JP2006151956A5 - - Google Patents

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JP2006151956A5
JP2006151956A5 JP2005309217A JP2005309217A JP2006151956A5 JP 2006151956 A5 JP2006151956 A5 JP 2006151956A5 JP 2005309217 A JP2005309217 A JP 2005309217A JP 2005309217 A JP2005309217 A JP 2005309217A JP 2006151956 A5 JP2006151956 A5 JP 2006151956A5
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benzazepine
ylidene
tetrahydro
benzoyl
trifluoromethyl
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JP2005309217A
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Japanese (ja)
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JP4765545B2 (en
JP2006151956A (en
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Claims (1)

請求項１記載の医薬組成物のうち、
(2Z)-N-(2-アミノ-2-オキソエチル)-2-{4,4,7-トリフルオロ-1-[4-{[(2R)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}アセトアミド、
(2Z)-N-(2-ヒドロキシエチル)-2-{4,4,7-トリフルオロ-1-[4-{[(2S)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}アセトアミド、
(2Z)-N-(2-ヒドロキシエチル)-2-{4,4,7-トリフルオロ-1-[4-{[(2R)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}アセトアミド、
(2Z)-2-{4,4-ジフルオロ-1-[4-{[(2R)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}-N-[(2S)-2,3-ジヒドロキシプロピル]アセトアミド、
3-[((2Z)-2-{4,4,7-トリフルオロ-1-[4-{[(2R)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}アセチル)アミノ]プロパンアミド、
(2Z)-N-[(2R)-2,3-ジヒドロキシプロピル]-2-{4,4,7-トリフルオロ-1-[4-{[(2R)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}アセトアミド、
(2Z)-N-(2-アミノ-2-オキソエチル)-2-{4,4,7-トリフルオロ-1-[4-{[(2S)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}アセトアミド、
(2Z)-2-{1-[4-(2,2-ジフルオロプロポキシ)-2-(トリフルオロメチル)ベンゾイル]-4,4-ジフルオロ-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}-N-(2-ヒドロキシエチル)アセトアミド、
(2Z)-2-{4,4-ジフルオロ-1-[4-{[(2S)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}-N-(2-ヒドロキシエチル)アセトアミド、
(2Z)-2-{4,4-ジフルオロ-1-[4-{[(2R)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}-N-(2-ヒドロキシエチル)アセトアミド、
(2Z)-2-{1-[4-(2,2-ジフルオロプロポキシ)-2-(トリフルオロメチル)ベンゾイル]-4,4,7-トリフルオロ-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}-N-(2-ヒドロキシエチル)アセトアミド、
(2Z)-N-[(2R)-2,3-ジヒドロキシプロピル]-2-{4,4,7-トリフルオロ-1-[4-プロポキシ-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}アセトアミド、
(2Z)-2-{4,4-ジフルオロ-1-[4-{[(2S)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}-N-[(2S)-2,3-ジヒドロキシプロピル]アセトアミド、
(2Z)-2-{4,4-ジフルオロ-1-[4-{[(2R)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}-N-[(2R)-2,3-ジヒドロキシプロピル]アセトアミド、
3-[((2Z)-2-{4,4,7-トリフルオロ-1-[4-{[(2S)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}アセチル)アミノ]プロパンアミド、
(2Z)-N-[(2R)-2,3-ジヒドロキシプロピル]-2-{4,4,7-トリフルオロ-1-[4-{[(2S)-2-フルオロプロピル]オキシ}-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}アセトアミド、
3-[((2Z)-2-{1-[4-(2,2-ジフルオロプロポキシ)-2-(トリフルオロメチル)ベンゾイル]-4,4,7-トリフルオロ-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}アセチル)アミノ]プロパンアミド、
(2Z)-2-{4,4-ジフルオロ-1-[4-プロポキシ-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}-N-[(2R)-2,3-ジヒドロキシプロピル]アセトアミド、若しくは、
(2Z)-2-{4,4-ジフルオロ-1-[4-プロポキシ-2-(トリフルオロメチル)ベンゾイル]-1,2,3,4-テトラヒドロ-5H-1-ベンゾアゼピン-5-イリデン}-N-[(2S)-2,3-ジヒドロキシプロピル]アセトアミド、
又はその製薬学的に許容される塩を有効成分とする医薬組成物。


Among the pharmaceutical compositions according to claim 1,
(2Z) -N- (2-Amino-2-oxoethyl) -2- {4,4,7-trifluoro-1- [4-{[(2R) -2-fluoropropyl] oxy} -2- ( Trifluoromethyl) benzoyl] -1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene} acetamide,
(2Z) -N- (2-hydroxyethyl) -2- {4,4,7-trifluoro-1- [4-{[(2S) -2-fluoropropyl] oxy} -2- (trifluoromethyl ) Benzoyl] -1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene} acetamide,
(2Z) -N- (2-hydroxyethyl) -2- {4,4,7-trifluoro-1- [4-{[(2R) -2-fluoropropyl] oxy} -2- (trifluoromethyl ) Benzoyl] -1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene} acetamide,
(2Z) -2- {4,4-Difluoro-1- [4-{[(2R) -2-fluoropropyl] oxy} -2- (trifluoromethyl) benzoyl] -1,2,3,4- Tetrahydro-5H-1-benzazepine-5-ylidene} -N-[(2S) -2,3-dihydroxypropyl] acetamide,
3-[((2Z) -2- {4,4,7-trifluoro-1- [4-{[(2R) -2-fluoropropyl] oxy} -2- (trifluoromethyl) benzoyl] -1 , 2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene} acetyl) amino] propanamide,
(2Z) -N-[(2R) -2,3-Dihydroxypropyl] -2- {4,4,7-trifluoro-1- [4-{[(2R) -2-fluoropropyl] oxy}- 2- (trifluoromethyl) benzoyl] -1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene} acetamide,
(2Z) -N- (2-amino-2-oxoethyl) -2- {4,4,7-trifluoro-1- [4-{[(2S) -2-fluoropropyl] oxy} -2- ( Trifluoromethyl) benzoyl] -1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene} acetamide,
(2Z) -2- {1- [4- (2,2-difluoropropoxy) -2- (trifluoromethyl) benzoyl] -4,4-difluoro-1,2,3,4-tetrahydro-5H-1 -Benzazepine-5-ylidene} -N- (2-hydroxyethyl) acetamide,
(2Z) -2- {4,4-Difluoro-1- [4-{[(2S) -2-fluoropropyl] oxy} -2- (trifluoromethyl) benzoyl] -1,2,3,4- Tetrahydro-5H-1-benzazepine-5-ylidene} -N- (2-hydroxyethyl) acetamide,
(2Z) -2- {4,4-Difluoro-1- [4-{[(2R) -2-fluoropropyl] oxy} -2- (trifluoromethyl) benzoyl] -1,2,3,4- Tetrahydro-5H-1-benzazepine-5-ylidene} -N- (2-hydroxyethyl) acetamide,
(2Z) -2- {1- [4- (2,2-difluoropropoxy) -2- (trifluoromethyl) benzoyl] -4,4,7-trifluoro-1,2,3,4-tetrahydro- 5H-1-Benzazepine-5-ylidene} -N- (2-hydroxyethyl) acetamide,
(2Z) -N-[(2R) -2,3-dihydroxypropyl] -2- {4,4,7-trifluoro-1- [4-propoxy-2- (trifluoromethyl) benzoyl] -1, 2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene} acetamide,
(2Z) -2- {4,4-Difluoro-1- [4-{[(2S) -2-fluoropropyl] oxy} -2- (trifluoromethyl) benzoyl] -1,2,3,4- Tetrahydro-5H-1-benzazepine-5-ylidene} -N-[(2S) -2,3-dihydroxypropyl] acetamide,
(2Z) -2- {4,4-Difluoro-1- [4-{[(2R) -2-fluoropropyl] oxy} -2- (trifluoromethyl) benzoyl] -1,2,3,4- Tetrahydro-5H-1-benzazepine-5-ylidene} -N-[(2R) -2,3-dihydroxypropyl] acetamide,
3-[((2Z) -2- {4,4,7-trifluoro-1- [4-{[(2S) -2-fluoropropyl] oxy} -2- (trifluoromethyl) benzoyl] -1 , 2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene} acetyl) amino] propanamide,
(2Z) -N-[(2R) -2,3-Dihydroxypropyl] -2- {4,4,7-trifluoro-1- [4-{[(2S) -2-fluoropropyl] oxy}- 2- (trifluoromethyl) benzoyl] -1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene} acetamide,
3-[((2Z) -2- {1- [4- (2,2-difluoropropoxy) -2- (trifluoromethyl) benzoyl] -4,4,7-trifluoro-1,2,3, 4-tetrahydro-5H-1-benzazepine-5-ylidene} acetyl) amino] propanamide,
(2Z) -2- {4,4-Difluoro-1- [4-propoxy-2- (trifluoromethyl) benzoyl] -1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene } -N-[(2R) -2,3-dihydroxypropyl] acetamide, or
(2Z) -2- {4,4-Difluoro-1- [4-propoxy-2- (trifluoromethyl) benzoyl] -1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene } -N-[(2S) -2,3-dihydroxypropyl] acetamide,
Or a pharmaceutical composition comprising a pharmaceutically acceptable salt thereof as an active ingredient.


JP2005309217A 2004-10-27 2005-10-25 Pharmaceutical composition comprising a benzazepine derivative as an active ingredient Expired - Fee Related JP4765545B2 (en)

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JP2005309217A JP4765545B2 (en) 2004-10-27 2005-10-25 Pharmaceutical composition comprising a benzazepine derivative as an active ingredient

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JP2004311901 2004-10-27
JP2004311901 2004-10-27
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RS56804B1 (en) 2012-06-11 2018-04-30 Tacurion Method for producing 4,4,7-trifluoro-1,2,3,4-tetrahydro-5h-1-benzazepine compound and intermediate for synthesis thereof
AU2017296338A1 (en) 2016-07-14 2019-01-03 Pfizer Inc. Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme

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JPH04334403A (en) * 1991-05-10 1992-11-20 Toto Ltd Cast molding die for washing basin or the like
PL182011B1 (en) * 1993-08-26 2001-10-31 Yamanouchi Pharma Co Ltd Benzazepine derivative, pharmaceutic composition and intermediate compounds
JP3215910B2 (en) * 1994-06-15 2001-10-09 大塚製薬株式会社 Benzoheterocyclic derivatives
JP3599403B2 (en) * 1995-02-24 2004-12-08 山之内製薬株式会社 A new method for producing benzazepine derivatives

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