Amino acid derivatives

Details Amino acid derivatives Amino acid derivatives

1991-04-02

1993-04-13

Bond, Robert T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514371, 514372, 514375, 514377, 514380, 548163, 548190, 548192, 548195, 548213, 548214, 548206, 548222, 548245, 548246, A61K 3154, C07D27782

Patent

active

052023400

ABSTRACT:
The compounds of the formula: ##STR1## (wherein R.sup.1 is hydrogen or alkyl; R.sup.2 is carbocyclic or heterocyclic ring, unsubstituted or substituted by R.sup.3 s; R.sup.3 is halogen, trihalomethyl, hydroxy, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfornyl, cyano, nitro, or group of the formula: --C.sub.6 H.sub.4 --R.sup.4, --NR.sup.5 R.sup.6, --CO--R.sup.7, --COOR.sup.8, --CONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6 or --NHCO--R.sup.7, in which R.sup.4 is hydrogen, halogen, trihalomethyl, hydroxy, alkyl or alkoxy, R.sup.5 and R.sup.6 are each hydrogen or alkyl, R.sup.7 is alkyl or phenyl substituted by R.sup.4 and R.sup.8 is hydrogen or alkyl; Z is hydrogen or group of the formula: --COR.sup.9, ##STR2## in which R.sup.9 is alkyl or phenyl substituted by R.sup.10, in which R.sup.10 is hydrogen, halogen, trihalomethyl, alkyl or alkoxy, R.sup.11 and R.sup.12 are each hydrogen, alkyl or phenyl substituted by R.sup.10, or R.sup.11 and R.sup.12 together represent alkylene and p is 1 or 2; A is phenyl or cycloalkyl substituted by R.sup.13 in which R.sup.13 is hydrogen, halogen, trihalomethyl, alkyl or alkoxy; and m is zero and n is 1 to 4 or n is zero and m is 1 to 4; and non-toxic salts thereof have inhibitory effect on enkephalinase, and therefore, are useful as analgesic, antianxiety and anticonvulsant.

REFERENCES:
patent: 4401677 (1983-08-01), Greenberg et al.
Nature, vol. 258, Dec. 18, 1975, Hughes eta l., pp. 577-579 "Identification of Two Related Pentapeptides from the Brain . . . ".
Nature, vol. 276, Nov. 30, 1978, pp. 523-526.
Nature, vol. 288, Nov. 20, 1990, pp. 286-288 Roques et al., "The Enkephalinase Inhibitor Thiorphan Shows . . . ".
Derwent Patent Abstract No. 84-202873/33 (Corresponding to EP-A-115997).
Derwent Patent Abstract No. 82006 D/45 (Corresponding to EP-A-38758).

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