60175-04-4

Usage

Uses

Used in Pharmaceutical Industry:
Gabapentin Ethyl Ester Hydrochloride is used as an anticonvulsant medication for the treatment of various seizure disorders. Its ability to cross the blood-brain barrier allows it to effectively target the central nervous system and provide relief from seizures.
As a protected form of Gabapentin, G117250 offers enhanced bioavailability and improved pharmacokinetic properties, making it a promising candidate for the development of new therapies for neurological conditions.

Upstream product

• 64-17-5 ethanol 
• 60142-96-3 H-Gpn-OH 

Relevant academic research and scientific papers

An ester derivative of the drug gabapentin: PH dependent crystal stability

Gabapentin solutions with different pHs were prepared and slow crystallization was allowed to occur. Different crystalline forms were obtained at pHs up to 7, whereas alkaline media (pH 9) gave rise to an amorphous product. A new crystal structure of an ethyl ester derivative, obtained at pH 2 under Fischer esterification conditions, is described herein. Esterification blocked the supramolecular interactions typically observed through the carboxyl group of gabapentin, which resulted in a dramatic change in the solid-state structure. As it is known, this change could have a marked influence on the physiological absorption characteristics of the drug, which supports the search for ester-based gabapentin prodrugs as a means of improving the limited bioavailability of the drug.

Mutual prodrugs containing bio-cleavable and drug releasable disulfide linkers

We report herein the design and synthesis of several representative examples of novel mutual prodrugs containing nine distinct types of self-immolative drug-releasable disulfide linkers with urethane, ester, carbonate, or imide linkages between the linker and any two amine/amide/urea (primary or secondary) or carboxyl or hydroxyl (including phenolic)-containing drugs. We also report drug release profiles of a few representative mutual prodrugs in biological fluids such as simulated gastric fluid and human plasma. We also propose plausible mechanisms of drug release from these mutual prodrugs. We have also conducted a few mechanistic studies based on suggested sulfhydryl-assisted cleavage of mutual prodrugs and characterized a few important metabolites to give support to the proposed mechanism of drug release from the reported mutual prodrugs.

New compounds, synthesis and use thereof in the treatment of pain

The present invention relates to a compound of formula (I), or pharmaceutically acceptable, stereoisomers, salts or solvates thereof to methods for its synthesis, and use in the treatment of pain.

NEW COMPOUNDS, SYNTHESIS AND USE THEREOF IN THE TREATMENT OF PAIN

The present invention relates to a compound of formula (I), or pharmaceutically acceptable, stereoisomers, salts or solvates thereof to methods for its synthesis, and use in the treatment of pain and to a method of treatment of pain using the compounds of