Benzoylguanidine derivatives as medicaments

Details Benzoylguanidine derivatives as medicaments Benzoylguanidine derivatives as medicaments

1997-02-03

1999-10-19

Kight, John

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

514618, 564180, 564187, A01N 3718, C07C23300

Patent

active

059689854

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP95/011479 filed Jul. 25, 1995.


TECHNICAL FIELD

This invention relates to new guanidine derivatives and a pharmaceutically acceptable salts thereof which are useful as a medicament.


DISCLOSURE OF INVENTION

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.
The object guanidine derivatives of the present invention are novel and can be represented by the following general formula (I): ##STR1## wherein R.sup.1 is hydrogen, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, acyl(lower)alkoxy, acyl(lower)alkenyl, or acyl, and substituents; indenyl, indanyl, dihydrobenzocycloheptenyl, di(or tetra or hexa or octa or deca)hydronaphthyl, cyclopentenyl, dihydrothienyl, dihydrofuryl or heterobicyclic group, each of which may have suitable substituent(s); lower alkylthienyl; mono(or di)halothienyl; mono(or di or tri)halo(lower)alkylthienyl; acylthienyl; halofuryl; or mono(or di or tri)halo(lower)alkylfuryl.
The object compound (I) of the present invention can be prepared by the following process. ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above.
The starting compound can be prepared by the following processes or Preparations mentioned below, or similar manners thereto. ##STR3## Process (B) ##STR4## Process (C) ##STR5## Process (D) ##STR6## Process (E) ##STR7## Process (F) ##STR8## Process (G) ##STR9## Process (H) ##STR10## wherein R.sup.1 and R.sup.2 are each as defined above,
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, isethionate, fumarate, 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.
The term "higher" is used to intend a group having 7 to 20 carbon atoms, unless otherwise provided.
Suitable "lower alkyl" and "lower alkyl moiety" in the terms "hydroxy(lower)alkyl", "protected hydroxy(lower)alkyl", "lower alkylthienyl", "mono(or di or tri)halo(lower)alkylthienyl" and "mono(or di or tri)halo(lower)alkylfuryl" may include straight or branched one having 1 to 6 carbon atom(s), such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, ter

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