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(11)    Patent No :    AP 1997   
(21)    Application No :    AP/P/2005/003350   
(22)    Filing Date :    19.12.2003   
(24)    Date of Grant &    22.04.2009   
(45)    Publication :

(30)  Priority Data       
(33) Country    (31) Number    (32) Date
US    60/437,505    31.12.2001

(84)    Designated State

GM    GH    KE   LS   MW  MZ   SL   SD   SZ
T Z    UG    ZW

(73) Applicant(s)

PFIZER PRODUCTS INC., Eastern Point Road, Groton,

Connecticut 06340,
United States of America

(72) Inventors

DOMBROSKI Mark Anthony, United States of


DUPLANTIER Allen Jacob, United States of America

(74) Representative

(51) International Classification A61K 31/53 (2006.01) C07D31//5377 (2006.01) A61P 19/02 (2006.01)

(54)    Title

3-(3,5-dioxo-4,5-dihydro-3H-(1,2,4)triazin-2-YL)-benzamide derivatives as P2X7 -inhibitors for the treatment of inflammatory

(57)    Abstract

The present invention provides benzamide inhibitors of the P2X7; receptor of the formula

(I), wherein R1 and R2 are as defined in claim 1. R3 is a nitrogen linked (C1 -C10) heterocyclyl of formula

(II), wherein R4 and R7 are as defined in claim 1. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma. COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

(56)  Documents Cited :    WO 00 61569 A


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