Fujisawa Pharmaceutical Company, Ltd.

Astellas Pharma Gmbh

Kenichi Washizuka

Minoru Sakurai

Masayoshi Murata

Kouji Hattori

Daisuke Tanabe

Masashi Imanishi

Takanobu Araki

Shinji Ito

Susumu Toda

Hiroshi Kayakiri

Toshiyuki Chiba

Kiyoshi Taniguchi

Fumiyuki Shirai

Naoaki Fujii

Hitoshi Hamashima

Motohiro Hino

Yasuyo Tomishima

Satoru Kuroda

Hiroaki Ohtake

Yutaka Nakajima

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.

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.

Preparation of optically active 3-substituted azetidinones of the formula (I) ##STR1## in which R.sup.1 is a hydroxy-protective group wherein an allylic alcohol of the formula (II) ##STR2## is acylated, then subjected to asymmetric enzymatic hydrolysis yielding the R-allylic alcohol. The hydroxyl group is protected and then stereoselectively reacted with an amine which is subsequently cyclized to yield the desired 3-substituted azetidinone. Two new species of microorganisms have been isolated, Pimelobacter sp. No. 1254 and Bacillus megaterium No. 1253 which exhibit stereoselective esterase activity.

Enzymatic process for preparing optically active 3-substituted

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Osaka, Japan

Kenichi Washizuka