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    Cyclic Diaryl Ureas Suitable as Tyrosine Kinase Inhibitors
    21.
    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。

    Heterobicyclic Carboxamides as Inhibitors for Kinases
    23.
    发明申请
    Heterobicyclic Carboxamides as Inhibitors for Kinases 失效
    异双环酰胺作为激酶抑制剂

    公开(公告)号：US20090030009A1

    公开(公告)日：2009-01-29

    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： A61K31/496 ,  C07D239/24 ,  A61P35/00 ,  A61K31/505

    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。

    Anthranilic acid amides and their use as VEGF receptor tyrosine kinase inhibitors
    25.
    发明申请
    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：US20060178409A1

    公开(公告)日：2006-08-10

    申请号：US11374720

    申请日：2006-03-14

    申请人： Guido Bold ,  Pascal Furet ,  Paul Manley

    发明人： Guido Bold ,  Pascal Furet ,  Paul Manley

    IPC分类号： C07D213/63 ,  A61K31/4412

    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为O或S，或其N-氧化物或互变异构体，与该邻氨基苯甲酸酰胺，其N-氧化物及其互变异构体的盐形成的盐; 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 pharmaceutical use thereof
    26.
    发明授权
    Anthranilic acid amides and pharmaceutical use thereof 失效
    邻氨基苯甲酸酰胺及其药物用途

    公开(公告)号：US07067543B2

    公开(公告)日：2006-06-27

    申请号：US10494222

    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： C07D213/38 ,  A61K31/44

    CPC分类号： C07C237/40 ,  C07D213/38 ,  C07D213/89

    摘要： The invention relates to anthranilic acid amide derivatives of formula (I), wherein Ar is represented by the subformula (Ia), wherein Ra represents H or lower alkyl, and R1 represents H or perfluoro lower alkyl, R2 represents H, halogen, C2–C7alkyl, C2–C7alkenyl or lower aklynyl; or Ar is represented by the subformula (Ib) and R1 represents perfluoro lower alkyl, and R2 represents bromo, iodo, C2–C7alkyl, C2–C7alkenyl or lower alkynyl, or R1 represents H, and R2 represents fluoro, bromo, iodo, ethyl, C5–C7alkyl, C2–C7alkenyl or lower alkynyl; to N-oxides and tautomers thereof, and to salts of such anthranilic acid amides, its N-oxides and tautomers; to processes for their preparation; to their application in the treatment of the human or animal body, to 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; to a method for the treatment of such diseases in animals; and to 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）的邻氨基苯甲酸酰胺衍生物，其中Ar由下式表示：其中R aa代表H或低级烷基，和 R 1表示H或全氟低级烷基，R 2表示H，卤素，C 2 -C 7烷基 C 2 -C 7链烯基或低级甲酰胺基; 或Ar由亚式（I B b）表示，R 1表示全氟低级烷基，R 2表示溴，碘，C 1 -C 6烷基， 或者R 1，R 2，R 2，R 3，R 6，R 6， / SUB代表H，R 2代表氟，溴，碘，乙基，C 5 -C 7烷基，C 1 -C 6烷基， 烯基或低级炔基; 其N-氧化物和互变异构体，以及这种邻氨基苯甲酰胺，其N-氧化物和互变异构体的盐; 进行准备; 其在治疗人或动物体中的应用，其单独使用或与一种或多种其它药学活性化合物的组合用于特别是治疗视网膜病变或年龄的肿瘤疾病如肿瘤疾病 相关性黄斑变性; 涉及在动物中治疗这些疾病的方法; 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性疾病，视网膜病变或年龄相关性黄斑变性的药物制剂。

    Anthranilic acid amides and their use as vegf receptor tyrosine kinase inhibitors
    28.
    发明申请
    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：US20050096356A1

    公开(公告)日：2005-05-05

    申请号：US10494591

    申请日：2002-11-07

    申请人： Guido Bold ,  Pascal Furet ,  Paul Manley

    发明人： Guido Bold ,  Pascal Furet ,  Paul Manley

    IPC分类号： A61K31/44 ,  A61K31/4412 ,  A61P9/10 ,  A61P9/14 ,  A61P11/06 ,  A61P15/00 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07D213/64 ,  C07D213/70 ,  C07D213/62

    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。

    Anilinopeptide derivatives
    29.
    发明授权
    Anilinopeptide derivatives 有权
    氨基肽衍生物

    公开(公告)号：US06451973B1

    公开(公告)日：2002-09-17

    申请号：US09214959

    申请日：1999-02-01

    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： C07K508

    CPC分类号： C07D295/135 ,  C07C271/22 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The invention relates to compounds of the formula I, in which R1 and R2 are, independently of each other, lower alkyl or lower alkoxy-lower alkyl; R3 and R4 are, independently of each other, sec-lower alkyl or tert-lower alkyl; R5 is phenyl or cyclohexyl; and R6 and R7 are, independently of each other, lower alkyl, or, together with the linking nitrogen atom, pyrrolidino, piperidino, 4-lower alkylpiperidino, 1,2,4-triazol-1-yl or 1,2,4-triazol-4-yl; or a salt thereof, provided that at least one salt-forming group is present. These compounds are inhibitors of HIV protease and are therefore suitable, for example, for treating AIDS or its preliminary stages.

    摘要翻译： 本发明涉及式I化合物，其中R 1和R 2彼此独立地为低级烷基或低级烷氧基 - 低级烷基; R 3和R 4彼此独立地为低级烷基或叔 - 低级烷基; R5是苯基或环己基; R 6和R 7彼此独立地为低级烷基，或与连接氮原子一起为吡咯烷子基，哌啶子基，4-低级烷基哌啶子基，1,2,4-三唑-1-基或1,2,4-三唑 -4-基或其盐，条件是至少存在一个成盐基团。这些化合物是HIV蛋白酶的抑制剂，因此适用于例如用于治疗AIDS或其初级阶段。

    Substituted pyrrolopyrimidines and processes for their preparation
    30.
    发明授权
    Substituted pyrrolopyrimidines and processes for their preparation 失效
    取代的吡咯并嘧啶及其制备方法

    公开(公告)号：US06180636B2

    公开(公告)日：2001-01-30

    申请号：US09242592

    申请日：1999-02-19

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

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

    IPC分类号： A61K31519

    CPC分类号： C07D487/04

    摘要： There are described 7H-pyrrolo[2,3-d]pyrimidine derivatives of the formula I in which the substituents are as defined in claim 1. These compounds inhibit the tyrosine kinase activity of the receptor for the epidermal growth factor (EGF) and c-erbB2 kinase and can be used as anti-tumor agents.

    摘要翻译： 描述了式Iin的7H-吡咯并[2,3-d]嘧啶衍生物，其取代基如权利要求1中所定义。这些化合物抑制表皮生长因子（EGF）受体的酪氨酸激酶活性和c- erbB2激酶，可用作抗肿瘤剂。