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    Quinazoline derivatives and pharmaceutical compositions containing them
    22.
    发明授权
    Quinazoline derivatives and pharmaceutical compositions containing them 有权
    喹唑啉衍生物和含有它们的药物组合物

    公开(公告)号：US07019012B2

    公开(公告)日：2006-03-28

    申请号：US10023099

    申请日：2001-12-17

    申请人： Frank Himmelsbach ,  Elke Langkopf ,  Stefan Blech ,  Birgit Jung ,  Anke Baum ,  Flavio Solca

    发明人： Frank Himmelsbach ,  Elke Langkopf ,  Stefan Blech ,  Birgit Jung ,  Anke Baum ,  Flavio Solca

    IPC分类号： A61K31/5377 ,  A61K31/517 ,  C07D239/72 ,  C07D413/02

    CPC分类号： C07D405/12 ,  C07D239/94

    摘要： A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.

    摘要翻译： 通式I的化合物，其中：R a a是苄基，1-苯乙基或3-氯-4-氟苯基; R b是二甲基氨基，N-甲基-N-乙基氨基，二乙基氨基，N-甲基-N-异丙基氨基，N-甲基-N-环丙基氨基，N-甲基-N-（2-甲氧基乙基） 氨基，N-乙基-N-（2-甲氧基乙基）氨基，双（2-甲氧基乙基）氨基，吗啉代，N-甲基-N-（四氢呋喃-3-基）氨基，N-甲基-N-（四氢呋喃-2 - 甲基）氨基，N-甲基-N-（四氢呋喃-3-基甲基）氨基，N-甲基-N-（四氢吡喃-4-基）氨基或N-甲基-N-（四氢吡喃-4-基甲基）氨基 组; 环烷基甲氧基，环丁氧基，四氢呋喃-3-基氧基，四氢呋喃-2-基甲氧基，四氢呋喃-3-基甲氧基，四氢吡喃-4-基氧基或四氢吡喃-4-基甲氧基， 或其互变异构体，立体异构体或其盐，特别是其具有有价值的药理学性质的无机或有机酸或碱的生理上可接受的盐，特别是对由酪氨酸激酶介导的信号转导的抑制作用，它们在治疗疾病中的用途， 特别是肺和气道的肿瘤疾病和疾病及其制备。

    Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
    28.
    发明申请
    Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them 审中-公开
    双环杂环，含有这些化合物的药物组合物，它们的用途和制备方法

    公开(公告)号：US20100267718A1

    公开(公告)日：2010-10-21

    申请号：US12826927

    申请日：2010-06-30

    申请人： Frank HIMMELSBACH ,  Rainer Soyka ,  Birgit Jung

    发明人： Frank HIMMELSBACH ,  Rainer Soyka ,  Birgit Jung

    IPC分类号： A61K31/5377 ,  C07D239/72 ,  C07D413/12 ,  A61K31/517 ,  A61P1/00 ,  A61P11/00

    CPC分类号： C07D413/12 ,  C07D239/94

    摘要： The present invention relates to bicyclic heterocycles of general formula whereinRa, Rb, Rc, Rd, X and n are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibiting effect on the signal transduction mediated by tyrosine kinases, their use in treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract and the preparation thereof.

    摘要翻译： 本发明涉及通式的双环杂环，其中Ra，Rb，Rc，Rd，X和n如权利要求1所定义，互变异构体，立体异构体，其混合物及其盐，特别是其生理上可接受的盐与 具有有价值的药理学特性的无机或有机酸，特别是对由酪氨酸激酶介导的信号转导的抑制作用，它们在治疗疾病尤其是肿瘤疾病以及良性前列腺增生（BPH），肺和呼吸道疾病中的用途 及其制备。

    Bicyclic heterocycles, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof
    29.
    发明申请
    Bicyclic heterocycles, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof 审中-公开
    双环杂环，含有这些化合物的药物组合物，其用途及其制备方法

    公开(公告)号：US20100234371A1

    公开(公告)日：2010-09-16

    申请号：US11996886

    申请日：2006-08-03

    申请人： Frank Himmelsbach ,  Birgit Jung

    发明人： Frank Himmelsbach ,  Birgit Jung

    IPC分类号： A61K31/5377 ,  C07D239/94 ,  A61K31/517 ,  C07D413/14 ,  A61P35/00

    CPC分类号： C07D401/12 ,  C07D239/94 ,  C07D403/12

    摘要： The invention relates to bicyclic heterocycles of general formula (I), in which Ra, Rb, Rc, Rd, Re and X are as defined in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, in particular, the physiologically-acceptable salts thereof with inorganic and organic acids with useful pharmacological properties, in particular, an inhibitory effect on signal transduction brought about by tyrosine kinases, the use thereof for the treatment of diseases, in particular of tumour diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and airways and production thereof.

    摘要翻译： 本发明涉及通式（I）的双环杂环，其中Ra，Rb，Rc，Rd，Re和X如权利要求1所定义，互变异构体，立体异构体，其混合物和盐，特别是生理上可接受的 其与具有有用药理学性质的无机和有机酸的盐，特别是对由酪氨酸激酶引起的信号转导的抑制作用，其用于治疗疾病，特别是肿瘤疾病和良性前列腺增生症（BPH），疾病 的肺和气道及其生产。

    PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF RESPIRATORY AND GASTROINTESTINAL DISORDERS
    30.
    发明申请
    PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF RESPIRATORY AND GASTROINTESTINAL DISORDERS 审中-公开
    用于治疗呼吸道感染和胃肠疾病的药物组合物

    公开(公告)号：US20100099651A1

    公开(公告)日：2010-04-22

    申请号：US12446794

    申请日：2007-10-23

    申请人： Birgit Jung ,  Frank Himmelsbach ,  Gerald Pohl

    发明人： Birgit Jung ,  Frank Himmelsbach ,  Gerald Pohl

    IPC分类号： A61K31/517 ,  A61K31/5377 ,  A61K31/56 ,  A61P11/00

    CPC分类号： A61K9/0073 ,  A61K31/517 ,  A61K31/5375 ,  A61K31/55 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to novel pharmaceutical compositions comprising at least one EGFR kinase inhibitor and at least one additional active compound selected from beta-2 mimetics, steroids, PDE-IV inhibitors, p38 MAP kinase inhibitors, NK1 antagonists, anticholinergics and endothelin antagonists, processes for preparing the compositions and the use thereof as medicament in the treatment of respiratory or gastrointestinal complaints, as well as inflammatory diseases of the joints, the skin or the eyes.

    摘要翻译： 本发明涉及包含至少一种EGFR激酶抑制剂和至少一种选自β-2模拟物，类固醇，PDE-IV抑制剂，p38 MAP激酶抑制剂，NK1拮抗剂，抗胆碱能药和内皮素拮抗剂的其它活性化合物的新型药物组合物， 用于制备组合物及其用作治疗呼吸道或胃肠道疾病以及关节，皮肤或眼睛的炎性疾病的药物。