Mitsubishi Tanabe Pharma Corporation

Sanofi-aventis

Dainichiseika Color & Chemicals Mfg. Co., Ltd.

Sanofi

Sanofi-synthelabo

Mitsubishi Pharma Corporation

Yoshihiro Usui

Kazutoshi Watanabe

Masahiro Okuyama

Fumiaki Uehara

Aya Shoda

Keiichi Aritomo

Shinsuke Hiki

Osamu Saito

Kenji Fukunaga

Toshiyuki Kohara

Yoshihiro Shigemori

Satoshi Yokoshima

Mitsuru Ooizumi

Kazuki Nakayama

Tokushi Hanano

Daiki Sakai

Koichi Yamakoshi

Shin-ichi Kusaka

A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein Rrepresents a hydrogen or the like; Rrepresents methyl group or the like; Rrepresents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; Rrepresents hydrogen or the like; Rrepresents hydrogen or the like; Rrepresents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH, oxygen atom, NH, or the like; any one or more of Rand R, Rand R, Rand R, X and R, X and R, X and R, and Rand Rmay combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

2-(cyclic amino)-pyrimidone derivatives

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor: wherein X represents CH or nitrogen atom; Rrepresents a C?1#191-C?12#191 alkyl group which may be substituted; Rrepresents a C?1#191-C?8#191 alkyl group which may be substituted, a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom, and nitrogen atom, and having 5 to 10 ring-constituting atoms in total. 

3-substituted-4-pyrimidone derivatives

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein Rrepresents a C-Calkyl group which may be substituted;R represents, for example, a group represented by the following formula (II): wherein Rand Rindependently represent a hydrogen atom or a C-Calkyl group;Rrepresents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

3-Substituted-4-pyrimidone derivatives

A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C-Calkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C-Calkyl group, an optionally partially hydrogenated C-Caryl ring, an indan ring or the like; m represents an integer of 1 to 3; each independently represents a halogen atom, a hydroxy group, a cyano group, a C-Calkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C-Calkylene group. 

2,3,6-Trisubstituted-4-pyrimidone derivatives

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein Rrepresents a C-Calkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein Rand Rindependently represent a hydrogen atom or a C-Calkyl group; Rrepresents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total. 

Non-flying plastic microballoons are produced by bringing unexpanded, expandable plastic microballoons, which have been heated to a temperature lower than an expansion starting temperature thereof, and a mixture of a wetting agent and gas, the mixture having been heated to a temperature at least equal to the expansion starting temperature of the expandable plastic microballoons, into contact with each other to cause expansion of the expandable plastic balloons, and then cooling the resulting expanded plastic balloons.

Production process of non-flying plastic mircoballoons

A process for producing non-scattering hollow plastic balloons which comprises: (a) heating a mixture (A) of non-foamed plastic balloons and a first wetting agent, which is a plasticizer, to a temperature from 40.degree. C. to a temperature which is 40.degree. C. below an exit temperature of a heat exchanger, (b) contacting the mixture (A) with a second wetting agent being heated to a temperature equal to or above the foaming starting temperature of the non-foamed plastic balloons, wherein a ratio of the mixture (A) to the second wetting agent (B) is 1:0.5 to 1:1.5, the contacting being within 1 minute after heating the mixture (A) by the heat exchanger to a temperature ranging from 20.degree. to 50.degree. C. below the foaming starting temperature of the non-foamed plastic balloons, (c) foaming the non-foamed plastic balloons, and (d) cooling the resultant mixture from step (c) containing the foamed plastic balloons. Non-scattering foamed plastic balloons can thus be obtained simultaneously with the foaming. The present process needs a smaller amount of a plasticizer than the conventional process of wetting foamed plastic balloons with a plasticizer.

Process for producing non-scattering hollow plastic balloons

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Tokyo, Japan

Yoshihiro Usui