23170-45-8Relevant academic research and scientific papers
COMBINATION THERAPIES WITH FARNESOID X RECEPTOR (FXR) MODULATORS
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Paragraph 00706, (2017/12/29)
Described herein are methods of treating a metabolic disorder in an individual in need thereof, comprising co-administering to the individual a therapeutically effective amount of an FXR modulator, and at least one second agent that is an CCR2/CCR5 antagonist, ASKl inhibitor, DPP-IV inhibitor, caspase protease inhibitor, SGLT2 inhibitor, acetyl-CoA carboxylase (ACC) inhibitor, diacyl glycerol acyltransferase-1 inhibitor, sodium -bile acid cotransporter-inhibitor, TLR-4 antagonist, PPAR alpha/delta agonist, or GLP-1 agonist, or a combination thereof.
FUSED BICYCLIC COMPOUNDS FOR THE TREATMENT OF DISEASE
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Paragraph 00292, (2016/06/21)
Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.
Discovery, design, and synthesis of indole-based EZH2 inhibitors
Gehling, Victor S.,Vaswani, Rishi G.,Nasveschuk, Christopher G.,Duplessis, Martin,Iyer, Priyadarshini,Balasubramanian, Srividya,Zhao, Feng,Good, Andrew C.,Campbell, Robert,Lee, Christina,Dakin, Les A.,Cook, Andrew S.,Gagnon, Alexandre,Harmange, Jean-Christophe,Audia, James E.,Cummings, Richard T.,Normant, Emmanuel,Trojer, Patrick,Albrecht, Brian K.
supporting information, p. 3644 - 3649 (2015/08/11)
The discovery and optimization of a series of small molecule EZH2 inhibitors is described. Starting from dimethylpyridone HTS hit (2), a series of indole-based EZH2 inhibitors were identified. Biochemical potency and microsomal stability were optimized during these studies and afforded compound 22. This compound demonstrates nanomolar levels of biochemical potency (IC50 = 0.002 μM), cellular potency (EC50 = 0.080 μM), and afforded tumor regression when dosed (200 mpk SC BID) in an EZH2 dependent tumor xenograft model.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 00183; 00184, (2013/08/28)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Direct synthesis of pyrazolo[5,1-a]isoindoles via intramolecular palladium-catalyzed C-H bond activation
Choi, Young Lok,Lee, Hyuk,Kim, Bum Tae,Choi, Kihang,Heo, Jung-Nyoung
supporting information; experimental part, p. 2041 - 2049 (2010/11/19)
An efficient, direct synthesis of pyrazolo-[5,1-a]isoindoles employing a palladium-catalyzed intramolecular C-H bond activation of 1-(2-halobenzyl) pyrazoles has been developed. The use of lithium chloride (LiCl) was found to be essential in these reactions, to suppress further C-H bond activation at the C-3 position of pyrazolo[5,1-a]isoindole, when C-3 is unsubstituted. This protocol can be applied to the synthesis of a pyrazolo[5,1-a]isoquinoline possessing a six-membered central ring system and a fully substituted pyrazolo[5,1-a]isoindole using sequential intra- and intermolecular C-H bond activation.
INHIBITORS OF CHECKPOINT KINASES
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Page/Page column 42, (2008/06/13)
The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound
1,3-Dipolar Cycloaddition Reactions of Transition-Metal Carbene Complexes and the Formal Pyridinannulation of the Cycloadducts
Chan, Kin Shing,Wulff, William D.
, p. 5229 - 5236 (2007/10/02)
The first examples of 1,3-dipolar cycloadditions of α,β-unsaturated carbene complexes are described.The reaction of alkynylcarbene complexes with diazomethane gives a mixture of two products.The first arises from a cycloaddition on the carbon-carbon
