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40 条记录 (耗时 0.026 秒)

    Alfavbeta3 and alfavbet6 integrin antagonists as antifibrotic agents
    11.
    发明申请
    Alfavbeta3 and alfavbet6 integrin antagonists as antifibrotic agents 审中-公开
    Alfavbeta3和alfavbet6整合素拮抗剂作为抗纤维化剂

    公开(公告)号：US20070117849A1

    公开(公告)日：2007-05-24

    申请号：US10574215

    申请日：2004-09-16

    申请人： Simon Goodman ,  Detlef Schuppan ,  Eleonora Patsenker ,  Yury Popov ,  Michael Bauer ,  Matthias Wiesner ,  Alfred Jonczyk

    发明人： Simon Goodman ,  Detlef Schuppan ,  Eleonora Patsenker ,  Yury Popov ,  Michael Bauer ,  Matthias Wiesner ,  Alfred Jonczyk

    IPC分类号： A61K31/4439 ,  A61K31/44

    CPC分类号： A61K31/00

    摘要： This invention relates to inhibition of αv integrins, especially αvβ3 and αvβ6 integrins, by specific antagonists, preferably non-peptidic antagonists, related compounds and compounds with comparable specificity, that downregulate fibrogenesis by inhibiting cell migration and production of pro-fibrogenic molecules (e.g., collagens, TIMP-1) and cytokines (e.g., CTGF) by activated hepatic stellate cells/myofibroblasts, activated epithelia and endothelia. These antagonists alone or in combination with other agents can effectively prevent, mitigate or even reverse development of advanced fibrosis, such as fibrosis/cirrhosis of the liver and fibrosis of other organs, such as lungs, kidneys, intestine, pancreas, skin and arteries.

    摘要翻译： 本发明涉及通过特异性拮抗剂，优选非肽拮抗剂，相关化合物和具有相当特异性的化合物抑制alphav整合素，特别是alphavbeta3和alphavbeta6整联蛋白，通过抑制细胞迁移和产生促纤维化分子来下调纤维发生（例如， 胶原，TIMP-1）和活化的肝星状细胞/肌成纤维细胞，活化的上皮细胞和内皮细胞因子（例如CTGF）。 这些单独的或与其它药剂组合的拮抗剂可以有效地预防，减轻或甚至逆转晚期纤维化的发展，例如肝纤维化/肝硬化和其他器官如肺，肾，肠，胰腺，皮肤和动脉的纤维化。

    Isoquinoline derivatives
    12.
    发明授权
    Isoquinoline derivatives 失效
    异喹啉衍生物

    公开(公告)号：US07060707B2

    公开(公告)日：2006-06-13

    申请号：US10506820

    申请日：2003-02-07

    申请人： Matthias Wiesner ,  Simon Goodman ,  Horst Kessler ,  Georgette Thumshirn ,  Dirk Weber ,  Dirk Gottschling

    发明人： Matthias Wiesner ,  Simon Goodman ,  Horst Kessler ,  Georgette Thumshirn ,  Dirk Weber ,  Dirk Gottschling

    IPC分类号： A61K31/44 ,  C07D401/02

    CPC分类号： C07D401/12 ,  C07D217/16

    摘要： Isoquinoline derivatives of the general formula (I) in which X, Y, Z, R1, R2 and n are as defined in Patent Claim (1), and physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammation, tumors, osteoporosis, infections and restenosis after angioplasty or in pathological processes which are maintained or propagated by angiogenesis.

    摘要翻译： 通式（I）的异喹啉衍生物，其中X，Y，Z，R 1，R 2和n如专利权利要求（1）中所定义， 其可接受的盐或溶剂合物是整联蛋白抑制剂，可用于抵抗血管生成维持或传播的血管成形术后的血栓形成，心肌梗死，冠心病，动脉硬化，炎症，肿瘤，骨质疏松，感染和再狭窄。

    Asimadaline derivatives comprising covalently bonded acids
    13.
    发明申请
    Asimadaline derivatives comprising covalently bonded acids 有权
    包含共价键的酸的阿司达林衍生物

    公开(公告)号：US20060122255A1

    公开(公告)日：2006-06-08

    申请号：US10539256

    申请日：2003-11-25

    申请人： Matthias Wiesner ,  Christoph Seyfried

    发明人： Matthias Wiesner ,  Christoph Seyfried

    IPC分类号： A61K31/4015 ,  C07D207/46

    CPC分类号： C07D207/12

    摘要： The present invention relates to derivatives of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide with covalently bonded acids, and to the salts, solvates and prodrugs thereof, to the derivatives as medicaments, to the use of these derivatives for the preparation of a medicament, to the use of these derivatives for the preparation of a pharmaceutical composition, to a process for the preparation of the said pharmaceutical compositions, to pharmaceutical compositions obtainable by this process, and to a process for the treatment of diseases which comprises the administration of the said pharmaceutical composition.

    摘要翻译： 本发明涉及具有共价键的酸的N-甲基-N - [（1S）-1-苯基-2 - （（3S）-3-羟基吡咯烷-1-基）乙基] -2,2-二苯基乙酰胺的衍生物， 以及其盐，溶剂合物和前药，作为药物的衍生物，使用这些衍生物用于制备药物，将这些衍生物用于制备药物组合物的方法，用于制备 所述药物组合物，可通过该方法获得的药物组合物，以及用于治疗包括施用所述药物组合物的疾病的方法。

    Treatment of functional dyspepsia using asimadoline
    17.
    发明申请
    Treatment of functional dyspepsia using asimadoline 审中-公开
    使用阿莫达林治疗功能性消化不良

    公开(公告)号：US20070179098A1

    公开(公告)日：2007-08-02

    申请号：US11732309

    申请日：2007-04-02

    申请人： Matthias Wiesner ,  Christoph Seyfried

    发明人： Matthias Wiesner ,  Christoph Seyfried

    IPC分类号： A61K31/7024 ,  A61K31/4015

    CPC分类号： C07D207/12

    摘要： The present invention relates to derivatives of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide with covalently bonded acids, and to the salts, solvates and prodrugs thereof, to the derivatives as medicaments, to the use of these derivatives for the preparation of a medicament, to the use of these derivatives for the preparation of a pharmaceutical composition, to a process for the preparation of the said pharmaceutical compositions, to pharmaceutical compositions obtainable by this process, and to a process for the treatment of diseases which comprises the administration of the said pharmaceutical composition.

    摘要翻译： 本发明涉及具有共价键的酸的N-甲基-N - [（1S）-1-苯基-2 - （（3S）-3-羟基吡咯烷-1-基）乙基] -2,2-二苯基乙酰胺的衍生物， 以及其盐，溶剂合物和前药，作为药物的衍生物，使用这些衍生物用于制备药物，将这些衍生物用于制备药物组合物的方法，用于制备 所述药物组合物，可通过该方法获得的药物组合物，以及用于治疗包括施用所述药物组合物的疾病的方法。