Patent US4192878A successfully refreshed from Google Patents.
US4192878A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Derivatives of thiazolidinecarboxylic acids and related acids
Assignee: ER Squibb and Sons LLC
•
Filing: 1978-05-22
•
Granted: 1980-03-11
•
Expires: 1998-05-22
Abstract
Abstract New substituted derivatives of thiazolidine-, thiazane- and related carboxylic acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
Inventors
- 👤 Miguel A. Ondetti
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 13:31
CPC Classifications
C; C07; C07D; C07D265/00; C07D265/28; C07D265/30; C07D277/00; C07D277/02; C07D277/04; C07D277/06; C07D279/00; C07D279/04; C07D279/10; C07D279/12
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
99 words
A compound of the formula ##STR12## wherein R is hydroxy or lower alkoxy; R 1 , R 2 , R 5 and R 6 each is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl or mercapto-lower alkylene; R 4 is hydrogen, lower alkanoyl, benzoyl or ##STR13## X is S, SO, or SO 2 ; and p is 0 or 1; and basic salts thereof; wherein the terms lower alkyl, lower alkoxy and lower alkylene refer to groups having 1 to 7 carbon atoms and the term lower alkanoyl refers to groups having up to 7 carbon atoms.
Claim 2
Dependent Claim
99 words
A compound of the formula ##STR12## wherein R is hydroxy or lower alkoxy; R 1 , R 2 , R 5 and R 6 each is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl or mercapto-lower alkylene; R 4 is hydrogen, lower alkanoyl, benzoyl or ##STR13## X is S, SO, or SO 2 ; and p is 0 or 1; and basic salts thereof; wherein the terms lower alkyl, lower alkoxy and lower alkylene refer to groups having 1 to 7 carbon atoms and the term lower alkanoyl refers to groups having up to 7 carbon atoms.
Claim 3
Dependent Claim
15 words
A compound as in claim 1 wherein R 5 and R 6 each is hydrogen.
Claim 4
Dependent Claim
10 words
A compound as in claim 2 wherein X is sulfur.
Claim 5
Dependent Claim
11 words
A compound as in claim 1 wherein R 4 is ##STR14##
Claim 6
Dependent Claim
49 words
A compound as in claim 1 wherein R is hydroxy, methoxy or ethoxy; R 1 , R 2 , R 3 , R 5 and R 6 each is hydrogen, methyl or ethyl; R 4 is hydrogen, acetyl or benzoyl; X is sulfur; and p is 0 or 1.
Claim 7
Dependent Claim
11 words
A compound as in claim 1 wherein R 4 is hydrogen.
Claim 8
Dependent Claim
11 words
A compound as in claim 1 wherein R 4 is acetyl.
Claim 9
Dependent Claim
11 words
A compound as in claim 1 wherein R 4 is benzoyl.
Claim 10
Dependent Claim
10 words
A compound as in claim 1 wherein R is hydroxy.
Claim 11
Dependent Claim
10 words
A compound as in claim 1 wherein p is 1.
Claim 12
Dependent Claim
10 words
A compound as in claim 1 wherein X is sulfur.
Claim 13
Dependent Claim
35 words
A compound as in claim 11 wherein R is hydroxy; R 1 , R 2 , R 3 , R 5 and R 6 each is hydrogen; R 4 is benzoyl; and p is 1.
Claim 14
Dependent Claim
34 words
A compound as in claim 11 wherein R is hydroxy; R 1 , R 2 , R 3 , R 4 , R 5 and R 6 each is hydrogen; and p is 1.
Claim 15
Dependent Claim
35 words
A compound as in claim 11 wherein R is hydroxy; R 1 , R 2 , R 4 , R 5 and R 6 each is hydrogen; R 3 is methyl; and p is 1.
Claim 16
Dependent Claim
13 words
The compound of claim 13 in which the thiazolidine is in the L-form.
Claim 17
Dependent Claim
13 words
The compound of claim 14 in which the thiazolidine is in the L-form.
Claim 18
Dependent Claim
109 words
A composition comprising a compound of the formula ##STR15## wherein R is hydroxy or lower alkoxy; R 1 , R 2 , R 5 and R 6 each is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl or mercapto-lower alkylene; R 4 is hydrogen, lower alkanoyl, benzoyl or ##STR16## X is S, SO, or SO 2 ; and p is 0 or 1; or a basic salt thereof; wherein the terms lower alkyl, lower alkoxy and lower alkylene refer to groups having 1 to 7 carbon atoms and the term lower alkanoyl refers to groups having up to 7 carbon atoms; and a pharmaceutically acceptable vehicle therefor.
Claim 19
Dependent Claim
109 words
A composition comprising a compound of the formula ##STR15## wherein R is hydroxy or lower alkoxy; R 1 , R 2 , R 5 and R 6 each is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl or mercapto-lower alkylene; R 4 is hydrogen, lower alkanoyl, benzoyl or ##STR16## X is S, SO, or SO 2 ; and p is 0 or 1; or a basic salt thereof; wherein the terms lower alkyl, lower alkoxy and lower alkylene refer to groups having 1 to 7 carbon atoms and the term lower alkanoyl refers to groups having up to 7 carbon atoms; and a pharmaceutically acceptable vehicle therefor.
Claim 20
Dependent Claim
19 words
A composition as in claim 17 comprising a compound of the formula ##STR17## and a pharmaceutically acceptable vehicle therefor.
Claim 21
Dependent Claim
19 words
A composition as in claim 18 comprising a compound of the formula ##STR18## and a pharmaceutically acceptable vehicle therefor.
Claim 22
Independent Claim
118 words
A method for reducing blood pressure which comprises administering a composition comprising a compound of the formula ##STR19## wherein R is hydroxy or lower alkoxy; R 1 , R 2 , R 5 and R 6 each is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl or mercapto-lower alkylene; R 4 is hydrogen, lower alkanoyl, benzoyl or ##STR20## X is S, SO, or SO 2 ; and p is 0 or 1; or a basic salt thereof; wherein the terms lower alkyl, lower alkoxy and lower alkylene refer to groups having 1 to 7 carbon atoms and the term lower alkanoyl refers to groups having up to 7 carbon atoms; and a pharmaceutically acceptable vehicle therefor.
Claim 23
Independent Claim
118 words
A method for reducing blood pressure which comprises administering a composition comprising a compound of the formula ##STR19## wherein R is hydroxy or lower alkoxy; R 1 , R 2 , R 5 and R 6 each is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl or mercapto-lower alkylene; R 4 is hydrogen, lower alkanoyl, benzoyl or ##STR20## X is S, SO, or SO 2 ; and p is 0 or 1; or a basic salt thereof; wherein the terms lower alkyl, lower alkoxy and lower alkylene refer to groups having 1 to 7 carbon atoms and the term lower alkanoyl refers to groups having up to 7 carbon atoms; and a pharmaceutically acceptable vehicle therefor.
Claim 24
Dependent Claim
28 words
A method for reducing blood pressure as in claim 20 which comprises administering a composition comprising a compound of the formula ##STR21## and a pharmaceutically acceptable vehicle therefor.
Claim 25
Dependent Claim
28 words
A method for reducing blood pressure as in claim 20 which comprises administering a composition comprising a compound of the formula ##STR22## and a pharmaceutically acceptable vehicle therefor.
Claim 26
Dependent Claim
36 words
A compound as in claim 11 wherein R is hydroxy; R 1 , R 2 , R 5 and R 6 each is hydrogen; R 3 is methyl; R 4 is acetyl; and p is 1.
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) | 1983-03-11 | 1983-09-10 | 1984-03-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-03-11 | 1987-09-10 | 1988-03-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-03-11 | 1991-09-10 | 1992-03-11 | $7700.00 | Window Closed / Lapsed |