- Histone Deacetylase 6 Selective Inhibitors for the Treatment of Cisplatin-Induced Peripheral Neuropathy
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Disclosed are methods for treating cisplatin-induced peripheral neuropathy in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a histone deacetylase 6 selective inhibitor.
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Paragraph 0117-0118
(2017/04/04)
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- PYRIMIDINE HYDROXY AMIDE COMPOUNDS AS HDAC6 SELECTIVE INHIBITORS
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The present invention relates to pyrimidine hydroxy amide compounds, the use of such compounds in the inhibition of HDAC6, and the use of such compounds in the treatment of various diseases, disorders, or conditions related to HDAC6.
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Paragraph 0151; 0156; 0157
(2015/09/23)
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- TREATMENT OF POLYCYSTIC DISEASES WITH AN HDAC6 INHIBITOR
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An HDAC6-specific inhibitor (i.e., a compound of Formula I or II) is shown to reduce the pathogenesis associated with polycystic disease. Administration of an HDAC6-specific inhibitor attenuated many of the symptoms characteristic of polycystic liver disease including cyst formation, cyst growth and cholangiocyte proliferation. Treatment with a HDAC6-specific inhibitor also increased the amount of bile duct acetylated tubulin and β-catenin phosphorylation and/or acetylation while reducing bile duct β-catenin synthesis. These results demonstrate that HDAC6 is overexpressed in cystic cholangiocytes and that its pharmacological inhibition reduces cholangiocyte proliferation and cyst growth.
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Paragraph 0177
(2015/05/05)
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- Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists
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A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.
- Zhang, Xuqing,Hufnagel, Heather,Markotan, Thomas,Lanter, James,Cai, Chaozhong,Hou, Cuifen,Singer, Monica,Opas, Evan,McKenney, Sandra,Crysler, Carl,Johnson, Dana,Sui, Zhihua
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supporting information; experimental part
p. 5577 - 5582
(2011/10/09)
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- 4-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2
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The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
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Page/Page column 94
(2010/11/03)
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- 4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I.
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A series of novel 4,4-disubstituted cyclohexylamine based NK(1) antagonists is described. The effect of changes to the C(1)-C(4) relative stereochemistry on the cyclohexane ring and replacements for the flexible linker are discussed, leading to the identification of compounds with high affinity and good in vivo duration of action.
- Elliott, Jason M,Castro, Jose L,Chicchi, Gary G,Cooper, Laura C,Dinnell, Kevin,Hollingworth, Gregory J,Ridgill, Mark P,Rycroft, Wayne,Kurtz, Marc M,Shaw, Duncan E,Swain, Christopher J,Tsao, Kwei-Lan,Yang, Lihu
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p. 1755 - 1758
(2007/10/03)
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