公开(公告)号：US08148421B2

公开(公告)日：2012-04-03

申请号：US12440540

申请日：2007-09-10

申请人： Hideo Kato ,  Osamu Nagata ,  Yoshiyuki Iwabuchi ,  Takahiro Sato ,  Junichiro Uda ,  Tutomu Inoue ,  Hiroshi Nakamura ,  Nobuhide Kawasaki ,  Ippei Tanaka ,  Naoki Kurita ,  Tomohiko Ishikawa

发明人： Hideo Kato ,  Osamu Nagata ,  Yoshiyuki Iwabuchi ,  Takahiro Sato ,  Junichiro Uda ,  Tutomu Inoue ,  Hiroshi Nakamura ,  Nobuhide Kawasaki ,  Ippei Tanaka ,  Naoki Kurita ,  Tomohiko Ishikawa

IPC分类号： A61K31/382 ,  C07D335/02

CPC分类号： C07D335/02 ,  C07D333/24 ,  C07D333/28 ,  C07D333/32 ,  C07D333/38 ,  C07D333/48

摘要： A compound represented by the formula (1) or a salt thereof ( represents a single bond, or a double bond; R1 represents hydrogen atom, or an alkyl group; R2 and R3 represent hydrogen atom, or an alkyl group; R4 and R5 represent hydrogen atom, hydroxy group, an alkoxyl group, a halogen atom, or a mono- or di-alkyl-substituted amino group; R6 represents hydrogen atom, cyano group, an alkoxycarbonyl group, or carboxy group; R7 represents one or two of substituents on the benzene ring (the substituents are selected from hydrogen atom, a halogen atom, nitro group, cyano group, hydroxy group, amino group, an alkyl group, and an alkoxyl group); A represents a 5-membered or 6-membered non-aromatic heterocyclic ring containing one or two contiguous sulfur atoms (the sulfur atoms may independently form oxide); W represents oxo group, hydrogen atom, an alkyl group, hydroxy group, an alkoxyl group, or a halogen atom; and X represents oxygen atom, or sulfur atom), or a salt thereof, which has a superior suppressing action against prostaglandin E2 production and is useful as an active ingredient of medicaments with reduced adverse reactions such as gastrointestinal disorders.

摘要翻译： 由式（1）表示的化合物或其盐（表示单键或双键; R1表示氢原子或烷基; R2和R3表示氢原子或烷基; R4和R5表示 氢原子，羟基，烷氧基，卤素原子或一或二烷基取代的氨基; R 6表示氢原子，氰基，烷氧基羰基或羧基; R 7表示一个或两个取代基 在苯环上（取代基选自氢原子，卤素原子，硝基，氰基，羟基，氨基，烷基和烷氧基）; A表示5元或6元非 含有一个或两个相邻硫原子的杂环（硫原子可以独立地形成氧化物）; W表示氧代基，氢原子，烷基，羟基，烷氧基或卤素原子; X表示氧原子 ，或硫原子）或其盐 对前列腺素E2产生的抑制作用较差，并且可用作具有减少的不良反应如胃肠道疾病的药物的活性成分。

公开(公告)号：US20100048666A1

公开(公告)日：2010-02-25

申请号：US12440540

申请日：2007-09-10

申请人： Hideo Kato ,  Osamu Nagata ,  Yoshiyuki Iwabuchi ,  Takahiro Sato ,  Junichiro Uda ,  Tutomu Inoue ,  Hiroshi Nakamura ,  Nobuhide Kawasaki ,  Ippei Tanaka ,  Naoki Kurita ,  Tomohiko Ishikawa

发明人： Hideo Kato ,  Osamu Nagata ,  Yoshiyuki Iwabuchi ,  Takahiro Sato ,  Junichiro Uda ,  Tutomu Inoue ,  Hiroshi Nakamura ,  Nobuhide Kawasaki ,  Ippei Tanaka ,  Naoki Kurita ,  Tomohiko Ishikawa

IPC分类号： A61K31/382 ,  C07D335/02 ,  A61K31/381 ,  C07D333/38 ,  C07D333/32 ,  A61P13/02 ,  A61P13/08 ,  A61P13/10 ,  A61P3/10 ,  A61P35/00

CPC分类号： C07D335/02 ,  C07D333/24 ,  C07D333/28 ,  C07D333/32 ,  C07D333/38 ,  C07D333/48

摘要： A compound represented by the formula (1) or a salt thereof ( represents a single bond, or a double bond; R1 represents hydrogen atom, or an alkyl group; R2 and R3 represent hydrogen atom, or an alkyl group; R4 and R5 represent hydrogen atom, hydroxy group, an alkoxyl group, a halogen atom, or a mono- or di-alkyl-substituted amino group; R6 represents hydrogen atom, cyano group, an alkoxycarbonyl group, or carboxy group; R7 represents one or two of substituents on the benzene ring (the substituents are selected from hydrogen atom, a halogen atom, nitro group, cyano group, hydroxy group, amino group, an alkyl group, and an alkoxyl group); A represents a 5-membered or 6-membered non-aromatic heterocyclic ring containing one or two contiguous sulfur atoms (the sulfur atoms may independently form oxide); W represents oxo group, hydrogen atom, an alkyl group, hydroxy group, an alkoxyl group, or a halogen atom; and X represents oxygen atom, or sulfur atom), or a salt thereof, which has a superior suppressing action against prostaglandin E2 production and is useful as an active ingredient of medicaments with reduced adverse reactions such as gastrointestinal disorders.

摘要翻译： 由式（1）表示的化合物或其盐（表示单键或双键; R1表示氢原子或烷基; R2和R3表示氢原子或烷基; R4和R5表示 氢原子，羟基，烷氧基，卤素原子或一或二烷基取代的氨基; R 6表示氢原子，氰基，烷氧基羰基或羧基; R 7表示一个或两个取代基 在苯环上（取代基选自氢原子，卤素原子，硝基，氰基，羟基，氨基，烷基和烷氧基）; A表示5元或6元非 含有一个或两个相邻硫原子的杂环（硫原子可以独立地形成氧化物）; W表示氧代基，氢原子，烷基，羟基，烷氧基或卤素原子; X表示氧原子 ，或硫原子）或其盐 对前列腺素E2产生的抑制作用较差，并且可用作具有减少的不良反应如胃肠道疾病的药物的活性成分。