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1. 发明申请

WO2004083208A8 SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS 审中-公开
标题翻译：作为MELANOCORTIN-4受体调节剂的替代哌啶和哌啶衍生物
公开(公告)号：WO2004083208A8
公开(公告)日：2005-01-20
申请号：PCT/EP2004002896
申请日：2004-03-19
申请人： MYOCONTRACT LTD , SOEBERDT MICHAEL , WEYERMANN PHILIPP , VON SPRECHER ANDREAS , HENNEBOEHLE MARCO
发明人： SOEBERDT MICHAEL , WEYERMANN PHILIPP , VON SPRECHER ANDREAS , HENNEBOEHLE MARCO
IPC分类号： A61K31/451 , A61K31/4725 , A61P3/04 , A61P15/00 , A61P25/22 , A61P25/24 , C07D207/26 , C07D207/27 , C07D211/60 , C07D211/62 , C07D295/12 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D471/10 , C07D521/00
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症，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。

2. 发明申请

WO2004083208A1 SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS 审中-公开
标题翻译：作为MELANOCORTIN-4受体调节剂的替代哌啶和哌嗪衍生物
公开(公告)号：WO2004083208A1
公开(公告)日：2004-09-30
申请号：PCT/EP2004/002896
申请日：2004-03-19
申请人： MYOCONTRACT LTD. , SOEBERDT, Michael , WEYERMANN, Philipp , VON SPRECHER, Andreas , HENNEBÖHLE, Marco
发明人： SOEBERDT, Michael , WEYERMANN, Philipp , VON SPRECHER, Andreas , HENNEBÖHLE, Marco
IPC分类号： C07D471/10
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症，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。

3. 发明申请

WO2004083209A1 SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS 审中-公开
标题翻译：作为MELANOCORTIN-4受体调节剂的替代哌啶和哌嗪衍生物
公开(公告)号：WO2004083209A1
公开(公告)日：2004-09-30
申请号：PCT/EP2004/002907
申请日：2004-03-19
申请人： MYOCONTRACT LTD. , SOEBERDT, Michael , WEYERMANN, Philipp , VON SPRECHER, Andreas
发明人： SOEBERDT, Michael , WEYERMANN, Philipp , VON SPRECHER, Andreas
IPC分类号： C07D471/10
CPC分类号： C07D471/10 , A61K31/438 , A61K31/454 , A61K31/4545 , A61K31/496 , C07D311/24 , C07D401/12 , C07D401/14 , C07D405/14
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，例如癌症恶病质，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。

4. 发明申请

WO2004083198A1 SUBSTITUTED CYCLOHEXYL AND PIPERIDINYL DERIVATES AS MELANOCORTIN-4 RECEPTOR MODULATORS 审中-公开
标题翻译：作为MELANOCORTIN-4受体调节剂的替代环己基和哌啶衍生物
公开(公告)号：WO2004083198A1
公开(公告)日：2004-09-30
申请号：PCT/EP2004/002909
申请日：2004-03-19
申请人： MYOCONTRACT LTD. , SOEBERDT, Michael , WEYERMANN, Philipp , VON SPRECHER, Andreas
发明人： SOEBERDT, Michael , WEYERMANN, Philipp , VON SPRECHER, Andreas
IPC分类号： C07D401/10
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症，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。

5. 发明申请

WO2004003565A2 A SCREENING METHOD AND COMPOUNDS FOR TREATING FRIEDREICH ATAXIA 审中-公开
标题翻译：一种筛选方法和用于治疗苦荞麦的化合物
公开(公告)号：WO2004003565A2
公开(公告)日：2004-01-08
申请号：PCT/EP2003/007006
申请日：2003-07-01
申请人： MYOCONTRACT LTD , MEIER, Thomas , JAUSLIN, Matthias , SCHOUMACHER, Fabrice
发明人： MEIER, Thomas , JAUSLIN, Matthias , SCHOUMACHER, Fabrice
IPC分类号： G01N33/68
CPC分类号： G01N33/6896 , G01N2500/10 , G01N2800/2835
摘要： The present invention relates to a method for identifying and/or validating candidate substances for the treatment of Friedreich Ataxia (FRDA). Furthermore, the present invention relates to the use of selenium, Ebselen and Glutathione peroxidase (GPX) mimetics for the preparation of a medicament for the treatment of FRDA. Another aspect of the present invention relates to the use of cells with reduced frataxin expression for identifying and/or validating candidate substances for the treatment of Friedreich Ataxia.
摘要翻译：本发明涉及鉴定和/或验证用于治疗弗里德赖希氏共济失调（FRDA）的候选物质的方法。此外，本发明涉及硒，依布硒啉和谷胱甘肽过氧化物酶（GPX）模拟物在制备用于治疗FRDA的药物中的用途。本发明的另一方面涉及具有减少的frataxin表达的细胞用于鉴定和/或验证用于治疗Friedreich共济失调的候选物质的用途。

6. 发明申请

WO2004003565A3 A SCREENING METHOD AND COMPOUNDS FOR TREATING FRIEDREICH ATAXIA 审中-公开
标题翻译：一种用于处理FRIEDREICH ATAXIA的筛选方法和化合物
公开(公告)号：WO2004003565A3
公开(公告)日：2004-10-14
申请号：PCT/EP0307006
申请日：2003-07-01
申请人： MYOCONTRACT LTD , MEIER THOMAS , JAUSLIN MATTHIAS , SCHOUMACHER FABRICE
发明人： MEIER THOMAS , JAUSLIN MATTHIAS , SCHOUMACHER FABRICE
IPC分类号： G01N33/68 , A61K31/12
CPC分类号： G01N33/6896 , G01N2500/10 , G01N2800/2835
摘要： The present invention relates to a method for identifying and/or validating candidate substances for the treatment of Friedreich Ataxia (FRDA). Furthermore, the present invention relates to the use of selenium, Ebselen and Glutathione peroxidase (GPX) mimetics for the preparation of a medicament for the treatment of FRDA. Another aspect of the present invention relates to the use of cells with reduced frataxin expression for identifying and/or validating candidate substances for the treatment of Friedreich Ataxia.
摘要翻译：本发明涉及用于鉴定和/或验证用于治疗弗里德赖希共济失调（FRDA）的候选物质的方法。此外，本发明涉及硒，依布硒和谷胱甘肽过氧化物酶（GPX）模拟物在制备用于治疗FRDA的药物中的用途。本发明的另一方面涉及具有降低的frataxin表达的细胞用于鉴定和/或验证用于治疗Friedreich共济失调的候选物质的用途。

7. 发明申请

WO2004083199A1 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色素4受体调节剂
公开(公告)号：WO2004083199A1
公开(公告)日：2004-09-30
申请号：PCT/EP2004/002908
申请日：2004-03-19
申请人： MYOCONTRACT LTD. , SOEBERDT, Michael , WEYERMANN, Philipp , VON SPRECHER, Andreas
发明人： SOEBERDT, Michael , WEYERMANN, Philipp , VON SPRECHER, Andreas
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D405/12
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：本发明涉及作为黑皮质素-4受体（MC-4R）调节剂的新型取代的哌啶和哌嗪衍生物。本发明的MC-4R激动剂可用于治疗诸如肥胖症，糖尿病和性功能障碍的疾病和疾病，而MC-4R拮抗剂可用于治疗疾病和疾病，例如癌症恶病质，肌肉萎缩，厌食，焦虑和抑郁。所有涉及MC-4R调控的疾病和病症都可以用本发明的化合物治疗。

8. 发明申请

WO2004078908A2 ALPHA-KETO CARBONYL CALPAIN INHIBITORS 审中-公开
标题翻译： ALPHA-KETO CARBONYL CALPAIN抑制剂
公开(公告)号：WO2004078908A2
公开(公告)日：2004-09-16
申请号：PCT/EP2004/002142
申请日：2004-03-03
申请人： MYOCONTRACT LTD. , HERZNER, Holger , WEYERMANN, Philipp , VON SPRECHER, Andreas , HENNEBÖHLE, Marco , LESCOP, Cyrille , SIENDT, Hervé
发明人： HERZNER, Holger , WEYERMANN, Philipp , VON SPRECHER, Andreas , HENNEBÖHLE, Marco , LESCOP, Cyrille , SIENDT, Hervé
IPC分类号： C12N
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析蛋白酶（MCP）也可以被抑制，因此化合物可以是。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。

9. 发明公开

EP1460073A1 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：EP1460073A1
公开(公告)日：2004-09-22
申请号：EP03006254.1
申请日：2003-03-20
申请人： MyoContract Ltd.
发明人： Soeberdt, Michael , Weyermann, Philipp , Sprecher von, Andreas
IPC分类号： C07D471/10 , C07D311/24 , C07D405/14 , C07D401/12 , C07D401/14 , A61K31/438 , A61K31/496 , A61K31/454 , A61K31/4545 , A61P3/04 , A61P15/00 , A61P25/22 , A61P25/24
CPC分类号： C07D471/10 , A61K31/438 , A61K31/454 , A61K31/4545 , A61K31/496 , C07D311/24 , C07D401/12 , C07D401/14 , C07D405/14
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.

10. 发明公开

EP1460069A1 Substituted cyclohexyl and piperidinyl derivatives as melanocortin-4 receptor modulators 审中-公开
标题翻译：取代基环己基 - 和哌啶衍生物黑素皮质素-4受体调节剂
公开(公告)号：EP1460069A1
公开(公告)日：2004-09-22
申请号：EP03006255.8
申请日：2003-03-20
申请人： MyoContract Ltd.
发明人： Soeberdt, Michael , Weyermann, Philipp , Sprecher von, Andreas
IPC分类号： C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D217/26 , C07D211/70 , A61K31/4725 , A61P3/04 , A61P15/00 , A61P25/22 , A61P25/24
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：本发明涉及作为黑皮质素-4受体（MC-4R）调节剂的新型取代的环己基和哌啶衍生物。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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