Other

Taiho Pharmaceutical Company Limited

Yamasa Shoyu Kabushiki Kaisha

Eiichi Fujita

Yoshimitsu Nagao

Tetsuji Asao

Andrew T McPhail

Tomoyuki Mori

Chin-Chih Chiang

Han-Chin Ling

Ming L King

Takao Ikeda

Takehisa Inoue

Chieko Murayama

Masahito Ochiai

Substantially pure compounds having the general formula ##STR1## wherein (1) ##STR2## R.sup.2 is .beta.-hydroxy and R.sup.3 and R.sup.4 together form an oxygen bridge, or (2) ##STR3## R.sup.2 and R.sup.3 together form an additional carbon-carbon bond, and R.sup.4 is hydroxy, are disclosed. These compounds exhibit antileukemic activity against P388 lymphocytic leukemia in CDF.sub.1 mice and inhibitory activity in vitro against cells derived from human epidermoid carcinoma of the nasopharynx(KB) cells.

1H-Cyclopenta[b]benzofuran derivative and its analog

A novel optically active diamide derivative represented by the following general formula is provided, which is useful as a starting material for asymmetric synthesis of optically active compounds, ##STR1## wherein R.sup.1 is an acyclic or cyclic, divalent atomic group containing at least one carbon atom which will, upon substitution of one of the heterocyclic groups in the formula with a nucleophilic reagent, stand as an asymmetric center in the substitution product; R.sup.2 is a substituent which has such a configuration and a molecular size that the regioselectivity in the substitution reaction of the heterocyclic group with the nucleophilic reagent can be determined by a stereo-chemical interaction thereof with the substituent R.sup.1, the steric configuration of the two asymmetric carbon atoms to which the R.sup.2 substituents are attached being identical; X is a sulfur atom or an oxygen atom; and n is an integer which is 1 or 2. Such a diamide derivative can be prepared by subjecting the corresponding dicarboxylic acid or an anhydride thereof to a condensation reaction with the corresponding heterocyclic compound in the presence of a condensation agent. The optically-active diamide derivative can be used in the reaction with a nucleophilic reagent to obtain an optically-active compound. The resulting compound can be further modified by subjecting it to reaction with another nucleophilic reagent or to hydrolysis.

Optically-active diamide derivatives

Nitrobenzoic acid amide derivative represented by the formula ##STR1## wherein A is (CH.sub.2).sub.x NH(CH.sub.2).sub.y or (CH.sub.2).sub.x NH(CH.sub.2).sub.y NH(CH.sub.2).sub.z, n is 1 or 2, x, y and z are each 2 to 5, and pharmacologically acceptable acid salt thereof is an excellent radio-sensitizer.

Radiosensitizing nitrobenzoic acid amide derivatives

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Kyoto, Japan

Eiichi Fujita