Bipar Sciences, Inc.

Rigel Pharmaceuticals, Incorporated

Valeria S Ossovskaya

Barry M Sherman

Ying Luo

Xiang Xu

John P Burnier

Ernest Kun

Jerome Mendeleyev

Betty Huang

Eva Chan

Hassan Lemjabbar-Alaoui

Max Totrov

Esteban Masuda

Bruce Alan Keyt

Brian Wong

Carol Basbaum

Robert Booher

Jerome Moore

Carol Basbaurn

Charles Bradley

Lingyun Li

Methods of treating bone cancer are disclosed. The methods comprise administering to a patient a therapeutically effective amount of a compound of formula (Ia) wherein R, R, R, R, and Rare described herein, wherein at least two of the five R, R, R, R, and Rsubstituents are always hydrogen, at least one of the five substituents is always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts thereof.

Treatment of cancer

The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.

The present invention relates to a method of treating a fatty acid synthesis related disease comprising administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis, wherein the fatty acid synthesis related disease is obesity, diabetes, or cardiovascular disease. The present invention also relates to a method of treating a cancer in a subject comprising: (i) identifying a level of fatty acid in a sample from the subject, and (ii) administering an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis in the subject, wherein the administration is based on the level of fatty acid, thereby treating the cancer in the subject. The present invention further relates to a method of treating Her-2 related cancers by administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis.

Monitoring of the inhibition of fatty acid synthesis by iodo-nitrobenzamide compounds

In one aspect, the present invention provides a method of treating breast cancer that is negative for at least one of ER, PR, or HER2, comprising administering to a subject at least one PARP inhibitor. In another aspect, the present invention provides a method of treating breast cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one anti-tumor agent.

Treatment of breast cancer with a PARP inhibitor alone or in combination with anti-tumor agents

The present invention relates to regulation of the cell cycle. More particularly, the present invention is directed to nucleic acids encoding components of the ubiquitin ligation pathway, e.g., ubiquitin and ubiquitin-like molecules, E1, E2, and E3 proteins and their substrates, which are involved in modulation of cell cycle arrest. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, RNAi, antisense nucleic acids, and ribozymes, that modulate cell cycle arrest via modulation of the ubiquitin ligation pathway; as well as to the use of expression profiles and compositions in diagnosis and therapy related to cell cycle regulation and modulation of cellular proliferation, e.g., for treatment of cancer and other diseases of cellular proliferation.

Methods of assaying for cell cycle modulators using components of the ubiquitin ligation cascade

The present invention relates to a computer-assisted method of a designing of a tubulin inhibitor comprising: a) determining an interaction between a tubulin protein and a chemical known to bind the tubulin protein by evaluating a binding of the tubulin protein to the chemical known to bind the tubulin protein; b) based on the interaction, designing a candidate tubulin inhibitor; c) determining an interaction between the tubulin protein and the candidate tubulin inhibitor by evaluating a binding of the tubulin protein to the candidate tubulin inhibitor; and d) concluding that the candidate tubulin inhibitor inhibits the tubulin protein wherein the conclusion is based on the interaction of step c). The invention also provides compositions and methods of treatment of diseases with the candidate tubulin inhibitors.

Drug design for tubulin inhibitors, compositions, and methods of treatment thereof

Methods of treating ovarian cancer, endometrium cancer, cervical cancer, pancreatic cancer, bladder cancer, eve cancer, central nervous system cancer, thyroid cancer and lung cancer are disclosed. Specifically disclosed are methods of treating ovarian adenocarcinoma that has migrated into the abdominal cavity, a transitional cell carcinoma of the bladder, an epithelioid carcinoma in a pancreatic duct, an adenocarcinoma in a pancreatic duct, an adenocarcinoma in the cervical epithelium. The methods comprise administering to a patient a therapeutically effective amount of a compound of formula (Ia) wherein R, R, R, R, and Rare described herein, wherein at least two of the five R, R, R, R, and Rsubstituents are always hydrogen, at least one of the five substituents is always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts thereof.

The present invention is directed to novel polypeptides, nucleic acids and related molecules which have an effect on or are related to the cell cycle. Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention. Further provided by the present invention are methods for identifying novel compositions which mediate cell cycle bioactivity, and the use of such compositions in diagnosis and treatment of disease.

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San Francisco, CA, United States of America

Valeria S Ossovskaya