Optically-active derivatives of (R) 5-pentylamino-5-oxopentanoic

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...

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562448, 562450, 562449, A61K 31195

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active

053915747

ABSTRACT:
There are described optically active derivatives of (R) 5-pentylamino-5-oxopentanoic acid and their pharmaceutically acceptable salts, having antagonistic activity towards cholecystokinin, and with the formula: ##STR1## in which R.sub.1 is selected from the groups 2-naphthyl, 3,4-dichlorophenyl and 3,4-dimethylphenyl and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 carbon atoms, and in which the substituents on the central chiral group (marked with an asterisk in Formula (I)), have the R (rectus) conformation.

REFERENCES:
patent: 4880938 (1989-11-01), Freidinger
Makovec et al., Chem. Abst., vol. 106, #149938b (1987).
Makovec et al., Chem. Abst., vol. 107, #198,929 (1987).
Makovec et al., Chem. Abst., vol. 105, #91,509 (1986).
Makovec et al., Chem. Abst., vol. 103, #99,103r (1985).
Kotone et al., Chem. Abst., vol. 81, #121,028 (1974).
European Journal of Medicinal Chemistry, vol. 21, No. 1, 1986, pp. 9-20.
Arznemittel Forschung, vol. 35, No. 7, 1985, pp. 1048-1051.
Organic Chemistry, 3rd Edition, Morris & Boyd, p. 127.

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