- GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
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Paragraph 000829
(2015/04/15)
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- HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE
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Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
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Page/Page column 37
(2010/07/02)
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- Inhibition of uridine phosphorylase. Synthesis and structure-Activity relationships of aryl-substituted 1-((2-hydroxyethoxy)methyl)-5-(3- phenoxybenzyl)uracil
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Structure-activity relationship studies on a series of 1-((2- hydroxyethoxy)methyl)-5-(3-(substituted-phenoxy)benzyl)uracils as inhibitors of murine liver uridine phosphorylase have led to compounds with IC50s as low as 1.4 nM. The two most potent compounds, 10j (3-cyanophenoxy) and 11f (3-chlorophenoxy) were tested in vive for effects on steady-state concentrations of circulating uridine in mice and rats. Both compounds were substantially more efficacious than BAU (5-benzylacyclouridine) both in vitro and in vivo.
- Orr, G. Faye,Musso, David L.,Kelley, James L.,Joyner, Suzanne S.,Davis, Stephen T.,Baccanari, David P.
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p. 1179 - 1185
(2007/10/03)
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- Anti-inflammatory aryl derivatives
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The present inventions concerned with compounds of formula (I) wherein, Ar is 4-halophenyl;, Ar? is 1,3- or 1,4-phenylene;, Y is (E)-CH=CH-; and, R1 and R2 are independently selected from hydrogen and C1-4alkyl;, and base salts and physiologica
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