公开(公告)号：US10858376B2

公开(公告)日：2020-12-08

申请号：US16695253

申请日：2019-11-26

申请人： GlaxoSmithKline Intellectual Property (No. 2) Limited ,  Anacor Pharmaceuticals, Inc.

发明人： Michael Richard Kevin Alley ,  Vincent S. Hernandez ,  Jacob J. Plattner ,  Xianfeng Li ,  David Barros-Aguirre ,  Ilaria Giordano

IPC分类号： A61K31/69 ,  C07F5/04 ,  C07F5/02 ,  A61K45/06

摘要： Compounds of Formula II, wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2; compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.

公开(公告)号：US20140221631A1

公开(公告)日：2014-08-07

申请号：US14201459

申请日：2014-03-07

申请人： Anacor Pharmaceuticals, Inc.

发明人： Stephen J. BAKER ,  Tsutomu Akama ,  Michael Richard Kevin Alley ,  Stephen J. Benkovic ,  Michael Dipierro ,  Vincent S. Hernandez ,  Karin M. Hold ,  Isaac Kennedy ,  Igor Likhotvorik ,  Weimin Mao ,  Kirk Maples ,  Jacob J. Plattner ,  Fernando Rock ,  Virginia Sanders ,  Aaron M. Stemphoski ,  George Petros Yiannikouros ,  Siead Zagar ,  Yong-Kang Zhang ,  Huchen Zhou

IPC分类号： C07F5/04 ,  C07F5/02

CPC分类号： C07F5/025 ,  A61K9/0012 ,  A61K9/08 ,  A61K31/69 ,  A61K31/70 ,  A61K31/7076 ,  A61K47/10 ,  C07F5/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H23/00 ,  Y02A50/473

摘要： This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.

公开(公告)号：US10308668B2

公开(公告)日：2019-06-04

申请号：US15792251

申请日：2017-10-24

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED ,  ANACOR PHARMACEUTICALS INC.

发明人： Michael Richard Kevin Alley ,  Vincent Hernandez ,  Jacob J. Plattner ,  Xianfeng Li ,  David Barros-Aguirre ,  Ilaria Giordano

IPC分类号： C07F5/02 ,  A61K31/69 ,  C07F5/04 ,  A61K45/06

摘要： Compounds of Formula II, wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2; compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.

公开(公告)号：US20170355719A1

公开(公告)日：2017-12-14

申请号：US15685846

申请日：2017-08-24

申请人： Anacor Pharmaceuticals, Inc.

发明人： Vincent S. Hernandez ,  Charles Ding ,  Jacob J. Plattner ,  Michael Richard Kevin Alley ,  Fernando Rock ,  Suoming Zhang ,  Eric Easom ,  Xianfeng Li ,  Ding Zhou

IPC分类号： C07F5/02

CPC分类号： C07F5/025

摘要： This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections.

公开(公告)号：US09751898B2

公开(公告)日：2017-09-05

申请号：US14221637

申请日：2014-03-21

申请人： Anacor Pharmaceuticals, Inc.

发明人： Vincent S. Hernandez ,  Charles Ding ,  Jacob J. Plattner ,  Michael Richard Kevin Alley ,  Fernando Rock ,  Suoming Zhang ,  Eric Easom ,  Xianfeng Li ,  Ding Zhou

IPC分类号： C07F5/02

CPC分类号： C07F5/025

摘要： This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections.

公开(公告)号：US20150119364A1

公开(公告)日：2015-04-30

申请号：US14537771

申请日：2014-11-10

申请人： Anacor Pharmaceuticals, Inc.

发明人： Stephen J. BAKER ,  Tsutomu Akama ,  Michael Richard Kevin Alley ,  Stephen J. Benkovic ,  Michael DiPierro ,  Vincent S. Hernandez ,  Karin M. Hold ,  Isaac Kennedy ,  Igor Likhotvorik ,  Weimin Mao ,  Kirk Maples ,  Jacob J. Plattner ,  Fernando Rock ,  Virginia Sanders ,  Aaron M. Stemphoski ,  George Petros Yiannikouros ,  Siead Zegar ,  Yong-Kang Zhang ,  Huchen Zhou

IPC分类号： C07F5/04

CPC分类号： C07F5/025 ,  A61K9/0012 ,  A61K9/08 ,  A61K31/69 ,  A61K31/70 ,  A61K31/7076 ,  A61K47/10 ,  C07F5/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H23/00 ,  Y02A50/473

摘要： This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.

公开(公告)号：US20180016285A1

公开(公告)日：2018-01-18

申请号：US15718422

申请日：2017-09-28

申请人： Anacor Pharmaceuticals, Inc.

发明人： Stephen J. Baker ,  Vincent S. Hernandez ,  Rashmi Sharma ,  James A. Nieman ,  Tsutomu Akama ,  Yong-Kang Zhang ,  Jacob J. Plattner ,  Michael Richard Kevin Alley ,  Rajeshwar Singh ,  Fernando Rock

IPC分类号： C07F5/02 ,  A61K31/69

摘要： This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

公开(公告)号：US20150080342A1

公开(公告)日：2015-03-19

申请号：US14394427

申请日：2013-03-15

申请人： Anacor Pharmaceuticals, Inc. ,  GlaxoSmithKline LLC

发明人： Michael Richard Kevin Alley ,  Katherine Widdowson

IPC分类号： A61K31/69 ,  A61K31/198

CPC分类号： A61K31/69 ,  A61K31/198 ,  Y02A50/473 ,  A61K2300/00

摘要： Norvaline and/or other amino acids that are capable of being acylated onto tRNALeu by LeuRS, in combination with substituted benzoxaboroles, such as a compound having a structure according to formula III: and methods for decreasing the frequency of resistance and/or reducing the rate of resistance and/or suppressing the emergence of resistance that develops in bacteria exposed to a substituted benzoxaborole or salt thereof by administering a combination of a substituted benzoxaborole such as a compound of formula III or salt thereof and an amino acid or a salt thereof.

摘要翻译： 能够通过LeuRS酰化成tRNALeu的诺瓦宁和/或其它氨基酸与取代的苯并恶唑组合，例如具有根据式III的结构的化合物，以及降低抗性频率和/或降低速率的方法 的抗性和/或抑制暴露于取代的苯并恶唑或其盐的细菌中产生的抗性的出现，其通过给予取代的苯并恶灵如结构式III的化合物或其盐与氨基酸或其盐的组合。

公开(公告)号：US20140011768A1

公开(公告)日：2014-01-09

申请号：US13915494

申请日：2013-06-11

申请人： ANACOR PHARMACEUTICALS, INC.

发明人： Tsutomu Akama ,  Yong-Kang Zhang ,  Charles Z. Ding ,  Jacob J. Plattner ,  Kirk R. Maples ,  Yvonne Freund ,  Virginia Sanders ,  Yi Xia ,  Stephen J. Baker ,  James A. Nieman ,  Xiaosong Lu ,  Marcelo Sales ,  Rashmi Sharma ,  Rajeshwar Singh ,  Robert Jacobs ,  Daitao Chen ,  Michael Richard Kevin Alley

IPC分类号： C07F5/04

CPC分类号： C07F5/025 ,  A61K31/69 ,  C07F5/04 ,  Y02A50/411

摘要： Compounds and methods of treating anti-inflammatory conditions are disclosed.

摘要翻译： 公开了治疗抗炎症状的化合物和方法。

公开(公告)号：US10526352B2

公开(公告)日：2020-01-07

申请号：US16385547

申请日：2019-04-16

申请人： GlaxoSmithKline Intellectual Property (No.2) Limited ,  Anacor Pharmaceuticals, Inc.

发明人： Michael Richard Kevin Alley ,  Vincent S. Hernandez ,  Jacob J. Plattner ,  Xianfeng Li ,  David Barros-Aguirre ,  Ilaria Giordano

IPC分类号： A61K31/69 ,  C07F5/04 ,  C07F5/02 ,  A61K45/06

摘要： Compounds of Formula II, wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2; compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.