Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1998-04-15
1999-08-31
Cook, Rebecca
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514910, A61K 3113
Patent
active
059454555
DESCRIPTION:
BRIEF SUMMARY
This is a 371 of PCT/GB96/01191 filed May 17, 1996.
FIELD OF THE INVENTION
The present invention relates to the use of amine and amidine containing compounds such as galegine ((3-methyl-2-butenyl) guanidine) and related substituted amine and amidine containing compounds, as agents for reducing weight in mammals.
BACKGROUND OF THE INVENTION
Being obese or over-weight is a common problem. Aggravating factors may be depression or other psychosocial problems. Patients receiving drug treatment are also often predisposed to weight gain.
Obesity can be controlled to some extent by strict dieting, however, dieting is seldom successful in the long term as the subject may find it difficult to stick to a dieting regime.
Obesity can aggravate certain medical conditions, and is a risk factor for heart disease.
Galegine is an example of an amidine group containing compound which is known to have hypoglycaemic effect. It has now been unexpectedly found that When galegine is administered to a mammal, a weight reduction effect is observed.
SUMMARY OF THE INVENTION
One aspect of the present invention provides the use of a compound of formula (I): ##STR1## wherein R is selected from the group phenyl and ##STR2## where R.sup.1, R.sup.2 and R.sup.3 are independently selected from the group H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, and C.sub.2-6, alkynyl; C.sub.2-6 alkenyl, and C.sub.2-6 alkynyl; ##STR3## wherein R.sup.6 is selected from the group H, NH.sub.2 and C.sub.1-6 alkyl; n is a whole integer from 0 to 6; and physiologically acceptable salts thereof in the manufacture of a composition for weight reduction, with the ##STR4## and n.dbd.O, R is not phenyl and when R' is ##STR5## and n is 1, 2, 3 or 4 and R.sup.4 and R.sup.5 are both H, R is not phenyl.
Preferably R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently selected from the group H, C.sub.1-2 alkyl, C.sub.2-3, alkenyl and C.sub.2-3 alkynyl; ##STR6## wherein R.sup.6 is selected from the group NH.sub.2, H and C.sub.1-2 alkyl; and n is a whole integer from 0 to 2; and physiologically acceptable salts thereof.
In a preferment, the invention provides the use of a compound of formula (II) in the manufacture of a composition for weight reduction, ##STR7## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl and NH.sub.2 ; and n is from 0 to 6; and physiologically acceptable salts thereof.
Compounds of formula (I) or formula (II) hereafter are referred to as "weight reducing agent". Another aspect of the present invention provides a method of reducing weight in a subject which comprises administering to a subject an effective non-toxic amount of a weight reducing agent of formula (I). In a preferment, the effective non-toxic amount of weight reducing agent is of formula (II).
A further aspect of the present invention is the suppression of appetite i.e. food intake in a subject generically predisposed to obesity. Thus it has been found that food intake is suppressed in genetically obese subjects, but does not show a longterm suppression in a normal subject.
BRIEF DESCRIPTION OF THE DRAWINGS
The weight reduction effect demonstrated by weight reducing agents of the present invention is unexpected since reduction in glucose levels caused by known hypoglycaemic compounds does not necessarily lead to weight reduction and may in fact lead to increase in weight.
Preferably, R.sup.1 and R.sup.2 of formula (II) are both C.sub.1-6 alkyl, or C.sub.2-6 alkenyl or C.sub.2-6 alkynyl, particularly methyl or ethyl; ethenyl or methenyl; methynyl or ethynyl; or mixtures thereof. Generally, R.sup.3 of formula (II) is hydrogen or C.sub.1-6 alkyl. R.sup.4 and R.sup.5 of formula (II) are preferably hydrogen or C.sub.1-6 alkyl; and n is usually 1 or 2.
A particularly preferred compound is galegine, (3-methyl-2-butenyl) guanidine, where R.sup.1 and R.sup.2 are both methyl, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, and n is unity.
Also included as An aspect of the invention are novel
REFERENCES:
CA103:213827, Balogh, Abstract for HU 35160, 1985.
"The Merck Index, 11th Edition" 1989, Merck & Co., Inc., Monograph 616: Amphetamine, p. 92.
Hoppe-Seyler's Z. Physiol. Chem., vol. 353, No. 4, Apr. 1972, pp. 535-539, G. Weitzel et al: "Antilipolytische Wirksamkeit von Arginylverbindungen".
Hoppe-Seyler's Z. Physiol. Chem., vol. 352, No. 12, Dec. 1971, pp. 1617-1630, G. Weitzel et al: "Indulinahnliche Aktivitat von Arginylverbinsungen in vitro".
Eur. J. Clin. Invest. vol. 3, No. 3, 1973, p. 208, K.G.M.M. Alberti et al: "Mechanism of Action of the Monoguanidine Hypoglycaemic Agents, Galegine and Agmatine".
Fitoterapia, vol. 65, No. 5, 1994, pp. 423-426, K. Pundarikakshudu et al: "Studies on the hypoglycaemic activity of Galega officinalis (goat's rue)" .
Furman Brian Laurence
Gray Alexander Irvine
Palit Piali
Waigh Roger David
Cook Rebecca
University of Strathclyde
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