Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1992-10-29
1994-06-28
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540504, 540505, 540509, 540510, 540512, 540513, 540514, 540572, 540573, A61K 3155, C07D24324, C07D24322, C07D24316
Patent
active
053247264
ABSTRACT:
Benzodiazepine analogs of the formula: ##STR1## wherein: R.sup.3 is ##STR2## --NH(CH.sub.2).sub.2 --.sub.3 NHCOR.sup.7, ##STR3## or --X.sup.11 NR.sup.18 SO.sub.2 (CH.sub.2).sub.q R.sup.7 ; R.sup.7 is O,S,HH, or NR.sup.15 with the proviso that X.sup.7 can be NR.sup.15 only when R.sup.1 is not H.
are disclosed which are antagonists of gastrin and cholecystokinin (CCK) with enhanced aqueous solubility and have properties useful in the treatment of disorders of gastric secretion, appetite regulation, gastrointestinal motility, pancreatic secretion, and dopaminergic function, as well as in treatment producing potentiation of morphine and other opiate analgesics.
REFERENCES:
patent: 4820834 (1991-04-01), Evans et al.
Bradwejn, et al., Enhanced Sensitivity to Cholecystokinin Tetrapeptide in Panic Disorder, Soc. Neurosci. Abstr. 14(1), p. 291, (1988).
de Montigny, Cholecystokinin Tetrapeptide Induces Panic Attacks in Healthy Volunteers, Soc, Neurosci. Abstr. 14(1), p. 291, (1988).
Bradwejn, et al., Benzodiazepines Antagonize Cholecystokinin-Induced Activation of Rat Hippocampal, Neurones, Nature 312, p. 22, (1984).
de Montigny, Cholecystokinin Tetrapeptide Induces Panic-like Attacks in Healthy Volunteers, Arch. Gen. Psychiatry, 46, pp. 511-517, (1989).
Dourish, et al., Enhancement of Morphine Analgesia and Prevention of Morphine Tolerance in the Rat by the Cholecystokinin Antagonist L-364, 718 Pharm. 147, pp. 469-472, (1988).
Bouthillier, et al., Long-term Benzodiazepine Treatment Reduces Neuronal Responsiveness to Cholecystokinin: an Electrophysiological Study in the Rat, Eur. Jour. Pharm. 151, No. 1, pp. 135-138, (1988).
O'Neill et al. Morphine Induced Analgesia in the Rat Paw Pressure Test is Blocked by CCk and Enhanced by the CCK Antogonist MK-329, Neuropharmacology 28, No. 3, pp. 243-247 (1989).
Chang, et al., Biochemical and Pharmacological Characterization of an Extremely Potent and Selective Nonpeptide Cholecystokinin Antagonist, Proc. Natl. Sci., 83, pp. 4923-4926 (1986).
Bock Mark G.
Evans Ben E.
Freidinger Roger M.
Berch Mark L.
Daniel Mark R.
DiPrima Joseph F.
Merck & Co. , Inc.
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