Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1995-03-16
1997-01-28
Barts, Samuel
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514562, 560 12, 562427, 562430, A61K 3124
Patent
active
055978487
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP93/01382 filed Sep. 29, 1993 and published as WO94/07848 Apr. 14, 1994.
TECHNICAL FIELD
The present invention relates to benzenesulfonamide derivatives and their pharmacologically acceptable salts having thromboxane A.sub.2 antagonistic activity, leucotriene antagonistic activity and the like which are useful as platelet aggregation inhibitors, antithrombotic agents, antiasthmatic agents and antiallergic agents, and to uses thereof.
BACKGROUND ART
For example, the U.S. Pat. No. 4,258,058 discloses Sulotroban represented by the following formula and its derivatives: ##STR2## and the U.S. Pat. No. 4,443,477 discloses Daltroban represented by the following formula and its derivatives: ##STR3## as benzenesulfonamide derivatives having thromboxane A.sub.2 antagonistic activity. However, compounds structurally similar to the compounds of the present invention have never been known so far.
Thromboxane A.sub.2 is a potent physiologically active substance which is biosynthesized from arachidonic acid in living bodies. The substance has platelet aggregation activity and contracting activity on smooth muscles such as bronchi and coronary arteries. Although the substance is rather important in living bodies, it is considered that its excessive production may cause various disorders such as thrombosis and asthma. Leucotriene is also a potent physiologically active substance biosynthesized from arachidonic acid. This substance induces various pharmacological effects such as contraction of respiratory tract smooth muscle, hyper-secretion of respiratory tract and hyper-permeation of blood vessels, and is considered to be significantly involved in pathopoiesis of asthma and allergic inflammation.
For these reasons, drugs having thromboxane A.sub.2 antagonistic activity are expected to be useful as preventive and therapeutic agents for diseases associated with thromboxane A.sub.2 such as, for example, ischemic heart diseases such as angina pectoris and myocardial infarction, cerebrovascular diseases, thrombosis, and asthma. Drugs having leucotriene antagonistic activity are also expected to be useful as preventive and therapeutic agents for diseases associated with leucotriene such as, for example, asthma and allergic inflammation. Although several thromboxane A.sub.2 antagonists and leucotriene antagonists have been under clinical trials, they are not commercially available at present. Accordingly, further researches have been desired.
An object of the present invention is thus to provide medicaments having thromboxane A.sub.2 antagonistic activity and leucotriene antagonistic activity and useful as drugs for preventive and therapeutic treatments for ischemic heart diseases such as angina pectoris and myocardial infarction, cerebrovascular diseases, thrombosis, and asthma, or useful as drugs for preventive and therapeutic treatments for asthma and allergic inflammation.
The inventors of the present invention conducted various studies under these circumstances and, as a result, found that the novel benzenesulfonamide derivatives of the present invention have inhibitory activities against thromboxane A.sub.2 synthetase in addition to thromboxane A.sub.2 antagonistic activities and leucotriene D.sub.4 antagonistic activities. The inventors also found that they are highly useful as platelet aggregation inhibitors, antithrombotic agents, antiasthmatic agents and antiallergic agents. The present invention was achieved on the basis of these findings.
DISCLOSURE OF THE INVENTION
According to the present invention, there are provided novel benzenesulfonamide derivatives represented by the following general Formula (I): ##STR4## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group or a halogen atom; R.sup.2 represents a C.sub.1 -C.sub.10 straight- or branched-chain alkyl group, a C.sub.3 -C.sub.8 cycloalkyl group which may be substituted with one or more C.sub.1 -C.sub.6 alkyl groups on its ring, a C.sub.1 -C.sub.6 alkyl group substituted with one or more C
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Ito Yasuo
Kato Hideo
Ogawa Nobuo
Sakurai Shunichiro
Suzuki Tomio
Barts Samuel
Hokuriku Seiyaku Co. Ltd.
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