Shionogi Company Limited

Shionogi Seiyaku Kabushiki Kaisha

Hirokuni Jyoyama

Saichi Matsumoto

Nobuhiro Haga

Susumu Kamata

Kohji Hanasaki

Ryuji Suzuki

Tsuneaki Sakata

Toshihiko Okada

Kenzo Koizumi

Takeshi Shiota

Shinji Kakudo

Masanao Inagaki

Izumi Saitoh

Tatsuo Tsuri

Katsumi Hirose

Shohei Egawa

Fujio Asanuma

Antirheumatic agent

Antirheumatic

Benzylidene derivatives having anti-inflammatory activities, are shown by the following formula I: ##STR1## wherein A is -CH.sub.2 - or -CH.sub.2 CH.sub.2 -; B is a bond or -CH.sub.2 -, -CHOH-, -CO-, -O-, or A and B may taken together form -CH=CH-; D is &gt;N- or &gt;CH-; R.sup.1 and R.sup.2 each independently is hydrogen, lower alkyl or lower alkoxy; R.sup.3 is hydrogen, lower alkyl, cycloalkyl, lower alkoxy, arylalkyloxy, heteroarylalkyloxy, lower alkylcarbonyl, arylcarbonyl, substituted or unsubstituted carbamoyl, or a group of the formula:

Benzylidene derivatives

The present invention relates to novel 3-benzylidene-1-carbamoyl-2-pyrroridone analogues having advantage anti-inflammatory activities, which is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is independently hydrogen, alkyl, alkoxy, or halogen; R.sup.3 is hydrogen or acyl; R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, cyano, or halogen; R.sup.5 and R.sup.6 each is independently hydrogen, alkyl, aryl, aralkyl, heterocyclic group, substituted or unsubstituted amino, or OR.sup.7 wherein R.sup.7 is hydrogen, alkyl, aryl, acyl, or aralkyl, or taken together with the adjacent nitrogen atom may form heterocyclic group which may contain N, O, and/or S, and X and Y each is independently O, S, substituted or unsubstituted imino, or substituted or unsubstituted methylene. In more detail, the present invention provides an anti-inflammatory agent which is useful for the treatment of chronic inflammation and has little side effect, e.g., stomach disease.

3-benzylidene-1-carbamoyl-2-pyrrolidone analogues

3-benzylidene-1-carbamoyl-2-pyrrolidone compounds useful as

Topical analgesic anti-inflammatory compositions containing a corticosteroid in addition to the conventional efficacy-proven ingredients are disclosed. They may be embodied in an aerosol, a solution and any other type of composition being convenient for administration. More than the sum of effects of the individual ingredients has been proved. In other words, the effects of the salicylate esters and L-menthol are synergistically enhanced by the addition of the corticosteroid. Particularly, the persistency of the analgesic/anti-inflammatory effects of the conventional ingredients has been proved to be dependent upon the the concentration of the corticosteroid in the composition.

Topical analgesic anti-inflammatory composition

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Nara, Japan

Hirokuni Jyoyama