Astellas Pharma Gmbh

Yohei Koganemaru

Koichi Yonezawa

Wataru Hamaguchi

Isao Kinoyama

Takuya Washio

Takehiro Miyazaki

Ryo Sato

Satoshi Aoki

Hiroshi Yamada

Noriyuki Kawano

Satoshi Miyamoto

Naoyuki Masuda

Akio Kamikawa

Kazuhiko Iikubo

Shigeki Kunikawa

Shinya Nagashima

Ryosuke Munakata

Shimpei Kawakami

Kiyohiro Samizu

Tetsuo Kiso

Ryuichi Sekioka

Takahiro Kuramochi

Yuka Koizumi

Junya Ohmori

Osamu Kaneko

Takashi Ogiyama

Shuichirou Kakimoto

Junichi Shishikura

Keisuke Tamaki

Yasuyuki Mitani

Keni Ni

Ryoji Hirabayashi

[Problem] Provided is a compound having a positive allosteric modulating activity (PAM activity) on an &#x3b1;7 nicotinic acetylcholine receptor (&#x3b1;7 nACh receptor). [Means for Solution] The present inventors have studied on a PAM activity on an &#x3b1;7 nACh receptor, and they have found that a tetrahydrooxepinopyridine compound has a PAM activity on an &#x3b1;7 nACh receptor, thereby completing the present invention. The tetrahydrooxepinopyridine compound of the present invention has a PAM activity on an &#x3b1;7 nACh receptor and can be expected as an agent for preventing or treating dementia, cognitive impairment, schizophrenia, Alzheimer's disease, CIAS, negative symptoms of schizophrenia, inflammatory diseases, or pain.

Tetrahydrooxepinopyridine compound

To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-HTreceptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a N atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-HTreceptor regulating action and an excellent pharmacological action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed.

Tetrahydroisoquinoline derivative

[Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HTreceptor modulating action, is provided. [Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z, Z, Z, Zand Zis nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HTreceptor modulating actions and excellent pharmacological actions based on the 5-HTreceptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed. 

Nitrogenous-ring acylguanidine derivative

[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

To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.

2-aminobenzamide derivatives

Growing community of inventors

Tokyo, Japan

Yohei Koganemaru