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-9663511-B2 优先权日:2012-03-26 标题:Sphingosine 1-phosphate receptor antagonists 发明人:SWENSON ROLF E 权利人:ARROYO BIOSCIENCES LLC 摘要:The present invention relates to sphingosine-1-phosphate (S1P) receptors and compounds of the general formula: n nthat are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1-phosphate receptor 2 (S1P 2 ) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1P 2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1P 2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers.
专利号:RU-2194701-C2 优先权日:1995-12-18 标 题 :Derivatives of quinazoline, methods of their synthesis, pharmaceutical composition comprising thereof and method of achievement of anti-angiogenic effect and/or effect of decrease of vascular penetration with their using
参考文献:10.1021/cg501783d 摘要:Mei L, Wang C, Wang L, Zhao Y, Chai Z, Shi W. Halogen Bonded Three-Dimensional Uranyl–Organic Compounds with Unprecedented Halogen–Halogen Interactions and Structure Diversity upon Variation of Halogen Substitution. Crystal Growth & Design. 2015 Feb 20;15(3):1395–406. doi: 10.1021/cg501783d.