Shionogi Company Limited

Kenji Kawada

Mitsuaki Ohtani

Fumihiko Watanabe

Susumu Kamata

Akinori Arimura

Nobuhiro Haga

Ryuji Suzuki

Tatsuo Tsuri

Tadahiko Tsushima

Masayuki Narisada

Kaoru Seno

Sanji Hagishita

Kimio Takahashi

Morio Kishi

Yasumasa Goh

Tadadiko Tsushima

The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R&#x2013;Rare hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is &#x2014;O&#x2014;, &#x2014;CH&#x2014;, &#x2014;NR&#x2014; or &#x2014;S(O)p- and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.

Para-terphenyl compounds

The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R&#x2013;Rare hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is &#x2014;O&#x2014;, CH&#x2014;, &#x2014;NR&#x2014; or &#x2014;S(O)&#x2014; and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.

P-terphenyl compounds

The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R&#x2013;Rare hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is &#x2014;O&#x2014;, &#x2014;CH&#x2014;, NR&#x2014; or &#x2014;S(O)p&#x2014; and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.

The present invention provides a pharmaceutical composition for use as a Th2 differentiation inhibitor comprising a compound represented by Formula (I):wherein each of ring A, ring B and ring C is an aromatic carbocyclic ring, a heterocyclic ring and the like, X is a single bond, &#x2014;O&#x2014;, &#x2014;CH&#x2014;, &#x2014;NH&#x2014;, &#x2014;SO&#x2014; and the like, Y is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl and the like, each of Vand Vis a single bond, &#x2014;O&#x2014;, &#x2014;NH&#x2014;, &#x2014;OCH&#x2014; and the like, a prodrug, pharmaceutically acceptable salt or solvate thereof.

Th2 differentiation inhibitors

The present invention relates to a 15-deoxyprostaglandin derivative of the formula (I): ##STR1## in which ##STR2## is a 5 membered ring which is selected from a group consisting of ##STR3## R.sup.1 is hydrogen or lower alkyl; R.sup.2 is C.sub.6 -C.sub.12 alkyl, C.sub.6 -C.sub.12 alkenyl or C.sub.6 -C.sub.12 alkadienyl; provided that the compound of the following formula is excluded: ##STR4## wherein R' is hydrogen or methyl; or pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical formulation comprising a 15-deoxyprostaglandin derivative as an active ingredient, which is useful as an intraocular pressure reducing agent.

Treatment for hypertension or glaucoma in eyes

The present invention relates to a method for treating hypertension or glaucoma in the eye comprising contacting the surface of the eye with a therapeutic amount of a 15-deoxyprostaglandin derivative of the formula (I): ##STR1## in which ##STR2## is a 5 membered ring which is selected from a group consisting of ##STR3## R.sup.1 is hydrogen or lower alkyl; R.sup.2 is C.sub.6 -C.sub.12 alkyl, C.sub.6 -C.sub.12 alkenyl or C.sub.6 -C.sub.12 alkadienyl or a pharmaceutically acceptable salt thereof. The invention also relates to a kit for delivery of a topical solution for treatment of glaucoma which comprises (a) container having a solution including a compound of the formula (I), and (b) means for topical delivery of said solution to the eye in a controlled dosage.

There are provided compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen or C.sub.1 -C.sub.5 alkyl; R.sub.2 is an C.sub.1 -C.sub.10 alkyl, aryl, aralkyl, or pyridyl, where the aryl, aralkyl, or pyridyl are unsubstituted or are substituted by C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, nitro, hydroxy, carboxy, amino, C.sub.1 -C.sub.5 alkylamino, C.sub.1 -C.sub.5 dialkyamino whose two alkyl groups may be different from each other, C.sub.2 -C.sub.3 alkanoylamino, or halogen and X is an C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.7 alkenylene, --CH(F)CH.dbd.CH(CH.sub.2).sub.3 --, --(CH.sub.2).sub.3 --S--(CH.sub.2).sub.2 --, --(CH.sub.2).sub.2 --S--(CH.sub.2).sub.3 --, --C.sub.6 H.sub.4 -O--CH.sub.2 -- or --CH.sub.2 CH.dbd.CH--m--C.sub.6 H.sub.4 --, or their pharmaceutically accepatble salts. The compounds are useful as antithrombotic, anti-vasconstricting and anti-bronchoconstricting drugs.

6-oxa and thiabicyclo [3.1.0.] compounds

There are provided compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen or C.sub.1 -C.sub.5 alkyl; R.sub.2 is an C.sub.1 -C.sub.10 alkyl, aryl, aralkyl, or pyridyl, where the aryl, aralkyl, or pyridyl are unsubstituted or are substituted by C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, nitro, hydroxy, carboxy, amino, C.sub.1 -C.sub.5 alkylamino, C.sub.1 -C.sub.5 dialkylamino whose two alkyl groups may be different from each other, C.sub.2 -C.sub.3 alkanoylamino, or halogen and X is an C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.7 alkenylene, --CH(F)CH.dbd.CH(CH.sub.2).sub.3 --, --(CH.sub.2).sub.3 --S--(CH.sub.2).sub.2 --, --CH.sub.2).sub.2 --S--(CH.sub.2).sub.3 --, --C.sub.6 H.sub.4 --O--CH.sub.2 --or --CH.sub.2 CH.dbd.CH--m--C.sub.6 H.sub.4 --, or their pharmaceutically acceptable salts. The compounds are useful as antithrombotic, anti-vasoconstricting and anti-bronchoconstricting drugs.

Bicyclo (2.2.1.) hept-exo-2-yl and bicyclo (2.2.2.) oct-endo-2-yl

Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or hetelocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms and may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.

7-oxabicyclo[2.2.1] heptane sulfonamide derivatives

Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or heterocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms an may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene, oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.

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Osaka, Japan

Kenji Kawada