- Overcoming the Pregnane X Receptor Liability: Rational Design to Eliminate PXR-Mediated CYP Induction
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The pregnane X receptor (PXR) regulates expression of proteins responsible for all three phases required for the detoxification mechanism, which include CYP450 enzymes, phase II enzymes, and multidrug efflux pumps. Therefore, PXR is a prominent receptor t
- Ramanjulu, Joshi M.,Williams, Shawn P.,Lakdawala, Ami S.,Demartino, Michael P.,Lan, Yunfeng,Marquis, Robert W.
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supporting information
p. N
(2021/09/02)
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- 5-SULFAMOYL-2-HYDROXYBENZAMIDE DERIVATIVES
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The invention is directed to substituted salicylamide derivatives. Specifically, the invention is directed to compounds according to Formula (I): wherein R, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, the treatment of HIV, autoimmune diseases, infections, atherosclerosis, and ischemia–reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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Page/Page column 213
(2017/09/27)
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- CALCILYTIC COMPOUNDS
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Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.
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Page/Page column 46
(2008/06/13)
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- PARP inhibitors
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A compound of the formula (I): and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 /su
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Page/Page column 27-28
(2008/06/13)
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- A short and efficient preparation of methyl-[1,2,4]oxadiazolium derivatives with plant-inducing activity
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A short and efficient preparation of methyl-[1,2,4]oxadiazolium derivatives with plant-inducing activity is discussed. A concise and efficient synthetic method leading to structurally diverse array of oxadiazolium derivatives, starting from halogenated phenols is also developed. The starting point of the synthesis is the Lewis acid mediated addition of isocyanates to phenols. The strategy also involves a new and rapid access to all meta-halogenated salicylic acids, compounds of high synthetic value.
- Dobler, Markus R.
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p. 963 - 964
(2007/10/03)
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