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-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.
专利号:CN-105017160-B 优先权日:2015-06-24 标 题:A kind of pyrimidine EGFRT790M inhibitor and its synthesis method and application
参考文献:10.1104/pp.17.00433 摘要:Wase N, Tu B, Allen JW, Black PN, DiRusso CC. Identification and Metabolite Profiling of Chemical Activators of Lipid Accumulation in Green Algae. Plant Physiol. 2017 Aug;174(4):2146–65.