Amino acid derivatives and their use as phospholipase A.sub.2 in

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514311, 514277, 514299, 514279, 546139, 546151, 546152, 546164, 540166, 540174, 540175, A61K 31325, A61K 3116, C07D21700, C07D21502

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active

061109339

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to a novel fatty acid derivative and a pharmaceutically acceptable salt thereof which are useful as a medicament.


BACKGROUND ART

A phospholipase A.sub.2 inhibitor having the structure of that of the present invention has not been known.


DISCLOSURE OF INVENTION

The present invention relates to novel fatty acid derivative and a pharmaceutically acceptable salt thereof, which are phospholipase A.sub.2 inhibitors and are useful for the prevention and/or the treatment of pancreatitis, hepatitis, chronic renal failure, etc; shock (e.g. endotoxin shock, gram-negative septic shock, etc), arthritis (e.g. rheumatoid arthritis, osteoarthritis, etc), respiratory disease (e.g. bronchial asthma, bronchitis, adult respiratory distress syndrome, etc), heart disease (e.g. myocardial ischemia, etc), allergic disease, thrombosis, arteriosclerosis, pain, autoimmune disease, dermal disease (e.g. atopic dermatitis, psoriasis, contact dermatitis, etc), inflammatory bowel disease (e.g. Crohn's disease, ulcerative colitis, etc), ophthalmic disease (e.g. allergic ophthalmic disease, inflammatory ophthalmic disease, etc), nasal diseases (e.g. allergic rhinitis, etc), gout, trauma induced inflammation (e.g. spinal cord injury, etc), liver diseases (e.g. cirrhosis, hepatitis, etc), or the like; to a process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for using the same therapeutically in human being and animals for the prevention and/or treatment of the aforesaid diseases.
The object fatty acid derivative can be represented by the following formula (I): ##STR2## wherein R.sup.1 is acyl group or lower aliphatic hydrocarbon group which may have one or more suitable substituent(s), and ##STR3## [wherein R.sup.5 is hydrogen or acyl(lower)alkyl].
It is to be noted the object compound (I) may include one or more stereoisomers due to asymmetric carbon atom(s) and double bond, and all of such isomers and a mixture thereof are included within the scope of the present invention.
It is further to be noted isomerization or rearrangement of the object compound (I) may occur due to the effect of the light, acid, base or the like, and the compound obtained as the result of said isomerization or rearrangement is also included within the scope of the present invention.
It is also to be noted that the solvating form of the compound (I) (e.g. hydrate, etc) and any form of the crystal of the compound (I) are included within the scope of the present invention.
The object compound (I) or a salt thereof can be prepared according to the following reaction schemes. ##STR4## wherein more suitable substituent(s),
Suitable pharmaceutically acceptable salts of the object compound (I) are conventional ones 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, trifluoroacetate, maleate, tartrate, fumarate, methanesulfonate, benzenesulfonate, formate, toluenesulfonate, etc), an inorganic acid salt (e.g. hydrochloride, hydrobromide, hydriodide, sulfate, phosphate, etc), a salt with an amino acid (e.g. arginine, aspartic acid, glutamic acid, etc), and the like.
In the above and following descriptions of the present specification, suitable examples and illustrations of the various definitions which the present invention includes within the scope thereof are explained in detail as follows.
The term "lower" is intended to mean 1 to 6 carbon atom(s) unless otherwise indicated.
The term "higher" is intended to mean 7 to 20 carbon atoms unless otherwise indicated.
Suitable "lower aliphatic hydrocarbon group" in the term "lower aliphatic hydrocarbon group which may have one or more suitable substituent(s)" may include lower alkyl, lower alkenyl and

REFERENCES:
Lettieri et al., Boll. Chim. Farm. (1981), 120 (5), pp. 308-310.
Ahmad et al., J. Indian Chem. Soc., Dec. (1979), vol. LVI (12), pp. 1265-1268.
Donia S. G., Pak. J. Sci. ind. res., Oct. (1992), vol. 35, No. 10, pp. 388-390, 1990.
Bhat et al., Ind. J. Chem. Sect. B, (1981)vol. 20 B (4), pp. 331-333.
Jouln et al., Tetrahederon Letters, (1987), vol. 28, No. 15, pp. 1665-1668.
Hanabusa et al., J. Macromol. Sci-Chem.,(1989) A26(12), pp. 1571-1584.
Cantacuzene et al., Tetrahederon, 1989, vol. 45, No. 3, pp. 741-745.
Ichikawa et al., Chemical abstracts No. 116:6968g, EP 443,592, 1991.
Mendes et al. (CA 113:6315 abstract of EP 346208) 1989.

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