欧盟法规
C&L通报REACH预注册专利信息
专利号:US-9982005-B2
优先权日:2013-04-04
标 题 :Macrolides and methods of their preparation and use
发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:US-9771356-B2
优先权日:2012-09-21
标题 :Inhibitors of beta-hydroxylase for treatment of cancer
发明人:WANDS JACK R; DE LA MONTE SUZANNE; AIHARA ARIHIRO; OLSEN MARK JON; THOMAS JOHN-MICHAEL
权利人:RHODE ISLAND HOSPITAL; UNIV MIDWESTERN
摘要:The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydroxylase (e.g., Asparatyl (asparaginyl) β-hydroxylase (ASPH)), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.
专利号:US-8470889-B2
优先权日:2008-11-26
标题:Hybrid-ionone and curcumin molecules as anticancer agents
发明人:Wu jian hui; BATIST GERALD; ZHOU JINMING; GENG GUOYAN; LIN RONGTUAN; LI YI
权利人:Wu jian hui; BATIST GERALD; ZHOU JINMING; GENG GUOYAN; LIN RONGTUAN; LI YI; TRT PHARMA INC
摘要:The present invention relates to the synthesis of a series of ionone and curcumin derivatives as multi-targeting agents effective against both hormone-sensitive and hormone-independent cancers. In particular, the present invention is directed to a distinct class of bifunctional antiandrogens, which inhibit both AR and IKBkinases (IKK). A series of ionone-based chalcones were synthesized and their in vitro cytotoxicity against prostate cancer cell lines were demonstrated. A series of derivatives formed by reacting ionone-based chalcones and hydrazines demonstrate substantial antiproliferative activities in prostate cancer, breast cancer and lung cancer cell lines.
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.