Mitsubishi Kasei Corporation

Mitsubishi Chemical Corporation

Mitsubishi Pharma Corporation

Sanofi-aventis

Sanofi-synthelabo

Ryoichi Ando

Yasuhiro Morinaka

Chizuko Takahashi

Yoshikuni Tamao

Akihiro Tobe

Kazutoshi Watanabe

Aya Shoda

Naoko Ando

Hirokazu Masuda

Jonathan Reid Frost

Adrien Tak Li

Fumiaki Uehara

Toshiro Sakaki

Keiichi Arimoto

Makoto Kawamura

Eiichi Nakamura

Toshiro Sasaki

Antonio Almario Garcia

Ken-ichi Saito

Noriko Chiba

Antonio Almario Carcia

Yoshiyuki Fujimura

Rie Kawamoto

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 the formula (I) or a salts thereof: wherein Rrepresents an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group and the like; Rrepresents a hydrogen atom, hydroxyl group, an alkyl group, an alkenyl group and the like, Rrepresents a pyridyl group, and a medicament comprising said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as Alzheimer disease.

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.

2-amino-3-(alkyl)-pyrimidone derivatives as GSK3.&#x3b2;.inhibitors

Amide derivatives

A novel ketone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.

Ketone derivatives

Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infarction, stroke, Alzheimer's disease, amyotrophia, osteoporosis, hypercalcemia or the like.

Sulfonamide derivatives

Aminoketone derivatives according to the present invention strongly inhibit thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L or the like and have excellent properties concerning absorbance on oral administration, tissue distribution and cell membrane permeability. The aminoketone derivatives cart thus be used as therapeutic agents for treating muscular dystrophy, cataract, cardiac infarction, stroke, Alzheimer's disease, amyotrophy, osteoporosis and hypercalcemia and so on. It may also be used as therapeutic agents for preventing metastasis of cancer. In addition, the present derivatives are also applicable as intermediates for the preparation of ketone derivatives, which have inhibitory activity against thiol protease.

Aminoketone derivatives

Alpha-aminoketone derivatives of the present invention strongly inhibit thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L and calpain or the like and have excellent properties in absorbance on oral administration, tissue distribution and cell membrane permeability. The alpha-aminoketone derivatives can thus be used as therapeutic agents for treating muscular dystrophy, amyotrophy, cardiac infarction, stroke, Alzheimer's disease, disturbance of consciousness or dyskinesia caused upon brain trauma, multiple sclerosis, peripheral nervous neuropathy, cataract, inflammation, allergosis, fulminant hepatitis, osteoporosis, hypercalcemia, breast carcinoma, prostatic carcinoma or prostatomegaly. They may also be used as therapeutic agents for suppressing growth of cancer cells, preventing metastasis of cancer or suppressing aggregation of plaques.

.alpha.-aminoketone derivatives

A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.

Cyclopropenone derivatives

The cyclopropene derivatives of the present invention are useful as the intermediates for producing cyclopropenone derivatives exhibiting strong inhibition activity of thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L and the like.

Cyclopropene derivatives

Growing community of inventors

Machida, Japan

Ryoichi Ando