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1. 发明申请

WO2012047907A1 SYNTHESIS OF C5-SUBSTITUTED TETRACYCLINES, USES THEREOF, AND INTERMEDIATES THERETO 审中-公开
标题翻译： C5取代的四环素的合成，其用途及其中间体
公开(公告)号：WO2012047907A1
公开(公告)日：2012-04-12
申请号：PCT/US2011/054791
申请日：2011-10-04
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE , MYERS, Andrew, G. , WRIGHT, Peter, M. , HECKER, Evan
发明人： MYERS, Andrew, G. , WRIGHT, Peter, M. , HECKER, Evan
IPC分类号： C07D261/20 , C07D295/15 , C07C237/26 , C07C311/07 , A61K31/165 , A61P31/04
CPC分类号： C07D261/20 , C07C237/26 , C07C271/34 , C07C311/07 , C07D295/15
摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
摘要翻译：四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。通过手性烯酮中间体最近开发的四环素类似物的模块合成使得能够高效合成以前从未制备的新型四环素类似物。本发明提供了更有效的制备烯酮中间体的途径，并且允许在四环素环体系的5位的多种取代基。

2. 发明申请

WO2011119549A1 TRIOXACARCINS AND USES THEREOF 审中-公开
标题翻译：三氧化二砷及其用途
公开(公告)号：WO2011119549A1
公开(公告)日：2011-09-29
申请号：PCT/US2011/029343
申请日：2011-03-22
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE , MYERS, Andrew, G. , HILL, Nicholas, E. , SVENDA, Jakub , YU, Robert, T. , SMALTZ, Daniel, J. , MAGUER, Thomas
发明人： MYERS, Andrew, G. , HILL, Nicholas, E. , SVENDA, Jakub , YU, Robert, T. , SMALTZ, Daniel, J. , MAGUER, Thomas
IPC分类号： C07H17/04 , A61K31/704 , A61P31/04 , A61P35/00
CPC分类号： C07H17/04 , C07D493/22 , C07H15/24 , C07H15/26
摘要： The present invention relates to trioxacarcin compounds of the formula: (I) or pharmaceutically acceptable forms thereof; wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and R 9 are as defined herein. The present invention also provides processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; and methods of use and treatment.
摘要翻译：本发明涉及式（I）的三恶草酮化合物或其药学上可接受的形式; 其中R1，R2，R3，R4，R5，R6，R7，R8和R9如本文所定义。本发明还提供了制备这些化合物及其中间体的方法; 包含这些化合物的药物组合物; 以及使用和治疗方法。

3. 发明申请

WO2016057798A1 14-MEMBERED KETOLIDES AND METHODS OF THEIR PREPARATION AND USE 审中-公开
标题翻译： 14成员的硬脂酸酯及其制备和使用方法
公开(公告)号：WO2016057798A1
公开(公告)日：2016-04-14
申请号：PCT/US2015/054700
申请日：2015-10-08
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE
发明人： MYERS, Andrew, G. , SEIPLE, Ian, Bass , ZHANG, Ziyang
IPC分类号： A01N43/02 , A61K31/335 , A61K31/365
CPC分类号： C07H17/08 , C07D498/04
摘要： Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.
摘要翻译：本文提供了通过东部和西部半部分的偶联，随后进行大环化和任选官能化制备新的14-元酮内酯的方法。还提供了合成这些酮内酯的中间体，包括东部和西部两半。还提供了使用这些酮内酯处理感染性疾病和炎性病症的药物组合物和方法。

4. 发明申请

WO2014082065A1 TRIOXACARCINS, TRIOXACARCIN-ANTIBODY CONJUGATES, AND USES THEREOF 审中-公开
标题翻译：三氧化二铁，抗胆碱凝集素及其用途
公开(公告)号：WO2014082065A1
公开(公告)日：2014-05-30
申请号：PCT/US2013/071924
申请日：2013-11-26
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE
发明人： MYERS, Andrew, G. , SMALTZ, Daniel, J. , SCHUMACHER, Andreas
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： A61K47/6829 , A61K47/6807 , A61K47/6851 , C07K16/18
摘要： Provided herein are trioxacarcin-antibody drug conjugates of Formula (A): and pharmaceutically acceptable salts thereof, comprising at least one instance of the group - L 1 -(A-L 2 )a-B attached thereto, wherein a is an integer between 1 and 10, inclusive, L 1 is absent or is a linking group, A is a moiety formed from the reaction of two complimentary groups (X and Y), L 2 is absent or is another linking group, and B is an antibody or antibody fragment. Also provided are methods of preparing these antibody-drug conjugates, pharmaceutically acceptable compositions thereof, and methods of their use and treatment. Further provided are precursors to the trioxacarcin-antibody drug conjugates, novel trioxacarcins without an antibody conjugated thereto, pharmaceutical compositions thereof, and methods of their use and treatment.
摘要翻译：本文提供式（A）的三恶菌素抗体药物偶联物及其药学上可接受的盐，其包含与其连接的基团-L1 - （A-L2）aB的至少一个实例，其中a为1至10的整数，包括L 1不存在或是连接基团，A是由两个互补基团（X和Y）的反应形成的部分，L2不存在或是另一个连接基团，B是抗体或抗体片段。还提供制备这些抗体 - 药物偶联物的方法，其药学上可接受的组合物，及其使用和治疗方法。进一步提供的是三恶菌素抗体药物缀合物的前体，没有缀合有抗体的新型trioxacacin，其药物组合物及其使用和治疗方法。

5. 发明申请

WO2021236911A8 LINCOSAMIDE ANTIBIOTICS AND USES THEREOF 审中-公开
公开(公告)号：WO2021236911A8
公开(公告)日：2021-11-25
申请号：PCT/US2021/033371
申请日：2021-05-20
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE
发明人： POTE, Aditya , TESTOLIN, Giambattista , SILVESTRE, Katherine, J. , MYERS, Andrew, G. , MITCHELTREE, Matthew, James , MASON, Jeremy, D. , TERWILLIGER, Daniel
IPC分类号： C07H15/16 , A61K31/7056 , A61P31/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/00
摘要： Provided are compounds of Formula (I) for the treatment of infectious and inflammatory diseases. The compounds described herein are lincosamides modified at the amino acid (southern) region. The compounds may have further modification at the C-7 position of the aminooctose (northern) region, thus distinguishing them from lincomycin and clindamycin. Also provided are methods for preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating infectious diseases using the disclosed compounds.

6. 发明申请

WO2019032956A1 LINCOSAMIDE ANTIBIOTICS AND USES THEREOF 审中-公开
公开(公告)号：WO2019032956A1
公开(公告)日：2019-02-14
申请号：PCT/US2018/046200
申请日：2018-08-10
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE
发明人： MYERS, Andrew, G. , MITCHELTREE, Matthew, James
IPC分类号： A61K31/409 , A61K31/7042 , A61K31/7056 , C07D309/02 , C07D498/02 , C07H15/16
CPC分类号： A61K31/409 , A61K31/7042 , A61K31/7056 , C07D309/02 , C07D498/02 , C07H15/16
摘要： Provided are lincosamide compounds for the treatment of infectious diseases. The lincosamides described herein are modified at the C-7 position of the aminooctose (northern) region, thus distinguishing them from lincomycin and clindamycin. Also provided are methods for preparing the lincosamide compounds, pharmaceutical compositions comprising the lincosamide compounds, and methods of treating infectious diseases using the disclosed lincosamide compounds.

7. 发明申请

WO2010126607A2 SYNTHESIS OF TETRACYCLINES AND INTERMEDIATES THERETO 审中-公开
标题翻译：四氯乙烯的合成及其中间体
公开(公告)号：WO2010126607A2
公开(公告)日：2010-11-04
申请号：PCT/US2010/001284
申请日：2010-04-30
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE , MYERS, Andrew, G. , KUMMER, David, A. , LI, Derun , HECKER, Evan , DION, Amelie , WRIGHT, Peter, Maughan
发明人： MYERS, Andrew, G. , KUMMER, David, A. , LI, Derun , HECKER, Evan , DION, Amelie , WRIGHT, Peter, Maughan
IPC分类号： C07C237/26
CPC分类号： C07D261/20 , C07B2200/07 , C07C29/32 , C07C45/00 , C07C45/29 , C07C45/67 , C07C45/673 , C07C45/69 , C07C49/637 , C07C237/26 , C07C311/05 , C07C2601/02 , C07C2601/08 , C07C2603/46 , C07C2603/66 , C07D207/16 , C07D209/58 , C07D213/30 , C07D213/74 , C07D233/61 , C07D261/18 , C07D277/24 , C07D277/64 , C07D295/15 , C07D295/155 , C07D498/04 , C07F7/0814 , C07F7/188
摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
摘要翻译：四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。通过手性烯酮中间体最近开发的四环素类似物的模块合成使得能够高效合成以前从未制备的新型四环素类似物。本发明提供了更有效的制备烯酮中间体的途径，并允许四环素环体系的4a，5,5a和12a位置的取代基。

8. 发明申请

WO2010024930A2 CORTISTATIN ANALOGUES AND SYNTHESES THEROF 审中-公开
标题翻译： CORTISTATIN类似物及其合成
公开(公告)号：WO2010024930A2
公开(公告)日：2010-03-04
申请号：PCT/US2009/004911
申请日：2009-08-28
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE , FLYER, Alec, Nathanson , LEE, Hong, Myung , MYERS, Andrew, G. , NIETO-OBERHUBER, Cristina, Montserrat , SHAIR, Matthew, D. , SI, Chong
发明人： FLYER, Alec, Nathanson , LEE, Hong, Myung , MYERS, Andrew, G. , NIETO-OBERHUBER, Cristina, Montserrat , SHAIR, Matthew, D. , SI, Chong
IPC分类号： C07D493/08 , C07D493/02 , A61K31/34 , A61P35/00
CPC分类号： C07D493/08 , A61K31/34 , A61K31/4725
摘要： The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: I and salts thereof, wherein R 1 , R 2 , R 3 , R 4 , n, and m are as defined herein; processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; methods for treating a proliferative disease; methods for treating a disease associated with aberrant angiogenesis; methods for inhibiting angiogenesis; and processes for preparing cortistatin A, J, K, and L, and analogs thereof.
摘要翻译：本发明涉及具有以下通式的皮质抑素A，J，K和L的类似物：及其盐，其中R 1，R 1， 2，R 3，R 4，n和m如本文所定义; 制备这些化合物及其中间体的方法; 包含此类化合物的药物组合物治疗增殖性疾病的方法; 治疗与异常血管生成相关的疾病的方法; 抑制血管生成的方法; 以及制备皮质抑素A，J，K和L及其类似物的方法。

9. 发明申请

WO2021252708A1 STABILIZED TRIOXACARCIN ANTIBODY DRUG CONJUGATES AND USES THEREOF 审中-公开
公开(公告)号：WO2021252708A1
公开(公告)日：2021-12-16
申请号：PCT/US2021/036718
申请日：2021-06-10
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE , MYERS, Andrew, G. , MAGNO, Ethan, L.
发明人： MYERS, Andrew, G. , MAGNO, Ethan, L.
IPC分类号： A61K47/68 , A61P35/00 , C07D493/22 , C07H15/00 , C07K16/32 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6889 , C07H15/203
摘要： Provided herein are antibody drug conjugates of Formula (I): G-R7(I) and pharmaceutically acceptable salts thereof, wherein G is a molecular payload; and R7 is - L-A-B, wherein L is a linking group, A is a conjugating group, and B is an antibody or antibody fragment. Also provided are methods of preparing the antibody-drug conjugates, pharmaceutically acceptable compositions thereof, and methods of their use and treatment. Further provided are precursors to the antibody drug conjugates (e.g., compounds of Formula (III), novel trioxacarcins without an antibody conjugated thereto), pharmaceutical compositions thereof, and methods of their use and treatment.

10. 发明申请

WO2021236911A1 LINCOSAMIDE ANTIBIOTICS AND USES THEREOF 审中-公开
公开(公告)号：WO2021236911A1
公开(公告)日：2021-11-25
申请号：PCT/US2021/033371
申请日：2021-05-20
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE , MYERS, Andrew, G. , SILVESTRE, Katherine, J. , MITCHELTREE, Matthew, James , TESTOLIN, Giambattista , MASON, Jeremy, D. , POTE, Aditya , TERWILLIGER, Daniel
发明人： MYERS, Andrew, G. , SILVESTRE, Katherine, J. , MITCHELTREE, Matthew, James , TESTOLIN, Giambattista , MASON, Jeremy, D. , POTE, Aditya , TERWILLIGER, Daniel
IPC分类号： C07H15/16 , A61K31/7056 , A61P31/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/00
摘要： Provided are compounds of Formula (I) for the treatment of infectious and inflammatory diseases. The compounds described herein are lincosamides modified at the amino acid (southern) region. The compounds may have further modification at the C-7 position of the aminooctose (northern) region, thus distinguishing them from lincomycin and clindamycin. Also provided are methods for preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating infectious diseases using the disclosed compounds.

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