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42 条记录 (耗时 0.037 秒)

    Pyridine derivatives inhibiting angiogenesis and/or VEGF receptor tyrosine kinase
    6.
    发明授权
    Pyridine derivatives inhibiting angiogenesis and/or VEGF receptor tyrosine kinase 失效
    抑制血管发生和/或VEGF受体酪氨酸激酶的吡啶衍生物

    公开(公告)号：US06706731B2

    公开(公告)日：2004-03-16

    申请号：US10203579

    申请日：2002-10-11

    申请人： Guido Bold ,  Paul William Manley

    发明人： Guido Bold ,  Paul William Manley

    IPC分类号： C07D47104

    CPC分类号： C07D401/06 ,  C07D471/04

    摘要： The invention relates to pyridine derivatives of formula I: wherein the substituents and symbols are defined as indicated in the description, processes for the preparation thereof, their usage in the preparation of a pharmaceutical composition for the treatment of a disease which responds to an inhibition of angiogenesis, and pharmaceutical compositions containing such compounds.

    摘要翻译： 本发明涉及式I的吡啶衍生物：其中取代基和符号如说明书所述定义，其制备方法，它们在制备用于治疗对抑制作用的疾病的药物组合物中的用途 血管生成和含有这些化合物的药物组合物。

    2-amino-nicotinamide derivatives and their use as VEGF-receptor tyrosine kinase inhibitors
    7.
    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的用途

    公开(公告)号：US06624174B2

    公开(公告)日：2003-09-23

    申请号：US10181005

    申请日：2002-07-11

    申请人： Paul William Manley ,  Guido Bold

    发明人： Paul William Manley ,  Guido Bold

    IPC分类号： C07D21382

    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 acceptable 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.

    摘要翻译： 本发明涉及式I的2种氨基 - 烟酰胺衍生物的用途，其中n为1至6，W为O或S; R 1和R 3彼此独立地为氢，低级烷基或低级酰基; R 2表示 环烷基，芳基或包含一个或多个环氮原子和0,1或2个彼此独立地选自氧和硫的杂原子的单环或双环杂芳基，这些基团在每种情况下是未取代的 或单取代或多取代; R和R'彼此独立地为氢或低级烷基; X表示芳基，或单环或双环杂芳基，其包含一个或多个环氮原子和0,1或2个独立地为 彼此选自氧和硫，这些基团在每种情况下都是未取代的或单取代或多取代的;或N-氧化物，其可能的互变异构体或这种化合物的药学上可接受的盐，alo ne或与一种或多种其它药学活性化合物组合用于制备用于治疗对VEGF-受体酪氨酸激酶活性的抑制作出反应的疾病的药物组合物;以及新的2-氨基 - 烟酰胺衍生物 式I及其制备方法。

    Phthalazine Derivatives with Angiogenesis Inhibiting Activity
    8.
    发明申请
    Phthalazine Derivatives with Angiogenesis Inhibiting Activity 审中-公开
    具有血管发生抑制活性的酞嗪衍生物

    公开(公告)号：US20090076003A1

    公开(公告)日：2009-03-19

    申请号：US12141179

    申请日：2008-06-18

    申请人： Guido Bold ,  Paul William Manley

    发明人： Guido Bold ,  Paul William Manley

    IPC分类号： A61K31/5377 ,  C07D237/30 ,  A61K31/498 ,  A61P29/00 ,  A61P35/00 ,  C07D413/14

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

    摘要： The invention relates 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 alone or in combination with one or more other pharmaceutically active compounds for the treatment of a disease, especially of a disease that responds to the inhibition of tyrosine kinases, more especially the inhibition of the vascular endothelial growth factor (VEGF) receptor kinase, preferably the treatment of a proliferative disease, such as a tumour disease.

    摘要翻译： 本发明涉及新的酞嗪衍生物，其制备方法，其在治疗人或动物体的方法中的应用，其单独使用或与一种或多种其它药物活性化合物组合用于治疗 疾病，特别是对酪氨酸激酶的抑制作出反应的疾病，更特别地抑制血管内皮生长因子（VEGF）受体激酶，优选治疗增殖性疾病如肿瘤疾病。

    Isoquinoline derivatives with angiogenesis inhibiting activity
    10.
    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。