Naphthalene derivatives as prostaglandin I.sub.2 agonsists

Details Naphthalene derivatives as prostaglandin I.sub.2 agonsists Naphthalene derivatives as prostaglandin I.sub.2 agonsists

1996-10-10

1998-06-09

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514552, 558233, 558242, A01N 3712, A01N 3702, C07C33300

Patent

active

057634890

DESCRIPTION:

BRIEF SUMMARY
This is a 371 of PCT/JP95/00373 filed Mar. 8, 1995.


TECHNICAL FIELD

This invention relates to new naphthalene derivatives and pharmaceutically acceptable salts thereof which are useful as a medicament.
1. Background Art
Some naphthalene derivatives have been known as described, for example, in EP 0542203A2.
2. Disclosure of Invention
This invention relates to new naphthalene derivatives. More particularly, this invention relates to new naphthalene derivatives and pharmaceutically acceptable salts thereof which have pharmacological activities such as an inhibitory activity on platelet aggregation, vasodilating activity, antihypertensive activity or the like and are prostaglandin I.sub.2 agonists, to processes for their production, to a pharmaceutical composition containing the same and to a use thereof for manufacture of medicaments.
Accordingly, one object of this invention is to provide new and useful naphthalene derivatives and pharmaceutically acceptable salts thereof.
Another object of this invention is to provide processes for production of the naphthalene derivatives and salts thereof.
A further object of this invention is to provide a pharmaceutical composition containing, as an active ingredient, said naphthalene derivatives or pharmaceutically acceptable salts thereof.
Still further object of this invention is to provide use of the naphthalene derivatives and pharmaceutically acceptable salts thereof for manufacture of medicaments for the therapeutic and/or prophylactic treatment of arterial obstruction, cerebrovascular disease, hepatic cirrhosis, arteriosclerosis, ischemic heart disease, restenosis after percutaneous transluminal coronary angioplasty, hypertension or the like.
The naphthalene derivatives of this invention can be represented by the following formula (I): ##STR4## wherein R.sup.1 is carboxy or protected carboxy, ##STR5## (in which R.sup.6 is mono(or di or tri)aryl(lower)alkyl and Z is N or CH), or ##STR6## in which --A.sup.3 -- is ##STR7## (wherein R.sup.9 is hydrogen or lower alkyl), Q is N or CH, R.sup.7 is aryl and R.sup.8 is aryl!, and ##STR8##
According to the present invention, the new naphthalene derivatives (I) can be prepared by the processes which are illustrated in the following scheme. ##STR9## Process 2 ##STR10## Process 3 ##STR11## Process 4 ##STR12## Process 5 ##STR13## Process 6 ##STR14## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.8, R.sup.9, A.sup.1, A.sup.2, Q and ##STR15## are each as defined above, X.sup.1 is acid residue,
Some of the starting compounds are novel and can be prepared by the following processes. ##STR16## Process B ##STR17## Process C ##STR18## Process D ##STR19## Process E ##STR20## Process F ##STR21## Process G ##STR22## Process H ##STR23## Process I ##STR24## Process J ##STR25## Process K ##STR26## Process L ##STR27## Process M ##STR28## Process N ##STR29## Process O ##STR30## Process P ##STR31## Process Q ##STR32## Process R ##STR33## Process S ##STR34## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, A.sup.1, A.sup.2, Z, Q, X.sup.1, X.sup.3 and ##STR35## are each as defined above, R.sup.10 is hydrogen or hydroxy protective group,
Suitable pharmaceutically acceptable salts of the object compound (I) are conventional non-toxic salts and include a metal salt such as an alkali metal salt (e.g. sodium salt, potassium salt, etc.) and an alkaline earth metal salt (e.g. calcium salt, magnesium salt, etc.), an ammonium salt, an organic base salt (e.g. trimethylamine salt, triethylamine salt, pyridine salt, picoline salt, dicyclohexylamine salt, N,N'-dibenzylethylenediamine salt, etc.), an organic acid salt (e.g. acetate, maleate, tartrate, methanesulfonate, benzenesulfonate, formate, toluenesulfonate, trifluoroacetate, etc.), an inorganic acid salt (e.g. hydrochloride, hydrobromide, sulfate, phosphate, etc.), a salt with an amino acid (e.g. arginine, aspartic acid, glutamic acid, etc.), and the like.
In the above and subsequent descriptions of the present specification, suitable exam

REFERENCES:
Takemura et al., "Studies on Benzhyddryl Derivatives . . . ", Chem. Pharm. Bull., vol. 31 (1983), No. 8, pp. 2632-2638.

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