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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

US20130310592A1 PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES 有权
标题翻译：制备吡唑羧酸酰胺的方法
公开(公告)号：US20130310592A1
公开(公告)日：2013-11-21
申请号：US13981913
申请日：2012-01-25
申请人： Miroslav Terinek , Dominik Faber , Stefan Koenig
发明人： Miroslav Terinek , Dominik Faber , Stefan Koenig
IPC分类号： C07D231/14 , C07C251/56
CPC分类号： C07C231/14 , C07C251/56 , C07C251/64 , C07C329/02 , C07C329/04 , C07C2603/66 , C07D231/14
摘要： The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1 H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide by acylating the oxime oxygen of the compound of formula (VIII), in the presence of a solvent and an acylating agent of formula (XI) R 1C(X)—CI (XI); wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(═CH2)-0-, phenoxy or trichloromethoxy if X is oxygen; and a) if R1 is chloro and the compound of formula (XI) was added to the compound of formula (VIII); reacting the so obtained product of formula (XIIa) wherein X is oxygen or sulfur; with the compound of formula (IX) b) if R1 is chloro and the compound of formula (VIII) was added to the compound of formula (XI); or R1 is C1-C6alkoxy, CH3—C(═CH2)-0-, phenoxy or trichloromethoxy if X is oxygen; reacting the so obtained product of formula (XII) wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(═CH2)-0-, phenoxy or trichloromethoxy if X is oxygen; with the compound of formula (IX).
摘要翻译：本发明涉及制备3-二氟甲基-1-甲基-1H-吡唑-4-羧酸（9-二氯亚甲基-1,2,3,4-四氢-1,4-亚甲基 - 萘-1-基）（XI）R 1C（X）-CI（XI）的溶剂和酰化剂的存在下酰化式（Ⅷ）化合物的肟氧; 其中X是氧或硫; 如果X是氧或硫，则R1是氯; 或者如果X是氧，R 1是C 1 -C 6烷氧基，CH 3 C（= CH 2）-O-，苯氧基或三氯甲氧基; 和a）如果R1是氯，并且将式（XI）化合物加入到式（VIII）化合物中; 使所得的式（XIIa）化合物与X为氧或硫反应; 与式（Ⅸ）化合物b）如果R 1是氯，并将式（Ⅷ）化合物加到式（Ⅺ）化合物中; 或者如果X是氧，R 1是C 1 -C 6烷氧基，CH 3 C（= CH 2）-O-，苯氧基或三氯甲氧基; 使所得的式（XII）化合物（其中X是氧或硫）反应; 如果X是氧或硫，则R1是氯; 或者如果X是氧，R 1是C 1 -C 6烷氧基，CH 3 C（= CH 2）-O-，苯氧基或三氯甲氧基; 与式（IX）的化合物反应。

6. 发明授权

US08895757B2 Process for the preparation of pyrazole carboxylic acid amides 有权
标题翻译：制备吡唑羧酸酰胺的方法
公开(公告)号：US08895757B2
公开(公告)日：2014-11-25
申请号：US13981913
申请日：2012-01-25
申请人： Miroslav Terinek , Dominik Faber , Stefan Koenig
发明人： Miroslav Terinek , Dominik Faber , Stefan Koenig
IPC分类号： C07D231/14 , C07C251/56 , C07C329/04 , C07C231/14 , C07C329/02 , C07C251/64
CPC分类号： C07C231/14 , C07C251/56 , C07C251/64 , C07C329/02 , C07C329/04 , C07C2603/66 , C07D231/14
摘要： The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide by acylating the oxime oxygen of the compound of formula (VIII), in the presence of a solvent and an acylating agent of formula (XI) R1C(X)—CI (XI); wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(═CH2)—O—, phenoxy or trichloromethoxy if X is oxygen; and a) if R1 is chloro and the compound of formula (XI) was added to the compound of formula (VIII); reacting the so obtained product of formula (XIIa) wherein X is oxygen or sulfur; with the compound of formula (IX) b) if R1 is chloro and the compound of formula (VIII) was added to the compound of formula (XI); or R1 is C1-C6alkoxy, CH3—C(═CH2)—O—, phenoxy or trichloromethoxy if X is oxygen; reacting the so obtained product of formula (XII) wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(═CH2)—O—, phenoxy or trichloromethoxy if X is oxygen; with the compound of formula (IX).
摘要翻译：本发明涉及制备3-二氟甲基-1-甲基-1H-吡唑-4-羧酸（9-二氯亚甲基-1,2,3,4-四氢-1,4-亚甲基 - 萘-5 （XI）R1C（X）-CⅠ（XI）的溶剂和酰化剂的存在下酰化式（Ⅷ）化合物的肟氧; 其中X是氧或硫; 如果X是氧或硫，则R1是氯; 或者如果X是氧，则R1是C1-C6烷氧基，CH3-C（= CH2）-O-，苯氧基或三氯甲氧基; 和a）如果R1是氯，并且将式（XI）化合物加入到式（VIII）化合物中; 使所得的式（XIIa）化合物与X为氧或硫反应; 与式（Ⅸ）化合物b）如果R 1是氯，并将式（Ⅷ）化合物加到式（Ⅺ）化合物中; 或者如果X是氧，则R1是C1-C6烷氧基，CH3-C（= CH2）-O-，苯氧基或三氯甲氧基; 使所得的式（XII）化合物（其中X是氧或硫）反应; 如果X是氧或硫，则R1是氯; 或者如果X是氧，则R1是C1-C6烷氧基，CH3-C（= CH2）-O-，苯氧基或三氯甲氧基; 与式（IX）的化合物反应。

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