Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1988-11-10
1990-11-20
Lee, Mary C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
558401, A61K 31275, C07C12175
Patent
active
049719963
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
1. Technical Field
The present invention relates to a novel hydroxystyrene derivative or a salt thereof, which has antiallergic activity, 5-lipoxygenase inhibiting activity, antibacterial activity, tyrosine kinase inhibiting activity, ultraviolet (hereinafter referred to as "UV") absorbing activity and reverse transcriptase inhibiting activity and is useful as an intermediate for preparing various organic compounds, and relates to an antiallergic agent, a 5-lipoxygenase inhibiting agent, an antibacterial agent, a tyrosine kinase inhibiting agent, an UV absorber and a reverse transcriptase inhibiting agent containing the same as an active ingredient.
2. Background Art
The compound of the present invention is a novel compound which has not yet been reported in a literature and is first synthesized by the present inventors.
3. Disclosure of the Invention
It has now been found that a novel hydroxystyrene derivative of the present invention is a useful intermediate for preparing various organic compounds and has itself antiallergic activity, 5-lipoxygenase inhibiting activity, antibacterial activity, tyrosine kinase inhibiting activity, UV absorbing activity and reverse transcriptase inhibiting activity.
In accordance with the present invention, there is provided a hydroxystyrene derivative represented by the formula (I): ##STR5## wherein when R.sup.1 and R.sup.2 are the same or different and each is phenyl group, benzyl group or phenethyl group, or R.sup.1 is a group having the formula: R.sup.5 O-- in which R.sup.5 is hydrogen atom, an alkyl group having 1 to 5 carbon atoms or benzyl group and R.sup.2 is benzyl group or a group of PhSCH.sub.2 in which Ph is phenyl group, hereinafter the same, R.sup.1 and R.sup.4 are taken together to represent a group having the formula: --CONH--CS--S--, a group having the formula: ##STR6## a group having the formula: ##STR7## or a group having the formula: ##STR8## in which R.sup.6 is a group having the formula: ##STR9## in which X.sup.1 is hydrogen atom, a halogen atom, methyl group, ethyl group, an alkoxyl group having the formula: R.sup.7 O-- (in which R.sup.7 is methyl group or ethyl group), nitro group, aminosulfonyl group or amino group, and m.sup.1 is 1 or 2], pyridyl group, furyl group or thienyl group, and n.sup.1 is 0 or an integer of 1 to 3; when R.sup.1 and R.sup.2 are the same or different and each is phenyl group, benzyl group or phenethyl group, or R.sup.1 is a group having the formula: R.sup.5 O-- in which R.sup.5 is as defined above, and R.sup.2 is benzyl group, R.sup.3 is cyano group and R.sup.4 is carbamoyl group, or R.sup.3 and R.sup.4 are taken together to represent a group having the formula: --CO--Y--CH.sub.2 CH.sub.2 -- in which Y is oxygen atom or --NH--, or a group having the formula: ##STR10## and when R.sup.1 and R.sup.2 are the same or different and each is an alkyl group having 1 to 3 carbon atoms, R.sup.3 and R.sup.4 are taken together to represent a group having the formula: ##STR11## in which n.sup.1 and R.sup.6 are as defined above, or a salt thereof.
The compound having the formula (I) of the present invention can form a salt with a base or an acid. The salt of the present invention may be any which can be formed from the compound of the present invention and the base or the acid.
Examples of the salt with the base are, for instance, (1) a salt with metal, especially an alkali metal salt, an alkaline earth metal salt and a salt with aluminum; (2) an ammonium salt; and (3) an amine salt, especially a salt with methylamine, ethylamine, diethylamine, triethylamine, pyrrolidine, piperidine, morpholine, hexamethyleneimine, aniline or pyridine, and the like.
Examples of the salt with the acid are, for instance, (1) a salt with an inorganic acid, especially a salt with hydrochloric acid, sulfuric acid, phosphoric acid, nitric acid or carbonic acid; (2) a salt with an organic acid, especially a salt with a carboxylic acid such as formic acid, acetic acid, propionic acid, succinic acid, oxalic acid, tartaric acid, maleic acid, lactic aci
REFERENCES:
patent: Re29467 (1977-11-01), Nussim et al.
patent: 3912519 (1975-10-01), Takagi et al.
patent: 4594460 (1986-06-01), Mignami et al.
Chemical Abstracts, vol. 106, No. 25, 22nd Jun. 1989, p. 661, abstract No. 213918z, Columbus, Ohio.
Ariki Yutaka
Domoto Takeshi
Hidaka Takayoshi
Hosoe Kazunori
Imai Naohiro
Kanegafuchi Kagaku Kogyo & Kabushiki Kaisha
Lee Mary C.
Northington-Davis Zinna
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