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21. 发明申请

US20110034679A1 HEMIFUMARATE OF A PYRAZOLE DERIVATIVE 有权
标题翻译：吡唑衍生物的高密度脂蛋白
公开(公告)号：US20110034679A1
公开(公告)日：2011-02-10
申请号：US12988273
申请日：2009-04-13
申请人： Hideki Takeuchi , Eiji Tsuru
发明人： Hideki Takeuchi , Eiji Tsuru
IPC分类号： C07H17/02
CPC分类号： C07H17/02
摘要： The present invention provides a novel form of 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}-propylamino)-2,2-dimethylpropionamide hemifumarate dihydrate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.
摘要翻译：本发明提供3-（3- {4- [3-（＆bgr。-D-吡喃葡萄糖氧基）-5-异丙基-1H-吡唑-4-基甲基] -3-甲基苯氧基}丙基氨基）具有改善的储存稳定性的2-二甲基丙酰胺。由于3-（3- {4- [3-（＆bgr。-D-吡喃葡萄糖氧基）-5-异丙基-1H-吡唑-4-基甲基] -3-甲基苯氧基} - 丙基氨基）-2,2-二甲基丙酰胺半富马酸盐二水合物极好的储存稳定性，作为药物有用。此外，其显示出非常好的结晶性，并且可以通过方便的方法进行纯化，因此适用于工业制备。

22. 发明授权

US07763654B2 Crystal polymorph of hydroxynorephedrin derivative hydrochloride 失效
标题翻译：羟基去甲基苯酚衍生物盐酸盐的晶体多晶型物
公开(公告)号：US07763654B2
公开(公告)日：2010-07-27
申请号：US11912407
申请日：2006-04-24
申请人： Kiyoshi Kasai , Michio Toda
发明人： Kiyoshi Kasai , Michio Toda
IPC分类号： A61K31/24 , C07C229/00
CPC分类号： C07C217/60
摘要： The present invention provides a novel crystal polymorph of ethyl (−)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride which can be determined by characteristic diffraction peaks of the powder X-ray diffraction or the like, and obtained from ethyl (−)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.
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] 可以通过粉末X射线衍射等的特征衍射峰确定，并由（ - ） - 2- [4- [2 - [[1S，2R] -2- 羟基-2-（4-羟基苯基）-1-甲基乙基]氨基]乙基] -2,5-二甲基苯氧基乙酸酯。

23. 发明申请

US20100081674A1 FUSED HETEROCYCLIC DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE DERIVATIVE, AND USE OF THE COMPOSITION FOR MEDICAL PURPOSES 有权
标题翻译：融合的杂环衍生物，包含衍生物的药物组合物，以及用于医疗用途的组合物的用途
公开(公告)号：US20100081674A1
公开(公告)日：2010-04-01
申请号：US12595931
申请日：2008-04-16
申请人： Kohsuke Ohno , Noboru Kamada
发明人： Kohsuke Ohno , Noboru Kamada
IPC分类号： A61K31/519 , C07D495/04
CPC分类号： C07D495/04
摘要： The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides fused heterocyclic derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A is 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA is halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; ring B is aryl or heteroaryl; RB is halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; E1 and E2 are oxygen atom, etc.; Q is hydrogen atom, alkyl, alkylsulfonyl, acyl, etc.; X is -(alkylene)-Z, —CO—Y, —SO2—Y, etc. (in which Y is Z or amino, etc.; Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
摘要翻译：本发明提供了可用作预防或治疗性激素依赖性疾病等的试剂的化合物。也就是说，本发明提供具有GnRH拮抗活性的由以下通式（I）表示的稠合杂环衍生物，含有它们的药物组合物，其药用用途等。在式（I）中，环A是5元环状不饱和烃或5元杂芳基; RA是卤素，烷基，烯基，炔基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; 环B是芳基或杂芳基; RB是卤素，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; E1和E2是氧原子等; Q是氢原子，烷基，烷基磺酰基，酰基等; X是 - （亚烷基）-Z，-CO-Y，-SO2-Y等（其中Y是Z或氨基等; Z是环烷基，杂环烷基，芳基，杂芳基等）

24. 发明申请

US20100056521A1 (AZA)INDOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 有权
标题翻译：（AZA）INDOLE DERIVATIVE及其用于医疗用途
公开(公告)号：US20100056521A1
公开(公告)日：2010-03-04
申请号：US12595476
申请日：2008-04-10
申请人： Kazuo Shimizu , Yasushi Takigawa , Hideki Fujikura , Masato Iizuka , Masahiro Hiratochi , Norihiko Kikuchi
发明人： Kazuo Shimizu , Yasushi Takigawa , Hideki Fujikura , Masato Iizuka , Masahiro Hiratochi , Norihiko Kikuchi
IPC分类号： A61K31/404 , C07D209/18 , C07D409/12 , C07D413/10 , C07D401/04 , C07D471/04 , A61K31/4439 , A61K31/5377 , A61P43/00
CPC分类号： C07D209/30 , A61K31/165 , A61K31/404 , A61K31/407 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D209/42 , C07D401/04 , C07D405/04 , C07D405/10 , C07D409/12 , C07D417/04 , C07D471/04 , C07D491/056 , A61K2300/00
摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, nitro, alkyl, alkoxy and the like; X1, X2 and X3 independently represent CR2 or N; R1 and R2 independently represent halogen, cyano, haloalkyl, A-D-E-G, —N(-D-E-G)2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO2 and the like.
摘要翻译：本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的（aza）吲哚衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病，其前药或盐其中。在式（I）中，T表示硝基或氰基等; 环J表示芳基或杂芳基等; Q表示羧基或5-四唑基等; Y表示H，OH，NH 2，卤素，硝基，烷基，烷氧基等; X1，X2和X3独立地表示CR2或N; R 1和R 2独立地表示卤素，氰基，卤代烷基，A-D-E-G，-N（-D-E-G）2等，式中，A表示单键O，S等; D和G独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E表示单键O，S，COO，SO 2等。

25. 发明授权

US07666899B2 Pharmaceutical composition for treatment of lipid metabolism disorder 失效
标题翻译：用于治疗脂质代谢紊乱的药物组合物
公开(公告)号：US07666899B2
公开(公告)日：2010-02-23
申请号：US11596109
申请日：2005-04-27
申请人： Juichi Fukuyama , Masayuki Yamada
发明人： Juichi Fukuyama , Masayuki Yamada
IPC分类号： A61K31/40
CPC分类号： A61K31/4035 , Y10S514/866
摘要： The present invention provides pharmaceutical compositions for the prevention or treatment of lipid metabolism disorders. The pharmaceutical compositions comprising, as an active ingredient, (2S)-2-benzl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic aid (generic name: mitiglinide) or a pharmaceutically acceptable salt thereof, or a hydrate thereof exert remarkable lipid metabolism improving effect, and are useful for, for example, hyperlipidemia such as hypertriglyceridemia of diabetic patients or the like.
摘要翻译：本发明提供了用于预防或治疗脂质代谢紊乱的药物组合物。作为活性成分的（2S）-2-苄基-3-（顺式 - 六氢-2-异吲哚啉基羰基）丙酸（通用名：米格列奈）或其药学上可接受的盐或其水合物的药物组合物发挥显着的作用脂质代谢改善效果，并且可用于例如高脂血症如糖尿病患者的高甘油三酯血症等。

26. 发明申请

US20100029919A1 PYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE IN PRODUCING THE SAME 失效
标题翻译：吡唑衍生物，含有该药物的药物组合物，在其生产中的药物用途及其中间体
公开(公告)号：US20100029919A1
公开(公告)日：2010-02-04
申请号：US12534452
申请日：2009-08-03
申请人： Hideki Fujikura , Norihiko Kikuchi , Shigeki Tazawa , Tokuhisa Yamato , Masayuki Isaji
发明人： Hideki Fujikura , Norihiko Kikuchi , Shigeki Tazawa , Tokuhisa Yamato , Masayuki Isaji
IPC分类号： C07H17/02
CPC分类号： C07D405/04 , A61K31/7056 , C07D231/20 , C07D401/04 , C07D409/04 , C07H17/02 , Y10S514/866
摘要： The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group selected from the following groups: , and the other represents —(CH2)n—Ar wherein Ar represents an optionally substituted C6-10 aryl group or an optionally substituted C1-9 heteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted C1-6 alkoxyl group, an optionally substituted amino group, an optionally substituted C2-9 heterocycloalkyl group or an optionally substituted heterocycle-fused phenyl group; R represents an optionally substituted C3-8 cycloalkyl group, an optionally substituted C6-10 aryl group etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose or a disease associated with hyperglycemia (e.g., diabetic complications, diabetes, etc.), and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.
摘要翻译：本发明提供由以下通式表示的吡唑衍生物：其中R1表示H，任选取代的C 1-6烷基等; Q和T中的一个表示选自以下基团的基团：另一个表示 - （CH 2）n -Ar，其中Ar表示任选取代的C 6-10芳基或任选取代的C 1-8杂芳基; n表示0〜2的整数，可以具有取代基的C 1-6烷氧基，可以具有取代基的氨基，可以具有取代基的C2-9杂环烷基或任意取代的杂环稠合苯基; R表示任选取代的C 3-8环烷基，任选取代的C 6-10芳基等，其药学上可接受的盐或其前体药物，其在人1,5-脱水葡萄糖醇/果糖/甘露糖转运蛋白中表现出优异的抑制活性，可用作预防，抑制与选自葡萄糖，果糖和甘露糖中的至少一种碳水化合物或与高血糖相关疾病（例如，糖尿病并发症，糖尿病等）的过量摄取相关疾病进展或治疗的药剂。），以及包含该药物组合物的药物组合物，其药学用途及其生产用中间体。

27. 发明申请

US20090325900A1 FUSED HETEROCYCLIC DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND MEDICINAL USE THEREOF 有权
标题翻译：熔化的杂环衍生物，含有它们的药物组合物及其药物用途
公开(公告)号：US20090325900A1
公开(公告)日：2009-12-31
申请号：US12089674
申请日：2006-10-17
申请人： Kohsuke Ohno , Takashi Miyagi , Tomonaga Ozawa , Nobuhiko Fushimi
发明人： Kohsuke Ohno , Takashi Miyagi , Tomonaga Ozawa , Nobuhiko Fushimi
IPC分类号： A61K31/695 , C07D215/58 , C07D211/72 , C07D311/02 , A61K31/47 , A61K31/44 , C07D223/16 , A61K31/55 , A61P5/24
CPC分类号： C07D495/04
摘要： The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O— (alkylene)-Y, —O-Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.
摘要翻译：本发明提供了可用作预防或治疗性激素依赖性疾病等的药剂的化合物。也就是说，本发明提供由以下通式（I）表示的稠合杂环衍生物，含有该杂环衍生物的药物组合物，其医药用途等。在式（I）中，环A表示5元环状不饱和烃或5元杂芳基; 烷基，烯基，炔基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; 环B表示芳基或杂芳基; RB代表卤素，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; E1和E2表示氧原子等; U表示单键或亚烷基; X表示Y表示的基团，-SO 2 -Y，-O-（亚烷基）-Y，-O-Z，Y表示Z，氨基等; Z表示环烷基，杂环烷基，芳基，杂芳基等; 或类似物。

28. 发明申请

US20090163571A1 PHARMACEUTICAL FOR USE IN THE TREATMENT OF URETEROLITHIASIS 审中-公开
标题翻译：用于治疗尿毒症的药物
公开(公告)号：US20090163571A1
公开(公告)日：2009-06-25
申请号：US12093230
申请日：2006-11-22
申请人： Mamoru Kobayashi , Yoshitaka Tomiyama , Kumi Kobayashi
发明人： Mamoru Kobayashi , Yoshitaka Tomiyama , Kumi Kobayashi
IPC分类号： A61K31/404 , A61P13/00
CPC分类号： C07D209/08 , A61K31/4045
摘要： The present invention provides pharmaceutical compositions useful for relieving pain caused by ureteral calculi, facilitating exclusion of ureteral calculi or the like. That is, the present invention provides a pharmaceutical composition for the treatment of ureteral lithiasis, which comprises as an active ingredient an indoline derivative represented by the following general formula (I) or a salt thereof. In the formula, R represents saturated or unsaturated aliphatic acyl which may have a substituent; hydroxyalkyl; aliphatic acyloxyalkyl; lower alkyl which has as a substituent lower alkoxy, carboxy, lower alkoxycarbonyl, aryl-substituted lower alkoxycarbonyl, carbamoyl, mono or di(lower alkyl)-substituted carbamoyl or cyano; optionally substituted aromatic acyl; furoyl or pyridylcarbonyl; R1 represents cyano or carbamoyl; and R2 represents lower alkyl which may have as a substituent halogen, cyano or aryl.
摘要翻译：本发明提供了用于缓解由输尿管结石引起的疼痛，有助于排除输尿管结石等的药物组合物。也就是说，本发明提供了用于治疗输尿管结石的药物组合物，其包含作为活性成分的由以下通式（I）表示的二氢吲哚衍生物或其盐。在该式中，R表示可具有取代基的饱和或不饱和脂肪族酰基; 羟烷基; 脂肪酰氧基烷基; 羧基，低级烷氧基羰基，芳基取代的低级烷氧基羰基，氨基甲酰基，一或二（低级烷基）取代的氨基甲酰基或氰基的低级烷基; 任选取代的芳族酰基; 糠酰基或吡啶基羰基; R1表示氰基或氨基甲酰基; 并且R 2表示可以具有卤素，氰基或芳基的取代基的低级烷基。

29. 发明申请

US20090043110A1 Asymmetric Reduction Method 失效
标题翻译：不对称还原法
公开(公告)号：US20090043110A1
公开(公告)日：2009-02-12
申请号：US12087092
申请日：2006-12-26
申请人： Yoshinori Matsumoto , Yuki Takeuchi , Hiroyuki Yamamoto
发明人： Yoshinori Matsumoto , Yuki Takeuchi , Hiroyuki Yamamoto
IPC分类号： C07D209/44
CPC分类号： C07B53/00 , C07D209/44
摘要： The present invention is to provide a novel method for producing (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid which is useful as a therapeutic agent for diabetes. The present invention relates to a method for producing (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid, which is characterized in that 2-benzylidene-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid is subjected to a catalytic reduction reaction in the presence of an asymmetric catalyst prepared from a pyrrolidinebisphosphine compound (I) represented by the following general formula (I): wherein, R1 represents a linear or branched alkyl group having 1-10 carbon atoms, cycloalkyl group, aralkyl group or aryl group which may respectively have a substituent; and R2 and R3 independently represent an optionally substituted aryl group. The * mark in the pyrrolidine ring shows that the carbon atom at that position has the S configuration, and a rhodium compound.
摘要翻译：本发明提供可用作糖尿病治疗剂的（2S）-2-苄基-3-（顺式 - 六氢-2-异吲哚基羰基）丙酸的新方法。本发明涉及（2S）-2-苄基-3-（顺 - 六氢-2-异二氢吲哚基羰基）丙酸的制备方法，其特征在于2-亚苄基-3-（顺式 - 六氢-2-异吲哚基羰基））丙酸在由以下通式（I）表示的吡咯烷二膦化合物（I）制备的不对称催化剂存在下进行催化还原反应：其中，R1表示具有1-10个碳原子的直链或支链烷基原子，环烷基，芳烷基或可分别具有取代基的芳基; 并且R 2和R 3独立地表示任选取代的芳基。吡咯烷环中的*标记表示该位置的碳原子具有S构型和铑化合物。

30. 发明授权

US07465713B2 Glucopyranosyloxypyrazole derivatives and use thereof in medicines 有权
标题翻译：吡喃葡萄糖氧吡唑衍生物及其在药物中的应用
公开(公告)号：US07465713B2
公开(公告)日：2008-12-16
申请号：US11247216
申请日：2005-10-12
申请人： Hideki Fujikura , Nobuhiko Fushimi , Toshihiro Nishimura , Takeshi Nakabayashi , Masayuki Isaji
发明人： Hideki Fujikura , Nobuhiko Fushimi , Toshihiro Nishimura , Takeshi Nakabayashi , Masayuki Isaji
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： A61K45/06 , A61K31/7056 , C07H17/02 , A61K2300/00
摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts 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表示氢原子，低级烷基或形成前药的基团; Q和T之一表示由通式表示的基团：（其中P表示氢原子或形成前药的基团），而另一个表示低级烷基或卤代（低级烷基）基团; R2表示氢原子，低级烷基，低级烷氧基，低级烷硫基，卤代（低级烷基）或卤素原子; 并且条件是当R表示氢原子或低级烷基时，P不表示氢原子，或其药学上可接受的盐，其在人SGLT2中具有抑制活性并具有改善的口服吸收，因此可用作用于预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂及其药学上可接受的盐及其药学用途。

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