Back to results
US 5,663,414 AGranted
Benzenesulfonamide derivatives
AssigneeEisai Co., Ltd.
InventorsHitoshi Oinuma, Takashi Hasegawa, Tadanobu Takamura, Kenichi Nomoto, Yoshiharu Daiku, Toshihiko Naito, Sachiyuki Hamano
Life of this patent
Estimating the term…
Abstract
A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.
Claims11
A pharmaceutical composition which comprises an effective phospholipase A.sub.2 inhibiting amount of a benzenesulfonamide derivative represented by the general formula:
- ##STR192## wherein R.sup.1 stands for a hydrogen atom, a cyano, nitro hydroxy group, a halogen atom, a lower alkoxy group, an acyloxy group wherein said acyl moiety is a residue of an organic saturated or unsaturated aliphatic, carbocyclic or heteroaryl carboxylic acid wherein the hetero atom is oxygen, nitrogen or sulfur, --SO.sub.2 --R.sup.8 wherein R.sup.8 stands for a lower alkyl group, a heteroaryl wherein the hetero atom is a nitrogen, oxygen or sulfur atom, a glycyloxy group, or a group represented by the formula:
- ##STR193## wherein p is an integer of 1 to 3;
- n is an integer of 1 to 4;
- R.sup.2 stands for a hydrogen atom or a pyridyl group.;
- R.sup.3 stands for a hydrogen atom or a lower alkyl, cyano or pyridyl group;
- R.sup.4 stands for a hydrogen atom or a lower alkyl group;
- R.sup.5 and R.sup.6 may be the same or different from each other and each 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:
- ##STR194## wherein R.sup.9 and R.sup.10 may be the same or different and each stand for a hydrogen atom or a lower alkyl group;
- or
- R.sup.5 and R.sup.6 each stand for an unsubstituted cycloalkyl group, or a cycloalkyl substituted with a lower alkyl or halogen or condensed with an aromatic ring, a bicycloalkyl, or tricycloalkyl, said bicycloalkyl or tricycloalkyl being an aliphatic saturated hydrocarbon group made of two or three rings, respectively, with at least two carbon atoms being common to each ring;
- a plurality of R.sup.7 groups each independently stand for a hydrogen atom, a lower alkyl group, a lower alkoxy group or a halogen atom;
- and r is an integer of 1 to 2, provided that when r is 2, the two R.sup.7 groups may form a cyclohexenyl or phenyl ring together with two adjacent carbon atoms constituting the benzene ring;
- and
- m is an integer of 1 to 2;
- or a pharmacologically acceptable salt thereof;
- and a pharmaceutically acceptable carrier.
15 more elements
Dependencies are inferred from the claim text.