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35 条记录 (耗时 0.031 秒)

    PHTHALAZINE DERIVATIVES FOR TREATING INFLAMMATORY DISEASES
    4.
    发明授权
    PHTHALAZINE DERIVATIVES FOR TREATING INFLAMMATORY DISEASES 有权
    酞炎症性疾病的治疗

    公开(公告)号：EP1165085B1

    公开(公告)日：2006-06-14

    申请号：EP00920604.6

    申请日：2000-03-28

    申请人： Novartis AG ,  Novartis Pharma GmbH

    发明人： BOLD, Guido ,  DAWSON KING, Janet ,  FREI, Jörg ,  HENG, Richard ,  MANLEY, Paul, William ,  WIETFELD, Bernhard ,  WOOD, Jeanette, Marjorie

    IPC分类号： A61K31/50 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  A61P29/00 ,  A61P19/02

    CPC分类号： C07D401/06 ,  A61K31/501 ,  A61K31/502 ,  C07D401/14

    摘要： The invention relates to the treatment of an inflammatory disease, and/or pain with an inhibitor of VEGF receptor tyrosine kinase of formula (I), wherein r is 0 to 2, n is 0 to 3, R1 and R2 a) are independently in each case lower alkyl; b) together form a bridge of subformula (I*), wherein the bond is achieved via the two terminal C atoms and m is 0 to 4, or c) together form a bridge of subformula (I**), wherein one or two of the ring members T1, T2, T3 and T4 are nitrogen and the others are in each case CH, and the bond is achieved via atoms T1 and T4; G is -C(=O)-, CHF-, -CF2-, lower alkylene, C2-C6alkenylene, lower alkylene or C3-C6alkenylene substituted by acyloxy or hydroxy, -CH2-O-, -CH2-S-, -CH2-NH-, -CH2-O-CH2-, -CH2-S-CH2-, -CH2-NH-CH2-, oxa (-O-), thia (-S-), imino (-NH-), -CH2-O-CH2-, -CH2-S-CH2- or -CH2-NH-CH2-; A, B, D, E and T are independently N or CH subject to the proviso that at least one and not more than three of these radicals are N; Q is lower alkyl, lower alkoxy or halogen; Ra and Ra' are each independently H or lower alkyl; X is imino, oxa, or thia; Y is hydrogen, aryl, heteroaryl, or unsubstituted or substituted cycloalkyl; and Z is mono- or disubstituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono-or N, N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, alkylphenylsulfonyl, or (alternatively or, in a broader aspect of the invention, in addition) selected from the group consisting of ureido, halo-lower alkylthio, halo-lower alkansulfonyl, pyrazolyl, lower-alkyl pyrazolyl and C2-C7alkenyl; wherein - if more than 1 radical Z (m ≥ 2) is present - the substituents Z are selected independently from each other; and wherein the bonds characterized in subformula (I) by a wavy line are either single or double bonds; or an N-oxide of said compound, wherein 1 or more N atoms carry an oxygen atom; or a pharmaceutically acceptable salt thereof.

    ANTHRANILIC ACID AMIDES AND PHARMACEUTICAL USE THEREOF
    6.
    发明公开
    ANTHRANILIC ACID AMIDES AND PHARMACEUTICAL USE THEREOF 有权
    邻氨基和它们的药物用途

    公开(公告)号：EP1446381A1

    公开(公告)日：2004-08-18

    申请号：EP02779536.8

    申请日：2002-11-07

    申请人： Novartis AG ,  Novartis Pharma GmbH

    发明人： BOLD, Guido ,  FURET, Pascal ,  MANLEY, Paul, William

    IPC分类号： C07D213/38 ,  C07D213/89 ,  C07C237/40 ,  A61K31/44 ,  A61K31/165 ,  A61P35/00

    CPC分类号： C07C237/40 ,  C07D213/38 ,  C07D213/89

    摘要： The invention relates to anthranilic acid amide derivatives of formula (I), wherein Ar is represented by the subformula (Ia), wherein Ra represents H or lower alkyl, and R1 represents H or perfluoro lower alkyl, R2 represents H, halogen, C2-C7alkyl, C2-C7alkenyl or lower aklynyl; or Ar is represented by the subformula (Ib) and R1 represents perfluoro lower alkyl, and R2 represents bromo, iodo, C2-C7alkyl, C2-C7alkenyl or lower alkynyl, or R1 represents H, and R2 represents fluoro, bromo, iodo, ethyl, C5-C7alkyl, C2-C7alkenyl or lower alkynyl; to N-oxides and tautomers thereof, and to salts of such anthranilic acid amides, its N-oxides and tautomers; to processes for their preparation; to their application in the treatment of the human or animal body, to 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; to a method for the treatment of such diseases in animals; and to 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.

    PHTHALAZINE DERIVATIVES WITH ANGIOGENESIS INHIBITING ACTIVITY
    7.
    发明公开
    PHTHALAZINE DERIVATIVES WITH ANGIOGENESIS INHIBITING ACTIVITY 有权
    与血管生成抑制作用酞嗪衍生物

    公开(公告)号：EP1387836A1

    公开(公告)日：2004-02-11

    申请号：EP02738031.0

    申请日：2002-05-03

    申请人： Novartis AG ,  Novartis Pharma GmbH

    发明人： BOLD, Guido ,  MANLEY, Paul, William

    IPC分类号： C07D401/06 ,  C07D405/12 ,  C07D409/12 ,  A61K31/502 ,  A61P29/00 ,  A61P19/02

    CPC分类号： C07D401/06 ,  C07D405/12 ,  C07D409/12

    摘要： The invention relates to new phthalazine derivatives of formula (I), wherein R1 and R2: a) are independently in each case a lower alkyl; b) together form a bridge of subformula (I*), wherein the bond is achieved via the two terminal C atoms and m is 0 to 4; or c) together form a bridge of subformula (I**), wherein one or two of the ring members T1, T2, T3 and T4 are nitrogen, and the others are in each case CH, and the bond is achieved via atoms T1 and T4; A, B, D, E and T are independently N or CH subject to the proviso that at least one and not more than three of these radicals are N; X is imino, oxa, or thia; Y is hydrogen, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or unsubstituted or substituted cycloalkyl; and wherein the bonds characterized in subformula (I*) by a wavy line are either single or double bonds; to an N-oxide of a compound of formula I; a tautomer or mixture of tautomers of a compound of formula (I) of an N-oxide thereof; and a pharmaceutically acceptable salt of a compound of formula (I), of an N-oxide or of a tautomer ormixture of tautomers thereof; processes for their preparation and pharmaceutical uses.

    2-AMINO-NICOTINAMIDE DERIVATIVES AND THEIR USE AS VEGF-RECEPTOR TYROSINE KINASE INHIBITORS
    8.
    发明授权
    2-AMINO-NICOTINAMIDE DERIVATIVES AND THEIR USE AS VEGF-RECEPTOR TYROSINE KINASE INHIBITORS 有权
    2-氨基烟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：EP1259487B1

    公开(公告)日：2009-12-23

    申请号：EP01946854.5

    申请日：2001-01-25

    申请人： Novartis AG ,  Novartis Pharma GmbH

    发明人： MANLEY, Paul, William ,  BOLD, Guido

    IPC分类号： C07D213/82 ,  C07D213/89 ,  C07D401/14 ,  A61K31/455 ,  A61P35/00

    CPC分类号： C07D213/82 ,  A61K31/445 ,  C07D213/89 ,  C07D401/14 ,  C07D417/14

    摘要： The invention relates to the use of 2-amino-nicotinamide derivatives of formula (I) wherein n is from 1 up to and including 6; W is O or S; R1 and R3 represent independently of each other hydrogen, lower alkyl or lower acyl; R2 represents a cycloalkyl group, an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; R and R' are independently of each other hydrogen or lower alkyl; X represents an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; or a N-oxide, a possible tautomer thereof or a pharmaceutically acceptale salt of such a compound, alone or in combination with one or more other pharmaceutically active compounds for the preparation of a pharmaceutical composition for use for therapy of a disease which responds to an inhibition of the VEGF-receptor tyrosine kinase activity; and to new 2-amino-nicotinamide derivatives of formula (I) and processes for the preparation thereof.