专利号:WO-2011106929-A1 优先权日:2010-03-02 标题:Inhibitors of hepatitis c virus ns5b polymerase 发明人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO 权利人:MERCK SHARP & DOHME; ANGELETTI P IST RICHERCHE BIO; MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO 摘要:Compounds of formula I that are used 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 infection and for inhibiting HCV viral replication and /or viral production in a cell-based system.
专利号:US-3869456-A 优先权日:1972-03-13 标 题 :Synthesis of 5-pyrimidinecarbinols 发明人:TAYLOR HAROLD M; DAVENPORT JAMES D; HACKLER RONALD E 权利人:LILLY CO ELI 摘要:There is disclosed an improved method of synthesizing 5pyrimidinecarbinols by the addition of an alkyllithium to a mixture of 5-halopyrimidine and a ketone at a low temperature. The product compounds are useful as plant fungicides and as plant growth regulators.
专利号:US-4835280-A 优先权日:1985-01-18 标 题 :Indoline compounds for synthesis of pharmaceutically active pyrrolobenzimidazoles 发明人:MARTENS ALFRED; HOELCK JENS-PETER; BERGER HERBERT; MUELLER-BECKMAN BERND; STREIN KLAUS; ROESCH EGON 权利人:BOEHRINGER MANNHEIM GMBH 摘要:The present invention provides Indolines of the formula: (II) (III) ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: (I) These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
专利号:US-7161024-B2 优先权日:2003-07-10 标题 :Process for the preparation and purification of 2-(alkoxyalkylidene)-3-ketoalkanoic acid esters from 3-ketoalkanoic acid esters 发明人:DRAPER RICHARD W 权利人:SCHERING CORP 摘要:In its several embodiments, this invention discloses a novel process to prepare the compounds of Formula 3: n nwherein R 1 is lower alkyl, and R 2 and R 3 can be the same or different, each being independently selected from the group consisting of alkyl, aryl and aralkyl; said process being carried out in a suitable solvent with at least one tert-amine carboxylate salt catalyst. The compounds of formula 3 are chemical intermediates useful for the synthesis of various heterocyclic compounds. These heterocyclic compounds are in turn useful precursors for diverse pharmaceutical, herbicidal and insecticidal agents. In particular, these intermediates are useful precursors to a variety of CCR5 inhibitors.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2010004245-A1 优先权日:2006-10-20 标 题:Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:OBALLA RENATA M; DESCHENES DENIS; GAGNON MARC; LEBLANC YVES; POWELL DAVID; RAMTOHUL YEEMAN K 权利人:MERCK FROSST CANADA LTD 摘要:Azacycloalkane 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, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.