US4470972A
Expired / Lapsed
US
⏱️ 0.0 years remaining
7-Carboxyalkylaminoacyl-1,4-dithia-7-azaspiro[4.4]-nonane-8-carboxylic acids
Assignee: Merck Sharp & Dohme LLC
•
Filing: 1982-12-06
•
Granted: 1984-09-11
•
Expires: 2002-12-06
Abstract
Abstract This invention relates to 7-carboxyalkyl-aminoacyl-1,4-adithia-7-azaspiro[4.4]nonane-8-carboxylic acids. The compounds of the invention are useful in the treatment of cardiovascular disorders and especially as antihypertensive agents.
Inventors
- 👤 Elijah H. Gold
- 👤 Bernard R. Neustadt
- 👤 Elizabeth M. Smith
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 01:56
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/02; C07K5/022; C07K5/0222; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 32
Claim 1
Independent Claim
34 words
A compound represented by the formula ##STR6## wherein: R is a lower alkyl, benzyl, benzylthio, benzyloxy, phenylthio, or phenoxy; R 1 is hydroxy or lower alkoxy; R 2 is hydrogen, lower alkyl or aminoloweralkyl;
Claim 2
Dependent Claim
34 words
A compound represented by the formula ##STR6## wherein: R is a lower alkyl, benzyl, benzylthio, benzyloxy, phenylthio, or phenoxy; R 1 is hydroxy or lower alkoxy; R 2 is hydrogen, lower alkyl or aminoloweralkyl;
Claim 3
Dependent Claim
6 words
and the pharmaceutically acceptable salts thereof.
Claim 4
Dependent Claim
6 words
and the pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim
10 words
A compound of claim 1 wherein R 2 is methyl.
Claim 6
Dependent Claim
11 words
A compound of claim 2 wherein R 1 is lower alkoxy.
Claim 7
Dependent Claim
9 words
A compound of claim 3 wherein R is benzyl.
Claim 8
Dependent Claim
10 words
A compound of claim 4 wherein R 1 is ethoxy.
Claim 9
Dependent Claim
10 words
A compound of claim 5 which is 7-[N-(1(S)-carboethoxy-3-phenylpropyl)-(S)-alanyl]-1,4-dithia-7-azaspiro[4.4]-nonane-8(S)-carboxylic acid hydrochloride.
Claim 10
Dependent Claim
10 words
A compound of claim 2 which is 7-[N-(1(S)-carboxy-3-phenylpropyl)-(S)-alanyl]-1,4-dithia-7-azaspiro[4.4]-nonane-8(S)-carboxylic acid hydrochloride.
Claim 11
Dependent Claim
9 words
A compound of claim 2 which is 7-[N-(1(S)-carboxy-3-phenylpropyl)-(S)-alanyl]-1,4-dithia-7-azaspiro[4.4]-nonane-8(S)-carboxylic acid.
Claim 12
Dependent Claim
10 words
A compound of claim 5 which is 7-[N-(1(S)-carboethoxy-3-phenylpropyl)-(S)-alanyl]-1,4-dithia-7-azaspiro[4.4]-nonane-8(S)-carboxylic acid hemimaleate.
Claim 13
Dependent Claim
10 words
A compound of claim 1 wherein R 2 is hydrogen.
Claim 14
Dependent Claim
10 words
A compound of claim 1 wherein R 2 is aminobutyl.
Claim 15
Dependent Claim
10 words
A compound of claim 11 which is 7-[Nα-(1(S)-carboethoxy-3-phenylpropyl)-(S)-lysyl]-1,4-dithia-7-azaspiro[4.4]nonane-8(S)-carboxylic acid dihydrochloride.
Claim 16
Dependent Claim
9 words
A compound of claim 11 which is 7-[Nα-(1(S)-carboethoxy-3-phenylpropyl)-(S)-lysyl]-1,4-dithia-7-azaspiro[4.4]nonane-8(S)-carboxylic acid.
Claim 17
Dependent Claim
10 words
A compound of claim 11 which is 7-[Nα-(1(S)-carboxy-3-phenylpropyl)-(S)-lysyl]-1,4-dithia-7-azaspiro[4.4]nonane-8(S)-carboxylic acid dihydrochloride.
Claim 18
Dependent Claim
9 words
A compound of claim 11 which is 7-[Nα-(1(S)-carboxy-3-phenylpropyl)-(S)-lysyl]-1,4-dithia-7-azaspiro[4.4]nonane-8(S)-carboxylic acid.
Claim 19
Dependent Claim
9 words
A compound of claim 1 wherein R is benzylthio.
Claim 20
Dependent Claim
9 words
A compound of claim 1 wherein R is benzyloxy.
Claim 21
Dependent Claim
9 words
A compound of claim 1 wherein R is phenylthio.
Claim 22
Dependent Claim
9 words
A compound of claim 1 wherein R is phenyloxy.
Claim 23
Dependent Claim
10 words
A compound of claim 1 wherein R is lower alkyl.
Claim 24
Dependent Claim
11 words
A compound of claim 20 which is 7-[N-(1(S)-carboethoxypentyl)-(S)-alanyl]-1,4-dithia-7-azaspiro [4.4]-nonane-8(S)-carboxylic acid hydrochloride.
Claim 25
Dependent Claim
10 words
A compound of claim 20 which is 7-[N-(1(S)-carboethoxybutyl)-(S)-alanyl]-1,4-dithia-7-azaspiro[4.4]-nonane-8(S)-carboxylic acid hydrochloride.
Claim 26
Dependent Claim
11 words
A compound of claim 20 which is 7-[N-(1(S)-carboethoxyhexyl)-(S)-alanyl]-1,4[-dithia-7-azaspiro [4.4]-nonane-8(S)-carboxylic acid hydrochloride.
Claim 27
Dependent Claim
14 words
A compound of claim 1 wherein the pharmaceutically acceptable salts is an acid salt.
Claim 28
Dependent Claim
13 words
A compound of claim 24 wherein the acid salt is hydrochloride or hemimaleate.
Claim 29
Dependent Claim
21 words
A pharmaceutical composition comprising an antihypertensive effective amount of a compound according to claim 1 together with a pharmaceutically acceptable carrier.
Claim 30
Dependent Claim
21 words
A pharmaceutical composition comprising an antihypertensive effective amount of a compound according to claim 6 together with a pharmaceutically acceptable carrier.
Claim 31
Dependent Claim
25 words
A method of treating hypertension in mammals comprising administering to a mammal afflicted with hypertension an effective amount of a compound according to claim 1.
Claim 32
Dependent Claim
25 words
A method of treating hypertension in mammals comprising administering to a mammal afflicted with hypertension an effective amount of a compound according to claim 6.
References Cited (Backward Citations)
US4311697A
Cited
US4325945A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-09-11 | 1988-03-12 | 1988-09-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-09-11 | 1992-03-12 | 1992-09-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-09-11 | 1996-03-12 | 1996-09-11 | $7700.00 | Window Closed / Lapsed |