Water-soluble L-DOPA esters

• Main Authors: WEISSER JURGEN, LAUBE THORSTEN, WYRWA RALF, SCHNALBELRAUCH MATTHIAS, VOLKEL CHRISTOPH, TACK JOHANNES
• Format: Patent
• Language: Chinese; English
• Published: 27.03.2018
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; DERIVATIVES THEREOF; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SUGARS

The present invention relates to novel compounds of the formula I, methods for their preparation and their use for treatment of diseases. The invention discloses the synthesis of levodopa (L-DOPA) esters by coupling polyhydroxy compounds or their derivatives to the L-DOPA carboxyl group. The synthesis allows to produce L-DOPA derivatives which are highly soluble in water as well as aqueous and biocompatible liquids and have an improved hydrolytic stability in water or aqueous and biocompatible media for an application over several days. The invention helps producing L-DOPA substances for applications in the fields of medicine, biology and medical engineering as well as in the pharmaceutical industry. 本发明涉及式I的新型化合物、其制备方法和它们用于治疗疾病的用途。本发明公开了通过将多羟基化合物或其衍生物与L-DOPA羧基偶联来合成左旋多巴(L-DOPA)酯。所述合成允许产生在水以及水性和生物相容性液体中高度可溶且在水或水性和生物相容性介质中经施加几天具有改善的水解稳定性的L-DOPA衍生物。本发明有助于生产应用于医药、生物和医学工程领域以及制药工业的L-DOPA物质。