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1. 发明申请

US20110213158A9 Crystalline forms of thiazolidinedione compound and its manufacturing method 失效
公开(公告)号：US20110213158A9
公开(公告)日：2011-09-01
申请号：US12311610
申请日：2008-02-08
申请人： Hisaki Kajino , Yutaka Ikeuchi , Hiroshi Miyamoto , Eiji Numagami , Satoru Nihei
发明人： Hisaki Kajino , Yutaka Ikeuchi , Hiroshi Miyamoto , Eiji Numagami , Satoru Nihei
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： It is an object of the present invention to provide the crystalline form of a thiazolidinedione compound, which is effective as a pharmaceutical ingredient for manufacturing a peroxisome proliferator-activated receptor (PPAR) activator and an anticancer pharmaceutical composition. The present invention relates to a crystalline form of a hydrate of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione dihydrochloride represented by the following formula (I). [Formula 1]

2. 发明申请

US20110046388A1 Crystalline forms of thiazolidinedione compound and its manufacturing method 失效
标题翻译：噻唑烷二酮化合物的结晶形式及其制备方法
公开(公告)号：US20110046388A1
公开(公告)日：2011-02-24
申请号：US12311610
申请日：2008-02-08
申请人： Hisaki Kajino , Yutaka Ikeuchi , Hiroshi Miyamoto , Eiji Numagami , Satoru Nihei
发明人： Hisaki Kajino , Yutaka Ikeuchi , Hiroshi Miyamoto , Eiji Numagami , Satoru Nihei
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： It is an object of the present invention to provide the crystalline form of a thiazolidinedione compound, which is effective as a pharmaceutical ingredient for manufacturing a peroxisome proliferator-activated receptor (PPAR) activator and an anticancer pharmaceutical composition. The present invention relates to a crystalline form of a hydrate of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione dihydrochloride represented by the following formula (I). [Formula 1]
摘要翻译：本发明的目的是提供作为制备过氧化物酶体增殖物激活受体（PPAR）活化剂和抗癌药物组合物的药物成分的噻唑烷二酮化合物的结晶形式。本发明涉及5-（4 - {[6-（4-氨基-3,5-二甲基苯氧基）-1-甲基-1H苯并咪唑-2-基]甲氧基}苄基） -1,3-噻唑烷-2,4-二酮盐酸盐，由下式（I）表示。 [公式1]

3. 发明申请

US20120252854A1 CRYSTALLINE FORMS OF THIAZOLIDINEDIONE COMPOUND AND ITS MANUFACTURING METHOD 失效
标题翻译：噻唑烷二酮化合物的结晶形式及其制备方法
公开(公告)号：US20120252854A1
公开(公告)日：2012-10-04
申请号：US13465202
申请日：2012-05-07
申请人： Hisaki Kajino , Yutaka Ikeuchi , Hiroshi Miyamoto , Eiji Numagami , Satoru Nihei
发明人： Hisaki Kajino , Yutaka Ikeuchi , Hiroshi Miyamoto , Eiji Numagami , Satoru Nihei
IPC分类号： C07D417/12 , A61P35/02 , A61P35/00 , A61K31/427 , A61P3/10
CPC分类号： C07D417/12
摘要： A crystalline form of a hydrate of a dihydrochloride 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by the following formula: wherein the crystalline form shows main peaks at interplanar spacings of 10.42, 5.85, 5.52, 3.84, 3.46 and 2.95 angstroms in X-ray powder diffraction obtained with Cu Kα line radiation (wavelength λ=1.54 angstroms).
摘要翻译：二盐酸盐的水合物的结晶形式5-（4 - {[6-（4-氨基-3,5-二甲基苯氧基）-1-甲基-1H-苯并咪唑-2-基]甲氧基}苄基）-1 由下式表示的3-噻唑烷-2,4-二酮：其中结晶形式在CuKα线获得的X射线粉末衍射中显示在面间距为10.42,5.85,5.52,3.84,346和2.95埃的主峰辐射（波长λ= 1.54埃）。

4. 发明授权

US07816552B2 Intermediate of 6-substituted 1-methyl-1-H-benzimidazole derivative and method for producing same 失效
标题翻译： 6-取代的1-甲基-1-H-苯并咪唑衍生物的中间体及其制备方法
公开(公告)号：US07816552B2
公开(公告)日：2010-10-19
申请号：US11664140
申请日：2005-09-26
申请人： Hisaki Kajino , Hiroshi Miyamoto , Rei Okazaki , Yutaka Ikeuchi
发明人： Hisaki Kajino , Hiroshi Miyamoto , Rei Okazaki , Yutaka Ikeuchi
IPC分类号： C07C271/28 , C07C217/90
CPC分类号： C07D277/34 , C07C217/90 , C07C271/28 , C07C323/36 , C07D417/12
摘要： A method for preparing a compound having the following formula (I) by reducing a nitro group of the following formula (III) followed by carrying out an intramolecular dehydration condensation, wherein R2 is hydrogen, alkyl, cycloalkyl, phenyl or a 5- or 6-membered heterocyclic, and X is oxygen, sulfur or nitrogen.
摘要翻译：一种通过还原下式（III）的硝基进行分子内脱水缩合制备具有下式（I）的化合物的方法，其中R 2是氢，烷基，环烷基，苯基或5-或6 X是氧，硫或氮。

5. 发明授权

US08106079B2 Intermediate of 6-substituted-1-methyl-1-H-benzimidazole derivative and method for producing same 失效
标题翻译： 6-取代-1-甲基-1-H-苯并咪唑衍生物的中间体及其制备方法
公开(公告)号：US08106079B2
公开(公告)日：2012-01-31
申请号：US12800612
申请日：2010-05-19
申请人： Hisaki Kajino , Hiroshi Miyamoto , Yutaka Ikeuchi
发明人： Hisaki Kajino , Hiroshi Miyamoto , Yutaka Ikeuchi
IPC分类号： A61K31/427 , C07D417/12 , C07D277/34
CPC分类号： C07D277/34 , C07C217/90 , C07C271/28 , C07C323/36 , C07D417/12
摘要： A compound having the following formula (III) wherein R2 is hydrogen, alkyl, cycloalkyl, phenyl or a 5- or 6-membered heterocyclic, and X is oxygen, sulfur or nitrogen, and a method for preparing said compound.
摘要翻译：具有下式（III）的化合物，其中R 2是氢，烷基，环烷基，苯基或5-或6-元杂环，X是氧，硫或氮，以及制备所述化合物的方法。

6. 发明申请

US20100234612A1 Intermediate of 6-substituted-1-methyl-1-H-benzimidazole derivative and method for producing same 失效
标题翻译： 6-取代-1-甲基-1-H-苯并咪唑衍生物的中间体及其制备方法
公开(公告)号：US20100234612A1
公开(公告)日：2010-09-16
申请号：US12800612
申请日：2010-05-19
申请人： Hisaki Kajino , Hiroshi Miyamoto , Yutaka Ikeuchi
发明人： Hisaki Kajino , Hiroshi Miyamoto , Yutaka Ikeuchi
IPC分类号： C07D277/34
CPC分类号： C07D277/34 , C07C217/90 , C07C271/28 , C07C323/36 , C07D417/12
摘要： A compound having the following formula (III) wherein R2 is hydrogen, alkyl, cycloalkyl, phenyl or a 5- or 6-membered heterocyclic, and X is oxygen, sulfur or nitrogen, and a method for preparing said compound.
摘要翻译：具有下式（III）的化合物，其中R 2是氢，烷基，环烷基，苯基或5-或6-元杂环，X是氧，硫或氮，以及制备所述化合物的方法。

7. 发明申请

US20090023929A1 Intermediate of 6-Substituted 1-Methyl-1-H-Benzimidazole Derivative and Method for Producing Same 失效
标题翻译： 6-取代的1-甲基-1H-苯并咪唑衍生物的中间体及其制备方法
公开(公告)号：US20090023929A1
公开(公告)日：2009-01-22
申请号：US11664140
申请日：2005-09-26
申请人： Hisaki Kajino , Hiroshi Miyamoto , Rei Okazaki , Yutaka Ikeuchi
发明人： Hisaki Kajino , Hiroshi Miyamoto , Rei Okazaki , Yutaka Ikeuchi
IPC分类号： C07D277/04 , C07C217/90 , C07C271/28
CPC分类号： C07D277/34 , C07C217/90 , C07C271/28 , C07C323/36 , C07D417/12
摘要： A method for preparing a compound having the following formula (I) by reducing a nitro group of the following formula (III) followed by carrying out an intramolecular dehydration condensation, wherein R2 is hydrogen, alkyl, cycloalkyl, phenyl or a 5- or 6-membered heterocyclic, and X is oxygen, sulfur or nitrogen.
摘要翻译：一种通过还原下式（III）的硝基进行分子内脱水缩合制备具有下式（I）的化合物的方法，其中R 2是氢，烷基，环烷基，苯基或5-或6 X是氧，硫或氮。

8. 发明申请

US20110092555A1 Thiazolidinedione compound 审中-公开
标题翻译：噻唑烷二酮化合物
公开(公告)号：US20110092555A1
公开(公告)日：2011-04-21
申请号：US12928525
申请日：2010-12-14
申请人： Yoshitaka Nakamura , Chiharu Satoh , Hiroshi Miyamoto , Hisaki Kajino
发明人： Yoshitaka Nakamura , Chiharu Satoh , Hiroshi Miyamoto , Hisaki Kajino
IPC分类号： A61K31/427 , C07D417/12 , C07D277/34 , A61P3/10 , A61P9/12 , A61P9/10 , A61P15/08
CPC分类号： C07D417/12 , C07D277/34 , Y02P20/55
摘要： A compound which is 5-{4-[(6-methoxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzyl}thiazolidine-2,4-dione hydrochloride, in crystal form wherein a powder x-ray diffraction pattern obtained by irradiation with a Cu Kα line shows main peaks at interplanar spacings d=14.29, 7.12, 5.34, 4.97, 4.74, 3.95, 3.85, 3.75, 3.55, 3.51, 3.15, 2.84, 2.76, 2.52 and 2.37.
摘要翻译：一种结晶形式的5- {4 - [（6-甲氧基-1-甲基-1H-苯并咪唑-2-基）甲氧基]苄基}噻唑烷-2,4-二酮盐酸盐的化合物，其中粉末X射线衍射通过用CuKα线照射获得的图案在晶面间距处显示主峰d = 14.29,7.12,2.534,4.97,44.75,3.95,3.85,3.75,3.55,3.51,3.15,2.84,2.72,2.52和2.37。

9. 发明申请

US20080103185A1 Process for Producing Thiazolidinedione Compound and Production Intermediate Thereof 审中-公开
标题翻译：生产噻唑烷二酮化合物及其制备方法
公开(公告)号：US20080103185A1
公开(公告)日：2008-05-01
申请号：US11795270
申请日：2006-01-24
申请人： Yoshitaka Nakamura , Chiharu Satoh , Hiroshi Miyamoto , Hisaki Kajino
发明人： Yoshitaka Nakamura , Chiharu Satoh , Hiroshi Miyamoto , Hisaki Kajino
IPC分类号： A61K31/427 , A61P3/00 , A61P3/06 , A61P3/10 , A61P9/10 , C07D417/12
CPC分类号： C07D417/12 , C07D277/34 , Y02P20/55
摘要： There are provided crystals of a thiazolidinedione derivative having excellent prophylactic and therapeutic effects on a disease caused by insulin resistance and a process for producing the thiazolidinedione derivative with a high purity. As described above, a process for producing a compound represented by the general formula (A) or a salt thereof, comprising converting 4-[(2,4-dioxothiazolidin-5-yl)methyl]phenoxyacetic acid represented by the following formula into a compound of the general formula (I), wherein X=a halogen atom; then reacting the compound with a compound represented by the general formula (II), wherein R1, R2, R3 and R4=a hydrogen atom, a hydroxyl group, C1-C6 alkyl, C1-C6 alkoxy, benzyloxy, acetoxy, trifluoromethyl or a halogen atom, R5=C1-C6 alkyl, and R6=a protecting group for an amino group, to produce a compound represented by the general formula (III); and subsequently cyclizing the compound into the final product, and crystals of a compound represented by the general formula (A) or a salt thereof.
摘要翻译：提供了对由胰岛素抵抗引起的疾病具有优异的预防和治疗效果的噻唑烷二酮衍生物的晶体和具有高纯度的噻唑烷二酮衍生物的制备方法。如上所述，制备由通式（A）表示的化合物或其盐的方法，包括将由下式表示的4 - [（2,4-二氧代噻唑烷-5-基）甲基]苯氧基乙酸转化为通式（I）的化合物，其中X =卤素原子; 然后使化合物与通式（II）表示的化合物反应，其中R 1，R 2，R 3和R SUP > 4 =氢原子，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，苄氧基，乙酰氧基，三氟甲基或卤素原子，R 5 = C 1 -C 6烷基，和R 6 =氨基的保护基，以制备由通式（III）表示的化合物。随后将化合物环化成最终产物，和由通式（A）表示的化合物或其盐的晶体。

10. 发明授权

US09115661B2 Fuel injection amount control system and fuel injection amount control device for multi-cylinder internal combustion engine 有权
标题翻译：燃油喷射量控制系统和多缸内燃机燃油喷射量控制装置
公开(公告)号：US09115661B2
公开(公告)日：2015-08-25
申请号：US13194922
申请日：2011-07-30
申请人： Yasushi Iwazaki , Hiroshi Miyamoto
发明人： Yasushi Iwazaki , Hiroshi Miyamoto
IPC分类号： G06F7/00 , G06F17/00 , F02D41/30 , F02D41/14 , F02D41/24
CPC分类号： F02D41/1441 , F02D41/2493 , F02D2041/1432 , Y02T10/22
摘要： A fuel injection amount control system corrects the amount of fuel injected from each fuel injection valve in a feedback manner, based on an output value of an upstream air-fuel ratio sensor, so that the air-fuel ratio of exhaust gas flowing into a three-way catalyst coincides with a target air-fuel ratio. Also, the control system performs a high-pass filtering operation on the output value of the upstream air-fuel ratio sensor, so as to obtain a post-high-pass-filtering output value by removing a component that varies with variations in the center air-fuel ratio of the engine, from the output value of the upstream air-fuel ratio sensor. Then, the control system acquires an air-fuel ratio imbalance index value that increases as the degree of ununiformity in the air-fuel ratio among cylinders is larger, based on the post-high-pass-filtering output value.
摘要翻译：燃料喷射量控制系统基于上游空燃比传感器的输出值，以反馈方式校正从每个燃料喷射阀喷射的燃料量，使得流入三个燃料喷射量的排气的空燃比 - 催化剂与目标空燃比一致。此外，控制系统对上游空燃比传感器的输出值进行高通滤波操作，以便通过去除随中心变化而变化的分量来获得后高通滤波输出值发动机的空燃比从上游空燃比传感器的输出值。然后，控制系统基于后高通滤波输出值，获取随着气缸中的空燃比的不均匀程度越大而增加的空燃比不平衡指数值。

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