ANTHRANILIC ACID AMIDES AND THEIR USE AS VEGF RECEPTOR TYROSINE KINASE INHIBITORS
    2.
    发明授权
    ANTHRANILIC ACID AMIDES AND THEIR USE AS VEGF RECEPTOR TYROSINE KINASE INHIBITORS 有权
    邻氨基苯甲酰胺衍生物及其作为VEGF受体酪氨酸激酶抑制剂

    公开(公告)号:EP1446382B1

    公开(公告)日:2011-01-26

    申请号:EP02787595.4

    申请日:2002-11-07

    申请人: Novartis AG

    CPC分类号: C07D213/64 C07D213/70

    摘要: The invention relates to anthranilic acid amide derivatives of formula (I), wherein R1 represents H or lower alkyl, R2 represents H or lower alkyl, R3 represents perfluoro lower alkyl, and X is O or S, or an N-oxide or a tautomer thereof, to salts of such anthranilic acid amides, their N-oxides and their tautomers; processes for the preparation thereof, the application thereof for the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age - related macular degeneration; a method for the treatment of such a disease in animals, especially in humans, and the use of such a compound-alone or in combination with one or more other pharmaceutically active compounds - for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.

    INHIBITORS OF TYROSINE KINASES
    4.
    发明公开
    INHIBITORS OF TYROSINE KINASES 有权
    酪氨酸激酶抑制剂

    公开(公告)号:EP1532138A1

    公开(公告)日:2005-05-25

    申请号:EP03762632.2

    申请日:2003-07-04

    IPC分类号: C07D401/14

    CPC分类号: C07D401/14 C07D405/14

    摘要: The invention relates to compounds of formula (I) Wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such disease.

    4-AMINO-5-PHENYL-7-CYCLOBUTYL-PYRROLO(2,3-D)PYRIMIDINE DERIVATIVES
    6.
    发明公开
    4-AMINO-5-PHENYL-7-CYCLOBUTYL-PYRROLO(2,3-D)PYRIMIDINE DERIVATIVES 有权
    5-氨基-5-苯基-7-环丁基 - 吡咯并(2,3-D)嘧啶衍

    公开(公告)号:EP1390369A1

    公开(公告)日:2004-02-25

    申请号:EP02738065.8

    申请日:2002-05-13

    IPC分类号: C07D487/04 A61P35/00

    CPC分类号: C07D487/04

    摘要: The invention relates to new 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof-alone or in combination with one or more other pharmaceutically active compounds-for the treatment of a disease, especially a proliferative disease, such as a tumour disease, a method for the treatment of such diseases in mammals, especially in humans, and the use of such a compound-alone or in combination with one or more other pharmaceutically active compounds-for the preparation of a pharmaceutical composition (medicament) for the treatment especially of a proliferative disease, such as a tumour.

    ISOQUINOLINE DERIVATIVES WITH ANGIOGENESIS INHIBITING ACTIVITY
    8.
    发明授权
    ISOQUINOLINE DERIVATIVES WITH ANGIOGENESIS INHIBITING ACTIVITY 有权
    异喹啉与血管生成锁效果衍生物

    公开(公告)号:EP1107964B1

    公开(公告)日:2010-03-03

    申请号:EP99942827.9

    申请日:1999-08-09

    申请人: Novartis AG

    摘要: The invention relates to compounds of formula (I) wherein r is from 0 to 2; n is from 0 to 2; m is from 0 to 4; A, B, D and E are each independently of the others N or CH, with the proviso that not more than two of those radicals are N; G is lower alkylene, -CH2-O-, -CH2-S-, -CH2-NH-, oxa (-O-), thia (-S-) or imino (-NH-), or is lower alkylene substituted by acyloxy or by hydroxy; Q is lower alkyl, especially methyl; R is H or lower alkyl; X is imino, oxa or thia; Y is lower alkyl or, especially, aryl, heteroaryl or unsubstituted or substituted cycloalkyl; and Z is amino, mono- or di-substituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-di-substituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulphonyl, phenyl-lower alkanesulfonyl or alkylphenylsulfonyl, and where, if more than one radical Z is present (m≥2), the substituents Z are identical or different; and wherein the bonds indicated by a wavy line are either single bonds or double bonds; or an N-oxide of the mentioned compound, wherein one or more N atoms carry an oxygen atom; or a salt thereof. The compounds inhibit especially angiogenesis.

    INHIBITORS OF TYROSINE KINASES
    10.
    发明授权
    INHIBITORS OF TYROSINE KINASES 有权
    酪氨酸激酶抑制剂

    公开(公告)号:EP1532138B1

    公开(公告)日:2008-11-19

    申请号:EP03762632.2

    申请日:2003-07-04

    IPC分类号: C07D401/14

    CPC分类号: C07D401/14 C07D405/14

    摘要: The invention relates to compounds of formula (I) Wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such disease.