Ss Pharmaceutical Co., Ltd.

Tadayuki Kuraishi

Susumu Sato

Naokata Taido

Hideaki Matsuda

Takemitsu Asaoka

Hiroyuki Mizuno

Kazuo Isomae

Masaru Matsumoto

Mari Ohtsuka

Tatsuhiko Katori

Kinichi Mogi

Haruyoshi Honda

Akihiro Shibata

Hiroshi Hasegawa

Noriaki Shioiri

Teruo Komoto

Takeshi Kotsugai

Yoichiro Ogawa

Ryuichi Kawahara

Kumiko Sekine

Minoru Tokizawa

Hiromichi Eto

Sunao Takeda

Toshiaki Nakashima

Koichi Yokoi

Hidehiko Kohya

Fujiko Konno

Tadayuki Kouda

Kazuo Yamazaki

Hiroyuki Hirota

Yoshihiko Kanamaru

Shigeru Adegawa

Hidehiko Koya

Teruo Kohmoto

Youichiro Ogawa

Teruo Koumoto

Yasushi Kaneko

Kazunori Maebashi

Terumitsu Kaihoh

Junji Okawa

Yoshikuni Ito

Masaki Ogawa

Tadatoshi Kuriyama

4-quinolinone derivative or salt thereof

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.

A 1,4-benzoxazine derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents an unsubstituted or halogen-substituted lower alkyl, unsubstituted or halogen-substituted lower alkylsulfonyl, nitro or cyano group, R.sup.2 and R.sup.3 may be the same or different and individually represent a hydrogen atom or a lower alkyl group or are fused together with the adjacent carbon atom into a 3- to 6-membered carbon ring, R.sup.4 represents a hydrogen atom or an unsubstituted or substituted lower alkyl or acyl group, R.sup.5 represents a hydrogen atom or a unsubstituted or substituted lower alkyl, lower alkenyl, lower alkoxyl, aryl, aryloxyl or heterocyclic ring group, and Y represents an oxygen or sulfur atom, with the proviso that R.sup.1 is other than a nitro or cyano group when R.sup.2 and R.sup.3 are individually a methyl group, R.sup.4 is a hydrogen atom, R.sup.5 is a 3-chloropropyl group and Y is an oxygen atom; or a salt thereof.

1,4-benzoxazine derivatives

5-aminoquinolone carboxylic acid derivative and antibacterial agent

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 quinolone carboxylic acid derivative having the following formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in living bodies, R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom, Y is CH.sub.2, O, S, SO, SO.sub.2, or N--R.sup.3, wherein R.sup.3 is a hydrogen atom or a lower alkyl group, and Z is an oxygen atom or two hydrogen atoms; or a salt thereof; and an antimicrobial agent comprising the same. The compound exhibits a superior antimicrobial activity, especially against gram positive microorganisms, and is thus useful for the treatments and prevention of various infectious diseases in clinics.

Quinoline carboxylic acid derivatives

Piperidine compounds of formula II: ##STR1## that exhibit anticholinesterase activity and are effective in treating dementia.

Piperidine compounds having anti-acetylcholinesterase activity

Quinoline derivatives of the formula, ##STR1## wherein &gt;A represents a group &gt;N--(CH.sub.2).sub.n --, &gt;C.dbd., &gt;C.dbd.CH(CH.sub.2).sub.n --, or &gt;CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group &gt;C.dbd.O or &gt;CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior anti-acetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

Quinoline derivatives

Benzo[5,6]cyclohepta[1,2-b]pyridine derivatives of the following formula: ##STR1## wherein R.sup.1 represents a cyano, carbamoyl, alkylsulfoxy, alkylsulfonyl, tetrazolyl or sulfonic acid group, and R.sup.2 represents a hydrogen atom, a cyano, phenyl, aralkyl, alkoxycarbonylalkyl, aminoalkylcarbamoylalkyl or lower alkyl group, or a group ##STR2## or --X--R.sub.4, X being an oxygen or sulfur atom, R.sup.3 standing for a hydrogen atom or a substituted or unsubstituted lower alkyl, phenyl or aralkyl group, and R.sup.4 being a substituted or unsubstituted lower alkyl, phenyl or aralkyl group or an aminoalkyl group, and salts thereof. Antiallergic and antihistamic agents containing one of the above derivatives or salts as an active ingredient are also described.

Benzo[5,6]cyclohepta[1,2-B]pyridine derivatives and antiallergic agents

Quinoline derivatives of the formula, ##STR1## wherein &gt; A represents a group &gt;N--(CH.sub.2).sub.n --, &gt;C.dbd., &gt;C.dbd.CH(CH.sub.2).sub.n --, or &gt;CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group &gt;C.dbd.O or &gt;CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior antiacetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

A process for preparing 21-desoxyprednisolone 17-esters of formula (IV) is disclosed. ##STR1## The process comprises reacting a prednisolone 17.alpha.,21-cyclic orthoester with an acid in a 40-60% lower alcohol solution to produce a prednisolone 17-ester, sulfonylating the prednisolone 17-ester into a prednisolone 17-ester 21-sulfonate, and reacting the sulfonate with an alkali metal iodide in methyl ethyl ketone in the presence of a lower fatty acid to produce the compound of formula (IV). The process ensures economical industrial production of high purity 21-desoxyprednisolone 17-esters, an excellent local anti-inflammatory medicine, in a high yield by simple procedures.

Process for preparing 21-desoxyprednisolone 17-esters

A triazole derivative is disclosed. The compound have a general formula, ##STR1## wherein R.sup.1 and R.sup.2 represent a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 together form a lower alkylene group, R.sup.3 represents a lower alkyl group, and n denotes an integer of 0 to 2, provided that not both R.sup.1 and R.sup.2 are a hydrogen atom at the same time. The triazole derivatives and their salts are effective for curing or preventing deep-seated mycoses, e.g. mycotic meningitis, mycotic infectious diseases of respiratory organs, fungemia, and urinary tract mycosis.

Triazole derivatives and a composition for treating mycoses

Growing community of inventors

Chiba, Japan

Tadayuki Kuraishi