TUBULIN BINDING LIGANDS AND CORRESPONDING PRODRUG CONSTRUCTS

Title:

TUBULIN BINDING LIGANDS AND CORRESPONDING PRODRUG CONSTRUCTS

Document Type and Number:

WIPO Patent Application WO2001068654

Kind Code:

A3

Abstract:

A diverse set of tubulin binding ligands have been discovered which are structural by 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, and phosphoramides capable of demonstrating selective targeting and destruction of tumor cell vasculature.

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Inventors:

PINNEY KEVIN G
MOCHARLA VANI P
CHEN ZHI
GARNER CHARLES M
GHATAK ANJAK
HADIMANI MALLINATH
KESSLER JIMMY
DORSEY JAMES M

Application Number:

PCT/US2001/007539

Publication Date:

February 28, 2002

Filing Date:

March 09, 2001

Export Citation:

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Assignee:

UNIV BAYLOR (US)

International Classes:

A61K31/09; A61K31/343; A61K31/381; A61K31/661; A61P17/06; A61P19/02; A61P27/02; A61P35/00; A61P35/02; A61P43/00; C07C43/215; C07C43/23; C07C45/51; C07C45/64; C07C49/84; C07C205/45; C07C217/84; C07C217/94; C07C225/22; C07D233/54; C07D307/80; C07D307/81; C07D333/56; C07D333/58; C07D333/64; C07F9/12; C07F9/18; C07F9/24; C07F9/655; C07F9/6553; (IPC1-7): C07F9/6553; C07D333/56; C07D333/58; C07C43/215; C07C217/94; C07C43/23; C07F9/24; C07F9/12; C07F9/18; C07C49/84; C07C225/22; C07D307/80; C07D307/81; C07F9/655; C07C217/84; C07D333/64; C07C45/51; A61K31/66; A61K31/381; A61K31/343; A61K31/075; A61K31/12; A61K31/13; A61P35/00; A61P27/02; A61P17/06; A61P19/02

Domestic Patent References:

WO1998039323A1	1998-09-11
WO2000048606A1	2000-08-24

Other References:

FLYNN, BERNARD L. ET AL: "A novel palladium-mediated coupling approach to 2,3-disubstituted benzo[b]thiophenes and its application to the synthesis of tubulin binding agents", ORG. LETT. (2001), 3(5), 651-654, - 8 March 2001 (2001-03-08), XP002171975
PINNEY, KEVIN G. ET AL: "Synthesis of a benzo [b]thiophene-based vascular targeting prodrug and related anti-tubulin ligands.", ABSTR. PAP. - AM. CHEM. SOC. (2000), 220TH, ORGN-196, August 2000 (2000-08-01), XP001014188

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