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12 条记录 (耗时 0.052 秒)

    4-(4-pyridinyl)-benzamides and their use as rock activity modulators
    1.
    发明授权
    4-(4-pyridinyl)-benzamides and their use as rock activity modulators 有权
    4-（4-吡啶基） - 苯甲酰胺及其作为岩石活性调节剂的用途

    公开(公告)号：US08445686B2

    公开(公告)日：2013-05-21

    申请号：US12675430

    申请日：2008-08-26

    申请人： Helmut Mack ,  Nicole Teusch ,  Bernhard K. Mueller ,  Wilfried Hornberger ,  Michael F. Jarvis ,  Daryl Sauer ,  Steve Swann, Jr. ,  Dominique Bonafoux ,  Ryan Keddy ,  Adrian Donald Hobson ,  Anil Vasudevan

    发明人： Helmut Mack ,  Nicole Teusch ,  Bernhard K. Mueller ,  Wilfried Hornberger ,  Michael F. Jarvis ,  Daryl Sauer ,  Steve Swann, Jr. ,  Dominique Bonafoux ,  Ryan Keddy ,  Adrian Donald Hobson ,  Anil Vasudevan

    IPC分类号： C07D211/78 ,  C07D211/72 ,  C07D211/84 ,  A61K31/44

    CPC分类号： C07D401/12 ,  C07D213/56 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

    摘要： The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R1 and R2 are, independently of each other, hydrogen, hydroxy, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-haloalkoxy; R3, R4, R5 and R6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, amino, C1-C8-alkylamino or di-(C1-C8-alkyl)-amino; R7 is hydrogen, C1-C8-alkyl, C1-C8-haloalkyl, aryl or aryl-C1-C8-alkyl; R8 is a group of the formula —X—W, where X is a single bond, C1-C4-alkylene or C1-C4-alkylene-O—, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected from O, S and N and optionally 1 or 2 carbonyl groups; R9 is a group of the formula —Y—Z, where Z is hydrogen, halogen, OR11, NR12R13, S(O)m—R14, phenyl which may carry 1, 2, 3 or 4 substituents R15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C1C4-alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.

    摘要翻译： 本发明涉及式（I）的新型4-（4-吡啶基） - 苯甲酰胺。 化合物I具有有价值的治疗特性，特别适用于治疗对Rho激酶（ROCK）的调节作用的疾病。 R 1和R 2彼此独立地为氢，羟基，氰基，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，C 1 -C 8 - 烷氧基或C 1 -C 8 - 卤代烷氧基; R3，R4，R5和R6彼此独立地为氢，羟基，卤素，氰基，C1-C8-烷基，C1-C8-卤代烷基，C1-C8-烷氧基，C1-C8-卤代烷氧基，氨基，C1- C 8 - 烷基氨基或二 - （C 1 -C 8 - 烷基） - 氨基; R 7是氢，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，芳基或芳基-C 1 -C 8 - 烷基; R8是式-XW的基团，其中X是单键，C1-C4-亚烷基或C1-C4-亚烷基-O-，其中三个最后提及的基团中的亚烷基可以是直链或支链的，并且可以 部分或完全卤化和/或可以被羟基取代和/或可被氧原子中断; 并且W是选自苯基和5-或6-元饱和，部分不饱和或芳族杂环的环状基团，其含有作为环成员1,2或3的选自O，S和N的杂原子以及任选的1或2个羰基 ; R9是式-YZ的基团，其中Z是氢，卤素，OR11，NR12R13，S（O）m -R14，可以带有1,2,3或4个取代基R15或5-或6-元的苯基 饱和，部分不饱和或芳族杂环; Y是可部分或完全卤化和/或可被羟基和/或苯环取代的直链或支链C 1 -C 4亚烷基; 或者Z为苯基或上述5-或6-元杂环的情况下，Y也可以是单键。

    Therapeutic use of antibodies directed against repulsive guidance molecule (RGM)
    6.
    发明授权
    Therapeutic use of antibodies directed against repulsive guidance molecule (RGM) 有权
    针对排斥指导分子（RGM）的抗体的治疗用途

    公开(公告)号：US07981420B2

    公开(公告)日：2011-07-19

    申请号：US10451586

    申请日：2001-12-21

    申请人： Bernhard K. Mueller ,  Philippe P. Monnier ,  Paolo Macchi ,  Friedrich Bonhoeffer ,  Bernd Stahl ,  Matthias Mann ,  Jens S. Anderson

    发明人： Bernhard K. Mueller ,  Philippe P. Monnier ,  Paolo Macchi ,  Friedrich Bonhoeffer ,  Bernd Stahl ,  Matthias Mann ,  Jens S. Anderson

    IPC分类号： A61K39/395 ,  C07K16/28

    CPC分类号： C07K14/47 ,  A61K38/1709 ,  A61K2039/505 ,  C07K14/465 ,  C07K14/4702 ,  C07K16/28

    摘要： The present invention relates to the use of a modulator of a polypeptide having or comprising an amino acid sequence as disclosed herein or of a functional fragment or derivative thereof or of a polynucleotide encoding said polypeptide or fragment or derivative for the preparation of a pharmaceutical composition for preventing, alleviating or treating diseases or conditions associated with the degeneration or injury of vertebrate nervous tissue, associated with seizures or associated with angiogenic disorders or disorders of the cardio-vascular system. Furthermore, the invention provides for the use of a modulator of a polypeptide having or comprising said amino acid sequence of a functional fragment or derivative thereof or of a polynucleotide encoding said polypeptide or fragment or derivative for the preparation of a pharmaceutical composition for preventing, alleviating or treating diseases or conditions associated with the degeneration or injury of vertebrate nervous tissue, associated with angiogenic disorders or disorders of the cardio-vascular system. In addition the invention provides for the use of said polypeptide or said functional fragment or derivative thereof for the preparation of a pharmaceutical composition for preventing or treating tumor growth or formation of tumor metastases or as a marker of stem cells.

    摘要翻译： 本发明涉及具有或包含本文公开的氨基酸序列或其功能片段或衍生物或编码所述多肽或片段或衍生物的多核苷酸的调节剂用于制备药物组合物的用途 预防，减轻或治疗与癫痫相关的脊椎动物神经组织的退化或损伤相关的疾病或病症或与心血管系统的血管生成障碍或病症有关。 此外，本发明提供了具有或包含其功能片段或其衍生物的所述氨基酸序列或编码所述多肽或片段或衍生物的多核苷酸的多肽的调节剂用于制备用于预防，缓解的药物组合物 或治疗与脊髓动物神经组织的变性或损伤相关的疾病或病症，与血管生成障碍或心血管系统的病症有关。 此外，本发明提供了所述多肽或其功能片段或其衍生物用于制备用于预防或治疗肿瘤生长或肿瘤转移形成或作为干细胞标记的药物组合物的用途。

    USE OF RGM AND ITS MODULATORS
    7.
    发明申请
    USE OF RGM AND ITS MODULATORS 审中-公开
    RGM及其调制器的使用

    公开(公告)号：US20110112280A1

    公开(公告)日：2011-05-12

    申请号：US12939823

    申请日：2010-11-04

    申请人： Bernhard K. Mueller ,  Philippe P. Monnier ,  Paolo Macchi ,  Friedrich Bonhoeffer ,  Bernd Stahl ,  Matthias Mann ,  Jens S. Andersen

    发明人： Bernhard K. Mueller ,  Philippe P. Monnier ,  Paolo Macchi ,  Friedrich Bonhoeffer ,  Bernd Stahl ,  Matthias Mann ,  Jens S. Andersen

    IPC分类号： C07K16/00 ,  C07K14/00 ,  C07H21/04

    CPC分类号： C07K14/47 ,  A61K38/1709 ,  A61K2039/505 ,  C07K14/465 ,  C07K14/4702 ,  C07K16/28

    摘要： The present invention relates to the use of a modulator of a polypeptide having or comprising an amino acid sequence as disclosed herein or of a functional fragment or derivative thereof or of a polynucleotide encoding said polypeptide or fragment or derivative for the preparation of a pharmaceutical composition for preventing, alleviating or treating diseases or conditions associated with the degeneration or injury of vertebrate nervous tissue, associated with seizures or associated with angiogenic disorders or disorders of the cardiovascular system. Furthermore, the invention provides for the use of a modulator of a polypeptide having or comprising said amino acid sequence of a functional fragment or derivative thereof or of a polynucleotide encoding said polypeptide or fragment or derivative for the preparation of a pharmaceutical composition for preventing, alleviating or treating diseases or conditions associated with the degeneration or injury of vertebrate nervous tissue, associated with angiogenic disorders or disorders of the cardiovascular system. In addition, the invention provides for the use of said polypeptide or said functional fragment or derivative thereof for the preparation of a pharmaceutical compositions for preventing or treating tumor growth or formation of tumor metastases or as a marker of stem cells.

    摘要翻译： 本发明涉及具有或包含本文公开的氨基酸序列或其功能片段或衍生物或编码所述多肽或片段或衍生物的多核苷酸的调节剂用于制备药物组合物的用途 预防，减轻或治疗与癫痫相关的脊髓动物神经组织的退化或损伤相关的疾病或病症，或与心血管系统的血管生成障碍或病症有关。 此外，本发明提供了具有或包含其功能片段或其衍生物的所述氨基酸序列或编码所述多肽或片段或衍生物的多核苷酸的多肽的调节剂用于制备用于预防，缓解的药物组合物 或治疗与血管生成障碍或心血管系统疾病相关的脊椎动物神经组织的退化或损伤相关的疾病或病症。 此外，本发明提供了所述多肽或其功能片段或衍生物用于制备用于预防或治疗肿瘤生长或肿瘤转移形成或作为干细胞标志物的药物组合物的用途。