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1. 发明申请

WO2012080371A1 NEW THIOCARBONATES AS ANTI-INFLAMMATORY AND ANTIOXIDANT COMPOUNDS USEFUL FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译：作为抗炎和抗氧化剂的新型硫酸盐可用于治疗代谢障碍
公开(公告)号：WO2012080371A1
公开(公告)日：2012-06-21
申请号：PCT/EP2011/072819
申请日：2011-12-14
申请人： GENMEDICA THERAPEUTICS SL , CESAR CASTRO PALOMINO LARIA, Julio , MARTI CLAUZEL, Luc , ZORZANO OLARTE, Antonio , GARCIA VICENTE, Silvia , MIAN, Alec
发明人： CESAR CASTRO PALOMINO LARIA, Julio , MARTI CLAUZEL, Luc , ZORZANO OLARTE, Antonio , GARCIA VICENTE, Silvia , MIAN, Alec
IPC分类号： C07C329/06 , A61K31/265 , A61P3/10
CPC分类号： C07C329/06
摘要： The invention is directed to thiocarbonate compounds of Formula (I)-( III) and methods of treating atherosclerosis, neuropathy, nephropathy, retinopathy, inflammatory disorders, COPD, cardiovascular diseases, metabolic disorders, type I diabetes mellitus, type II diabetes mellitus, LAD A, Wolfram Syndrome 1, Wolcott-Rallison syndrome, metabolic syndrome, dyslipidemia, hyperglycemia, or insulin resistance. The compounds of the invention are also useful for protecting pancreatic beta-cells and for reducing free fatty acids, triglycerides, advanced glycated end products, ROS, lipid peroxidation, tissue and plasma TNFalpha and IL6 levels, or for delaying or preventing cardiovascular complications associated with atherosclerosis.
摘要翻译：本发明涉及式（I） - （III）的硫代碳酸酯化合物和治疗动脉粥样硬化，神经病，肾病，视网膜病，炎症性疾病，COPD，心血管疾病，代谢紊乱，I型糖尿病，II型糖尿病，LAD A，Wolfram综合征1，Wolcott-Rallison综合征，代谢综合征，血脂异常，高血糖或胰岛素抵抗。本发明的化合物还可用于保护胰腺β-细胞和用于减少游离脂肪酸，甘油三酯，晚期糖基化终产物，ROS，脂质过氧化，组织和血浆TNFalpha和IL6水平，或用于延迟或预防与动脉粥样硬化。

2. 发明申请

WO2007131996A1 META-XYLYLENEDIAMINE VANADATE SALTS 审中-公开
公开(公告)号：WO2007131996A1
公开(公告)日：2007-11-22
申请号：PCT/EP2007/054668
申请日：2007-05-14
申请人： GENMEDICA THERAPEUTICS SL , UNIVERSIDAD DE BARCELONA , YRAOLA FONT, Francesc , GARCIA VICENTE, Silvia , FERNANDEZ-RECIO, Juan , ALBERICIO, Fernando , ZORZANO OLARTE, Antonio , ROYO EXPOSITO, Miriam , MARTI CLAUZEL, Luc
发明人： YRAOLA FONT, Francesc , GARCIA VICENTE, Silvia , FERNANDEZ-RECIO, Juan , ALBERICIO, Fernando , ZORZANO OLARTE, Antonio , ROYO EXPOSITO, Miriam , MARTI CLAUZEL, Luc
IPC分类号： C07C233/36 , C07C233/78 , C07C235/50 , C07C311/18 , C07C311/16 , A61K31/165 , A61K31/18 , A61P3/10
CPC分类号： C07C311/18 , C07B2200/07 , C07C233/36 , C07C233/78 , C07C235/50 , C07C237/22 , C07C237/34 , C07C271/20
摘要： The invention provides compounds of Formula (I) and Formula (II) or a pharmaceutically-acceptable salt, solvate, or hydrate thereof. Compounds of this invention, or pharmaceutical compositions thereof, are useful for treating diabetes, elevated plasma glucose levels, and/or ketoacidosis in mammals.
摘要翻译：本发明提供式（I）和式（II）的化合物或其药学上可接受的盐，溶剂合物或水合物。本发明的化合物或其药物组合物可用于治疗哺乳动物中的糖尿病，升高的血浆葡萄糖水平和/或酮症酸中毒。

3. 发明申请

WO2010106082A1 ANTI-INFLAMMATORY AND ANTIOXIDANT CONJUGATES USEFUL FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译：抗炎和抗氧化剂联合用于治疗代谢障碍
公开(公告)号：WO2010106082A1
公开(公告)日：2010-09-23
申请号：PCT/EP2010/053418
申请日：2010-03-16
申请人： GENMEDICA THERAPEUTICS SL , MIAN, Alec , MARTI CLAUZEL, Luc , MAYOUX, Eric , GARCIA VICENTE, Silvia , SERRANO MUÑOZ, Marta , ZORZANO OLARTE, Antonio , CESAR CASTRO PALOMINO LARIA, Julio
发明人： MIAN, Alec , MARTI CLAUZEL, Luc , MAYOUX, Eric , GARCIA VICENTE, Silvia , SERRANO MUÑOZ, Marta , ZORZANO OLARTE, Antonio , CESAR CASTRO PALOMINO LARIA, Julio
IPC分类号： A61K31/166 , A61K31/185 , A61K31/192 , A61K31/198 , A61P3/06 , A61P3/10
CPC分类号： C07D339/04 , A61K31/166 , A61K31/185 , A61K31/192 , A61K31/197 , A61K31/198 , A61K31/24 , A61K31/385 , C07C309/15 , C07C317/44 , C07C323/20 , C07C323/59 , C07C323/60 , C07C327/34 , C07C329/06 , C07C2602/08
摘要： The present invention is directed to methods for treating metabolic disorders with compounds that are conjugates. The conjugates of the present invention are comprised of salicylic acid, triflusal, diflusinal, salsalate, IMD-0354, ibuprofen. diclofenac, licofelone, or HTB, and one or more antioxidants.
摘要翻译：本发明涉及用缀合物化合物治疗代谢紊乱的方法。本发明的缀合物由水杨酸，三氟甲磺酸，二氟苯醚，辛酸酯，IMD-0354，布洛芬组成。双氯芬酸，licofoneone或HTB，以及一种或多种抗氧化剂。

4. 发明申请

WO2013037984A1 ANTI-INFLAMMATORY AND ANTIOXIDANT CONJUGATES USEFUL FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译：抗炎和抗氧化剂联合用于治疗代谢障碍
公开(公告)号：WO2013037984A1
公开(公告)日：2013-03-21
申请号：PCT/EP2012/068178
申请日：2012-09-14
申请人： GENMEDICA THERAPEUTICS SL , CESAR CASTRO PALOMINO LARIA, JULIO , MARTI CLAUZEL, Luc , ZORZANO OLARTE, Antonio , GARCIA VICENTE, Silvia , MIAN, Alec
发明人： CESAR CASTRO PALOMINO LARIA, JULIO , MARTI CLAUZEL, Luc , ZORZANO OLARTE, Antonio , GARCIA VICENTE, Silvia , MIAN, Alec
IPC分类号： C07C327/34 , A61K31/265 , A61K47/48 , A61P3/06 , A61P3/10
CPC分类号： C07C327/34 , A61K47/55
摘要： The present invention provides an anti-inflammatory agent/anti-oxidant agent conjugate of formula (I) where is selected from the groups of formula (i), (ii) or (iii), L is CH2CH2 and the other variables are as defined in the claims. Another aspect of the present invention relates to methods for treating metabolic disorders with such conjugates.
摘要翻译：本发明提供式（I）的抗炎剂/抗氧化剂缀合物，其中选自式（i），（ii）或（iii），L是CH 2 CH 2，其它变量如所定义在权利要求中。本发明的另一方面涉及用这种缀合物治疗代谢紊乱的方法。

5. 发明申请

WO2010106083A1 COMBINATION THERAPIES FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译：治疗代谢障碍的组合治疗
公开(公告)号：WO2010106083A1
公开(公告)日：2010-09-23
申请号：PCT/EP2010/053419
申请日：2010-03-16
申请人： GENMEDICA THERAPEUTICS SL , MAYOUX, Eric , MARTI CLAUZEL, Luc , GARCIA VICENTE, Silvia , SERRANO MUÑOZ, Marta , ZORZANO OLARTE, Antonio , MIAN, Alec
发明人： MAYOUX, Eric , MARTI CLAUZEL, Luc , GARCIA VICENTE, Silvia , SERRANO MUÑOZ, Marta , ZORZANO OLARTE, Antonio , MIAN, Alec
IPC分类号： A61K31/00 , A61K31/192 , A61K31/196 , A61K31/198 , A61K31/385 , A61K31/60 , A61P3/06 , A61P3/08
CPC分类号： A61K31/198 , A61K31/00 , A61K31/192 , A61K31/196 , A61K31/385 , A61K31/60 , A61K45/06 , A61K2300/00
摘要： This invention is directed to pharmaceutical combinations comprising an antioxidant agent, an anti-inflammatory agent, and optionally at least one other anti-diabetic agent useful for treating metabolic disorders. This invention also encompasses pharmaceutically acceptable compositions comprising an antioxidant agent, an anti-inflammatory agent, optionally at least one other anti-diabetic agent, and at least one pharmaceutically acceptable earner. The combinations and compositions of this invention are useful as methods for treating metabolic disorders including diabetes, particularly Type I and Type II diabetes, as well as diseases and disorders associated with diabetes, including but not limited to atherosclerosis, cardiovascular disease, inflammatory disorders, nephropathy, neuropathy, retinopathy, β-cell dysfunction, dyslipidemia, LADA, metabolic syndrome, hyperglycemia, insulin resistance, and/or chronic obstructive pulmonary disease in a mammal, particularly a diabetic mammal, and specifically a human patient. This invention is particularly directed to pharmaceutical compositions comprising an lipoic acid, one or more anti-inflammatories selected from the group consisting of diflunisal, diclofenac, dexibuprofen, dexketoprofen, naproxen, and salicylate, and optionally one or more pharmaceutically acceptable carriers. The compositions of this invention are useful as methods for treating metabolic disorders including type II diabetes, insulin resistance, beta-cell dysfunction, and hyperglycemia in a patient, particularly a diabetic patient.
摘要翻译：本发明涉及包含抗氧化剂，抗炎剂和任选的至少一种其它用于治疗代谢紊乱的其它抗糖尿病药物的药物组合。本发明还包括药学上可接受的组合物，其包含抗氧化剂，抗炎剂，任选的至少一种其它抗糖尿病药物和至少一种药学上可接受的吸收剂。本发明的组合和组合物可用作治疗代谢紊乱的方法，包括糖尿病，特别是I型和II型糖尿病，以及与糖尿病相关的疾病和病症，包括但不限于动脉粥样硬化，心血管疾病，炎症性疾病，肾病，神经病，视网膜病变，β细胞功能障碍，血脂异常，LADA，代谢综合征，高血糖症，胰岛素抵抗和/或慢性阻塞性肺疾病，特别是糖尿病哺乳动物，特别是人类患者。本发明特别涉及药物组合物，其包含硫辛酸，一种或多种选自二氟尼柳，双氯芬酸，右布洛芬，右克洛芬，萘普生和水杨酸酯的抗炎剂，以及任选的一种或多种药学上可接受的载体。本发明的组合物可用作治疗患者，特别是糖尿病患者中的II型糖尿病，胰岛素抵抗，β细胞功能障碍和高血糖症的代谢疾病的方法。

6. 发明申请

WO2009138437A1 SALICYLATE CONJUGATES USEFUL FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译：适用于治疗代谢障碍的盐酸盐
公开(公告)号：WO2009138437A1
公开(公告)日：2009-11-19
申请号：PCT/EP2009/055788
申请日：2009-05-13
申请人： GENMEDICA THERAPEUTICS SL , MIAN, Alec , MARTI CLAUZEL, Luc , MAYOUX, Eric , GARCIA VICENTE, Silvia , SERRANO MUNOZ, Marta , ZORZANO OLARTE, Antonio
发明人： MIAN, Alec , MARTI CLAUZEL, Luc , MAYOUX, Eric , GARCIA VICENTE, Silvia , SERRANO MUNOZ, Marta , ZORZANO OLARTE, Antonio
IPC分类号： A61K31/166 , A61K31/185 , A61K31/192 , A61K31/198 , A61P3/06 , A61P3/10
CPC分类号： A61K47/481 , A61K31/166 , A61K31/185 , A61K31/192 , A61K31/198 , A61K47/55
摘要： The present invention is directed to methods for treating metabolic disorders with compounds that are salicylate conjugates.
摘要翻译：本发明涉及用水杨酸缀合物的化合物治疗代谢紊乱的方法。

7. 发明公开

EP2408441A1 COMBINATION THERAPIES FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译：联合治疗代谢疾病的治疗
公开(公告)号：EP2408441A1
公开(公告)日：2012-01-25
申请号：EP10710278.2
申请日：2010-03-16
申请人： Genmedica Therapeutics SL
发明人： MAYOUX, Eric , MARTI CLAUZEL, Luc , GARCIA VICENTE, Silvia , SERRANO MUÑOZ, Marta , ZORZANO OLARTE, Antonio , MIAN, Alec
IPC分类号： A61K31/00 , A61K31/192 , A61K31/196 , A61K31/198 , A61K31/385 , A61K31/60 , A61P3/06 , A61P3/08
CPC分类号： A61K31/198 , A61K31/00 , A61K31/192 , A61K31/196 , A61K31/385 , A61K31/60 , A61K45/06 , A61K2300/00
摘要： This invention is directed to pharmaceutical combinations comprising an antioxidant agent, an anti-inflammatory agent, and optionally at least one other anti-diabetic agent useful for treating metabolic disorders. This invention also encompasses pharmaceutically acceptable compositions comprising an antioxidant agent, an anti-inflammatory agent, optionally at least one other anti-diabetic agent, and at least one pharmaceutically acceptable earner. The combinations and compositions of this invention are useful as methods for treating metabolic disorders including diabetes, particularly Type I and Type II diabetes, as well as diseases and disorders associated with diabetes, including but not limited to atherosclerosis, cardiovascular disease, inflammatory disorders, nephropathy, neuropathy, retinopathy, β-cell dysfunction, dyslipidemia, LADA, metabolic syndrome, hyperglycemia, insulin resistance, and/or chronic obstructive pulmonary disease in a mammal, particularly a diabetic mammal, and specifically a human patient. This invention is particularly directed to pharmaceutical compositions comprising an lipoic acid, one or more anti-inflammatories selected from the group consisting of diflunisal, diclofenac, dexibuprofen, dexketoprofen, naproxen, and salicylate, and optionally one or more pharmaceutically acceptable carriers. The compositions of this invention are useful as methods for treating metabolic disorders including type II diabetes, insulin resistance, beta-cell dysfunction, and hyperglycemia in a patient, particularly a diabetic patient.

8. 发明公开

EP1796681A2 COMPOUNDS FOR INHIBITING COPPER-CONTAINING AMINE OXIDASES AND USES THEREOF 审中-公开
标题翻译： VERBINDUNGEN ZUR HEMMUNG VON KUPFERHALTIGEN AMINOXIDASEN UND IHRE VERWENDUNGEN
公开(公告)号：EP1796681A2
公开(公告)日：2007-06-20
申请号：EP05777845.8
申请日：2005-08-02
申请人： Genmedica Therapeutics SL
发明人： MARTI CLAUZEL, Luc , YRAOLA FONT, Francesc , GARCIA VICENTE, Silvia , ROYO EXPOSITO, Miriam
IPC分类号： A61K31/65 , A61K31/66 , A61K31/67 , A61K31/18 , A61K31/198 , A61K31/401 , A61K31/404 , A61K31/47 , A61K31/4709 , C07C259/00 , A61K31/16 , A61K31/405
CPC分类号： C07D207/16 , C07C233/51 , C07C237/44 , C07C259/06 , C07C259/08 , C07C259/10 , C07C2601/08 , C07C2602/08 , C07D209/18 , C07D209/42 , C07D215/36 , C07D401/06
摘要： This invention is directed to inhibitors of copper-containing amine oxidases (E.C.1.4.3.6) including semicarbazide-sensitive amine oxidase (SSAO; also known as vascular adhesion protein- 1, VAP-I), and their therapeutic use in inflammatory diseases, diabetes and its associated complications, atherosclerosis, neurodegenerative diseases, obesity, hypertension and cancer.
摘要翻译：本发明涉及包含氨基脲敏感性胺氧化酶（SSAO;也称为血管粘附蛋白-1，VAP-1）的含铜胺氧化酶（EC1.4.3.6）的抑制剂及其在炎性疾病，糖尿病中的治疗用途及其相关并发症，动脉粥样硬化，神经变性疾病，肥胖症，高血压和癌症。

9. 发明公开

EP2755645A1 PHARMACEUTICAL COMBINATIONS INCLUDING ANTI-INFLAMMATORY AND ANTIOXIDANT CONJUGATES USEFUL FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译：具有抗炎及抗氧化缀合物的药物化合物的代谢疾病的治疗
公开(公告)号：EP2755645A1
公开(公告)日：2014-07-23
申请号：EP12761959.1
申请日：2012-09-14
申请人： Genmedica Therapeutics SL
发明人： CESAR CASTRO PALOMINO LARIA, Julio , MARTI CLAUZEL, Luc , ZORZANO OLARTE, Antonio , GARCIA VICENTE, Silvia , MIAN, Alec
IPC分类号： A61K31/166 , A61P3/10
CPC分类号： A61K31/265 , A61K31/155 , A61K31/192 , A61K31/216 , A61K31/235 , A61K31/381 , A61K38/2207 , A61K38/23 , A61K38/26 , A61K38/33 , A61K45/06 , A61K47/55 , A61K2300/00
摘要： One aspect of the present invention is a pharmaceutical combination comprising (a) an anti-inflammatory agent/anti-oxidant agent conjugate; and (b) an insulin secretogogue, an insulin sensitizer, an alpha-glucosidase inhibitor, a peptide analog, or a combination thereof. Another aspect of the invention relates to methods of treating metabolic disorders with such conjugates.

10. 发明公开

EP2408443A1 ANTI-INFLAMMATORY AND ANTIOXIDANT CONJUGATES USEFUL FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译： ENTZÜNDUNGSHEMMENDE抗氧化剂KUJUGATE ZUR BEHANDLUNG VON STOFFWECHSELERKRANKUNGEN
公开(公告)号：EP2408443A1
公开(公告)日：2012-01-25
申请号：EP10708228.1
申请日：2010-03-16
申请人： Genmedica Therapeutics SL
发明人： MIAN, Alec , MARTI CLAUZEL, Luc , MAYOUX, Eric , GARCIA VICENTE, Silvia , SERRANO MUÑOZ, Marta , ZORZANO OLARTE, Antonio , CESAR CASTRO PALOMINO LARIA, Julio
IPC分类号： A61K31/166 , A61K31/185 , A61K31/192 , A61K31/198 , A61P3/06 , A61P3/10
CPC分类号： C07D339/04 , A61K31/166 , A61K31/185 , A61K31/192 , A61K31/197 , A61K31/198 , A61K31/24 , A61K31/385 , C07C309/15 , C07C317/44 , C07C323/20 , C07C323/59 , C07C323/60 , C07C327/34 , C07C329/06 , C07C2602/08
摘要： The present invention is directed to methods for treating metabolic disorders with compounds that are conjugates. The conjugates of the present invention are comprised of salicylic acid, triflusal, diflusinal, salsalate, IMD-0354, ibuprofen. diclofenac, licofelone, or HTB, and one or more antioxidants.
摘要翻译：本发明涉及用缀合物化合物治疗代谢紊乱的方法。本发明的缀合物由水杨酸，三氟乙酸，二氟苯醚，辛酸盐，IMD-0354，布洛芬，双氯芬酸，licofelone或HTB以及一种或多种抗氧化剂组成。

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