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    ISOQUINOLINE DERIVATIVES WITH ANGIOGENESIS INHIBITING ACTIVITY
    3.
    发明授权
    ISOQUINOLINE DERIVATIVES WITH ANGIOGENESIS INHIBITING ACTIVITY 有权
    具有血管生成抑制活性的异喹啉衍生物

    公开(公告)号：EP1107964B8

    公开(公告)日：2010-04-07

    申请号：EP99942827.9

    申请日：1999-08-09

    申请人： Novartis AG

    发明人： ALTMANN, Karl-Heinz ,  BOLD, Guido ,  MANLEY, Paul, William

    IPC分类号： C07D401/06 ,  A61K31/4725 ,  C07D401/14 ,  C07D401/12 ,  C07D405/14

    CPC分类号： C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

    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.

    摘要翻译： 本发明涉及式（I）的化合物，其中r为0-2; n是从0到2; m为0至4; A，B，D和E各自独立于其它N或CH，条件是这些基团中不超过两个是N; G是低级亚烷基，-CH 2 -O-，-CH 2 -S-，-CH 2 -NH-，氧杂（-O-），硫杂（-S-）或亚氨基（-NH-），或者是被 酰氧基或羟基; Q是低级烷基，特别是甲基; R是H或低级烷基; X是亚氨基，氧杂或硫杂; Y是低级烷基或尤其是芳基，杂芳基或未取代或取代的环烷基; 和Z是氨基，一或二取代的氨基，卤素，烷基，取代的烷基，羟基，醚化或酯化的羟基，硝基，氰基，羧基，酯化的羧基，烷酰基，氨基甲酰基，N-单或N， 巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯基硫基，苯基亚磺酰基，苯基 - 低级烷基亚磺酰基，烷基苯基亚磺酰基，苯基磺酰基，苯基 - 低级链烷磺酰基或烷基苯基磺酰基，并且如果存在多于一个基团Z （m≥2）时，取代基Z相同或不同; 并且其中由波浪线表示的键是单键或双键; 或所述化合物的N-氧化物，其中一个或多个N原子带有氧原子; 或其盐。 这些化合物特别抑制血管生成。

    PHTHALAZINE DERIVATIVES FOR TREATING INFLAMMATORY DISEASES
    5.
    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
    7.
    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
    8.
    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.