Fujisawa Pharmaceutical Company, Ltd.

Astellas Pharma Gmbh

Minoru Sakurai

Kiyoshi Taniguchi

Yasuyo Tomishima

Hisashi Takasugi

Naoaki Fujii

Kenichi Washizuka

Akito Tanaka

Kouji Hattori

Hiroaki Mizuno

Daisuke Tanabe

Takanobu Araki

Masashi Imanishi

Shinji Ito

Susumu Toda

Naomi Hanioka

Hirofumi Ishikawa

Hajime Sogabe

Kumi Hosoi

Takayuki Suzuki

Masayoshi Murata

Hiroshi Kayakiri

Hiroyuki Moritomo

Noriyuki Kawano

Wataru Hamaguchi

Kazunori Tsubaki

Hitoshi Hamashima

Nobuyuki Shiraishi

Satoru Kuroda

Norio Hashimoto

Hiroaki Ohtake

Shimpei Kawakami

Ryuichi Sekioka

Yutaka Nakajima

Takumi Okamoto

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

The present invention relates to a compound of the formula [I]: wherein (a), in which &#x2014;Y&#x2014;, R, Rand RareReach as defined in the description, etc., Ris hydrogen, halogen, lower alkyl, hydroxy, etc., Ris hydrogen, lower alkyl or hydroxy(lower)alkyl, Ris hydrogen or an amino protective group,is hydrogen, lower alkyl, cyclo(lower)alkyl, lower R9 alkenyl, &#x2014;Z&#x2014;Ror (b), in which &#x2014;Z&#x2014; is &#x2014;0&#x2014;, &#x2014;S&#x2014;, R&#x2014;SO&#x2014; or &#x2014;SO&#x2014;, and each Ris independently hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and Ris -D-E-R, in which -D- is &#x2014;CONHSO&#x2014; or &#x2014;S0NHCO&#x2014;, E is bond or lower alkylene, and Ris halogen, cyano, carboxy, etc., or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of ulcer, overactive bladder, and the like. 

Aminoalcohol derivatives

The present invention relates to a compound formula[I]: wherein  The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Propanolamine derivatives

The present invention relates to a compound formula (I) wherein X is bond or &mdash;O&mdash;CH &mdash;, (II) or (III) R is hydrogen or an amino protective group, a is phenyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s), and B is hydrogen; halogen; lower alkyl; lower alkoxycarbonyl; cyclo(lower)alkyl; or a heterocyclic group, naphthyl, 1,2,3,4-tetrahydronaphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s), or a salt thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiures or urinary incontinence.

Amidino substituted tetrahydrobenzo thiophene or furan derivatives and their use as urokinase inhibitors

Benzothiophene derivatives, their preparation and use as urokinase

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Osaka, Japan

Minoru Sakurai