Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-04-22
1996-04-09
Dees, Jose G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5142352, 514253, 514278, 546157, 546158, 546 16, 544128, 544363, A61K 3147
Patent
active
055062393
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to a carbostyril derivative and a platelets aggregation inhibitory agent containing said derivative as an active ingredient.
BACKGROUND ART
Compounds having structural formulas similar to that of the carbostyril derivative of the present invention are disclosed in the following prior art literature (patents).
The prior art by the present applicant
U.S. Pat. Nos. 4,070,470, 4,216,220, 4,313,947, 4,298,739, 4,277,479, 4,435,404, 5,008,274 and 5,053,514; EP-A-8910919; Japanese Patent Application Kokai (Laid-open) Nos. 50-82218, 50-106977, 50-142576, 50-151881, 54-30180, 54-30183, 54-30184, 55-79371, 57-9780, 57-14574, 57-93962, 57-159778, 58-59980, 56-8319, 57-80322, 52-108980 and 63-290821.
The prior art by other applicants
Japanese Patent Application Kokai (Laid-open) No. 56-16470 (U.S. Pat. No. 4329347); Japanese Patent Application Kokai (Laid-open) No. 56-36452; Japanese Patent Application Kokai (Laid-open) No. 59-31753 (EP-A-96006A); U.S. Pat. No. 3994900; BE-A-859415; and EP-A-71150 [Japanese Patent Application Kokai (Laid-open) No. 58-24559].
The structural formulas of the carbostyril compounds disclosed in the above prior art literature (patents) are similar to that of the carbostyril derivative of the present invention, but are different from the latter in the side chain structures. Although some of the carbostyril compounds disclosed in the prior art literature, similarly to the carbostyril derivative of the present invention, have a platelets aggregation inhibitory activity, the compounds of the prior art include also those showing different pharmacological activities such as antithrombotic activity, antihistaminic activity, antiarrhythmic activity, cardiotonicactivity, .alpha.- and .beta.-adrenergic blocking activity and the like.
[DISCLOSURE OF THE INVENTION]
The carbostyril derivative of the present invention is represented by the following general formula (1). ##STR2## {wherein A represents a lower alkylene group.
R represents a group ##STR3## a group ##STR4## or a group ##STR5## [wherein R.sup.1 represents a group ##STR6## (wherein l and m independently represent 0 or 1. B represents a lower alkylene group. Each of R.sup.7 and R.sup.8, which may be the same or different, represents a hydrogen atom, a lower alkyl group which may have a hydroxyl group, or a lower alkanoyl group. Further, R.sup.7 and R.sup.8 may form a five- or six-membered saturated heterocyclic ring, together with the nitrogen atom to which they bond and further with or without a nitrogen, oxygen or sulfur atom which may be present between R.sup.7 and R.sup.8. Said heterocyclic ring may have 1-3 substituents selected from the group consisting of a hydroxyl group, a lower alkyl group which may have a lower alkoxy-lower alkoxy group or a hydroxyl group, a lower alkyl group-substituted or unsubstituted amino group, a lower alkoxy-lower alkoxy group, an oxo group and a lower alkyl group-substituted or unsubstituted aminocarbonyl group. Said heterocylic ring may also have a lower alkylenedioxy group as a substituent.); a lower alkoxycarbonyl group-substituted lower alkyl group; a carboxy group-substituted lower alkyl group; a lower alkyl group having, as a substituent, a lower alkyl group-substituted or unsubstituted aminocarbonyl group; a hydroxyl group-containing lower alkyl group; an imidazolyl-substituted lower alkyl group; a pyridyl-substituted lower alkyl group; a pyrrolidinyl-lower alkyl group which may have, as substituent(s) on the pyrrolidine ring, 1-3 groups selected from the group consisting of a lower alkyl group, a lower alkoxy-lower alkoxy group and a hydroxyl group; or a group--SO.sub.2 --D--R.sup.9 (wherein D represents a lower alkylene group. R.sup.9 represents a five- or six-membered saturated or unsaturated heterocylic ring residue having from 1-3 halogen atoms or nitrogen atoms. Said heterocyclic ring may have, as a substituent, a hydroxyl group, a lower alkoxy-lower alkoxy group, a lower alkoxycarbonyl group, or a lower alkyl group which may have a low
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Kihara Yoshito
Koga Nobuyuki
Nishi Takao
Saitoh Masahiro
Sato Seiji
Barts Samuel
Dees Jos,e G.
Otsuka Pharmaceutical Co. Ltd.
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