ACID SALT FORMS OF POLYMER-DRUG CONJUGATES AND ALKOXYLATION METHODS

• Main Authors: LAVATY, GREG, TIPNIS, SACHIN, HANDLEY, JOHN R, MCMANUS, SAMUEL, SWALLOW, DAVID, KOZLOWSKI, ANTONI, SCHAEFER, ANTHONY G
• Format: Patent
• Language: English; French
• Published: 03.01.2023
• Subjects: CHEMISTRY; COMPOSITIONS BASED THEREON; COMPOSITIONS OF MACROMOLECULAR COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONSONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC MACROMOLECULAR COMPOUNDS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; THEIR PREPARATION OR CHEMICAL WORKING-UP

Among other aspects, provided herein is a mixed-acid salt of a water-soluble polymer-drug conjugate, along with related methods of making and using the same. The mixed-acid salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding predominantly pure acid salt or free base forms of the polymer- drug conjugate. The mixed acid salt is reproducibly prepared and recovered, and provides surprising advantages over non-mixed acid salt forms of the water-soluble polymer drug conjugate. Il est décrit un sel dacides mixtes dun conjugué de médicament polymère soluble dans leau, ainsi que des méthodes de production connexes. Le sel dacides mixtes étant formé de manière stable, il semble avoir une plus grande résistance à la dégradation hydrolytique que les conjugués de médicament polymère comportant principalement un sel dacide pur ou une base libre. Le sel dacides mixtes fournit des avantages étonnants comparativement aux conjugués de médicament polymère soluble dans leau qui nen contiennent pas et sa production ainsi que sa récupération se font de manière reproductible.