CAS: 537049-40-4; Rel-N1-(4-((2R,4R,6S)-4-(((4,5-Diphenyloxazol-2-yl)Thio)Methyl)-6-(4-(Hydroxymethyl)Phenyl)-1,3-Dioxan-2-yl)Phenyl)-N8-Hydroxyoctanediamide

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42H44N2O7SC42H44N2O7S

专利信息

专利号:US-11666569-B2
优先权日:2013-10-24
标题 :Treatment of polycystic diseases with an HDAC6 inhibitor
发明人：GRADILONE SERGIO A; LARUSSO NICHOLAS F
权利人:MAYO FOUND MEDICAL EDUCATION & RES; NAT INSTITUTES OF HEALTH NIH U S DEPT OF HEALTH AND HUMAN SERVICES DHHS U S GOVERNMENT
摘要:An HDAC6-specific inhibitor (i.e., a compound of Formula I or II) is shown to reduce the pathogenesis associated with polycystic disease. Administration of an HDAC6-specific inhibitor attenuated many of the symptoms characteristic of polycystic liver disease including cyst formation, cyst growth and cholangiocyte proliferation. Treatment with a HDAC6-specific inhibitor also increased the amount of bile duct acetylated tubulin and β-catenin phosphorylation and/or acetylation while reducing bile duct β-catenin synthesis. These results demonstrate that HDAC6 is overexpressed in cystic cholangiocytes and that its pharmacological inhibition reduces cholangiocyte proliferation and cyst growth.

专利号:US-2008227851-A1
优先权日:2007-03-12
标题 :Laulimalide and laulimalide analogs
发明人：WENDER PAUL A
权利人:WENDER PAUL A
摘要:Novel laulimalide analogs, methods for the treatment of proliferative disease and processes for the synthesis of laulimalide and novel laulimalide analogs are described.

专利号:US-10272065-B2
优先权日:2013-01-14
标题 :Gem-difluorinated C-glycoside compounds as anti-cancer agents
发明人：SLILATY STEVE N
权利人:ADVANOMICS CORP; BENOIT & COTE
摘要:The present document describes a synthesis of a class of gem-difluorinated C-glycoside compounds derived from podophyllotoxin, which may be used, but not exclusively, in oncology for the treatment of cancer. More particularly, the podophyllotoxin gem-difluorinated C-glycoconjugated derivatives display improved conformational and chemical stability, and improved cytotoxicity exhibited against drug-resistant cancer cell lines.

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.