Nihon Nohyaku Co., Ltd.

Pitney Pharmaceuticals Pty Limited

Tomokazu Hino

Nobuharu Andoh

Koji Tanaka

David Lawson Morris

Roger Aston

Osamu Sanpei

Tetsuo Toga

Hiroshi Hamaguchi

Atsushi Kanaoka

Kenji Tsubata

Tateki Nishida

Hiroki Kodama

Takeshi Katsuhira

Koki Mametsuka

Toshihiko Shigenari

Yasuko Yamada

The present invention relates to an anticancer agent having a high safety and a superior anticancer activity, and anticancer agent containing, as an active ingredient, an aminoacetonitrile compound represented by the formula (I) wherein Ris a hydrogen atom, an alkyl group and the like, R, R, and Rare the same or different and each is a hydrogen atom, an alkyl group and the like, Rand Rare the same or different and each is a hydrogen atom, a halogen atom and the like, m is 0 or 1, R is a halogen atom, a cyano group, a nitro group, a phenyl group optionally substituted by an alkyl group and the like, an alkyl group and the like, Aris a phenyl group, a naphthyl group, a pyridyl group, a pyrazolyl group, or the like, each of which is optionally substituted by a halogen atom, a cyano group, a nitro group, alkyl group and the like, and W is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, or &#x2014;N(R)&#x2014; wherein Ris a hydrogen atom, a (C-C)alkyl group and the like, or a pharmacologically acceptable salt thereof. 

Anti-cancer agent comprising aminoacetonitrile compound as active ingredient

The present invention relates to an anticancer agent having a high safety and a superior anticancer activity, and an anticancer agent containing, as an active ingredient, an aminoacetonitrile compound represented by the formula (I) wherein Ris a hydrogen atom, an alkyl group and the like, R, R, and Rare the same or different and each is a hydrogen atom, an alkyl group and the like, Rand Rare the same or different and each is a hydrogen atom, a halogen atom and the like, m is 0 or 1, R is a halogen atom, a cyano group, a nitro group, a phenyl group optionally substituted by an alkyl group and the like, an alkyl group and the like, Aris a phenyl group, a naphthyl group, a pyridyl group, a pyrazolyl group, or the like, each of which is optionally substituted by a halogen atom, a cyano group, a nitro group, alkyl group and the like, and W is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, or &#x2014;N(R)&#x2014; wherein Ris a hydrogen atom, a (C-C) alkyl group and the like, or a pharmacologically acceptable salt thereof.

Anticancer agent comprising aminoacetonitrile compound as active ingredient

The present invention relates to an anticancer agent having a high safety and a superior anticancer activity, and an anticancer agent containing, as an active ingredient, an aminoacetonitrile compound represented by the formula (I) wherein Ris a hydrogen atom, an alkyl group and the like, R, R, and Rare the same or different and each is a hydrogen atom, an alkyl group and the like, Rand Rare the same or different and each is a hydrogen atom, a halogen atom and the like, m is 0 or 1, R is a halogen atom, a cyano group, a nitro group, a phenyl group optionally substituted by an alkyl group and the like, an alkyl group and the like, Aris a phenyl group, a naphthyl group, a pyridyl group, a pyrazolyl group, or the like, each of which is optionally substituted by a halogen atom, a cyano group, a nitro group, alkyl group and the like, and W is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, or &#x2014;N(R)&#x2014; wherein Ris a hydrogen atom, a (C-C)alkyl group and the like, or a pharmacologically acceptable salt thereof. 

A haloalkylsulfonanilide derivative represented by general formula (I) or a salt thereof wherein Rrepresents a halo(C-C)alkyl group, R, R, R, R, R, R, R, Rand Rrepresent hydrogen atoms, etc., n represents 1 or 2, A represents an oxygen atom, W represents an oxygen atom, X represents a halogen atom and m represents an integer of 0 to 4, are compounds useful as herbicides having both of remarkable herbicidal effect and characteristics such as excellent crop-weed selectivity. General formula (I): 

Haloalkylsulfonanilide derivatives or salt thereof, herbicide comprising the derivatives as active ingredient, and use of the herbicide

The present invention provides a process for producing 2-halobenzoic acids of the general formula (I), characterized by reacting a benzoic acid of formula (II) with a halogenating agent in the presence of Pd catalyst: (wherein A is &#x2014;OH, &#x2014;OM (M is alkali metal), &#x2014;N(R)R(Rand Rare each H, C&#x2013;Calkyl, optionally substituted phenyl, or the like); R is H, C&#x2013;Calkyl, C&#x2013;Calkylcarbonyl, carboxyl, C&#x2013;Calkoxycarbonyl, optionally substituted phenylcarbonyl, or the like; n is 0 to 4; X is Cl, Br or I, or alternatively (R)n may be present on benzene-constituting carbon atoms adjacent to each other and form a C&#x2013;Calkylene- or C&#x2013;Calkenylene-fused ring).

Process for the preparation of 2-halobenzoic acids

The present invention relates to a hydrazone derivative represented by the general formula (I) shown below: ##STR1## wherein the substituents are as defined in the specification, processes for preparing the derivative, and uses of the derivative as an insecticide. The hydrazone derivative has a marked insecticidal effect on insect pests, especially against LEPIDOPTERA and COLEOPTERA.

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Kawachinagano, Japan

Tomokazu Hino