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公开(公告)号：US08410303B2
公开(公告)日：2013-04-02
申请号：US13053756
申请日：2011-03-22
申请人： Igor Alabugin , Abdulkader Baroudi
发明人： Igor Alabugin , Abdulkader Baroudi
IPC分类号： C07C69/84 , C07C233/65
CPC分类号： C07D215/20 , C07C67/00 , C07C231/10 , C07C329/04 , C07C333/04 , C07C333/08 , C07C2603/26 , C07C69/76 , C07C69/92 , C07C69/78 , C07C233/65 , C07C235/56
摘要： A method is provided for the preparation of an aromatic carboxylic acid aryl ester or an N-aryl aromatic carboxamide. The method comprises contacting an O,O-diaryl thiocarbonate or an O-aryl-N-aryl thiocarbamate with a reactant that regioselectively reacts with sulfur, which contact causes an O-neophyl rearrangement, thereby forming either the aromatic carboxylic acid aryl ester or the N-aryl aromatic carboxamide, respectively.
摘要翻译： 提供了制备芳族羧酸芳基酯或N-芳基芳族羧酰胺的方法。 该方法包括使O，O-二芳基硫代碳酸酯或O-芳基-N-芳基硫代氨基甲酸酯与与硫区域选择性反应的反应物接触，所述反应物与硫接触，导致O-新茶碱重排，由此形成芳族羧酸芳酯或 N-芳基芳族羧酰胺。
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公开(公告)号：US20110237798A1
公开(公告)日：2011-09-29
申请号：US13053756
申请日：2011-03-22
申请人： Igor Alabugin , Abdulkader Baroudi
发明人： Igor Alabugin , Abdulkader Baroudi
IPC分类号： C07C67/00 , C07D215/20 , C07C231/00
CPC分类号： C07D215/20 , C07C67/00 , C07C231/10 , C07C329/04 , C07C333/04 , C07C333/08 , C07C2603/26 , C07C69/76 , C07C69/92 , C07C69/78 , C07C233/65 , C07C235/56
摘要： A method is provided for the preparation of an aromatic carboxylic acid aryl ester or an N-aryl aromatic carboxamide. The method comprises contacting an O,O-diaryl thiocarbonate or an O-aryl-N-aryl thiocarbamate with a reactant that regioselectively reacts with sulfur, which contact causes an O-neophyl rearrangement, thereby forming either the aromatic carboxylic acid aryl ester or the N-aryl aromatic carboxamide, respectively.
摘要翻译： 提供了制备芳族羧酸芳基酯或N-芳基芳族羧酰胺的方法。 该方法包括使O，O-二芳基硫代碳酸酯或O-芳基-N-芳基硫代氨基甲酸酯与与硫区域选择性反应的反应物接触，所述反应物与硫接触，导致O-新茶碱重排，由此形成芳族羧酸芳酯或 N-芳基芳族羧酰胺。
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3.发明授权Dipeptide acetylene conjugates and a method for photocleavage of double strand DNA by dipeptide acetylene conjugates 有权二肽乙炔缀合物和通过二肽乙炔缀合物对双链DNA进行光切割的方法公开(公告)号：US08927728B2
公开(公告)日：2015-01-06
申请号：US13465529
申请日：2012-05-07
申请人： Igor Alabugin , Wang-Yong Yang , Saumya Roy , Kemal Kaya , Qing-Xiang Sang
发明人： Igor Alabugin , Wang-Yong Yang , Saumya Roy , Kemal Kaya , Qing-Xiang Sang
IPC分类号： C07D213/16 , C07D213/56 , C07D213/61 , C07K5/062 , C07K5/065 , C07K5/068
CPC分类号： C07D213/61 , C07K5/06026 , C07K5/06078 , C07K5/06086
摘要： Photoreactive DNA cleaving conjugate compounds are provided comprising a DNA cleaving moiety which comprises an aryl alkyne group and a polyfunctional pH-regulated DNA-binding moiety which comprises at least one or two amino groups.
摘要翻译： 提供了光反应性DNA切割缀合化合物，其包括DNA切割部分，其包含芳基炔基和多官能pH调节的DNA结合部分，其包含至少一个或两个氨基。
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4.发明授权Route to synthetic analogues of Rocaglamide and Aglafoline using cascade transformations initiated by oxy-cope rearrangement of bis-alkynes 有权使用由双 - 炔的氧基 - 重排排列引发的级联转化，路由到罗格列酰胺和阿格拉福林的合成类似物公开(公告)号：US09206100B2
公开(公告)日：2015-12-08
申请号：US13820176
申请日：2011-09-13
申请人： Igor Alabugin , Runa Pal
发明人： Igor Alabugin , Runa Pal
CPC分类号： C07C29/68 , C07C41/30 , C07C41/32 , C07C45/511 , C07C45/68 , C07C2601/10 , C07F7/083 , C07C33/28 , C07C33/486 , C07C49/798 , C07C49/747 , C07C43/1788 , C07C49/84 , C07C49/753
摘要： A method for preparing a cyclobutene compound or a cyclopentenone is provided. The method comprises contacting an α,β-diketone with a metal acetylide at a temperature below 0° C. to thereby form a reaction mixture comprising a bis-alkyne precursor. The bis-alkyne precursor rearranges into a bis-allenic intermediate, which undergoes further rearrangement into the cyclobutene compound or the cyclopentenone compound as the temperature of the reaction mixture increases from below 0° C. to above 0° C.
摘要翻译： 提供了制备环丁烯化合物或环戊烯酮的方法。 该方法包括在低于0℃的温度下使α和bgr-二酮与金属乙炔化物接触，从而形成包含双炔前体的反应混合物。 双炔前体重新排列成双 - 烯类中间体，当反应混合物的温度从0℃升至0℃以上时，其进一步重排成环丁烯酮化合物或环戊烯酮化合物。
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5.发明授权C-lysine conjugates as pH-controlled, light-activated reagents for double stranded DNA cleavage and associated methods 有权作为用于双链DNA切割的pH控制的光活化试剂和相关方法的C-赖氨酸缀合物公开(公告)号：US08334403B1
公开(公告)日：2012-12-18
申请号：US12640877
申请日：2009-12-17
IPC分类号： C07C229/00 , C12Q1/68
CPC分类号： C12N15/10 , A61K41/0042 , C12Q1/68 , C12Q2523/107 , C12Q2523/319 , C12Q2527/119
摘要： Compounds and methods for double-stranded DNA cleavage of light-activated lysine conjugates are enhanced at the slightly acidic pH suitable for selective targeting of cancer cells by the presence of two amino groups of different basicities. The first amino group plays an auxiliary role enhancing solubility and affinity to DNA whereas the second amino group which is positioned next to the light-activated DNA-cleaver undergoes protonation at the desired pH threshold. Protonation results in two synergetic effects which account for the increased DNA-cleaving ability at the lower pH: tighter binding to DNA at the lower pH; and the unproductive pathway which quenches the excited state of the photocleaver through intramolecular electron transfer is eliminated once the donor amino group next to the chromophore is protonated. The utility of these molecules for phototherapy of cancer is confirmed by the drastic increase in toxicity of five conjugates against cancer cell lines upon photoactivation.
摘要翻译： 光活化赖氨酸缀合物的双链DNA切割的化合物和方法在适于通过存在不同碱性的两个氨基的癌细胞的选择性靶向的微酸性pH下得到增强。 第一个氨基起增强对DNA的溶解度和亲和力的辅助作用，而位于光激活的DNA切割器旁边的第二个氨基在期望的pH阈值下进行质子化。 质子化导致两个协同作用，这说明在较低的pH值下增加的DNA切割能力：在较低pH下更紧密地结合DNA; 一旦发色团旁边的供体氨基被质子化，就消除了通过分子内电子转移而猝灭光致变色器的激发态的非生产途径。 这些分子用于癌症光疗的效用通过光活化后五种缀合物对癌细胞系的毒性急剧增加来证实。
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6.发明申请NEW ROUTE TO SYNTHETIC ANALOGUES OF ROCAGLAMIDE AND AGLAFOLINE USING CASCADE TRANSFORMATIONS INITIATED BY OXY-COPE REARRANGEMENT OF BIS-ALKYNES 有权通过氧化亚铜离子引发的CASCADE变换的新戊酰胺和酰胺的合成方法的新途径公开(公告)号：US20130165683A1
公开(公告)日：2013-06-27
申请号：US13820176
申请日：2011-09-13
申请人： Igor Alabugin , Runa Pal
发明人： Igor Alabugin , Runa Pal
CPC分类号： C07C29/68 , C07C41/30 , C07C41/32 , C07C45/511 , C07C45/68 , C07C2601/10 , C07F7/083 , C07C33/28 , C07C33/486 , C07C49/798 , C07C49/747 , C07C43/1788 , C07C49/84 , C07C49/753
摘要： A method for preparing a cyclobutene compound or a cyclopentenone is provided. The method comprises contacting an α,β-diketone with a metal acetylide at a temperature below 0° C. to thereby form a reaction mixture comprising a bis-alkyne precursor. The bis-alkyne precursor rearranges into a bis-allenic intermediate, which undergoes further rearrangement into the cyclobutene compound or the cyclopentenone compound as the temperature of the reaction mixture increases from below 0° C. to above 0° C.
摘要翻译： 提供了制备环丁烯化合物或环戊烯酮的方法。 该方法包括在低于0℃的温度下使α，β-二酮与金属乙炔化物接触，从而形成包含双炔前体的反应混合物。 双炔前体重新排列成双 - 烯类中间体，当反应混合物的温度从0℃升至0℃以上时，其进一步重排成环丁烯酮化合物或环戊烯酮化合物。
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7.发明申请DIPEPTIDE ACETYLENE CONJUGATES AND A METHOD FOR PHOTOCLEAVAGE OF DOUBLE STRAND DNA BY DIPEPTIDE ACETYLENE CONJUGATES 有权丙酸乙酯共聚物和双酚A乙烯共聚物双链DNA光电离方法公开(公告)号：US20120288940A1
公开(公告)日：2012-11-15
申请号：US13465529
申请日：2012-05-07
申请人： Igor Alabugin , Wang-Yong Yang , Saumya Roy , Kemal Kaya , Qing-Xiang Sang
发明人： Igor Alabugin , Wang-Yong Yang , Saumya Roy , Kemal Kaya , Qing-Xiang Sang
IPC分类号： C07D213/61 , C07H21/04 , C12N15/00
CPC分类号： C07D213/61 , C07K5/06026 , C07K5/06078 , C07K5/06086
摘要： Photoreactive DNA cleaving conjugate compounds are provided comprising a DNA cleaving moiety which comprises an aryl alkyne group and a polyfunctional pH-regulated DNA-binding moiety which comprises at least one or two amino groups.
摘要翻译： 提供了光反应性DNA切割缀合化合物，其包括DNA切割部分，其包含芳基炔基和多官能pH调节的DNA结合部分，其包含至少一个或两个氨基。
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