Ss Pharmaceutical Co., Ltd.

Hisamitsu Medical Co., Ltd.

Mari Ohtsuka

Susumu Sato

Hiroyuki Mizuno

Hiroyuki Hirota

Tadayuki Kuraishi

Teruo Komoto

Kinichi Mogi

Fumio Ishii

Hidehiko Koya

Akihiro Shibata

Koichi Yokoi

Hidehiko Kohya

Koichi Tachibana

Yoshihiko Kanamaru

Hiroyuki Naito

Hideaki Matsuda

Tatsuhiko Katori

Sunao Takeda

Haruyoshi Honda

Yoshiyuki Takahashi

Kazuo Isomae

Fujiko Konno

Kazuhiko Irinoda

Noriyuki Kawamoto

Yoshihiro Nagao

Hitoshi Nakazawa

The invention is directed to an imidazole derivative represented by formula (1):wherein each of Rand Rrepresents an aryl group, a heteroaryl group, etc.; each of A, X, and Xrepresents N or CH; each of Y and Z represents O, S, etc.; each of R, R, and Rrepresents a hydrogen atom, an alkyl group, etc.; m is a number of 1 to 4; and n is a number of 0 to 4, or a salt thereof. The invention is also directed to a drug containing the derivative or the salt as an active ingredient. These compounds exert excellent effects of inhibiting production of NO and IL-6 and are useful for preventing or treating diseases induced by overproduction of NO and IL-6.

Imidazole derivatives or salts thereof and drugs containing the derivatives or the salts

Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

Substituted benzylurea derivatives and medicine containing the same

A diamine-platinum (IV) complex represented by the following formula (1): ##STR1## wherein R.sup.1 and R.sup.2 together represent R.sup.5 O--CH(CH.sub.2 NH.sub.2).sub.2 (R.sup.5 represents hydrogen, acetyl, trifluoroacetyl, benzoyl, cycloalkylcarbonyl or methanesulfonyl) or a C.sub.5-8 1,2-cycloalkanediamine; R.sup.3 and R.sup.4 each represents hydrogen or R.sup.6 CO-- (R.sup.6 represents alkyl, halogenoalkyl, cycloalkyl, aryl or aralkyl); and two X's together represent a malonic acid residue or glycolic acid residue which may have a substituent capable of coordinating to the platinum in formula (1) by an O,O-coordination or an N-acylamino acid residue coordinating to the platinum in formula (1) by an O,N-coordination; and a pharmaceutical composition comprising as an active ingredient the above-described diamine-platinum (IV) complex.

Platinum (IV) complex and pharmaceutical composition comprising the same

Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

Substituted vinylurea derivatives and medicine containing the same

A platinum complex represented by the following formula (1): ##STR1## wherein the all symbols are defined in the disclosure; and a malignant tumor treating drug which contains the complex as an active ingredient. The platinum complex is excellent in antitumor effects and safety and is highly soluble in water, and therefore it is useful as an agent for use in the treatment of various malignant tumors.

Platinum complex and malignant tumor treating drug containing the same

An arylamide derivative of formula (1), a salt thereof and a therapeutic agent for hyperlipemia which comprises the derivative or salt: ##STR1## wherein Ar represents a group ##STR2## a naphthyl group, a pyridinyl group, a furyl group, a thienyl group, a quinolyl group or an indolyl group; Y represents a group ##STR3## and Q represents --O-- or a single bond, Z represents an alkylene group, and R.sup.4 represents a hydroxyl group, an alkoxy group or a group --NH(CH.sub.2).sub.m COOH.

Piperazine substituted carboxylic acid derivatives for treating

A diamine-platinum complex represented by the following formula (1): ##STR1## wherein the all definitions are defined in the disclosure, and a malignant tumor treating drug which contains the above complex as an active ingredient. The diamine-platinum complex has a high water solubility and an excellent antitumor effect.

An arylamide derivative of formula (1), a salt thereof and a therapeutic agent for hyperlipemia which comprises the derivative or salt: ##STR1## wherein Ar represents a group ##STR2## a naphthyl group, a pyridinyl group, a furyl group, a thienyl group, a quinolyl group or an indolyl group; Y represents a group ##STR3## and Q represents --O-- or a single bond, Z represents an alkylene group, and R.sup.4 represents a hydroxyl group, an alkoxy group or a group --NH(CH.sub.2).sub.m COOH, useful for the treatment and prevention of hyperlipemia due to their excellent cholesterol reducing action, triglyceride reducing action and high safety.

Arylamide derivatives for treating hyperlipemia

A method of curing or alleviating hepatic disease comprising administrating to the patient 1,3-dithiole-2-thione or 1,3-dithiolane-2-thione is disclosed. Adminstration of the compound can be made in various dosing forms, including tablets, granules, powders, capsules, suspensions, injections, and suppositories. Normal dosing amount can be determined from the range of 0.01 to 50 mg/kg/day for oral administration, and 0.002 to 10 mg/kg/day for injection or other forms of administration.

Method of curing hepatic disease

Growing community of inventors

Narashino, Japan

Mari Ohtsuka