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公开(公告)号：US20090221647A1
公开(公告)日：2009-09-03
申请号：US12298861
申请日：2007-04-27
申请人： Ana Martinez Gil , Ana Castro Morera , Miguel Medina Padilla , Ester Martin Aparicio , Mercedes Alonso Cascon , Ana Fuertes Huerta , Maria Luisa Navarro Rico , Maria Jose Perez Puerto , Maria Del Monte Millan
发明人： Ana Martinez Gil , Ana Castro Morera , Miguel Medina Padilla , Ester Martin Aparicio , Mercedes Alonso Cascon , Ana Fuertes Huerta , Maria Luisa Navarro Rico , Maria Jose Perez Puerto , Maria Del Monte Millan
IPC分类号： A61K31/4439 , C07D417/12 , A61P25/28 , A61P25/16 , C12Q1/48
CPC分类号： C07D417/12 , A61K31/41
摘要： The present invention relates to the use of N-(2-thiazolyl)-amide derivatives of formula (I), for the treatment and/or prophylaxis of a disease in which glycogen synthase kinase 3 (GSK-3) is involved, especially neurodegenerative diseases, such as Alzheimer's disease, or non-insulin dependent diabetes mellitus.
摘要翻译： 本发明涉及式（I）的N-（2-噻唑基） - 酰胺衍生物用于治疗和/或预防涉及糖原合酶激酶3（GSK-3）的疾病，特别是神经变性 疾病如阿尔茨海默病或非胰岛素依赖性糖尿病。
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公开(公告)号：US20090124686A1
公开(公告)日：2009-05-14
申请号：US11996962
申请日：2006-07-28
申请人： Ana Martinez Gil , Miguel Medina Padilla , Mercedes Alonso Cascon , Ana Fuertes Huerta , Maria Luisa Navarro Rico , Maria Jose Perez Puerto , Ana Castro Morera , Ester Martin Aparicio
发明人： Ana Martinez Gil , Miguel Medina Padilla , Mercedes Alonso Cascon , Ana Fuertes Huerta , Maria Luisa Navarro Rico , Maria Jose Perez Puerto , Ana Castro Morera , Ester Martin Aparicio
IPC分类号： A61K31/343 , A61K31/17 , C07D317/46 , A61P3/10 , A61P35/00 , A61P29/00 , A61P25/00 , C12Q1/48 , C07C275/28
CPC分类号： C07D317/66 , A61K31/17 , A61K31/36
摘要： The invention relates to urea derivatives of formula (I) as inhibitors of glycogen synthase kinase 3β, GSK-3, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which GSK-3 is involved, such as Alzheimer's disease or non-insulin dependent diabetes mellitus.
摘要翻译： 本发明涉及式（I）的脲衍生物作为糖原合酶激酶3β，GSK-3的抑制剂，其制备方法，包含它们的药物组合物及其用于治疗和/或预防疾病的用途 其中涉及GSK-3，例如阿尔茨海默病或非胰岛素依赖性糖尿病。
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公开(公告)号：US20090192204A1
公开(公告)日：2009-07-30
申请号：US12298866
申请日：2007-04-27
申请人： Ana Martinez Gil , Ana Castro Morera , Miguel Medina Padilla , Ester Martin Aparicio , Mercedes Alonso Cascon , Ana Fuertes Huerta , Maria Luisa Navarro Rico , Maria Jose Perez Puerto , Maria Del Monte Millan
发明人： Ana Martinez Gil , Ana Castro Morera , Miguel Medina Padilla , Ester Martin Aparicio , Mercedes Alonso Cascon , Ana Fuertes Huerta , Maria Luisa Navarro Rico , Maria Jose Perez Puerto , Maria Del Monte Millan
IPC分类号： A61K31/427 , A61P3/00 , A61P25/00 , C07D417/12
CPC分类号： C07D417/12 , A61K31/41
摘要： The present invention relates to the use of N-(2-thiazolyl)-amide derivatives of formula (I) for the treatment and/or prophylaxis of a disease in which glycogen synthase kinase 3 (GSK-3) is involved, especially neurodegenerative diseases, such as Alzheimer's disease, or non-insulin dependent diabetes mellitus.
摘要翻译： 本发明涉及式（I）的N-（2-噻唑基） - 酰胺衍生物用于治疗和/或预防涉及糖原合酶激酶3（GSK-3）的疾病，特别是神经变性疾病 ，如阿尔茨海默病，或非胰岛素依赖性糖尿病。
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公开(公告)号：US08686042B2
公开(公告)日：2014-04-01
申请号：US11996962
申请日：2006-07-28
申请人： Ana Martinez Gil , Miguel Medina Padilla , Mercedes Alonso Cascon , Ana Fuertes Huerta , Maria Luisa Navarro Rico , Maria Jose Perez Puerto , Ana Castro Morera , Ester Martin Aparicio
发明人： Ana Martinez Gil , Miguel Medina Padilla , Mercedes Alonso Cascon , Ana Fuertes Huerta , Maria Luisa Navarro Rico , Maria Jose Perez Puerto , Ana Castro Morera , Ester Martin Aparicio
CPC分类号： C07D317/66 , A61K31/17 , A61K31/36
摘要： The invention relates to urea derivatives of formula (I) as inhibitors of glycogen synthase kinase 3β, GSK-3, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which GSK-3 is involved, such as Alzheimer's disease or non-insulin dependent diabetes mellitus.
摘要翻译： 本发明涉及式（I）的脲衍生物作为糖原合成酶激酶3＆bgr，GSK-3的抑制剂，其制备方法，包含它们的药物组合物及其用于治疗和/或预防 涉及GSK-3的疾病，如阿尔茨海默病或非胰岛素依赖性糖尿病。
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公开(公告)号：US20090233971A1
公开(公告)日：2009-09-17
申请号：US12428442
申请日：2009-04-22
申请人： Miguel Medina Padilla , Mercedes Alonso Cascon , Isabel Dorronsoro Diaz , Ana Martinez Gil , Gema Panizo del Pliego , Ana Fuertes Huerta , Maria Jose Perez Puerto
发明人： Miguel Medina Padilla , Mercedes Alonso Cascon , Isabel Dorronsoro Diaz , Ana Martinez Gil , Gema Panizo del Pliego , Ana Fuertes Huerta , Maria Jose Perez Puerto
IPC分类号： A61K31/433 , A61P25/28 , A61P25/16 , A61P25/08 , A61P25/18 , A61P9/10 , A61P3/04 , A61P9/12 , A61P35/00 , A61P25/24 , G01N33/566
CPC分类号： C07D285/08 , C07D417/04
摘要： Provided are thiadiazolidine compounds of formula I wherein R1 is an organic group having at least 8 atoms selected from C or O, which is not linked directly to the N through a —C(O)— and comprising at least an aromatic ring, and their pharmaceutical compositions. These compounds are selective GSK-3 inhibitors and have improved bioavailability. They are useful for the treatment of GSK-3 mediated diseases, among others Alzheimer's disease, type II diabetes, depression and brain injury.
摘要翻译： 提供式I的噻二唑烷化合物，其中R 1是具有至少8个选自C或O的原子的有机基团，其不直接与N直接通过-C（O） - 并且至少包含芳环，并且它们 药物组合物。 这些化合物是选择性GSK-3抑制剂并具有改善的生物利用度。 它们可用于治疗GSK-3介导的疾病，其中包括阿尔茨海默病，II型糖尿病，抑郁症和脑损伤。
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公开(公告)号：US08158661B2
公开(公告)日：2012-04-17
申请号：US12428442
申请日：2009-04-22
申请人： Miguel Medina Padilla , Mercedes Alonso Cascon , Isabel Dorronsoro Diaz , Ana Martinez Gil , Gema Panizo Del Pliego , Ana Fuertes Huerta , Maria Jose Perez Puerto
发明人： Miguel Medina Padilla , Mercedes Alonso Cascon , Isabel Dorronsoro Diaz , Ana Martinez Gil , Gema Panizo Del Pliego , Ana Fuertes Huerta , Maria Jose Perez Puerto
IPC分类号： A61K31/41 , C07D285/08
CPC分类号： C07D285/08 , C07D417/04
摘要： Provided are thiadiazolidine compounds of formula I wherein R1 is an organic group having at least 8 atoms selected from C or O, which is not linked directly to the N through a —C(O)— and comprising at least an aromatic ring, and their pharmaceutical compositions. These compounds are selective GSK-3 inhibitors and have improved bioavailability. They are useful for the treatment of GSK-3 mediated diseases, among others Alzheimer's disease, type II diabetes, depression and brain injury.
摘要翻译： 提供式I的噻二唑烷化合物，其中R 1是具有至少8个选自C或O的原子的有机基团，其不直接与N直接通过-C（O） - 并且至少包含芳环，并且它们 药物组合物。 这些化合物是选择性GSK-3抑制剂并具有改善的生物利用度。 它们可用于治疗GSK-3介导的疾病，其中包括阿尔茨海默病，II型糖尿病，抑郁症和脑损伤。
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公开(公告)号：US20110144148A1
公开(公告)日：2011-06-16
申请号：US13030239
申请日：2011-02-18
申请人： Ana Martinez Gil , Isabel Dorronsoro Diaz , Laura Rubio Arrieta , Diana Alonso Gordillo , Ana Fuertes Huerta , Susana Morales-Alcelay , Maria Del Monte Millan , Esther Garcia Palomero , Paola Usan Egea , Celia De Austria , Miguel Medina Padilla , Pilar Munoz Ruiz
发明人： Ana Martinez Gil , Isabel Dorronsoro Diaz , Laura Rubio Arrieta , Diana Alonso Gordillo , Ana Fuertes Huerta , Susana Morales-Alcelay , Maria Del Monte Millan , Esther Garcia Palomero , Paola Usan Egea , Celia De Austria , Miguel Medina Padilla , Pilar Munoz Ruiz
IPC分类号： A61K31/473 , A61P25/28 , A61P9/00 , A61P25/16 , G01N33/53
CPC分类号： C07D401/12
摘要： The invention provides compounds of formula: which have a tacrine moiety connected to an heterocyclic moiety through a linker. Through careful selection of the substituents and the linker, the activity and selectivity towards acetylcholinesterase can be modulated. The compounds show potent AChE inhibition activities together with modifications in the β-amyloid aggregation properties by binding simultaneously to the catalytic and peripheral AChE sites. They are useful in the treatment of AChE mediated diseases, such as the Alzheimer's disease.
摘要翻译： 本发明提供下式的化合物：其具有通过接头与杂环部分连接的他克林部分。 通过仔细选择取代基和接头，可以调节对乙酰胆碱酯酶的活性和选择性。 化合物通过同时结合催化和外周AChE位点显示出有力的AChE抑制活性以及对淀粉样蛋白聚集性质的修饰。 它们可用于治疗AChE介导的疾病，例如阿尔茨海默氏病。
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公开(公告)号：US07910739B2
公开(公告)日：2011-03-22
申请号：US10887974
申请日：2004-07-09
申请人： Ana Martinez Gil , Isabel Dorronsoro Diaz , Laura Rubio Arrieta , Diana Alonso Gordillo , Ana Fuertes Huerta , Susana Morales-Alcelay , Maria Del Monte Millan , Esther Garcia Palomero , Paola Usan Egea , Celia De Austria , Miguel Medina Padilla , Pilar Munoz Ruiz
发明人： Ana Martinez Gil , Isabel Dorronsoro Diaz , Laura Rubio Arrieta , Diana Alonso Gordillo , Ana Fuertes Huerta , Susana Morales-Alcelay , Maria Del Monte Millan , Esther Garcia Palomero , Paola Usan Egea , Celia De Austria , Miguel Medina Padilla , Pilar Munoz Ruiz
IPC分类号： C07D219/12 , A61K31/435
CPC分类号： C07D401/12
摘要： The invention provides compounds of formula: which have a tacrine moiety connected to an heterocyclic moiety through a linker. Through careful selection of the substituents and the linker, the activity and selectivity towards acetylcholinesterase can be modulated. The compounds show potent AChE inhibition activities together with modifications in the β-amyloid aggregation properties by binding simultaneously to the catalytic and peripheral AChE sites. They are useful in the treatment of AChE mediated diseases, such as the Alzheimer's disease.
摘要翻译： 本发明提供下式的化合物：其具有通过接头与杂环部分连接的他克林部分。 通过仔细选择取代基和接头，可以调节对乙酰胆碱酯酶的活性和选择性。 化合物通过同时结合催化和外周AChE位点显示出有力的AChE抑制活性以及对淀粉样蛋白聚集性质的修饰。 它们可用于治疗AChE介导的疾病，例如阿尔茨海默氏病。
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公开(公告)号：US07531561B2
公开(公告)日：2009-05-12
申请号：US11098610
申请日：2005-04-05
申请人： Miguel Medina Padilla , Mercedes Alonso Cascón , Isabel Dorronsoro Díaz , Ana Martínez Gil , Gema Panizo del Pliego , Ana Fuertes Huerta , María José Pérez Puerto
发明人： Miguel Medina Padilla , Mercedes Alonso Cascón , Isabel Dorronsoro Díaz , Ana Martínez Gil , Gema Panizo del Pliego , Ana Fuertes Huerta , María José Pérez Puerto
IPC分类号： A61K31/41 , C07D285/08
CPC分类号： C07D285/08 , C07D417/04
摘要： Provided are thiadiazolidine compounds of formula I wherein R1 is an organic group having at least 8 atoms selected from C or O, which is not linked directly to the N through a —C(O)— and comprising at least an aromatic ring, and their pharmaceutical compositions. These compounds are selective GSK-3 inhibitors and have improved bioavailability. They are useful for the treatment of GSK-3 mediated diseases, among others Alzheimer's disease, type II diabetes, depression and brain injury.
摘要翻译： 提供式I的噻二唑烷化合物，其中R 1是具有至少8个选自C或O的原子的有机基团，其不直接与N直接通过-C（O） - 并且至少包含芳环，并且它们 药物组合物。 这些化合物是选择性GSK-3抑制剂并具有改善的生物利用度。 它们可用于治疗GSK-3介导的疾病，其中包括阿尔茨海默病，II型糖尿病，抑郁症和脑损伤。
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10.发明申请BIPYRIDINE SULFONAMIDE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES OR CONDITIONS 有权用于治疗神经损伤性疾病或病症的二吡啶磺酰胺衍生物公开(公告)号：US20140005195A1
公开(公告)日：2014-01-02
申请号：US13988722
申请日：2011-11-21
申请人： Francisco Palomo Nicolau , Jorge Sánchez-Quesada , Javier López Ogalla , Félix Hernández Juan , Javier Villasante Prieto , Miguel Medina Padilla , Ana Fuertes Huerta , Juan Manuel Dominguez Correa , Susan Herrero Santos , Mercedes Alonso Cascón
发明人： Francisco Palomo Nicolau , Jorge Sánchez-Quesada , Javier López Ogalla , Félix Hernández Juan , Javier Villasante Prieto , Miguel Medina Padilla , Ana Fuertes Huerta , Juan Manuel Dominguez Correa , Susan Herrero Santos , Mercedes Alonso Cascón
IPC分类号： C07D417/14 , C07D405/14 , C07D401/14 , C07D401/04 , C07D409/14
CPC分类号： C07D401/04 , C07D213/68 , C07D213/71 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D513/04
摘要： The present invention relates to novel bipyridine sulfonamide derivatives of formula (I) and their use for the treatment and/or prophylaxis of a neurodegenerative disease or condition, particularly Alzheimers disease (AD), a cardiovascular disease or a pathology involving ischemia. Additionally, processes for preparing such derivatives5 and pharmaceutical compositions comprising them are provided.
摘要翻译： 本发明涉及式（I）的新型联吡啶磺酰胺衍生物及其用于治疗和/或预防神经变性疾病或病症，特别是阿尔茨海默病（AD），心血管疾病或涉及缺血的病理学的用途。 此外，提供了制备这些衍生物的方法5和包含它们的药物组合物。
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