Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1992-12-04
1994-09-06
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
564168, 549491, 544391, 544398, 546216, 546236, 560104, 514485, 514486, 514683, 514317, 514330, 514255, 514464, A61K 31165, A61K 31495, C07C10382, C07D21375
Patent
active
053448456
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel compound which has IV-type allergic reaction-suppressive function and which is useful as a medicine such as IV-type allergy suppressive drug.
BACKGROUND ART
It has been reported that IV-type allergic reaction is greatly responsible for the pathopoiesis of refractory diseases such as refractory asthma, chronic hepatitis and nephrotic syndrome. To cure these refractory diseases, immunosuppressive agents, a typical example of which is asteroid drug, are used. However, the use of the immunosuppressive agents is limited, inevitably because of their strong side effects.
DISCLOSURE OF INVENTION
Therefore it has been demanded that a IV-type allergic reaction-suppressive agent be developed in place of the immunosuppressive agents hitherto known.
In order to meet the demand described above, the inventors hereof have been making research and study, in search for a substance which works against IV-type allergic reaction in its effector phase. They successfully synthesized the compounds represented by the following formulas I, II, III, IV and V, and examined these compounds for their pharmacological activities to find that these compounds have desired IV-type allergic reaction-suppressive function, thus completing the present invention.
The present invention provides the compounds represented by the formulas I, II, III, IV and V or pharmaceutically acceptable salts thereof, and IV-type allergic reaction-suppressive agents containing, as effective components, the compounds represented by the formula I, II, III, IV and V, or pharmaceutically acceptable salts thereof. ##STR1## where L represents --(CH.dbd.CH).sub.k -- or --(CH.sub.2).sub.k --; j represents an integer of 1 to 6; k represents represents an integer of 0 to 5; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are either identical or different, and each represents a hydrogen atom, an amino group, an acylamino group (preferably, one in which the acyl moiety has 1 to 3 carbon atoms), a dialkylamino group in which each alkyl moiety has 1 to 5 carbon atoms, a halogen atom, a hydroxyl group, an acetoxy group, an alkoxy group having 1 to 3 carbon atoms, a trifluoromethyl group, a nitro group, tetrahydropyranyloxy group, or a benzyloxy group; and R.sub.1 and R.sub.2 may combine together to form a methylenedioxy group. ##STR2## where L represents --(CH.dbd.CH).sub.k -- or --(CH.sub.2).sub.k --; each k represents an integer of 0 to 5; R.sub.5, R.sub.6 and R.sub.7 are either identical or different, and each represents a hydrogen atom, a hydroxyl group, an acetoxy group, an amino acid ester group in which the amino moiety may be protected by a protective group, an alkoxy group having 1 to 3 carbon atoms, or --O--(CH.sub.2).sub.j --Y.sub.1 ; R.sub.5 and R.sub.6 may combine together to form a methylenedioxy group. j represents an integer of 1 to 6, and Y.sub.1 is a halogen atom, an amino group, an amino group substituted with 1 or 2 thioethanol groups, an amino group substituted with 1 or 2 allyl groups, a monoalkylamino group having 1 to 10 carbon atoms, a dialylamino group in which each alkyl moiety has 1 to 10 carbon atoms, an imidazole group substituted with 1 to 3 substituent groups (e.g., a nitro group, a cyano group, a phenyl group, an alkoxy group having 1 to 3 carbon atoms, a halogen atom, or an alkyl group having 1 to 3 carbon atoms), a benzimidazole group substituted with 1 to 3 substituent groups (e.g., a nitro group, a cyano group, a phenyl group, an alkoxy group having 1 to 3 carbon atoms, a halogen atom, or an alkyl group having 1 to 3 carbon atoms), a diazole group, a triazole group, a tetrazole group, a piperidine group, a piperidinopiperidine group, an isonipecotic acid group or an ester thereof with an alkyl group having 1 to 5 carbon atoms, a thiazolidine group, a pyrrolidine group, a morpholine group, a 4-methylpiperazine group, a carboxyl group (--COOH), a carboxylic acid alkylester group in which the alkyl moiety has 1 to 5 carbon atoms (--COO--C.sub.1 to C.sub.5 alkyl) or a carboxamide group.
In th
REFERENCES:
patent: 4673684 (1987-06-01), Wakabayashi et al.
Johnson et al., Journal of the American Chemical Society, 92(19) (1971), 4880-4883.
Eckhardt et al., Chemical Abstracts 89(3) 23, 2924, 1978.
Kawamura Hideki
Koda Akihide
Maruno Masao
Ono Yutaka
Ozawa Hideyuki
Grumbling Matthew V.
Shah Mukund J.
Tsumura & Co.
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