Sanofi-aventis

Mitsubishi Tanabe Pharma Corporation

Sanofi-synthelabo

Mitsubishi Pharma Corporation

Shinsuke Hiki

Kazutoshi Watanabe

Fumiaki Uehara

Kenji Fukunaga

Toshiyuki Kohara

Masahiro Okuyama

Yoshihiro Usui

Aya Shoda

Keiichi Aritomo

Satoshi Yokoshima

Mitsuru Ooizumi

Koichi Yamakoshi

A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein Rrepresents a C-Calkyl; Rrepresents a hydrogen atom or the like; Rrepresents a halogen or the like; q represents an integer of 1 to 7; Rrepresents a halogen or the like; p represents 0 or an integer of 1 to 5; Rrepresents a C-Caryl, a heterocycle or the like; and X represents oxygen, NH, or the like, 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).

6-(pyridinyl)-4-pyrimidone derivates as tau protein kinase 1 inhibitors

A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C-Calkyl; Rrepresents a hydrogen atom, or the like; R' represents a C-Calkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C-Calkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, 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-morpholino-4-pyrimidone compound

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

Shinsuke Hiki