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    Heterobicyclic carboxamides as inhibitors for kinases
    2.
    发明授权
    Heterobicyclic carboxamides as inhibitors for kinases 失效
    异环碳酰胺作为激酶抑制剂

    公开(公告)号：US08058276B2

    公开(公告)日：2011-11-15

    申请号：US12281715

    申请日：2007-03-09

    申请人： Guido Bold ,  Andrea Vaupel ,  Marc Lang

    发明人： Guido Bold ,  Andrea Vaupel ,  Marc Lang

    IPC分类号： C07D413/12 ,  C07D417/12 ,  A61K31/41

    CPC分类号： C07D413/12 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    摘要： The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.

    摘要翻译： 本发明涉及式（I）的新型有机化合物及其在治疗动物或人体中的用途，包括式（I）化合物的药物组合物和式（I）化合物用于 制备用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病，特别是肿瘤疾病的药物组合物。

    Cyclic diaryl ureas suitable as tyrosine kinase inhibitors
    4.
    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。

    Organic Compounds
    6.
    发明申请
    Organic Compounds 审中-公开
    有机化合物

    公开(公告)号：US20090069360A1

    公开(公告)日：2009-03-12

    申请号：US12293257

    申请日：2007-03-14

    申请人： David Bryant Batt ,  Rene Beerli ,  Guido Bold ,  Giorgio Caravatti ,  Timothy Michael Ramsey

    发明人： David Bryant Batt ,  Rene Beerli ,  Guido Bold ,  Giorgio Caravatti ,  Timothy Michael Ramsey

    IPC分类号： A61K31/506 ,  C07D401/04 ,  A61P35/00

    CPC分类号： C07D401/04

    摘要： The present invention relates to the discovery that certain compounds inhibit, regulate and/or modulate tyrosine and serine/threonine kinase and kinase-like proteins, such as RAF kinase, a serine/threonine kinase that functions in the MAP kinase signaling pathway, and is concerned with compositions which contain these compounds, and methods of using them to treat tyrosine and serine/threonine kinase and kinase-like dependent diseases, such as angiogenesis, cancer and cardiac hypertrophy.

    摘要翻译： 本发明涉及某些化合物抑制，调控和/或调节酪氨酸和丝氨酸/苏氨酸激酶和激酶样蛋白质，例如在MAP激酶信号通路中起作用的丝氨酸/苏氨酸激酶的RAF激酶，并且是 涉及含有这些化合物的组合物，以及使用它们治疗酪氨酸和丝氨酸/苏氨酸激酶和激酶样依赖性疾病如血管生成，癌症和心脏肥大的方法。

    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。

    Phthalazine derivatives for treating inflammatory diseases
    9.
    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：US07329660B2

    公开(公告)日：2008-02-12

    申请号：US11441961

    申请日：2006-05-26

    申请人： Guido Bold ,  Janet D King ,  Joerg Frei ,  Richard Heng ,  Paul W Manley ,  Bernhard Wietfeld ,  Jeanette M Wood

    发明人： Guido Bold ,  Janet D King ,  Joerg Frei ,  Richard Heng ,  Paul W Manley ,  Bernhard Wietfeld ,  Jeanette M Wood

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495

    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。

    7H-pyrrolo[2,3-d]pyrimidine derivatives
    10.
    发明授权
    7H-pyrrolo[2,3-d]pyrimidine derivatives 失效
    7H-吡咯并[2,3-d]嘧啶衍生物

    公开(公告)号：US07323469B2

    公开(公告)日：2008-01-29

    申请号：US10783000

    申请日：2004-02-20

    申请人： Guido Bold ,  Hans-Georg Capraro ,  Giorgio Caravatti ,  Peter Traxler

    发明人： Guido Bold ,  Hans-Georg Capraro ,  Giorgio Caravatti ,  Peter Traxler

    IPC分类号： A61K31/519 ,  A61K31/497 ,  C07D487/04 ,  A61P35/04

    CPC分类号： C07D487/04

    摘要： The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumor.

    摘要翻译： 本发明涉及式I的7H-吡咯并[2,3-d]嘧啶衍生物，其中符号和取代基如说明书中所定义，其制备方法，包含该衍生物的药物组合物及其用途 衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病如肿瘤的药物组合物。