Astellas Pharma Gmbh

Seldar Pharma Inc.

Yamanouchi Pharmaceutical Company Ltd.

Tsukasa Ishihara

Norio Seki

Hiroyuki Hisamichi

Fukushi Hirayama

Yuji Koga

Keizo Sugasawa

Itsuro Shimada

Takafumi Shimizu

Tomofumi Takuwa

Kyoichi Maeno

Noriko Ishikawa

Takeshi Shigenaga

Hiroyuki Koshio

Yuzo Matsumoto

Souichirou Kawazoe

Ryota Shiraki

Shunichiro Hachiya

Kazuhiro Ikegai

Ryuichi Takezawa

Ikumi Kuriwaki

Nobuaki Takeshita

Takeshi Kadokura

Minoru Okada

Koyo Matsuda

Eiji Kawaminami

Toru Yoden

Masafumi Kudou

Masashi Funatsu

Tomihisa Kawasaki

Masahiko Isaka

Yoshiaki Shimada

Hirotoshi Kakuta

Hiroshi Moritani

To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.

Tetrahydroisoquinolin-1-one derivative or salt thereof

A method for preventing or treating a disease selected from the group consisting of visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, and fibromyalgia in a subject in need thereof, comprising administering to said subject an effective amount of the compound of the following formula (I) or a salt thereof: wherein R, R, R, R, R, X and n are as described herein.

Benzothiophene compound

The present invention is directed to compounds of Formula I: 

[Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). [Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.

To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-methyl-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4'-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.

Diazepan derivatives or salts thereof

There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4'-bromo-2&#x2032;-[(5-chloro-2-pyridyl) carbamoyl]-6&#x2032;-&#x3b2;-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2&#x2032;-(2-acetamido-2-deoxy-&#x3b2;-D-glucopyranosyloxy)-4&#x2032;-bromo-6&#x2032;-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.

Substituted benzene derivatives or salts thereof

There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4'-bromo-2&#x2032;-[(5-chloro-2-pyridyl)carbamoyl]-6&#x2032;-&#x3b2;-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2&#x2032;-(2-acetamido-2-deoxy-&#x3b2;-D-glucopyranosyloxy)-4&#x2032;-bromo-6&#x2032;-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.

To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-&lsqb;(3-carbamimidoylphenylamino)methyl&rsqb;-3-&lsqb;4-(4-METHYL-1,4-diazepan-1-yl)benzoylamino&rsqb;benzoic acid and 3-hydroxy-4&prime;-methoxy-2-&lcub;&lsqb;4-(4-methyl-1,4-diazepan-1-yl)benzoyl&rsqb;amino&rcub;benzanilide or a salt thereof is an effective ingredient.

Hexahydro-1,4-diazepine derivatives represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs containing the same as the active ingredient, such as activated blood coagulation factor X inhibitor, wherein A: phenylene, pyridylene, or the like; B: a 5- or 6-membered aryl or heteroaryl ring; X: &mdash;CO&mdash;, &mdash;CONH&mdash;, &mdash;CSNH&mdash;, &mdash;SO,&mdash;, &mdash;SO,NH&mdash;, or the like; Y: a bond or alkylene; R,: hydrogen, alkyl, &mdash;Y&mdash;(hetero) aryl, or the like; R,: hydrogen, alkoxy, &mdash;COOH, or the like; R,: amidino or a group capable of being converted into amidino; and R,, R,: each independently hydrogen or lower alkyl.

Hexahydro-1,4-diazepine derivatives or salts thereof

Quinuclidine derivative having tricyclic hetero condensed ring

Azole derivative and pharmaceutical composition thereof

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Tokyo, Japan

Tsukasa Ishihara