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1. 发明申请

US20100093697A1 Substituted Imidazopyridine Derivatives As Melanocortin-4 Receptor Antagonists 失效
标题翻译：取代的咪唑并吡啶衍生物作为黑皮质素-4受体拮抗剂
公开(公告)号：US20100093697A1
公开(公告)日：2010-04-15
申请号：US12530676
申请日：2008-03-28
申请人： Günther Metz , Holger Deppe , Ulrich Abel , Achim Feurer , Inge Ott , Sonja Nordhoff , Michael Soeberdt , Barbara Hoffmann-Enger , Philipp Weyermann , Hervé Siendt , Christian Rummey , Miroslav Terinek , Marco Henneböhle , Holger Herzner , Cesare Mondadori
发明人： Günther Metz , Holger Deppe , Ulrich Abel , Achim Feurer , Inge Ott , Sonja Nordhoff , Michael Soeberdt , Barbara Hoffmann-Enger , Philipp Weyermann , Hervé Siendt , Christian Rummey , Miroslav Terinek , Marco Henneböhle , Holger Herzner , Cesare Mondadori
IPC分类号： A61K31/551 , C07D471/04 , A61K31/437 , A61K31/497
CPC分类号： C07D471/04 , C07D519/00
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 cancer cachexia, muscle wasting, anorexia, amytrophic lateral sclerosis (ALS), 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，例如癌症恶病质，肌肉消瘦，厌食，肌萎缩性侧索硬化（ALS），焦虑和抑郁。

2. 发明授权

US08236818B2 Substituted imidazopyridine derivatives as melanocortin-4 receptor antagonists 失效
标题翻译：取代的咪唑并吡啶衍生物作为黑皮质素-4受体拮抗剂
公开(公告)号：US08236818B2
公开(公告)日：2012-08-07
申请号：US12530676
申请日：2008-03-28
申请人： Günther Metz , Holger Deppe , Ulrich Abel , Achim Feurer , Inge Ott , Sonja Nordhoff , Michael Soeberdt , Barbara Hoffmann-Enger , Philipp Weyermann , Hervé Siendt , Christian Rummey , Miroslav Terinek , Marco Henneböhle , Holger Herzner , Cesare Mondadori
发明人： Günther Metz , Holger Deppe , Ulrich Abel , Achim Feurer , Inge Ott , Sonja Nordhoff , Michael Soeberdt , Barbara Hoffmann-Enger , Philipp Weyermann , Hervé Siendt , Christian Rummey , Miroslav Terinek , Marco Henneböhle , Holger Herzner , Cesare Mondadori
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04 , C07D519/00
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 cancer cachexia, muscle wasting, anorexia, amytrophic lateral sclerosis (ALS), 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，例如癌症恶病质，肌肉消瘦，厌食，肌萎缩性侧索硬化（ALS），焦虑和抑郁。

3. 发明申请

US20100249093A1 Substituted Heteroarylpiperidine Derivatives As Melanocortin-4 Receptor Modulators 审中-公开
标题翻译：取代的杂芳基哌啶衍生物作为黑皮质素-4受体调节剂
公开(公告)号：US20100249093A1
公开(公告)日：2010-09-30
申请号：US12665771
申请日：2008-07-18
申请人： Marco Henneböhle , Holger Herzner , Michael Soeberdt , Philipp Weyermann , Sonja Nordhoff , Achim Feurer , Holger Deppe , Hervé Siendt , Miroslav Terinek , Christian Rummey
发明人： Marco Henneböhle , Holger Herzner , Michael Soeberdt , Philipp Weyermann , Sonja Nordhoff , Achim Feurer , Holger Deppe , Hervé Siendt , Miroslav Terinek , Christian Rummey
IPC分类号： A61K31/397 , C07D401/14 , A61K31/4545 , C07D403/14 , A61K31/496 , C07D413/14 , A61K31/553 , A61P35/00 , A61P3/04 , A61P3/10 , A61P25/22 , A61P15/00
CPC分类号： C07D401/04 , C07D401/14 , C07D417/14 , C07D453/02
摘要： The present invention relates to substituted heteroarylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, amyotrophic lateral sclerosis (ALS), anxiety and depression. Generally 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：本发明涉及作为黑皮质素-4受体调节剂的取代的杂芳基哌啶衍生物。根据结构和立体化学，本发明的化合物是人黑素皮质素-4受体（MC-4R）的选择性激动剂或选择性拮抗剂。激动剂可以用于治疗疾病和疾病如肥胖，糖尿病和性功能障碍，而拮抗剂可用于治疗疾病和疾病，例如癌症恶病质，肌肉消瘦，厌食，肌萎缩性侧索硬化（ALS）焦虑和抑郁。通常所有涉及MC-4R调节的疾病和病症都可以用本发明的化合物治疗。

4. 发明申请

US20100324036A1 SUBSTITUTED IMIDAZOPYRIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为MELANOCORTIN-4受体拮抗剂的取代的咪唑吡啶衍生物
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。

5. 发明申请

US20110086836A1 Substituted Phenylpiperidine Derivatives As Melanocortin-4 Receptor Modulators 审中-公开
标题翻译：取代的苯基哌啶衍生物作为黑皮质素-4受体调节剂
公开(公告)号：US20110086836A1
公开(公告)日：2011-04-14
申请号：US12293905
申请日：2007-04-05
申请人： Michael Soeberdt , Holger Deppe , Philipp Weyermann , Stephan Bulat , Andreas Von Sprecher , Achim Feurer , Cyrille Lescop , Marco Hennebohle , Sonja Nordhoff
发明人： Michael Soeberdt , Holger Deppe , Philipp Weyermann , Stephan Bulat , Andreas Von Sprecher , Achim Feurer , Cyrille Lescop , Marco Hennebohle , Sonja Nordhoff
IPC分类号： A61K31/454 , C07D401/14 , C07D413/14 , A61K31/5377 , A61K31/4545 , C07D401/12 , A61K31/55 , A61P15/10 , A61P15/00 , A61P3/10 , A61P3/04 , A61P25/22 , A61P25/24 , A61P21/06
CPC分类号： C07D401/10 , C07D211/22 , C07D211/26 , C07D401/12
摘要： The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally 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：本发明涉及取代的苯基哌啶衍生物作为黑皮质素-4受体调节剂。根据结构和立体化学，本发明的化合物是人黑素皮质素-4受体（MC-4R）的选择性激动剂或选择性拮抗剂。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。通常所有涉及MC-4R调节的疾病和病症都可以用本发明的化合物治疗。

6. 发明申请

US20060258598A1 Alpha-keto carbonyl calpain inhibitors 审中-公开
标题翻译： 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。

7. 发明申请

US20080058324A1 Alpha-Keto Carbonyl Calpain Inhibitors 审中-公开
标题翻译： α-酮羰基钙蛋白酶抑制剂
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。

8. 发明申请

US20070293486A1 Alpha-Keto Carbonyl Calpain Inhibitors 审中-公开
标题翻译： α-酮羰基钙蛋白酶抑制剂
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。

9. 发明申请

US20070155783A1 Substituted cyclohexyl and piperidinyl derivates as melanocortin-4 receptor modulators 审中-公开
标题翻译：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。

10. 发明申请

US20070037823A1 Substituted piperidine and piperazine derivatives as melanocortin-4 receptor modulators 审中-公开
标题翻译：取代的哌啶和哌嗪衍生物作为黑皮质素-4受体调节剂
公开(公告)号：US20070037823A1
公开(公告)日：2007-02-15
申请号：US10549942
申请日：2004-03-19
申请人： Michael Soeberdt , Philipp Weyermann , Andreas Von Sprecher , Marco Hennebohle
发明人： Michael Soeberdt , Philipp Weyermann , Andreas Von Sprecher , Marco Hennebohle
IPC分类号： A61K31/496 , A61K31/4709 , A61K31/353
CPC分类号： C07D207/27 , C07D211/60 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D471/10
摘要： The present invention relates to novel substituted piperidine and piperazine 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哌啶和哌嗪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。涉及MC-4R调节的所有疾病和病症均可用本发明的化合物治疗。

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