DETAILED DESCRIPTION OF THE INVENTION The invention relates to biguanide salts.
In another aspect, the invention relates to pharmaceutical preparations which contain the aforementioned biguanide salts.
The biguanide salts of the invention are characterized by the formula ##STR4## wherein R.
sup.
1 is hydrogen, lower alkyl or lower alkenyl; R.
sup.
2 is lower alkyl, aryl, aryl-lower alkyl, or aryloxy-lower alkyl; or R.
sup.
1 and R.
sup.
2, taken together, are lower alkylene; R.
sup.
3 is hydrogen or a residue of the formula ##STR5## wherein R.
sup.
4 and R.
sup.
5 are hydrogen or a cation, or R.
sup.
4 is hydrogen and R.
sup.
5 is lower alkyl, or R.
sup.
4 and R.
sup.
5, taken together, are lower alkylene; and n is 1 to 2.
As used herein, the term "lower alkyl" denotes an alkyl group of 1-7 carbon atoms, for example, methyl, ethyl, propyl, isopropyl, butyl, isomers thereof, and the like.
The term "lower alkenyl" denotes an alkenyl group of 2-7 carbon atoms, for example, vinyl, allyl, and the like.
The term "aryl" denotes an aromatic hydrocarbon radical, for example, phenyl, which may contain one or more substituents, such as, for example, lower alkyl, lower alkoxy and halogen.
Halogen denotes chlorine, bromine, fluorine, and iodine; preferably chlorine.
As used herein, the term "cation" denotes a cation such as, Na.
sup.
+, K.
sup.
+ or NH.
sub.
4 .
sup.
+; Ca.
sup.
+.
sup.
+, Mg.
sup.
+.
sup.
+.
The term "lower alkylene" denotes an alkylene group having 2-7 carbon atoms such as ethylene, trimethylene, tetramethylene and penta methylene.
Compounds of formula I wherein R.
sup.
1 is hydrogen or lower alkyl, R.
sup.
2 is lower alkyl or phenyl-lower alkyl and R.
sup.
3 is hydrogen are preferred.
Examples of the compounds of formula I are: 1-phenethylbiguanide mono-dichloroacetate, 1-phenethylbiguanide bis-dichloroacetate, 1-n-butylbiguanide mono-dichloroacetate, 1-n-butylbiguanide bis-dichloroacetate, 1,1-dimethylbiguanide mono-dichloroacetate, 1,1-dimethylbiguanide bis-dichloroacetate, 1-pentylbiguanide mono-dichloroacetate, 1-pentylbiguanide bis-dichloroacetate, 1-isopentylbiguanide mono-dichloroacetate, 1-isopentylbiguanide bis-dichloroacetate, 1-benzyl-1-methylbiguanide mono-dichloroacetate, 1-benzyl-1-methylbiguanide bis-dichloroacetate, 1-benzyl-5-phosphorylbiguanide (benfosformin) mono di-chloroacetate, or the like
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