Baylor University

Oxigene, Inc.

Mateon Therapeutics, Inc.

Other

Kevin G Pinney

David J Chaplin

Klaus Edvardsen

Joseph Anthony Prezioso

Vani P Mocharla

Zhi Chen

Robert Ronald Kane

James Michael Dorsey

Charles Manly Garner, Iii

Mary Lynn Trawick

Kishore Kumar Gaddale Devanna

Anupama Shirali

Mallinath Hadimani

Jiangli Song

Erica Parker

George R Pettit

Charles M Garner

Madhavi Sriram

Ming Zhou

Ronald W Pero

David I Sherris

Jimmy Kessler

Haichan Niu

Usha R Ghatak, Legal Representative

Feng Wang

Anjan Ghatak

Maria Del Pilar Mejia

Maria Del Mejia

Usha Ghatak, Legal Representative

Raymond Kessler

Phyllis Arthasary

Maria Graciela Miranda

Wara Milenka Arispe-Angulo

Shen-En Chen

J Freeland Ackley

Rogelio Siles

Mark Wood

Deboprosad Mondal

Kumar Kishore Gaddale Devanna

A series of benzosuberene analogues demonstrate effective inhibition of tubulin polymerization, cytotoxicity against human cancer cell lines, and vascular disruption in tumors.

Benzosuberene analogues and related compounds with activity as anticancer agents

This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful. 

Compositions and methods for inhibition of cathepsins

Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.

Functionalized stilbene derivatives as improved vascular targeting agents

Analogs of combretastatin have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.

Combretastatin analogs with tubulin binding activity

Novel quinone and catechol compositions, compositions containing prodrugs of quinone and catechol compositions, and methods of use for the treatment of solid tumor cancers and other vascular proliferative disorders. The disclosure particularly relates to the discovery of dual activity agents capable of generating both a vascular targeting effect and direct tumor cell cytotoxicity in order to achieve an enhanced anti-tumor response in a patient.

Compositions and methods with enhanced therapeutic activity

The present invention relates to semicarbazone or thiosemicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.

Inhibitors of cysteine proteases and methods of use thereof

A serotonin reuptake inhibitor which can be used in the treatment of depression and which has a decreased occurrence of unwanted side effects. The serotonin reuptake inhibitors are bi-functional organic molecules which combine serotonin transporter reuptake inhibition with serotonin (5-HT, such as 5-HT2A) receptor antagonism in one molecular entity. The serotonin-selective reuptake inhibitor (SSRI) homologue portion of the molecule shows an affinity to the serotonin reuptake transporter (SERT) and has antidepressant properties. The piperazine or piperidine portion of the molecule demonstrates an affinity to 5-HT receptors and restores the undesired side effects of SSRIs.

Serotonin reuptake inhibitors

Chrome compounds have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.

Chromene-containing compounds with anti-tubulin and vascular targeting activity

A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.

Tubulin binding ligands and corresponding prodrug constructs

Tubulin binding agents and corresponding prodrug constructs

Growing community of inventors

Woodway, TX, United States of America

Kevin G Pinney