75782-77-3Relevant academic research and scientific papers
INHIBITION OF P38 KINASE ACTIVITY USING SUBSTITUTED HETEROCYCLIC UREAS
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Page/Page column 14-15, (2012/03/10)
This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.
Inhibition of p38 Kinase Activity Using Aryl and Heteroaryl Substituted Heterocyclic Ureas
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, (2009/01/20)
This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.
INHIBITION OF RAF KINASE USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS
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Page/Page column 9, (2008/06/13)
Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se,
INHIBITION OF RAF KINASE USING SUBSTITUTED HETEROCYCLIC UREAS
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Page/Page column 14, (2010/11/28)
Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
INHIBITION OF RAF KINASE USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS
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Page/Page column 14-15, (2010/11/08)
Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS
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Page/Page column 16, (2010/11/24)
This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.
Discovery of a new class of p38 kinase inhibitors
Dumas, Jacques,Sibley, Robert,Riedl, Bernd,Monahan, Mary Katherine,Lee, Wendy,Lowinger, Timothy B.,Redman, Aniko M.,Johnson, Jeffrey S.,Kingery-Wood, Jill,Scott, William J.,Smith, Roger A.,Bobko, Mark,Schoenleber, Robert,Ranges, Gerald E.,Housley, Timothy J.,Bhargava, Ajay,Wilhelm, Scott M.,Shrikhande, Alka
, p. 2047 - 2050 (2007/10/03)
The MAP kinase p38 has been implicated in cytokine signaling, and its inhibitors are potentially useful for the treatment of arthritis and osteoporosis. Novel small-molecule inhibitors of p38 kinase were derived from a combinatorial chemistry effort and e
Solvent Effects in Thermal (2+2) Cycloaddition Reactions. Intramolecular Capture of 1,4-Dipolar Intermediates vs. (2+2) Cycloaddition in Reactions of 3-(1-Pyrrolidinyl)thiophenes with Electron-Deficient Acetylenes
Reinhoudt, David N.,Geevers, Jan,Trompenaars, Willem P.,Harkema, Sybolt,Hummel, Gerrit J. van
, p. 424 - 434 (2007/10/02)
3-(1-Pyrrolidinyl)thiophenes (1) react as "pseudo" enamines with electron-deficient acetylenes, such as dimethyl acetylenedicarboxylate (DMAD), dicyanoacetylene, and methyl propiolate.In apolar solvents with DMAD (2+2) cycloadducts are formed.These cycloadducts (2) isomerize under the reaction conditions to yield thiepins (3), which are also thermally unstable and eliminate sulfur via the isomeric norcaradienes (4) to give the benzene derivates (5), the isolated products.In protic polar solvents with DMAD, 6,7,7a,8-tetrahydro-5H-thienopirrolizines (6) are formed by intramolecular abstraction of hydrogen, or deuterium in specifically labeled 1d, in the initially formed 1,4-dipolar intermediate.In aprotic polar solvents the two modes of reaction compete and in these solvents and with excess of DMAD present, thiophenol derivatives (12) and a 4H-1-benzothia-pyran-4-one (13) were also isolated.Compounds 12 and 13 arise from S-alkylation of the thianorcaradienes (4), the valence isomers of the thiepins (3), by DMAD.The structures of the 5H-thienopyrrolizine 6e and the thiophenol derivatives 12d (E isomer) were proven by single-crystal X-ray analyses.A 1,4-dipolar intermediate formed from 1d and DMAD in acetonitrile has been intercepted by phenyl isocyanate; the 1:1:1 reaction product was obtained in 15percent yield.Dicyanoacetylene reacts with 1f in apolar solvent (CH2Cl2) to give a 6,7,7a,8-tetrahydro-5H-thienopyrrolizine (17).Methyl propiolate and 1d and DMAD and 4-(4-morpholinyl)-2-phenylthiophene afford linear Michael adducts (19 and 20, respectively) in methanol.
