有效的抗增殖剂SDZ LAP 977在光化性角化病患者的临床概念验证研究中已显示出功效,先前已证明它可以阻断有丝分裂中的细胞周期。在本研究中,我们进一步探讨了作用方式:SDZ LAP 977与微管蛋白上的“秋水仙碱结合位点”结合,从而在体外抑制微管蛋白的聚合。此外,我们建立了结构-活性关系,以用于修饰分子的2,5-二甲氧基苯基部分(“环A”)对体外抗增殖活性的影响。
有效的抗增殖剂SDZ LAP 977在光化性角化病患者的临床概念验证研究中已显示出功效,先前已证明它可以阻断有丝分裂中的细胞周期。在本研究中,我们进一步探讨了作用方式:SDZ LAP 977与微管蛋白上的“秋水仙碱结合位点”结合,从而在体外抑制微管蛋白的聚合。此外,我们建立了结构-活性关系,以用于修饰分子的2,5-二甲氧基苯基部分(“环A”)对体外抗增殖活性的影响。
BENZODIAZEPINONE COMPOUNDS USEFUL IN THE TREATMENT OF SKIN CONDITIONS
申请人:Glick Gary D.
公开号:US20090118244A1
公开(公告)日:2009-05-07
The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.
[EN] BENZODIAZEPINONE COMPOUNDS AND METHODS OF TREATMENT USING SAME<br/>[FR] COMPOSÉS DE BENZODIAZÉPINONE ET MÉTHODES DE TRAITEMENT LES UTILISANT
申请人:UNIV MICHIGAN
公开号:WO2011035124A1
公开(公告)日:2011-03-24
The invention provides 1,4-benzodiazepinone compounds, pharmaceutical compositions, and methods of treating autoimmune disorders, chronic inflammatory disorders, and hyperproliferative disorders. For example, the 1,4-benzodiazepinone compounds and pharmaceutical compositions are contemplated to be useful for treating rheumatoid arthritis, graft-versus-host disease, inflammatory bowel disease, and the like.
BENZODIAZEPINONE COMPOUNDS AND METHODS OF TREATMENT USING SAME
申请人:Glick Gary D.
公开号:US20120232067A1
公开(公告)日:2012-09-13
The invention provides 1,4-benzodiazepinone compounds, pharmaceutical compositions, and methods of treating autoimmune disorders, chronic inflammatory disorders, and hyperproliferative disorders. For example, the 1,4-benzodiazepinone compounds and pharmaceutical compositions are contemplated to be useful for treating rheumatoid arthritis, graft-versus-host disease, inflammatory bowel disease, and the like.