Abstract: The present invention relates to a novel crystalline polymorph of (¾)-2-amino-4-(0-42R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyptetrahydrofuran-2-yl)-2-oxo-1,2- dihydropyrimidin-4-yl)amino)-4-oxobutanoic acid (also known as BST-236, Astarabine® or aspacytarabine), processes of preparation thereof, and uses thereof for the treatment of neoplastic diseases.

Abstract: The invention provides methods and uses for the treatment of hematological cancer in a subject in need thereof.

Abstract: The present invention relates to a composition comprising aspacytarabine (also known as BST-236 and Astarabine®) or a pharmaceutically acceptable salt thereof and an stabilizer and/or solubilizer, wherein the stabilizer and/or solubilizer is selected from at least one water soluble stabilizer and/or solubilizer such as a linear polymer or derivative thereof, an inclusion compound (i.e. cyclodextrin) and combination thereof. The present invention further relates to uses of the composition, particularly for use in the treatment of neoplastic disease.

Abstract: The present invention relates to pharmaceutically acceptable salts of conjugates comprising a chemotherapeutic drug and an amino acid or a derivative thereof, which are readily taken up by a target cell and reduce side effects induced by the chemotherapeutic drug. In particular, the present invention relates to pharmaceutically acceptable salts of conjugates comprising cytidine analog drugs and aspartic or glutamic acid and analogs thereof, pharmaceutical compositions comprising these conjugates and use thereof for the treatment of cancer or a pre-cancer condition or disorder.

Abstract: The present invention relates to conjugates comprising cytarabine and an amino acid for use in the treatment of cancer. In particular, the present invention relates to conjugates of cytarabine and aspartic acid for use in the treatment of hematological cancers.

Abstract: Provided relates to pharmaceutically acceptable salts of conjugates including a chemotherapeutic drug and an amino acid or a derivative thereof, which are readily taken up by a target cell and reduce side effects induced by the chemotherapeutic drug. Further, the subject matter relates to pharmaceutically acceptable salts of conjugates comprising cytidine analog drugs and aspartic or glutamic acid and analogs thereof, pharmaceutical compositions including these conjugates and use thereof for the treatment of cancer or a pre-cancer condition or disorder.

Abstract: Provided relates to conjugates including cytarabine and an amino acid for use in the treatment of cancer. Further, the subject matter relates to conjugates of cytarabine and aspartic acid for use in the treatment of hematological cancers in medically compromised patients.

Abstract: The present invention relates to combination therapies of a cytarabine conjugate and one or more anti-neoplastic agents for inhibiting cancer cell growth. In particular, the present invention relates to a conjugate of cytarabine and aspartic acid (BST-236) in combination with one or more additional anti-neoplastic agents for use in the treatment of hematological cancers.

Abstract: Provided relates to conjugates including cytarabine and an amino acid for use in the treatment of cancer. Further, the subject matter relates to conjugates of cytarabine and aspartic acid for use in the treatment of hematological cancers in medically compromised patients.

Abstract: Provided relates to pharmaceutically acceptable salts of conjugates including a chemotherapeutic drug and an amino acid or a derivative thereof, which are readily taken up by a target cell and reduce side effects induced by the chemotherapeutic drug. Further, the subject matter relates to pharmaceutically acceptable salts of conjugates comprising cytidine analog drugs and aspartic or glutamic acid and analogs thereof, pharmaceutical compositions including these conjugates and use thereof for the treatment of cancer or a pre-cancer condition or disorder.

Abstract: The present invention relates to conjugates of a drug and an amino acid or an amino acid derivative or analog, pharmaceutical compositions that include the conjugates and methods of use thereof. In particular, the present invention relates to conjugates of anti-proliferative drugs and asparagine and glutamine and analogs thereof as compositions for treatment of cancer, and conjugates of imaging agent carriers and amino acids for the diagnosis of tumors and metastases.

Abstract: The present invention relates in general to labeling reagents useful for labeling biomolecules. In particular, the invention provides activated labeling reagents having the formula L-Ph, wherein L is an activated labeling molecule and Ph is a phenol. The invention further provides methods of preparing the labeling reagents, methods of using the labeling reagents for synthesizing a labeled biomolecule, kits that include reagents for labeling a biomolecule and kits containing labeled biomolecules.

Abstract: The present invention relates to prodrug molecules comprising conjugates of an antiproliferative drug, a protease specific cleavable peptide, and, optionally, a targeting peptide, with the prodrugs being substantially inactive prior to degradation of the cleavable sequence by proteolytic enzymes abundant within or in close proximity to the target cancer cell. Also, pharmaceutical compositions of the conjugates and the use of these compositions for treatment of cancer are disclosed.

Abstract: The present invention relates to conjugates of a drug and an amino acid or an amino acid derivative or analog, pharmaceutical compositions that include the conjugates and methods of use thereof. In particular, the present invention relates to conjugates of anti-proliferative drugs and asparagine and glutamine and analogs thereof as compositions for treatment of cancer, and conjugates of imaging agent carriers and amino acids for the diagnosis of tumors and metastases.

Abstract: The present invention relates to pharmaceutical compositions that include a targeting peptide, a protease specific cleavable peptide, and a chemotherapeutic drug that when conjugated are substantially inactive, but upon degradation of the cleavable sequence by a proteolytic enzyme abundant in or within the target cancer cell, the chemotherapeutic drug is released and becomes active, and to methods of use of these compositions for treatment of cancer.

Abstract: The present invention relates to pharmaceutical compositions that include a targeting peptide, a protease specific cleavable peptide, and a chemotherapeutic drug that when conjugated are substantially inactive, but upon degradation of the cleavable sequence by a proteolytic enzyme abundant in or within the target cancer cell, the chemotherapeutic drug is released and becomes active, and to methods of use of these compositions for treatment of cancer.

Abstract: The present invention relates to pharmaceutical compositions that include a targeting peptide, a protease specific cleavable peptide, and a chemotherapeutic drug that when conjugated are substantially inactive, but upon degradation of the cleavable sequence by a proteolytic enzyme abundant in or within the target cancer cell, the chemotherapeutic drug is released and becomes active, and to methods of use of these compositions for treatment of cancer.