Patent classifications
C07K7/23
GANIRELIX PRECURSOR AND METHOD FOR PREPARING GANIRELIX ACETATE BY USING THE SAME
Disclosed is a method for preparing ganirelix acetate. The method includes the following steps: respectively replacing Fmoc-HArg(Et).sub.2-OH and Fmoc-D-HArg(Et).sub.2-OH by employing Fmoc-Lys(Boc)-OH and Fmoc-D-Lys(Boc)-OH or Fmoc-Lys(Alloc)-OH and Fmoc-D-Lys(Alloc)-OH; synthesizing a ganirelix precursor I or ganirelix precursor II-peptide resin in advance; and then respectively performing modifications and treatments on side chain amino groups of Lys and D-Lys in the precursor I or the precursor II-peptide resin to obtain ganirelix acetate. The ganirelix acetate synthesized therefrom is high in purity, has few impurities and a relatively low cost, and is suitable for large-scale production.
Methods and compositions related to improving properties of pharmacological agents targeting nervous system
Disclosed are compositions and methods related to improving pharmacological properties of bioactive compounds targeting nervous system.
Methods and compositions related to improving properties of pharmacological agents targeting nervous system
Disclosed are compositions and methods related to improving pharmacological properties of bioactive compounds targeting nervous system.
METHOD FOR MANUFACTURING GANIRELIX
In a method for manufacturing ganirelix, a peptide intermediate A represented by Chemical Formula 19 is obtained, a peptide intermediate B represented by Chemical Formula 21 is obtained, and ganirelix represented by Chemical Formula 13 is obtained through a convergent synthesis of the peptide intermediate A and the peptide intermediate B. Ganirelix can be obtained in high purity and high yield, and the commercial mass-production process therefor is feasible, and also, an economical advantage, that is, the reduction in the production costs compared to conventional technologies, is provided. Furthermore, it is possible to obtain a large quantity of Ganirelix more safely than conventional technologies.
METHOD FOR MANUFACTURING GANIRELIX
In a method for manufacturing ganirelix, a peptide intermediate A represented by Chemical Formula 19 is obtained, a peptide intermediate B represented by Chemical Formula 21 is obtained, and ganirelix represented by Chemical Formula 13 is obtained through a convergent synthesis of the peptide intermediate A and the peptide intermediate B. Ganirelix can be obtained in high purity and high yield, and the commercial mass-production process therefor is feasible, and also, an economical advantage, that is, the reduction in the production costs compared to conventional technologies, is provided. Furthermore, it is possible to obtain a large quantity of Ganirelix more safely than conventional technologies.
Compound or salt thereof and preparation method and application of same
The invention relates to a compound or a salt thereof, a method for preparation thereof, and use thereof, wherein the compound has the structure of Formula (1): ##STR00001## the substituents in Formula (1) are as defined in the specification. The compound of Formula (1) or a salt thereof can be attached to a solid-phase resin, on which solid-phase synthesis may be performed.
Compound or salt thereof and preparation method and application of same
The invention relates to a compound or a salt thereof, a method for preparation thereof, and use thereof, wherein the compound has the structure of Formula (1): ##STR00001## the substituents in Formula (1) are as defined in the specification. The compound of Formula (1) or a salt thereof can be attached to a solid-phase resin, on which solid-phase synthesis may be performed.
USE OF GNRH ANTAGONISTS IN MAMMALS TO SYNCHRONIZE FOLLICULAR WAVE EMERGENCE
The present disclosure relates to methods for reproductive management of mammalian animals using a GnRH antagonist such as Cetrorelix. Specifically, the GnRH antagonist can be used for synchronizing follicular wave emergence in a population of female mammals, and/or for fixed-time reproductive management protocols such as oocyte collection protocols, embryo collection protocols, artificial insemination protocols or embryo transfer protocols. Also described are devices and kits for reproductive management, comprising a GnRH antagonist and optionally one or more additional drugs useful for reproductive management.