05-12-2013 дата публикации
Номер: US20130323169A1
Принадлежит:
The present invention relates to linker molecules that readily conjugate cellular recognition ligand at one end and drug payload at the other, and are useful in treating or preventing cancer, an autoimmune disease, an inflammatory condition, a central nervous system disorder or an infection. The linker inker molecules of the invention are represented by Formula I, II and III; Linker-Drug compounds represented by Formula IV, V and VI; and Ligand-Linker-Drug conjugates represented by Formula VII, VIII and IX: 2. A method of claim 1 , wherein each X is a spacer.3. A method of claim 1 , wherein each X is non-cleavable spacer when the conjugates contains radioisotopes.4. A method of claim 1 , step (a) claim 1 , wherein the said Linker-Drug conjugate compound of Formula IV claim 1 , V or VI is formed between the functional group Z present in a linker compound of Formula I claim 1 , II or III and a functional group claim 1 , either natively present or chemically introduced claim 1 , in the drug moiety selected from primary or secondary amine claim 1 , hydroxyl claim 1 , sulfhydryl claim 1 , carboxyl claim 1 , aldehyde or ketone via a covalent bond by esterification claim 1 , amidation claim 1 , reductive amination or aldol reaction.10. A composition comprising a compound of and a pharmaceutically acceptable carrier claim 6 , excipient claim 6 , or diluent.11. A method of treating or preventing cancer claim 6 , an autoimmune disease claim 6 , an inflammatory condition claim 6 , a central nervous system disorder or an infection in a patient claim 6 , said method comprising administering to a patient an effective amount of a compound according to .12. A composition comprising a compound according to and a pharmaceutically acceptable carrier claim 7 , excipient claim 7 , or diluent.13. A method of treating or preventing cancer claim 7 , an autoimmune disease claim 7 , an inflammatory condition claim 7 , a central nervous system disorder or an infection in a patient claim 7 , ...
Подробнее