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(11)    Patent No :    AP 1917   
(73) Applicant(s)    AVENTIS PHARMA LIMITED, Aventis House, 50 Kings Hill       
            Avenue, West Mailling, ME19 4AH, Kent,       
(21)    Application No :    AP/P/2006/003492       
                   
(22)    Filing Date :    27.12.2000    United Kingdom       
(24)    Date of Grant &    12.11.2008           
                   
(45)    Publication :

(30)  Priority Data    (72) Inventors

    (33) Country    (31) Number    (32) Date    COX Paul Joseph, United States of America   
    GB            9930698.7    24.12.1999    MAJID Tahir Nadeem, United Kingdom   
    US            60/215,818    05.07.2000       
                        EDLIN Chris, United Kingdom   
                           
                        et al       
                        (74) Representative   
(84)    Designated State           
                   
    GM    GH    KE    LS   MW  MZ    SL   SD   SZ    FISHER CORMACK & BOTHA   
    T Z    UG    ZW                   
(51)    International    Classification    C07D471/04 (2006.01)    C07D487/04 (2006.01)   
                    C07D519/00(2006.01)       


(54)    Title

Azaindoles.

(57)    Abstract

The invention is directed to compositions containing physiologically active compounds of general formula (I) wherein R1 is aryl or heteroaryl: R2 represent hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z1R8,-C(=O)-NY3Y4,-CO2R8, -N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4,-N(R6)-C(=O) -R7,-N(R6)-SO2-R7,-N(R6)-SO2-NY3Y4 and one or more halogen atoms; R3 represents hydrogen, aryl, cyno, halo, heteroaryl, lower

alkyl,-C(=O) -OR5 or -C(=O)-NY3Y4; C-N(R8)-C(=O)-R7, C-SO2-NY3Y4, C-N(R8)-SO2-R7, and X1 represents N.CH, C-halo, C-CN, C-R7,CNY3Y4, C-OH,C-Z2R7, C-C(=O)-OR5, C-C(=O)-NY3Y4, C-N(R8)-C(=O)-7,C-SO2_NY3Y4, C_N(R8)-SO2-R7,C-alkenyl or C-NO2; and their produgs, and pharmaceutically acceptable salts and solvates of such compounds and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of fomula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.



(56)    Documents Cited :    WO 9920624 A    EP 0 737 685 A    WO 98 47899 A    WO 98 22457 A

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