Mitsui Toatsu Chemicals, Incorporated

Mitsui Toatsu Kagaku Kabushiki Kaisha

Makoto Odate

Tsuneji Suzuki

Nobuyuki Fukazawa

Kengo Otsuka

Takashi Tsuruo

Wakao Sato

Hiroyuki Yamashita

Hajime Iizuka

Takuo Nakano

Akira Matsubara

Hiroshi Kawazura

Yoshio Shiga

Hideaki Sakai

Hiroshi Namekawa

Tatsuro Yokoyama

Yoshitsugu Kohno

Toshio Suganuma

Yoshimasa Ike

Atsushi Kojima

Heterocyclic compounds useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells are disclosed, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.

Quinoline derivatives

Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.

Heterocyclic compounds and anticancer-drug potentiaters conaining them

2-Pyrazoline derivatives of the formula (A): ##STR1## where R.sup.1 is a pyridyl, a pyrazyl or an alkoxyl group; and R.sup.2 is a hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group, and to a process for producing the same. Therapeutic agents for treating cerebrovascular diseases containing, as the active ingredient, a 2-pyrazoline derivative represented by the formula (G): ##STR2## where R.sup.3 is a hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcabonyl, a thienylcarbonyl, a pyrazylocarbonyl, an N-substituted carbamoyl, an N-substituted thiocarbamoyl, or carboxyl group; and R.sup.4 is a hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group or a pharmaceutically acceptable salt thereof. These therapeutic agents cope with cerebral edemas in the acute stage of cerebral apoplexy and regulates the whole-body and intracranial body circulation, thereby protecting ischemic lesions and minimizing the spread to affected parts.

Pyrazolone derivatives for treating cerebrovascular diseases

2-Pyrazoline derivatives of the formula (A): ##STR1## where R.sup.1 is a pyridyl, a pyrazyl or an alkoxy group; and R.sup.2 is a hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group, and to a process for producing the same. Therapeutic agents for treating cerebrovascular diseases containing, as the active ingredient, a 2-pyrazoline derivative represented by the formula (G): ##STR2## where R.sup.3 is a hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcarbonyl, a thienylcarbonyl, a pyrazylcarbonyl, an N-substituted carbamoyl, an N-substituted thiocarbamoyl, or carboxy group; and R.sup.4 is a hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group or a pharmaceutically acceptable salt thereof. These therapeutic agents cope with cerebral edemas in the acute stage of cerebral apoplexy and regulates the whole-body and intracranial body circulation, thereby protecting ischemic lesions and minimizing the spread to affected parts.

Pyrazoline derivatives for treating cerebrovascular diseases

A cephalosporanic acid of the general formula ##STR1## wherein A represents ##STR2## and the pharmaceutically acceptable salt and ester thereof.

Cephalosporins

Disclosed is a quinoline derivative having the general formula ##STR1## where A represents a six-membered hydrocarbon ring; X represents an oxygen atom, an .dbd.NOR.sup.1 group in which R.sup.1 is a hydrogen atom or a lower alkyl radical of from 1 to 5 carbon atoms, a hydroxyl group, or an --NHR.sup.2 group in which R.sup.2 is a hydrogen atom or an acyl group; and Y represents a hydrogen atom, a salt-forming radical, or an ester-forming radical. This quinoline derivative is a novel compound which has antiallergic effects in itself and is useful as an intermediate in the production of penicillin or cephalosporin derivatives.

4-Hydroxy-5,6,7,8-tetrahydroquinoline-3-carboxylic acids and derivatives

A process for efficiently preparing 1-(2-tetrahydrofuryl)-5-fluorouracil useful as an antitumor agent or an antiviral agent which comprises reacting 5-fluorouracil with 2,3-dihydrofuran. This reaction proceeds advantageously in the presence of a reaction accelerator such as a Lewis acid in a polar solvent such as pyridine.

Process for the preparation of 1-(2-tetrahydrofuryl)-5-fluorouracil

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Yokohama, Japan

Makoto Odate