摘要:
The invention described herein pertains to drug delivery conjugates for targeted therapy. The invention described herein relates to methods of treating folate receptor-expressing cancers with a folate-tubulysin conjugate. The invention described herein also relates to methods of treating folate-expressing cancers with a folate tubulysin conjugate in patients where stable disease results after treatment with the folate-tubulysin conjugate.
摘要:
The present disclosure relates to a method for imaging cancer by administering to a patient a labeled chelating compound and an unlabeled chelating compound.
摘要:
The disclosure provided herein pertains to CCK2R-drug conjugates. In particular, the disclosure pertains to CCK2R-drug conjugates that target the delivery of drugs to a mammalian recipient. Also described are methods of making and using CCK2R-drug conjugates.
摘要:
The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using a conjugate of the general formula B-L-(D)n as further defined in the claims.
摘要:
The invention described herein pertains to processes for preparing tubulysin derivatives, conjugates of tubulysins, and intermediates therefore. In one illustrative embodiment of the invention, processes for derivatives or analogs of natural tubulysins including compounds of formula (T). In another embodiment, vitamin receptor binding conjugates of tubulysins are described. The processes include one or more steps described herein. In another embodiment, a process is described for preparing a compound of formula B, wherein R5 and R6 are as described in the various embodiments herein, such as each being independently selected from optionally substituted alkyl or optionally substituted cycloalkyl; and R8 is C1-C6 n-alkyl; wherein the process comprises the step of treating a compound of formula A with a silylating agent, such as triethylsilyl chloride, and a base, such as imidazole in an aprotic solvent.