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    • 4. 发明申请
    • C5a RECEPTOR ANTAGONISTS HAVING SUBSTANTIALLY NO AGONIST ACTIVITY
    • C5a受体拮抗剂具有主要的无激素活性
    • WO1995016033A1
    • 1995-06-15
    • PCT/IB1994000359
    • 1994-11-16
    • CIBA-GEIGY AGVAN OOSTRUM, JanBOYAR, William, C.GALAKATOS, Nicholas, G.PEPPARD, Jane, V.
    • CIBA-GEIGY AG
    • C12N15/12
    • C07K14/472A61K38/00C07K16/18C07K2319/00
    • Disclosed are polypeptide analogues of human C5a which are C5a receptor antagonists that exhibit substantially no analphylatoxin or agonist activity, and derivatives of the analogues, and dimeric forms of the analogues or derivatives. DNA molecules encoding the polypeptides and methods of making the analogues are also provided. Pharmaceutical formulations containing a C5a analogue are used therapeutically in the treatment of C5a-mediated diseases and inflammatory conditions in mammals, and prophylactically to prevent or reduce inflammation caused by an event which causes inflammation or aggravates an existing inflammatory condition, respectively. Further disclosed are antibodies specific to the C5a analogues, derivatives thereof, and dimers of the analogues and derivatives which exhibit substantially no cross-reactivity with human C5a. The antibodies are used to detect or quantify circulating C5a analogue or derivative, as well as to modify, e.g., neutralize, the activity of the C5a receptor antagonist in vivo.
    • 公开了人C5a的多肽类似物,其是显示基本上没有分泌毒素或激动剂活性的C5a受体拮抗剂,以及类似物的衍生物和类似物或衍生物的二聚体形式。 还提供了编码多肽的DNA分子和制备类似物的方法。 含有C5a类似物的药物制剂治疗性地用于治疗哺乳动物中C5a介导的疾病和炎性病症,并预防性地预防或减少由引起炎症或加剧现有炎性病症的事件引起的炎症。 进一步公开的是对C5a类似物,其衍生物和类似物和衍生物的二聚体特异的抗体,其表现出与人C5a基本上没有交叉反应性。 所述抗体用于检测或定量循环C5a类似物或衍生物,以及修饰,例如中和体内C5a受体拮抗剂的活性。
    • 6. 发明申请
    • C5a RECEPTOR ANTAGONISTS HAVING SUBSTANTIALLY NO AGONIST ACTIVITY AND METHODS FOR PREPARATION
    • C5a受体拮抗剂具有大量无激素活性及其制备方法
    • WO1996039503A1
    • 1996-12-12
    • PCT/EP1996002422
    • 1996-06-04
    • CIBA-GEIGY AGVAN OOSTRUM, JanVAN HEEKE, GinoSCHMITZ, Albert
    • CIBA-GEIGY AG
    • C12N15/12
    • C07K16/18A61K38/00C07K14/472C07K2319/00
    • Disclosed are polypeptide analogues or derivatives of human C5a which are C5a receptor antagonists that exhibit substantially no analphylatoxin or agonist activity, and derivatives of the analogues, and dimeric forms of the analogues or derivatives. DNA molecules encoding the polypeptides and methods of making the analogues are also provided. Pharmaceutical formulations containing a C5a analogue or derivative, are used therapeutically in the treatment of C5a-mediated diseases and inflammatory conditions in mammals, and prophylactically to prevent or reduce inflammation caused by an event which causes inflammation or aggravates an existing inflammatory condition, respectively. Further disclosed are antibodies specific to the C5a analogues, derivatives thereof, and dimers of the analogues and derivatives which exhibit substantially no cross-reactivity with human C5a. The antibodies are used to detect or quantify circulating C5a analogue or derivative, as well as to modify, e.g., neutralize, the activity of the C5a receptor antagonist in vivo.
    • 公开了人C5a的多肽类似物或衍生物,其是显示基本上没有分泌毒素或激动剂活性的C5a受体拮抗剂,以及类似物的衍生物和类似物或衍生物的二聚体形式。 还提供了编码多肽的DNA分子和制备类似物的方法。 含有C5a类似物或衍生物的药物制剂可用于治疗哺乳动物中C5a介导的疾病和炎性病症,并预防性地预防或减少由引起炎症或加重现有炎性疾病的事件引起的炎症。 进一步公开的是对C5a类似物,其衍生物和类似物和衍生物的二聚体特异的抗体,其表现出与人C5a基本上没有交叉反应性。 所述抗体用于检测或定量循环C5a类似物或衍生物,以及修饰,例如中和体内C5a受体拮抗剂的活性。