US4774256A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Use of enkephalinase inhibitors as analgesic agents
Assignee: ER Squibb and Sons LLC
•
Filing: 1987-11-13
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Granted: 1988-09-27
•
Expires: 2007-11-13
Abstract
Abstract Mercaptoalkanoyl and acylmercaptoalkanoyl compounds of the formula ##STR1## wherein n is an integer from one to fifteen possess enkephalinase inhibition activity and are useful as analgesic agents.
Inventors
- 👤 Norma G. Delaney
- 👤 Eric M. Gordon
- 👤 Miguel A. Ondetti
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 21:13
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/16
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
215 words
A method of relieving pain in a mammalian specie which comprises administering to said mammalian specie a composition containing an analgesically effective amount of a compound of the formula: ##STR90## including a pharmaceutically acceptable salt thereof wherein: R 1 is hydrogen or ##STR91## R 2 is lower alkyl, ##STR92## R 3 is hydrogen, lower alkyl, ##STR93## or --(CH 2 ) p -cycloalkyl; R 4 is hydroxy, lower alkoxy, ##STR94## R 10 is hydrogen, lower alkyl, cycloalkyl, or phenyl; R 11 is hydrogen, lower alkyl, lower alkoxy, or phenyl; n is an integer from 1 to 15; R 5 is lower alkyl, ##STR95## p is an integer from 1 to 4; m is zero or an integer from 1 to 4; R 6 is lower alkyl of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, hydroxy, Cl, Br, F, amino, --NH-lower alkyl of 1 to 4 carbons, --N(lower alkyl) 2 wherein lower alkyl is of 1 to 4 carbons, nitro or trifluoromethyl; r is an integer from 1 to 3 provided that r is more than one only if R 6 is hydroxy, methyl, methoxy, Cl, or F; and R 7 and R 8 are independently selected from the group consisting of hydrogen, lower alkyl, ##STR96##
Claim 2
Independent Claim
215 words
A method of relieving pain in a mammalian specie which comprises administering to said mammalian specie a composition containing an analgesically effective amount of a compound of the formula: ##STR90## including a pharmaceutically acceptable salt thereof wherein: R 1 is hydrogen or ##STR91## R 2 is lower alkyl, ##STR92## R 3 is hydrogen, lower alkyl, ##STR93## or --(CH 2 ) p -cycloalkyl; R 4 is hydroxy, lower alkoxy, ##STR94## R 10 is hydrogen, lower alkyl, cycloalkyl, or phenyl; R 11 is hydrogen, lower alkyl, lower alkoxy, or phenyl; n is an integer from 1 to 15; R 5 is lower alkyl, ##STR95## p is an integer from 1 to 4; m is zero or an integer from 1 to 4; R 6 is lower alkyl of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, hydroxy, Cl, Br, F, amino, --NH-lower alkyl of 1 to 4 carbons, --N(lower alkyl) 2 wherein lower alkyl is of 1 to 4 carbons, nitro or trifluoromethyl; r is an integer from 1 to 3 provided that r is more than one only if R 6 is hydroxy, methyl, methoxy, Cl, or F; and R 7 and R 8 are independently selected from the group consisting of hydrogen, lower alkyl, ##STR96##
Claim 3
Dependent Claim
97 words
The method of claim 1 wherein: R 1 is hydrogen, ##STR97## R 2 is ##STR98## R 3 is hydrogen, straight or branched chain alkyl of 1 to 4 carbons, ##STR99## m is one or two; R 6 is methyl, methoxy, Cl, F, hydroxy, amino or nitro; R 4 is hydroxy, methoxy, --NH 2 , or ##STR100## R 10 is hydrogen, straight or branched chain lower alkyl of 1 to 4 carbons, or cyclohexyl; R 11 is straight or branched chain lower alkyl of 1 to 4 carbons; and n is an integer from 1 to 9. PG,64
Claim 4
Dependent Claim
19 words
The method of claim 2 wherein: R 2 is benzyl; and n is an integer from 3 to 6.
Claim 5
Dependent Claim
19 words
The method of claim 3 wherein R 1 is hydrogen; R 3 is hydrogen; and R 4 is hydroxy.
Claim 6
Dependent Claim
9 words
The method of claim 4 wherein n is three.
Claim 7
Dependent Claim
9 words
The method of claim 4 wherein n is four.
Claim 8
Dependent Claim
9 words
The method of claim 4 wherein n is five.
Claim 9
Dependent Claim
9 words
The method of claim 4 wherein n is six.
Claim 10
Dependent Claim
26 words
The method of claim 2 wherein R 2 is benzyl; n is 9; R 1 is hydrogen; R 3 is hydrogen; and R 4 is hydroxy.
Claim 11
Dependent Claim
15 words
The method of claim 3 wherein R 1 is hydrogen; and R 4 is methoxy.
Claim 12
Dependent Claim
9 words
The method of claim 10 wherein n is three.
Claim 13
Dependent Claim
9 words
The method of claim 10 wherein n is five.
Claim 14
Dependent Claim
19 words
The method of claim 3 wherein: R 1 is ##STR101## R 3 is hydrogen; and R 4 is methoxy.
Claim 15
Dependent Claim
9 words
The method of claim 13 wherein n is 5.
Claim 16
Dependent Claim
21 words
The method of claim 3 wherein R 1 is hydrogen; R 3 is hydrogen; and R 4 is --NH 2 .
Claim 17
Dependent Claim
9 words
The method of claim 15 wherein n is 3.
Claim 18
Dependent Claim
26 words
The method of claim 2 wherein R 2 is benzyl; n is one; R 1 is hydrogen; R 3 is hydrogen; and R 4 is hydroxy.
Claim 19
Dependent Claim
26 words
The method of claim 2 wherein R 2 is benzyl; n is two; R 1 is hydrogen; R 3 is hydrogen; and R 4 is hydroxy.
Claim 20
Dependent Claim
26 words
The method of claim 2 wherein R 2 is benzyl; n is one; R 1 is hydrogen; R 3 is benzyl; and R 4 is hydroxy.
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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) | 1991-09-27 | 1992-03-28 | 1992-09-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-09-27 | 1996-03-28 | 1996-09-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-09-27 | 2000-03-28 | 2000-09-27 | $7700.00 | Window Closed / Lapsed |