公开(公告)号：US06790865B2

公开(公告)日：2004-09-14

申请号：US10358214

申请日：2003-02-05

申请人： Tetsuro Tamai ,  Nobuyuki Tanaka ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Hideyuki Muranaka ,  Masaaki Sato ,  Masuo Akahane

发明人： Tetsuro Tamai ,  Nobuyuki Tanaka ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Hideyuki Muranaka ,  Masaaki Sato ,  Masuo Akahane

IPC分类号： A61K3124

CPC分类号： C07C217/60 ,  C07C229/18

摘要： The present invention provides novel 2-methylpropionic acid derivatives represented by the general formula: (wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group; R2 represents a hydrogen atom, a lower alkyl group or a halogen atom; A represents an oxygen atom or an imino group; the carbon atom marked with (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have excellent &bgr;3-adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of the biliary tract.

摘要翻译： 本发明提供由以下通式表示的新型2-甲基丙酸衍生物：其中R 1表示氢原子，低级烷基或芳烷基; R 2表示氢原子，低级烷基或 卤素原子; A表示氧原子或亚氨基;由（R）表示的碳原子表示R构型的碳原子，标有（S）的碳原子表示S构型的碳原子）和药学上可接受的 其具有优异的β3肾上腺素能受体刺激作用，并且可用作预防或治疗肥胖症，高血糖症，由肠蠕动过多引起的疾病，尿频尿症，尿失禁，抑郁症或由胆汁结石或运动障碍引起的疾病 胆道。

公开(公告)号：US06353025B1

公开(公告)日：2002-03-05

申请号：US09581851

申请日：2000-06-19

申请人： Tetsuro Tamai ,  Nobuyuki Tanaka ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Hideyuki Muranaka ,  Masaaki Sato ,  Masuo Akahane

发明人： Tetsuro Tamai ,  Nobuyuki Tanaka ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Hideyuki Muranaka ,  Masaaki Sato ,  Masuo Akahane

IPC分类号： A01N3712

CPC分类号： C07D295/185 ,  C07C229/18 ,  C07C237/06

摘要： The present invention provides novel phenylaminoalkyl-carboxylic acid derivatives represented by the general formula: (wherein R1 represents a hydroxy group, a lower alkoxy group, an aralkoxy group, an amino group, an alicyclic amino group or a mono or di(lower alkyl)amino group which may have a hydroxy group or a lower alkoxy group as a substituent; R2 represents a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom or a halogen atom; R4 and R5 are the same or different and each represents a hydrogen atom, a halogen atom or a lower alkyl group; A represents a lower alkylene group; the carbon atom marked with (R) represents a carbon atom in (R) configuration; and the carbon atom marked with (S) represents a carbon atom in (S) configuration) and pharmaceutically acceptable salts thereof, which have excellent &bgr;3-adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of biliary tract.

摘要翻译： 本发明提供由通式（其中R1表示羟基，低级烷氧基，芳烷氧基，氨基，脂环族氨基或单或二（低级烷基））表示的新型苯基氨基烷基 - 羧酸衍生物， 可以具有羟基或低级烷氧基作为取代基的氨基; R2表示氢原子或低级烷基; R3表示氢原子或卤素原子; R4和R5相同或不同，表示 氢原子，卤素原子或低级烷基; A表示低级亚烷基;（R）表示的碳原子表示（R）构型的碳原子，（S）表示的碳原子表示碳原子 （S）构型）及其药学上可接受的盐，其具有优异的β3肾上腺素能受体刺激作用，并且可用作预防或治疗肥胖症，高血糖症，由肠道超嗜热引起的疾病 遗尿，尿频，尿失禁，抑郁症或由胆汁结石或胆汁运动障碍引起的疾病。

公开(公告)号：US06696489B1

公开(公告)日：2004-02-24

申请号：US09673308

申请日：2000-10-13

申请人： Tetsuro Tamai ,  Nobuyuki Tanaka ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Hideyuki Muranaka ,  Masaaki Sato ,  Masuo Akahane

发明人： Tetsuro Tamai ,  Nobuyuki Tanaka ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Hideyuki Muranaka ,  Masaaki Sato ,  Masuo Akahane

IPC分类号： A61K3124

CPC分类号： C07C217/60 ,  C07C229/18

摘要： The present invention provides novel 2-methylpropionic acid derivatives represented by the general formula: (wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group; R2 represents a hydrogen atom a lower alkyl group or a halogen atom; A represents an oxygen atom or an imino group; the carbon atom marked with (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have excellent &bgr;3-adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of the biliary tract.

摘要翻译： 本发明提供由以下通式表示的新型2-甲基丙酸衍生物：其中R 1表示氢原子，低级烷基或芳烷基; R 2表示氢原子，低级烷基或 卤素原子; A表示氧原子或亚氨基;由（R）标记的碳原子表示R构型的碳原子;标有（S）的碳原子表示S构型的碳原子）和药学上可接受的盐 其具有优异的β3肾上腺素能受体刺激作用，并且可用作预防或治疗肥胖症，高血糖症，由肠蠕动过多引起的疾病，尿尿症，尿失禁，抑郁症或由胆汁结石或运动障碍引起的疾病 胆道。

公开(公告)号：US06538152B1

公开(公告)日：2003-03-25

申请号：US09720976

申请日：2001-01-03

申请人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Hideyuki Muranaka ,  Masaaki Sato ,  Masuo Akahane

发明人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Hideyuki Muranaka ,  Masaaki Sato ,  Masuo Akahane

IPC分类号： C07C22900

CPC分类号： C07C217/60 ,  C07C233/43 ,  C07C235/06 ,  C07C235/60 ,  C07C255/59

摘要： The present invention provides novel phenoxyacetic acid derivatives represented by the general formula: wherein R1 represents a hydroxy group, a lower alkoxy group, an aralkoxy group, an amino group, or a mono or di(lower alkyl)amino group; one of R2 and R3 is a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, while the other is a hydrogen atom; R4 represents a halogen atom, a lower alkyl group, a halo(lower alkyl) group, a hydroxy group, a lower alkoxy group, an aralkoxy group, a cyano group, a nitro group, an amino group, a mono or di(lower alkyl)amino group, a carbamoyl group, a mono or di(lower alkyl)carbamoyl group or a group represented by the general formula: —NHCOR5 (wherein R5 represents a hydrogen atom or a lower alkyl group); the carbon atom marked with (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration, and pharmaceutically acceptable salts thereof, which have excellent &bgr;3-adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of biliary tract.

摘要翻译： 本发明提供由通式表示的新型苯氧基乙酸衍生物：其中R1表示羟基，低级烷氧基，芳烷氧基，氨基或单或二（低级烷基）氨基; R2和R3中的一个是氢原子，卤素原子，低级烷基或低级烷氧基，而另一个是氢原子; R4表示卤原子，低级烷基，卤代（低级烷基），羟基，低级烷氧基，芳烷氧基，氰基，硝基，氨基，单或二（低级） 烷基）氨基，氨基甲酰基，一或二（低级烷基）氨基甲酰基或由通式表示的基团：其中R5表示氢原子或低级烷基; 用（R）标记的碳原子表示R构型的碳原子; 标记有（S）的碳原子表示S构型的碳原子及其药学上可接受的盐，其具有优异的β3肾上腺素能受体刺激作用，并且可用作预防或治疗肥胖，高血糖，由高血糖引起的疾病 肠蠕动过多，尿频尿失禁，抑郁症，胆汁结石或胆汁运动障碍引起的疾病。

公开(公告)号：US06399660B1

公开(公告)日：2002-06-04

申请号：US09463432

申请日：2000-03-31

申请人： Tetsuro Tamai ,  Nobuyuki Tanaka ,  Hideyuki Muranaka ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Masaaki Sato ,  Masuo Akahane

发明人： Tetsuro Tamai ,  Nobuyuki Tanaka ,  Hideyuki Muranaka ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Masaaki Sato ,  Masuo Akahane

IPC分类号： A01N3712

CPC分类号： C07C217/60

摘要： Novel aminoethylphenoxyacetic acid derivatives represented by the general formula: (wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group; R2 represents a hydrogen atom or a halogen atom; the carbon atom marked with (R) represents a carbon atom in (R) configuration; and the carbon atom marked with (S) represents a carbon atom in (S) configuration) and pharmaceutically acceptable salts thereof, which have stimulating effects on both &bgr;2- and &bgr;3-adrenoceptors and are useful as agents for relieving pain and promoting the removal of calculi in urolithiasis.

摘要翻译： 由以下通式表示的新型氨基乙基苯氧基乙酸衍生物（其中R1表示氢原子，低级烷基或芳烷基; R2表示氢原子或卤素原子;用（R）表示的碳原子表示碳原子 （S）构型的标记的碳原子和（S）标记的碳原子表示（S）构型的碳原子）及其药学上可接受的盐，其对β2-和β3-肾上腺素受体具有刺激作用，并且可用作缓解疼痛的药剂 并促进排尿结石的结石。