公开(公告)号：US20110263693A1

公开(公告)日：2011-10-27

申请号：US12294507

申请日：2007-03-30

申请人： Haley Vinson-Hieronymus ,  Todd R. Golub ,  Justin Lamb ,  Kimberly Stegmaier

发明人： Haley Vinson-Hieronymus ,  Todd R. Golub ,  Justin Lamb ,  Kimberly Stegmaier

IPC分类号： A61K31/352 ,  A61K31/225 ,  A61K31/19 ,  A61P35/00 ,  C07D311/78 ,  C07C69/604 ,  C07C63/44 ,  A61P35/02 ,  C12N5/09 ,  C07D493/04

CPC分类号： A61K31/203

摘要： Based on the discovery that celastrol and gedunin are Hsp90 inhibitors, the present invention provides novel inhibitors of Hsp90. and pharmaceutically acceptable salts, derivatives, and compositions thereof. The invention provides two classes of compounds. One class includes celastrol and its derivatives. The other class includes gedunin and its derivatives. The present invention further provides methods for treating disorders wherein Hsρ90 inhibition is desired (e.g., proliferative diseases, cancer, inflammatory diseases, fungal infections, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. Celastrol, gedunin, and derivatives thereof are particularly useful in the treatment of prostate cancer, breast cancer, ovarian cancer, lung cancer, and leukemia.

摘要翻译： 基于发现celastrol和gedunin是Hsp90抑制剂，本发明提供了新型的Hsp90抑制剂。 及其药学上可接受的盐，衍生物和组合物。 本发明提供了两类化合物。 一类包括celastrol及其衍生物。 另一类包括gedunin及其衍生物。 本发明进一步提供了治疗其中需要抑制Hs＆gt; 90抑制（例如增殖性疾病，癌症，炎性疾病，真菌感染等）的疾病的方法，包括向有需要的受试者施用治疗有效量的本发明化合物。 Celastrol，gedunin及其衍生物特别可用于治疗前列腺癌，乳腺癌，卵巢癌，肺癌和白血病。