- HETEROCYCLIC WDR5 INHIBITORS AS ANTI-CANCER COMPOUNDS
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The present invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; (I) which are inhibitors of WDR5. The present invention also provides pharmaceutical compositions comprising such compounds, compositions comprising such compounds with an additional therapeutic agent and the therapeutic uses of such compounds.
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Page/Page column 100
(2021/02/19)
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- Strategies to lower the Pgp efflux liability in a series of potent indole azetidine MCHR1 antagonists
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A series of potent indolyl azetidine rMCHR1 antagonists were found to show poor CNS penetration due to Pgp efflux. We envisioned a strategy which included: lowering basicity; changing the conformational flexibility motif; and removal of a hydrogen bond donor, in an attempt to optimize this property while maintaining target receptor efficacy. This work resulted in mitigation of Pgp efflux, and led us to identify 1-dihydroindolyl azetidine derivatives with CNS penetration and excellent rMCHR1 binding affinity.
- Lu, Kai,Jiang, Yu,Chen, Bin,Eldemenky, Eman M.,Ma, Gil,Packiarajan, Mathivanan,Chandrasena, Gamini,White, Andrew D.,Jones, Kenneth A.,Li, Boshan,Hong, Sang-Phyo
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supporting information; experimental part
p. 5310 - 5314
(2011/10/03)
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- Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase
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The identification and evolution of a series of potent and selective p38 inhibitors is described. p38 inhibitors based on a N-benzyl pyridinone high-throughput screening hit were prepared and their SAR explored. Their design was guided by ligand bound co-
- Selness, Shaun R.,Devraj, Rajesh V.,Monahan, Joseph B.,Boehm, Terri L.,Walker, John K.,Devadas, Balekudru,Durley, Richard C.,Kurumbail, Ravi,Shieh, Huey,Xing, Li,Hepperle, Michael,Rucker, Paul V.,Jerome, Kevin D.,Benson, Alan G.,Marrufo, Laura D.,Madsen, Heather M.,Hitchcock, Jeff,Owen, Tom J.,Christie, Lance,Promo, Michele A.,Hickory, Brian S.,Alvira, Edgardo,Naing, Win,Blevis-Bal, Radhika
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scheme or table
p. 5851 - 5856
(2010/07/05)
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- PYRIDONE DERIVATIVE
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The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R 1 and R 2 may be same or different and stands for H, etc., or R 1 and R 2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X 1 -X 3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X 4 -X 7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y 1 and Y 3 may be same or different and stand for single bond, -0-, -NR-, -S-, etc ; Y 2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z 1 and Z 2 may be same or different and stand for single bond or lower alkylene; or R 1 , L and Z 2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R 1 binds; and Ar stands for aromatic carbocyclic group, etc.].
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Page/Page column 62-63
(2010/11/25)
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- Syntheses and Ring-opening Reactions of 5-Alkoxy- and 5-Acetoxy-3-oxo-2-azabicyclohex-5-enes
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The efficient photochemical synthesis of 5-alkoxy- and 5-acetoxy-3-oxo-2-azabicyclohex-5-enes (2a-e and f, g), and a new rearrangement reaction of the former compounds (2a-e) to 6-alkoxy-2-pyridones (3a-e), are reported.
- Kaneko, Chikara,Shiba, Kazuhiro,Fujii, Harure,Momose, Yu
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p. 1177 - 1178
(2007/10/02)
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