Basic derivatives of glutamic acid and aspartic acid as gastrin

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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540 1, 540477, 540478, 540480, 540481, 540546, 540582, 540585, 540597, 540602, 540606, 544 3, 544 60, 544 62, 544 63, 544124, 544128, 544131, 544132, 544142, 544152, 544153, 544359, 544360, 544363, 544373, 544376, C07D22120, C07D40106, C07D20954, A61K 3140

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057446075

ABSTRACT:
The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R.sub.1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, a 2(beta)naphthyl group, and heterocyclic, monocyclic and dicyclic groups; R.sub.2 is selected from heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group having from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group; and r is 1 or 2. The compounds have a potent antagonistic effect on gastrin and cholecystokinin and can be used to treat diseases which are linked to imbalances in the physiological levels of gastrin, cholecystokinin or other biologically active polypeptides related thereto.

REFERENCES:
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Konturek J W; Konturek S J; Kurek A; Bogdal J; Oleksy J; Rovati L CCK receptor antagonism by loxiglumide and gall bladder contractions in response to cholecystokinin, sham feeding and ordinary feeding in man. GUT, 30 (8) 1136-42, Aug. 1989.

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