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42 条记录 (耗时 0.057 秒)

    Phthalazine derivatives for treating inflammatory diseases
    6.
    发明授权
    Phthalazine derivatives for treating inflammatory diseases 失效
    用于治疗炎性疾病的酞嗪衍生物

    公开(公告)号：US06686347B2

    公开(公告)日：2004-02-03

    申请号：US09964025

    申请日：2001-09-26

    申请人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

    发明人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

    IPC分类号： A61K3133

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

    摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.

    摘要翻译： 本发明涉及治疗炎症性疾病，特别是炎性类风湿病或风湿性疾病，和/或具有式I的VEGF受体酪氨酸激酶的活性抑制剂的疼痛，所述取代基在本说明书中定义;以及 新的酞嗪衍生物; 制备方法; 其用于治疗人或动物体的过程中的应用; 其用于治疗疾病，特别是由眼睛新生血管形成引起的疾病，例如年龄相关性黄斑变性或糖尿病性视网膜病，或其它对酪氨酸激酶（例如增殖性疾病）的抑制作用的疾病; 哺乳动物治疗这种疾病的方法; 以及这种化合物用于制造特别是上述疾病的药物制剂的用途。

    Isoquinoline derivatives with angiogenesis inhibiting activity
    7.
    发明授权
    Isoquinoline derivatives with angiogenesis inhibiting activity 失效
    具有血管生成抑制活性的异喹啉衍生物

    公开(公告)号：US06608071B2

    公开(公告)日：2003-08-19

    申请号：US09781036

    申请日：2001-02-09

    申请人： Karl-Heinz Altmann ,  Guido Bold ,  Paul William Manley

    发明人： Karl-Heinz Altmann ,  Guido Bold ,  Paul William Manley

    IPC分类号： A61K31505

    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, alkylphenyl-sulfinyl, phenylsulfonyl, 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0至2; n为0〜2; m为0至4; A，B，D和E各自独立地为N或CH，条件是不多于两个这些基团为N; G为低级亚烷基，-CH 2 -O-， - CH2-，-CH2-NH-，氧杂（-O-），硫杂（-S-）或亚氨基（-NH-），或被酰氧基或羟基取代的低级亚烷基; Q是低级烷基， ; R为H或低级烷基; X为亚氨基，氧杂或硫杂; Y为低级烷基或特别是芳基，杂芳基或未取代或取代的环烷基; 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，N-二 - 取代的烷基， 取代的氨基甲酰基，脒基，胍基，巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯硫基，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 - 低级烷基磺酰基或烷基苯基磺酰基，其中如果多于一个基团Z 存在（m> = 2）时，取代基Z相同或不同;其中由波浪线表示的键为单键或双键;或所述化合物的N-氧化物，其中一个或多个N原子携带 氧原子;或其盐。 该化合物特别抑制血管生成。