公开(公告)号：US20140163238A1

公开(公告)日：2014-06-12

申请号：US14063868

申请日：2013-10-25

申请人： President and Fellows of Harvard College

发明人： Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

IPC分类号： C07D261/20 ,  C07C231/10

CPC分类号： C07D261/20 ,  C07C231/10 ,  C07C237/26 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77

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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

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。 所描述的四环素和四环素类似物的模块合成为通过先前的四环素合成和半合成方法先前难以接近的各种四环素类似物和聚环状体提供了有效和对映选择性的途径。 这些类似物可以用作抗微生物剂或抗增殖剂来治疗人类或其他动物的疾病。

公开(公告)号：US20180230111A1

公开(公告)日：2018-08-16

申请号：US15887956

申请日：2018-02-02

申请人： President and Fellows of Harvard College

发明人： Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

IPC分类号： C07D261/20 ,  C07C231/10 ,  C07D277/66 ,  C07D307/77 ,  C07C237/26 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64

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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

公开(公告)号：US09884830B2

公开(公告)日：2018-02-06

申请号：US15161165

申请日：2016-05-20

申请人： President and Fellows of Harvard College

发明人： Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

IPC分类号： C07D413/00 ,  C07C237/26 ,  C07D261/20 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77 ,  C07C231/10

CPC分类号： C07D261/20 ,  C07C231/10 ,  C07C237/26 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77

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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

公开(公告)号：US10669244B2

公开(公告)日：2020-06-02

申请号：US15887956

申请日：2018-02-02

申请人： President and Fellows of Harvard College

发明人： Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

IPC分类号： C07C237/26 ,  C07D209/56 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D307/77 ,  C07D261/20 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07C231/10

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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

公开(公告)号：US20160340325A1

公开(公告)日：2016-11-24

申请号：US15161165

申请日：2016-05-20

申请人： President and Fellows of Harvard College

发明人： Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

IPC分类号： C07D261/20

CPC分类号： C07D261/20 ,  C07C231/10 ,  C07C237/26 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77

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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

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。 所描述的四环素和四环素类似物的模块合成为通过先前的四环素合成和半合成方法先前难以接近的各种四环素类似物和聚环状体提供了有效和对映选择性的途径。 这些类似物可以用作抗微生物剂或抗增殖剂来治疗人类或其他动物的疾病。

公开(公告)号：US09365493B2

公开(公告)日：2016-06-14

申请号：US14063868

申请日：2013-10-25

申请人： President and Fellows of Harvard College

发明人： Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

IPC分类号： C07C237/26 ,  C07D413/02 ,  C07C231/10 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D261/20 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77

CPC分类号： C07D261/20 ,  C07C231/10 ,  C07C237/26 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77

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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

公开(公告)号：US20140179929A1

公开(公告)日：2014-06-26

申请号：US14076924

申请日：2013-11-11

申请人： President and Fellows of Harvard College

发明人： Andrew G. Myers ,  Jason D. Brubaker

IPC分类号： C07D231/20

CPC分类号： C07D231/20 ,  C07C237/26 ,  C07D261/12 ,  C07D261/20 ,  C07D413/06 ,  C07D498/18 ,  C07F7/1804 ,  C07F7/1892

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 a more efficient route for preparing the enone intermediate.

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。 本发明提供了制备烯酮中间体的更有效的途径。

公开(公告)号：US11192866B2

公开(公告)日：2021-12-07

申请号：US16417458

申请日：2019-05-20

申请人： President and Fellows of Harvard College

发明人： Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

IPC分类号： C07C237/26 ,  C07D221/18 ,  C07D261/20 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77 ,  C07C231/10

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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

公开(公告)号：US08907104B2

公开(公告)日：2014-12-09

申请号：US14076924

申请日：2013-11-11

申请人： President and Fellows of Harvard College

发明人： Andrew G. Myers ,  Jason D. Brubaker

IPC分类号： C07D231/20 ,  C07D413/06 ,  C07C237/26 ,  C07F7/18 ,  C07D261/12 ,  C07D498/18 ,  C07D261/20

CPC分类号： C07D231/20 ,  C07C237/26 ,  C07D261/12 ,  C07D261/20 ,  C07D413/06 ,  C07D498/18 ,  C07F7/1804 ,  C07F7/1892

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 a more efficient route for preparing the enone intermediate.

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。 本发明提供了制备烯酮中间体的更有效的途径。