Toyama Chemical Co., Ltd.

Yukihiko Aikawa

Shunichi Shiozawa

Keiichi Tanaka

Shuntaro Takano

Chosaku Yoshida

Takihiro Inaba

Hisaaki Chaki

Yoichi Taniguchi

Shuichi Hirono

Shinji Makino

Tomoya Shimotori

Ichiro Oshio

Hironori Kotsubo

Tadashi Tanaka

Mikako Miyajima

Mari Yamamoto

Tadakazu Takakura

Hiroshi Kuroda

Kimiko Morimoto

Keiichi Tsuchida

Morihiro Nishio

Disclosed are use of a benzophenone derivative represented by general formula (I) or a salt thereof and one or more immunosuppressing agents in combination, and a pharmaceutical composition containing the benzophenone derivative or a salt thereof and one or more immunosuppressing agents. The use and the composition are useful for treatment or prevention of autoimmune diseases and the like. (In the formula, Rrepresents an optionally substituted heterocyclic group, a substituted phenyl group or the like; Z represents an alkylene group or the like; Rrepresents a carboxyl group, which may be protected by an alkyl group, or the like; Rrepresents an optionally protected hydroxyl group or the like; Rrepresents an optionally substituted cycloalkyloxy group or the like; and Rrepresents a hydrogen atom or the like.)

Method of utilization of combination of benzophenone derivative or salt thereof and immunosuppressing agent, and pharmaceutical composition comprising these components

Pharmaceutical agents characterized by containing benzophenone derivatives represented by the general formula: wherein the each substituent is as defined in the specification, or salts thereof have suppressive effect on RANKL production, suppressive effect on OPG reduction and inhibitory effects on differentiation/activation of osteoclasts, and are extremely useful for treating, for example therapy and/or prevention, of various diseases in which differentiation/activation of osteoclast are involved, such as osteoporosis.

Drug containing benzophenone derivative or its salt

A benzophenone derivative represented by the following formula: wherein

Benzophenone derivatives or salts thereof

A compound or a salt thereof having the atom corresponding to Nand the two or more atoms selected from N, N, Nand N, said atoms constitute the pharmacophore represented by the following formula: 

Compounds and medicinal use thereof

Spiro compounds or salts thereof and preventives/remedies for autoimmune diseases and AP-1 inhibitors containing the same

Autoimmune diseases, cell adhesion inhibition and immunomodulation are treated or effected by a method, comprising, treating a patient with a therapeutically effective amount of a 4H-1-benzopyran-4-one compound represented by the following formula or a salt thereof: ##STR1## wherein R.sup.1 is an unsubstituted or halogen-substituted alkyl, alkenyl or aryl group; R.sup.2 is a hydrogen atom or an alkyl or acyl group; R.sup.3 is a hydrogen or halogen atom or a cyano, azido, carboxyl, hydroxyl, formyl or alkoxycarbonyl group or a substituted or unsubstituted alkyl, alkoxy, phenoxy, cycloalkyl, carbamoyl, amino or phenyl group; R.sup.4 is a hydrogen or halogen atom, a nitro, cyano, carboxyl, acyl, hydroxyl or alkoxycarbonyl group, or a substituted or unsubstituted alkyl, alkoxy, alkylthio, phenylthio, alkynyl, alkenyl, sulfamoyl, alkanesulfonyl, alkanesulfonyl, amidino, phenyl or heterocyclic group or a group of the formula ##STR2## where R.sup.6 is a hydrogen atom, a hydroxyl, cyano or alkoxycarbonyl group or a substituted or unsubstituted alkyl, cycloalkyl, phenyl, amino, acyl, carbamoyl, alkanesulfonyl, iminomethyl or amidino group and R.sup.7 is a hydrogen atom or a substituted or unsubstituted alkyl, alkoxy, phenyl, cycloalkyl or heterocyclic group, or R.sup.6 and R.sup.7, when taken together with the nitrogen atom to which the two are bonded, form a 3- to 7-membered, substituted or unsubstituted heterocyclic group; R.sup.5 is a substituted or unsubstituted phenyl, thienyl, furyl or pyridyl group; Z is an oxygen or sulfur atom or an imino group; and the broken line means a single or double bond.

Immunomodulator, cell adhesion inhibitor, and agent for treating, and

Immunomodulator, cell adhesion inhibtor, and agent for treating, and

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Toyama, Japan

Yukihiko Aikawa