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Fragment synthesis of cyclic peptides

A suitable and compound technology, applied in the field of cyclic amino acid molecules and their preparation, can solve the problems of poor stability and low bioavailability

Pending Publication Date: 2018-12-21
ZEALAND PHARM AS +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the great therapeutic potential of peptides is not always easy to realize due to their low bioavailability
This disadvantage is due to the degradation of the peptide by endo- and exo-peptidases, which leads to poor stability of the peptide in vivo

Method used

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  • Fragment synthesis of cyclic peptides
  • Fragment synthesis of cyclic peptides
  • Fragment synthesis of cyclic peptides

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0121] Fragment Preparation—General Synthetic Protocol

[0122]

[0123] for which R 3 , R 4 , R 5 and R 6 = H case

[0124] R 5 and R 6 = H but R 3 or R 4 When one of ≠H, a further scheme is adopted.

[0125]

[0126] Fragment Preparation

[0127]

[0128] Reaction Molarity: 0.15M

[0129] In CH 2 Cl 2 (200 mL) was cooled to 0 °C. Then DIPEA (16.04 mL, 92.1 mmol) was slowly added to the stirred mixture. The cooling bath was removed and the reaction was stirred at room temperature (rt) for 16 hours. A solution of 10% HCl (100 mL) was added resulting in the formation of a precipitate which was removed by filtration. The filtrate was washed with 10% HCl (3 x 100 mL) and brine (2 x 100 mL). Then the organic phase was washed with Na 2 SO 4 dry. The solvent was removed under reduced pressure to obtain crude compound 1 (10.5 g, 29.6 mmol, 97% yield), which was used in the next reaction without purification.

[0130]

[0131] Reaction molar concentra...

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Abstract

There is described herein use of a compound of formula (I) below to make cyclic peptides.

Description

[0001] related application [0002] This application claims priority to U.S. Provisional Application No. 62 / 254003, filed November 11, 2015, which is hereby incorporated by reference in its entirety. technical field [0003] The present invention relates to cyclic amino acid molecule and its preparation method. Background technique [0004] Peptides play important roles by mediating a wide range of biological processes, acting as hormones, antibiotics and signaling molecules. Peptides have been widely used in medicine due to their highly specific interactions with their biological targets. However, the great therapeutic potential of peptides is not always easy to realize due to their low bioavailability. This disadvantage is caused by the degradation of the peptide by endo- and exo-peptidases, which leads to poor stability of the peptide in vivo. Cyclic peptides are more resistant to degradation than their linear counterparts. There are two main reasons for this stabilit...

Claims

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Application Information

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IPC IPC(8): C07D207/16C07C223/02C07C237/06C07C259/06C07C271/18C07C271/22C07D487/04C07K1/04C07K1/06C07K7/06
CPCC07C271/18C07C271/22C07D207/16C07C2603/18C07D487/04C07K7/56C07K1/1075A61P1/00A61P1/04A61P1/14A61P1/16A61P1/18A61P11/02A61P11/06A61P11/08A61P15/14A61P19/02A61P19/10A61P25/00A61P25/04A61P25/24A61P25/28A61P29/00A61P3/04A61P31/12A61P31/14A61P31/18A61P31/20A61P35/00A61P3/10A61P37/06A61P7/00A61P7/04Y02P20/55C07K7/06C07K7/64A61K38/00A61K9/0014A61K9/0053C07K7/54
Inventor 曼努埃尔·佩雷斯·巴斯克斯M·曼苏尔·穆尔希德珍妮弗·L·希基马克-安德·普帕特杨高强詹姆斯·吉尔拉德阿达姆·保罗·卡法尔安德鲁·L·拉夫顿
Owner ZEALAND PHARM AS
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