专利号:US-8754237-B2 优先权日:2006-02-14 标题:Bifunctional histone deacetylase inhibitors 发明人:BRADNER JAMES ELLIOT; MAZITSCHEK RALPH; TANG WEIPING; SCHREIBER STUART L 权利人:BRADNER JAMES ELLIOT; MAZITSCHEK RALPH; TANG WEIPING; SCHREIBER STUART L; HARVARD COLLEGE; DANA FARBER CANCER INST INC 摘要:In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
专利号:US-8304451-B2 优先权日:2006-05-03 标题 :Histone deacetylase and tubulin deacetylase inhibitors 发明人:MAZITSCHEK RALPH; KWIATKOWSKI NICHOLAS PAUL; BRADNER JAMES ELLIOT 权利人:MAZITSCHEK RALPH; KWIATKOWSKI NICHOLAS PAUL; BRADNER JAMES ELLIOT; HARVARD COLLEGE; DANA FARBER CANCER INST INC 摘要:In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel inhibitors of histone deacetylases, tubulin deacetylases, and/or aggresome inhibitors, and pharmaceutically acceptable salts and derivatives thereof. The inventive compounds fall into two classes—“isotubacinâ€? class and “isoisotubacinâ€? class—all of which include a 1,3-dioxane core. The present invention further provides methods for treating disorders regulated by histone deacetylase activity, tubulin deacetylase activity, and/or the aggresome (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, protein degradation disorders, protein deposition disorders, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
专利号:US-8178579-B2 优先权日:2001-05-09 标 题:Dioxanes and uses thereof 发明人:SCHREIBER STUART L; STERNSON SCOTT M; WONG JASON C; GROZINGER CHRISTINA M; HAGGARTY STEPHEN J; KOELLER KATHRYN M 权利人:SCHREIBER STUART L; STERNSON SCOTT M; WONG JASON C; GROZINGER CHRISTINA M; HAGGARTY STEPHEN J; KOELLER KATHRYN M; HARVARD COLLEGE 摘要:In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): n nand pharmaceutically acceptable derivatives thereof, wherein R 1 , R 2 , R 3 , n, X and Y are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The present invention further provides compounds capable of inhibiting histone deacetylatase activity and methods for treating disorders regulated by histone deacetylase activity (e.g., cancer and protozoal infections) comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p. The present invention also provides methods for preparing compounds of the invention.
参考标题:α-Heteroarylation Of Thioethers Via Photoredox And Weak Brønsted Base Catalysis 作者:Edwin Alfonzo,Sudhir M. Hande |发布日期:2021.8.6 摘要:Thioethers To α-Thio Alkyl Radicals And Their Addition To N-Methoxyheteroarenium Salts For The Redox-Neutral Synthesis Of α-Heteroaromatic Thioethers. Studies Are Consistent With A Two-Step Activation Mechanism, Where Oxidation Of Thioethers To Sulfide Radical Cations By A Photoredox Catalyst Is Followed By α-C-H Deprotonation By A Weak Brønsted Base Catalyst To Afford α-Thio Alkyl Radicals. Further,
合成参考文献
参考文献:10.1055/a-1731-3852 摘要:Tang Y, Yu B. A Mild Heteroatom (O-, N-, and S-) Methylation Protocol Using Trimethyl Phosphate (TMP)–Ca(OH)2Combination. Synthesis. 2022 Mar 03;54(10):2373–90. doi: 10.1055/a-1731-3852.