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参考文献:Synthesis,Sar,And X-Ray Structure Of Novel Potent Dppiv Inhibitors: Oxadiazolyl Ketones
标题:Synthesis,Sar,And X-Ray Structure Of Novel Potent Dppiv Inhibitors: Oxadiazolyl Ketones
摘要:Synthesis Of A Novel Series Of Dppiv Inhibitors With 1,2,4-And 1,3,4-Oxadiazolyl Ketone Derivatives And Its Structure-Activity Relationships Are Discussed. Compound 18H Showed Good Inhibitory Activity Against Dppiv And Favorable Pharmacokinetic Properties. In Vivo Pharmacodynamic Efficacy And Co-Crystal Structure Of Compound 18H With Dppiv Is Also Described. (C) 2007 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2007.05.046

专利信息

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-2021261583-A1
优先权日:2018-06-14
标 题:Synthetic Cytotoxic Molecules, Drugs, Methods of Their Synthesis and Methods of Treatment
发明人：EDINGER AIMEE; HANESSIAN STEPHEN
权利人:UNIV CALIFORNIA; UNIV MONTREAL
摘要:Small molecules compounds and methods of their synthesis are provided. Formulations and medicaments are also provided that are directed to the treatment of disease, such as, for example, neoplasms, cancers, and other diseases. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.

专利号:CA-3103805-A1
优先权日:2018-06-14
标 题:Synthetic cytotoxic molecules, drugs, methods of their synthesis and methods of treatment