公开(公告)号：WO2019046465A3

公开(公告)日：2019-03-07

申请号：PCT/US2018/048607

申请日：2018-08-29

申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  FREUNDLICH, Joel S. ,  ALLAND, David ,  NEIDITCH, Matthew B. ,  INOYAMA, Daigo ,  CAPODAGLI, Glenn ,  KUMAR, Pradeep

发明人： FREUNDLICH, Joel S. ,  ALLAND, David ,  NEIDITCH, Matthew B. ,  INOYAMA, Daigo ,  CAPODAGLI, Glenn ,  KUMAR, Pradeep

IPC分类号： A61K31/166 ,  A61K31/404

摘要： The invention provides compounds of formula I and salts thereof wherein R1-R4 have any of the meanings described in the specification. The compounds are useful for treating bacterial infections (e.g. tuberculosis).

公开(公告)号：WO2019173507A1

公开(公告)日：2019-09-12

申请号：PCT/US2019/021004

申请日：2019-03-06

申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  EBRIGHT, Richard, H. ,  EBRIGHT, Yon, W. ,  FREUNDLICH, Joel, S. ,  GALLARDO-MACIAS, Ricardo ,  LI, Shao-Gang

发明人： EBRIGHT, Richard, H. ,  EBRIGHT, Yon, W. ,  FREUNDLICH, Joel, S. ,  GALLARDO-MACIAS, Ricardo ,  LI, Shao-Gang

IPC分类号： C07D239/34 ,  C07C237/48 ,  C07D295/155 ,  C07D213/56 ,  C07D213/65 ,  A61K31/505 ,  A61K31/4409 ,  A61K31/5375 ,  A61K31/4406 ,  A61K31/4402 ,  A61K31/166 ,  A61P31/04 ,  A61P31/02

摘要： The invention provides compounds of formula (I) or (II) and tautomers and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula (I) or (II) or a tautomer or salt thereof, methods of making a compound of formula (I) or (II) or a tautomer or salt thereof, and methods of using a compound of formula (I) or (II) or a tautomer or salt thereof as, e.g., inhibitors of bacterial RNA polymerase or as antibacterial agents.

公开(公告)号：WO2019046465A2

公开(公告)日：2019-03-07

申请号：PCT/US2018/048607

申请日：2018-08-29

申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  FREUNDLICH, Joel S. ,  ALLAND, David ,  NEIDITCH, Matthew B. ,  INOYAMA, Daigo ,  CAPODAGLI, Glenn ,  KUMAR, Pradeep

发明人： FREUNDLICH, Joel S. ,  ALLAND, David ,  NEIDITCH, Matthew B. ,  INOYAMA, Daigo ,  CAPODAGLI, Glenn ,  KUMAR, Pradeep

IPC分类号： A61K31/541 ,  C07D417/10

CPC分类号： C07D209/42 ,  A61K31/404 ,  A61K31/4409 ,  A61K45/06 ,  C07D209/08 ,  C07D209/14 ,  C07D209/30 ,  C07D405/12 ,  A61K2300/00

摘要： The invention provides compounds of formula I and salts thereof wherein R1-R4 have any of the meanings described in the specification. The compounds are useful for treating bacterial infections (e.g. tuberculosis).

公开(公告)号：WO2017100645A3

公开(公告)日：2017-06-15

申请号：PCT/US2016/065931

申请日：2016-12-09

申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  EBRIGHT, Richard H. ,  FREUNDLICH, Joel ,  MITTAL, Nisha ,  JASKOWSKI, Mark ,  SHEN, Juan

发明人： EBRIGHT, Richard H. ,  FREUNDLICH, Joel ,  MITTAL, Nisha ,  JASKOWSKI, Mark ,  SHEN, Juan

IPC分类号： A61K38/12 ,  A01N37/18 ,  C07K11/02

摘要： The invention provides compounds that are inhibitors of bacterial RNA polymerase. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.

摘要翻译： 本发明提供了作为细菌RNA聚合酶抑制剂的化合物。 本发明还提供包含此类化合物的组合物，制备此类化合物的方法以及使用所述化合物的方法。 本发明可用于控制细菌基因表达，控制细菌生长，抗菌化学和抗菌疗法。

公开(公告)号：WO2017100645A2

公开(公告)日：2017-06-15

申请号：PCT/US2016/065931

申请日：2016-12-09

申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  EBRIGHT, Richard H. ,  FREUNDLICH, Joel ,  MITTAL, Nisha ,  JASKOWSKI, Mark ,  SHEN, Juan

发明人： EBRIGHT, Richard H. ,  FREUNDLICH, Joel ,  MITTAL, Nisha ,  JASKOWSKI, Mark ,  SHEN, Juan

IPC分类号： A61K31/381 ,  A61K31/12

CPC分类号： A61K31/12 ,  A61K31/381 ,  C07C49/753 ,  C07C49/83 ,  C07C49/835 ,  C07C49/84 ,  C07C2601/02 ,  C07C2601/16 ,  C07D213/64 ,  C07D213/643 ,  C07D333/22

摘要： The invention provides compounds that are inhibitors of bacterial RNA polymerase. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.

公开(公告)号：WO2019046467A1

公开(公告)日：2019-03-07

申请号：PCT/US2018/048611

申请日：2018-08-29

申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  FREUNDLICH, Joel S. ,  ALLAND, David ,  NEIDITCH, Matthew B. ,  KUMAR, Pradeep ,  CAPODAGLI, Glenn ,  AWASTHI, Divya ,  EKINS, Sean

发明人： FREUNDLICH, Joel S. ,  ALLAND, David ,  NEIDITCH, Matthew B. ,  KUMAR, Pradeep ,  CAPODAGLI, Glenn ,  AWASTHI, Divya ,  EKINS, Sean

IPC分类号： C07D231/56 ,  A61K31/416 ,  A61P31/06

CPC分类号： C07D231/56 ,  A61P31/06

摘要： The invention provides compounds of formula (I): and salts thereof wherein R 1 -R 5 have any of the meanings described in the specification. The compounds are useful for treating bacterial infections (e.g. tuberculosis).

公开(公告)号：WO2008008059A1

公开(公告)日：2008-01-17

申请号：PCT/US2006/026935

申请日：2006-07-12

申请人： LOCUS PHARMACEUTICALS, INC. ,  KELLY, Martha ,  LEE, Younghee ,  LIU, Bin ,  FUJIMOTO, Ted ,  FREUNDLICH, Joel ,  DORSEY, Bruce ,  FLYNN, Gary A. ,  HUSAIN, Arifa ,  MOORE, William R., Jr.

发明人： KELLY, Martha ,  LEE, Younghee ,  LIU, Bin ,  FUJIMOTO, Ted ,  FREUNDLICH, Joel ,  DORSEY, Bruce ,  FLYNN, Gary A. ,  HUSAIN, Arifa ,  MOORE, William R., Jr.

IPC分类号： A61K31/44 ,  A61K31/505 ,  A61K31/506 ,  C07D213/02 ,  C07D239/02 ,  C07D401/02

CPC分类号： C07D209/08 ,  C07D213/40 ,  C07D213/74 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10

摘要： The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula (I): and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A 1 is N or CR 1 ; A 3 is N or CR 3 ; A 5 is N or CR 5 ; R 1 , R 3 R 6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6- 10 carbons in the ring portion, an optionally-substituted 6- membered heteroaryl group having 1- 3 nitrogen atoms in the ring portion, an optionally-substituted 5- membered heteroaryl group having 0- 4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6- membered ring is fused either to a 5- membered ring or to a 6- membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.

摘要翻译： 本发明涉及新型化合物及其盐，其合成及其作为抗癌剂的用途。 化合物包括式（I）的化合物及其溶剂化物，水合物及其药学上可接受的盐，其中A 1是N或CR 1; N 3或N 3是N或CR 3; A <5>为N或CR 5; R 1，R 3，S 6和L在说明书中定义; n为0或1; 并且X是在环部分中具有6-10个碳的任选取代的芳基，在环部分中具有1-3个氮原子的任选取代的6-元杂芳基，任选取代的具有0个碳原子的五元杂芳基 环部分中的4个氮原子，并且在环部分中任选具有1个硫原子或1个氧原子，或任选取代的杂芳基，其中6-元环与5-元环或六 其中在每种情况下，1,2,3或4个环原子是独立地选自氮，氧和硫的杂原子。 它们对广泛的癌症尤其是白血病，前列腺，非小细胞肺和结肠有效。 它们还可用于治疗增殖性视网膜病变，例如糖尿病性神经病变和黄斑变性。