📜3,5-二溴吡啶置于氢化钾,铜,Sodium Hydride体系中,用 N,N-二甲基甲酰胺,异丙醇,Mineral Oil 用作溶剂,化学反应 31.0H,反应生成3-苯甲氧基-5-溴吡啶 参考文献:Structure-activity Studies Of 7-Heteroaryl-3-Azabicyclo[3.3.1]Non-6-Enes: A Novel Class Of Highly Potent Nicotinic Receptor Ligands 标题:Structure-activity Studies Of 7-Heteroaryl-3-Azabicyclo[3.3.1]Non-6-Enes: A Novel Class Of Highly Potent Nicotinic Receptor Ligands 摘要:The Potential For Nicotinic Ligands With Affinity For The Alpha 4 Beta 2 Or Alpha 7 Subtypes To Treat Such Diverse Diseases As Nicotine Addiction,Neuropathic Pain,And Neurodegenerative And Cognitive Disorders Has Been Exhibited Clinically For Several Compounds While Preclinical Activity In Relevant In Vivo Models Has Been Demonstrated For Many More. For Several Therapeutic Programs,We Sought Nicotinic Ligands With Various Combinations Of Affinity And Function Across Both Subtypes,With An Emphasis On Dual Alpha 4 Beta 2-Alpha 7 Ligands,To Explore,The Possibility Of Synergistic Effects. We Report Here The Structure-Activity Relationships (Sar) For A Novel Series Of 7-Heteroaryl-3-Azabicyclo[3.3.1]Non-6-Enes And Characterize Many Of The Analogues For Activity At Multiple Nicotinic Subtypes. Doi:10.1021/jm3011299
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-9744252-B2 优先权日:2011-08-17 标 题:Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi 发明人:BERGER MARKUS; KRUGER MARTIN; LOHRKE JESSICA; REINHARDT MICHAEL; SIEBENEICHER HOLGER 权利人:PIRAMAL IMAGING SA 摘要:The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein IIb/IIIa antagonists for imaging of thrombi.