专利号:US-2009264680-A1 优先权日:2004-07-07 标题:Process for the synthesis and purification of (4-methoxybutyl) (4-trifluoromethylphenyl) methanone 发明人:CASTELLIN ANDREA; GREGORI LUCA; GONZALES TRUEBA GUADALUPE; RUBELLO ALBINO; NICOLE ANDREA 权利人:CASTELLIN ANDREA; GREGORI LUCA; GONZALES TRUEBA GUADALUPE; RUBELLO ALBINO; NICOLE ANDREA 摘要:A process for the preparation of 4-trifluoromethylvalerophenone is described. The process described is a three step process comprising the synthesis of organomagnesium specie, coupling reaction between the organomagnesium specie and trifluoromethylbenzonitrile or trifluoromethylbenzoyl chloride and preferably a purification of the product obtained in suitable reaction conditions. In the process an extraction phase of the final product is not required.
专利号:WO-9700244-A1 优先权日:1995-06-19 标题 :Process for parallel synthesis of a non-peptide library 发明人:FRITZ JAMES E; KALDOR STEPHEN W 权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W 摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
专利号:US-2009118296-A1 优先权日:2005-07-20 标 题:Heteroaromatic Compounds As Inhibitors Of Stearoyl-Coenzyme A Delta-9 Desaturase 发明人:BLACK CAMERON; DESCHENES DENIS; GAGNON MARC; LACHANCE NICOLAS; LEBLANC YVES; LEGER SERGE; LI CHUN SING; OBALLA RENATA M 权利人:MERCK FROSST CANADA LTD 摘要:Heteroaromatic compounds 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; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and fatty liver disease.
专利号:US-5936128-A 优先权日:1993-11-19 标题:5,6-dihydropyrone derivatives as protease inhibitors and antiviral agents 发明人:ELLSWORTH EDMUND LEE; LUNNEY ELIZABETH; TAIT BRADLEY DEAN 权利人:WARNER LAMBERT CO 摘要:The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.
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:US-2011301143-A1 优先权日:2009-02-23 标题 :Heterocyclic derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN 权利人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN 摘要:Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, Câ•?CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds 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, cancer, liver steatosis, and non-alcoholic steatohepatitis.