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血小板反應素1結合肽
专利权人:
DAIICHI SANKYO COMPANY, LIMITED;PEPTIDREAM INC.
发明人:
YAMAGUCHI, TAKAHIRO,山口孝弘,MORI, YUTAKA,森裕,SAITO, HIRONAO,齐藤博直,齊藤博直,KUBOTA, HIDEKI,洼田秀树,窪田秀樹,FURUKAWA, AKIHIRO,古川诏大,古川詔大,OTSUKA, ERI,大塚绘里,大塚繪里,ISHIGAI, YUTAKA,石贝裕,石貝裕,IJIRI, HIROSHI,井尻宏志,RE
申请号:
TW106131360
公开号:
TW201811817A
申请日:
2017.09.13
申请国别(地区):
TW
年份:
2018
代理人:
摘要:
Provided is a compound which can promote angiogenesis by inhibiting the function of TSP1, and is useful in the treatment or prevention of diseases such as critical limb ischemia. Specifically provided is a macrocyclic polypeptide represented by formula (1) [in the formula: A is selected from among linking groups A1 to A6; Xaa1 is an aliphatic amino acid, aromatic amino acid, basic amino acid, neutral amino acid, or acidic amino acid residue, or is not present; Xaa2 is an aromatic amino acid or neutral amino acid residue; Xaa3 is an aliphatic amino acid, aromatic amino acid, or basic amino acid residue; Xaa4 is Ser, Thr, Ala, or mS; Xaa5 is Gly or Ser; Xaa6 is a basic amino acid or neutral amino acid residue; Xaa7 is a neutral amino acid or acidic amino acid residue; Xaa8 is an aromatic amino acid residue; Xaa9 is an aliphatic amino acid, neutral amino acid, or aromatic amino acid residue; Xaa10 is a basic amino acid, aliphatic amino acid, aromatic amino acid, or neutral amino acid residue; Xaa11 is an aromatic amino acid residue; and Xaa12 is an aliphatic amino acid, aromatic amino acid, or basic amino acid residue], or a pharmacologically acceptable salt thereof.本發明之課題係提供一種化合物,其可藉由抑制TSP1的功能而促進血管生成,且有用於嚴重下肢缺血等之疾病之治療或預防。解決手段為一種式(I)所表示的大環狀多肽或其藥理學上可容許的鹽等,[式中,A係選自連結基A1~A6,Xaa1係脂肪族胺基酸、芳香族胺基酸、鹼性胺基酸、中性胺基酸、或酸性胺基酸之殘基,或不存在;Xaa2係芳香族胺基酸或中性胺基酸之殘基;Xaa3係脂肪族胺基酸、芳香族胺基酸、或鹼性胺基酸之殘基;Xaa4係Ser、Thr、Ala、或mS;Xaa5係Gly或Ser;Xaa6係鹼性胺基酸或中性胺基酸之殘基;Xaa7係中性胺基酸或酸性胺基酸之殘基;Xaa8係芳香族胺基酸殘基;Xaa9係脂肪族胺基酸、中性胺基酸、或芳香族胺基酸之殘基;Xaa10係鹼性胺基酸、脂肪族胺基酸、芳香族胺基酸、或中性胺基酸之殘基;Xaa11係芳香族胺基酸殘基;Xaa12係脂肪族胺基酸、芳香族胺基酸、或鹼性胺基酸之殘基]。
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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