专利号:US-8188282-B2 优先权日:2006-07-15 标 题:Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; HALLAND NIS; RKYEK OMAR; URMANN MATTHIAS 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; HALLAND NIS; RKYEK OMAR; URMANN MATTHIAS; SANOFI AVENTIS 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
专利号:US-9243002-B2 优先权日:2013-02-07 标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C 发明人:DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; BROCKUNIER LINDA L; NARGUND RAVI; MARCANTONIO KAREN; ZORN NICOLAS; XIAO DONG; PENG XUANJIA; LI PENG; GUO TAO 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-2009099200-A1 优先权日:2005-06-09 标题 :Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS 权利人:LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS 摘要:Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
专利号:AU-2007276514-A1 优先权日:2006-07-15 标题:A regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
专利号:US-5149814-A 优先权日:1987-09-30 标 题:Alkyl 2-benzylidene-4-(2-alkylimidazopyrid-1-yl) benzoylacetate esters as intermediate compounds 发明人:COOPER KELVIN; FRAY MICHAEL J; RICHARDSON KENNETH; STEELE JOHN 权利人:PFIZER 摘要:Intermediates useful in the synthesis of dihydropyridine platelet activating factor antagonists of the formula ##STR1## where R is phenyl or substituted phenyl; R 3 is lower alkyl; Y is 1,4-phenylene and X is 2-alkylimidazopyridyl.
专利号:CA-2657717-A1 优先权日:2006-07-15 标 题 :A regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles