PYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE

Title:

PYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE

Document Type and Number:

WIPO Patent Application WO2003053366

Kind Code:

A3

Abstract:

The subject invention provides compounds having the structure:, wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; R12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.

Inventors:

CASTELHANO ARLINDO (US)
MCKIBBEN BRYAN (US)
STEINIG ARNO (US)
COLLINGTON ERIC WILLIAM (GB)

Application Number:

PCT/US2002/041273

Publication Date:

January 29, 2004

Filing Date:

December 20, 2002

Export Citation:

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Assignee:

OSI PHARM INC (US)
CASTELHANO ARLINDO (US)
MCKIBBEN BRYAN (US)
STEINIG ARNO (US)
COLLINGTON ERIC WILLIAM (GB)

International Classes:

A61K31/506; A61K31/513; A61K31/519; A61K31/5377; A61K31/55; A61K31/551; A61P1/00; A61P1/12; A61P3/10; A61P9/00; A61P9/10; C07D243/08; A61P9/12; A61P11/06; A61P17/00; A61P17/04; A61P19/02; A61P27/02; A61P35/00; A61P37/08; A61P43/00; C07D239/42; C07D239/48; C07D401/12; C07D401/14; C07D403/12; C07D405/12; C07D405/14; C07D409/12; C07D409/14; C07D411/12; C07D413/12; C07D417/12; C07D471/10; C07D487/04; (IPC1-7): A61K31/495; A61K31/50; A61K31/505; A61K31/535; A61K31/55; A61P9/00; C07D239/02; C07D243/08; C07D403/00; C07D413/00; C07D473/00

Domestic Patent References:

WO1999064407A1

1999-12-16

Other References: