专利号:US-8367871-B2 优先权日:2007-03-09 标 题 :Process for production of optically active sulfoxide compound using iron-salan complex catalyst 发明人:KATSUKI TSUTOMU; EGAMI HIROMICHI 权利人:NISSAN CHEMICAL IND LTD; KATSUKI TSUTOMU; EGAMI HIROMICHI 摘要:An optically active sulfoxide compound that is useful as an intermediate for synthesis or an active ingredient of a physiologically active substance such as a pharmaceutical agent is produced at a high optical purity. A process for producing an optically active sulfoxide compound of formula (4) comprises oxidizing a sulfide compound of formula (3) in the presence of an optically active metal complex of formula (1), (1′), (2) or (2′) by using an oxidizing agent. The present invention is also directed to the optically active metal complex.
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.
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