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参考文献:脂肪酶催化α-羟甲基砜的拆分.通过cd光谱的半经验计算确定绝对构型并通过x射线结构分析进行验证
标题:脂肪酶催化α-羟甲基砜的拆分.通过cd光谱的半经验计算确定绝对构型并通过x射线结构分析进行验证
摘要:的南极假丝酵母脂肪酶催化的羟甲基砜的酯化和导致的分离(92%ee)和图1B(>=99%ee)的,分别.该酰氧甲基砜(ee>=99%)是由南极假丝酵母脂肪酶催化水解得到的.在甲基取代的醇和苄基取代的醇的酯化反应中,不仅南极念珠菌脂肪酶,洋葱假单胞菌脂肪酶也显示出相反的对映体分化.和1B的绝对配置通过测量它们的圆二色性和通过半经验方法计算1A和1B的cd光谱来确定.通过1B和的x射线结构分析验证了构型分配.
DOI:10.1016/s0957-4166(97)00377-7
专利信息
专利号:US-2003187027-A1
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
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 n n and 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 (1) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p.
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.