Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1993-11-17
1996-02-20
Griffin, Ronald W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544367, 514906, 514968, A61K 31535
Patent
active
054929113
DESCRIPTION:
BRIEF SUMMARY
The invention relates to the use of linsidomine and its pharmacologically compatible salts for the treatment of erectils dysfunctions.
About 5% of men in the 40th year of life and 20% in the 60th year of life suffer from an erectils dysfunction. The loss of potency is a shock to the man's, in particular the young man's, view of himself in physical, emotional and social terms. Patients with chronic erectils dysfunction are unsure of their sexuality and personality and should be regarded as ill.
Disturbances of potency, which were mainly attributed to psychological causes until the 1970s, have been treated, besides psychotherapeutic measures, by use of testosterones or of aphrodisiacs of disputed value. Not until the physiology of the process of erection was investigated was it found that in more than 60% of patients the erection impairments are brought about by organic causes, with contributions from autonomic efferences from the parssympathetic portion of the sacral region of the spinal cord, neurotransmitters, dilatation of the penis arteries, relaxation of the cavernous spaces and constriction of the veins. In more than 70% of cases there is causal involvement of vascular factors such as pathological arterial blood supplies or abnormally increased venous outflow from the cavernous spaces. Neurogenic disturbances are involved to the extent of about 20%.
Oral therapy of these organic dysfunctions with vasoactive substances such as yohimbine, phenoxybenzamine, terbutaline, bethanechol, levodopa, verapamil or theophylline has proved unsuccessful. Besides the use of prosthetic implants or revascularization operations, success has been achieved with intracavernous injection of papaverine (Virag, Lancet, 2, 938, 1982), the .alpha.-receptor blocker phenoxybenzamine (Brindley, Br. J. Psychiatr., 143, 332, 1983) and a combination of papaverine and the d-receptor blocker phentolemine (Stief, Urologe A, 25, 63, 1986). The latter therapeutic method can be carried out by the patient himself and is also called cavernous body autoinjection therapy (CBAT).
However, the disadvantages which have emerged are in some cases undesired prolonged erection with the risk of priapism on use of papaverine, undesired painfulness on use of phenoxybenzamine and a possible carcinogenicity of this compound.
In addition, in an animal experiment (Cynomolgus) with 1-2 intracavernous injections of papaverine each week for 12 months there was found to be extensive fibrosis of wide parts of the cavernous body, which would lead to extremely adverse long-term results in humans because erection is no longer possible when there is fibrosis of the corpus cavernosum.
The use of acetylcholine is, while the erection is only short-lasting, associated with severe systemic side effects, and the injection of prostaglandin E.sub.1 is refused by patients because the pain is too great.
The object of the invention was therefore to develop and produce medicaments for the treatment of neurogenic, arterial, neurotransmitter-related, myopathic, venous and psychogenic erectile dysfunctions in mammals, preferably in humans, without the said side effects. It has now been found, surprisingly, that intracavernous injection of linsidomine hydrochloride leads to erection with complete rigidity.
The invention therefore relates to the use of 3-morpholinosydnone imine (linsidomine, SIN-1) and its pharmacologically compatible salts, preferably linsidomine hydrochloride, for the production of medicaments for the treatment of erectile dysfunctions in mammals, preferably in humans, and to the treatment of erectile dysfunctions in mammals and humans.
The invention also relates to the use of linsidomine which has been converted, for pharmaceutical reasons, into the pharmacologically compatible salts. The salts are obtained in a conventional way, by neutralizing the base with inorganic or organic acids.
Suitable inorganic acids are, for example, hydrochloric acid, sulfuric acid, phosphoric acid or hydrobromic acid, and of organic acids are, for example, carboxylic, sulfo or sulfo
REFERENCES:
patent: 3312690 (1967-04-01), Masuda et al.
patent: 4421754 (1983-12-01), Hidaka et al.
patent: 4687771 (1987-08-01), Gamble et al.
patent: 4801587 (1989-01-01), Voss et al.
patent: 4840952 (1989-06-01), Gamble et al.
patent: 4931445 (1990-06-01), Goldstein et al.
patent: 5059603 (1991-10-01), Rubin
patent: 5110820 (1992-05-01), Fujikura et al.
patent: 5145852 (1992-09-01), Virag
patent: 5155109 (1992-10-01), Schonafinger et al.
patent: 5214030 (1993-05-01), Stief
patent: 5236904 (1993-08-01), Gerstenberg et al.
patent: 5256652 (1993-10-01), El-Rashidy
patent: 5267963 (1993-12-01), Bachynsky
patent: 5298496 (1994-03-01), Vikmon et al.
The FASEB Journal, vol. 5, No. 4, Mar. 1991, 2 pages, No. 175.
The Physiological Society, The Journal of Physiology, vol. 438, 1991, p. 103 p.
Acta Physiologica Scandinavica, vol. 141, No. 3, Mar. 1991, 3 pages, pp. 441-442.
Characterization of Inhibitory Neurotransmission in the Isolated Corpus Cavernosum from Rabbit and Man. F. Homquist, et al. pp. 109-130 Lund University doctoral dissertation 20 Sep. 1991.
The Journal of Urology, vol. 9, No. 4, 1991, 4 pages, pp. 237-239.
Schwellkorper-Autoinjektionstherapie (SKAT): erste Erfahrungen bei erektiler Dysfunktion, C. G. Stief et al., 5 pages, pp. 63-66.
Blood Vessels, Form and Functio nof Blood and Lymphatic Vessels, Mechanisms of Vasodilatation, Jul. 5-7, 1989, 14 pages, pp. 282-294.
The Journal of Urology, Aua Eighty-Seventh Annual Meeting, May 10-14, 1992, 2 pages, No. 205.
International Search Report, Aug. 10, 1992.
Griffin Ronald W.
Stief Christian
LandOfFree
Linsidomine for the treatment for erectile dysfunctions does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Linsidomine for the treatment for erectile dysfunctions, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Linsidomine for the treatment for erectile dysfunctions will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1356013