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1. 发明授权

US07402692B2 Intermediates in producing phenoxyacetic acid derivatives and method of using the same 失效
标题翻译：制备苯氧基乙酸衍生物的中间体及其使用方法
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

2. 发明申请

US20080045740A1 INTERMEDIATES IN PRODUCING PHENOXYACETIC ACID PREVENTIVES AND METHOD OF USING THE SAME 失效
标题翻译：制备苯氧基酸预防剂的中间体及其使用方法
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。

3. 发明授权

US07208520B2 Crystals of hydroxynorephedrine derivative 失效
标题翻译：羟基麻黄碱衍生物的晶体
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。

4. 发明申请

US20060135605A1 Intermediates in producing phenoxyacetic acid derivatives and method of using the same 失效
标题翻译：制备苯氧基乙酸衍生物的中间体及其使用方法
公开(公告)号：US20060135605A1
公开(公告)日：2006-06-22
申请号：US10526660
申请日：2002-09-05
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： A61K31/235 , 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。

5. 发明授权

US07446128B2 Agent for treating interstitial cystitis 失效
标题翻译：间质性膀胱炎的治疗剂
公开(公告)号：US07446128B2
公开(公告)日：2008-11-04
申请号：US11267299
申请日：2005-11-07
申请人： Kouichi Kaidoh , Satoshi Akahane
发明人： Kouichi Kaidoh , Satoshi Akahane
IPC分类号： A61N31/24 , C07C229/00
CPC分类号： A61K31/24
摘要： A compound which can be used as an agent for treating interstitial cystitis. An agent for treating interstitial cystitis, which comprises a phenoxyacetic acid derivative represented by a general formula (I) wherein R1 represents hydroxyl group or a lower alkoxy group, or a pharmacologically acceptable salt thereof. Since the phenoxyacetic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof or a hydrate or solvate thereof has a selective β3-adrenoceptor stimulating activity and a remarkable action to inhibit a capsaicin-sensitive sensory nerve, it can be used as a preventive or therapeutic agent for interstitial cystitis and hyperactive bladder which are accompanied by pain, other diseases in which the capsaicin-sensitive sensory nerve is concerned (e.g., acute or chronic and systemic or topical pain and inflammation) and irritable bowel syndrome (IBS) and the like.
摘要翻译：可用作治疗间质性膀胱炎的药剂的化合物。一种治疗间质性膀胱炎的药剂，其包含由通式（I）表示的苯氧基乙酸衍生物，其中R 1表示羟基或低级烷氧基，或其药理学上可接受的盐。由于由通式（I）表示的苯氧基乙酸衍生物或其药学上可接受的盐或其水合物或溶剂合物具有选择性β3 - 肾上腺素能受体刺激活性和抑制辣椒素 - 敏感的感觉神经，它可以用作间质性膀胱炎和活动性膀胱的预防或治疗剂，其伴随着疼痛，其中涉及辣椒素敏感性感觉神经的其它疾病（例如，急性或慢性和全身或局部疼痛和炎症）和肠易激综合征（IBS）等。

6. 发明申请

US20080249177A1 AMINO ALCOHOL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND USE THEREOF 失效
标题翻译：氨基醇衍生物，含有它们的药物组合物及其用途
公开(公告)号：US20080249177A1
公开(公告)日：2008-10-09
申请号：US11936680
申请日：2007-11-07
申请人： Junichi KOBAYASHI , Tetsuya Nakamura , Ritsu Suzuki , Hideyuki Muranaka , Tomonaga Ozawa , Yuichiro Kai , Takehiro Ishikawa , Tatsuhiro Kondo , Tetsuro Tamai , Satoshi Akahane
发明人： Junichi KOBAYASHI , Tetsuya Nakamura , Ritsu Suzuki , Hideyuki Muranaka , Tomonaga Ozawa , Yuichiro Kai , Takehiro Ishikawa , Tatsuhiro Kondo , Tetsuro Tamai , Satoshi Akahane
IPC分类号： A61K31/192 , C07C229/00 , A61P3/00
CPC分类号： C07D307/79 , A61K31/195 , C07C217/18 , C07C217/20 , C07C323/62 , C07C2601/04
摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
摘要翻译：本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢或低级烷基; R 3，R 4，R 5和R 6各自为氢，卤素，低级烷基或低级烷氧基 ; R 7和R 8各自为氢，卤素，低级烷基，卤代低级烷基，低级烷氧基，环烷基，芳基，杂芳基，氰基，羟基，低级酰基，羧基等; R 9是-C（O）-R 10，-A 1 -C（O）-R 10 O > - O 2 -C（O）-R 10或四唑-5-基，其显示出有效和选择性的β3肾上腺素受体刺激活性。本发明还提供含有所述化合物的药物组合物及其用途。

7. 发明申请

US20080045741A1 INTERMEDIATES IN PRODUCING PHENOXYACETIC ACID DERIVATIVES AND METHOD OF USING THE SAME 失效
公开(公告)号：US20080045741A1
公开(公告)日：2008-02-21
申请号：US11923149
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.

8. 发明申请

US20070078184A1 Amino alcohol derivatives, medicinal composition containing the same, and use of these 失效
标题翻译：氨基醇衍生物，含有该组合物的药用组合物及其用途
公开(公告)号：US20070078184A1
公开(公告)日：2007-04-05
申请号：US10576753
申请日：2004-10-05
申请人： Junichi Kobayashi , Tetsuya Nakamura , Hideyuki Muranaka , Takehiro Ishikawa , Tetsuro Tamai , Satoshi Akahane
发明人： Junichi Kobayashi , Tetsuya Nakamura , Hideyuki Muranaka , Takehiro Ishikawa , Tetsuro Tamai , Satoshi Akahane
IPC分类号： A61K31/195 , C07C309/50
CPC分类号： C07D235/24 , C07C233/43 , C07C311/21
摘要： The present invention provides compounds represented by general formula (I): a prodrug thereof, or pharmaceutical acceptable salts thereof, wherein R1 is hydrogen or lower alkyl; each of R2 and R3 is independently hydrogen or lower alkyl; each of R4, R5 and R6 is independently hydrogen, halogen, lower alkyl or lower alkoxy; R7 is hydrogen or lower alkyl; R8 is hydrogen, halogen, lower alkyl, lower alkoxy, etc; R9 is —COR10, -A1-COR10, —O-A2-COR10, etc; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, —OCH2—, etc, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
摘要翻译：本发明提供由通式（I）表示的化合物：其前药或其药学上可接受的盐，其中R 1是氢或低级烷基; R2和R3各自独立地为氢或低级烷基; R 4，R 5和R 6各自独立地是氢，卤素，低级烷基或低级烷氧基; R 7是氢或低级烷基; R 8是氢，卤素，低级烷基，低级烷氧基等; R 9是-COR 10，-A 1 -OR 10，-OA 2， SUP> -COR 10等; Ar是任选取代的苯基或杂芳基; 并且A是表现出有效和选择性的β3肾上腺素受体刺激活性的键-OCH 2 - 2等。本发明还提供含有所述化合物的药物组合物及其用途。

9. 发明申请

US20050143457A1 Novel crystals of 5-hydroxycarbamimidoyl-2-hydroxybenzenesulfonamide derivative 失效
标题翻译： 5-羟基甲脒基-2-羟基苯磺酰胺衍生物的新晶体
公开(公告)号：US20050143457A1
公开(公告)日：2005-06-30
申请号：US10507616
申请日：2003-03-04
申请人： Harunobu Mukaiyama , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Satoshi Akahane
发明人： Harunobu Mukaiyama , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Satoshi Akahane
IPC分类号： A61P7/02 , C07C317/32 , A61K31/235 , C07C311/35
CPC分类号： C07C317/32
摘要： The present invention provides a novel crystalline form of n-butyl[4-[2-[2-hydroxy-5-(N-hydroxycarbamimidoyl) benzenesulfonylamino]ethyl]-2′-methanesulfonyl-3-yloxy] acetate hydrochloride, pharmaceutical compositions containing the same and their uses, which exhibits excellent inhibitory activities against activated blood coagulation factor X, and is useful for the treatment or prevention of a tromboembolic disease.
摘要翻译：本发明提供了一种新型的[4- [2- [2-羟基-5-（N-羟基甲脒基）苯磺酰基氨基]乙基] -2'-甲磺酰基-3-基氧基]乙酸盐酸盐的结晶形式，其含有对活化凝血因子X表现出优异的抑制活性，并且可用于治疗或预防血栓栓塞性疾病。

10. 发明授权

US07674938B2 Amino alcohol derivatives, pharmaceutical compositions containing the same, and use thereof 失效
标题翻译：氨基醇衍生物，含有它们的药物组合物及其用途
公开(公告)号：US07674938B2
公开(公告)日：2010-03-09
申请号：US11936680
申请日：2007-11-07
申请人： Junichi Kobayashi , Tetsuya Nakamura , Ritsu Suzuki , Hideyuki Muranaka , Tomonaga Ozawa , Yuichiro Kai , Takehiro Ishikawa , Tatsuhiro Kondo , Tetsuro Tamai , Satoshi Akahane
发明人： Junichi Kobayashi , Tetsuya Nakamura , Ritsu Suzuki , Hideyuki Muranaka , Tomonaga Ozawa , Yuichiro Kai , Takehiro Ishikawa , Tatsuhiro Kondo , Tetsuro Tamai , Satoshi Akahane
IPC分类号： C07C217/14 , C07C217/20 , C07D307/79 , A61K31/195 , A61P1/16 , A61P3/04
CPC分类号： C07D307/79 , A61K31/195 , C07C217/18 , C07C217/20 , C07C323/62 , C07C2601/04
摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
摘要翻译：本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢或低级烷基; R3，R4，R5和R6各自为氢，卤素，低级烷基或低级烷氧基; R 7和R 8各自为氢，卤素，低级烷基，卤代低级烷基，低级烷氧基，环烷基，芳基，杂芳基，氰基，羟基，低级酰基，羧基等; R9是-C（O）-R10，-A1-C（O）-R10，-O-A2-C（O）-R10或四唑-5-基，其表现出有效和选择性的3-肾上腺素受体刺激活动。本发明还提供含有所述化合物的药物组合物及其用途。

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