Shionogi Company Limited

Kaoru Seno

Sanji Hagishita

Mitsuaki Ohtani

Fumihiko Watanabe

Susumu Kamata

Nobuhiro Haga

Masayuki Narisada

Tatsuo Tsuri

Kenji Kawada

Tadahiko Tsushima

Kimio Takahashi

Morio Kishi

Takeaki Matsui

Tomoyuki Ogawa

Takashi Ono

Toshio Fujishita

Kohji Hanasaki

Takaharu Matsuura

Toshiyuki Kato

Yozo Hori

Yoshiyuki Matsuo

Minoru Ikeda

Yasunobu Ishihara

Koichi Nishi

Sanji Hagashita

A compound represented by the formula (Ia) (wherein R1, R2, and R3 to R5 are the same as defined in the description), a prodrug thereof, a pharmaceutically acceptable salt thereof, or solvate thereof. The compounds are useful in the prevention of or treatment for diseases relating to NAD(P)H.

Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same

A compound represented by the general formula:wherein Ris &#x2014;CHCOOH and the like; Ris &#x2014;COCONHand the like; Ris C4&#x2013;C6 alkyl; and the like; Ris &#x2014;CH&#x2014;Rwherein Ris aryl and the like; Ris hydrogen or C1&#x2013;C6 alkyl and the like; an optical active compound, a prodrug thereof, or a pharmaceutically acceptable salt, or a solvate having type X sPLAinhibitory effect was found.

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A composition for treating or preventing arrhythmia containing as an active ingredient a cPLAinhibitor, for example a compound represented by formula (I):wherein Ris optionally substituted aralkyl or the like; Z is &#x2014;S&#x2014; or the like; Xis &#x2014;(CH)s-N(R)&#x2014;CO&#x2014; (wherein Ris hydrogen atom or the like, s is an integer of 0 to 3) or the like; Xis optionally substituted arylene or the like; Xis a bond or the like; A, B, and E are each independently oxygen atom or sulfur atom; D is hydrogen atom or the like; Yis &#x2014;(CH)mCO&#x2014; (m is an integer of 0 to 3) or the like; Yis optionally substituted aryl or the like.

Composition for treating or preventing arrhythmia

Pyrrolidine derivatives having phospholipase A.sub.2  inhibitory activity

Pyrrolidine derivatives having phospholipase A.sub.2 inhibitory activity

Benzodiazepine derivative

Lipid derivatives represented by the formula: ##STR1## wherein R.sub.1 is alkyl or alkylcarbamoyl; R.sub.2 is lower alkyloxy, lower alkylcarbamoyloxy, lower alkylcarbonylamino, lower alkyloxycarbonylamino, lower alkylureido, lower alkyloxymethyl, lower alkylcarbonylmethyl, cyanomethyl, heterocyclic group, or heterocyclyloxy; R.sub.2 ' is hydrogen or R.sub.2 and R.sub.2 ' taken together with R.sub.2 form --O(CH.sub.2).sub.m -- wherein m is an integer of 1 to 5; R.sub.3, R.sub.4, and R.sub.5 each is hydrogen or lower alkyl or two or three of R.sub.3, R.sub.4, and R.sub.5 taken together with the adjacent nitrogen atom form cyclic ammonio; R.sub.6 is hydrogen or lower alkylcarbonyl; X.sup.- is a counter anion; Y is oxygen or sulfur; and n is an integer of 1 to 10, being useful as PAF antagonists, e.g., as antithrombotic, antivasoconstricting, antibronchoconstricting agent or antitumor agent.

Lipid derivatives

This invention relates to an optically active (+)-secondary amine of the formula: ##STR1## wherein R.sup.1 is a lower alkyl, and to a process for preparing a useful intermediate for the production of the optically active dopamine derivatives, namely, optically active (+)-primary amine of the formula: ##STR2## wherein R.sup.1 is a lower alkyl, characterized by the reduction of said optically active (+)-secondary amine.

4-(4-alkoxyphenyl)-2-butylamine derivative and process therefor

Lipid derivatives represented by the formula: ##STR1## wherein R.sub.1 is alkyl or alkylcarbamoyl; R.sub.2 is lower alkyloxy, lower alkylcarbamoyloxy, lower alkylcarbonylamino, lower alkyloxycarbonylamino, lower alkylureido, lower alkyloxymethyl, lower alkylcarbonylmethyl, cyanomethyl, heterocyclic group, or he0 terocyclyloxy; R.sub.2 ' is hydrogen or R.sub.2 and R.sub.2 ' taken together form --O(CH.sub.2).sub.m -- wherein m is an integer of 1 to 5; R.sub.3, R.sub.4, and R.sub.5 each is hydrogen or lower alkyl or two or three of R.sub.3, R.sub.4, and R.sub.5 taken together with the adjacent nitrogen atom form cyclic ammonio; R.sub.6 is hydrogen or lower alkylcarbonyl; X.sup.- is a counter anion; Y is oxygen or sulfur; and n is an integer of 1 to 10, being useful as PAF antagonists, e.g., as antithrombotic, antivasoconstricting, antibronchoconstricting agent or antitumor agent.

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 arly, aralkyl or hetelocycle; R.sub.3 is 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 alkeneylene, 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.

Bicyclic 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 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

Tetrazole derivatives represented by the formula: ##STR1## wherein R is naphthyl or phenyl optionally substituted by phenyl, lower alkyo, halogen, lower alkoxy, hydroxy or acetoxy; X is methylene, dimethylmethylene or oxygen; n is an integer of 0 or 1; and p and r each is an integer of 0 or 1 and q is an integer of 1 or 2 provided that p+q+r=2; or a tautomer in tetrazole ring and a pharmaceutically acceptable salt thereof, which are useful as TXA.sub.2 receptor antagonist.

Alkenyltetrazole derivatives

Bicyclic sulfonamide derivatives represented by the formula: ##STR1## (wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 is lower alkyl, aralkyl, or aryl which may be substituted by lower alkyl, alkoxy, acetoxy, hydroxy, halogen, nitro or phenyl; and the wavy line indicates R or S configuration or their mixture) or their salt being used as antithrombotic, antivasoconstricting, and antibronchoconstricting drugs and the process therefor.

Bicyclic sulfonamide derivatives and process therefor

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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Hyogo, Japan

Kaoru Seno