US4746676A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Carboxyalkyl dipeptide compounds
Assignee: Aventis Pharmaceuticals Inc
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Filing: 1984-09-12
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Granted: 1988-05-24
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Expires: 2004-09-12
Abstract
Abstract Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.
Inventors
- 👤 Edward S. Neiss
- 👤 John T. Suh
- 👤 John R. Regan
- 👤 Jerry W. Skiles
- 👤 Jeffrey N. Barton
- 👤 Paul Menard
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 12:40
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/02; C07K5/022; C07K5/0222; A; A61; A61P; A61P27/00; A61P27/02; A61P43/00; A61P7/00; A61P7/10; A61P9/00; A61P9/12; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06026; C07K5/06191; A61K; A61K38/00
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
167 words
A compound of the formula ##STR10## wherein Y 1 and Y 2 are independently OH or alkoxy having 1 to 8 carbon atoms; R 1 is H, C 1 -C 8 -alkyl, phenyl-C 1 -C 8 -alkyl or indanyl; R 2 is H, C 1 -C 8 -alkyl or amino-C 1 -C 8 -alkyl; R 3 is H or C 1-8 alkyl; G with the nitrogen and carbon to which it is joined forms a proline, Z is --(CH 2 ) i --N(R 3 )SO 2 --M; ═N(CH 2 ) i --SO 2 --M; --(CH 2 ) i --N(R 3 )--M; ═N(CH 2 ) i --M; ═CH--(CH 2 ) i --C(O)--M; or --(CH 2 ) i --N(R 3 )--C(O)--M; i is 0 to 6 inclusive; M is ##STR11## A is SO 2 NH 2 or halogen; D is SO 2 NH 2 or halogen; E is SO 2 NH 2 , halogen, or NH 2 or a pharmaceutically acceptable acid addition, alkali or alkaline earth metal salt.
Claim 2
Dependent Claim
167 words
A compound of the formula ##STR10## wherein Y 1 and Y 2 are independently OH or alkoxy having 1 to 8 carbon atoms; R 1 is H, C 1 -C 8 -alkyl, phenyl-C 1 -C 8 -alkyl or indanyl; R 2 is H, C 1 -C 8 -alkyl or amino-C 1 -C 8 -alkyl; R 3 is H or C 1-8 alkyl; G with the nitrogen and carbon to which it is joined forms a proline, Z is --(CH 2 ) i --N(R 3 )SO 2 --M; ═N(CH 2 ) i --SO 2 --M; --(CH 2 ) i --N(R 3 )--M; ═N(CH 2 ) i --M; ═CH--(CH 2 ) i --C(O)--M; or --(CH 2 ) i --N(R 3 )--C(O)--M; i is 0 to 6 inclusive; M is ##STR11## A is SO 2 NH 2 or halogen; D is SO 2 NH 2 or halogen; E is SO 2 NH 2 , halogen, or NH 2 or a pharmaceutically acceptable acid addition, alkali or alkaline earth metal salt.
Claim 3
Dependent Claim
9 words
A compound of claim 1 having the formula ##STR12##
Claim 4
Dependent Claim
23 words
The compound according to claim 1 which is N-[N-[(1S)-1-(Hydroxycarbonyl)-3-phenylpropyl]-L-alanyl]-4-(2,4-disulfamoyl-5-chloroanilino)proline or a pharmaceutically acceptable acid addition alkali metal, or alkaline earth metal salt thereof.
Claim 5
Dependent Claim
23 words
The compound according to claim 1 which is N-[N-[(1S)-1-(Hydroxycarbonyl)-3-phenylpropyl]-L-alanyl]-4-(2,4-disulfamoyl-5-chlorophenylimino)proline or a pharmaceutically acceptable acid addition alkali metal, or alkaline earth metal salt thereof.
Claim 6
Dependent Claim
23 words
The compound according to claim 1 which is N-[N-[(1S)-1-(Hydroxycarbonyl)-3-phenylpropyl]-L-alanyl]-4-(2-chloro-4-amino-5-sulfamoylphenyl-sulfonylimino)proline or a pharmaceutically acceptable acid addition alkali metal, or alkaline earth metal salt thereof.
Claim 7
Dependent Claim
23 words
The compound according to claim 1 which is (4S)-1-((2S)-2-(N-((1S)-1-Carboxy-3-phenylpropyl)amino)propionyl)-4-(4-amino-2-chloro-5-sulfonamidobenzenesulfonyl)aminoproline or a pharmaceutically acceptable acid addition, alkali metal, or alkaline earth metal salt thereof.
Claim 8
Dependent Claim
18 words
An antihypertensive pharmaceutical preparation comprising a compound or salt according to claim 1 and a pharmaceutically acceptable carrier.
Claim 9
Dependent Claim
18 words
An anti-glaucoma pharmaceutical preparation comprising a compound or salt according to claim 1 and a pharmaceutically acceptable carrier.
Claim 10
Dependent Claim
28 words
A method of relieving hypertension in a host suffering therefrom, comprising administering to said host a therapeutically effective amount of a compound or salt according to claim 1.
Claim 11
Dependent Claim
30 words
A method of relieving elevated intraocular pressure in a host suffering therefrom, comprising administering to said host a therapeutically effective amount of a compound or salt according to claim 1.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-05-24 | 1991-11-23 | 1992-05-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-05-24 | 1995-11-23 | 1996-05-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-05-24 | 1999-11-23 | 2000-05-24 | $7700.00 | Window Closed / Lapsed |