CAS: 676559-83-4; Abt-279

📜Tert-Butyl 2-(4-(2-((2S,5R)-2-Cyano-5-Ethynylpyrrolidin-1-yl)-2-Oxoethylamino)-4-Methylpiperidin-1-yl)Isonicotinate (2S,3S)-2,3-Dihydroxysuccinate置于磷酸,水体系中,化学反应 16.0H,以91%的收率获得产物abt 279; 2-[4-[[2-[(2S,5R)-2-氰基-5-乙炔基-1-吡咯烷基]-2-氧代乙基]氨基]-4-甲基-1-哌啶基]-4-吡啶羧酸
参考文献:Wo2008/11499
标题:Wo2008/11499

专利信息

专利号:WO-2011047481-A1
优先权日:2009-10-23
标题 :Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：FORTIN REJEAN; LACHANCE NICOLAS; LI CHUN SING; TRANMER GEOFFREY
权利人:MERCK FROSST CANADA LTD; FORTIN REJEAN; LACHANCE NICOLAS; LI CHUN SING; TRANMER GEOFFREY
摘要:Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl- coenzyme. A delta-9 desaturase (SCDl) 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. Formula (I).

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.

专利号:US-2010120784-A1
优先权日:2007-04-20
标题 :Novel heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILPPE; RAMTOHUL YEEMAN K
权利人:LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILPPE; RAMTOHUL YEEMAN K
摘要:Heteroaromatic compounds of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein W is a substituted heteroaryl, X and Y are each independently a bond, —O—, —S—, —S(O)—, —S(O) 2 —, —NR 6 —, —C(O)—, —C(CH 3 )(OH)— or —C(CH 3 )â• CH—, u (I) is an integer from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) 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, Type 2 diabetes, insulin resistance, hyperglycemia, Metabolic Syndrome, neurological disease, cancer, and liver steatosis

专利号:US-8455479-B2
优先权日:2008-01-24
标 题 :Heterocyclic compounds
发明人：JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; SINGH NISHAN; NANDA GURMEET KAUR; MAGADI SITARAM KUMAR; SHARMA SUDHIR KUMAR
权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; SINGH NISHAN; NANDA GURMEET KAUR; MAGADI SITARAM KUMAR; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD
摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).

专利号:US-2008058528-A1
优先权日:2006-07-20
标题 :Synthesis of (2S,5R)-5-ethynyl-1-{N-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile

专利号:US-9168248-B2
优先权日:2009-02-17
标 题:Spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase
发明人：LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LI CHUN SING; MORADEI OSCAR MIGUEL
权利人:LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LI CHUN SING; MORADEI OSCAR MIGUEL; MERCK CANADA INC
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, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.