- BIARYL PYRAZOLES AS NRF2 REGULATORS
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The present invention relates to biaryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
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- Efficient synthesis of 1,3,4-oxadiazoles promoted by NH4Cl
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An efficient and inexpensive approach to the synthesis of 2-substituted and 2,5-disubstituted 1,3,4-oxadiazoles from arylhydrazides and orthoesters is reported using catalytic NH4Cl. The conditions are mild, and thus, compatible with a variety of functional groups. The optimized reaction is performed using 30 mol % of NH4Cl in 100% EtOH and is generally complete within 1 h for non-aromatic orthoesters and 2-10 h for aromatic orthoesters. The reaction permits both electron-releasing and electron-withdrawing groups on the arylhydrazide substrate. Most products are formed in high yields and require only minimal purification. Compared with earlier reports, the current reactions proceed in shorter time and require less of the orthoester.
- Gnanasekaran, Krishna Kumar,Nammalwar, Baskar,Murie, Maeghan,Bunce, Richard A.
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supporting information
p. 6776 - 6778
(2015/01/09)
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- Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR
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The biphenyl amides are a novel series of p38 MAP kinase inhibitors. Structure-activity relationships of the series against p38α are discussed with reference to the X-ray crystal structure of an example. The series was optimised rapidly to a compound showing oral activity in an in vivo disease model.
- Angell, Richard M.,Angell, Tony D.,Bamborough, Paul,Brown, David,Brown, Murray,Buckton, Jacky B.,Cockerill, Stuart G.,Edwards, Chris D.,Jones, Katherine L.,Longstaff, Tim,Smee, Penny A.,Smith, Kathryn J.,Somers, Don O.,Walker, Ann L.,Willson, Malcolm
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p. 324 - 328
(2008/12/22)
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- 2-Heteroaryl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1-isoxazolyl, R1-oxadiazolyl, R1-dihydrofuranyl, R1-pyrazolyl, R1-imidazolyl, R1-pyrazinyl or R1-pyrimidinyl; R1 is 1, 2 or 3 substituents selected from H, alkyl, alkoxy and halo; Z is optionally substituted-aryl, or optionally substituted-heteroaryl; are disclosed, as well as their use in the treatment of central nervous system diseases, in particular Parkinson's disease and Extra Pyramidal Syndrome, pharmaceutical compositions comprising them, and combinations with other agents.
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Page/Page column 19
(2008/06/13)
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