Shionogi Company Limited

Gaku Sakaguchi

Akira Kato

Kazuo Ueda

Akihiro Hori

Naotake Kobayashi

Naohiro Itoh

Hidekazu Haraguchi

Ken Yasui

Shinji Suzuki

Akira Yukimasa

Yasuhiko Kanda

Yuji Koriyama

Yuuji Kooriyama

Satoshi Orita

Akihiko Saiga

Kouichi Okumura

Hisanaga Igarashi

Shuji Yonezawa

A composition having BACE 1 inhibitory activity containing a compound represented by the formula (I): 

Aminodihydrothiazine derivatives

A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I): 

Pharmaceutical composition for treating alzheimer's disease

A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): 

The present invention provides a compound which has an effect of inhibiting amyloid-&#x3b2; production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-&#x3b2; proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; Ris a group such as optionally substituted lower alkyl; Ris a group such as hydrogen; and Rand Rare each independently a group such as hydrogen, provided that the following compound is excluded. 

2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity

A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I); wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;

Pharmaceutical composition for treating Alzheimer's disease

A composition having BACE 1 inhibitory activity containing a compound represented by the formula (I): wherein ring A is an optionally substituted heterocyclic group;E is lower alkylene;X is S;Ris a hydrogen atom or lower alkyl;R, R, R, R, Rand Ris each independently a hydrogen atom, halogen, or hydroxy etc.;n and m are each independently an integer of 0 to 3;n+m is an integer of 0 to 3;Ris a hydrogen atom or substituted lower alkyl;or its pharmaceutically acceptable salt thereof.

A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;

A DNA molecule having a gene expression repressing function derived from human T-cell leukemia virus type I (HTLV-I) existing in a region which is missing in a mutant provirus that is expressing p21Xm RNA but exists in the genome of a complete provirus, and a plasmid including the DNA molecule are provided. Furthermore, a novel protein (TRP-1) which specifically binds to U5RE and a structural gene for the protein is provided, which can be useful for elucidation of the transcription repression activity and elucidation of the oncogenesis mechanism of neurocytes, in which a transcriptional repressive region (U5RE) existing in the U5 region of human T-cell leukemia virus type I gene LTR is involved. Furthermore, an expression vector including the gene, a transformant into which the expression vector is introduced, and a process for producing the TRP-1 protein using the transformant are provided.

Growing community of inventors

Shiga, Japan

Gaku Sakaguchi