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1.发明授权Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds 有权取代的甲基甲酰基试剂及其使用方法来改变化合物的物理化学和/或药代动力学性质公开(公告)号：US09359376B2
公开(公告)日：2016-06-07
申请号：US14110373
申请日：2012-04-09
IPC分类号： C07D307/77 , C07D305/00 , C07D413/00 , C07D405/00 , C07D495/14 , C07D401/14 , C07D405/14 , C07D213/80 , C07D213/81 , C07D213/82 , C07D401/04 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04 , C07D487/22 , C07D491/22 , C07D295/20 , C07D305/14 , C07D213/803 , C07D491/147
CPC分类号： C07D495/14 , C07D213/80 , C07D213/803 , C07D213/81 , C07D213/82 , C07D295/20 , C07D305/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D471/04 , C07D487/04 , C07D487/22 , C07D491/147 , C07D491/22
摘要： The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
摘要翻译： 本发明涉及合成和应用新的手性/非手性取代的甲酰甲酰基试剂以改性药物和/或生物活性物质，以改变未经修饰的原始药剂的所得化合物的物理化学，生物学和/或药代动力学性质。
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公开(公告)号：US20130303516A1
公开(公告)日：2013-11-14
申请号：US13981579
申请日：2012-01-25
申请人： Sundeep Dugar , Dinesh Mahajan , Chandraban Rhushikesh Deokar , Peter Frank Hollinger , Kamal Kishore Kapoor
发明人： Sundeep Dugar , Dinesh Mahajan , Chandraban Rhushikesh Deokar , Peter Frank Hollinger , Kamal Kishore Kapoor
IPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , C07D403/14 , C07D491/107 , C07D498/08 , C07D401/14
CPC分类号： C07D413/14 , C07D401/14 , C07D403/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07D491/107 , C07D498/08
摘要： The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.
摘要翻译： 本发明涉及式（1）的新型三嗪化合物，其制备方法，含有这些化合物的药物组合物以及这些化合物用于治疗增殖性疾病如肿瘤和癌症的用途，以及与其相关或与之相关的其他病症和病症 PI3激酶，PI3激酶途径，mTOR和/或mTOR途径的调节异常。
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公开(公告)号：US20150252027A1
公开(公告)日：2015-09-10
申请号：US14433485
申请日：2013-10-07
IPC分类号： C07D405/14 , C07D471/14 , C07D401/14
CPC分类号： C07D405/14 , C07D213/82 , C07D401/14 , C07D471/14 , C07D487/04
摘要： The present invention discloses novel chemical compounds obtained by causing a covalent attachment of a modifying agent of the structure provided for formula 1, to a functional group or a heteroatom of a heterocyclic ring system in chemical compound with improved chemical and biological properties. Wherein: Y is DRUG-CO; DRUG-OCO; DRUG-NRCO, and X is selected from.
摘要翻译： 本发明公开了通过使具有式1的结构的改性剂共价连接到具有改进的化学和生物学特性的化合物中的杂环体系的官能团或杂原子而获得的新型化合物。 其中：Y为DRUG-CO; DRUG-OCO; DRUG-NRCO，X选自。
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公开(公告)号：US20140100225A1
公开(公告)日：2014-04-10
申请号：US14046682
申请日：2013-10-04
IPC分类号： C07D401/04 , A61K31/095 , A61K31/5377 , C07C309/04 , A61K31/506 , A61K45/06
CPC分类号： A61K31/506 , A61K31/095 , A61K31/5377 , A61K45/06 , C07C309/04 , C07D401/04 , Y02A50/475
摘要： Novel compounds and their synthesis are described. Methods for using these compounds in the prevention or treatment of cancer, a bacterial infection or a viral infection in a subject are also described.
摘要翻译： 描述了新型化合物及其合成。 还描述了使用这些化合物预防或治疗受试者中的癌症，细菌感染或病毒感染的方法。
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公开(公告)号：US20140031421A1
公开(公告)日：2014-01-30
申请号：US13981279
申请日：2012-01-24
申请人： Sundeep Dugar , Dinesh Mahajan , Pantelis Peter Giannousis , Vijay Singh , Kamal Kishore Kapoor
发明人： Sundeep Dugar , Dinesh Mahajan , Pantelis Peter Giannousis , Vijay Singh , Kamal Kishore Kapoor
IPC分类号： C07D311/74
CPC分类号： C07D311/74 , C07D311/30
摘要： The present invention provides synthetic processes for preparing racemic and/or optically pure epicatechin, epigallocatechin and related polyphenols as such or as their variously functionalized derivatives. A principle objective of the disclosure is to provide a new and useful method of synthesis to obtain polyphenols in isomerically pure and/or racemic forms.
摘要翻译： 本发明提供用于制备外消旋和/或光学纯的表儿茶素，表没食子儿茶素和相关多酚本身或其各种官能化衍生物的合成方法。 本公开的主要目的是提供一种新的有用的合成方法以获得异构纯和/或外消旋形式的多酚。
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公开(公告)号：US09630958B2
公开(公告)日：2017-04-25
申请号：US14416140
申请日：2013-07-23
发明人： Sundeep Dugar , Dinesh Mahajan , Frank Hollinger Peter , Amit Sharma , Vinayak Tripathi , Bilash Kuila
IPC分类号： C07D413/14 , C07D401/04 , C07D403/04 , A61K31/53 , A61K31/5377 , A61K31/4427 , A61P35/00 , C07D417/14 , C07D401/14 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/08 , C07D498/08
CPC分类号： C07D417/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D491/08 , C07D498/08
摘要： The present invention relates to novel triazine compounds of formula (1). The present invention also discloses compounds of formula I along with other pharmaceutical acceptable excipients and use of the compounds to modulate the PI3K/mTOR pathway.
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公开(公告)号：US09428482B2
公开(公告)日：2016-08-30
申请号：US13981279
申请日：2012-01-24
申请人： Sundeep Dugar , Dinesh Mahajan , Peter Giannousis Pantelis , Vijay Singh , Kamal Kishore Kapoor
发明人： Sundeep Dugar , Dinesh Mahajan , Peter Giannousis Pantelis , Vijay Singh , Kamal Kishore Kapoor
IPC分类号： C07D311/74 , C07D311/30
CPC分类号： C07D311/74 , C07D311/30
摘要： The present invention provides synthetic processes for preparing racemic and/or optically pure epicatechin, epigallocatechin and related polyphenols as such or as their variously functionalized derivatives. A principle objective of the disclosure is to provide a new and useful method of synthesis to obtain polyphenols in isomerically pure and/or racemic forms.
摘要翻译： 本发明提供用于制备外消旋和/或光学纯的表儿茶素，表没食子儿茶素和相关多酚本身或其各种官能化衍生物的合成方法。 本公开的主要目的是提供一种新的有用的合成方法以获得异构纯和/或外消旋形式的多酚。
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公开(公告)号：US20150197515A1
公开(公告)日：2015-07-16
申请号：US14416140
申请日：2013-07-23
发明人： Sundeep Dugar , Dinesh Mahajan , Frank Hollinger Peter , Amit Sharma , Vinayak Tripathi , Bilash Kuila
IPC分类号： C07D417/14 , C07D401/04 , C07D417/04
CPC分类号： C07D417/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D491/08 , C07D498/08
摘要： The present invention relates to novel triazine compounds of formula (1). The present invention also discloses compounds of formula I along with other pharmaceutical acceptable excipients and use of the compounds to modulate the PI3K/mTOR pathway.
摘要翻译： 本发明涉及式（1）的新型三嗪化合物。 本发明还公开了式I化合物以及其它药学上可接受的赋形剂以及该化合物用于调节PI3K / mTOR途径的用途。
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公开(公告)号：US09556156B2
公开(公告)日：2017-01-31
申请号：US14433485
申请日：2013-10-07
IPC分类号： C07D405/14 , C07D213/82 , C07D401/14 , C07D471/14 , C07D487/04
CPC分类号： C07D405/14 , C07D213/82 , C07D401/14 , C07D471/14 , C07D487/04
摘要： The present invention discloses novel chemical compounds obtained by causing a covalent attachment of a modifying agent of the structure provided for formula 1, to a functional group or a heteroatom of a heterocyclic ring system in chemical compound with improved chemical and biological properties. Wherein: Y is DRUG-CO; DRUG-OCO; DRUG-NRCO, and X is selected from.
摘要翻译： 本发明公开了通过使具有式1的结构的改性剂共价连接到具有改进的化学和生物学特性的化合物中的杂环体系的官能团或杂原子而获得的新型化合物。 其中：Y为DRUG-CO; DRUG-OCO; DRUG-NRCO，X选自。
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公开(公告)号：US09481670B2
公开(公告)日：2016-11-01
申请号：US13981579
申请日：2012-01-25
申请人： Sundeep Dugar , Dinesh Mahajan , Chandraban Rhushikesh Deokar , Frank Peter Hollinger , Kamal Kishore Kapoor
发明人： Sundeep Dugar , Dinesh Mahajan , Chandraban Rhushikesh Deokar , Frank Peter Hollinger , Kamal Kishore Kapoor
IPC分类号： C07D401/14 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/14 , A61K31/53 , A61P35/00 , C07D471/04 , C07D491/107 , C07D498/08
CPC分类号： C07D413/14 , C07D401/14 , C07D403/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07D491/107 , C07D498/08
摘要： The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.
摘要翻译： 本发明涉及式（1）的新型三嗪化合物，其制备方法，含有这些化合物的药物组合物以及这些化合物用于治疗增殖性疾病如肿瘤和癌症的用途，以及与其相关或与之相关的其他病症和病症 PI3激酶，PI3激酶途径，mTOR和/或mTOR途径的调节异常。
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