University of Texas System

Pg-txl Company, L.p.

Taiwan Hopaz Chems, Mfg. Co., Ltd.

Taiwan Hopax Chems. Mfg. Co., Ltd.

Dong-Fang Yu

David J Yang

Sidney Wallace

Chun Li

E Edmund Kim

Chun W Liu

Chang-Sok Oh

Ali Azhdarinia

Saady Kohanim

Jerry L Bryant, Jr

I-Chien Wei

Richard O Mendez

Tommy L Lee

E Edmond Kim

Jerry Bryant

Chang Sok Oh

Chun-Wei Liu

Sydney Wallace

The invention include glycopeptides having a glycoside and a peptide covalently bound through an amide bond. The glycopeptides may also include a diagnostic or therapeutic agent bound to the glycopeptide. A metal, such as a radionuclide, may also be chelated to the glycopeptide. Specific embodiments of the invention relate to glycopeptides made of chitosan covalently bound to a poly(amino acid) such as poly(glutamic acid) or poly(aspartic acid). Diagnostic agents conjugated to the glycopeptide may facilitate imaging. Specific therapeutic agents that may be conjugated to the glycopeptide include anticancer drugs, rheumatoid arthritis drugs, anticoagulants, anti-angiogenesis drugs, apoptosis drugs, osteoporosis drugs, steroids, and anti-inflammatory drugs. Some agents, such as radionuclides, may have both diagnostic and therapeutic effects. The glycopeptides may be made by combining a glycoside and a peptide in the presence of a carbodiimide and an acid group activator to form an amide bond between the glycoside and the peptide.

Glycopeptide compositions

Novel methods of synthesis of ethylenedicysteine-sugar conjugates and therapeutic and diagnostic applications of such conjugates are disclosed. Methods of synthesizing these conjugates in high purity are also presented as using starting materials such as thiazolidine carboxylic acid. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these conjugates prepared herein, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

Efficient synthesis of ethylenedicysteine-sugar conjugates for imaging and therapy

The invention provides, in a general sense, a new labeling strategy employing compounds that are NSchelates conjugated to a targeting ligand, wherein the targeting ligand is a disease cell cycle targeting compound, a tumor angiogenesis targeting ligand, a tumor apoptosis targeting ligand, a disease receptor targeting ligand, amifostine, angiostatin, monoclonal antibody C225, monoclonal antibody CD31, monoclonal antibody CD40, capecitabine, a COX-2 inhibitor, deoxycytidine, fullerene, herceptin, human serum albumin, lactose, leuteinizing hormone, pyridoxal, quinazoline, thalidomide, transferrin, or trimethyl lysine. The present invention also pertains to kits employing the compounds of interest, and methods of assessing the pharmacology of an agent of interest using the present compounds.

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The present invention relates generally to the fields of chemistry and radionuclide imaging. More particularly, it concerns compositions, kits and methods for imaging and therapy involving Ncompounds and derivatives.

Compositions and methods for cellular imaging and therapy

Compositions and methods for imaging and for chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns agents comprising a targeting moeity comprising a beta-adrenergic receptor targeting compound conjugated or embedded with ethylenediamine. The present invention also concerns methods of application of such agents for imaging and treatment of cardiovascular diseases, and kits for preparing a radiolabeled therapeutic or diagnostic agent.

Image-guided therapy of myocardial disease: composition, manufacturing and applications

The invention provides, in a general sense, a new labeling strategy employingTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated toTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.

Bisaminoethanethiol-targeting ligand conjugates and compositions

Ethylenedicysteine (EC)-drug conjugates, compositions and methods for tissue specific disease imaging

Metal ion-labeled bis-aminoethanethiol-targeting ligand conjugates, compositions, and methods for tissue-specific disease imaging

Compositions for imaging pancreatic beta cells comprise chelator-antidiabetic agent conjugates and optionally chelated metals.

Mechanism-based targeted pancreatic beta cell imaging and therapy

Ethylenedicysteine (EC)-drug conjugates compositions and methods for tissue specific disease imaging

Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include the coating of implantable stents for prevention of restenosis.

Water soluble paclitaxel prodrugs

Water soluble paclitaxel derivatives

Growing community of inventors

Houston, TX, United States of America

Dong-Fang Yu