Mitsubishi Tanabe Pharma Corporation

Sanofi-Aventis

Mitsubishi Pharma Corporation

Sanofi

Sanofi-Synthelabo

Fumiaki Uehara

Kazutoshi Watanabe

Kenji Fukunaga

Toshiyuki Kohara

Aya Shoda

Shinsuke Hiki

Masahiro Okuyama

Yoshihiro Usui

Satoshi Yokoshima

Keiichi Aritomo

Jonathan Reid Frost

Adrien Tak Li

Ryoichi Ando

Mitsuru Ooizumi

Keiichi Arimoto

Antonio Almario Garcia

Kazuki Nakayama

Daiki Sakai

Hiroshi Iwamura

Koichi Yamakoshi

Antonio Almario Carcia

Shin-ichi Kusaka

A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein each Rrepresents hydrogen atom or the like; X represents oxygen atom or the like; A represents a C-Ccycloalkyl group, a C-Caryl group or a heterocyclic group; Rrepresents a halogen atom or the like; s represents 0 or an integer of 1 to 5; Q represents a pyridine ring which may be substituted or pyrimidine ring; and Rrepresents hydrogen atom or the like, 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). 

2-substituted-6-heterocyclic pyrimidone derivatives 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 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 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

Production method of an optically active morpholine compound represented by the formula 10, or a compound represented by the formula 55, which includes the following steps:  wherein each symbol is as defined in the specification. An optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4']bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.

Intermediate compound for synthesizing pharmaceutical agent and production method thereof

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

A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3&#x3b2; such as Alzheimer's disease.

2-amino-3-(alkyl)-pyrimidone derivatives

A pyrimidone derivative represented by formula (I) or a salt thereof: And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3&#x3b2; such as Alzheimer's disease.

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Tokyo, Japan

Fumiaki Uehara