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公开(公告)号:EP0074008A2
公开(公告)日:1983-03-16
申请号:EP82107714.6
申请日:1982-08-23
发明人: Amano, Takehiro , Yoshikawa, Kensei , Sano, Tatsuhiko , Ohuchi, Yutaka , Ishiguro, Michihiro , Shiono, Manzo , Fujita, Yoshiji , Nishida, Takashi
IPC分类号: C07C69/612 , C07C67/343 , C07C69/736 , C07C69/65 , C07C69/618 , C07D207/20 , C07D235/02 , C07D491/052 , C07D333/08 , C07D263/58
CPC分类号: C07D263/57 , C07C57/30 , C07C57/42 , C07D207/20 , C07D333/24 , C07D471/04 , C07D491/04
摘要: A process for producing an a-arylalkanoic acid ester represented by the general formula
wherein Ar represents an aryl group which may optionally be substituted, and R' and R 2 , independently from each other, represents a lower alkyl group, which comprises reacting a Grignard reagent prepared from an aryl halide of the general formula
wherein Ar is as defined above and X 1 represents a halogen atom, and magnesium, with an a-haloalkanoic acid ester of the general formula
wherein R' and R 2 are as defined above, and X 2 represents a halogen atom, said reaction of the Grignard reagent with the a-haloalkanoic acid ester of general formula (III) being carried out in the presence of a nickel compound.-
公开(公告)号:EP0073447B1
公开(公告)日:1984-11-21
申请号:EP82107715.3
申请日:1982-08-23
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公开(公告)号:EP0074008B1
公开(公告)日:1984-10-10
申请号:EP82107714.6
申请日:1982-08-23
发明人: Amano, Takehiro , Yoshikawa, Kensei , Sano, Tatsuhiko , Ohuchi, Yutaka , Ishiguro, Michihiro , Shiono, Manzo , Fujita, Yoshiji , Nishida, Takashi
IPC分类号: C07C69/612 , C07C67/343 , C07C69/736 , C07C69/65 , C07C69/618 , C07D207/20 , C07D235/02 , C07D491/052 , C07D333/08 , C07D263/58
CPC分类号: C07D263/57 , C07C57/30 , C07C57/42 , C07D207/20 , C07D333/24 , C07D471/04 , C07D491/04
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公开(公告)号:EP0074008A3
公开(公告)日:1983-05-25
申请号:EP82107714
申请日:1982-08-23
发明人: Amano, Takehiro , Yoshikawa, Kensei , Sano, Tatsuhiko , Ohuchi, Yutaka , Ishiguro, Michihiro , Shiono, Manzo , Fujita, Yoshiji , Nishida, Takashi
IPC分类号: C07C69/612 , C07C67/343 , C07C69/736 , C07C69/65 , C07C69/618 , C07D207/20 , C07D235/02 , C07D491/052 , C07D333/08 , C07D263/58
CPC分类号: C07D263/57 , C07C57/30 , C07C57/42 , C07D207/20 , C07D333/24 , C07D471/04 , C07D491/04
摘要: A process for producing an a-arylalkanoic acid ester represented by the general formula
wherein Ar represents an aryl group which may optionally be substituted, and R' and R 2 , independently from each other, represents a lower alkyl group, which comprises reacting a Grignard reagent prepared from an aryl halide of the general formula
wherein Ar is as defined above and X 1 represents a halogen atom, and magnesium, with an a-haloalkanoic acid ester of the general formula
wherein R' and R 2 are as defined above, and X 2 represents a halogen atom, said reaction of the Grignard reagent with the a-haloalkanoic acid ester of general formula (III) being carried out in the presence of a nickel compound.-
公开(公告)号:EP0073447A1
公开(公告)日:1983-03-09
申请号:EP82107715.3
申请日:1982-08-23
发明人: Amano, Takehiro , Yoshikawa, Kensei , Sano, Tatsuhiko , Ohuchi, Yutaka , Ishiguro, Michihiro , Shiono, Manzo , Fujita, Yoshiji , Nishida, Takashi
摘要: A process for producing 1-(p-prenylphenyl)ethanol, which comprises reacting p-chloroprenylbenzene with magnesium at a temperature between 100°C and 150°C to form a Grignard reagent, and then reacting it with acetaldehyde.
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公开(公告)号:EP0067008A1
公开(公告)日:1982-12-15
申请号:EP82302681.0
申请日:1982-05-25
发明人: Amano, Takehiro , Ogawa, Toshihisa , Yoshikawa, Kensei , Shiobara, Yoshinori , Sano, Tatsuhiko , Ito, Shoichi , Ohuchi, Yutaka , Sawada, Jiro , Tanami, Tohru
IPC分类号: C07C69/618 , C07D307/12 , A61K31/215 , A61K31/34
CPC分类号: C07D307/12
摘要: A novel carboxylic acid ester having the following general formula
wherein R is alkoxyalkyl having 2 to 6 carbon atoms, cycloalkyl having 5 or 6 carbon atoms, tetrahydrofurfuryl, alkyl having 1 to 6 carbon atoms or said alkyl substituted with 1 or 2 hydroxyl groups, is a useful anti-inflammatory and analgesic agent.摘要翻译: 具有下列通式的新型羧酸酯,其中R为具有2至6个碳原子的烷氧基烷基,具有5或6个碳原子的环烷基,四氢糠基,具有1至6个碳原子的烷基或所述被1或2个羟基取代的烷基, 一种有用的抗炎和镇痛剂。
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公开(公告)号:EP0067008B1
公开(公告)日:1985-08-21
申请号:EP82302681.0
申请日:1982-05-25
发明人: Amano, Takehiro , Ogawa, Toshihisa , Yoshikawa, Kensei , Shiobara, Yoshinori , Sano, Tatsuhiko , Ito, Shoichi , Ohuchi, Yutaka , Sawada, Jiro , Tanami, Tohru
IPC分类号: C07C69/618 , C07D307/12 , A61K31/215 , A61K31/34
CPC分类号: C07D307/12
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公开(公告)号:EP0317332B1
公开(公告)日:1993-05-19
申请号:EP88310899.5
申请日:1988-11-18
发明人: Yoshikawa, Kensei , Ohuchi, Yutaka , Sekiuchi, Kazuto , Saito, Shiuji , Hatayama, Katsuo , Sota, Kaoru
IPC分类号: C07C311/08 , C07D309/12 , C07D211/46 , C07C317/14 , C07C323/18 , C07D335/02 , A61K31/18 , A61K31/33
CPC分类号: C07D211/46 , C07C311/08 , C07C311/09 , C07C317/40 , C07C323/35 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D309/12 , C07D335/02
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公开(公告)号:EP0317332A3
公开(公告)日:1990-07-04
申请号:EP88310899.5
申请日:1988-11-18
发明人: Yoshikawa, Kensei , Ohuchi, Yutaka , Sekiuchi, Kazuto , Saito, Shiuji , Hatayama, Katsuo , Sota, Kaoru
IPC分类号: C07C311/08 , C07D309/12 , C07D211/46 , C07C317/14 , C07C323/18 , C07D335/02 , A61K31/18 , A61K31/33
CPC分类号: C07D211/46 , C07C311/08 , C07C311/09 , C07C317/40 , C07C323/35 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D309/12 , C07D335/02
摘要: Sulfonanilide compounds represented by the formula
wherein R¹ is a lower alkyl group or a trifluoromethyl group, R² is a cycloalkylidenemethyl group, a group of the formula -A-R³ (wherein A is an oxygen atom, a sulfur atom, a sulfonyl group or a sulfinyl group and R³ is a cycloalkyl group having 5 - 8 carbon atoms; a cycloalkyl group having 5-8 carbon atoms substituted by one or two of a lower alkyl group, an oxo group, a hydroxyl group or a methanesulfonyloxy group; a tetrahydropyranyl group; a tetrahydrothiopyranyl group; or a 1-methylpiperidyl group) or a group of the formula -B-R⁴ wherein B is a carbonyl group, a hydroxymethylene group or a methylene group, R⁴ is a cycloalkyl group having 5-8 carbon atoms) and the pharmaceutically acceptable salts thereof have anti-inflammatory activity.摘要翻译: 由式
表示的磺酰苯胺化合物,其中R 1是低级烷基或三氟甲基,R 2是环烷基亚甲基,式-AR 3的基团(其中A是氧原子 硫原子,磺酰基或亚磺酰基,R 3是具有5-8个碳原子的环烷基;具有5-8个碳原子的环烷基被一个或两个低级烷基,氧代 基团,羟基或甲磺酰氧基;四氢吡喃基;四氢噻喃基;或1-甲基哌啶基)或式-BR 4基团,其中B是羰基,羟基亚甲基或亚甲基 R 4为具有5-8个碳原子的环烷基),其药学上可接受的盐具有抗炎活性。 -
公开(公告)号:EP0317332A2
公开(公告)日:1989-05-24
申请号:EP88310899.5
申请日:1988-11-18
发明人: Yoshikawa, Kensei , Ohuchi, Yutaka , Sekiuchi, Kazuto , Saito, Shiuji , Hatayama, Katsuo , Sota, Kaoru
IPC分类号: C07C311/08 , C07D309/12 , C07D211/46 , C07C317/14 , C07C323/18 , C07D335/02 , A61K31/18 , A61K31/33
CPC分类号: C07D211/46 , C07C311/08 , C07C311/09 , C07C317/40 , C07C323/35 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D309/12 , C07D335/02
摘要: Sulfonanilide compounds represented by the formula
wherein R¹ is a lower alkyl group or a trifluoromethyl group, R² is a cycloalkylidenemethyl group, a group of the formula -A-R³ (wherein A is an oxygen atom, a sulfur atom, a sulfonyl group or a sulfinyl group and R³ is a cycloalkyl group having 5 - 8 carbon atoms; a cycloalkyl group having 5-8 carbon atoms substituted by one or two of a lower alkyl group, an oxo group, a hydroxyl group or a methanesulfonyloxy group; a tetrahydropyranyl group; a tetrahydrothiopyranyl group; or a 1-methylpiperidyl group) or a group of the formula -B-R⁴ wherein B is a carbonyl group, a hydroxymethylene group or a methylene group, R⁴ is a cycloalkyl group having 5-8 carbon atoms) and the pharmaceutically acceptable salts thereof have anti-inflammatory activity.摘要翻译: 由下式表示的磺酰苯胺化合物其中R 1是低级烷基或三氟甲基,R 2是亚环烷基甲基,式-A-R 3的基团(其中A是氧原子,硫原子,磺酰基或 亚硫酰基和R 3是具有5-8个碳原子的环烷基;被低级烷基,氧代基,羟基或甲磺酰氧基中的一个或两个取代的具有5-8个碳原子的环烷基;四氢吡喃基 ;四氢噻喃基;或1-甲基哌啶基)或式-B-R 4的基团,其中B是羰基,羟基亚甲基或亚甲基,R 4是具有5-8个碳原子的环烷基)和 其药学上可接受的盐具有抗炎活性。
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