473732-94-4Relevant academic research and scientific papers
PROCESS FOR CONTROLLED CRYSTAL SIZE IN 1,2-SUBSTITUTED 3,4-DIOXO-1-CYCLOBUTENE COMPOUNDS
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Page/Page column 23-24, (2009/03/07)
This application discloses a novel process for the preparation of 2-Hydroxy-N,N-dimethyl-3-[[2-[[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide, which has utility, for example, in the treatment of CXC chemokine-mediated diseases.
PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 1,2-SUBSTITUTED 3,4-DIOXO-1-CYCLOBUTENE COMPOUNDS
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Page/Page column 33-34, (2009/03/07)
This application discloses a novel process for the preparation of 1.2 - substituted 3, 4 - dioxo - 1 - cyclobutene compounds of formula (A), which have utility, for example, in the treatment of CXC chemokine -mediated diseases, and intermediates useful in the synthesis thereof.
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5-methylfuran-2-yl) propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): A potent, orally bioavailable CXCR2/CXCR1 receptor antagonist
Dwyer, Michael P.,Yu, Younong,Chao, Jianping,Aki, Cynthia,Chao, Jianhua,Biju, Purakkattle,Girijavallabhan, Viyyoor,Rindgen, Diane,Bond, Richard,Mayer-Ezel, Rosemary,Jakway, James,Hipkin, R. William,Fossetta, James,Gonsiorek, Waldemar,Bian, Hong,Fan, Xuedong,Terminelli, Carol,Fine, Jay,Lundell, Daniel,Merritt, J. Robert,Rokosz, Laura L.,Kaiser, Bernd,Li, Ge,Wang, Wei,Stauffer, Tara,Ozgur, Lynne,Baldwin, John,Taveras, Arthur G.
, p. 7603 - 7606 (2007/10/03)
Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity. Compound 4 displayed good oral bioavailability in rat and may be a potential therapeutic agent for the treatment of various inflammatory diseases.
Synthesis of 2-hydroxy-N,N-dimethyl-3-[[2-[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-l]aminobenzamide
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Page/Page column 24-25, (2008/06/13)
Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C1-C10)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.
THIADIAZOLEDIOXIDES AND THIADIAZOLEOXIDES AS CXC- AND CC-CHEMOKINE RECEPTOR LIGANDS
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Page 262, (2008/06/13)
Disclosed are novel compounds of the formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula (IA).
3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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Page 136; 137, (2008/06/13)
There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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Page 138, (2008/06/13)
There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
