- THIENO (2,3 - C) PYRAZOLES FOR USE AS POTASSIUM CHANNEL INHIBITORS
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The present invention provides compounds of formula (I): wherein A, R1, R2, R3 IX, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.
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Paragraph 0446
(2014/12/09)
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- THIENO [2, 3 - C] PYRAZOLES FOR USE AS POTASSIUM CHANNEL INHIBITORS
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The present invention provides compounds of formula (I): wherein A, R1, R2, R3IX, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.
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Page/Page column 70
(2013/06/05)
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- Concise synthesis of bicyclic aminals by way of catalytic intramolecular C-H amination and evaluation of their reactivity as iminium precursors
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The concise synthesis of fused bicyclic aminals by way of intramolecular rhodium-catalyzed C-H amination is reported as well as the evaluation of their reactivity as iminium precursors. In contrast to the well-studied N,O-acetal systems, the aminals synthesized were found to be particularly stable under reaction conditions used for nucleophilic addition.
- Rodriguez-Lucena, David,Morin, Marie S.T.,Compain, Philippe
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p. 155 - 162
(2012/04/04)
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- A library of conformationally restricted saturated heterocyclic sulfonyl chlorides
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An approach to the synthesis of conformationally restricted saturated heterocyclic sulfonyl chlorides is described. Being guided by the principle of diversity-oriented conformational restriction, a mini-library of saturated heterocyclic sulfonyl chlorides
- Zhersh, Sergey,Buryanov, Volodymyr V.,Karpenko, Oleksandr V.,Grygorenko, Oleksandr O.,Tolmachev, Andrey A.
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scheme or table
p. 3669 - 3674
(2011/12/16)
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- Disubstituted pyrimidines as Lck inhibitors
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We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are also low-nanomolar inhibitors of cell
- Hunt, Julianne A.,Beresis, Richard T.,Goulet, Joung L.,Holmes, Mark A.,Hong, Xinfang J.,Kovacs, Ernest,Mills, Sander G.,Ruzek, Rowena D.,Wong, Frederick,Hermes, Jeffrey D.,Park, Young-Whan,Salowe, Scott P.,Sonatore, Lisa M.,Wu, Lin,Woods, Andrea,Zaller, Dennis M.,Sinclair, Peter J.
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supporting information; experimental part
p. 5440 - 5443
(2010/04/26)
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- 5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE-DERIVATIVES AND THEIR USES AS ANTIBACTERIALS
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The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; Rsup
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Page/Page column 15
(2009/10/06)
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- 5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE DERIVATIVES
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The invention relates to novel chimeric antibiotics of formula (I) wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; Rs
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Page/Page column 37
(2008/12/05)
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- The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents
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Several novel series of nitrile-containing fluoroquinolones with weakly basic amines are reported which have reduced potential for hERG (human ether-a-go-go gene) channel inhibition as measured by the dofetilide assay. The new fluoroquinolones are potent
- Murphy, Sean T.,Case, Heather L.,Ellsworth, Edmund,Hagen, Susan,Huband, Michael,Joannides, Themis,Limberakis, Chris,Marotti, Keith R.,Ottolini, Amy M.,Rauckhorst, Mark,Starr, Jeremy,Stier, Michael,Taylor, Clarke,Zhu, Tong,Blaser, Adrian,Denny, William A.,Lu, Guo-Liang,Smaill, Jeff B.,Rivault, Freddy
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p. 2150 - 2155
(2008/02/02)
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- QUINOLONE ANTIBACTERIAL AGENTS
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Compounds of formula (I) and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula (I) as well as pharmaceutically acceptable compositions comprising compounds of formula (I). Compounds of formula (I) as disclosed herein can be used in a variety of applications including use as antibacterial agents.
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Page/Page column 109-110
(2010/02/11)
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- QUINOLONE ANTIBACTERIAL AGENTS
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Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents.
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Page/Page column 136-137
(2010/02/11)
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