公开(公告)号：US06555677B2

公开(公告)日：2003-04-29

申请号：US10002061

申请日：2001-10-22

申请人： Daniel E. Petrillo ,  Steven A. Weissman ,  Shouichi Hiraga ,  Nobuya Satake ,  Kai Rossen

发明人： Daniel E. Petrillo ,  Steven A. Weissman ,  Shouichi Hiraga ,  Nobuya Satake ,  Kai Rossen

IPC分类号： C07H1900

CPC分类号： C07H19/23 ,  C07H17/02

摘要： The present invention relates to a novel glycosidation process to make intermediates useful in the preparation of indolopyrrolocarbazole derivatives which inhibit the growth of tumor cells and are therefore useful in the treatment of cancer in mammals, and the like.

公开(公告)号：US06642237B1

公开(公告)日：2003-11-04

申请号：US09718223

申请日：2000-11-21

申请人： James R. Tata ,  Kevin T. Chapman ,  Joseph Leslie Duffy ,  Nancy J. Kevin ,  Yuan Cheng ,  Thomas A. Rano ,  Fengqi Zhang ,  Tracy Huening ,  Brian Anthony Kirk ,  Zhijian Lu ,  Subharekha Raghavan ,  Fred J. Fleitz ,  Daniel E. Petrillo ,  Joseph D. Armstrong, III ,  Richard J. Varsolona ,  David Askin ,  R. Scott Hoerrner ,  Robert Purick

发明人： James R. Tata ,  Kevin T. Chapman ,  Joseph Leslie Duffy ,  Nancy J. Kevin ,  Yuan Cheng ,  Thomas A. Rano ,  Fengqi Zhang ,  Tracy Huening ,  Brian Anthony Kirk ,  Zhijian Lu ,  Subharekha Raghavan ,  Fred J. Fleitz ,  Daniel E. Petrillo ,  Joseph D. Armstrong, III ,  Richard J. Varsolona ,  David Askin ,  R. Scott Hoerrner ,  Robert Purick

IPC分类号： C07D491048

CPC分类号： C07D401/06 ,  A61K31/00 ,  A61K45/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07D495/04 ,  A61K2300/00

摘要： &ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

摘要翻译： γ-羟基-2-（氟烷基氨基羰基）-1-哌嗪戊酰胺化合物是HIV蛋白酶和HIV复制抑制剂的抑制剂。 这些化合物可用于预防或治疗HV的感染和治疗AIDS，无论是化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。 这些化合物对HIV病毒突变体有效，其对目前用于治疗AIDS和HIV感染的HIV蛋白酶抑制剂具有抗性。