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公开(公告)号：US20090285772A1
公开(公告)日：2009-11-19
申请号：US12422067
申请日：2009-04-10
申请人： Pasit Phiasivongsa , Sanjeev G. Redkar , Swarna Gamage , Darby Brooke , William Denny , David J. Bearss , Hariprasad Vankayalapati , Yong Xu , Krzysztof Swierczek
发明人： Pasit Phiasivongsa , Sanjeev G. Redkar , Swarna Gamage , Darby Brooke , William Denny , David J. Bearss , Hariprasad Vankayalapati , Yong Xu , Krzysztof Swierczek
IPC分类号： A61K31/47 , C07D215/38 , C07D401/12 , A61K31/506 , A61K31/7064 , A61K38/20 , A61K38/21 , A61K39/395 , A61P35/00
CPC分类号： C07D401/12
摘要： Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.
摘要翻译： 喹啉衍生物，特别是4-苯胺基喹啉衍生物。 这样的喹啉衍生物可用于DNA甲基化的调节，例如通过选择性抑制DNA甲基转移酶DNMT1有效抑制C-5位上胞嘧啶的甲基化。 提供了合成大量4-苯胺基喹啉衍生物和调节DNA甲基化的方法。 还提供了用于配制和施用这些化合物或组合物以治疗诸如癌症和血液学疾病的病症的方法。
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32.发明授权Pharmaceutical formulations comprising salts of a protein kinase inhibitor and methods of using same 有权包含蛋白激酶抑制剂的盐的药物制剂及其使用方法公开(公告)号：US07820684B2
公开(公告)日：2010-10-26
申请号：US12041565
申请日：2008-03-03
申请人： David J. Bearss , Rajashree Joshi-Hangal , Xiao-Hui Liu , Pasit Phiasivongsa , Sanjeev G. Redkar , Hariprasad Vankayalapati
发明人： David J. Bearss , Rajashree Joshi-Hangal , Xiao-Hui Liu , Pasit Phiasivongsa , Sanjeev G. Redkar , Hariprasad Vankayalapati
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： A61K31/519 , A61K31/7048 , A61K33/24 , A61K45/06 , C07D491/048 , A61K2300/00
摘要： The present invention relates to pharmaceutical formulations comprising the protein kinase inhibitor, MP470, and methods of using same in treating conditions involving undesirable cell proliferation, such as cancer.
摘要翻译： 本发明涉及包含蛋白激酶抑制剂MP470的药物制剂，以及用于治疗涉及不期望的细胞增殖的病症如癌症的方法。
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![IMIDAZO[1,2-beta]PYRIDAZINE AND PYRAZOLO[1,5-alpha]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS](/abs-image/US/2010/09/09/US20100227861A1/abs.jpg.150x150.jpg)
33.发明申请IMIDAZO[1,2-beta]PYRIDAZINE AND PYRAZOLO[1,5-alpha]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS 审中-公开咪唑并[1,2-β]吡嗪和吡唑并[1,5-α]吡啶衍生物及其作为蛋白激酶抑制剂的用途公开(公告)号：US20100227861A1
公开(公告)日：2010-09-09
申请号：US12785322
申请日：2010-05-21
IPC分类号： A61K31/5377 , A61K31/5025 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.
摘要翻译： 本发明提供包含以下结构（I）和（II）的咪唑并[1,2-b]哒嗪和吡唑并[1,5-a]嘧啶化合物的蛋白激酶抑制剂：或其立体异构体，前药或药学上可接受的盐 其中R，R 1，R 2和X如本文所定义。 还公开了用于治疗癌症和其它Pim激酶相关病症的组合物和方法。
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公开(公告)号：US07790746B2
公开(公告)日：2010-09-07
申请号：US11959181
申请日：2007-12-18
申请人： Pasit Phiasivongsa , Sanjeev G. Redkar , Swarna Gamage , Darby Brooke , William Denny , David J. Bearss , Hariprasad Vankayalapati
发明人： Pasit Phiasivongsa , Sanjeev G. Redkar , Swarna Gamage , Darby Brooke , William Denny , David J. Bearss , Hariprasad Vankayalapati
IPC分类号： A61K31/47
CPC分类号： C07D401/12
摘要： Quinoline derivatives, particularly 4-anilinoquinoline derivatives of formula (I), are provided: Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT 1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.
摘要翻译： 提供了喹啉衍生物，特别是式（I）的4-苯胺基喹啉衍生物：这样的喹啉衍生物可用于DNA甲基化的调节，例如有效抑制胞嘧啶在C-5位甲基化，例如通过选择性抑制 DNA甲基转移酶DNMT 1.提供了合成大量4-苯胺基喹啉衍生物和调节DNA甲基化的方法。 还提供了用于配制和施用这些化合物或组合物以治疗诸如癌症和血液学疾病的病症的方法。
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公开(公告)号：US20080293733A1
公开(公告)日：2008-11-27
申请号：US12101591
申请日：2008-04-11
IPC分类号： A61K31/496 , C07D487/04 , C07D495/04 , A61K31/519 , A61P35/04 , C07D403/14 , C07D409/14
CPC分类号： C07D417/12 , C07D239/94 , C07D285/135 , C07D487/04 , C07D495/04
摘要： Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.
摘要翻译： 公开了Axl激酶抑制化合物，以及使用它们在治疗癌症和由Axl激酶介导和/或与其相关的其它病症的组合物和方法。
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![IMIDAZO[1,2-beta]PYRIDAZINE AND PYRAZOLO[1,5-alpha]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS](/abs-image/US/2008/10/23/US20080261988A1/abs.jpg.150x150.jpg)
36.发明申请IMIDAZO[1,2-beta]PYRIDAZINE AND PYRAZOLO[1,5-alpha]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS 有权咪唑并[1,2-β]吡嗪和吡唑并[1,5-α]吡啶衍生物及其作为蛋白激酶抑制剂的用途公开(公告)号：US20080261988A1
公开(公告)日：2008-10-23
申请号：US11935959
申请日：2007-11-06
IPC分类号： A61K31/5025 , C07D487/04 , A61K31/519 , A61P35/04
CPC分类号： C07D487/04
摘要： The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.
摘要翻译： 本发明提供包含以下结构（I）和（II）的咪唑并[1,2-b]哒嗪和吡唑并[1,5-a]嘧啶化合物的蛋白激酶抑制剂：或其立体异构体，前药或药学上可接受的盐 其中R，R 1，R 2和X如本文所定义。 还公开了用于治疗癌症和其它Pim激酶相关病症的组合物和方法。
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公开(公告)号：US20080175814A1
公开(公告)日：2008-07-24
申请号：US11871762
申请日：2007-10-12
申请人： Pasit Phiasivongsa , Sanjeev Redkar , Swarna Gamage , Darby Brooke , William Denny , David J. Bearss , Hariprasad Vankayalapati
发明人： Pasit Phiasivongsa , Sanjeev Redkar , Swarna Gamage , Darby Brooke , William Denny , David J. Bearss , Hariprasad Vankayalapati
IPC分类号： A61K38/20 , C07D215/00 , A61K31/47 , C07D239/02 , A61K38/21 , A61K38/16 , A61P35/00 , A61K39/395 , A61K31/506 , A61K31/53 , C12N5/00
CPC分类号： C07D401/12
摘要： Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.
摘要翻译： 喹啉衍生物，特别是4-苯胺基喹啉衍生物。 这样的喹啉衍生物可用于DNA甲基化的调节，例如通过选择性抑制DNA甲基转移酶DNMT1有效抑制C-5位上胞嘧啶的甲基化。 提供了合成大量4-苯胺基喹啉衍生物和调节DNA甲基化的方法。 还提供了用于配制和施用这些化合物或组合物以治疗诸如癌症和血液学疾病的病症的方法。
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公开(公告)号：US08759384B2
公开(公告)日：2014-06-24
申请号：US12454062
申请日：2009-05-11
申请人： David J. Bearss , Hariprasad Vankayalapati , Yong Xu , Charles Erec Stabbins , Vincent A. Fischetti
发明人： David J. Bearss , Hariprasad Vankayalapati , Yong Xu , Charles Erec Stabbins , Vincent A. Fischetti
IPC分类号： A61K31/415 , C07D233/00 , C07D405/06 , C07D409/06 , A61K31/4166
CPC分类号： C07D405/06 , A61K31/4166 , C07D403/04 , C07D409/06
摘要： Compounds represented by Formula I and II, or pharmaceutically acceptable salts thereof: inhibit bacterial 2-epimerase and are useful anti-infective agents.
摘要翻译： 由式I和II表示的化合物或其药学上可接受的盐：抑制细菌2-差向异构酶，并且是有用的抗感染剂。
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![Imidazo[1,2-B]pyridazine and pyrazolo[1 .5-A]pyrimidine derivatives and their use as protein kinase inhibitors](/abs-image/US/2014/04/29/US08710057B2/abs.jpg.150x150.jpg)
39.发明授权Imidazo[1,2-B]pyridazine and pyrazolo[1 .5-A]pyrimidine derivatives and their use as protein kinase inhibitors 有权咪唑并[1,2-B]吡嗪和吡唑并[1,5-A]吡啶衍生物及其作为蛋白激酶抑制剂的用途公开(公告)号：US08710057B2
公开(公告)日：2014-04-29
申请号：US13188195
申请日：2011-07-21
IPC分类号： C07D487/04 , A61K31/5025
CPC分类号： C07D487/04
摘要： The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.
摘要翻译： 本发明提供包含以下结构（I）和（II）的咪唑并[1,2-b]哒嗪和吡唑并[1,5-a]嘧啶化合物的蛋白激酶抑制剂：或其立体异构体，前药或药学上可接受的盐 其中R，R 1，R 2和X如本文所定义。 还公开了用于治疗癌症和其它Pim激酶相关病症的组合物和方法。
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![Imidazo[1,2-beta]pyridazine and pyrazolo[1,5-alpha]pyrimidine derivatives and their use as protein kinase inhibitors](/abs-image/US/2010/07/06/US07750007B2/abs.jpg.150x150.jpg)
40.发明授权Imidazo[1,2-beta]pyridazine and pyrazolo[1,5-alpha]pyrimidine derivatives and their use as protein kinase inhibitors 有权咪唑并[1,2-β]哒嗪和吡唑并[1,5-a]嘧啶衍生物及其作为蛋白激酶抑制剂的用途公开(公告)号：US07750007B2
公开(公告)日：2010-07-06
申请号：US11935959
申请日：2007-11-06
IPC分类号： A61K31/5025 , A61K31/519 , C07D413/12 , C07D487/04 , A61K31/5375 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.
摘要翻译： 本发明提供包含以下结构（I）和（II）的咪唑并[1,2-b]哒嗪和吡唑并[1,5-a]嘧啶化合物的蛋白激酶抑制剂：或其立体异构体，前药或药学上可接受的盐 其中R，R 1，R 2和X如本文所定义。 还公开了用于治疗癌症和其它Pim激酶相关病症的组合物和方法。
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