Polyamines and anti-diarrheal and gastrointestinal anti-spasmodi

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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514867, 544296, A61K 31505, C07D40308

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active

053937570

ABSTRACT:
Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms;
R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;
R.sub.7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;
m is an integer from 3 to 6, inclusive; and
n is an integer from 3 to 6, inclusive; or
(IV) a salt thereof with a pharmaceutically acceptable acid; and a pharmaceutically acceptable carrier therefor. Methods of treatment utilizing the composition are also disclosed.

REFERENCES:
patent: 4013507 (1977-03-01), Rembaum
patent: 4507321 (1985-03-01), Raisfeld
patent: 4529729 (1985-07-01), Regnier et al.
patent: 5155137 (1992-10-01), Keefer et al.
Weinstock et al, `Synthesis of New Polyamine Derivatives for Cancer Chemotherapeutic Studies`, Journal Phar. Sci. vol. 70, No. 8, Aug. 1981.
Chantrapromma et al, `Chemistry of Naturally Occurring Polyamines`, 1981, Tetrahedron Letters., 22 (1), 23-24.
Tansy et al, `Spermine and Spermidine as Inhibitors of Gastro Intestinal Motor Activity`, 1982, Surg. Gynecol Obstet 154 (1), 74-80.
Aihara et al, `Polyamine Inhibition of Gastric Ulceration and Secretion in Rats, 1983, Biochem Pharmacol 32 (11), 1733-1736.
Ray et al `Polyamines are Inhibitors of Gastric and Secretion` Proc Natl Acad Sci USA 79 (5), 1982, 1448-1452.

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