Derivatives of D-glutamic acid and D-aspartic acid

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546156, C07D21522, A61K 3147

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active

049719785

ABSTRACT:
A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are substituents; R.sub.6 is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is a bond, an alkylene group, an alkenylene group, an alkadienylene group or a heteroatom containing linking group; D is a substituted acyl group or tetrazolyl; Z is CO, C(S) or S(O).sub.2 ; Ar is a heterocyclic group; and n is 1 to 3.
Also disclosed are a composition and a method for antagonizing CCK, a composition and method for treating or preventing gastrointestinal, central nervous, appetite regulating and pain regulating systems, a composition and method for treating or preventing hyperinsulinemia, methods of making the compounds and intermediates useful in making the compounds.

REFERENCES:
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F. Makovec et al., Arzneim.-Forsch./Drug Res. 35(II), 1048 (1985) "New Glutaramic Acid Derivatives with Potent Competitive and Specific Cholecystokinin-antagonistic Activity".
F. Makovec et al., Arzneim-Forsch./Drug Res. 36(I), 98 (1986) "Differentiation of Central & Peripheral Cholecystokinin Receptors by New Glutaramic Acid Derivatives with Cholecystokinin-antagonistic Activity".
J. Regan et al., Eur. J. Pharmacol. 144, 241 (1987) "Fasting and L-364,718 Prevent Cholecystokinin-induced Elevators of Plasma Insulin Levels".
L. Rossetti et al., Diabetes 36, 1212 (1987) "Physiological Role of Cholecystokinin in Meal.varies.Induced Insulin Secretion in Conscious Rats-Studies with L364,718, A Specific Inhibitor of CCK-Receptor Binding".

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