Entremed, Inc.

Ergon Pharmaceuticals LLC

Children's Medical Center Corporation

Adonia E Papathanassiu

Shawn J Green

Jamshed H Shah

John W Madsen

William E Fogler

Robert J D'Amato

Glenn M Swartz, Jr

Glenn M Swartz

Victor P Pribluda

Todd Hembrough

The present invention is directed to itaconic acid derivatives, compounds comprising the derivatives and methods of using the derivatives in the treatment of cancer, inflammation, and autoimmune diseases.

Compositions and methods of using itaconic acid derivatives

The present invention is directed to compounds and methods that inhibit the cytosolic form of BCAT1.

Compositions and methods of treatment using a BCAT1 inhibitor

The present invention is directed to BCAT inhibitors with the following formula: 

Methods of treatment using a BCAT1 inhibitor

The present invention provides a treatment for mammalian diseases characterized by pathological angiogenesis. The treatment consists of administering therapeutically active dosages of peptides containing specific amino acid sequences or antibodies that bind to cell membrane antigens on the surface of rapidly dividing endothelial cells.

Compositions and methods for inhibiting angiogenesis

The invention provides new and useful analogs of 2-phthalimidinoglutaric acid. These analogs include DL-2-methyl-2-phthalimidinoglutaric acid and hydroxylated analogs of 2-phthalimidinoglutaric. The invention also provides processes for making these analogs. The invention also provides the two individual enantiomers of DL-2-methyl-2-phthalimidinoglutaric acid, (R)-(+)-2-methyl-2-phthalimidinoglutaric acid and (S)-(&#x2212;)-2-methyl-2-phthalimidinoglutaric acid, and processes for separating these individual enantiomers from the racemate. Further, the invention provides methods for inhibiting angiogenesis and treating angiogenesis-associated diseases, including cancer and macular degeneration, by administering one or more of these compounds.

Methods of treating undesired angiogenesis with 2-methyl-EM-138

Compositions and methods effective in inhibiting abnormal or undesirable cell proliferation, particularly endothelial cell proliferation and angiogenesis related to neovascularization and tumor growth are provided. The compositions comprise a naturally occurring or synthetic protein, peptide, or protein fragment containing all or an active portion of the C-terminal portion of proteinase inhibitors such as TFPI. The methods involve administering to a human or animal the composition described herein in a dosage sufficient to inhibit cell proliferation, particularly endothelial cell proliferation. The methods are useful for treating diseases and processes mediated by undesired and uncontrolled cell proliferation, such as cancer, particularly by inhibiting angiogenesis. Administration of the composition to a human or animal having prevascularized, metastasized tumors is useful for preventing the growth or expansion of such tumors.

Compositions and methods for inhibiting cellular proliferation comprising TFPI fragments

Compositions and methods for inhibiting cellular proliferation wherein the composition contains Tissue Factor Pathway Inhibitor (TFPI), a TFPI homolog, or an active fragment thereof. TFPI exhibits potent anti-proliferative activity on human and other animal cells, particularly endothelial cells. More particularly, the TFPI, TFPI homolog, and inhibitory fragment thereof may be combined with a pharmaceutically acceptable excipient or carrier and used to inhibit angiogenesis and angiogenesis-related diseases such as cancer, arthritis, macular degeneration, and diabetic retinopathy.

Compositions and methods for inhibiting cellular proliferation

The invention provides new and useful analogs of 2-phthalimidinoglutaric acid. These analogs include DL-2-methyl-2-phthalimidinoglutaric acid and hydroxylated analogs of 2-phthalimidinoglutaric. The invention also provides processes for making these analogs. The invention also provides the two individual enantiomers of DL-2-methyl-2-phthalimidinoglutaric acid, (R)-(&plus;)-2-methyl-2-phthalimidinoglutaric acid and (S)-(&minus;)-2-methyl-2-phthalimidinoglutaric acid, and processes for separating these individual enantiomers from the racemate. Further, the invention provides methods for inhibiting angiogenesis and treating angiogenesis-associated diseases, including cancer and macular degeneration, by administering one or more of these compounds.

Analogs of 2-Phthalimidinoglutaric acid

The present invention provides compounds that are useful for inhibiting the proliferation of fungi. The compounds are estrogenic derivatives, such as 2ME2, or anti-estrogenic compounds. The compounds may be used for treating infections of fungi in humans and animals, or to prevent or inhibit the growth of fungi on any surface.

Use of anti-estrogenic compounds as anti-fungal agents

Compositions and methods effective in inhibiting abnormal or undesirable cell proliferation, particularly endothelial cell proliferation and angiogenesis related to neovascularization and tumor growth are provided. The compositions comprise naturally occurring, or synthetic proteins, peptides, or protein fragments capable of binding to components of the blood coagulation pathway. The compositions may be administered using a pharmaceutically acceptable carrier. The methods involve administering to a human or animal the composition described herein in a dosage sufficient to inhibit cell proliferation, particularly endothelial cell proliferation. The methods are useful for treating diseases and processes mediated by undesired and uncontrolled cell proliferation, such as cancer, particularly by inhibiting angiogenesis. Administration of the composition to a human or animal having prevascularized metastasized tumors is useful for preventing the growth or expansion of such tumors.

Compositions and methods of use of ligands that bind components of the blood coagulation/clotting pathway for the treatment of cancer and angiogenic-based disease

The present invention provides a treatment for mammalian diseases characterized by aberrant cell proliferation. The treatment consists of administering therapeutically active dosages of antibiotic inhibitors such as efrapeptin oligopeptides or mycotoxin derivatives including those comprising a-zearalenol structural motifs resulting in inhibition of cell mitosis.

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Silver Spring, MD, United States of America

Adonia E Papathanassiu