EP0136883A2
Expired / Lapsed
EP
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Enkephalinase inhibitors
Assignee: ER Squibb and Sons LLC
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Filing: 1984-09-27
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Granted: —
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Expires: 2004-09-27
Abstract
Abstract New mercaptoalkanoyl and acylmercaptoalkanoyl compounds of the formula wherein R 1 , R 2 , R 3 and R 4 are as defined herein and 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
EP
Data Source
google_patents
Last Synchronized
2026-11-06 01:01
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/16
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
228 words
A compound of the formula: including a pharmaceutically acceptable salt thereof wherein: R 1 is hydrogen or R 3 is hydrogen, lower alkyl, or -(CH 2 ) p -cycloalkyl; R 4 is hydroxy, lower alkoxy, n is an integer from 1 to 15; R 5 is lower alkyl, 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, -N H -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; R 10 is hydrogen, lower alkyl, cycloalkyl or phenyl; R 11 is hydrogen, lower alkyl, lower alkoxy, or phenyl; and R 7 and R 8 are independently selected from the group consisting of hydrogen, lower alkyl, or R 7 and R 8 join together with the N-atom to form a ring of the formula wherein q is zero or one, A is CH-R 9 , oxygen, or N-R 9 , and R 9 is hydrogen or lower alkyl of 1 to 4 carbons.
Claim 2
Dependent Claim
228 words
A compound of the formula: including a pharmaceutically acceptable salt thereof wherein: R 1 is hydrogen or R 3 is hydrogen, lower alkyl, or -(CH 2 ) p -cycloalkyl; R 4 is hydroxy, lower alkoxy, n is an integer from 1 to 15; R 5 is lower alkyl, 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, -N H -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; R 10 is hydrogen, lower alkyl, cycloalkyl or phenyl; R 11 is hydrogen, lower alkyl, lower alkoxy, or phenyl; and R 7 and R 8 are independently selected from the group consisting of hydrogen, lower alkyl, or R 7 and R 8 join together with the N-atom to form a ring of the formula wherein q is zero or one, A is CH-R 9 , oxygen, or N-R 9 , and R 9 is hydrogen or lower alkyl of 1 to 4 carbons.
Claim 3
Dependent Claim
93 words
A compound of Claim 1 wherein: R 1 is hydrogen, R 2 is R 3 is hydrogen, straight or branched chain alkyl of 1 to 4 carbons, or m is one or two; R 6 is methyl, methoxy, Cl, F, hydroxy, nitro, or amino; R 4 is hydroxy, methoxy, -NH 2 , or 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.
Claim 4
Dependent Claim
16 words
A compound of Claim 1 or 2 wherein n is an integer from 3 to 6.
Claim 5
Dependent Claim
11 words
A compound of Claim 1 or 2 wherein n is one.
Claim 6
Dependent Claim
11 words
A compound of Claim 1 or 2 wherein n is 2.
Claim 7
Dependent Claim
11 words
A compound of Claim 1 or 2 wherein n is three.
Claim 8
Dependent Claim
11 words
A compound of Claim 1 or 2 wherein n is four.
Claim 9
Dependent Claim
11 words
A compound of Claim 1 or 2 wherein n is five.
Claim 10
Dependent Claim
11 words
A compound of Claim 1 or 2 wherein n is six.
Claim 11
Dependent Claim
11 words
A compound of Claim 1 or 2 wherein n is nine.
Claim 12
Dependent Claim
15 words
A compound of any one of Claims 1 to 10 wherein R 1 is hydrogen.
Claim 13
Dependent Claim
14 words
A compound of any one of Claims 1 to 10 wherein R 1 is
Claim 16
Dependent Claim
15 words
A compound of any one of Claims 1 to 12 wherein R 2 is benzyl.
Claim 17
Dependent Claim
15 words
A compound of any one of Claims 1 to 13 wherein R 3 is hydrogen.
Claim 18
Dependent Claim
15 words
A compound of any one of Claims 1 to 13 wherein R 3 is benzyl.
Claim 19
Dependent Claim
15 words
A compound of any one of Claims 1 to 15 wherein R 4 is hydroxy.
Claim 20
Dependent Claim
16 words
A compound of any one of Claims 1 to 15 . wherein R 4 is methoxy.
Claim 21
Dependent Claim
17 words
A compound of any one of Claims 1 to 15 wherein R 4 is -NH 2 .
Claim 22
Independent Claim
35 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 any one of the preceding Claims 1 to 18.
References Cited (Backward Citations)
No citation records indexed.
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