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1. 发明授权

US08236834B2 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：US08236834B2
公开(公告)日：2012-08-07
申请号：US12311610
申请日：2008-02-08
申请人： Hisaki Kajino , Yutaka Ikeuchi , Eiji Numagami
发明人： Hisaki Kajino , Yutaka Ikeuchi , Eiji Numagami
IPC分类号： A61K31/427 , C07D277/34
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]

2. 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。

3. 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。

4. 发明授权

US5212322A Macrolide compounds, their preparation and their use 失效
标题翻译：大环内酯类化合物，其制备及其用途
公开(公告)号：US5212322A
公开(公告)日：1993-05-18
申请号：US644100
申请日：1991-01-22
申请人： Takao Okazaki , Shuji Takahashi , Seigo Iwado , Keiji Tanaka , Toshiaki Yanai , Hisaki Kajino
发明人： Takao Okazaki , Shuji Takahashi , Seigo Iwado , Keiji Tanaka , Toshiaki Yanai , Hisaki Kajino
IPC分类号： A01N49/00 , C07H19/01 , C12P17/18
CPC分类号： C07H19/01 , A01N49/00 , C12P17/181 , Y02P20/55 , Y10S424/08
摘要： Compounds with acaricidal, insecticidal and anthelmintic activities have the formula: ##STR1## wherein: --X--Y-- is selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHOH--, --CH.dbd.CH--, and --CH.sub.2 --C(.dbd.O)--;R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, an isopropyl group, a sec-butyl group and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group;R.sup.2 represents a group of formula --(CH.sub.2).sub.n --C(R.sup.6).dbd.C(R.sup.7)(R.sup.8) in which n is 0, 1 or 2, R.sup.6 and R.sup.7 each is selected from the group consisting of a hydrogen atom and a methyl group and R.sup.8 is selected from the group consisting of a hydrogen atom, a C.sub.1-4 alkyl group, a phenyl group and a phenyl group substituted with at least one substituent selected from the group consisting of halogen, methyl and nitro substituents;R.sup.3 is selected from the group consisting of a hydrogen atom, a methyl group, a hydroxy-protecting group, an ester-forming carboxylic acid residue, and an ester-forming carbonic acid residue; andR.sup.4 is selected from the group consisting of a hydrogen atom and an .alpha.-L-oleandrosyl-.alpha.-L-oleandrosyloxy group, with the proviso that R.sup.4 represents a hydrogen atom when the group R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group.
摘要翻译：具有杀螨，杀虫和驱虫活性的化合物具有下式：其中：-XY-选自-CH 2 -CH 2 - ， - CH 2 -CHOH - ， - CH = CH-和 - CH2-C（= O） - ; R 1选自甲基，乙基，异丙基，仲丁基和式-C（CH 3）= CHR 5的基团，其中R 5选自甲基，乙基和异丙基; R 2表示式 - （CH 2）n C（R 6）= C（R 7）（R 8）的基团，其中n为0,1或2，R 6和R 7各自为氢原子和甲基并且R 8选自氢原子，C 1-4烷基，苯基和被至少一个选自卤素，甲基和硝基取代基的取代基取代的苯基; R3选自氢原子，甲基，羟基保护基，成酯羧酸残基和形成酯的碳酸残基; 并且R 4选自氢原子和α-L-甘氨酰基-α-L-胆碱基氧基，条件是当R 1选自甲基时，R 4表示氢原子，乙基和式-C（CH 3）= CHR 5基团，其中R 5选自甲基，乙基和异丙基。

5. 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）。

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

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]

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. 发明申请

US20120238759A1 METHOD FOR MANUFACTURING A 6-SUBSTITUTED 1-METHYL-1H-BENZIMIDAZOLE DERIVATIVE AND AN INTERMEDIATE OF SAID METHOD 审中-公开
标题翻译：制备6-取代的1-甲基-1H-苯并咪唑衍生物的方法和所述方法的中间体
公开(公告)号：US20120238759A1
公开(公告)日：2012-09-20
申请号：US13511190
申请日：2010-11-25
申请人： Yutaka Ikeuchi , Chiharu Satoh , Eiji Numagami , Satoru Nihei , Hisaki Kajino
发明人： Yutaka Ikeuchi , Chiharu Satoh , Eiji Numagami , Satoru Nihei , Hisaki Kajino
IPC分类号： C07D417/12 , C07C217/90 , C07C213/02 , C07D277/34
CPC分类号： C07C213/02 , A61K31/427 , C07C217/90 , C07D277/34 , C07D417/12 , Y02P20/55
摘要： A method for manufacturing a 6-substituted 1-methyl-1H-benzimidazole derivative represented by the formula (IV) wherein R3 represents a hydrogen atom or a C1-C4 alkyl group. A 4-substituted N2-methylbenzene-1,2-diamine derivative is prepared from a particular 5-substituted N-methyl-2-nitroaniline derivative, subsequently reacting the resulting compound with {4-[(2,4-dioxo-1,3-thiazolidin-5-yl)methyl]phenoxy}acetic acid or an acid chloride or a mixed acid anhydride thereof, and subsequently subjecting the resulting compound to intramolecular dehydration condensation. A compound of the formula (II) wherein R1 represents a hydrogen atom, a C1-C4 alkyl group, or a protective group for the nitrogen atom, and R2 represents a hydrogen atom or a protective group for the nitrogen atom is prepared and used as an intermediate.
摘要翻译：制备由式（IV）表示的6-取代的1-甲基-1H-苯并咪唑衍生物的方法，其中R 3表示氢原子或C 1 -C 4烷基。 4-取代的N-甲基苯-1,2-二胺衍生物由特定的5-取代的N-甲基-2-硝基苯胺衍生物制备，随后将得到的化合物与{4 - [（2,4-二氧代-1,2-二氢 - 3-噻唑烷-5-基）甲基]苯氧基}乙酸或其酰氯或其混合酸酐，然后将所得化合物进行分子内脱水缩合。制备式（II）化合物，其中R1表示氢原子，C1-C4烷基或氮原子的保护基，R2表示氢原子或氮原子的保护基，并用作一个中间人

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