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公开(公告)号：US08362016B2
公开(公告)日：2013-01-29
申请号：US13079460
申请日：2011-04-04
申请人： Per Sauerberg , Pavel Pihera , Zdenek Polivka , Miroslav Havranek , Ingrid Pettersson , John Patrick Mogensen
发明人： Per Sauerberg , Pavel Pihera , Zdenek Polivka , Miroslav Havranek , Ingrid Pettersson , John Patrick Mogensen
IPC分类号： A61K31/5375 , C07D295/155
CPC分类号： A61K31/5377 , A61K31/192 , A61K31/195 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4402 , A61K31/445 , A61K31/495 , A61K31/5375 , C07C59/70 , C07C217/48 , C07C323/16 , C07C323/32 , C07C2601/02 , C07D211/46 , C07D213/30 , C07D213/36 , C07D231/12 , C07D265/30 , C07D295/096 , C07D295/112 , C07D307/79 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/54
摘要： Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPARδ and should be useful for treating conditions mediated by the same.
摘要翻译： 通式（I）的新型化合物，这些化合物作为药物组合物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。 本发明化合物是PPARδ的活化剂，应用于治疗由其介导的病症。
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公开(公告)号：US20110245244A1
公开(公告)日：2011-10-06
申请号：US13079460
申请日：2011-04-04
申请人： Per Sauerberg , Pavel Pihera , Zdenek Polivka , Miroslav Havranek , Ingrid Pettersson , John Patrick Mogensen
发明人： Per Sauerberg , Pavel Pihera , Zdenek Polivka , Miroslav Havranek , Ingrid Pettersson , John Patrick Mogensen
IPC分类号： A61K31/5377 , C07D413/12 , C07D333/60 , A61K31/381 , C07D265/30 , A61K31/5375 , C07D211/62 , A61K31/445 , C07C59/68 , A61K31/192 , C07D213/55 , A61K31/4402 , C07D231/12 , A61K31/415 , C07D241/04 , A61K31/495 , C07D207/04 , A61K31/40 , C07D405/10 , A61K31/4025 , A61P3/10
CPC分类号： A61K31/5377 , A61K31/192 , A61K31/195 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4402 , A61K31/445 , A61K31/495 , A61K31/5375 , C07C59/70 , C07C217/48 , C07C323/16 , C07C323/32 , C07C2601/02 , C07D211/46 , C07D213/30 , C07D213/36 , C07D231/12 , C07D265/30 , C07D295/096 , C07D295/112 , C07D307/79 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/54
摘要： Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPARδ and should be useful for treating conditions mediated by the same.
摘要翻译： 通式（I）的新型化合物，这些化合物作为药物组合物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。 本发明化合物是PPARδ的活化剂，应用于治疗由其介导的病症。
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公开(公告)号：US07723323B2
公开(公告)日：2010-05-25
申请号：US12038255
申请日：2008-02-27
申请人： Henrik Sune Andersen , Gita Camilla Tejlgaard Kampen , Inge Thoger Christensen , John Patrick Mogensen , Annette Rosendal Larsen
发明人： Henrik Sune Andersen , Gita Camilla Tejlgaard Kampen , Inge Thoger Christensen , John Patrick Mogensen , Annette Rosendal Larsen
IPC分类号： A61K31/397 , C07D233/00
CPC分类号： C07D471/04 , A61K31/4745 , A61K31/4985 , A61K31/519 , A61K31/5513 , A61K45/06 , C07D487/04 , C07D487/08
摘要： The use of fused 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
摘要翻译： 已经描述了使用稠合的1,2,4-三唑来调节11β-羟基类固醇脱氢酶1型（11＆amp; HSD1）的活性和这些化合物作为药物组合物的用途。 还描述了一类新的稠合的1,2,4-三唑，它们在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途。 本发明化合物是调节剂，更具体地说是11β和HSD1活性的抑制剂，并且可用于治疗，预防和/或预防一系列医学病症，其中期望活性糖皮质激素的细胞内浓度降低。
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公开(公告)号：US20090093484A1
公开(公告)日：2009-04-09
申请号：US12097564
申请日：2006-12-21
申请人： Per Sauerberg , Pavel Pihera , Zdenek Polivka , Miroslav Havranek , Ingrid Pettersson , John Patrick Mogensen
发明人： Per Sauerberg , Pavel Pihera , Zdenek Polivka , Miroslav Havranek , Ingrid Pettersson , John Patrick Mogensen
IPC分类号： A61K31/192 , C07C321/26 , C07D295/182 , C07D213/55 , C07C59/58 , A61P3/10 , C07D231/12 , A61K31/5375 , A61K31/44 , A61K31/415
CPC分类号： A61K31/5377 , A61K31/192 , A61K31/195 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4402 , A61K31/445 , A61K31/495 , A61K31/5375 , C07C59/70 , C07C217/48 , C07C323/16 , C07C323/32 , C07C2601/02 , C07D211/46 , C07D213/30 , C07D213/36 , C07D231/12 , C07D265/30 , C07D295/096 , C07D295/112 , C07D307/79 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/54
摘要： Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPARδ and should be useful for treating conditions mediated by the same.
摘要翻译： 通式（I）的新型化合物，这些化合物作为药物组合物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。 本发明化合物是PPARδ的活化剂，应用于治疗由其介导的病症。
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5.发明授权Peroxisome proliferator activated receptor-active arylene acetic acid derivatives 有权过氧化物酶体增殖物激活受体活性亚芳基乙酸衍生物公开(公告)号：US07129268B2
公开(公告)日：2006-10-31
申请号：US10693161
申请日：2003-10-24
申请人： Lone Jeppesen , John Patrick Mogensen , Ingrid Pettersson , Per Sauerberg , Pavel Pihera , Miroslav Havranek
发明人： Lone Jeppesen , John Patrick Mogensen , Ingrid Pettersson , Per Sauerberg , Pavel Pihera , Miroslav Havranek
IPC分类号： A61K31/19 , C07C59/48 , C07C69/76 , C07D333/56 , C07D307/38
CPC分类号： C07C323/20 , C07C59/68 , C07C69/712
摘要： Novel compounds of the general formula (I), wherein Ar, R1, R2, X1, X2, Y1, Y, and Z are as defined in the specification, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPARδ subtype.
摘要翻译： 新的通式（I）化合物，其中Ar，R 1，R 2，X 1，X 2， Y 1和Y 1如说明书中所定义，这些化合物作为药物组合物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。 本发明化合物可用于治疗和/或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，特别是PPARδ亚型。
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公开(公告)号：US06242443B1
公开(公告)日：2001-06-05
申请号：US08877456
申请日：1997-06-17
申请人： Bernard Pirotte , Philippe Lebrun , Pascal De Tullio , Fabian Somers , Jacques Delarge , John Bondo Hansen , Flemming Elmelund Nielsen , Holger Claus Hansen , John Patrick Mogensen , Tina Møller-Tagmose
发明人： Bernard Pirotte , Philippe Lebrun , Pascal De Tullio , Fabian Somers , Jacques Delarge , John Bondo Hansen , Flemming Elmelund Nielsen , Holger Claus Hansen , John Patrick Mogensen , Tina Møller-Tagmose
IPC分类号： C07D28524
CPC分类号： A61K31/541 , A61K31/5415 , C07D285/24 , C07D453/02 , C07D453/06
摘要： 1,2,4-Benzothiadiazine derivatives represented by formula wherein D, R1, R2, R3, R4, R5, R12, R13, R14, R15 are defined in the description, composition thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.
摘要翻译： 所述化合物的制备方法及其制备方法在本说明书中进行了说明，其中，式（Ⅳ）所示的1,2,4-苯并噻二嗪衍生物由式Ⅵ所示，D，R 1，R 2，R 3，R 4，R 5，R 12，R 13，R 14， 可用于治疗中枢神经系统疾病，心血管系统，肺系统，胃肠系统和内分泌系统。
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公开(公告)号：US07943613B2
公开(公告)日：2011-05-17
申请号：US12097564
申请日：2006-12-21
申请人： Per Sauerberg , Pavel Pihera , Zdenek Polivka , Miroslav Havranek , Ingrid Pettersson , John Patrick Mogensen
发明人： Per Sauerberg , Pavel Pihera , Zdenek Polivka , Miroslav Havranek , Ingrid Pettersson , John Patrick Mogensen
IPC分类号： C07D295/155 , A61K31/5375
CPC分类号： A61K31/5377 , A61K31/192 , A61K31/195 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4402 , A61K31/445 , A61K31/495 , A61K31/5375 , C07C59/70 , C07C217/48 , C07C323/16 , C07C323/32 , C07C2601/02 , C07D211/46 , C07D213/30 , C07D213/36 , C07D231/12 , C07D265/30 , C07D295/096 , C07D295/112 , C07D307/79 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/54
摘要： Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPARδ and should be useful for treating conditions mediated by the same.
摘要翻译： 通式（I）的新型化合物，这些化合物作为药物组合物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。 本发明化合物是PPARδ的活化剂，可用于治疗由其介导的病症。
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公开(公告)号：US20080153807A1
公开(公告)日：2008-06-26
申请号：US12038255
申请日：2008-02-27
申请人： Henrik Sune Andersen , Gita Camilla Tejlgaard Kampen , Inge Thoger Christensen , John Patrick Mogensen , Annette Rosendal Larsen
发明人： Henrik Sune Andersen , Gita Camilla Tejlgaard Kampen , Inge Thoger Christensen , John Patrick Mogensen , Annette Rosendal Larsen
IPC分类号： A61K31/55 , C07D487/04 , A61K31/437 , A61P3/10 , A61P3/00
CPC分类号： C07D471/04 , A61K31/4745 , A61K31/4985 , A61K31/519 , A61K31/5513 , A61K45/06 , C07D487/04 , C07D487/08
摘要： The use of fused 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
摘要翻译： 已经描述了使用稠合的1,2,4-三唑来调节11β-羟类固醇脱氢酶1型（11betaHSD1）的活性以及这些化合物作为药物组合物的用途。 还描述了一类新的稠合的1,2,4-三唑，它们在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途。 本发明化合物是调节剂，更具体地是11betaHSD1活性的抑制剂，并且可用于治疗，预防和/或预防一系列需要活性糖皮质激素的细胞内浓度降低的医学疾病。
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公开(公告)号：US07358238B2
公开(公告)日：2008-04-15
申请号：US11247847
申请日：2005-10-11
申请人： Henrik Sune Andersen , Gita Camilla Tejlgaard Kampen , Inge Thoger Christensen , John Patrick Mogensen , Annette Rosendal Larsen
发明人： Henrik Sune Andersen , Gita Camilla Tejlgaard Kampen , Inge Thoger Christensen , John Patrick Mogensen , Annette Rosendal Larsen
IPC分类号： A61K31/397 , C07D233/00
CPC分类号： C07D471/04 , A61K31/4745 , A61K31/4985 , A61K31/519 , A61K31/5513 , A61K45/06 , C07D487/04 , C07D487/08
摘要： The use of fused 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
摘要翻译： 已经描述了使用稠合的1,2,4-三唑来调节11β-羟类固醇脱氢酶1型（11betaHSD1）的活性以及这些化合物作为药物组合物的用途。 还描述了一类新的稠合的1,2,4-三唑，它们在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途。 本发明化合物是调节剂，更具体地是11betaHSD1活性的抑制剂，并且可用于治疗，预防和/或预防一系列需要活性糖皮质激素的细胞内浓度降低的医学疾病。
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10.发明授权Combination therapy using a dual PPAR-α/PPAR-γ activator and a GLP-1 derivative for the treatment of metabolic syndrome and related diseases and disorders 失效使用双重PPAR-α/ PPAR-γ激活剂和GLP-1衍生物治疗代谢综合征和相关疾病和病症的联合疗法公开(公告)号：US07202213B2
公开(公告)日：2007-04-10
申请号：US10442284
申请日：2003-05-20
IPC分类号： A61K38/00
CPC分类号： C07C69/734 , C07C59/68
摘要： The present invention relates to a pharmaceutical composition comprising a dual Peroxisome Proliferator-Activated Receptor-alpha/Peroxisome Proliferator-Activated Receptor-gama activator (PPAR-α/PPAR-γ) and a Glucagon Like Peptide-1 (GLP-1) derivative for treating, preventing and reducing the risk of developing Type 2 diabetes, insulin resistance, dyslipidemia, obesity, hypertension and other related diseases and disorders.
摘要翻译： 本发明涉及一种药物组合物，其包含双过氧化物酶体增殖物激活受体-α/过氧化物酶体增殖物激活受体激动剂（PPAR-α/ PPAR-γ）和胰高血糖素样肽-1（GLP-1）衍生物 治疗，预防和降低发生2型糖尿病，胰岛素抵抗，血脂异常，肥胖，高血压和其他相关疾病和病症的风险。
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