119924-96-8Relevant articles and documents
IMIDAZO[1,2-B]PYRIDAZINE IL-17A INHIBITORS
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Page/Page column 22; 57-58, (2020/07/25)
The invention provides certain difluorocyclohexyl-imidazopyridazinyl-imidazolidinone compounds of formula II as IL-17A inhibitors, pharmaceutical compositions thereof, and methods of using a compound of formula II to treat certain symptoms of psoriasis, rheumatoid arthritis or multiple sclerosis.
SULFONYLUREA DERIVATIVES AND USES THEREOF
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Paragraph 01135-01136, (2020/12/30)
The present disclosure relates to compounds of Formula (I) and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies
Lange, Jos H.M.,van der Neut, Martina A.W.,Wals, Henri C.,Kuil, Gijs D.,Borst, Alice J.M.,Mulder, Arie,den Hartog, Arnold P.,Zilaout, Hicham,Goutier, Wouter,van Stuivenberg, Herman H.,van Vliet, Bernard J.
scheme or table, p. 1084 - 1089 (2010/06/11)
The synthesis and structure-activity relationship studies of imidazoles are described. The target compounds 6-20 represent a novel chemotype of potent and CB2/CB1 selective cannabinoid CB2 receptor antagonists/inverse agonists with very high binding efficiencies in combination with favourable log P and calculated polar surface area values. Compound 12 exhibited the highest CB2 receptor affinity (Ki = 1.03 nM) in this series, as well as the highest CB2/CB1 subtype selectivity (>9708-fold).
Unusual domino Michael/aldol condensation reactions employing oximes as N-selective nucleophiles: Synthesis of N-hydroxypyrroles
Tan, Bin,Shi, Zugui,Chua, Pei Juan,Li, Yongxin,Zhong, Guofu
supporting information; experimental part, p. 758 - 761 (2009/05/06)
(Figure Presented) A facile synthesis of N-hydroxypyrroles has been developed using readily available α-carbonyl oximes and α,β-unsaturated aldehydes. The domino reaction proceeds through iminium activation of α,β-unsaturated aldehydes, Michael addition u
α2 Adrenoceptor agonists as potential analgesic agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles
Boyd, Robert E.,Press, Jeffery B.,Rasmussen, C. Royce,Raffa, Robert B.,Codd, Ellen E.,Connelly, Charlene D.,Bennett, Debra J.,Kirifides, Alex L.,Gardocki, Joseph F.,Reynolds, Brian,Hortenstein, John T.,Reitz, Allen B.
, p. 5064 - 5071 (2007/10/03)
A series of (imidazolylmethyl)oxazoles and -thiazoles were prepared and evaluated as α2 adrenoceptor agonists. These compounds were also tested in in vivo paradigms that are predictive of analgesic activity. Variations in both the imidazole and thiazole portions of the molecule were investigated. Some of the more potent compounds such as 22, 26, 45, and 53 displayed α2 receptor binding in the 10-20 nM range and also had significant antinociceptive activity in the mouse abdominal irritant test (MAIT).
Porphyrins with Exocyclic Rings. 1. Chemistry of 4,5,6,7-Tetrahydro-1H-indoles: Synthesis of Acetoxy Derivatives, Dihydroindoles, and Novel Porphyrins with Four Exocyclic Rings
Lash, Timothy D.,Bladel, Karla A.,Shiner, Craig M.,Zajeski, Donna L.,Balasubramaniam, Rajiv P.
, p. 4809 - 4820 (2007/10/02)
A variety of 4,5,6,7-tetrahydro-1H-indoles (THI's) and 4-oxo-4,5,6,7-tetrahydro-1-indoles (4-oxoTHI's) have been synthesized from cyclohexanone and 1,3-cyclohexanedione, respectively.The THI's reacted regioselectively with lead tetraacetate in acetic acid
Cardiotonic Agents. 5. Fragments from the Heterocycle-Phenyl-Imidazole Pharmacophore
Erhardt, Paul W.,Hagedorn, Alfred A.,Davey, David,Pease, Cynthia A.,Venepalli, Bhaskar R.,et al.
, p. 1173 - 1176 (2007/10/02)
To examine the role of each component in the heterocycle-phenyl-imidazole inotropic pharmacophore, several imidazolone derivatives, an arylimidazole, a substituted 3,4-dihydro-4-oxopyrimidine, and a quinolin-2(1H)-one derivative were prepared as structura
