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公开(公告)号：US06291684B1
公开(公告)日：2001-09-18
申请号：US09528230
申请日：2000-03-17
IPC分类号： C07D20326
CPC分类号： C07D491/04
摘要： The present invention relates to a stereospecific process to produce aziridinyl epothilones from oxiranyl epothilones and the intermediates derived therein.
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公开(公告)号：US06800653B2
公开(公告)日：2004-10-05
申请号：US10144879
申请日：2002-05-14
IPC分类号： A61K31425
CPC分类号： C07D417/06 , A61K31/427 , A61K31/5377 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor.
摘要翻译： 本发明涉及12,13位修饰的埃坡霉素衍生物，衍生物的制备方法及其中间体。
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公开(公告)号：US07211593B2
公开(公告)日：2007-05-01
申请号：US10386059
申请日：2003-03-11
IPC分类号： A61K31/427 , C07D277/30
CPC分类号： C07D417/06 , C07D493/04
摘要： The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by the formula wherein: R1, R2, R3, R4, R5 are hydrogen or lower alkyl; R6 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo; X is hydrogen and Y is hydroxy, or X and Y taken together represent a carbon-carbon bond; and pharmaceutically acceptable salts, solvates, or hydrates thereof. Also included are therapeutic compositions containing the compounds represented by formula I as active ingredients, alone or in combination with other therapeutic agents useful in the treatment of cancer or other proliferative diseases.
摘要翻译： 本发明涉及可用于治疗由下式表示的癌症或其它增殖性疾病的化合物：其中：R 1，R 2，R 3， >，R 4，R 5是氢或低级烷基; R 6选自氢，烷基，取代的烷基，芳基，取代的芳基，环烷基或杂环; X是氢，Y是羟基，X或Y一起代表碳 - 碳键; 及其药学上可接受的盐，溶剂化物或水合物。 还包括含有式I表示的化合物作为活性成分的治疗组合物，单独或与用于治疗癌症或其它增殖性疾病的其它治疗剂组合。
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公开(公告)号：US06719540B2
公开(公告)日：2004-04-13
申请号：US10386072
申请日：2003-03-11
IPC分类号： C07D49304
CPC分类号： C07D417/06 , A61K31/425 , A61K45/06 , C07D491/08 , C07D493/04 , C07D493/08 , A61K2300/00
摘要： The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by formula I: wherein: Q is selected from the group consisting of M is O, NR9, or CR10R11; X is O or NH; and the R groups are as defined, and therapeutic compositions containing them alone or in combination with other therapeutic agents useful in the treatment of cancer or other proliferative diseases.
摘要翻译： 本发明涉及可用于治疗由式I表示的癌症或其它增殖性疾病的化合物：其中：Q选自M为O，NR 9或CR 10 R 11; X是O或NH; 并且R基团如所定义，和治疗组合物单独含有它们或与用于治疗癌症或其它增殖性疾病的其它治疗剂组合。
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5.发明申请公开(公告)号：US20120142707A1
公开(公告)日：2012-06-07
申请号：US13151706
申请日：2011-06-02
申请人： Alicia Regueiro-Ren , Jacob Swidorski , Zheng Liu , Nicholas A. Meanwell , Sing-Yuen Sit , Jie Chen
发明人： Alicia Regueiro-Ren , Jacob Swidorski , Zheng Liu , Nicholas A. Meanwell , Sing-Yuen Sit , Jie Chen
IPC分类号： A61K31/235 , C07C63/66 , C07D257/04 , C07D215/50 , C07D333/40 , C07D213/64 , C07D239/28 , A61K31/194 , A61K31/196 , A61K31/41 , A61K31/47 , A61K31/381 , A61K31/4418 , A61K31/505 , A61P31/12 , A61P31/18 , A61P37/02 , C07C309/65 , C07C69/753
CPC分类号： C07J63/008
摘要： Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 betulinic acid and other structurally related natural products derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
摘要翻译： 阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，具有独特抗病毒活性的改良的C-3桦木酸和其他与结构相关的天然产物衍生物作为HIV成熟抑制剂提供。 这些化合物可用于治疗艾滋病毒和艾滋病。
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6.发明申请C-28 AMIDES OF MODIFIED C-3 BETULINIC ACID DERIVATIVES AS HIV MATURATION INHIBITORS 有权C-28作为HIV成熟抑制剂的改性C-3白蛋白酸衍生物公开(公告)号：US20120142653A1
公开(公告)日：2012-06-07
申请号：US13151722
申请日：2011-06-02
申请人： Alicia Regueiro-Ren , Zheng Liu , Jacob Swidorski , Nicholas A. Meanwell , Sing-Yuen Sit , Jie Chen , Yan Chen , Ny Sin
发明人： Alicia Regueiro-Ren , Zheng Liu , Jacob Swidorski , Nicholas A. Meanwell , Sing-Yuen Sit , Jie Chen , Yan Chen , Ny Sin
CPC分类号： C07J63/008
摘要： Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 and C-28 betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
摘要翻译： 阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，具有独特抗病毒活性的改良的C-3和C-28桦木酸衍生物作为HIV成熟抑制剂提供。 这些化合物可用于治疗艾滋病毒和艾滋病。
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7.发明申请公开(公告)号：US20120095017A1
公开(公告)日：2012-04-19
申请号：US13324371
申请日：2011-12-13
申请人： Tao Wang , Zhongxing Zhang , Nicholas A. Meanwell , John F. Kadow , Zhiwei Yin , Qiufen May Xue , Alicia Regueiro-Ren , John D. Matiskella , Yasutsugu Ueda
发明人： Tao Wang , Zhongxing Zhang , Nicholas A. Meanwell , John F. Kadow , Zhiwei Yin , Qiufen May Xue , Alicia Regueiro-Ren , John D. Matiskella , Yasutsugu Ueda
IPC分类号： A61K31/496 , A61P31/18
CPC分类号： C07D471/04 , A61K31/496 , A61K45/06 , C07D491/048
摘要： This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
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![Diketo substituted pyrrolo[2,3-C]pyridines](/abs-image/US/2012/02/28/US08124615B2/abs.jpg.150x150.jpg)
公开(公告)号：US08124615B2
公开(公告)日：2012-02-28
申请号：US13101591
申请日：2011-05-05
申请人： Tao Wang , Yasutsugu Ueda , Lawrence G. Hamann , Zhongxing Zhang , Zhiwei Yin , Alicia Regueiro-Ren , David J. Carini , Jacob Swidorski , Zheng Liu , Barry L. Johnson , Nicolas A. Meanwell , John F. Kadow
发明人： Tao Wang , Yasutsugu Ueda , Lawrence G. Hamann , Zhongxing Zhang , Zhiwei Yin , Alicia Regueiro-Ren , David J. Carini , Jacob Swidorski , Zheng Liu , Barry L. Johnson , Nicolas A. Meanwell , John F. Kadow
IPC分类号： A61K31/44
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives of Formula I: that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.
摘要翻译： 阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，提供具有独特抗病毒活性的二酮稠合偶氮哌啶和式I的偶氮哌嗪衍生物。 这些化合物可用于治疗艾滋病毒和艾滋病。
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9.发明申请PHARMACEUTICAL FORMULATIONS OF SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES WITH PROTEASE INHIBITORS 审中-公开替代酰基氨基哌啶衍生物与蛋白酶抑制剂的药物制剂公开(公告)号：US20110245268A1
公开(公告)日：2011-10-06
申请号：US13161205
申请日：2011-06-15
申请人： TAO WANG , Zhongxing Zhang , Nicholas A. Meanwell , John F. Kadow , Zhiwei Yin , Qiufen May Xue , Alicia Regueiro-Ren , John D. Matiskella , Yasutsugu Ueda
发明人： TAO WANG , Zhongxing Zhang , Nicholas A. Meanwell , John F. Kadow , Zhiwei Yin , Qiufen May Xue , Alicia Regueiro-Ren , John D. Matiskella , Yasutsugu Ueda
IPC分类号： A61K31/497 , A61P31/12 , A61P31/18
CPC分类号： C07D471/04 , A61K31/496 , A61K45/06 , C07D491/048
摘要： This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
摘要翻译： 本发明提供具有药物和生物影响性质的化合物，其药物组合物和使用方法。 特别地，本发明涉及氮杂吲哚乙酰基哌嗪衍生物。 这些化合物具有独特的抗病毒活性，无论是单独使用还是与其他抗病毒药，抗感染剂，免疫调节剂或HIV进入抑制剂组合使用。 更具体地说，本发明涉及艾滋病毒和艾滋病的治疗。
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公开(公告)号：US07807671B2
公开(公告)日：2010-10-05
申请号：US11733283
申请日：2007-04-10
申请人： Tao Wang , John F. Kadow , Zhongxing Zhang , Zhiwei Yin , Nicholas A. Meanwell , Alicia Regueiro-Ren , Jacob Swidorski , Ying Han , David J. Carini
发明人： Tao Wang , John F. Kadow , Zhongxing Zhang , Zhiwei Yin , Nicholas A. Meanwell , Alicia Regueiro-Ren , Jacob Swidorski , Ying Han , David J. Carini
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/437 , C07D471/04 , A61K31/4436 , A61K31/4427 , A61K31/18 , C07D403/12 , C07D519/00
CPC分类号： C07D471/04 , C07D403/12 , C07D417/14
摘要： This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity useful for the treatment of HIV and AIDS. More particularly, the present disclosure relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, wherein: A is selected from the group consisting of:
摘要翻译： 本公开提供具有药物和生物影响性质的化合物，其药物组合物和使用方法。 特别地，本公开涉及具有用于治疗HIV和AIDS的独特抗病毒活性的二酮哌嗪和哌嗪衍生物。 更具体地说，本公开涉及式I化合物或其药学上可接受的盐，其中：A选自：
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