Nihon Nohyaku Co., Ltd.

Pitney Pharmaceuticals Pty Limited

Osamu Sanpei

Nobuharu Andoh

Koji Tanaka

David Lawson Morris

Roger Aston

Tomokazu Hino

Tetsuo Toga

Kazuyuki Sakata

Kenji Tsubata

Hiroki Kodama

Masahiro Uehara

Nobuyuki Niino

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 process for producing a substituted aminoquinazolinone derivative of formula (I), characterized by reducing a substituted iminoquinazolinone derivative of formula (II) with hydrogen in the presence of a catalyst and either of a halogen compound and a sulfur compound; a substituted iminoquinazolinone derivative of formula (II'); and a pest control agent containing the derivative of formula (II&#x2032;) or a salt thereof as an active ingredient and a method of using the same (in the formulae, R represents hydrogen, formyl, (C-C) alkyl, (C-C)alkoxy(C-C)alkyl, (C-C) alkylsulfonyl, optionally substituted phenylcarbonyl, etc.; Rrepresents an optionally substituted, 5- or 6-membered heterocycle having one to three heteroatoms selected among oxygen, sulfur, and nitrogen; Rrepresents hydrogen or (C-C) alkyl; X and X&#x2032; may be the same or different and each represents (C-C) haloalkyl, (C-C) haloalkoxy, etc.; n is an integer of 0; and n&#x2032; is an integer of 1-4).  

Process for producing substituted aminoquinazolinone derivative, intermediate therefor, and pest control agent

Process for production of thioalkylamine derivatives

An aminoacetonitrile derivative of the formula (I):

Growing community of inventors

Kawachinagano, Japan

Osamu Sanpei