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178 条记录 (耗时 0.052 秒)

    Pyrazole derivatives and processes for the preparation thereof
    1.
    发明授权
    Pyrazole derivatives and processes for the preparation thereof 失效
    吡唑衍生物及其制备方法

    公开(公告)号：US5981533A

    公开(公告)日：1999-11-09

    申请号：US930904

    申请日：1997-10-03

    申请人： Peter Traxler ,  Pascal Furet ,  Guido Bold ,  Jorg Frei ,  Marc Lang

    发明人： Peter Traxler ,  Pascal Furet ,  Guido Bold ,  Jorg Frei ,  Marc Lang

    IPC分类号： C07D231/38 ,  A61K31/505 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula I ##STR1## wherein the symbols are as defined in claim 1, and intermediates for their manufacture are described.The compounds of formula I inhibit especially the tyrosine kinase activity of the receptor for epidermal growth factor and can be used, for example, in the case of epidermal hyperproliferation (psoriasis) and as anti-tumor agents.

    摘要翻译： PCT No.PCT / EP96 / 01263。 371日期1997年10月3日第 102（e）日期1997年10月3日PCT 1996年3月22日PCT公布。 公开号WO96 / 31510PC。 日期：19964年10月10日 - 描述了式I的氨基-1H-吡唑并[3,4-d]嘧啶衍生物，其中符号如权利要求1中所定义，其中描述其制备方法。 式I的化合物特别地抑制表皮生长因子受体的酪氨酸激酶活性，并且可以用于例如表皮过度增生（牛皮癣）和作为抗肿瘤剂的情况。

    Cyclic diaryl ureas suitable as tyrosine kinase inhibitors
    5.
    发明授权
    Cyclic diaryl ureas suitable as tyrosine kinase inhibitors 失效
    适合作为酪氨酸激酶抑制剂的环状二芳基脲

    公开(公告)号：US07855215B2

    公开(公告)日：2010-12-21

    申请号：US11575601

    申请日：2005-09-27

    申请人： Guido Bold ,  Giorgio Caravatti ,  Andreas Floersheimer ,  Pascal Furet ,  Paul W Manley ,  Carole Pissot Soldermann ,  Andrea Vaupel

    发明人： Guido Bold ,  Giorgio Caravatti ,  Andreas Floersheimer ,  Pascal Furet ,  Paul W Manley ,  Carole Pissot Soldermann ,  Andrea Vaupel

    IPC分类号： A61K31/505 ,  A61K31/506 ,  C07D239/02 ,  C07D401/12 ,  C07D413/12

    CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14

    摘要： The invention relates to novel compounds of Formula I: wherein p is 1, 2 or 3; n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; A is CRc, S, NRc or O, where Rc is H or lower alkyl; X, Y and Z are each independently selected from N or C—R3, wherein at least two of X, Y and Z are N; and each Ra is independently selected from hydrogen and lower-alkyl; each Rb is hydrogen or lower-alkyl; G is a group Ar or represents CN or unsubstituted or substituted lower alkyl; Ar is a saturated or unsaturated cyclic group, which is substituted or unsubstituted and maybe a five or six membered monocyclic or a 8, 9, 10, 11 or 12 membered bicyclic or tricyclic ring and may contain 0, 1, 2 or 3 heteroatoms selected from O, N and S; and wherein the radicals have R1, R2, R3 and R4 have the meanings as defined herein, to salts, esters, N-oxides or prodrugs thereof; and their use in the treatment of protein kinase dependent diseases, their use in the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diary urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.

    摘要翻译： 本发明涉及式I的新化合物：其中p是1,2或3; n为0,1,2或3; m为0,1,2或3; A是CRc，S，NRc或O，其中Rc是H或低级烷基; X，Y和Z各自独立地选自N或C-R 3，其中X，Y和Z中的至少两个是N; 并且每个R a独立地选自氢和低级烷基; 每个R b是氢或低级烷基; G是基团Ar或代表CN或未取代或取代的低级烷基; Ar是饱和或不饱和的环状基团，其是取代或未取代的，并且可以是五或六元单环或8,9,10,11或12元双环或三环，并且可以含有0,1,2或3个选自 来自O，N和S; 并且其中所述基团的R1，R2，R3和R4具有如本文所定义的含义，其盐，酯，N-氧化物或前药; 以及它们在治疗蛋白激酶依赖性疾病中的应用，它们在制备用于治疗所述疾病的药物组合物中的应用，用于治疗所述疾病的日用脲衍生物的使用方法，包含这些新型二芳基脲 衍生物，制备新型二芳基脲衍生物的方法，上述新型二芳基脲衍生物的使用或使用方法，和/或这些新型二芳基脲衍生物用于动物或人体的治疗。

    Pyrimidinyl Aryl Urea Derivatives Being Fgf Inhibitors
    7.
    发明申请
    Pyrimidinyl Aryl Urea Derivatives Being Fgf Inhibitors 有权
    作为Fgf抑制剂的嘧啶基芳基脲衍生物

    公开(公告)号：US20080312248A1

    公开(公告)日：2008-12-18

    申请号：US12158873

    申请日：2006-12-20

    申请人： Guido Bold ,  Pascal Furet ,  Vito Guagnano

    发明人： Guido Bold ,  Pascal Furet ,  Vito Guagnano

    IPC分类号： A61K31/5377 ,  C07D413/12 ,  A61K31/506 ,  C07D403/12 ,  A61K31/505 ,  C07D239/28 ,  A61P43/00

    CPC分类号： C07D239/48 ,  C07D401/12

    摘要： The invention relates to heteroaryl aryl ureas of the formula IA, wherein the radicals and symbols have the meanings as defined herein, the use of such compounds in the treatment of protein kinase dependent diseases; to pharmaceutical preparations comprising said heteroaryl aryl ureas, to processes for the manufacture of such novel compounds and to methods of treatment comprising the use of such heteroaryl aryl ureas.

    摘要翻译： 本发明涉及式IA的杂芳基芳基脲，其中基团和符号具有本文定义的含义，这些化合物在治疗蛋白激酶依赖性疾病中的用途; 涉及包含所述杂芳基芳基脲的药物制剂，以及制备这些新化合物的方法和包括使用这种杂芳基芳基脲的治疗方法。

    Anthranilic acid amides and their use as VEGF receptor tyrosine kinase inhibitors
    8.
    发明授权
    Anthranilic acid amides and their use as VEGF receptor tyrosine kinase inhibitors 失效
    邻氨基苯甲酸酰胺及其作为VEGF受体酪氨酸激酶抑制剂的用途

    公开(公告)号：US07482369B2

    公开(公告)日：2009-01-27

    申请号：US11374720

    申请日：2006-03-14

    申请人： Guido Bold ,  Pascal Furet ,  Paul W Manley

    发明人： Guido Bold ,  Pascal Furet ,  Paul W Manley

    IPC分类号： A01N43/40 ,  A61K31/44

    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.

    摘要翻译： 本发明涉及式I的邻氨基苯甲酰胺衍生物，其中R1表示H或低级烷基，R2表示H或低级烷基，R3表示全氟低级烷基，X表示O或S，或其N-氧化物或互变异构体， 这种邻氨基苯甲酸酰胺的盐，它们的N-氧化物及其互变异构体; 其制备方法，其用于治疗人或动物体的应用，其单独使用或与一种或多种其它药学活性化合物组合用于特别是肿瘤性疾病如肿瘤疾病的治疗 ，视网膜病变或年龄相关性黄斑变性; 用于治疗动物，特别是人类中的这种疾病的方法，以及使用这样的化合物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗肿瘤的药物制剂 视网膜病变或年龄相关性黄斑变性疾病。

    Anthranilic acid amides and their use as VEGF receptor tyrosine kinase inhibitors
    10.
    发明授权
    Anthranilic acid amides and their use as VEGF receptor tyrosine kinase inhibitors 失效
    邻氨基苯甲酸酰胺及其作为VEGF受体酪氨酸激酶抑制剂的用途

    公开(公告)号：US07091224B2

    公开(公告)日：2006-08-15

    申请号：US10494591

    申请日：2002-11-07

    申请人： Guido Bold ,  Pascal Furet ,  Paul W Manley

    发明人： Guido Bold ,  Pascal Furet ,  Paul W Manley

    IPC分类号： A61K31/44 ,  C07D211/72

    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.

    摘要翻译： 本发明涉及式（I）的邻氨基苯甲酰胺衍生物，其中R 1代表H或低级烷基，R 2代表H或低级烷基，R 3 表示全氟低级烷基，X是O或S，或其N-氧化物或互变异构体，与邻氨基苯甲酸酰胺的盐，它们的N-氧化物及其互变异构体; 其制备方法，其用于治疗人或动物体的应用，其单独使用或与一种或多种其它药学活性化合物组合用于特别是肿瘤性疾病如肿瘤疾病的治疗 ，视网膜病变或年龄相关性黄斑变性; 用于治疗动物，特别是人类中的这种疾病的方法，以及使用这样的化合物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗肿瘤的药物制剂 视网膜病变或年龄相关性黄斑变性疾病。