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    Phthalazine derivatives for treating inflammatory diseases
    1.
    发明申请
    Phthalazine derivatives for treating inflammatory diseases 审中-公开

    公开(公告)号：US20050176711A1

    公开(公告)日：2005-08-11

    申请号：US11099292

    申请日：2005-04-05

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

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

    IPC分类号： A61K31/502 ,  A61K31/506 ,  A61P1/16 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/12 ,  A61P17/06 ,  A61P19/02 ,  A61P25/04 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  A61K31/53 ,  A61K31/501 ,  C07D43/02

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

    摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, wherein r is 0 to 2, n is 0 to 3 R1 and R2 a) are independently in each case a lower alkyl; b) together form a bridge of subformula I*, wherein the bond is achieved via the two terminal C atoms and m is 0 to 4, or c) together form a bridge of subformula I**, wherein one or two of the ring members T1, T2, T3 and T4 are nitrogen, and the others are in each case CH, and the bond is achieved via atoms T1 and T4; G is —C(═O)—, —CHF—, —CF2—, lower alkylene, C2-C6alkenylene, lower alkylene or C3-C6alkenylene substituted by acyloxy or hydroxy, —CH2—O—, —CH2S—, —CH2—NH—, —CH2—O—CH2—, —CH2—S—CH2—, —CH2—NH—CH2—, oxa (—O—), thia (—S—), imino (—NH—), —CH2—O—CH2—, —CH2S—CH2— or —CH2—NH—CH2—; A, B, D, E and T are independently N or CH subject to the proviso that at least one and not more than three of these radicals are N; Q is lower alkyl, lower alkoxy or halogen; Ra and Ra′ are each independently H or lower alkyl; X is imino, oxa, or thia; Y is hydrogen, aryl, heteroaryl, or unsubstituted or substituted cycloalkyl; and Z is mono- or disubstituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl phenylsulfonyl, phenyl-lower alkylsulfonyl, alkylphenylsulfonyl, or (alternatively or, in a broader aspect of the invention, in addition) selected from the group consisting of ureido, halo-lower alkylthio, halo-lower alkansulfonyl, pyrazolyl, lower-alkyl pyrazolyl and C2-C7alkenyl; wherein—if more than 1 radical Z (m≧2) is present—the substituents Z are selected independently from each other; and wherein the bonds characterized in subformula I* by a wavy line are either single or double bonds; or an N-oxide of said compound, wherein 1 or more N atoms carry an oxygen atom; or a pharmaceutically acceptable salt thereof; 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 neovascularisation, 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.

    Phthalazine derivatives for treating inflammatory diseases
    2.
    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。

    Phthalazine derivatives for treating inflammatory diseases
    3.
    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。

    Phthalazine derivatives for treating inflammatory diseases
    4.
    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：US06686347B2

    公开(公告)日：2004-02-03

    申请号：US09964025

    申请日：2001-09-26

    申请人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

    发明人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

    IPC分类号： A61K3133

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

    摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain 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： 本发明涉及治疗炎症性疾病，特别是炎性类风湿病或风湿性疾病，和/或具有式I的VEGF受体酪氨酸激酶的活性抑制剂的疼痛，所述取代基在本说明书中定义;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。

    Anthranilic acid amides and their use as VEGF receptor tyrosine kinase inhibitors
    8.
    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 their use as vegf receptor tyrosine kinase inhibitors
    9.
    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。

    Cyclic Diaryl Ureas Suitable as Tyrosine Kinase Inhibitors
    10.
    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。