Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1991-09-26
1994-01-25
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
540575, 540597, 540606, 544335, 546133, 546171, 546208, 546223, 546280, 546337, 548193, 548568, 558391, 560138, 562428, 564 86, C07C31146, A61K 3118
Patent
active
052816265
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a benzenesulfonamide derivative or a pharmacologically acceptable salt thereof exhibiting excellent activity as a drug.
BACKGROUND ART
Phospholipase A is an enzyme catalyzing the hydrolysis of the acyl linkage of glycerophospholipid and includes phospholipase A catalyzing the hydrolysis of 1-ester linkage of glycerophospholipid and phospholipase A.sub.2 catalyzing that of 2-ester linkage thereof. Although both of the phospholipases are widely distributed in the biological world, they have recently been noted from the standpoint of their connection to various diseases.
For example, in ischemic diseases such as cardiac infarction, it is believed that phospholipase is activated to disintegrate membrane phospholipid, giving an increased infarct size. Furthermore, studies have been made on the connection of the phospholipase to other various troubles.
Under these circumstances, various phospholipase A.sub.2 inhibitors have been proposed from the standpoint that the inhibition of phospholipase, particularly phospholipase A.sub.2 (PLA.sub.2) is effective in the prevention and treatment of various diseases (see Japanese Patent Laid-Open Nos. 255,749/1985, 175,466/1987, 2,968/1988 and 258,854/1988).
The inventors of the present invention have eagerly studied for many years on substances which can inhibit phospholipase A.sub.2 to find out that a benzenesulfonamide derivative or a pharmacologically acceptable salt thereof which will be described below exhibits a high inhibitory activity against phospholipase A.sub.2 and therefore is useful in the prevention and treatment of various diseases, for example, ischemic diseases such as cardiac infarction. The present invention has been accomplished on the basis of this finding.
DISCLOSURE OF INVENTION
The compound of the present invention is a sulfonamide derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR2## wherein a plurality of R.sup.1 groups each independently stand for a hydrogen atom, a cyano, nitro or hydroxyl group, a halogen atom, a lower alkoxy group, an acyloxy group, a group represented by the formula: --SO.sub.2 --R.sup.8 (wherein R.sup.8 stands for a lower alkyl group), a heteroaryl or glycyloxy group or a group represented by the formula: ##STR3## wherein p is an integer of 1 to 3), and n is an integer of 1 to 4; R.sup.2 stands for a hydrogen atom or a pyridyl group; group; stand for a hydrogen atom, a lower alkyl group, a group represented by the formula: --(CH.sub.2).sub.q --A [wherein q is an integer of 1 to 4; and A stands for a hydroxyl group, a group represented by the formula: ##STR4## (wherein R.sup.9 and R.sup.10 may be the same or different from each other and each stand for a hydrogen atom or a lower alkyl group), a group represented by the formula: ##STR5## (wherein R.sup.11 stands for a hydrogen atom or a lower alkyl group) or a group represented by the formula: ##STR6## wherein s is an integer of 2 to 5)], an unsubstituted or substituted cycloalkyl group, a bicycloalkyl, tricycloalkyl or azabicycloalkyl group or a group represented by the formula: ##STR7## (wherein g and h are each an integer of 1 to 4; and B stands for a lower alkyl group, a substituted or unsubstituted arylalkyl group or a substituted or unsubstituted pyridyl alkyl group), or alternatively R.sup.5 and R.sup.6 may be combined together to form a 6- or 7-membered ring which may contain a nitrogen or oxygen atom in addition to the nitrogen atom to which R.sup.5 and R.sup.6 are bonded, and said 6- or 7-membered ring may be substituted with a lower alkyl, arylalkyl, cycloalkylalkyl or heteroarylalkyl group; a lower alkyl group, a lower alkoxy group or a halogen atom; and r is an integer of 1 or 2, provided that when r is 2, the two R.sup.7 groups may form a ring together with two adjacent carbon atoms constituting the benzene ring; and
In the above definition of the compound (I) according to the present invention, the lower alkyl group defined with respect to R.sup.3, R.su
REFERENCES:
patent: 4925861 (1990-05-01), Hayashi et al.
patent: 4992469 (1991-02-01), Ozawa et al.
Islam, Egyptian J. Chem. 17, 689, (1974).
Teofino, Gazz Chim. Ital. 89, 1200 (1959).
Naoya Yoda et al.: Journal of Polymer Science Part A, vol. 3 (6) 2229-2242 (1965) Abstract.
R. J. Cremlyn et al.: J. Chem. Soc. Pak., vol. 7, No. 2, 1985, pp. 111-124.
Daiku Yoshiharu
Hamano Sachiyuki
Hasegawa Takashi
Naito Toshihiko
Nomoto Ken-ichi
Eisai Co. Ltd.
Gerstl Robert
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