Daiichi Sankyo Company, Limited

Btg International Limited

Yasuhiro Nakagami

Kazuhiro Yoshida

Yasunori Ono

Satoshi Komoriya

Kayoko Masuda

Emiko Hatano

Mayumi Iizuka

Takashi Ohnuki

Yuji Kasuya

Kazuo Koyama

Tatsuya Inoue

Isao Kaneko

Shinji Marumoto

Masaki Meguro

Atsunobu Sakamoto

Masako Minami

Yoko Murakami

Masaru Iwasaki

Tomiichiro Oda

Tomichiro Oda

The present invention relates to a terpenoid derivative that has the ability to activate the Keap1/Nrf2/ARE signaling pathway and is excellent in anti-inflammatory action and cytoprotective action, and a sustained-release pharmaceutical composition effective for the treatment and prevention of a posterior eye disease caused by oxidative stress, comprising the terpenoid derivative as an active ingredient. The present invention provides a local administration-type sustained-release pharmaceutical composition for the treatment or prevention of a posterior eye disease, comprising the terpenoid derivative of the present invention as an active ingredient, wherein the sustained-release pharmaceutical composition maintains a pharmacological action thereof for 1 week or longer by the sustained release of the terpenoid derivative under physiological conditions and has a base material administrable to the vitreous body and a form administrable to the vitreous body.

Sustained-release pharmaceutical composition for treatment and prevention of eye disease

It is intended to provide a novel terpenoid derivative that exhibits anti-inflammatory action and a cytoprotective action by activating the Keap1/Nrf2/ARE signaling pathway. The present invention provides terpenoid derivative A represented by the following formula (I): 

Terpenoid derivatives

The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, Rand Rare H or alkyl; Zand Zare H, alkyl, alkoxy, haloalkyl or halogeno; Zis alkoxy, SH, alkylthio, NH, mono- or di-alkylamino, OH or halogeno; Zand Zare H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

Preventives or remedies for Alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound

Pharmaceutical compositions and methods of treatment are provided for treating amyloidosis, containing, as an active ingredient, at least one nitrogen-containing heteroaryl compound represented by the following general formula or a pharmacologically permitted salt thereof; together with nitrogen-containing heteroaryl derivatives, and pharmacologically permitted salts thereof: 

Preventives or remedies for alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound

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Kobe, Japan

Yasuhiro Nakagami