- ANTIBACTERIAL COMPOUNDS
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Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting the growth of gram-negative bacteria. Furthermore, the subject compounds and compositions are useful for the treatment of bacterial infection, such as urinary tract infection and the like.
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Paragraph 00205
(2020/06/05)
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- PYRIDINONE AND PYRIMIDINONE PHOSPHATES AND BORONATES USEFUL AS ANTIBACTERIAL AGENTS
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The present invention is directed to new pyridinone or pyrimidinone hydroxamic acid phosphates of Formula (1 ) and boronates of Formula (2), stereoisomers thereof; wherein Q is selected from the group consisting of -P(0)(OH)2, -P(0)(OH)(0"M+), - P(0)(0"M+)2 and -P(0)(0")2M2+; M+ at each occurrence is a pharmaceutically acceptable monovalent cation; and M2+ is a pharmaceutically acceptable divalent cation; X is CH or N; and Z is as defined herein; and their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
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Page/Page column 42; 43
(2019/10/04)
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- Concise Entries to 4-Halo-2-pyridones and 3-Bromo-4-halo-2-pyridones
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Methods for the synthesis of both simple 4-halo-2-pyridones and more functionalized 3,4-di- and (3,4,5-tri)-halo-2-pyridones are described that are based on a combination of Sandmeyer and regioselective (copper-mediated) halogenation, with a 2-chloro or a 2-benzyloxy moiety serving as a masked 2-pyridone.
- Honraedt, Aurélien,Gallagher, Timothy
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- FUSED THIOPHENE AND THIAZOLE DERIVATIVES AS ROR GAMMA MODULATORS
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The present invention provides fused thiophene and thiazole derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; in which R1, R2, R3, R4, R5, R6, R7, X1, X2, L, m, n and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in disease(s) or disorder(s) where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the fused thiophene and thiazole derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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Page/Page column 48
(2015/07/16)
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- ETHYNE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them
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Page/Page column 94
(2012/03/27)
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- New compounds, pharmaceutical compositions and uses thereof
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The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 40
(2012/09/05)
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- New compounds, pharmaceutical compositions and uses thereof
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The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 41
(2012/09/05)
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- N-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS
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The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections. Formula (I).
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Page/Page column 31
(2011/07/07)
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- CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
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This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, Io1, Io2, Io5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
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Page/Page column 89; 90
(2011/01/05)
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