C07D207/46

REAGENTS FOR RAPID CHIRAL LABELING AND ANALYSIS OF AMINE CONTAINING ENANTIOMERS

Provided herein chiral derivatization reagents for use in separating and detecting of amine containing enantiomers. The said chiral derivatization reagents provide a combination of improved detectable properties to facilitate various downstream analyses. In particular, the chiral derivatization reagents include at least one chiral carbon atom; at least one strongly basic moiety; at least one chromophore moiety or at least one fluorophore moiety; and at least one reactive group. The present disclosure further provides methods for analyzing amine-containing enantiomeric isomers using a chromatographic separation device and a mass spectroscopy.

REAGENTS FOR RAPID CHIRAL LABELING AND ANALYSIS OF AMINE CONTAINING ENANTIOMERS

Provided herein chiral derivatization reagents for use in separating and detecting of amine containing enantiomers. The said chiral derivatization reagents provide a combination of improved detectable properties to facilitate various downstream analyses. In particular, the chiral derivatization reagents include at least one chiral carbon atom; at least one strongly basic moiety; at least one chromophore moiety or at least one fluorophore moiety; and at least one reactive group. The present disclosure further provides methods for analyzing amine-containing enantiomeric isomers using a chromatographic separation device and a mass spectroscopy.

PROCESS OF PREPARING ARACHIDONOYLETHANOLAMINE ANALOGUES

The present application provides new processes for preparing arachidonoylethanolamine analogues. Intermediates useful for preparing the compounds are also provided.

PROCESS OF PREPARING ARACHIDONOYLETHANOLAMINE ANALOGUES

The present application provides new processes for preparing arachidonoylethanolamine analogues. Intermediates useful for preparing the compounds are also provided.

METHODS OF PREPARING N6-((2-AZIDOETHOXY)CARBONYL)LYSINE

Disclosed herein are methods of preparing N.sup.6-((2-azidoethoxy)carbonyl)lysine, N.sup.6-((2-azidoethoxy)carbonyl)-L-lysine, and N.sup.6-((2-azidoethoxy)carbonyl)-D-lysine. Also disclosed herein are the compounds tert-butyl N.sup.2-(tert-butoxycarbonyl)-N.sup.6-((2-chloroethoxy)carbonyl)-L-lysinate and tert-butyl N.sup.6-((2-azidoethoxy)carbonyl)-N.sup.2-(tert-butoxycarbonyl)-L-lysinate, and uses thereof.

SITE-SPECIFIC ANTIBODY CONJUGATION AND ANTIBODY-DRUG CONJUGATE AS SPECIFIC EMBODIMENT THEREOF

The present invention relates to technology capable of labeling a certain site of an antibody with a certain number of chemical functional groups or cargo moieties. The present invention may provide an antibody product having high uniformity. The present invention may provide an antibody product whose antibody functions are not degraded. That is, the present invention may provide an antibody product whose antibody binding affinity and half-life are not degraded. The present invention is of great significance as being the first technology allowing site-specific labeling of an antibody without any complicated processes.

SITE-SPECIFIC ANTIBODY CONJUGATION AND ANTIBODY-DRUG CONJUGATE AS SPECIFIC EMBODIMENT THEREOF

The present invention relates to technology capable of labeling a certain site of an antibody with a certain number of chemical functional groups or cargo moieties. The present invention may provide an antibody product having high uniformity. The present invention may provide an antibody product whose antibody functions are not degraded. That is, the present invention may provide an antibody product whose antibody binding affinity and half-life are not degraded. The present invention is of great significance as being the first technology allowing site-specific labeling of an antibody without any complicated processes.

CONJUGATES UNDERGOING INTRAMOLECULAR REARRANGEMENTS
20230110994 · 2023-04-13 ·

The present invention relates to conjugates and pharmaceutically acceptable salts thereof, reagents, intermediates, methods for the synthesis of said conjugates, pharmaceutical compositions comprising said conjugates and the use of said conjugates.

SYNTHETIC PROCESSES AND INTERMEDIATES

The invention provides synthetic processes and synthetic intermediate compounds that can be used to prepare therapeutic conjugates. The invention also provides methods for treating HBV and/or HDV infection in a human by administering a therapeutic conjugate prepared by the synthetic methods of the invention.

SYNTHETIC PROCESSES AND INTERMEDIATES

The invention provides synthetic processes and synthetic intermediate compounds that can be used to prepare therapeutic conjugates. The invention also provides methods for treating HBV and/or HDV infection in a human by administering a therapeutic conjugate prepared by the synthetic methods of the invention.