Guanidine derivatives

Details Guanidine derivatives Guanidine derivatives

1998-06-26

2000-01-25

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514616, 544169, 544382, 548567, 564139, 564156, A37G 2530

Patent

active

060179171

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to new guanidine derivatives.
One object of this invention is to provide the new and useful guanidine derivatives and pharmaceutically acceptable salts thereof which possess a strong inhibitory activity on Na.sup.+ /H.sup.+ exchange in cells.
Another object of this invention is to provide processes for preparation of the guanidine derivatives and salts thereof.
A further object of this invention is to provide a pharmaceutical composition comprising said guanidine derivatives or a pharmaceutically acceptable salt thereof.
Still further object of this invention is to provide a use of said guanidine derivatives or a pharmaceutically acceptable salt thereof as a medicament for the treatment and/or prevention of cardiovascular diseases, cerebrovascular diseases, renal diseases, arteriosclerosis, shock and the like in human being and animals.


BACKGROUND ART

Some guanidine derivatives having pharmaceutical activities such as inhibitory activity on Na.sup.+ /H.sup.+ exchange in cells have been known as described in WO 94/26709.


DISCLOSURE OF INVENTION

The object guanidine derivatives of the present invention are novel and can be represented by the following general formula (I): ##STR2## wherein R.sup.1 is [di(lower)alkylamino](lower)alkyl, morpholinyl(lower)alkyl, lower alkylpinerazinyl or [lower alkylpyrrolidinyl](lower)alkyl, tri)halo(lower)alkyl.
The object compound (I) of the present invention can be prepared by the following process. ##STR3## wherein R.sup.1, R.sup.2 and R.sup.3 are each as defined above.
The starting compound can be prepared by the following processes or Preparations mentioned below, or similar manners thereto. ##STR4## wherein
Suitable pharmaceutically acceptable salts of the object compound (I) are conventional non-toxic salts and may include a salt with a base or an acid addition salt such as a salt with an inorganic base, for example, an alkali metal salt (e.g., sodium salt, potassium salt, etc.), an alkaline earth metal salt (e.g., calcium salt, magnesium salt, etc.), an ammonium salt; a salt with an organic base, for example, an organic amine salt (e.g., triethylamine salt, pyridine salt, picoline salt, ethanolamine salt, triethanolamine salt, dicyclohexylamine salt, N,N'-dibenzylethylenediamine salt, etc.); an inorganic acid addition salt (e.g., hydrochloride, hydrobromide, sulfate, phosphate, etc.); an organic carboxylic or sulfonic acid addition salt (e.g., formate, acetate, trifluoroacetate, maleate, tartrate, fumarate, citrate, methanesulfonate, benzenesulfonate, toluenesulfonate, etc.); a salt with a basic or acidic amino acid (e.g., arginine, aspartic acid, glutamic acid, etc.).
In the above and subsequent descriptions of the present specification, suitable examples and illustration of the various definitions which the present invention intends to include within the scope thereof are explained in detail as follows.
The term "lower" is used to intend a group having 1 to 6, preferably 1 to 4, carbon atom(s), unless otherwise provided.
Suitable "lower alkyl" and "lower alkyl moiety" in the terms "[di(lower)alkylamino](lower)alkyl", "morpholinyl(lower)alkyl", "lower alkylpiperazinyl", "[lower alkylpyrrolidinyl](lower)alkyl", "mono(or di or tri)halo(lower)alkyl" may include straight or branched one having 1 to 6 carbon atom(s), such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, tert-pentyl, hexyl, and the like, and in which more preferable example may be C.sub.1 -C.sub.4 alkyl.
Suitable "lower alkoxy" may include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, tert-butoxy, pentyloxy, tert-pentyloxy, hexyloxy and the like.
Suitable "halogen" and "halogen moiety" in the term "mono(or di or tri)halo(lower)alkyl" may include fluorine, bromine, chlorine and iodine.
Suitable "leaving group" may include acid residue, lower alkoxy as exemplified above, and the like.
Suitable "acid residue" may include halogen as exemplified above, acyloxy, and the like.
Suitable "acyl moiety" in the term "acyloxy" m

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