Astellas Pharma Gmbh

Comentis, Inc.

Kiyohiro Samizu

Ryosuke Munakata

Makoto Inoue

Noriyuki Kawano

Shingo Yamasaki

Hisao Hamaguchi

Hiroaki Tominaga

Lin Hong

Makoto Takeuchi

Satoshi Aoki

Masahiko Hayakawa

Takahiro Ishii

Ken Ikeda

Naoyuki Masuda

Takashi Sugane

Kazuhiko Iikubo

Yasuhiro Shiina

Yohei Koganemaru

Junya Ohmori

Yasuhiro Shina

Yasuyuki Mitani

Keni Ni

Hiromasa Oka

Hiroshi Uebayashi

The present invention provides a hydrate of N-[(4S)-2-amino-2',2&#x2032;-dimethyldispiro[1,3-oxazole-4,4&#x2032;-chromene-3&#x2032;,3&#x2033;-oxetan]-6&#x2032;-yl]-5-chloropyridine-2-carboxamide which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by &#x3b2;-secretase activity, hydrolysis of a &#x3b2;-secretase site of a &#x3b2;-amyloid precursor protein, and/or &#x3b2;-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.

Chromane compounds

The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by &#x3b2;-secretase activity, hydrolysis of a &#x3b2;-secretase site of a &#x3b2;-amyloid precursor protein, and/or &#x3b2;-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.

[Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.

Imidazo[1,2-a]pyridine derivative

A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided. The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that an azole compound substituted with an N-(pyridine-3-yl)oxycarbonyl-piperidin-4-yl group and a phenyl group or a pharmaceutically acceptable salt thereof has an excellent FAAH inhibitory activity, thereby completing the present invention. The compound of the present invention is confirmed to have an excellent FAAH inhibitory activity and an antiallodynic effect in rat models with neuropathic pain, and thus is useful as an agent for preventing and/or an agent for treating neuropathic pain.

Azole compound

There is provided an acid addition salt of (&#x2212;)-(3R)-quinuclidin-3-yl(1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate with an acid selected from the group consisting of (&#x2212;)-(2S,3S)-tartaric acid, (+)-(2S,3S)-di-O-benzoyltartaric acid, (+)-(2S,3S)-di-O-(4-methylbenzoyl)tartaric acid, (&#x2212;)-L-phenylalanine, benzenesulfonic acid, cyclohexanesulfamic acid, hydrobromic acid, naphthalene-2-sulfonic acid, sebacic acid, (+)-camphor-10-sulfonic acid, p-toluenesulfonic acid, ethanesulfonic acid, methanesulfonic acid and methyl phosphate, which has little hygroscopicity that affects the use as a drug or its drug substance, and is very useful as a drug or its drug substance.

Salts of quinuclidine derivative

Growing community of inventors

Tokyo, Japan

Kiyohiro Samizu