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    • 4. 发明授权
    • Modified peptides as therapeutic agents
    • 修饰肽作为治疗剂
    • US07166707B2
    • 2007-01-23
    • US10609217
    • 2003-06-27
    • Ulrich Feige
    • Ulrich Feige
    • C07K1/00
    • C12N9/6491A61K38/00C07K14/505C07K14/52C07K14/524C07K14/525C07K14/545C07K14/8146C07K2319/00C07K2319/30
    • The present invention concerns fusion of Fc domains with biologically active peptides and a process for preparing pharmaceutical agents using biologically active peptides. In this invention, pharmacologically active compounds are prepared by a process comprising: a) selecting at least one peptide that modulates the activity of a protein of interest; and b) preparing a pharmacologic agent comprising an Fc domain covalently linked to at least one amino acid of the selected peptide. Linkage to the vehicle increases the half-life of the peptide, which otherwise would be quickly degraded in vivo. The preferred vehicle is an Fc domain. The peptide is preferably selected by phage display, E. coli display, ribosome display, RNA-peptide screening, or chemical-peptide screening.
    • 本发明涉及Fc结构域与生物活性肽的融合以及使用生物活性肽制备药物的方法。 在本发明中,药理活性化合物通过以下方法制备,该方法包括:a)选择至少一种调节目的蛋白质活性的肽; 和b)制备包含与选定肽的至少一个氨基酸共价连接的Fc结构域的药理学试剂。 与载体的连接增加了肽的半衰期,否则其将在体内迅速降解。 优选的载体是Fc结构域。 优选通过噬菌体展示,大肠杆菌展示,核糖体展示,RNA-肽筛选或化学 - 肽筛选来选择肽。
    • 7. 发明授权
    • Use of carbazones as novel active ingredients in medicaments
    • 使用CARBAZONES作为药物中的新型活性成分
    • US5177091A
    • 1993-01-05
    • US795210
    • 1991-11-20
    • Ulrich FeigeIrmgard WiesenbergLeo WidlerPier G. FerriniMartin Missbach
    • Ulrich FeigeIrmgard WiesenbergLeo WidlerPier G. FerriniMartin Missbach
    • A61K31/425A61K31/426A61P29/00C07D277/20C07D277/38
    • A61K31/425
    • Compounds of formula I ##STR1## wherein X and Y are each independently of the other thio or sulfynyl, R.sub.1 is lower alk-2-en-1-yl, lower alk-3-en-2-yl, lower alk-2--yn-1-yl, or lower alkyl that is substituted in the 2,3-position by radicals that can be eliminated to form a double bond, R.sub.2 is hydrogen and R.sub.3 is unsubstituted methyl or methyl substituted by a radical that can be eliminated together with hydrogen Rhd 2 to form a double bond, or R.sub.2 and R.sub.3 are each hydrogen or lower alkyl or together are methylene, R.sub.4 is free or protected hydroxy, or hydrogen, and R.sub.5 is hydrogen, lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, or lower alkyl that is substituted in the 2,3-position by radicals that can be eliminated to form a double bond, and their pharmaceutically acceptable salts may be used in a novel manner for the treatment of disorders of the rheumatoid type.
    • 式I的化合物其中X和Y各自独立地为其它硫代或亚硫炔基,R 1为低级烷-2-烯-1-基,低级烯-3-烯-2-基,低级烷基 -2-yn-1-基或在2,3位被可以被去除以形成双键的基团取代的低级烷基,R 2是氢,R 3是未被取代的甲基或被以下基团取代的甲基: 可以与氢Rhd 2一起消除以形成双键,或者R 2和R 3各自为氢或低级烷基或一起为亚甲基,R 4为游离或被保护的羟基或氢,R 5为氢,低级烷基,低级烷基, 2-烯-1-基,低级烷-2-炔-1-基或在2,3位被可以被去除以形成双键的自由基取代的低级烷基,及其药学上可接受的盐可以 以新颖的方式用于治疗类风湿病的病症。