Shionogi Company Limited

Takami Murashi

Hiroyuki Kai

Akira Kugimiya

Masahiko Fujioka

Yuki Tachibana

Koji Hanasaki

Akira Takase

Shinji Suzuki

Hideyuki Takenaka

Michio Masuko

Toshikazu Ohtsuka

Naohiro Onodera

Minoru Tomida

The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): 

Sulfonamide derivative having PGD2 receptor antagonistic activity

The present invention relates to 2-imino-1,3-thiazine derivatives, in specific, 2-imino-1,3-thiazine derivatives having a selective antagonistic activity or agonistic activity to a cannabinoid type 2 receptor and their pharmaceutical use.

2-imino-1,3-thiazine derivatives

A compound of the formula (I) having a binding activity to the cannabinoid type 2 receptor:wherein Ris optionally substituted heterocyclic group or the like; Rand Reach is independently hydrogen or the like; m is an integer of 0 to 2; A is optionally substituted aromatic carbocyclic group or the like.

Medicinal composition containing 1,3-thiazine derivative

It is found out that compounds represented by general formula (I) bind selectively to cannabinoid 2 receptor (CB2R) and thus exhibit CB2R antagonism or CB2R agonis wherein R represents optionally substituted alkylene; R represents hydrogen, alkyl, a group represented by the formula &mdash;C(&boxH;R )&mdash;R (wherein R represents O or S; and R represents alkyl, alkoxy, alkylthio, etc.) or a group represented by the formula SO R (wherein R represents allyl, etc.); m is an integer of from 0 to 2; and A represents optionally substituted aryl, etc.

An &agr;-substituted phenylacetic acid derivative useful as an agricultural fungicide, represented by general formula (I), or a salt thereof, a process for producing the same, an intermediate for the production thereof, and an agricultural fungicide containing the same as the active ingredient, wherein R,represents halogen, alkyl, OH, alkylthio, alkylsulfinyl, alkylsulfonyl, amino or nitro; Q represents aryl, heterocycle, mono- or disubstituted methyleneamino, (substituted amino-)methyl, alkyl, alkenyl, alkynyl, substituted carbonyl or substituted sulfonyl; X represents hydrogen, halogen, alkyl or OH; Y represents OH, alkylthio or amino; Z represents oxygen or sulfur; M represents oxygen, S(O)i (i being 0, 1 or 2), NR,(R,being hydrogen, alkyl or acyl) or a single bond; and n represents 0, 1 or 2.

&agr;-substituted phenylacetic acid derivative, its production and agricultural fungicide containing it

A process for producing a compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen or alkyl, and R is hydrogen or alkyl, which comprises removing the protective group (P) of hydroxyl of a compound of the formula (II): ##STR2## wherein P is a protective group of hydroxyl, .about. indicates an E-isomer, Z-isomer or a mixture thereof, and the other symbols are as defined above; and an intermediate for the production of the compound of the formula (I).

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Osaka, Japan

Takami Murashi