Eg5 co-crystals
    102.
    发明授权
    Eg5 co-crystals 失效
    Eg5共晶体

    公开(公告)号:US07662581B1

    公开(公告)日:2010-02-16

    申请号:US11018091

    申请日:2004-12-20

    摘要: This invention provides methods of identifying an Eg5 binding ligand. The ligand is identified by using the atomic coordinates of an Eg5 crystal to generate a three dimensional structure. The three dimensional structure is used in molecular modeling techniques and docking experiments to identify ligands that bind to the binding pocket of Eg5. A novel binding pocket is identified. The invention also provides a crystallized Eg5 and ligand complex.

    摘要翻译: 本发明提供鉴定Eg5结合配体的方法。 通过使用Eg5晶体的原子坐标来鉴定配体以产生三维结构。 三维结构用于分子建模技术和对接实验以鉴定结合Eg5的结合口袋的配体。 识别出新的装订口袋。 本发明还提供了结晶的Eg5和配体络合物。

    Semi-synthetic glycopeptides with antibiotic activity
    104.
    发明授权
    Semi-synthetic glycopeptides with antibiotic activity 失效
    具有抗菌活性的半合成糖肽

    公开(公告)号:US07632918B2

    公开(公告)日:2009-12-15

    申请号:US11361852

    申请日:2006-02-24

    IPC分类号: A61K38/14

    CPC分类号: A61K38/14 C07K9/008

    摘要: Semi-synthetic glycopeptides having antibacterial activity are based on modifications of the eremomycin, A82846B, vancomycin, teicoplanin, and A-40,926 scaffolds, in particular, acylation of the sugar moieties on these scaffolds with certain acyl groups; and/or conversion of an acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides; or having a combination of an alkylation modification of the amino substituent on the amino-substituted sugar moiety on these scaffolds with certain alkyl groups or acylation modification of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain alkyl groups, and conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

    摘要翻译: 具有抗菌活性的半合成糖肽基于依依霉素,A82846B,万古霉素,替考拉宁和A-40,926支架的修饰,特别是在具有某些酰基的这些支架上糖部分的酰化; 和/或将这些支架的大环上的酸部分转化为某些取代的酰胺; 或具有这些支架上的氨基取代的糖部分上的氨基取代基的烷基化修饰与某些烷基的组合或在该支架上的某些烷基上的氨基取代的糖部分上的氨基取代基的酰化修饰和转化 的该支架的大环上的酸部分与某些取代的酰胺。 还提供了合成化合物的方法,含有该化合物的药物组合物,以及该化合物用于治疗和/或预防疾病,特别是细菌感染的方法。

    Human cyclin-dependent kinase (hPNQALRE)
    109.
    发明授权
    Human cyclin-dependent kinase (hPNQALRE) 失效
    人细胞周期蛋白依赖性激酶(hPNQALRE)

    公开(公告)号:US07566559B2

    公开(公告)日:2009-07-28

    申请号:US11774306

    申请日:2007-07-06

    CPC分类号: C12N9/1205 C07K2319/00

    摘要: A human gene encoding a novel cyclin-dependent kinase termed hPNQALRE and its expression products can be used to provide reagents and methods for detecting neoplasia. Compositions and methods for treating proliferative disorders and neoplasia are also provided.

    摘要翻译: 编码称为hPNQALRE的新型细胞周期蛋白依赖性激酶及其表达产物的人基因可用于提供检测肿瘤的试剂和方法。 还提供了治疗增殖性疾病和瘤形成的组合物和方法。

    Methods and compositions for the treatment of peripheral artery disease

    公开(公告)号:US07541337B2

    公开(公告)日:2009-06-02

    申请号:US11671382

    申请日:2007-02-05

    摘要: Compositions and methods for treating peripheral artery disease in a patient are provided. Compositions comprise recombinant fibroblast growth factor-2. Fibroblast growth factor, such as FGF-2, is administered in therapeutically effective amounts to treat or prevent peripheral artery disease including claudication and critical limb ischemia. Pharmaceutical compositions comprising a therapeutically effective amount of FGF-2 and a pharmaceutically acceptable carrier are also provided. The methods of the invention to treat peripheral artery disease and claudication comprise administering at least a single dose of a pharmaceutical composition comprising the FGF, such as FGF-2, via intra-arterial, intravenous, or intramuscular infusion to the patient. It is recognized that increased benefits may result from multiple dosing, including intermittent dosing.