- COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES AS GLUTAMINASE INHIBITORS FOR TREATING CANCERS THEREOF
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Provided are compounds of formula (I), wherein X, Y, Z, W, m, n, o, p, R1, R2 and R6 are defined as in the description. Pharmaceutical compositions and uses as glutaminase inhibitors for treating cancers thereof are also provided.
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Page/Page column 148-149; 156-157
(2014/06/11)
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- Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity
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Some κ opioid receptor agonists of the arylacetamide class, for example, ICI 199441 (1), were found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50 = 26 nM). Certain analogs bearing a substituted sulfonylamino group, for example, 13, were discovered to have significantly reduced CYP2D6 inhibitory activity (13: CYP2D6 IC50 > 10 μM) while displaying high affinity toward the cloned human κ opioid receptor, good κ/δ and κ/μ selectivity, and potent in vitro and in vivo agonist activity.
- Le Bourdonnec, Bertrand,Ajello, Christopher W.,Seida, Pamela R.,Susnow, Roberta G.,Cassel, Joel A.,Belanger, Serge,Stabley, Gabriel J.,DeHaven, Robert N.,DeHaven-Hudkins, Diane L.,Dolle, Roland E.
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p. 2647 - 2652
(2007/10/03)
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- Sulfonylamino phenylacetamide derivatives and methods of their use
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Sulfonylamino phenylacetamide derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed. In certain embodiments, the compounds of the invention that, preferably: (1) bind with high affinity to κ opioid receptors; (2) display good opioid receptor selectivity of κ versus μ and κ versus δ; and (3) do not substantially inhibit cytochrome P450 enzymatic activity, in particular CYP2D6, CYP2C9 and CYP3A4.
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- Tetrahydroquinoline derivatives useful for neurodegenerative disorders
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A class of 1,2,3,4-tetrahydroquinolines possessing at least one substituent, or a spirocyclic moiety, at the 4-position, and an acidic group or a group convertible thereto in vivo at the 2-position, are specific antagonists of N-methyl-D-aspartate (NMDA) receptors and are therefore useful in the treatment and/or prevention of neurodegenerative disorders.
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- 7-Acyl-3-(sulfonic acid and sulfamoyl substituted tetrazolyl thiomethyl) cephalosporins
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The compounds of this invention are cephalosporins having a 3- or 4-aminomethylphenylacetamido substituent at the 7-position and a sulfonic acid substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus. The compounds have antibacterial activity.
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