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参考文献:Rational Design Of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity Over The Phosphoinositide 3-Kinase β Isoform
标题:Rational Design Of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity Over The Phosphoinositide 3-Kinase β Isoform
摘要:Of The Four Class I Phosphoinositide 3-Kinase (Pi3K) Isoforms,Pi3K Alpha Has Justly Received The Most Attention For Its Potential In Cancer Therapy. Herein We Report Our Successful Approaches To Achieve Pi3K Alpha Vs Pi3K Beta Selectivity For Two Chemical Series. In The Thienopyrimidine Series Of Inhibitors,We Propose That Select Ligands Achieve Selectivity Derived From A Hydrogen Bonding Interaction With Arg770 Of Pi3K Alpha That Is Not Attained With The Corresponding Lys777 Of Pi3K Beta. In The Benzoxepin Series Of Inhibitors,The Selectivity Observed Can Be Rationalized By The Difference In Electrostatic Potential Between The Two Isoforms In A Given Region Rather Than Any Specific Interaction.
Doi:10.1021/jm2007084
专利信息
专利号:US-2023399302-A1
优先权日:2020-10-29
标题:Process for the preparation of heteroaryl-substituted sulfur(vi) compounds
发明人:LOPCHUK JUSTIN M; SHULTZ ZACHARY P; SCATTOLIN THOMAS
权利人:H LEE MOFFITT CANCER CT & RES
摘要:The present disclosure provides processes for the synthesis of organic compounds, in particular processes for the synthesis of heteroaryl-substituted sulfur(VI) compounds by nucleophilic aromatic substitution.
专利号:WO-2006079916-A1
优先权日:2005-01-26
标 题 :Thieno [2,3-d] pyrimidine compounds as inhibitors of adp-mediated platelets aggregation
发明人:ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; RAHMAN HAYAT; SCHWEITZER BARBARA ANN; TENBRINK RUTH ELIZABETH
权利人:PHARMACIA & UPJOHN CO LLC; ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; RAHMAN HAYAT; SCHWEITZER BARBARA ANN; TENBRINK RUTH ELIZABETH
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I): wherein A1, A2, A3, A4, A5, A6, A7, A8, X4, X6, R2, R4, R5, and R6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.