(Des-Gly10,Leu6,Pro-NHEt9)-LHRH Trifluoroacetate

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (Des-Gly10,Leu6,Pro-NHEt9)-LHRH Trifluoroacetate
• 英文别名: (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide;2,2,2-trifluoroacetic acid
• 化学式: C61H85F3N16O14
• 分子量: 1323.4
• InChiKey: VIKVLAJTEHLRFY-XNHQSDQCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  94
• 可旋转键数：
  32
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  469
• 氢给体数：
  16
• 氢受体数：
  19

文献信息

• Purification of Organic Compounds Using Surrogate Stationary Phases on Reversed Phase Columns
  申请人：NEULAND HEALTH SCIENCES PRIVATE LIMITED

  公开号：US20150360146A1

  公开（公告）日：2015-12-17

  There are only two ways to increase the amount of sample that can be purified by preparative reversed phase high performance liquid chromatography (Prep-RP-HPLC) in a single run: (1) The traditional approach is to use a bigger column (greater amount of stationary phase); and (2) Use displacement chromatography which uses the stationary phase more effectively. This invention describes a unique Prep-RP-HPLC technique that uses a C-18/C-8 derivatized silica coated with a hydrophobic quaternary ammonium salt or quaternary phosphonium salt to result in 7 to 12 fold increase in sample loading (of the crude mixture of organic compounds including synthetic crude peptides) in contrast to the conventional Prep-RP-HPLC technique. This increase in sample loading capacity and output is due to the additional surrogate stationary phase characteristic of the C-18/C8 bound quaternary salt. The quaternary surfactant is bound to the C-18/C-8 chains and silanols of the stationary phase.

  在单次运行中，只有两种方法可以增加制备性反相高效液相色谱（Prep-RP-HPLC）可纯化样品的数量：（1）传统方法是使用更大的柱子（更多的固定相）；（2）使用位移色谱，更有效地利用固定相。本发明描述了一种独特的制备性反相高效液相色谱技术，该技术使用C-18 / C-8衍生的硅胶，涂有疏水性季铵盐或季膦盐，与传统的Prep-RP-HPLC技术相比，可将样品负荷（包括合成粗制肽的有机化合物混合物）提高7到12倍。这种样品负荷容量和产出的增加是由于C-18 / C8结合的季铵盐的额外代理固定相特性。季铵表面活性剂结合到固定相的C-18 / C-8链和硅醇上。
• [EN] COMPOUND OR SALT THEREOF AND PREPARATION METHOD AND APPLICATION OF SAME<br/>[FR] COMPOSÉ OU SEL DE CELUI-CI ET SON PROCÉDÉ DE PRÉPARATION ET SON APPLICATION<br/>[ZH] 一种化合物或其盐及其制备方法与应用
  申请人：ZHEJIANG PEPTITES BIOTECH CO LTD

  公开号：WO2019242010A1

  公开（公告）日：2019-12-26

  一种化合物或其盐作为连接链，可将该化合物或其盐加载在固相树脂上，进行多肽药物的固相合成，能提高多肽药物的合成收率。
• PURIFICATION OF ORGANIC COMPOUNDS USING SURROGATE STATIONARY PHASES ON REVERSED PHASE COLUMNS
  申请人：Neuland Health Sciences Private Limited

  公开号：EP2950904A1

  公开（公告）日：2015-12-09
• LEUPROLIDE ACETATE COMPOSITIONS AND METHODS OF USING THE SAME TO TREAT BREAST CANCER
  申请人：Tolmar International Limited

  公开号：EP3975990A1

  公开（公告）日：2022-04-06
• Method of Treating a Child with Central Precocious Puberty using an Extended Release Composition
  申请人：Tolmar International Limited

  公开号：US20200330547A1

  公开（公告）日：2020-10-22

  An extended release formulation is provided for use in a method for the treatment of Central Precocious Puberty (CPP) in pediatric patients 2 years of age or older. The extended release formulation comprises leuprolide or a pharmaceutically acceptable salt thereof, a biodegradable polymer, and a biocompatible organic solvent. The biodegradable polymer is comprised of poly(lactide-co-glycolide) (PLG) copolymer segments, poly(lactic acid-co-glycolic acid) (PLGA) copolymer segments, poly(lactide) (PL) polymer segments, poly(lactic acid) (PLA) polymer segments, or a combination thereof. The extended release formulation is administered as a subcutaneous injection of a flowable composition that forms a solid in situ depot. The extended release formulation releases leuprolide for a period of about 6 months for the effective treatment of CPP within a pediatric patient.