Use of amino hydrogenated quinazoline compounds and derivatives

Details Use of amino hydrogenated quinazoline compounds and derivatives Use of amino hydrogenated quinazoline compounds and derivatives

1996-05-21

1998-12-08

MacMillan, Keith D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

A61K 31505

Patent

active

058469753

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention is concerned with amino hydrogenated quinazoline compounds and derivatives thereof, particularly their new application for causing humans to abstain from drug dependence on alkaloids and synthetic non-amino acid nitrogen.


BACKGROUND OF THE INVENTION

The research of amino-hydro quinazoline and its derivatives originated from the knowledge for crystal tetrodotoxin(TTX).
TTX is a well-known amino-perhydro quinazoline with its molecular formula as C.sub.11 H.sub.17 N.sub.3 O.sub.8 and its molecular weight 319.27.The chemical structure for TTX is shown as following: ##STR1## TTX has been found in many puffers up to one hundred, such as tetrodontidae, diodontidae, molidae, triodontidae and other families of puffer. These puffers are classified as hard-fish sub-class, fish class. Tissues of these puffers rich in TTX include ovary, liver, skin, and gastrointestinal. Methods of TTX extracting from these tissues have been reported by T. Goto et al. (Tetrohedron, 21, 2059. 1965) and E. F. Murtha (Expte. Therap., 122, 246. 1958). For TTX synthesis method, see Y. Kishi, et al., J. Am. Chem. Soc., 94(26), 9217, 9219. 1972. Later studies revealed that TTX and its derivatives could be detected in amphibians like salamanders, in mollusks like octopus, shellfish, and snails, in arthropods like crabs, limulus, starfish and in plants like red algae. Very recently, it was found that TTX was also produced by some geneses bacteria such as vibros, pseusdomona, streptomyces josamycetinus and etc. TTX is an extreme poison whose toxicity is 1,250 times more than that of sodium cyanide. It was estimated that dosage of TTX as little as 0.5 mg could bring death of a person with 70 kg body weight. In another report, subcutaneous injection of 300 .mu.g TTX was enough to put death of a man with 50 kg body weight.
Although TTX has been long recognized, its clinical indications limit in following aspects:
(1). TTX produces pronounced analgesic effect on various pains caused by burning, trauma, injuries from falls, fractures, contusions and strains, especially for neuragia, myalgia and arthralgia. Unless the diseases are inveterate, TTX is a powerful analgesic.
(2). Local anesthesia
TTX can be used as local anesthetic and is ten thousand-fold more powerful than those commonly used local narcotics (Kao CY and Fulman FA, J. Pharmacol., 140, 31-40, 1965). The combined preparations of TTX with widely-used local anesthetics have been published in U.S. Pat. No. 4,022,899 and U.S. Pat. No. 4,029,793.
(3). As a potent analgesic for late cancer patients. TTX exerted satisfactory effect of pain relieving on cancer pain, and no drug
(1) As antipruritic for winter skin itch, prurigo, thylacitis, itch mite and sarcoptic mite. It also facilitated recovery from these dermatosises.
(2) As asthma and pertusis abirritant.
(3) As enuresis inhabitant.
TTX is an effective antispasmodic for myospasm, gastrospasm and other kinds of spasms, particularly for tetanospasm.
TTX produced strong depressing effect on blood pressure, for example, administration of 2-3 .mu.g/kg TTX to the cat (i.v.) could abruptly lower its arterial pressure as much as two thirds of the normal value, and the duration of it action is fairly short, these characteristics possibly make it useful in first aid of hypertension crisis in the clinic.
(1) TTX was reportedly effective on pain relieving for lepers (Nomiyama S: Fed. Proc.31:1 117,1972)
(2) Due to its function of congestion, TTX can elicit therapeutic effect on man's impotence and woman's asexuality.
Up to now, no applications of TTX, amino hydrogenated quinazoline compounds and derivatives thereof in abstaining from drug dependence have been reported in prior art. Here, the conception of drug dependence refers to such a physical (or physiological) state of subjects as we call it, withdrawal syndrome, which is produced by everlasting interaction between the body and drug, the symptoms include perspiration, lacrimation, yawn, rigor, goose flesh, mydriasis, vomiting, diarrhea, achycadia, hypertension, ins

REFERENCES:
patent: 3898339 (1975-08-01), Adams et al.
patent: 5474547 (1995-12-01), Aebisher et al.
Y. Kishi et al., J. Am. Chem. Soc., 94:26, pp. 9217-9221 (Dec. 27, 1972).
T. Goto et al., Tetrahedron, vol. 21, pp. 2059-2088 (1965).
E. Murtha et al., Journal of Pharmacology and Experimental Therapeutics., vol. 122, pp. 247-254 (1958).
Chemical Abstracts AN 1977: 268, Fredrikson et al, 1976.

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