Endocyte, Inc.

Hari Krishna R Santhapuram

Christopher Paul Leamon

Iontcho Radoslavov Vlahov

Paul Joseph Kleindl

Fei You

Kevin Yu Wang

Le-Cun Xu

Allen Ritter

Katheryn Marie Stanford

Michael Groaning

Yingjuan June Lu

Stephen J Howard

Apparao Satyam

Joseph Anand Reddy

Matthew A Parker

Yu Wang

Fei Yu

Daniel S Reno

Katheryn M Stanford

This disclosure relates to processes for preparing compounds that are useful in the treatment of disease, such as cancer, in mammals. In particular, the invention described herein pertains to processes for preparing compounds capable of targeting PSMA expressing cells and useful in the treatment of diseases caused by PSMA expressing cells, such as prostate cancer.

Methods for preparing PSMA conjugates

The invention described herein relates to conjugates and compositions for imaging, diagnosing, and/or monitoring diseases using radionuclide-based imaging. In particular, the invention described herein relates to conjugates and compositions for imaging, diagnosing, and/or monitoring diseases using positron emission tomography.

Conjugates for imaging

Described herein are compositions and methods for use in targeted drug delivery using cell-surface receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in treating disease states caused by pathogenic cell populations.

Conjugates containing hydrophilic spacer linkers

Described herein are compositions, methods, compounds, conjugates, and kits for use in targeted drug delivery using drug delivery conjugates containing hydrophilic spacer linkers for use in treating disease states caused by pathogenic cell populations, such as inflammatory cells.

Vitamin receptor drug delivery conjugates for treating inflammation

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.

Processes for preparing tubulysin derivatives and conjugates thereof

Tubulysins are a series of naturally occurring cytotoxic agents that are of interest as anticancer therapeutic agents. Processes and intermediates useful for preparing naturally occurring and non-naturally occurring tubulysins and analogs and derivatives thereof are described.

Processes for preparing tubulysins

Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.

The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

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West Lafayette, IN, United States of America

Hari Krishna R Santhapuram