Mitsubishi Tanabe Pharma Corporation

Sanofi-aventis

Sanofi-synthelabo

Mitsubishi Pharma Corporation

Keiichi Aritomo

Kazutoshi Watanabe

Masahiro Okuyama

Fumiaki Uehara

Yoshihiro Usui

Aya Shoda

Shinsuke Hiki

Toshiyuki Kohara

Mitsuru Ooizumi

Kenji Fukunaga

Yoshiyuki Aoki

Masahiro Eda

Kazuki Nakayama

Daiki Sakai

Satoshi Yokoshima

Satoshi Kaneko

Tomoko Kuroda

Koichi Yamakoshi

A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C&#x2014;X; X represents hydrogen atom or fluorine atom; Ris hydrogen atom or a C-Calkyl group; L represents single bond or a C-Calkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; Rrepresents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).

Pyrimidone derivatives

The problem of the present invention is to provide a compound having a GR selective binding activity, which shows less action on other nuclear receptors such as progesterone receptor (PR), mineralocorticoid receptor (MR) and the like. The present invention provides a condensed tetrahydroquinoline compound represented by the following formula (I) 

Condensed tetrahydroquinoline derivative and use thereof for medical purposes

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. 

3-substituted-4-pyrimidone derivatives

Growing community of inventors

Tokyo, Japan

Keiichi Aritomo