6-Chloro-Pyridazine-3-Carbonyl Chloride置于吡啶,氨,三乙胺,三氟乙酸酐体系中,用 二氯甲烷 用作溶剂,化学反应 2.5H,反应生成3-氰基-6-氯哒嗪 参考文献:Discovery Of Potent,Selective,Orally Bioavailable Stearoyl-Coa Desaturase 1 Inhibitors 标题:Discovery Of Potent,Selective,Orally Bioavailable Stearoyl-Coa Desaturase 1 Inhibitors 摘要:Stearoyl-Coa Desaturase 1 (Scd1) Catalyzes The Committed Step In The Biosynthesis Of Monounsaturated Fatty Acids From Saturated,Long-Chain Fatty Acids. Studies With Scd1 Knockout Mice Have Established That These Animals Are Lean And Protected From Leptin Deficiency-Induced And Diet-Induced Obesity,With Greater Whole Body Insulin Sensitivity Than Wild-Type Animals. In This Work,We Have Discovered A Series Of Potent,Selective,Orally Bioavailable Scd1 Inhibitors Based On A Known Pyridazine Carboxamide Template. The Representative Lead Inhibitor 28C Also Demonstrates Excellent Cellular Activity In Blocking The Conversion Of Saturated Long-Chain Fatty Acid-Coas (Lcfa-Coas) To Monounsaturated Lcfa-Coas In Hepg2 Cells. Doi:10.1021/jm070219P
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-8138188-B2 优先权日:2006-02-23 标题 :Melanocortin type 4 receptor agonist piperidinoylpyrrolidines 发明人:ANDREWS MARK DAVID; BROWN ALAN DANIEL; LANSDELL MARK IAN; SUMMERHILL NICHOLAS WILLIAM 权利人:ANDREWS MARK DAVID; BROWN ALAN DANIEL; LANSDELL MARK IAN; SUMMERHILL NICHOLAS WILLIAM; PFIZER 摘要:The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) n nwherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
参考文献:10.1177/1087057116635503 摘要:Voter AF, Manthei KA, Keck JL. A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. J Biomol Screen. 2016 Jul;21(6):626–33.