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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：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：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：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：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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