US4401677A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Enkephalinase inhibitors
Assignee: ER Squibb and Sons LLC
•
Filing: 1981-10-09
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Granted: 1983-08-30
•
Expires: 2001-10-09
Abstract
Abstract The degradation of enkephalins in a mammalian host is inhibited by administration of an enkephalinase enzyme inhibitor of the formula ##STR1##
Inventors
- 👤 Roland Greenberg
- 👤 David W. Cushman
- 👤 B. Richard Vogt
- 👤 Frank L. Weisenborn
- 👤 Michael J. Antonaccio
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 05:30
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/20
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
113 words
A method of inhibiting the degradation of enkephalins by the enkephalinase enzyme in a mammalian host which comprises administering to said mammal an enkephalinase inhibiting effective amount of the enkephalinase inhibitor of the formula ##STR46## or a pharmaceutically acceptable salt thereof wherein: R 1 is straight or branched chain alkyl of 1 to 4 carbons, benzyl or phenethyl; R 2 is straight or branched chain alkyl of 1 to 4 carbons, ##STR47## --(CH 2 ) n --NH 2 , --(CH 2 ) n --SH, --(CH 2 ) n --S-lower alkyl wherein lower alkyl is straight or branched chain of 1 to 4 carbons, ##STR48## and n is an integer from 1 to 4.
Claim 2
Independent Claim
113 words
A method of inhibiting the degradation of enkephalins by the enkephalinase enzyme in a mammalian host which comprises administering to said mammal an enkephalinase inhibiting effective amount of the enkephalinase inhibitor of the formula ##STR46## or a pharmaceutically acceptable salt thereof wherein: R 1 is straight or branched chain alkyl of 1 to 4 carbons, benzyl or phenethyl; R 2 is straight or branched chain alkyl of 1 to 4 carbons, ##STR47## --(CH 2 ) n --NH 2 , --(CH 2 ) n --SH, --(CH 2 ) n --S-lower alkyl wherein lower alkyl is straight or branched chain of 1 to 4 carbons, ##STR48## and n is an integer from 1 to 4.
Claim 3
Dependent Claim
21 words
A method of claim 1 wherein R 1 is --CH 3 , --CH 2 --CH(CH 3 ) 2 , or ##STR49##
Claim 4
Dependent Claim
10 words
A method of claim 2 wherein R 1 is ##STR50##
Claim 5
Dependent Claim
10 words
The method of claim 3 wherein R 2 is ##STR51##
Claim 6
Dependent Claim
16 words
The method of claim 3 wherein R 2 is --CH 2 --CH(CH 3 ) 2 .
Claim 7
Dependent Claim
16 words
The method of claim 2 wherein R 1 is --CH 3 and R 2 is ##STR52##
Claim 8
Dependent Claim
16 words
The method of claim 2 wherein R 1 is --CH 3 and R 2 is ##STR53##
Claim 9
Dependent Claim
16 words
The method of claim 2 wherein R 1 is --CH 3 and R 2 is ##STR54##
Claim 10
Dependent Claim
11 words
The method of claim 8 wherein said enkephalinase inhibitor is 3-hydroxy-N-(DL-3-mercapto-2-methyl-1-oxopropyl)-L-tyrosine.
Claim 11
Dependent Claim
11 words
The method of claim 8 wherein said enkephalinase inhibitor is 3-hydroxy-N-(D-3-mercapto-2-methyl-1-oxopropyl)-L-tyrosine.
Claim 12
Dependent Claim
20 words
The method of claim 2 wherein R 1 is --CH 2 --CH(CH 3 ) 2 and R 2 is ##STR55##
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) | 1986-08-29 | 1987-02-28 | 1987-08-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-08-29 | 1991-02-28 | 1991-08-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-08-29 | 1995-02-28 | 1995-08-30 | $7700.00 | Window Closed / Lapsed |