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13 条记录 (耗时 0.026 秒)

    Substituted cyclohexyl and piperidinyl derivates as melanocortin-4 receptor modulators
    1.
    发明申请
    Substituted cyclohexyl and piperidinyl derivates as melanocortin-4 receptor modulators 审中-公开
    取代的环己基和哌啶基衍生物作为黑皮质素-4受体调节剂

    公开(公告)号：US20070155783A1

    公开(公告)日：2007-07-05

    申请号：US10550268

    申请日：2004-03-19

    申请人： Michael Soeberdt ,  Philipp Weyermann ,  Andreas Sprecher

    发明人： Michael Soeberdt ,  Philipp Weyermann ,  Andreas Sprecher

    IPC分类号： A61K31/4709 ,  A61K31/452 ,  A61K31/353 ,  C07D405/02 ,  C07D401/02

    CPC分类号： C07D405/12 ,  C07D217/26 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

    摘要： The present invention relates to novel substituted cyclohexyl and piperidinyl derivatives as melanocortin-4. receptor (MC-4R) modulators. MC-4R agonists of the invention can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the MC-4R antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. All diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.

    摘要翻译： 本发明涉及新型取代的环己基和哌啶衍生物作为黑皮质素-4。 受体（MC-4R）调节剂。 本发明的MC-4R激动剂可用于治疗疾病和疾病如肥胖，糖尿病和性功能障碍，而MC-4R拮抗剂可用于治疗疾病和疾病如癌症恶病质，肌肉消瘦，厌食 ，焦虑和抑郁。 可以用本发明的化合物治疗涉及MC-4R调节的所有疾病和病症。

    Alpha-keto carbonyl calpain inhibitors
    9.
    发明申请
    Alpha-keto carbonyl calpain inhibitors 审中-公开
    α-酮羰基钙蛋白酶抑制剂

    公开(公告)号：US20060258598A1

    公开(公告)日：2006-11-16

    申请号：US10548239

    申请日：2004-03-03

    申请人： Holger Herzner ,  Philipp Weyermann ,  Andreas Sprecher ,  Marco Henneböhle ,  Cyrille Lescop ,  Hervé Siendt

    发明人： Holger Herzner ,  Philipp Weyermann ,  Andreas Sprecher ,  Marco Henneböhle ,  Cyrille Lescop ,  Hervé Siendt

    IPC分类号： A61K38/04 ,  C07K5/04

    CPC分类号： C07K5/06026 ,  A61K38/00 ,  C07D233/54 ,  C07D339/04 ,  C07K5/0202 ,  C07K5/0606

    摘要： The present invention relates to novel α-keto carbonyl calpain inhibitors for the treatment of neurodegenerative diseases and neuromuscular diseases including Duchenne Muscular Dystrophy, Becker Muscular Dystrophy and other muscular dystrophies. Disuse atrophy and general muscle wasting can also be treated. Diseases of the eye, in particular cataract, can be treated as well. Generally all conditions where elevated levels of calpains are involved can be treated. The compounds of the invention may also inhibit other thiol proteases such as cathepsin B, cathepsin H, cathepsin L, papain or the like. Multicatalytic Protease (MCP) also known as proteasome may also be inhibited and the compounds can therefore be used to treat cell proliferative diseases such as cancer, psoriasis, and restenosis. The compounds of the present invention are also inhibitors of cell damage by oxidative stress through free radicals and can be used to treat mitochondrial disorders and neurodegenerative diseases, where elevated levels of oxidative stress are involved.

    摘要翻译： 本发明涉及用于治疗神经变性疾病和神经肌肉疾病（包括杜氏肌营养不良症，贝克肌营养不良症和其他肌营养不良症）的新型α-酮羰基钙蛋白酶抑制剂。 也可以治疗消除萎缩和一般的肌肉消瘦。 眼睛疾病，特别是白内障也可以治疗。 一般来说，涉及钙蛋白水平升高的所有条件都可以被处理。 本发明的化合物还可以抑制其它巯基蛋白酶，例如组织蛋白酶B，组织蛋白酶H，组织蛋白酶L，木瓜蛋白酶等。 也称为蛋白酶体的多分解蛋白酶（MCP）也可能被抑制，因此化合物可用于治疗细胞增殖性疾病如癌症，牛皮癣和再狭窄。 本发明的化合物也是通过自由基的氧化应激的细胞损伤的抑制剂，并且可以用于治疗涉及氧化应激水平升高的线粒体疾病和神经变性疾病。