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51. 发明申请

US20060004044A1 3-glyoxylamideindoles for treating cancer 审中-公开
标题翻译： 3-乙醛酰胺吲哚治疗癌症
公开(公告)号：US20060004044A1
公开(公告)日：2006-01-05
申请号：US11136074
申请日：2005-05-24
申请人： Keizo Koya , Lijun Sun , Mitsunori Ono , Guiqing Liang , David James , Hao Li , Zhi-Qiang Xia
发明人： Keizo Koya , Lijun Sun , Mitsunori Ono , Guiqing Liang , David James , Hao Li , Zhi-Qiang Xia
IPC分类号： A61K31/4709 , A61K31/425 , A61K31/42 , A61K31/4196 , A61K31/405
CPC分类号： C07D249/08 , C07D209/12 , C07D209/18 , C07D231/12 , C07D233/56 , C07D401/12 , C07D403/12 , C07D405/14 , C07D413/12 , C07D417/12
摘要： Disclosed is an anti-cancer compound represented by Structural Formula (I): The variables in Structural Formula (I) are described hereinbelow. Also disclosed is a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by Structural Formula (I) (preferably an effective amount). Also disclosed is a method of treating a subject with cancer by administering to the subject an effective amount of a compound represented by Structural Formula (I).
摘要翻译：公开了由结构式（I）表示的抗癌化合物：结构式（I）中的变量如下所述。还公开了包含药学上可接受的载体或稀释剂和由结构式（I）表示的化合物（优选有效量））的药物组合物。还公开了通过向受试者施用有效量的由结构式（I）表示的化合物来治疗患有癌症的受试者的方法。

52. 发明申请

US20050272766A1 1-Glyoxylamide indolizines for treating lung and ovarian cancer 审中-公开
标题翻译： 1-乙酰氧基吲哚啉用于治疗肺癌和卵巢癌
公开(公告)号：US20050272766A1
公开(公告)日：2005-12-08
申请号：US11088253
申请日：2005-03-23
申请人： Keizo Koya , Lijun Sun , Hao Li , Mitsunori Ono
发明人： Keizo Koya , Lijun Sun , Hao Li , Mitsunori Ono
IPC分类号： A61K31/437 , A61K31/4745
CPC分类号： A61K31/437 , A61K31/4745
摘要： A method of treating a subject having lung cancer or ovarian cancer, comprising administering to the subject an effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt, solvate, or polymorph thereof: Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z1 and Z2 are independently ═O, ═S, ═N—OR12 or ═NR12 R1 and R2 are independently —H, an aliphatic group, a substituted aliphatic group, an unsubstituted non-aromatic heterocylic group, a substituted non-aromatic heterocylic group, an aryl group or a substituted aryl group, provided that R1 and R2 are not both —H. Alternatively, —NR1R2, taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, —C(R4R5)—, —N(R4)—, —O—, —S—, —S(O)—, —S(O)2—, —C(═O)—, —C(═O)—N(R4)—, or —N(R4)—C(═O)—. R4 and R5 are independently —H or a substituted or unsubstituted aliphatic group. R12 is —H or a substituted or unsubstituted alkyl group.
摘要翻译：一种治疗患有肺癌或卵巢癌的受试者的方法，其包括向所述受试者施用有效量的由结构式（I）表示的化合物或其药学上可接受的盐，溶剂化物或多晶型物：环A是取代或未取代的，任选地与芳基稠合。 Z 1和Z 2独立地是-O，-S，-N-OR 12或-NR 12， R 1和R 2独立地是-H，脂族基团，取代的脂族基团，未取代的非芳族杂环基团，取代的非芳族杂环基团，芳基或取代的芳基，条件是R 1和R 2不同时为-H。或者，-NR 1 R 2 R 2一起是取代或未取代的非芳族含氮杂环基或取代或未取代的含氮杂芳基。 R 3是取代或未取代的芳基或取代或未取代的脂族基。 X是共价键，-C（R 4 R 5） - ， - N（R 4） - ， - O - ， - ，-S（O） - ， - S（O）2 - ， - C（ - ） - >） - 或-N（R 4） - C（-O） - 。 R 4和R 5独立地是-H或取代或未取代的脂族基团。 R 12是-H或取代或未取代的烷基。

53. 发明申请

US20050203119A1 Dihydropyridine compounds for treating or preventing metabolic disorders 审中-公开
标题翻译：用于治疗或预防代谢紊乱的二氢吡啶化合物
公开(公告)号：US20050203119A1
公开(公告)日：2005-09-15
申请号：US10939252
申请日：2004-09-10
申请人： Mitsunori Ono , Yumiko Wada , Lijun Sun , Shoujun Chen , Teresa Przewloka , Shijie Zhang , Christopher Borella , Keizo Koya , Kevin Foley , Zhi-Qiang Xia , Hao Li , Dan Zhou
发明人： Mitsunori Ono , Yumiko Wada , Lijun Sun , Shoujun Chen , Teresa Przewloka , Shijie Zhang , Christopher Borella , Keizo Koya , Kevin Foley , Zhi-Qiang Xia , Hao Li , Dan Zhou
IPC分类号： A61K31/47 , A61K31/4741 , A61K31/4743 , A61K31/4745 , C07D215/54 , C07D221/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D471/02 , C07D491/02 , C07D491/04 , C07D498/02
CPC分类号： C04B35/632 , C07D215/54 , C07D221/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D491/04
摘要： This invention relates to dihydropyridine compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein A2, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, and m are defined herein, and compositions comprising such compounds. The invention also relates to methods of preventing or treating metabolic disorders, such as diabetes mellitus, and conditions and complications associated with diabetes mellitus, comprising administering to a subject in need thereof a compound of formula (1) or a composition comprising such a compound. The invention further relates to kits comprising a compound of formula (I).
摘要翻译：本发明涉及式（I）的二氢吡啶化合物：或其药学上可接受的盐，溶剂化物，包合物或前药，其中A 2，R 12，R 12， R 13，R 14，R 15，R 16，R 17，R 13， 18，R 19，R 20，R 21，R 22和m被定义和包含这些化合物的组合物。本发明还涉及预防或治疗诸如糖尿病的代谢性疾病以及与糖尿病相关的病症和并发症的方法，其包括向有需要的受试者施用式（1）化合物或包含这种化合物的组合物。本发明还涉及包含式（I）化合物的试剂盒。

54. 发明授权

US06861436B2 1-glyoxylamide indolizines for treating cancer 失效
标题翻译：用于治疗癌症的1-乙醛酰胺中氮茚
公开(公告)号：US06861436B2
公开(公告)日：2005-03-01
申请号：US10244088
申请日：2002-09-13
申请人： Keizo Koya , Lijun Sun , Mitsunori Ono , Weiwen Ying , Hao Li
发明人： Keizo Koya , Lijun Sun , Mitsunori Ono , Weiwen Ying , Hao Li
IPC分类号： A61K31/437 , A61K31/444 , A61K31/4709 , A61K31/496 , A61P35/00 , C07D471/04 , A61K31/44 , A61K31/47 , C07D215/38 , C07D215/46 , C07D221/02
CPC分类号： C07D471/04
摘要： Disclosed is a compound represented by Structural Formula (I): Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z1 and Z2 are independently ═O, ═S, ═N—OR12 or ═NR12 R1 and R2 are independently —H, an aliphatic group, a substituted aliphatic group, an unsubstituted non-aromatic heterocylic group, a substituted non-aromatic heterocylic group, an aryl group or a substituted aryl group, provided that R1 and R2 are not both —H. Alternatively, —NR1R2, taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, —C(R4R5)—, —N(R4)—, —O—, —S—, —S(O)—, —S(O)2—, —C(═O)—, —C(═O)—N(R4)—, or —N(R4)—C(═O)—. R4 and R5 are independently —H or a substituted or unsubstituted aliphatic group. R12 is —H or a substituted or unsubstituted alkyl group.
摘要翻译：公开了由结构式（I）表示的化合物：环A是取代或未取代的且任选地与芳基稠合.Z1和Z2独立地为= O，= S，= N-OR12或= NR12R1，R2独立地为-H ，脂肪族基团，取代脂肪族基团，未取代的非芳香族杂环基团，取代的非芳香族杂环基团，芳基或取代的芳基，条件是R1和R2不同时为-H。或者，-NR 1 R 2一起为取代或未取代的非芳香族含氮杂环基或取代或未取代的含氮杂芳基.R 3为取代或未取代的芳基或取代或未取代的脂族基.X为共价键，-C（R4R5） - ， - N（R4） - ， - O - ， - S - ， - S（O） - ， - S（O） C（= O）-N（R4） - 或-N（R4）-C（= O） - 。R4和R5独立地为-H或取代或未取代的脂族基.R12为-H或取代或未取代的烷基。

55. 发明授权

US6137003A Bis (haloethyl) aminobenzene derivatives 失效
标题翻译：双（卤代乙基）氨基苯衍生物
公开(公告)号：US6137003A
公开(公告)日：2000-10-24
申请号：US181436
申请日：1998-10-28
申请人： Mitsunori Ono , Keizo Koya , Lijun Sun , Wojciech Wrona , Sylvia Holden , Noriaki Tatsuta
发明人： Mitsunori Ono , Keizo Koya , Lijun Sun , Wojciech Wrona , Sylvia Holden , Noriaki Tatsuta
IPC分类号： C07D307/58 , A61K31/196 , A61K31/245 , A61K31/341 , A61K31/343 , A61P35/00 , C07C229/60 , C07C229/64 , C07D307/42 , C07C229/00
CPC分类号： C07D307/42 , C07C229/60 , C07C229/64 , C07C2101/02 , C07C2101/04
摘要： The present invention relates to bis(haloethyl)aminobenzene derivatives featured by having carboxyl-containing moiety and one other moiety at the ortho position with respect to the bis(haloethyl)amino substituent of the benzene ring. The moiety at the ortho position can be alkyl, cycloalkyl, heterocycloalkyl, aryl heteroaryl, alkyl(cycloalkyl), alkyl(heterocycloalkyl), alkyl(heteroaryl), alkyl(aryl), --(--O-alkyl).sub.2-5 or --Y.sup.1 --Y.sup.2 in which Y.sup.1 is O, S, or N(R.sup.5) wherein R.sup.5 is hydrogen or alkyl, and Y.sup.2 is alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroacryl, alkyl(cycloalkyl), alkyl(hetero-cycloalkyl), alkyl(aryl), or alkyl(heteroaryl).
摘要翻译：本发明涉及通过在相对于苯环的双（卤代乙基）氨基取代基的邻位具有含羧基的部分和一个其它部分而特征的双（卤代乙基）氨基苯衍生物。邻位的部分可以是烷基，环烷基，杂环烷基，芳基杂芳基，烷基（环烷基），烷基（杂环烷基），烷基（杂芳基），烷基（芳基）， - （ - O-烷基）2-5或-Y1 -Y 2，其中Y 1是O，S或N（R 5），其中R 5是氢或烷基，并且Y 2是烷基，烯基，环烷基，杂环烷基，芳基，异丙基丙烯酰基，烷基（环烷基），烷基（杂环烷基）（芳基）或烷基（杂芳基）。

56. 发明申请

US20130150440A1 USE OF BIS [THIOHYDRAZIDE AMIDE] COMPOUNDS SUCH AS ELESCLOMOL FOR TREATING CANCERS 有权
标题翻译：使用BIS [硫羟酰胺酰胺]化合物作为ELESCLOMOL治疗癌症
公开(公告)号：US20130150440A1
公开(公告)日：2013-06-13
申请号：US13642275
申请日：2011-04-20
申请人： Masazumi Nagai , Ronald K. Blackman , Patricia E. Rao , Yumiko Wada , Keizo Koya
发明人： Masazumi Nagai , Ronald K. Blackman , Patricia E. Rao , Yumiko Wada , Keizo Koya
IPC分类号： A61K31/30 , A61K31/337 , A61K45/06 , A61K31/19 , A61K31/16 , A61K31/28
CPC分类号： A61K31/30 , A61K31/00 , A61K31/16 , A61K31/18 , A61K31/19 , A61K31/195 , A61K31/28 , A61K31/337 , A61K31/555 , A61K45/06 , A61K2300/00
摘要： Improved cancer treatments with bis[thiohydrazide amide] compounds such as elesclomol, in particular for identifying patient populations that would benefit from such treatments.
摘要翻译：改进的双[硫代酰肼]化合物如elesclomol的癌症治疗，特别是用于鉴定将受益于这种治疗的患者群体。

57. 发明授权

US08815945B2 Use of bis [thiohydrazide amide] compounds such as elesclomol for treating cancers 有权
标题翻译：使用双[硫代酰肼]化合物如elesclomol用于治疗癌症
公开(公告)号：US08815945B2
公开(公告)日：2014-08-26
申请号：US13642275
申请日：2011-04-20
申请人： Masazumi Nagai , Ronald K. Blackman , Patricia E. Rao , Yumiko Wada , Keizo Koya
发明人： Masazumi Nagai , Ronald K. Blackman , Patricia E. Rao , Yumiko Wada , Keizo Koya
IPC分类号： A61K45/06 , A61K31/19 , A61K31/337
CPC分类号： A61K31/30 , A61K31/00 , A61K31/16 , A61K31/18 , A61K31/19 , A61K31/195 , A61K31/28 , A61K31/337 , A61K31/555 , A61K45/06 , A61K2300/00
摘要： Improved cancer treatments with bis[thiohydrazide amide] compounds such as elesclomol, in particular for identifying patient populations that would benefit from such treatments.
摘要翻译：改进的双[硫代酰肼]化合物如elesclomol的癌症治疗，特别是用于鉴定将受益于这种治疗的患者群体。

58. 发明授权

US06616959B2 Water-soluble bean-based extracts 失效
标题翻译：水溶性豆类提取物
公开(公告)号：US06616959B2
公开(公告)日：2003-09-09
申请号：US10006326
申请日：2001-11-13
申请人： Mitsunori Ono , Keizo Koya , Noriaki Tatsuta , Naoto Yamaguchi , Lan Bo Chen
发明人： Mitsunori Ono , Keizo Koya , Noriaki Tatsuta , Naoto Yamaguchi , Lan Bo Chen
IPC分类号： A23L120
CPC分类号： A23L33/105 , A23V2002/00 , A23V2250/2116
摘要： This invention relates to a water-soluble bean-based extract including one or more isoflavone glycosides. Also shown is a method of preparing such a water-soluble bean-based extract.
摘要翻译：本发明涉及包含一种或多种异黄酮糖苷的水溶性豆类提取物。还示出了制备这种水溶性豆类提取物的方法。

59. 发明申请

US20150025042A1 Compounds For Treating Proliferative Disorders 审中-公开
标题翻译：用于治疗增生性疾病的化合物
公开(公告)号：US20150025042A1
公开(公告)日：2015-01-22
申请号：US14108162
申请日：2013-12-16
申请人： Shoujun Chen , Keizo Koya , Zachary Demko , Lijun Sun
发明人： Shoujun Chen , Keizo Koya , Zachary Demko , Lijun Sun
IPC分类号： C07C327/56 , A61K31/16 , C07C257/22 , A61K31/277 , C07C311/55 , A61K31/18 , C07C243/34 , C07F9/22 , A61K31/664 , C07F9/46 , C07D307/66 , A61K31/341 , C07D207/34 , A61K31/40 , C07D271/113 , A61K31/4245 , A61K31/166
CPC分类号： C07C327/56 , A61K31/16 , A61K31/166 , A61K31/18 , A61K31/277 , A61K31/341 , A61K31/40 , A61K31/4245 , A61K31/664 , C07C243/28 , C07C243/34 , C07C255/66 , C07C257/22 , C07C261/04 , C07C281/06 , C07C307/04 , C07C311/49 , C07C311/51 , C07C311/55 , C07C337/06 , C07C2601/02 , C07D207/34 , C07D207/36 , C07D233/74 , C07D263/48 , C07D271/10 , C07D271/113 , C07D307/66 , C07F9/228 , C07F9/4423 , C07F9/4496 , C07F9/46
摘要： Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
摘要翻译：公开了式（I），（III），（IV），（VII），（X），（XI），（XII），（XIII）和（XIV）的化合物，其中变量如权利要求以及使用本发明化合物治疗患有增殖性疾病（例如癌症）的受试者的方法，以及用于治疗对Hsp70诱导和/或自然杀伤诱导反应的病症的方法。还公开了包含本发明化合物和药学上可接受的载体的药物组合物。

60. 发明申请

US20140031429A1 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS 有权
标题翻译：用于治疗增生性疾病的化合物
公开(公告)号：US20140031429A1
公开(公告)日：2014-01-30
申请号：US13900788
申请日：2013-05-23
申请人： Keizo Koya , Weiwen Ying , Teresa Kowalczyk-Prezewloka , Lijun Sun
发明人： Keizo Koya , Weiwen Ying , Teresa Kowalczyk-Prezewloka , Lijun Sun
IPC分类号： C07C391/00 , A61K31/165 , A61K45/06 , A61K31/18
CPC分类号： C07C391/00 , A61K31/165 , A61K31/18 , A61K45/06 , C07C259/20 , C07C2601/02
摘要： Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
摘要翻译：公开了使用本发明化合物治疗患有增殖性疾病如癌症的受试者的化合物和方法，以及用于治疗响应于Hsp70诱导和/或自然杀伤诱导的病症的方法。此外，公开了包含本发明化合物和药学上可接受的载体的药物组合物。

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