Tetrahydro-pyrido-indoles as cholecystokinin and gastrin antagon

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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546 85, 546 86, 546 87, C07D47104, A61K 3144

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active

051623366

ABSTRACT:
Disclosed are tetrahydro-pyrido-indoles having the general formula ##STR1## which are antagonists towards the neuropeptides cholexystokinin and gastrin processing valuable activities for the treatment of cholecystokinin or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems and their pharmaceutical compositions and processes for their preparation.

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patent: 4847248 (1989-07-01), Freidinger et al.
Coutts, R. T. et al., Heterocycles 22(1), 131-142 (1984) "Some 3-Carboxamides of .beta.-Carboline and Tetrahydro-.beta.-Carboline".
Cain, M., et al., J. Med. Chem. 25, 1081 (1982) ".beta.-Carbolines: Synthesis and Neurochemical and Pharmacological Actions on Brain Benzodiazepine Receptors".
Itonaga, M., et al., Japan. J. Pharmacol. 46, 319-324 (1988) "Cholecystokinin Antagonism by .beta.-Carboline Esters in the Central Nervous System in Mice".
Hahne, W. F., et al., Proc. Natl. Acad. Sci. USA 78(1), 6304-6308 (1981) "Proglumide and benzotript: Members of a Different Class of Cholecystokinin Receptor Antagonists".
Evans, B. E., et al., J. Med. Chem. 1988, 31, 2235-2246 "Methods for Drug Discovery: Development of Potent, Selective, Orally Effective Cholecystokinin Antagonists".
Parsons, W. H., et al., J. Med. Chem. 1989, 32, 1681-1685 "Cholecystokinin Antagonists, Synthesis and Biological Evaluation of 3-Substituted Benzolactams".

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