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1. 发明授权

US06696489B1 2-Methylpropionic acid derivatives and medicinal compositions containing the same 失效
标题翻译： 2-甲基丙酸衍生物和含有它们的药物组合物
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。

2. 发明授权

US06538152B1 Phenoxyacetic acid derivatives and medicinal compositions containing the same 失效
标题翻译：苯氧乙酸衍生物和含有它们的药物组合物
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。

3. 发明授权

US5177069A Naphthysulfonylalkanoic acid compounds and pharmaceutical compositions thereof 失效
标题翻译：萘磺酸钠化合物及其药物组合物
公开(公告)号：US5177069A
公开(公告)日：1993-01-05
申请号：US623107
申请日：1990-12-06
申请人： Makio Kitazawa , Masuo Akahane , Yasushi Nakano , Atsushi Tsubaki , Kazuaki Sato , Masaaki Ban , Michihiro Kobayashi
发明人： Makio Kitazawa , Masuo Akahane , Yasushi Nakano , Atsushi Tsubaki , Kazuaki Sato , Masaaki Ban , Michihiro Kobayashi
IPC分类号： C07C317/44 , C07C323/52
CPC分类号： C07C323/52 , C07C317/44
摘要： The present invention provides a novel class of naphthylsulfonylalkanoic acid compounds such as a structure corrresponding to the formula: ##STR1## or a pharmaceutically acceptable salt thereof. A present invention naphthylsulfonylalkanoic acid compound is useful for prevention or treatment of irritable bowel syndrome, biliary dyskinesia and acute pancreatitis.

4. 发明授权

US4780477A Isatin compositions having anti-ulcer activities 失效
标题翻译：靛红组合物具有抗溃疡活性
公开(公告)号：US4780477A
公开(公告)日：1988-10-25
申请号：US868146
申请日：1986-05-29
申请人： Michihiro Kobayashi , Makio Kitazawa , Masuo Akahane , Tsutomu Tsukamoto , Ryoji Yamamoto , Yasushi Nakano
发明人： Michihiro Kobayashi , Makio Kitazawa , Masuo Akahane , Tsutomu Tsukamoto , Ryoji Yamamoto , Yasushi Nakano
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P1/04 , C07D209/40 , C07D209/34
CPC分类号： C07D209/40
摘要： This invention provides novel isatin compounds which are useful as therapeutic agents. The invention isatin compounds and the pharmaceutically acceptable salts thereof exhibit anti-ulcer activities which are applicable for propylaxis and treatment of ulcer diseases in the digestive tract of animals.
摘要翻译：本发明提供了可用作治疗剂的新型靛红化合物。本发明的靛红化合物及其药学上可接受的盐具有抗菌活性，其适用于动物消化道中的丙肟酸和溃疡性疾病的治疗。

5. 发明授权

US06353025B1 Phenylaminoalkylcarboxylic acid derivatives and pharmaceutical compositions comprising the same 失效
标题翻译：苯基氨基烷基羧酸衍生物和包含它们的药物组合物
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。

6. 发明授权

US5145869A Phenylsulfonylalkanoic acid compounds and pharmaceuticals thereof 失效
标题翻译：苯磺酰链烷酸化合物及其药物
公开(公告)号：US5145869A
公开(公告)日：1992-09-08
申请号：US683247
申请日：1991-04-11
申请人： Makio Kitazawa , Masuo Akahane , Yasushi Nakano , Atsushi Tsubaki , Kazuaki Sato , Masaaki Ban , Michihiro Kobayashi
发明人： Makio Kitazawa , Masuo Akahane , Yasushi Nakano , Atsushi Tsubaki , Kazuaki Sato , Masaaki Ban , Michihiro Kobayashi
IPC分类号： C07C317/44 , C07C323/60
CPC分类号： C07C317/44 , C07C323/60
摘要： The present invention provides a novel class of phenylsulfonylalkanoic acid compounds such as a structure corresponding to the formula: ##STR1## or a pharmaceutically acceptable salt thereof. A present invention phenylsulfonylalkanoic acid compound is useful for prevention or treatment of irritable bowel syndrome, biliary dyskinesia and acute pancreatitis.
摘要翻译：本发明提供了一类新的苯基磺酰基链烷酸化合物，例如对应于下式的结构：或其药学上可接受的盐。本发明苯磺酰基链烷酸化合物可用于预防或治疗肠易激综合征，胆道运动障碍和急性胰腺炎。

7. 发明授权

US06790865B2 2-methylpropionic acid derivatives and pharmaceutical compositions comprising the same 失效
标题翻译： 2-甲基丙酸衍生物和包含它们的药物组合物
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。

8. 发明授权

US06376513B1 Drug for relieving pain and promoting the removal of calculi in urolithiasis 失效
标题翻译：用于缓解疼痛并促进排尿结石的结石的药物
公开(公告)号：US06376513B1
公开(公告)日：2002-04-23
申请号：US09448422
申请日：1999-11-24
申请人： Masuo Akahane , Yoshitaka Tomiyama
发明人： Masuo Akahane , Yoshitaka Tomiyama
IPC分类号： A61K3147
CPC分类号： A61K31/4704 , A61K31/00 , A61K31/137 , A61K31/138 , A61K31/4184
摘要： The present invention relates to a novel drug method for relieving pain and promoting the removal of calculi in urolithiasis which contains an active ingredient having stimulating effects on both &bgr;2- and &bgr;3-adrenoceptors and exerting a potent relaxing effect on human ureteral smooth muscle.
摘要翻译：本发明涉及一种用于缓解疼痛并促进尿石结石结石去除的新型药物方法，其包含对β2-和β3-肾上腺素受体具有刺激作用的活性成分，并对人输尿管平滑肌发挥有效的缓解作用。

9. 发明授权

US06410560B1 Drug for relieving pain and promoting the removal of calculi in urolithiasis 失效
标题翻译：用于缓解疼痛并促进排尿结石的结石的药物
公开(公告)号：US06410560B1
公开(公告)日：2002-06-25
申请号：US09448423
申请日：1999-11-24
申请人： Masuo Akahane , Yoshitaka Tomiyama
发明人： Masuo Akahane , Yoshitaka Tomiyama
IPC分类号： A61K3147
CPC分类号： A61K31/4704 , A61K31/00 , A61K31/137 , A61K31/138 , A61K31/4184
摘要： The present invention relates to a novel drug composition for relieving pain and promoting the removal of calculi in urolithiasis which contains an active ingredient having stimulating effects on both &bgr;2- and &bgr;3-adrenoceptors and exerting a potent relaxing effect on human ureteral smooth muscle.
摘要翻译：本发明涉及一种用于缓解疼痛并促进去除尿石结石的新型药物组合物，其含有对β2-和β3-肾上腺素受体具有刺激作用的活性成分，并对人输尿管平滑肌发挥有效的缓解作用。

10. 发明授权

US06399660B1 Aminoethylphenoxyacetic acid derivatives and drugs for pain remission and calculi removal promotion in urinary lithiasis 有权
标题翻译：氨基乙基苯氧基乙酸衍生物和用于尿液结石的疼痛缓解和结石去除促进药物
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。

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