Cornell University

University of California

Temple University

Justin Wilson

Nikki Thiele

John W Babich

James M Kelly

Shashikanth Ponnala

Sierra C Marker

Swati Sudhakar More

Sarah Nathan

Kathleen M Giacomini

Sook Wah Yee

Madesh Muniswamy

Ethan Geier

Shu-Bing Qian

Kevin Knopf

Robert Swanda

Arthur Paden King

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (“PSMA”) where the compounds are represented by the following:

Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer

A composition comprising the following structure: (1) wherein Re represents a rhenium ion having a +1 charge; (I) represents an uncharged bidentate ligand containing at least one ring containing a ring nitrogen atom bound to the rhenium (Re), and the bidentate ligand containing another nitrogen atom, either in a ring or not in a ring, bound to the rhenium (Re); and L, L, L, and Lare neutral ligands with at least one neutral ligand being an isonitrile ligand of the formula —CN—R, wherein R is an aliphatic or aromatic hydrocarbon group containing 1-20 carbon atoms; and Xrepresents a non-coordinating monovalent anion; wherein the bidentate ligand and R are optionally substituted by one or more groups selected from (i)-(xi) as further discussed above. Methods for treating a condition that benefits from ER stress induction, such as cancer, by administering the above rhenium complex are also disclosed.

Rhenium complexes and methods of use for treating cancer

Metal-chelating compositions having the structure (1a) wherein: R, R, R, and Rare independently selected from the following groups: (i) hydrogen atom, (ii) hydrocarbon groups (R) containing 1-12 carbon atoms; (iii) halogen atoms; (iv) &#x2014;P(R) (&#x2550;O)OH groups; (v) &#x2014;C(&#x2550;O)OH groups; (vi) &#x2014;S(&#x2550;O)OH groups; and (vii) &#x2014;OH groups, wherein Ris selected from hydrocarbon groups (R) and &#x2014;OH; Rand Rmay optionally interconnect to form Ring A fused to the ring on which Rand Rare present; Rand Rmay optionally interconnect to form Ring B fused to the ring on which Rand Rare present; wherein Ring A and Ring B are optionally and independently substituted with one or more of groups (ii)-(vii). Methods of using the above-described compositions for chelating metal ions having an atomic number of at least 56 (e.g., Ba or Ra) are also described.

Metal-chelating compositions and their use in methods of removing or inhibiting barium scale

The present technology provides compounds as well as compositions including such compounds useful for the treatment of cancers where the compounds are represented by the following formula (I) or a pharmaceutically acceptable salt thereof, wherein M is an alpha-emitting radionuclide. 

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen ('PSMA') where the compounds are represented by the following:   

A method for treating or preventing a disease or condition that operates by calcium transport through the mitochondrial calcium uniporter (MCU), the method comprising administering to a subject a therapeutically effective amount of an MCU inhibitor having the following structure: wherein L, L, L, L, L, L, L, L, X, and Xare independently selected from halide, amine groups &#x2014;NRRR, phosphine groups &#x2014;PRRR, carboxylate groups RC(O)O&#x2014;, and solvent molecules, and provided that at least one of L, L, L, L, L, L, L, L, X, and Xis selected from amine or phosphine groups; wherein R, R, R, and Rare independently selected from hydrogen atoms and hydrocarbon groups having up to six carbon atoms, wherein two of R, R, and Rwithin a &#x2014;NRRRgroup are optionally interconnected to form an N-containing ring; and R groups in adjacent amino or phosphine groups may optionally interconnect.

Ruthenium &#x3bc;-nitrido complexes and their use as calcium uptake inhibitors

A composition comprising the following structure: (formula I) wherein Re represents a rhenium ion having a +1 charge; (formula II) represents an uncharged bidentate bicyclic ligand bonded to the rhenium (Re) by two ring nitrogen (N) atoms; and L is a neutral ligand independently selected from CO and neutral phosphine molecules, wherein at least one of the L groups is a CO molecule; and Xrepresents a non-coordinating monovalent anion; wherein (formula II) is unsubstituted or substituted on any of its two rings, and said neutral phosphine molecule may or may not contain a phosphorus atom as a ring phosphorus atom; provided that, if (formula II) is unsubstituted, then one or two of said L groups are selected from said neutral phosphine molecules, with the provision that at least one of the neutral phosphine molecules has a phosphorus atom as a ring phosphorus atom. Methods for treating cancer by administering the above complex are also disclosed. 

Disclosed herein, inter alia, are platinum-based compounds useful for treating cancer.

Growing community of inventors

Ithaca, NY, United States of America

Justin Wilson