Kotobuki Seiyaku Co. Ltd.

Kotobuki Pharmaceutical Co Ltd

Astellas Pharma Gmbh

Motoharu Sonegawa

Tsuyoshi Tomiyama

Akira Tomiyama

Naoto Ueyama

Tomoyuki Kawai

Shuuichi Wakabayashi

Tadashi Shirai

Hiroshi Tomiyama

Toshihiro Watanabe

Jiro Fujiyasu

Norio Asai

Takashi Yanagisawa

Yoshinori Iwai

Makoto Oku

Kazuo Tokuzaki

Kazumi Kikuchi

Hiromi Baba

Yukinori Nagakura

Makoto Haketa

Satoru Takeuchi

Takeyuki Imamaki

The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.

Nitrogen&#x2014;containing heterocyclic derivatives having 2,6-disubstituted styryl

New therapeutic agents of isoquinuclidine derivatives are represented by the following formula or its hydrochloride salts. ##STR1## (wherein R.sub.1 is hydrogen, carboxyl group, ethoxycarbonyl group, 4-(ethoxycarbonyl)phenyl group, 4-(carboxy)phenyl group, 2-(carboxy)-thiophene-5-yl group, quinoline-5-yl group, 4-(quinoline-5-yl)phenyl group or 4-(3-oxo-2-azabicyclo[2.2.2]octane-2-yl)-phenyl group; R.sub.2 is hydrogen or allyl group; Both X.sub.1 and X.sub.2 are hydrogen and X.sub.1 and X.sub.2 may form an oxo group; m stands for an integer of 0 to 2.) These compounds, have excellent inhibitory activities against squalene synthase, and are useful as a treatment agent for hypercholesterolemia.

Isoquinuclidine derivatives, method of manufacturing the same and

New therapeutic agents of cycloheptimidazole derivatives are disclosed, which are represented by the following formula or its alkali-addition salts. ##STR1## (wherein R.sub.1 represents H or isopropyl group; R.sub.2 represents a lower alkyl; R.sub.3 represents a carboxylic acid or tetrazole group. A and A.sub.1 are substituted groups at 4 or 8 position and A.sub.1 is a hydrogen or hydroxy group when A is a hydrogen or A and A.sub.1 is an oxo group. The dotted line '- - - -' is two double bonds or saturated single bonds). These compounds are useful as anti-hypertensive or anti-congestive heart failure agents.

Cycloheptimidazole derivatives, method of manufacturing the same and

Derivatives of cyclic guanidine are disclosed, which are represented by the following formula:

Cyclic guanidine derivatives, anti-ulceratives and method of

Cyclic guanidine derivatives, anti-ulceratives and methods of

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Nagano, Japan

Motoharu Sonegawa