Endocyte, Inc.

Purdue Research Foundation

Bristol-Myers Squibb Compnay

Iontcho Radoslavov Vlahov

Christopher Paul Leamon

Hari Krishna R Santhapuram

Paul Joseph Kleindl

Kevin Yu Wang

Fei You

Philip Stewart Low

Stephen J Howard

Apparao Satyam

Joseph Anand Reddy

Marilynn Vetzel

Le-Cun Xu

Melissa Nelson

Ryan Dorton

Yu Wang

Michael Groaning

Alicia Bloomfield

Katheryn Marie Stanford

Allen Ritter

Yingjuan June Lu

Matthew A Parker

Garth L Parham

Hari Krishna Santhapuram

Albert E Felten

Gregory D Vite

Francis Lee

Ning Zou

Bindu Varghese

Longwu Qi

Chunhong Li

Yingcai Wang

Daniel S Reno

Katheryn M Stanford

Qingshou Chen

Christina M Dircksen

Nikki L Parker

Jonathan M Shillingford

Fei Yu

Kim Soong-Hoon

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

Described herein are compounds, compositions, and methods for diagnosing and/or monitoring pathogenic disease using positron emission tomography. Also described are conjugates of the formula B-L-P, wherein B is a radical of a targeting agent selected from vitamin receptor binding ligands (such as folate), PSMA binding ligands, or PSMA inhibitors; L is a divalent linker comprising aspartic acid, lysine, or arginine, and P is a radical of an imaging agent or radiotherapy agent, such as a radionuclide or radionuclide containing group, or a radical of a compound capable of binding a radionuclide, such as a metal chelating group.

Compounds for positron emission tomography

Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described.

Folate receptor binding conjugates of antifolates

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 compounds capable of targeting PSMA expressing cells.

Conjugates for treating diseases caused by PSMA expressing cells

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

The present disclosure relates to compositions and methods of carbonic anhydrase IX inhibitors. The present disclosure also relates to targeting conjugates of carbonic anhydrase IX inhibitors as therapeutics and imaging agents. The present disclosure also relates to the use of targeting conjugates of carbonic anhydrase IX inhibitors in imaging methods and cancer therapy.

Carbonic anhydrase IX inhibitor conjugates and uses thereof

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

This invention pertains to bivalent linkers, and the synthesis and use thereof. In particular, this invention pertains to the synthesis and use of bivalent linkers in preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates. The present invention includes divalent linkers, which are alternatively referred to as bivalent linkers, that may be used to couple, link, bond, attach, or otherwise associate two or more chemical entities. This coupling, linking, attachment, or association may be used in the formation of conjugates of such chemical entities. Those chemical entities include targeting ligands and receptor-binding ligands, such as vitamins. Those chemical entities also include drugs for treating various diseases or disease states, and imaging and diagnostic agents for diagnosing, detecting, or otherwise monitoring various diseases or disease states.

Bivalent linkers and conjugates thereof

The present disclosure relates to pyrrolobenzodiazepine (PBD) prodrugs and conjugates thereof. The present disclosure also relates to pharmaceutical compositions of the conjugates described herein, methods of making and methods of using the same.

Conjugates for treating diseases

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.

CCK2R-drug conjugates

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

Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating stroll diseases are also described.

Described are methods, uses, and kits for utilizing a targeted ligand conjugate in combination with a thiol inhibitor or a system xinhibitor for the treatment of cancer or inflammation. Also described are in vitro assays utilizing a targeted ligand conjugate in combination with a thiol inhibitor or a system xinhibitor.

Methods for treating cancer using combination therapies

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West Lafayette, IN, United States of America

Iontcho Radoslavov Vlahov