Astellas Pharma Gmbh

Junya Ohmori

Noriyuki Kawano

Daisuke Suzuki

Satoshi Miyamoto

Shingo Yamasaki

Naoyuki Masuda

Takatoshi Kanayama

Kazushi Watanabe

Satoshi Hayashibe

Nobuyuki Shiraishi

Kazuhiko Iikubo

Hiroaki Hoshii

Yohei Koganemaru

Kiyohiro Samizu

Ryo Mizoguchi

Takenori Kimura

Noritaka Hamada

Makoto Kasai

Yasuyuki Mitani

Keni Ni

[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

Anytime obtained is uniform crystal of N-(4-fluorophenyl)-N'-phenyl-N&#x2033;-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound A) and/or N,N&#x2032;-bis (4-fluorophenyl)-N&#x2033;-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound B) as a medicament or a starting material for the preparation of the medicament, and provided are a fumarate of the compound A and/or the compound B having excellent stability and a novel crystal thereof. A salt of the compound A and/or the compound B with fumaric acid enables uniform crystal to be anytime obtained, and thus, it is a compound that is very useful as a medicament or a starting material for the preparation of the medicament having excellent stability.

Salt of 1,3,5-triazine-2,4,6-triamine derivative

Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain. A novel compound or a salt thereof, which is characterized in that it has an amino group and R(lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3 -dihydro-1-benzofuran, 2,3-dihydro-1-benzothiophene, indoline ring, or the like, and has Rand R(the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.

Aminoindane derivative or salt thereof

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Tokyo, Japan

Junya Ohmori