公开(公告)号：US20100112053A1

公开(公告)日：2010-05-06

申请号：US12523117

申请日：2008-01-10

申请人： Denichi Momose ,  Nobuyuki Isshiki ,  Noboru Kamada

发明人： Denichi Momose ,  Nobuyuki Isshiki ,  Noboru Kamada

IPC分类号： A61K9/24 ,  A61K31/198 ,  A61P25/16 ,  A61K9/20

CPC分类号： A61K9/0065 ,  A61K9/2086 ,  A61K31/198

摘要： The present invention is to provide a levodopa preparation which is able to persistently release levodopa in the stomach, has a sufficient gastric residence time, is in an easily ingestible size and is able to be easily manufactured industrially with an object of maintaining a sustained concentration of levodopa in blood. It is a gastric retentive preparation for levodopa, characterized in that, the preparation contains a gastric resident layer showing a sufficient retentive property due to a high mechanical strength in the stomach and showing a good disintegrating property in an intestinal tract in addition to a drug releasing layer containing levodopa.

摘要翻译： 本发明提供一种能够在胃中持续释放左旋多巴的左旋多巴制剂，具有足够的胃停留时间，容易摄取的尺寸，并且能够容易地在工业上制造，其目的是保持持续浓度 左旋多巴在血液中 它是用于左旋多巴的胃保持制剂，其特征在于，该制剂含有由胃中的高机械强度显示出足够的保留性能的胃停留层，除了药物释放之外还显示出良好的肠道分解性 含有左旋多巴的层。

公开(公告)号：US20090311321A1

公开(公告)日：2009-12-17

申请号：US12376161

申请日：2007-08-03

申请人： Kazuki Mimura ,  Yasuhiro Takeda ,  Ken Kanada

发明人： Kazuki Mimura ,  Yasuhiro Takeda ,  Ken Kanada

IPC分类号： A61K9/20 ,  A61K31/403

CPC分类号： A61K31/4035 ,  A61K9/0056 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054

摘要： The present invention provides an orally disintegrating tablet containing mitiglinide calcium hydrate. The tablet has reduced bitterness and quickly disintegrates in the mouth, while exhibiting rapid dissolution in the digestive tract. The bitterness-masked orally disintegrating tablet comprises: (a) mitiglinide calcium hydrate; (b) microcrystalline cellulose; (c) at least one masking agent selected from the group consisting of aminoalkyl methacrylate copolymer E, polyvinylacetal diethylaminoacetate, an ethyl acrylate-methyl methacrylate copolymer, and ethyl cellulose; (d) a sugar or a sugar alcohol; and (e) at least one selected from corn starch and partially pregelatinized starch.

摘要翻译： 本发明提供含有米格列奈钙水合物的口腔崩解片剂。 片剂在口中减少了苦味并迅速崩解，同时在消化道中表现出快速溶解。 苦味口腔崩解片包括：（a）米格列奈钙水合物; （b）微晶纤维素; （c）至少一种选自甲基丙烯酸氨基烷基酯共聚物E，聚乙烯醇缩乙醛二乙基氨基乙酸酯，丙烯酸乙酯 - 甲基丙烯酸甲酯共​​聚物和乙基纤维素的掩蔽剂; （d）糖或糖醇; 和（e）选自玉米淀粉和部分预胶化淀粉中的至少一种。

公开(公告)号：US20090227651A1

公开(公告)日：2009-09-10

申请号：US11576678

申请日：2005-10-04

申请人： Yasuhiro Omori ,  Nobuhiko Arai ,  Tomoji Shimizu ,  Yoshio Okubo

发明人： Yasuhiro Omori ,  Nobuhiko Arai ,  Tomoji Shimizu ,  Yoshio Okubo

IPC分类号： A61K31/4035 ,  A61P13/02

CPC分类号： C07D209/14 ,  A61K31/4045 ,  A61K45/06 ,  A61K2300/00

摘要： An agent for the prevention and/or treatment of urine collection disorders associated with lower urinary tract obstructive disease, characterized by containing an indoline derivative represented by the following general formula (I): wherein R; R1; and R2 are defined in the specification. The derivative and salt are usable as an agent for the prevention and/or treatment of urine collection disorders associated with lower urinary tract obstructive disease. Silodosin is the preferred indoline derivative.

摘要翻译： 一种用于预防和/或治疗与下尿路阻塞性疾病相关的尿液收集障碍的药剂，其特征在于含有由以下通式（I）表示的二氢吲哚衍生物：其中R; R1; 和R2在说明书中定义。 衍生物和盐可​​用作预防和/或治疗与下尿路阻塞性疾病相关的尿液收集障碍的药剂。 西洛昔辛是优选的二氢吲哚衍生物。

公开(公告)号：US07566699B2

公开(公告)日：2009-07-28

申请号：US10551648

申请日：2004-03-24

申请人： Nobuhiko Fushimi ,  Shigeru Yonekubo ,  Hideyuki Muranaka ,  Hiroaki Shiohara ,  Hirotaka Teranishi ,  Kazuo Shimizu ,  Fumiaki Ito ,  Masayuki Isaji

发明人： Nobuhiko Fushimi ,  Shigeru Yonekubo ,  Hideyuki Muranaka ,  Hiroaki Shiohara ,  Hirotaka Teranishi ,  Kazuo Shimizu ,  Fumiaki Ito ,  Masayuki Isaji

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/00 ,  C07H17/00

CPC分类号： C07H15/203 ,  C07H17/00 ,  C07H17/02 ,  C07H17/04

摘要： The present invention provides fused heterocyclic derivatives represented by the general formula: wherein R1 represents H, halogen, OH, etc.; R2 represents H, halogen or an alkyl group; R3 and R4 represent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.

摘要翻译： 本发明提供由以下通式表示的稠合杂环衍生物：其中R1表示H，卤素，OH等; R2表示H，卤素或烷基; R3和R4代表H，OH，卤素等; Q表示亚烷基等。 环A表示芳基或杂芳基; 和G表示其药学上可接受的盐或其前体药物，其在人SGLT中表现出优异的抑制活性，并且可用作预防或治疗与高血糖相关的疾病如糖尿病，餐后高血糖，葡萄糖耐量异常，糖尿病 并发症或肥胖症，包含其的药物组合物及其药物用途。

公开(公告)号：US20090074738A1

公开(公告)日：2009-03-19

申请号：US11719201

申请日：2005-11-17

申请人： Shigeru Yonekubo ,  Nobuhiko Fushimi

发明人： Shigeru Yonekubo ,  Nobuhiko Fushimi

IPC分类号： A61K31/7076 ,  C07H7/06 ,  A61K31/7056

CPC分类号： A61K45/06 ,  A61K31/404 ,  A61K31/4166 ,  C07D405/04 ,  A61K2300/00

摘要： A compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-substituted-3-(β-D-glycopyranosyl) nitrogen-containing heterocyclic compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or a solvate thereof; an SGLT inhibitor containing the same; a pharmaceutical composition containing the same and a combination pharmacy of them. In the formula, A represents an alkylene group or alkenylene group; B represents a single bond, —O—, —S— or —NH—; C represents an optionally substituted aryl or heteroaryl group; Q independently represents a carbon atom which a hydrogen atom or a substituent binds to, or a nitrogen atom.

摘要翻译： 具有SGLT1和/或SGLT2抑制活性的化合物，其可用作预防或治疗糖尿病，餐后高血糖，葡萄糖耐量降低，糖尿病并发症，肥胖症等的药剂。它是1-取代-3-（β -D-糖吡喃糖基）含氮杂环化合物或其药学上可接受的盐，或其水合物或溶剂化物; 含有其的SGLT抑制剂; 含有它们的药物组合物和它们的组合药剂。 在该式中，A表示亚烷基或亚烯基; B表示单键，-O - ， - S-或-NH-; C表示任选取代的芳基或杂芳基; Q独立地表示氢原子或取代基结合的碳原子或氮原子。

公开(公告)号：US20090030218A1

公开(公告)日：2009-01-29

申请号：US11914915

申请日：2006-05-17

申请人： Kiyoshi Kasai ,  Minoru Kubota ,  Ritsu Suzuki ,  Tetsuji Ozawa ,  Takehiro Ishikawa ,  Makoto Kobayashi ,  Junichi Sonehara ,  Masahiro Kobayashi

发明人： Kiyoshi Kasai ,  Minoru Kubota ,  Ritsu Suzuki ,  Tetsuji Ozawa ,  Takehiro Ishikawa ,  Makoto Kobayashi ,  Junichi Sonehara ,  Masahiro Kobayashi

IPC分类号： C07D303/40 ,  C07C69/76 ,  C07C229/38 ,  C07C255/00

CPC分类号： C07D303/22 ,  C07B53/00 ,  C07C67/08 ,  C07C67/31 ,  C07C69/94 ,  C07C213/06 ,  C07C253/30 ,  C07C255/54 ,  C07C217/22

摘要： The present invention provides an industrial method for preparing aminoalcohol derivatives (I) having a biphenyl group, biphenyloxyacetaldehyde derivatives which are used therefore, preparing methods thereof, and intermediates used for the preparing method.The present invention also provides a preparing method including processes for preparing a 3-substituted biphenylcarboxylic acid derivative represented by the following general formula: by allowing a 3-fluorobiphenylcarboxylic acid derivative prepared from a 3-fluorobiphenylcarbonitrile derivative which can be prepared by allowing a 4-halophenol derivative to react with a 2-fluorobenzonitrile derivative which is substituted by a leaving group at 4-position to react with an organometallic reagent.

摘要翻译： 本发明提供了制备具有联苯基的氨基醇衍生物（I）的工业方法，因此使用的联苯氧基乙醛衍生物及其制备方法以及用于制备方法的中间体。 本发明还提供了一种制备方法，其包括由以下通式表示的3-取代的联苯基羧酸衍生物的制备方法：通过使由3-氟联苯基腈衍生物制备的3-氟联苯基羧酸衍生物，其可以通过使4- 卤代酚衍生物与在4-位上被离去基团取代的2-氟苄腈衍生物反应，与有机金属试剂反应。

公开(公告)号：US07402692B2

公开(公告)日：2008-07-22

申请号：US11923067

申请日：2007-10-24

申请人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

发明人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

IPC分类号： C07C229/00 ,  C07C69/76

CPC分类号： C07C217/60 ,  C07C43/315 ,  C07C69/712 ,  C07C213/02

摘要： The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates

摘要翻译： 本发明提供由通式（I）等表示的新型中间体，其用于制备具有β3肾上腺素受体刺激活性并用于治疗或预防肥胖的通式（X）表示的苯氧基乙酸衍生物或其药学上可接受的盐 ，高血糖症，由肠蠕动过多引起的疾病，尿尿症，尿失禁，抑郁症或胆道结石。 本发明还提供了制备所述中间体的方法和使用所述中间体的方法

公开(公告)号：US20080045740A1

公开(公告)日：2008-02-21

申请号：US11923093

申请日：2007-10-24

申请人： Nobuyuki TANAKA ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

发明人： Nobuyuki TANAKA ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

IPC分类号： C07C69/708

CPC分类号： C07C217/60 ,  C07C43/315 ,  C07C69/712 ,  C07C213/02

摘要： The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.

摘要翻译： 本发明提供由通式（I）等表示的新型中间体，其用于制备具有β3肾上腺素受体刺激活性并用于治疗或预防肥胖的通式（X）表示的苯氧基乙酸衍生物或其药学上可接受的盐 ，高血糖症，由肠蠕动过多引起的疾病，尿尿症，尿失禁，抑郁症或胆道结石。 本发明还提供了制备所述中间体的方法和使用所述中间体的方法。

公开(公告)号：US07294618B2

公开(公告)日：2007-11-13

申请号：US10469140

申请日：2002-02-26

申请人： Nobuhiko Fushimi ,  Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masayuki Isaji

发明人： Nobuhiko Fushimi ,  Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masayuki Isaji

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H17/00

CPC分类号： C07H17/02 ,  Y10S514/866

摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1, R2 and R3 represent a hydrogen atom or a halogen atom; R4 represents a lower alkyl group or a halo(lower alkyl) group; and R5 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, etc., a pharmaceutically acceptable salt thereof or a prodrug thereof., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.

摘要翻译： 本发明提供由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中R 1，R 2和R 3表示氢原子或卤素原子 ; R 4表示低级烷基或卤代（低级烷基）基团; 和R 5表示氢原子，低级烷基，低级烷氧基，低级烷硫基等，其药学上可接受的盐或其前药，其具有优异的抑制活性 在人SGLT2中，因此可用作预防或治疗与高血糖相关疾病如糖尿病，糖尿病并发症或肥胖症的药物，其药学上可接受的盐或其前药，其生产中间体及其药学用途。

公开(公告)号：US07208520B2

公开(公告)日：2007-04-24

申请号：US10489343

申请日：2002-08-27

申请人： Hidetoshi Isawa ,  Yukihiko Hotei ,  Kiyoshi Kasai ,  Junichi Sonehara ,  Satoshi Akahane ,  Hiromu Harada

发明人： Hidetoshi Isawa ,  Yukihiko Hotei ,  Kiyoshi Kasai ,  Junichi Sonehara ,  Satoshi Akahane ,  Hiromu Harada

IPC分类号： A01N37/12 ,  A01N37/44 ,  A61K31/24

CPC分类号： A61K31/216 ,  C07B2200/07 ,  C07C217/60

摘要： The present invention provides ethyl (−)-2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxy]acetate hydrochloride, crystalline forms thereof and pharmaceutical compositions containing them, which have excellent β3-adrenoceptor stimulating effects, therapeutic effects on pollakiuria or urinary incontinence and storage stabilities and are useful as a medicament.

摘要翻译： 本发明提供了（ - ） - 2- [4- [2 - [[（1S，2R）-2-羟基-2-（4-羟基苯基）-1-甲基乙基]氨基]乙基] 二甲基苯氧基]乙酸盐酸盐，其结晶形式和含有它们的药物组合物，其具有优异的β3 - 肾上腺素受体刺激作用，对尿频尿失禁和储尿稳定性的治疗作用，并且可用作药物。