专利号:US-8519168-B2 优先权日:2007-07-03 标 题 :Process and intermediates for the synthesis of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds 发明人:FU XIAOYONG; GUENTER FRANK BRUNO; KIM-MEADE AGNES S; MATTHEWS KENNETH STANLEY; MAUST MATHEW THOMAS; MCALLISTER TIMOTHY L; WERNE GERALD; WINTERS JASON L; YIN JIANGUO; ZHANG SHUYI 权利人:FU XIAOYONG; GUENTER FRANK BRUNO; KIM-MEADE AGNES S; MATTHEWS KENNETH STANLEY; MAUST MATHEW THOMAS; WERNE GERALD; WINTERS JASON L; YIN JIANGUO; ZHANG SHUYI; MOLOZNIK DAVID J; MERCK SHARP & DOHME 摘要:This application discloses a novel process for the preparation of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds, which have utility, for example, in the treatment of CXC chemokine-mediated diseases, and intermediates useful in the synthesis thereof.
专利号:US-8207221-B2 优先权日:2004-01-30 标 题:Crystalline polymorphs of a CXC-chemokine receptor ligand 发明人:HU MENGWEI; YU YOUNONG; DWYER MICHAEL P; TAVERAS ARTHUR G; KIM-MEADE AGNES; YIN JIANGUO; FU XIAOYONG; MCALLISTER TIMOTHY L; ZHANG SHUYI; KLOPFER KEVIN 权利人:HU MENGWEI; YU YOUNONG; DWYER MICHAEL P; TAVERAS ARTHUR G; KIM-MEADE AGNES; YIN JIANGUO; FU XIAOYONG; MCALLISTER TIMOTHY L; ZHANG SHUYI; KLOPFER KEVIN; SCHERING CORP 摘要:The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: n n n n n n n n n n These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.
专利号:US-7910775-B2 优先权日:2003-04-18 标题 :Synthesis 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 发明人:YIN JIANGUO; FU XIAOYONG; ZHANG SHUYI; MCALLISTER TIMOTHY L; KIM-MEADE AGNES S; WINTERS JASON L; SUDHAKAR ANANTHA; SCHUMACHER DORIS P 权利人:SCHERING CORP 摘要:Disclosed is a process for making the compound of formula I: n nusing the compounds of formulas II, Q, and XI or XII:n n nwherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C 1 -C 10 )alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.
专利号:US-2006205961-A1 优先权日:2003-04-18 标 题:Synthesis of 2-hydroxy-N,N-dimethyl-3-[[2-(1(R)-(5-methyl-2-furany)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide
专利号:US-2009048458-A1 优先权日:2003-04-18 标题:Synthesis 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
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摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749