TRIAZOLE DERIVATIVES AND THEIR USE AS PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONISTS

Title:

TRIAZOLE DERIVATIVES AND THEIR USE AS PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONISTS

Document Type and Number:

WIPO Patent Application WO2002038553

Kind Code:

A3

Abstract:

he present invention is directed to compounds represented by the following structural formula (I'), and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.

Inventors:

MANTLO NATHAN BRYAN (US)
COLLADO CANO IVAN (ES)
DOMINIANNI SAMUEL JAMES (US)
ETGEN GARRET JAY JUNIOR (US)
GARCIA-PAREDES CRISTINA (ES)
JOHNSTON RICHARD DUANE (US)
LETOURNEAU MICHAEL EDWARD (US)
MARTINELLI MICHAEL JOHN (US)
MAYHUGH DANIEL RAY (US)
SAEED ASHRAF (US)
THOMPSON RICHARD CRAIG (US)
WANG XIADONG (US)
COFFEY DAVID SCOTT (US)
SCHMID CHRISTOPHER RANDALL (US)
VICENZI JEFFREY THOMAS (US)
XU YANPING (US)

Application Number:

PCT/US2001/042928

Publication Date:

May 01, 2003

Filing Date:

November 09, 2001

Export Citation:

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Assignee:

LILLY CO ELI (US)
MANTLO NATHAN BRYAN (US)
COLLADO CANO IVAN (ES)
DOMINIANNI SAMUEL JAMES (US)
ETGEN GARRET JAY JUNIOR (US)
GARCIA-PAREDES CRISTINA (ES)
JOHNSTON RICHARD DUANE (US)
LETOURNEAU MICHAEL EDWARD (US)
MARTINELLI MICHAEL JOHN (US)
MAYHUGH DANIEL RAY (US)
SAEED ASHRAF (US)
THOMPSON RICHARD CRAIG (US)
WANG XIADONG (US)
COFFEY DAVID SCOTT (US)
SCHMID CHRISTOPHER RANDALL (US)
VICENZI JEFFREY THOMAS (US)
XU YANPING (US)

International Classes:

A61K31/4196; A61K31/42; A61K31/4245; A61K31/4439; A61K31/4709; A61K31/5377; A61P3/00; A61P3/04; A61P3/06; A61P3/10; A61P9/00; A61P43/00; C07C257/22; C07C281/04; C07C281/06; C07D249/12; C07D401/06; C07D403/12; C07D405/06; C07D405/12; C07D407/06; C07D409/06; C07D409/12; C07D413/06; C07D417/12; (IPC1-7): C07D249/12; A61K31/4196; C07D401/06; C07D413/06; C07D409/06; C07D409/12; C07D417/12; C07D405/06; A61K31/4439; A61K31/427; C07C257/22; C07C281/04; C07C281/06

Domestic Patent References:

WO1996035680A1	1996-11-14
WO1996013264A1	1996-05-09
WO2001040207A1	2001-06-07
WO1999008501A2	1999-02-25

Foreign References:

EP1028111A1

2000-08-16

Other References:

T.M.WILLSON ET AL: "The structure-activity relationship between PPAR-gamma agonism and the antihyperglycemic activity of thiazolidinediones", JOURNAL OF MEDICINAL CHEMISTRY, vol. 39, no. 3, 1996, pages 665 - 668, XP002007700

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