US4217359A
Expired / Lapsed
US
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Carbamate derivatives of mercaptoacyl hydroxy prolines
Assignee: ER Squibb and Sons LLC
•
Filing: 1979-08-13
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Granted: 1980-08-12
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Expires: 1999-08-13
Abstract
Abstract New carbamate derivatives of mercaptoacyl hydroxy prolines which have the general formula ##STR1## are useful as hypotensive agents.
Inventors
- 👤 John Krapcho
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 17:29
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
112 words
A compound of the formula ##STR20## wherein R, R 2 and R 3 each is hydrogen or lower alkyl; R o and R 1 each is hydrogen, lower alkyl, allyl, propargyl, cyclo-lower alkyl, phenyl or substituted phenyl, or R o and R 1 complete a pyrrolidine, piperidine or morpholine ring; R 4 is hydrogen, a hydrolyzable organic protecting group of the formula R 5 CO-- or ##STR21## R 5 is lower alkyl, phenyl, substituted phenyl, phenyl-lower alkyl, substituted phenyl-lower alkyl, cycloalkyl, thienyl, or furyl; the phenyl substituent in the above groups is halogen, lower alkyl, lower alkoxy, lower alkylthio or trifluoromethyl; n is 0, 1 or 2; and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
112 words
A compound of the formula ##STR20## wherein R, R 2 and R 3 each is hydrogen or lower alkyl; R o and R 1 each is hydrogen, lower alkyl, allyl, propargyl, cyclo-lower alkyl, phenyl or substituted phenyl, or R o and R 1 complete a pyrrolidine, piperidine or morpholine ring; R 4 is hydrogen, a hydrolyzable organic protecting group of the formula R 5 CO-- or ##STR21## R 5 is lower alkyl, phenyl, substituted phenyl, phenyl-lower alkyl, substituted phenyl-lower alkyl, cycloalkyl, thienyl, or furyl; the phenyl substituent in the above groups is halogen, lower alkyl, lower alkoxy, lower alkylthio or trifluoromethyl; n is 0, 1 or 2; and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
93 words
A compound of the formula ##STR22## wherein R, R 2 and R 3 each is hydrogen or lower alkyl; R o and R 1 each is hydrogen, lower alkyl, allyl, propargyl, cyclo-lower alkyl, phenyl or substituted phenyl wherein the phenyl substituent is halogen, lower alkyl, lower alkoxy, lower alkylthio or trifluoromethyl, or R o and R 1 complete a pyrrolidine, piperidine or morpholine ring; R 4 is hydrogen, R 5 CO-- or ##STR23## R 5 is lower alkyl, phenyl or phenyl-lower alkyl; n is 0, 1 or 2; and pharmaceutically acceptable salts thereof.
Claim 4
Dependent Claim
93 words
A compound of the formula ##STR22## wherein R, R 2 and R 3 each is hydrogen or lower alkyl; R o and R 1 each is hydrogen, lower alkyl, allyl, propargyl, cyclo-lower alkyl, phenyl or substituted phenyl wherein the phenyl substituent is halogen, lower alkyl, lower alkoxy, lower alkylthio or trifluoromethyl, or R o and R 1 complete a pyrrolidine, piperidine or morpholine ring; R 4 is hydrogen, R 5 CO-- or ##STR23## R 5 is lower alkyl, phenyl or phenyl-lower alkyl; n is 0, 1 or 2; and pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim
10 words
A compound as in claim 2 wherein R is hydrogen.
Claim 6
Dependent Claim
10 words
A compound as in claim 2 wherein n is 1.
Claim 7
Dependent Claim
11 words
A compound as in claim 2 wherein R 4 is hydrogen.
Claim 8
Dependent Claim
12 words
A compound as in claim 2 wherein R 2 is lower alkyl.
Claim 9
Dependent Claim
12 words
A compound as in claim 2 wherein R o is lower alkyl.
Claim 10
Dependent Claim
11 words
A compound as in claim 2 wherein R 4 is ##STR24##
Claim 11
Dependent Claim
32 words
A compound of the formula ##STR25## wherein R, R o , R 1 , R 2 , R 3 , R 4 and n have the same meaning as in claim 2.
Claim 12
Dependent Claim
55 words
A compound as in claim 9 wherein R is hydrogen or lower alkyl; R o and R 1 each is C 1 -C 4 -lower alkyl; R 2 and R 3 each is hydrogen or C 1 -C 4 -lower alkyl; R 4 is hydrogen, lower alkanoyl or benzoyl; and n is 0 or 1.
Claim 13
Dependent Claim
41 words
A compound as in claim 9 wherein R and R 4 each is hydrogen; R o and R 1 each is C 1 -C 4 -lower alkyl; R 2 and R 3 each is hydrogen or methyl; and n is 1.
Claim 14
Dependent Claim
31 words
A compound as in claim 9 wherein R, R 1 , R 3 and R 4 each is hydrogen; R o and R 2 each is methyl; and n is 1.
Claim 15
Dependent Claim
32 words
A compound as in claim 9 wherein R, R 1 and R 3 each is hydrogen; R o and R 2 each is methyl; R 4 is acetyl; and n is 1.
Claim 16
Dependent Claim
10 words
A compound as in claim 9 having the name trans-1-[D-(3-acetylthio)-2-methyl-1-oxopropyl]-4-[[(methylamino)carbonyl]oxy]-L-proline.
Claim 17
Dependent Claim
10 words
A compound as in claim 9 having the name trans-1-(D-3-mercapto-2-methyl-1-oxopropyl)-4-[[(methylamino)carbonyl]oxy]-L-proline.
Claim 18
Dependent Claim
11 words
A compound as defined in claim 9 having the name cis-1-[D-(3-acetylthio)-2-methyl-1-oxopropyl]-4-[[(methylamino)carbonyl]oxy]-L-proline.
Claim 19
Dependent Claim
10 words
A compound as in claim 9 having the name cis-1-(D-3-mercapto-2-methyl-1-oxopropyl)-4-[[(methylamino)carbonyl]oxy]-L-proline.
Claim 20
Dependent Claim
23 words
A composition useful for reducing blood pressure comprising an effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier therefor.
Claim 21
Dependent Claim
30 words
A method for reducing blood pressure in hypertensive mammals which comprises administering a composition comprising an effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier therefor.
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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) | 1983-08-12 | 1984-02-11 | 1984-08-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-08-12 | 1988-02-11 | 1988-08-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-08-12 | 1992-02-11 | 1992-08-12 | $7700.00 | Window Closed / Lapsed |