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94 条记录 (耗时 0.035 秒)

    Cyclic Diaryl Ureas Suitable as Tyrosine Kinase Inhibitors
    61.
    发明申请
    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：US20080039440A1

    公开(公告)日：2008-02-14

    申请号：US11575601

    申请日：2005-09-27

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

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

    IPC分类号： A61K31/506 ,  A61K31/496 ,  A61K31/55 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14

    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CR，C，NR C或O，其中R c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中的至少两个为N; 并且每个R a 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; 并且其中基团具有R 1，R 2，R 3和R 4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。

    Phthalazine derivatives for treating inflammatory diseases
    62.
    发明申请
    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：US20060217388A1

    公开(公告)日：2006-09-28

    申请号：US11441961

    申请日：2006-05-26

    申请人： Guido Bold ,  Janet King ,  Jorg Frei ,  Richard Heng ,  Paul Manley ,  Bernhard Wietfeld ,  Jeanette Wood

    发明人： Guido Bold ,  Janet King ,  Jorg Frei ,  Richard Heng ,  Paul Manley ,  Bernhard Wietfeld ,  Jeanette Wood

    IPC分类号： A61K31/501 ,  C07D403/02

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

    摘要： The invention relates to the treatment of leukemias 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： 本发明涉及用式I的VEGF受体酪氨酸激酶的活性抑制剂治疗白血病，所述取代基在说明书中定义; 以及新的酞嗪衍生物; 制备方法; 其用于治疗人或动物体的方法中的应用; 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。

    Pyridine derivatives inhibiting angiogenesis and/or VEGF receptor tyrosine kinase
    65.
    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
    66.
    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。

    Pyrimidine derivatives and processes for the preparation thereof
    68.
    发明授权
    Pyrimidine derivatives and processes for the preparation thereof 失效
    嘧啶衍生物及其制备方法

    公开(公告)号：US06251911B1

    公开(公告)日：2001-06-26

    申请号：US09269823

    申请日：1999-04-01

    申请人： Guido Bold ,  Jörg Frei ,  Marc Lang ,  Peter Traxler

    发明人： Guido Bold ,  Jörg Frei ,  Marc Lang ,  Peter Traxler

    IPC分类号： C07D48704

    CPC分类号： C07D487/04

    摘要： 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula I wherein the substituents are as defined in claim 1, are described. These compounds inhibit the tyrosine kinase activity of the receptor for epidermal growth factor (EGF) and c-erbB2 kinase and can be used as anti-tumor agents.

    摘要翻译： 描述了在取代基中如权利要求1所定义的式I的4-氨基-1H-吡唑并[3,4-d]嘧啶衍生物。这些化合物抑制表皮生长因子（EGF）和c的受体的酪氨酸激酶活性 -erbB2激酶，可用作抗肿瘤剂。

    Azahexane derivatives as substrate isosters of retroviral asparate proteases
    69.
    发明授权
    Azahexane derivatives as substrate isosters of retroviral asparate proteases 失效
    氮杂己烷衍生物作为逆转录病毒天冬氨酸蛋白酶的底物等价物

    公开(公告)号：US06225345B1

    公开(公告)日：2001-05-01

    申请号：US09068876

    申请日：1998-05-21

    申请人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang

    发明人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang

    IPC分类号： A61K3127

    CPC分类号： C07C271/22 ,  Y10S514/934

    摘要： The invention relates to compounds of formula (I): wherein R1 and R10 are each independently of the other lower alkoxycarbonyl; either R2, R3 and R4 are each independently of the other C1-C4alkyl and R7, R8 and R9 are each selected from hydrogen and C1-C4alkyl, with not more than 2 of the radicals being hydrogen; or R7, R8 and R9 are each independently of the other C1-C4alkyl and R2, R3 and R4 are each selected from hydrogen and C1-C4alkyl, with 1 or 2 of the radicals being hydrogen; R5 is phenyl or cyclohexyl; and R6 is phenyl or cyanophenyl; or salts thereof; those compounds are inhibitors of retroviral aspartate proteases and are effective, for example, against HIV.

    摘要翻译： 本发明涉及式（I）化合物：其中R 1和R 10各自独立地为低级烷氧基羰基; R 2，R 3和R 4各自独立地为C 1 -C 4烷基，R 7，R 8和R 9各自选自氢和C 1 -C 4烷基，不超过2个基团为氢; 或R 7，R 8和R 9各自独立地为C 1 -C 4烷基，R 2，R 3和R 4各自选自氢和C 1 -C 4烷基，其中1或2个是氢; R5是苯基或环己基; R6为苯基或氰基苯基; 或其盐; 这些化合物是逆转录病毒天冬氨酸蛋白酶的抑制剂，并且是有效的，例如针对HIV。