Ajinomoto Co., Ltd.

Masataka Shoji

Ryota Yoshimoto

Tadakiyo Nakagawa

Kazuyuki Sagi

Chikahiko Eguchi

Takashi Kayahara

Shunji Takehana

Yumiko Fukuda

Kaoru Yoshida

Shingo Makino

Akira Takahara

Akira Kamimura

Kozo Toyota

Hideki Domoto

Hiroshi Yamamoto

Hideki Matsumoto

Naoyuki Fukuchi

Munetaka Tokumasu

Mitsuo Takahashi

Sayaka Asari

Masaru Takayanagi

Shinichi Fujita

Tetsuo Yano

Itsuya Tanabe

Youji Yamada

Masaki Hashimoto

Harumi Arisaka

Yoshikatsu Koyama

Masahiro Yamanashi

Yosikatsu Koyama

Akira Hirasawa

Yuichi Gyotoku

The present invention provides a piperidine derivative represented by the following formula or analogs thereto, which are used for agents for treating or preventing various diseases related to 5-HT7. 

Piperidine derivative

Benzamidine derivatives of the following formulae or analogs thereof, i.e., pharmaceutically acceptable salts thereof, are provided. These compounds or salts thereof have a blood-coagulation inhibiting effect based on an excellent effect of inhibiting the action of activated blood coagulation factor X, and they are useful as anticoagulants 

Benzamidine derivatives

Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated blood-coagulation factor X, and they are useful as agents for preventing or treating various diseases caused by thrombi or emboli.

Benzamidine derivative

The present invention also relates to a method of using these novel materials, and other materials, to treat or prevent a disease caused by serotonin or a method of treating or preventing platelet aggregation. The compounds used are piperidine derivatives having the formula (I): ##STR1## wherein the various substituents are defined below.

Piperidine derivatives and anti-platelet agents containing the same

A piperidine compound of the formula (I): ##STR1## wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH.sub.2).sub.n, which may be substituted, in which n is 0 or an integer of 1 to 10, --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3)--, --N(COOC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO--, or --SO.sub.2 --; Y is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CO--, --O--, --S--, --NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, --CH(OH)CH.sub.2 -- or --CH(OH)CH(OH)--; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the --(CH.sub.2)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3), --N(COC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO-- or --SO.sub.2 --, and wherein one or more of the --(CH.sub.2)-groups in X and Q may be substituted by --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 -- thereby forming a ring structure.

Piperidine derivatives and hypotensives containing the same

An ethylamine derivative of formula (I): ##STR1## wherein A represents a carbon atom or a nitrogen atom;

Ethylamine derivatives and antihypertensives containing the same

A piperidine derivative of general formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein ##STR2## is any of several specified aromatic-containing groups; X is selected from one of several hetero atom-containing groups or C.sub.2 alkylene or a cyano-containing group; and Q is phenyl, cyclohexyl, piperidinyl, tetrahydropyranyl, pyridyl, pyrrolyl, N-methylpyrrolyl, thienyl, furyl, 1-hexyl, or cyano; from 1 to 3 hydrogen atoms in Q may be independently substituted by alkyl of from 1 to 3 carbon atoms, perfluoroalkyl of from 1 to 3 carbon atoms, acylamino of from 1 to 6 carbon atoms, perfluoroacylamino of from 1 to 3 carbon atoms, alkoxy of from 1 to 3 carbon atoms, alkanesulfonylamino of from 1 to 3 carbon atoms, perfluoroalkanesulfonylamino of from 1 to 3 carbon atoms, acetoxy of from 1 to 3 carbon atoms, aminocarbonyl, aminosulfonyl, fluoro, chloro, cyano, hydroxy, nitro, amino, imidazolylmethyl, cinnamoylamino, p-fluorobenzoyl, cyanomethyl, cyanoethyl, methoxyacetoxy, alkoxycarbonyl of from 1 to 3 carbon atoms; 1 is an integer of from 0 to 1; m is an integer of from 0 to 1; n is an integer of from 0 to 6. The derivatives are useful as antiarrhythmic agents.

Piperidine compounds and their use as antiarrhythmic agents

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Kawasaki, Japan

Masataka Shoji