Patent EP0038046A2 successfully refreshed from Google Patents.
EP0038046A2
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EP
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Pharmaceutical amides, and preparation, formulations and use thereof
Assignee: Wellcome Foundation Ltd
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Filing: 1981-04-10
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Granted: —
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Expires: 2001-04-10
Abstract
Abstract Compounds of the general formula (wherein X is a group capable of functioning as a ligand for a zinc ion; Ph ist a phenyl group which is optionally substituted by one or more substituents selected from halo and nitro radicals; Y is a group of formula: where R' is hydrogen or methyl; R 2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is a group of formula -OR 3 or -NR 4 R 5 where R 3 , R 4 and R 5 are each hydrogen or alkyl of 1 to 4 carbon atoms and R' can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl) and pharmacologically acceptable basic salts thereof. These compounds have an advantageous enkephalinase inhibitory activity which renders the compounds of use in medical therapy for example when it is desired to prolong and/or potentiate in a mammal the effects of enkephalins of either endogenous or exogenous origin including in the later case synthetic enkephalin analogues.
Inventors
- 👤 Samuel Wilkinson
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-30 07:17
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; A; A61; A61P; A61P25/00
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
128 words
1) Compounds of the general formula (wherein X is a group capable of functioning as a ligand for a zinc ion; Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo and nitro radicals; Y is a group of formula:- where R 1 is hydrogen or methyl; R 2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is a group of formula -OR 3 or - NR 4 R 5 where R 3 , R 4 and R 5 are each hydrogen or alkyl of 1 to 4 carbon atoms and R 3 can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl) and pharmacologically acceptable basic salts thereof.
Claim 2
Dependent Claim
128 words
1) Compounds of the general formula (wherein X is a group capable of functioning as a ligand for a zinc ion; Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo and nitro radicals; Y is a group of formula:- where R 1 is hydrogen or methyl; R 2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is a group of formula -OR 3 or - NR 4 R 5 where R 3 , R 4 and R 5 are each hydrogen or alkyl of 1 to 4 carbon atoms and R 3 can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl) and pharmacologically acceptable basic salts thereof.
Claim 3
Dependent Claim
11 words
2) Compounds as claimed in claim 1 wherein X represents carboxyl.
Claim 4
Dependent Claim
19 words
3) Compounds as claimed in claim 1 wherein X represents mercapto or alkanoylthio having 2 to 5 carbon atoms.
Claim 5
Dependent Claim
15 words
4) Compounds as claimed in any of the preceding claims wherein Ph is unsubstituted phenyl.
Claim 6
Dependent Claim
23 words
5) Compounds as claimed in any of the preceding claims wherein Y is a group of formula (in either the D- or L-configuration).
Claim 7
Dependent Claim
24 words
6) Compounds as clained in any of claims 1 to 4 wherein Y is a group of formula:- (in either the D- or L-configuration).
Claim 8
Dependent Claim
22 words
7) Compounds as claimed in any of the preceding claims wherein Z is a group of formula -OH or -NH 2 .
Claim 9
Dependent Claim
146 words
8) A process for the preparation of a compound of formula I (as defined in claim 1) or a pharmacologically acceptable basic salt thereof which comprises reacting a compound of formula (wherein Ph is as defined in claim 1; X 1 is a group X (as defined in claim 1) or a functionally protected derivative thereof; Q is carboxyl or a functionally activated derivative thereof; and Q 1 and Q 2 are both hydrogen or together form a bond) with a compound of formula (wherein Y is as defined in claim 1; and Z is a group Z (as defined in claim 1) or a functionally protected derivative thereof);followed (when Q 1 and Q 2 together form a bond) by selective reduction of the said bond and, as appropriate, by deprotection of the product into the compound of formula (I) or pharmacologically acceptable basic salt thereof.
Claim 10
Dependent Claim
32 words
9) Pharmaceutical formulations comprising a therepeutically effective amount of a compound of formula I (as defined in claim 1) or a pharmacologically acceptable basic salt thereof together with an acceptable carrier therfor.
Claim 11
Dependent Claim
17 words
10) Formulations as claimed in claim 9 adapted for oral, rectal, nasal, topical, vaginal or parenteral administration.
Claim 12
Dependent Claim
19 words
11) Formulations as claimed in claim 10 in the form of tablets, capsules, cachets or injectable solutions or suspensions.
Claim 13
Dependent Claim
24 words
12) Compounds of formula I (as defined in claim 1) and pharmacologically basic salts thereof, for use in the therapeutic treatment of a mammal.
Claim 14
Dependent Claim
24 words
13) Compounds of formula I (as defined in claim 1) and pharmacologically basic salts thereof, for use in the therapeutic treatment of a human.
Claim 15
Dependent Claim
30 words
14) Compounds of formula I (as defined in claim 1) and pharmacologically basic salts thereof, for use in the prolongation and/or potentiation in a mammal of the effects of enkephalins.
Claim 16
Dependent Claim
35 words
15) Compounds of formula I (as defined in claim 1) and pharmacologically basic salts thereof, for use in the treatment of a mammal for a condition where an agent with a morphine-like effect is indicated.
References Cited (Backward Citations)
No citation records indexed.
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