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karushitonin derivative

机译:卡鲁什和内德莉

摘要

PURPOSE:To obtain a new calcitonin derivative as a new and useful peptide, having a specific amino acid sequence, exhibiting excellent serum calcium level- lowering activity, thus useful for e.g. treating osteoporosis, hypercalcemia, Paget' s disease, etc. CONSTITUTION:A new calcitonin derivative having excellent serum calcium level-lowering activity, thus useful for e.g. treating osteoporosis, hypercalcemia or Paget's disease, etc., and consisting of a peptide expressed by formula I ((a), (b), (c), (d) and (e) each is 1 or 2, their total is 6). This new peptide is obtained by the following processes: using a peptide synthesizer, protected amino acids are bound successively to a carrier such as a p-methylbenzhydrylamine(MBHA)resin by solid phase synthesis to synthesize a peptide resin of formula II (Cl-Z is o-chlorobenzyloxycarbonyl; Bzl is benzyl; Cl2Bzl is 2,6-dichlobenzyl) followed by binding a peptide of formula III to this resin, and then deprotection and release from the resin.
机译:用途:为了获得新的降钙素衍生物,作为一种新的有用的肽,具有特定的氨基酸序列,表现出优异的降低血清钙水平的活性,因此可用于例如组成:一种新的降钙素衍生物,具有出色的降低血清钙水平的活性,因此可用于治疗例如骨质疏松,高钙血症,佩吉特氏病等。治疗骨质疏松症,高钙血症或佩吉特氏病等,由式I((a),(b),(c),(d)和(e)表示的肽组成,分别为1或2,共6个)。通过以下方法获得该新肽:使用肽合成仪,通过固相合成将受保护的氨基酸相继结合至载体,例如对甲基苯甲酰氨基胺(MBHA)树脂,从而合成式II(C1-Z)的肽树脂式中,O 2是邻氯苄氧基羰基; Bz1是苄基; Cl 2 Bzl是2,6-二氯苄基),然后将式III的肽结合到该树脂上,然后脱保护并从树脂上释放。

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