13
Dependent Claim
11 words
The renin inhibiting compounds of claim 4 wherein X is NH.
Claim 14
Dependent Claim
32 words
The renin inhibiting compounds of claim 2 wherein X is S, R 1 is benzyl, R 3 is imidazole-4-yl-methyl, R 5 is cyclohexylmethyl or benzyl and R 6 is isopropyl or cyclohexyl.
Claim 15
Dependent Claim
31 words
The renin inhibiting compounds of claim 2 wherein X is S, R 1 is β-naphthyl, R 3 is imidazole-4-yl-methyl, R 5 is cyclohexylmethyl, benzyl, or isobutyl and R 6 is cyclohexyl.
Claim 16
Dependent Claim
32 words
The renin inhibiting compounds of claim 2 wherein X is SO 2 , R 1 is benzyl, R 3 is imidazole-4-yl-methyl, R 5 is cyclohexylmethyl and R 6 is cyclohexyl or isopropyl.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-02-23 | 1990-08-25 | 1991-02-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-02-23 | 1994-08-25 | 1995-02-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-02-23 | 1998-08-25 | 1999-02-24 | $7700.00 | Window Closed / Lapsed |