Sri International

La Jolla Cancer Research Foundation

The United States Government as Represented by the Department of Veterans Affairs

Wayne State University

Oregon State University

Sanford-Burnham Medical Research Institute

The Burnham Institute

Molecular Medicine Research Institute

Ling Jong

Wan-Ru Chao

Masato Tanabe

Richard H Peters

Peter D Hobbs

Xiao-kun Zhang

James F Cameron

Magnus Pfahl

Marcia I Dawson

Jurgen M Lehmann

Faming Jiang

Marcia L Dawson

Mark Leid

Kristien Mortelmans

Joseph A Fontana

Gaoquan Li

Jaehyeon Park

J Urgen Lehmann

Chih-Tsung Chang

Xiao-Kun Zhang

Marcia Dawson

Wan Ru Chao

The disclosure provides bisindole suitable for inhibiting lipoxygenases or A&#x3b2;-formation, and treating associated diseases, such as Alzheimer's disease. The bisindoles are indolo[2,3-b]carbazole derivatives, and may be administered to a patient as part of a pharmaceutical formulation.

Lipoxygenase inhibitors

The invention provides mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) inhibitors, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant diminution of tumor cell growth, cancer or metastasis.

MAP4K4 (HGK) inhibitors

Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2'-diindolylmethane, 2&#x2032;,3-diindolylmethane, and 3,3&#x2032;-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.

Analogs of indole-3-carbinol and their use as agents against infection

The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.

Induction of apoptosis in cancer cells

Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds has the structure of formula (IV) wherein:

Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents

Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (III) wherein R, R, R, R, R, R, R, R, R, R, R, and Rare defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.

Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (I) wherein R, R, R, R, R, R, R, R, R, R, R, and Rare defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.

The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.

Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.

Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use

Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5(10)-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5(10)-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.

Growing community of inventors

Sunnyvale, CA, United States of America

Ling Jong