Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-05-17
1996-03-05
Gupta, Yogendra N.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549458, 549460, 549461, A61K 3134, C07D30780, C07D30778
Patent
active
054968496
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP93/01339 filed on Sep. 17, 1993.
1. Technical Field
The present invention relates to a sulfonic acid derivative having a cyclopenta[b]benzofuran ring which is used as a therapeutic drug for disorders caused by thromboxane A2.
2. Background Art
Thromboxane A2 (TXA2), discovered by Samuelsson et al. in 1975, has strong platelet coagulating action and smooth muscle contracting action (see Proc. Natl. Acad. Sci. U.S.A., vol. 72, p. 2994 (1975)). Thromboxane A2 is considered to be one of the causes which produces disorders such as ischemic heart disorders including angina pectoris and myocardial infarction, as well as cerebrovascular disease and bronchial asthma as a result of these actions. Thus, suppression of the action of thromboxane A2 is effective for treatment of disorders such as ischemic heart disorders including angina pectoris and myocardial infarction, cerebrovascular disease and bronchial asthma. Thromboxane A2 receptor antagonists have been reported to be drugs which suppress the action of thromboxane A2 (see Circulation, vol. 81, suppl. I, I-69 (1990)).
Thromboxane A2 receptor antagonists have attracted attention as therapeutic drugs for disorders caused by thromboxane A2, and a thromboxane A2 receptor antagonist is sought which has both high activity and long duration.
DISCLOSURE OF THE INVENTION
The present inventors, as a result of searching for a thromboxane A2 receptor antagonist having a novel structure, found a sulfonamide derivative that has a cyclopenta[b]benzofuran ring as a compound which has powerful thromboxane A2 receptor antagonistic action. Namely, the present invention relates to sulfonic acid derivatives represented with general formula [I]: ##STR2## [wherein, R.sub.1 is acceptable cation, or (3) an alkyl having 1 to 4 carbon atoms) or the group: ##STR3## (wherein, --R.sub.3 represents an alkyl having 1 to 4 carbon atoms); A is ##STR4## (wherein, --R.sub.4 and R.sub.5 represent (1) hydrogen or (2) an alkyl having 1 to 4 carbon atoms, and R.sub.4 and R.sub.5 may be identical or different); and, ##STR5## {wherein, R.sub.6 represents having 1 to 4 carbon atoms, (3) an acyl group having 2 to 5 carbon atoms, or (4) an aroyl group having 7 to 11 carbon atoms), ##STR6## (wherein, 1 represents an integer of 5 to 7 and R.sub.10 represents hydrogen or a phenyl group), ##STR7## --O--, R.sub.7 is alkylene represented by C.sub.t H.sub.2t (wherein, t is an integer of 1 to 5), and R.sub.11 represents an aryl group or aryl group having 6 to 16 carbon atoms substituted by 1 to 4 groups selected from the group consisting of alkyl, methoxy, chlorine, bromine, fluorine, iodine, trifluoromethyl, nitro, cyano, phenyl and phenoxy)}], as well as a thromboxane A2 receptor antagonistic drugs having said novel sulfonic acid derivative for its effective ingredient.
Among those compounds represented by the formula (I), those compounds wherein B is represented by the formula (II) or formula (III') ##STR8## (wherein, R.sub.6, R.sub.7, R.sub.8, Y and W are the same as previously defined) are used preferably.
In particular, the sulfonamide derivatives represented by the formula (I') below as well as the sulfonate ester derivatives represented by the formula (I") below are preferable. ##STR9## (wherein, R.sub.1, R.sub.6, R.sub.7, R.sub.8, A and Y are the same as previously defined) ##STR10## (wherein, R.sub.60 is having 1 to 4 carbon atoms, and R.sub.50 is an aryl group non-substituted or substituted with 1 to 4 groups of alkyl, methoxy, chlorine, bromine, fluorine, iodine, trifluoromethyl, nitro, cyano, phenyl and phenoxy)].
In addition, among the sulfonamide derivatives indicated in the above-mentioned general formula (I'), preferable sulfonamides are those wherein carbon atoms, or (3) an acyl group), and branched alkylene represented by C.sub.t H.sub.2t (where, t is an integer of 1-4), and R.sub.11 represents a phenyl group or a phenyl group substituted by 1 to 4 groups selected from the group consisting of alkyl, methoxy, chlorine, bromine, fluorine, iodine, trifluoromet
REFERENCES:
patent: 5126370 (1992-06-01), Misra
patent: 5158967 (1992-01-01), Hall
Hoshi Kazuhiro
Nishio Shintaro
Ohno Kiyotaka
Ohtake Atsushi
Tsukamoto Shunji
Gupta Yogendra N.
Miller Austin R.
Toray Industries Inc.
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