专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2009080291A1 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：WO2009080291A1
公开(公告)日：2009-07-02
申请号：PCT/EP2008/010849
申请日：2008-12-18
申请人： SANTHERA PHARMACEUTICALS (SCHWEIZ) AG , SOEBERDT, Michael , WEYERMANN, Philipp , SIENDT, Hervé , NORDHOFF, Sonja , FEURER, Achim , TERINEK, Miroslav
发明人： SOEBERDT, Michael , WEYERMANN, Philipp , SIENDT, Hervé , NORDHOFF, Sonja , FEURER, Achim , TERINEK, Miroslav
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4188
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。

2. 发明申请

WO2012101139A1 PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDE 审中-公开
标题翻译：制备吡唑羧酸酰胺的方法
公开(公告)号：WO2012101139A1
公开(公告)日：2012-08-02
申请号：PCT/EP2012/051075
申请日：2012-01-25
申请人： SYNGENTA PARTICIPATIONS AG , TERINEK, Miroslav , FABER, Dominik , KOENIG, Stefan
发明人： TERINEK, Miroslav , FABER, Dominik , KOENIG, Stefan
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 1 C(X)-CI (XI); wherein X is oxygen or sulfur; R 1 is chloro if X is oxygen or sulfur; or R1 is C 1 -C 6 alkoxy, CH 3 -C(=CH 2 )-0-, phenoxy or trichloromethoxy if X is oxygen; and a) if R 1 is chloro and the compound of formula (XI) was added to the compound of formula (VIII); reacting the so obtained product of formula (Xlla) wherein X is oxygen or sulfur; with the compound of formula (IX) b) if R 1 is chloro and the compound of formula (VIII) was added to the compound of formula (XI); or R 1 is C 1 -C 6 alkoxy, CH 3 -C(=CH 2 )-0-, phenoxy or trichloromethoxy if X is oxygen; reacting the so obtained product of formula (XII) wherein X is oxygen or sulfur; R 1 is chloro if X is oxygen or sulfur; or R 1 is C 1 -C 6 alkoxy, CH 3 -C(=CH 2 )-0-, phenoxy or trichloromethoxy if X is oxygen; with the compound of formula (IX).
摘要翻译：本发明涉及一种制备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）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，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; 使所得得到的式（XIII）的化合物（其中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。

3. 发明申请

WO2009010299A1 SUBSTITUTED HETEROARYLPIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS 审中-公开
标题翻译：作为MELANOCORTIN-4受体调节剂的替代异丙基哌啶衍生物
公开(公告)号：WO2009010299A1
公开(公告)日：2009-01-22
申请号：PCT/EP2008005913
申请日：2008-07-18
申请人： SANTHERA PHARMACEUTICALS CH , HERZNER HOLGER , SOEBERDT MICHAEL , WEYERMANN PHILIPP , NORDHOFF SONJA , FEURER ACHIM , DEPPE HOLGER , SIENDT HERVE , TERINEK MIROSLAV , RUMMEY CHRISTIAN
发明人： HERZNER HOLGER , SOEBERDT MICHAEL , WEYERMANN PHILIPP , NORDHOFF SONJA , FEURER ACHIM , DEPPE HOLGER , SIENDT HERVE , TERINEK MIROSLAV , RUMMEY CHRISTIAN
IPC分类号： C07D401/04 , A61K31/44 , A61P3/04 , A61P3/10 , A61P15/00 , A61P25/00 , A61P25/22 , A61P25/24 , A61P35/00 , C07D401/14 , C07D417/14 , C07D453/02
CPC分类号： C07D401/04 , C07D401/14 , C07D417/14 , C07D453/02
摘要： The present invention relates to substituted heteroarylpiperidine derivative (I) as melanocortin-4 receptor modulators. Depending on the structure and th 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：本发明涉及取代的杂芳基哌啶衍生物（I）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

WO2008116665A1 SUBSTITUTED IMIDAZOPYRIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：取代的咪唑并吡啶衍生物作为黑皮素-4受体拮抗剂
公开(公告)号：WO2008116665A1
公开(公告)日：2008-10-02
申请号：PCT/EP2008/002498
申请日：2008-03-28
申请人： SANTHERA PHARMACEUTICALS (SCHWEIZ) AG , METZ, Günther , DEPPE, Holger , ABEL, Ulrich , FEURER, Achim , OTT, Inge , NORDHOFF, Sonja , SOEBERDT, Michael , HOFFMANN-ENGERS, Barbara , WEYERMANN, Philipp , SIENDT, Hervé , RUMMEY, Christian , TERINEK, Miroslav , HENNEBÖHLE, Marco , HERZNER, Holger , MONDADORI, Cesare
发明人： METZ, Günther , DEPPE, Holger , ABEL, Ulrich , FEURER, Achim , OTT, Inge , NORDHOFF, Sonja , SOEBERDT, Michael , HOFFMANN-ENGERS, Barbara , WEYERMANN, Philipp , SIENDT, Hervé , RUMMEY, Christian , TERINEK, Miroslav , HENNEBÖHLE, Marco , HERZNER, Holger , MONDADORI, Cesare
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P35/00 , A61P25/00 , A61P21/00
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，特别是作为黑皮质素-4受体拮抗剂。拮抗剂可用于治疗诸如癌症恶病质，肌肉萎缩，厌食症，萎缩性侧索硬化（ALS），焦虑和抑郁等病症和疾病。

5. 发明申请

WO2010034500A1 SUBSTITUTED IMIDAZOPYRIDINE, IMIDAZOPYRAZINE, IMIDAZOPYRIDAZINE AND IMIDAZOPYRIMIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：取代的咪唑吡啶，咪唑嗪，咪唑吡嗪和咪唑啉酮衍生物作为梅毒素-4受体拮抗剂
公开(公告)号：WO2010034500A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/006917
申请日：2009-09-24
申请人： SANTHERA PHARMACEUTICALS (SCHWEIZ) AG , TERINEK, Miroslav , NORDHOFF, Sonja , SOEBERDT, Michael , RUMMEY, Christian , FEURER, Achim , WEYERMANN, Philipp
发明人： TERINEK, Miroslav , NORDHOFF, Sonja , SOEBERDT, Michael , RUMMEY, Christian , FEURER, Achim , WEYERMANN, Philipp
IPC分类号： C07D471/04 , A61K31/437 , A61P3/00
CPC分类号： C07D471/04
摘要： The present invention relates to substituted imidazopyridine derivatives, imidazopyrazine derivatives, imidazopyridazine derivatives and imidazopyrimidine derivatives according to formula (I) 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, nausea and emesis.
摘要翻译：本发明涉及作为黑皮质素-4受体（MC-4R）调节剂的取代咪唑并吡啶衍生物，咪唑并吡嗪衍生物，咪唑并哒嗪衍生物和式（I）咪唑并嘧啶衍生物，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，恶心和呕吐。

6. 发明申请

WO2009010299A8 SUBSTITUTED HETEROARYLPIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2009010299A8
公开(公告)日：2009-01-22
申请号：PCT/EP2008/005913
申请日：2008-07-18
申请人： SANTHERA PHARMACEUTICALS (SCHWEIZ) AG , HENNEBÖHLE, Marco , HERZNER, Holger , SOEBERDT, Michael , WEYERMANN, Philipp , NORDHOFF, Sonja , FEURER, Achim , DEPPE, Holger , SIENDT, Hervé , TERINEK, Miroslav , RUMMEY, Christian
发明人： HENNEBÖHLE, Marco , HERZNER, Holger , SOEBERDT, Michael , WEYERMANN, Philipp , NORDHOFF, Sonja , FEURER, Achim , DEPPE, Holger , SIENDT, Hervé , TERINEK, Miroslav , RUMMEY, Christian
IPC分类号： C07D401/04 , C07D401/14 , C07D417/14 , C07D453/02 , A61K31/44 , A61P3/04 , A61P3/10 , A61P15/00 , A61P35/00 , A61P25/00 , A61P25/22 , A61P25/24
摘要： The present invention relates to substituted heteroarylpiperidine derivative (I) 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.

7. 发明申请

WO2008116665A8 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：WO2008116665A8
公开(公告)日：2008-12-11
申请号：PCT/EP2008002498
申请日：2008-03-28
申请人： SANTHERA PHARMACEUTICALS CH , METZ GUENTHER , DEPPE HOLGER , ABEL ULRICH , FEURER ACHIM , OTT INGE , NORDHOFF SONJA , SOEBERDT MICHAEL , HOFFMANN-ENGER BARBARA , WEYERMANN PHILIPP , SIENDT HERVE , RUMMEY CHRISTIAN , TERINEK MIROSLAV , HENNEBOEHLE MARCO , HERZNER HOLGER , MONDADORI CESARE
发明人： METZ GUENTHER , DEPPE HOLGER , ABEL ULRICH , FEURER ACHIM , OTT INGE , NORDHOFF SONJA , SOEBERDT MICHAEL , HOFFMANN-ENGER BARBARA , WEYERMANN PHILIPP , SIENDT HERVE , RUMMEY CHRISTIAN , TERINEK MIROSLAV , HENNEBOEHLE MARCO , HERZNER HOLGER , MONDADORI CESARE
IPC分类号： C07D471/04 , A61K31/437 , A61P21/00 , A61P25/00 , A61P35/00 , C07D519/00
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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式