首页> 外国专利> SHORT-CHAIN PEPTIDES AS PARATHYROID HORMONE (PTH) RECEPTOR AGONIST.

SHORT-CHAIN PEPTIDES AS PARATHYROID HORMONE (PTH) RECEPTOR AGONIST.

机译:短链肽作为副甲状腺激素(PTH)受体激动剂。

摘要

The present invention provides novel short-chain peptides, which primarily act as parathyroid hormone (PTH/ PTH-I) receptor agonist. These short-chain peptides exhibit increased stability to proteolytic cleavage. Most of short-chain peptides were found to be stable in rat plasma upto 24 hours (in vitro), showed increased stability against GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes (in vitro). Due to increased metabolic stability, other than parenteral route of administration, some of the short-chain peptides can also be delivered by oral routes of administration, for the treatment / prevention of hypoparathyroidism and diseases characterized by bone mass reduction, such as osteoporosis, postmenopausal osteoporosis and for stimulating bone repair. A-Z1-Z2-Z3-Z4-Zsub 5-Z6-Z7-Z8-Z9 -Z10-Z11-Z12-Z13-Zs ub14-Z15-B.
机译:本发明提供了新颖的短链肽,其主要充当甲状旁腺激素(PTH / PTH-1)受体激动剂。这些短链肽表现出对蛋白水解切割的增加的稳定性。发现大多数短链肽在大鼠血浆中直至24小时都是稳定的(体外),显示出对GIT酶(如胃蛋白酶和酸性胃液pH)以及对肝微粒体(体外)具有更高的稳定性。由于增加的代谢稳定性,除了肠胃外给药途径外,一些短链肽还可以通过口服给药途径给药,用于治疗/预防甲状旁腺功能低下和以骨量减少为特征的疾病,例如骨质疏松症,绝经后骨质疏松症和刺激骨修复。 A-Z1-Z2-Z3-Z4-Z 5-Z6-Z7-Z8-Z9 -Z10-Z11-Z12-Z13-Z sub 14-Z15-B。

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