公开(公告)号：US08067441B2

公开(公告)日：2011-11-29

申请号：US11996966

申请日：2006-07-28

申请人： Ana Martinez Gil ,  Paola Usan Egea ,  Miguel Medina Padilla ,  Esther Garcia Palomero ,  Julia Perez Baz ,  Rosa Isabel Fernandez Chimeno ,  Antonio Medarde Fernandez ,  Librada Maria Canedo Hernandez ,  Francisco Romero Millan ,  Ana Castro Morera ,  Mercedes Alonso Cascon ,  Jorge Sanchez Quesada

发明人： Ana Martinez Gil ,  Paola Usan Egea ,  Miguel Medina Padilla ,  Esther Garcia Palomero ,  Julia Perez Baz ,  Rosa Isabel Fernandez Chimeno ,  Antonio Medarde Fernandez ,  Librada Maria Canedo Hernandez ,  Francisco Romero Millan ,  Ana Castro Morera ,  Mercedes Alonso Cascon ,  Jorge Sanchez Quesada

IPC分类号： A01N43/40 ,  A61K31/44

CPC分类号： A61K31/44

摘要： The present invention relates to the use of Collismycin and derivatives thereof as inhibitors of oxidative stress in cells and their use for the preparation of medicaments for the treatment of oxidative stress-induced diseases or conditions, especially neurodegenerative diseases, such as Alzheimer's Disease and Parkinson's Disease.

摘要翻译： 本发明涉及Collismycin及其衍生物作为细胞氧化应激抑制剂的用途及其用于制备用于治疗氧化应激诱发的疾病或病症，特别是神经变性疾病如阿尔茨海默病和帕金森病的药物的用途 。

公开(公告)号：US20080275088A1

公开(公告)日：2008-11-06

申请号：US11996966

申请日：2006-07-28

申请人： Ana Martinez Gil ,  Paola Usan Egea ,  Miguel Medina Padilla ,  Esther Garcia Palomero ,  Julia Perez Baz ,  Rosa Isabel Fernandez Chimeno ,  Antonio Medarde Fernandez ,  Librada Maria Canedo Hernandez ,  Francisco Romero Millan ,  Ana Castro Morera ,  Mercedes Alonso Cascon ,  Jorge Sanchez Quesada

发明人： Ana Martinez Gil ,  Paola Usan Egea ,  Miguel Medina Padilla ,  Esther Garcia Palomero ,  Julia Perez Baz ,  Rosa Isabel Fernandez Chimeno ,  Antonio Medarde Fernandez ,  Librada Maria Canedo Hernandez ,  Francisco Romero Millan ,  Ana Castro Morera ,  Mercedes Alonso Cascon ,  Jorge Sanchez Quesada

IPC分类号： A61K31/444 ,  C07D401/04 ,  A61P25/00 ,  A61P25/28 ,  A61P25/16 ,  A61P3/10 ,  A61P29/00

CPC分类号： A61K31/44

摘要： The present invention relates to the use of Collismycin and derivatives thereof as inhibitors of oxidative stress in cells and their use for the preparation of medicaments for the treatment and/or prevention of oxidative stress-induced diseases or conditions, especially neurodegenerative diseases, such as Alzheimer's Disease and Parkinson's Disease.

摘要翻译： 本发明涉及使用Collismycin及其衍生物作为细胞氧化应激的抑制剂及其用于制备用于治疗和/或预防氧化应激诱发的疾病或病症，特别是神经变性疾病如阿尔茨海默病的药物的用途 疾病和帕金森病。

公开(公告)号：US08592446B2

公开(公告)日：2013-11-26

申请号：US12664130

申请日：2008-06-11

申请人： Ana Martinez Gil ,  Ana Castro Morera ,  Miguel Medina Padilla ,  Jorge Sanchez-Quesada ,  Mercedes Alonso Cascon ,  Laura Rubio Arrieta ,  Esther Garcia Palomero ,  Paola Usan Egea

发明人： Ana Martinez Gil ,  Ana Castro Morera ,  Miguel Medina Padilla ,  Jorge Sanchez-Quesada ,  Mercedes Alonso Cascon ,  Laura Rubio Arrieta ,  Esther Garcia Palomero ,  Paola Usan Egea

IPC分类号： C07D221/16 ,  C07D487/04 ,  A61K31/4375

CPC分类号： C07D471/04

摘要： The present invention relates to a new family of [1,10]-phenantroline derivatives of formula (I), which are useful for the treatment or profilaxis of a neurodegenerative or haematological disease or condition, their use as a medicament, especially for treating a treatment neurodegenerative or haematological disease or condition, and a pharmaceutical composition comprising the compounds.

摘要翻译： 本发明涉及式（I）的[1,10] - phen啉衍生物的新家族，它们可用于治疗或表现神经变性或血液病学疾病或病症，其用作药物，特别是用于治疗 治疗神经变性或血液病或病症，以及包含该化合物的药物组合物。

公开(公告)号：US20100240692A1

公开(公告)日：2010-09-23

申请号：US12664130

申请日：2008-06-11

申请人： Ana Martinez Gil ,  Ana Castro Morera ,  Miguel Medina Padilla ,  Jorge Sanchez-Quesada ,  Mercedes Alonso Cascon ,  Laura Rubio Arrieta ,  Esther Garcia Palomero ,  Paola Usan Egea

发明人： Ana Martinez Gil ,  Ana Castro Morera ,  Miguel Medina Padilla ,  Jorge Sanchez-Quesada ,  Mercedes Alonso Cascon ,  Laura Rubio Arrieta ,  Esther Garcia Palomero ,  Paola Usan Egea

IPC分类号： A61K31/4745 ,  C07D471/04 ,  A61P25/00

CPC分类号： C07D471/04

摘要： The present invention relates to a new family of [1,10]-phenantroline derivatives of formula (I), which are useful for the treatment or profilaxis of a neurodegenerative or haematological disease or condition, their use as a medicament, especially for treating a treatment neurodegenerative or haematological disease or condition, and a pharmaceutical composition comprising the compounds.

摘要翻译： 本发明涉及式（I）的[1,10] - phen啉衍生物的新家族，它们可用于治疗或表现神经变性或血液病学疾病或病症，其用作药物，特别是用于治疗 治疗神经变性或血液病或病症，以及包含该化合物的药物组合物。

公开(公告)号：US20100267827A1

公开(公告)日：2010-10-21

申请号：US12375607

申请日：2007-08-01

申请人： Ana Martinez Gil ,  Ana Castro Morera ,  Miguel Medina Padilla ,  Pilar Munoz Ruiz ,  Javier Lopez Ogalla ,  Laura Rubio Arrieta ,  Esther Garcia Palomero ,  Pablo Garcia Fernandez ,  Celia De Austria De Luque ,  Elena Delgado Hernandez ,  Paola Usan Egea ,  Rita Valenzuela Liminana ,  Jorge Sanchez-Quesada

发明人： Ana Martinez Gil ,  Ana Castro Morera ,  Miguel Medina Padilla ,  Pilar Munoz Ruiz ,  Javier Lopez Ogalla ,  Laura Rubio Arrieta ,  Esther Garcia Palomero ,  Pablo Garcia Fernandez ,  Celia De Austria De Luque ,  Elena Delgado Hernandez ,  Paola Usan Egea ,  Rita Valenzuela Liminana ,  Jorge Sanchez-Quesada

IPC分类号： A61K31/245 ,  C07C69/92 ,  A61K31/235 ,  A61P25/28 ,  A61P25/16 ,  A61P25/24 ,  A61P25/08 ,  A61P25/18 ,  A61P9/10 ,  C07C43/215 ,  A61K31/085 ,  C07C65/21 ,  A61K31/192 ,  C07C229/64 ,  C07C235/46 ,  A61K31/166 ,  A61K31/196

CPC分类号： C07C235/46 ,  C07C43/215 ,  C07C65/28 ,  C07C69/92 ,  C07C229/60 ,  C07C233/54

摘要： The present invention is related to a family of phenyl-prenyl-ether derivatives of formula (I), and to their use in the treatment of cognitive, neurodegenerative or neuronal diseases or disorders, such as Alzheimer's disease or 5 Parkinson's Disease. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder.

摘要翻译： 本发明涉及式（I）的苯基 - 异戊烯基醚衍生物及其在治疗认知，神经变性或神经元疾病或病症如阿尔茨海默病或5帕金森病中的用途。 本发明还涉及包含其的药物组合物。 此外，本发明涉及该化合物在制备用于治疗和/或预防认知，神经变性或神经元疾病或病症的药物中的用途。

公开(公告)号：US20100041665A1

公开(公告)日：2010-02-18

申请号：US12375614

申请日：2007-08-01

申请人： Ana Martinez Gil ,  Ana Castro Morera ,  Miguel Medina Padilla ,  Pilar Munoz Ruiz ,  Javier Lopez Ogalla ,  Esther Garcia Palomero ,  Celia De Austria De Luque ,  Paola Usan Egea ,  Rita Valenzuela Liminana ,  Pablo Garcia Fernandez ,  Elena Delgado Hernandez ,  Daniel Ignacio Perez Fernandez

发明人： Ana Martinez Gil ,  Ana Castro Morera ,  Miguel Medina Padilla ,  Pilar Munoz Ruiz ,  Javier Lopez Ogalla ,  Esther Garcia Palomero ,  Celia De Austria De Luque ,  Paola Usan Egea ,  Rita Valenzuela Liminana ,  Pablo Garcia Fernandez ,  Elena Delgado Hernandez ,  Daniel Ignacio Perez Fernandez

IPC分类号： A61K31/4965 ,  C07C229/34 ,  C07C63/64 ,  C07D315/00 ,  C07D241/04 ,  C07D231/02 ,  A61K31/24 ,  A61K31/19 ,  A61K31/351 ,  A61K31/415 ,  A61P25/28 ,  A61P21/00 ,  A61P25/18 ,  A61P9/10

CPC分类号： C07C229/64 ,  C07C211/48 ,  C07C217/84 ,  C07C229/60 ,  C07C231/12 ,  C07C237/44 ,  C07C271/28 ,  C07C279/22 ,  C07D231/14 ,  C07D233/64 ,  C07D295/192 ,  C07D309/12

摘要： The present invention is related to a family of N-phenyl-prenylamine derivatives of formula (I), and to their use in the treatment of cognitive, neurodegenerative or neuronal diseases or disorders, such as Alzheimer's disease or Parkinson's Disease. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder.

摘要翻译： 本发明涉及式（I）的N-苯基 - 异戊胺衍生物家族及其在治疗认知，神经变性或神经元疾病或病症如阿尔茨海默氏病或​​帕金森病中的用途。 本发明还涉及包含其的药物组合物。 此外，本发明涉及该化合物在制备用于治疗和/或预防认知，神经变性或神经元疾病或病症的药物中的用途。

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。

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。

公开(公告)号：US20080039513A1

公开(公告)日：2008-02-14

申请号：US11570753

申请日：2005-06-17

申请人： Ana Martinez Gil ,  Diana Alonso Gordillo ,  Isabel Dorronsoro Diaz ,  Esther Garcia Palomero ,  Celia De Austria De Luque ,  Paola Usan Egea ,  Maria Del Monte Millan ,  Miguel Medina Padilla

发明人： Ana Martinez Gil ,  Diana Alonso Gordillo ,  Isabel Dorronsoro Diaz ,  Esther Garcia Palomero ,  Celia De Austria De Luque ,  Paola Usan Egea ,  Maria Del Monte Millan ,  Miguel Medina Padilla

IPC分类号： A61K31/42 ,  A61K31/422 ,  C07D413/02

CPC分类号： C07D261/20

摘要： The invention provides compounds having a spiro heterocyclic unit connected through a linker of a certain length to another spiro cycle, an imidazole ring or an amide group. Some of these compounds have been obtained from Aplysinia cavernicola and a mixture of Aplysina fulva and Oceanapia. The compounds exhibit VDCC blocker activity; some also show acetylcholinesterase and butyrylcholinesterase inhibition activities. Therefore they are useful in the treatment of cognitive and neurodegenerative disorders, such as brain ischemia, stroke, cognitive disorders as senile dementia, cerebrovascular dementia, mild recognition impairment, attention deficit disorder, and/or neurodegenerative dementing disease with aberrant protein aggregations as specially Alzheimers's disease or condition, or prion disease as Creutzfeld-Jakob disease or Gerstmann-Straussler-Scheinker disease.

摘要翻译： 本发明提供具有通过一定长度的连接体与另一个螺环连接的螺杂环单元的化合物，咪唑环或酰胺基。 这些化合物中的一些已经从盐酸阿利亚西亚（Aplysinia cavernicola）和阿维菌素（Aplysina fulva）和洋洋洋（Oceanapia）的混合物中获得。 化合物表现出VDCC阻断活性; 一些还显示乙酰胆碱酯酶和丁酰胆碱酯酶抑制活性。 因此，它们可用于治疗认知和神经变性疾病，例如脑缺血，中风，认知障碍，老年痴呆，脑血管性痴呆，轻度识别损伤，注意缺陷障碍和/或具有异常蛋白质聚集的神经退行性痴呆疾病，特别是阿尔茨海默病 疾病或病症，或作为克雅氏病或杰斯特曼 - 施特劳斯 - 斯温克病的朊病毒疾病。