CN Patent

CN103467575B — 一种帕西瑞肽的制备方法

Assigned to Hybio Pharmaceutical Co Ltd · Expires 2016-03-02 · 10y expired

What this patent protects

本发明属于药物化学领域，尤其涉及一种帕西瑞肽的制备方法。本发明所述制备方法通过改变片段偶联顺序得到H-Phg-DTrp(Boc)-Lys(Boc)-Tyr(4-Bzl)-Phe-(4-Boc-NH-C 2 H 4 -NH-CO-O)Pro-OH，再进行液相环化、裂解得到目标产物帕西瑞肽粗品，纯化得到帕西瑞肽纯品。与现有技术相比，本发明所述制备方法液相环化时羧基的活化是Pro，相比羧基端Phe的消旋大大降低，HPLC未检测到消旋，从而提高帕西瑞肽纯品收率，适合于大规模产业化生产。

USPTO Abstract

本发明属于药物化学领域，尤其涉及一种帕西瑞肽的制备方法。本发明所述制备方法通过改变片段偶联顺序得到H-Phg-DTrp(Boc)-Lys(Boc)-Tyr(4-Bzl)-Phe-(4-Boc-NH-C 2 H 4 -NH-CO-O)Pro-OH，再进行液相环化、裂解得到目标产物帕西瑞肽粗品，纯化得到帕西瑞肽纯品。与现有技术相比，本发明所述制备方法液相环化时羧基的活化是Pro，相比羧基端Phe的消旋大大降低，HPLC未检测到消旋，从而提高帕西瑞肽纯品收率，适合于大规模产业化生产。

Drugs covered by this patent

pasireotide-pamoate (PASIREOTIDE PAMOATE)

Patent Metadata

Patent number: CN103467575B
Jurisdiction: CN
Classification: —
Expires: 2016-03-02
Drug substance claim: No
Drug product claim: No
Assignee: Hybio Pharmaceutical Co Ltd
Source: FDA Orange Book + USPTO grounding via Google Patents

Bibliographic data sourced from FDA Orange Book + USPTO public records. Plain-English summary generated by AI grounded in source text. Patent term extensions (PTR, SPC, pediatric) may shift the effective expiry. Not legal advice.

Track this patent

Get a daily-checked alert when vulnerability score, expiry, classification, or assignee changes. Email, Slack, or Teams delivery. Pro: 50 watches, Free: 3.