公开(公告)号：US20100324036A1

公开(公告)日：2010-12-23

申请号：US12809824

申请日：2008-12-18

申请人： Michael Soeberdt ,  Philipp Weyermann ,  Herve Siendt ,  Sonja Nordhoff ,  Achim Feurer ,  Miroslav Terinek

发明人： Michael Soeberdt ,  Philipp Weyermann ,  Herve Siendt ,  Sonja Nordhoff ,  Achim Feurer ,  Miroslav Terinek

IPC分类号： A61K31/5383 ,  C07D471/04 ,  A61K31/437 ,  C07D498/04 ,  A61P9/00 ,  A61P21/00 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P13/12 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D471/04

摘要： The present invention relates to substituted imidazopyridine derivatives as melanocortin-4 receptor (MC-4R) modulators, in particular as melanocortin 4 receptor antagonists. The antagonists are useful for the treatment of disorders and diseases such as cachexia induced by e.g. cancer, chronic kidney disease (CKD) or chronic heart failure (CHF), muscle wasting, anorexia induced by e.g. chemotherapy or radiotherapy, anorexia nervosa, amyotrophic lateral sclerosis (ALS), pain, neuropathic pain, anxiety and depression.

摘要翻译： 本发明涉及作为黑皮质素-4受体（MC-4R）调节剂的取代的咪唑并吡啶衍生物，特别是黑皮质素4受体拮抗剂。 拮抗剂可用于治疗疾病和疾病，例如由例如， 癌症，慢性肾脏疾病（CKD）或慢性心力衰竭（CHF），肌肉消瘦，由例如， 化疗或放疗，神经性厌食，肌萎缩性侧索硬化（ALS），疼痛，神经性疼痛，焦虑和抑郁。

公开(公告)号：US20080058324A1

公开(公告)日：2008-03-06

申请号：US11574035

申请日：2005-08-22

申请人： Philipp Weyermann ,  Andreas Von Sprecher ,  Marco Hennebohle ,  Holger Herzner ,  Cyrille Lescop ,  Herve Siendt

发明人： Philipp Weyermann ,  Andreas Von Sprecher ,  Marco Hennebohle ,  Holger Herzner ,  Cyrille Lescop ,  Herve Siendt

IPC分类号： A61K31/381 ,  A61K31/4436 ,  A61K31/5377 ,  A61P21/00 ,  A61P25/00 ,  A61P9/00 ,  C07D333/24 ,  C07D409/02 ,  C07D413/02

CPC分类号： C07K5/0202

摘要： The present invention relates to novel a-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 condition 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 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 can he used to treat mitochondrial disorders and neurodegenerative diseases, where elevated levels of oxidative stress are involved. In addition they induce the expression of utrophin, which is beneficial for the treatment of Duchenne Muscular Dystrophy and Becker Muscular Dystrophy.

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的新型α-酮羰基钙蛋白酶抑制剂，包括Duchenne肌营养不良症，Becker肌营养不良症和其他肌营养不良症。 也可以治疗消除萎缩和一般肌肉消瘦。 眼睛疾病，特别是白内障也可以治疗。 一般来说，所有涉及钙蛋白水平升高的情况都可以被处理。 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析蛋白酶也可以被抑制，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，可用于治疗线粒体疾病和神经变性疾病，其中涉及氧化应激水平升高。 此外，它们诱导utrophin的表达，其有利于治疗杜氏肌营养不良症和贝克肌营养不良症。

公开(公告)号：US20070293486A1

公开(公告)日：2007-12-20

申请号：US11574095

申请日：2005-08-22

申请人： Philipp Weyermann ,  Andreas Von Sprecher ,  Marco Hennebohle ,  Holger Herzner ,  Cyrille Lescop ,  Herve Siendt

发明人： Philipp Weyermann ,  Andreas Von Sprecher ,  Marco Hennebohle ,  Holger Herzner ,  Cyrille Lescop ,  Herve Siendt

IPC分类号： A61K31/535 ,  A61K31/38 ,  A61K31/385 ,  C07D339/02 ,  C07D413/00 ,  C07D401/00 ,  C07D333/10 ,  A61K31/44

CPC分类号： C07K5/0202 ,  A61K38/00

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 condition 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 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 can be used to treat mitochondrial disorders and neurodegenerative diseases, where elevated levels of oxidative stress are involved. In addition they introduce the expression of utrophin, which is beneficial for the treatment of Duchenne Muscular Dystrophy and Becker Muscular Dystrophy.

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，所有涉及钙蛋白水平升高的情况都可以被处理。 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析蛋白酶也可以被抑制，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通过氧化应激的细胞损伤的抑制剂，其可用于治疗涉及氧化应激水平升高的线粒体病症和神经变性疾病。 此外，它们引入utrophin的表达，其有利于治疗Duchenne肌营养不良症和Becker肌营养不良症。