Raqualia Pharma Inc.

Pfizer Corporation

Fuji Yakuhin Co., Ltd

Bihoku Funka Kogyo Co., Ltd.

Tadashi Inoue

Yuji Shishido

Mikio Morita

Yoshimasa Arano

Satoshi Nagayama

Tatsuya Yamagishi

Kazunari Nakao

Hirotaka Tanaka

Misato Hirano

Takeshi Hanazawa

Hirohide Noguchi

Kaoru Shimada

Shuzo Watanabe

Hitoshi Kato

Takahiro Sato

Hiroaki Ito

Kiyoshi Kawamura

Hiroyuki Nakano

Junichiro Uda

Tadashi Kawashima

Yoshiyuki Iwabuchi

Sachiho Miyata

Takashi Kodama

Takamitsu Kandou

Satoshi Nahayama

Yorihiko Matsubara

The purpose of the present invention is to provide a solid pharmaceutical preparation of excellent stability and producibility, the preparation including, as an active ingredient, 3-(3,5-dichloro-4-hydroxybenzoyl)-1,1-dioxo-2,3-dihydro-1,3-benzothiazole. This solid pharmaceutical preparation contains 3-(3,5-dichloro-4-hydroxybenzoyl)-1,1-dioxo-2,3-dihydro-1,3-benzothiazole or a pharmaceutically acceptable salt thereof and a sugar alcohol and/or a cellulose derivative.

Solid pharmaceutical preparation

The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blocker such as Naand Na, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved. 

Aryl substituted carboxamide derivatives as calcium or sodium channel blockers

To provide crystal polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, which is a useful pharmaceutical, and a production method therefor. Through purification of a corresponding salt, recrystallization, or storage under humidified conditions, three different crystal forms; i.e., crystalline polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile are produced.

4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile crystalline polymorph and production method therefor

The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Naand Na, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved. 

The present invention relates to aryl carboxamide derivatives of formula (I), wherein Aris phenyl; Aris aryl; n is 1-4; X is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014; or &#x2014;SO&#x2014;, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved. 

Aryl carboxamide derivatives as TTX-S blockers

The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.

Picolinamide derivatives as TTX-S blockers

Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HTreceptor. The compound and salt are useful for treatment or prevention of various diseases and conditions associated with a 5-HTreceptor. 

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This invention provides a compound of the formula (I): wherein A and B are independently CRor N; D and E are each independently CRor N; Rrepresents (C-C)alkyl; Rrepresents hydrogen, halogen, hydroxy, (C-C) alkyl, halo(C-C) alkyl, hydroxy(C-C) alkyl, (C-C)alkoxy or (C-C)alkoxy-(C-C)alkyl; R, R, R, R, Rand Reach independently represent hydrogen, halogen, (C-C)alkyl, halo(C-C)alkyl, (C-C)alkoxy, hydroxy(C-C)alkyl or (C-C)alkoxy-(C-C)alkyl; or Rand Rare taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; Rand Reach independently represent hydrogen, halogen, (C-C)alkyl, halo(C-C)alkyl, hydroxy(C-C)alkyl, (C-C)alkoxy, hydroxy(C-C)alkoxy, (C-C)alkoxy-(C-C)alkyl, (C-C)alkoxy-(C-C)alkoxy, (C-C)alkylthio, (C-C)alkylsulfinyl, (C-C)alkylsulfonyl, NH, [(C-C)alkyl]NH&#x2014;, [(C-C)alkyl]N&#x2014;, HN&#x2014;(C-C)alkoxy, (C-C)alkyl-NH&#x2014;(C-C)alkoxy, [(C-C)alkyl]N(C-C)alkoxy; HN&#x2014;(C-C)alkoxy-(C-C)alkyl, (C-C)alkyl-NH&#x2014;(C-C)alkoxy-(C-C)alkyl, [(C-C)alkyl]N(C-C)alkoxy-(C-C)alkyl or 5- or 6- membered heterocyclic ring containing at least one nitrogen atom; Rrepresents halogen, (C-C)alkyl, halo(C-C)alkyl, hydroxy(C-C)alkyl, (C-C)alkoxy, hydroxy(C-C)alkoxy, (C-C)alkoxy-(C-C)alkyl, (C-C)alkoxy-(C-C)alkoxy, halo(C-C)alkylsulfonyl, halo(C-C)alkylsulfinyl, halo(C-C)alkoxy, halo(C-C)alkylthio, [(C-C)alkyl]NH&#x2014; or [(C-C)alkyl]N&#x2014;; or Rand R, when E is CR, are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C-C)alkyl, (C-C)alkoxy and hydroxy(C-C)alkyl; and Rrepresents hydrogen, halogen, (C-C)alkyl or hydroxy(C-C)alkyl; or a pharmaceutically acceptable salt or solvate thereof.

Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists

This invention provides a compound of the formula (I): wherein, variables A, B, D, E, and Rto Rare as defined in the specification.

This invention provides compounds of the formula (I) useful for the treatment of disease conditions caused by over activation of Vr1 receptors such as pain or the like in mammals as well as compositions comprising them.

Substituted N-sulfonylaminophenylethyl-2-phenoxyacetamide compounds as VR1 receptor antagonists

Compounds of the general formula (I): pharmaceutical compositions comprising a compound of general formula (I); and methods of treating disease conditions caused by overactivation of the VR1 receptor by administering a compound of general formula (I) to a subject.

Substituted aryloxymethyl bicyclicmethyl acetamide compounds

This invention provides a compound of the formula (I): wherein Rrepresents a (C&#x2013;C)alkyl group; Rrepresents a hydrogen atom, a halogen atom, a hydroxy group, a (C&#x2013;C)alkyl group or a (C&#x2013;C)alkoxy group; R, R, Rand Reach independently represents a hydrogen atom, a (C&#x2013;C)alkyl, or a halogen atom; Rrepresents a hydrogen atom, a halogen atom, a hydroxy group, a (C&#x2013;C)alkyl group optionally substituted with a piperidino group, a (C&#x2013;C)alkoxy group optionally substituted with a 3&#x2013;7 membered cycloalkyl ring, a hydroxy(C&#x2013;C)alkoxy group, a (C&#x2013;C)alkoxy-(C&#x2013;C)alkyl group, a (C&#x2013;C)alkoxy-(C&#x2013;C)alkoxy group, a halo (C&#x2013;C)alkyl group, a (C&#x2013;C)alkylthio group, a (C&#x2013;C)alkylsulfinyl group or a (C&#x2013;C)alkylsulfonyl group; Rrepresents a (C&#x2013;C)alkyl group, a halo(C&#x2013;C)alkyl group, a (C&#x2013;C)alkoxy group, a hydroxy(C&#x2013;C)alkoxy group, a (C&#x2013;C)alkoxy-(C&#x2013;C)alkyl group or a (C&#x2013;C)alkoxy-(C&#x2013;C)alkoxy group; or Rand R, when adjacent to each other, taken together with the carbon atoms to which they are attached form a 5&#x2013;8 membered carbocyclic or heterocyclic ring, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents selected from the group consisting of a hydroxy group, a (C&#x2013;C)alkyl group, a (C&#x2013;C)alkoxy group and a hydroxy(C&#x2013;C)alkyl group; and Rrepresents a hydrogen atom or a halogen atom; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor, such as pain or the like in mammalian. The present invention also provides a pharmaceutical composition comprising the compound of formula(I).

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Aichi, Japan

Tadashi Inoue