Astellas Pharma Gmbh

Icagen, Inc.

Ayako Moritomo

Takeshi Suzuki

Xiaodong Wang

Kerry Leigh Spear

Takahiro Ishii

Alan Bradley Fulp

Darrick Seconi

Takayuki Suzuki

Noriyuki Kawano

Hiroyuki Moritomo

Wataru Hamaguchi

Minoru Sakurai

Hiroyoshi Yamada

Nobuyuki Shiraishi

Eisuke Nozawa

Shimpei Kawakami

Hirotsune Itahana

Ryuichi Sekioka

Koichiro Harada

Shinobu Akuzawa

Takaho Matsuzawa

Xiadong Wang

To provide a compound useful as an active ingredient of a pharmaceutical composition for treating 11&#x3b2;-hydroxysteroid dehydrogenase type 1-related diseases such as dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance and the like. [Means for Solution] A bicyclic heterocyclic compound (the bicyclic heterocycle is formed when a cyclohexane ring is fused with a 5- to 6-membered monocyclic heterocycle that has only a nitrogen atom as a hetero atom) substituted with an acylamino group such as a (hetero)aroylamino group or the like or a pharmaceutically acceptable salt thereof was found to have an excellent selective inhibitory action against 11&#x3b2;-HSD1. Accordingly, the bicyclic heterocyclic compound of the present invention can be used for treating dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance, and the like.

Bicyclic heterocyclic compound

[Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HTreceptor and 5-HTreceptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HTreceptor and 5-HTreceptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HTreceptor and 5-HTreceptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.

Acylguanidine derivative or salt thereof

The present invention provides a genus of polycyclic pyrazines of formula (I): wherein A and B are independently substituted or unsubstituted 5- or 6- membered heterocycloalkyl, or substituted or unsubstituted 5- or 6- membered heteroaryl, Wis Wis &#x2014;CH&#x2550;, &#x2014;NH&#x2014;, &#x2014;N&#x2550;, &#x2014;S&#x2014;, or &#x2014;O&#x2014;; Zis Zis &#x2014;CH&#x2550;, &#x2014;NH&#x2014;, &#x2014;N&#x2550;, &#x2014;S&#x2014;, or &#x2014;O&#x2014;; Y is a bond, &#x2014;CH&#x2550;N&#x2014;NH&#x2014;, &#x2014;NH&#x2014;CH, or &#x2014;NR&#x2014;; s and t are independently integers from 1 to 4; and the substituents R, R, Rand Rare as defined in the specification for compounds of formula (I). The polycyclic pyrazine compounds are useful as modulators of potassium ion channels in both therapeutic and diagnostic methods.

Polycyclic pyrazines as potassium ion channel modulators

The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.

Polycyclic pyrimidines as potassium ion channel modulators

Growing community of inventors

Ibaraki, Japan

Ayako Moritomo