专利号:US-2019040070-A1 优先权日:2016-02-09 标 题:Process for the synthesis of stable amorphous ibrutinib 发明人:MAIER THOMAS; KARAPETYAN INNA; ARAKELYAN ALVARD; MARGARYAN TAMARA; SARGSYAN VARDAN; STEPANYAN HEGHINE; ABOVYAN HERMINE; GERBER AESCHBACHER ROMAN; HAFERKAMP SVEN 权利人:AZAD PHARMACEUTICAL INGREDIENTS AG 摘要:Disclosed herein is a new route of synthesis and a new stable amorphous form of ibrutinib. Also disclosed are pharmaceutical compositions, oral dosage forms and the use of the amorphous ibrutinib in the treatment of mantle cell lymphoma or chronic lymphocytic leukemia.
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-7129357-B2 优先权日:2003-09-15 标题:Synthesis of quinoline 5-carboxamides useful for the preparation of PDE IV inhibitors 发明人:ANDREWS DAVID R; TANG SUHAN; WU WENXUE; KALLINEY SAMI Y; SUDHAKAR ANANTHA; NIELSEN CHRISTOPHER 权利人:SCHERING CORP 摘要:In one embodiment, the present application discloses a process for making the compound of the formula:
专利号:US-9260428-B2 优先权日:2007-03-22 标 题 :Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds 发明人:MERGELSBERG INGRID; SCHERER DOMINIK HERMANN; HUTTENLOCH MONIKA ERIKA; TSUI HON-CHUNG; PALIWAL SUNIL; SHIH NENG-YANG 权利人:OPKO HEALTH INC 摘要:This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1.7-diaza-spiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.
专利号:US-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:US-9822116-B2 优先权日:2008-09-05 标 题:Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds 发明人:WU GEORGE G; WERNE GERALD; FU XIAOYONG; ORR ROBERT K; CHEN FRANK XING; CUI JIAN; SPRAGUE VICTORIA M; ZHANG FUCHENG; XIE JI; ZENG LIANSHENG; CASTELLANOS LOUIS PETER; CHEN YUYIN; POIRIER MARC; MERGELSBERG INGRID 权利人:OPKO HEALTH INC 摘要:This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.