公开(公告)号：EP1749552A1

公开(公告)日：2007-02-07

申请号：EP05380175.9

申请日：2005-07-29

申请人： Neuropharma S.A. ,  Instituto Biomar S.A.

发明人： Martinez Gil, Ana ,  Usán Egea, Paola ,  Medina Padilla, Miguel ,  Garcia Palomero, Esther ,  Pérez Baz, Julia ,  Fernández Chimeno, Rosa Isabel ,  Fernández Medarde, Antonio

IPC分类号： A61P39/06 ,  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, specially neurodegenerative diseases, such as Alzheimer's Disease and Parkinson's Disease.

摘要翻译： 本发明涉及Collicycin及其衍生物作为细胞氧化应激抑制剂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：EP2444121A1

公开(公告)日：2012-04-25

申请号：EP12151913.6

申请日：2006-07-28

申请人： Noscira, S.A. ,  Instituto Biomar S.A.

发明人： Martínez Gil, Ana ,  Castro Morera, Ana ,  Alonso Cascón, Mercedes ,  Sánchez Quesada, Jorge ,  Usán Egea, Paola ,  Medina Padilla, Miguel ,  García Palomero, Esther ,  Pérez Baz, Julia ,  Fernández Chimeno, Rosa Isabel ,  Fernández Medarde, Antonio ,  Cañedo Hernández, Librada María ,  Romero Millán, Francisco

IPC分类号： A61P39/06 ,  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 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Collismycin及其衍生物作为细胞氧化应激抑制剂及其在制备用于治疗和/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中的应用。 疾病和帕金森病。

公开(公告)号：EP1939192A1

公开(公告)日：2008-07-02

申请号：EP06127280.3

申请日：2006-12-28

申请人： Neuropharma S.A.

发明人： Martinez Gil, Ana ,  Medina Padilla, Miguel ,  Castro Morera, Ana ,  Fall Diop, Yagamare ,  Gomez Pacios, Generosa ,  Pérez Vasquez, Manuel ,  Alonso Cascon, Mercedes ,  Pérez Fernandez, Daniel Igancio ,  Herrero Santos, Susana ,  Martin Aparicio, Ester ,  Fuertes Huerta, Ana ,  Del Monte Millan, Maria ,  Navarro Rico, Maria Luisa ,  Pérez Puerto, Maria José

IPC分类号： C07D307/58 ,  C07D307/60 ,  C07D307/62 ,  C07D307/66 ,  C07D333/32 ,  C07D405/04 ,  C07D407/04 ,  C07D407/06 ,  C07F7/18 ,  A61K31/341 ,  A61P25/28 ,  A61P3/10 ,  A61P25/24

CPC分类号： C07D307/58 ,  C07D307/60 ,  C07D307/62 ,  C07D307/66 ,  C07D333/32 ,  C07D405/04 ,  C07D407/04 ,  C07D407/06 ,  C07F7/1856

摘要： The present invention relates to cyclopentanone derivatives of formula (I), their method of synthesis and uses thereof. Concretely, the compounds disclosed have proved to be inhibitors of glycogen synthase kinase 3β, GSK-3 β, which is known to be involved in different disease and conditions, such as Alzheimer's disease or non-insulin dependent diabetes mellitus. 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 GSK-3 mediated disease or condition.

摘要翻译： 本发明涉及式（I）的环戊酮衍生物，其合成方法及用途。 具体地说，所公开的化合物已被证明是糖原合成酶激酶3 2，GSK-3 2的抑制剂，其已知涉及不同的疾病和病症如阿尔茨海默病或非胰岛素依赖性糖尿病。 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GSK-3介导的疾病或病症的药物中的用途。

公开(公告)号：EP1849785A1

公开(公告)日：2007-10-31

申请号：EP06380099.9

申请日：2006-04-28

申请人： Neuropharma, S.A.

发明人： Martinez Gil, Ana ,  Castro Morera, Ana ,  Medina Padilla, Miguel ,  Martin Aparicio, Ester ,  Alonso Cascon, Mercedes ,  Fuertes Huerta, Ana ,  Navarro Rico, Maria Luisa ,  Perez Puerto, Maria Jose ,  Del Monte Millan, Maria

IPC分类号： C07D417/12 ,  A61K31/426 ,  A61K31/427 ,  A61P25/28

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)

wherein
X is selected from the group consisting of:
- an indol of formula (A) or (B), bonded respectively at positions 2 or 3:

- an indazol of formula (C), bonded at position 3:

- a pyridin, bonded at any positions 2 to 6; and
- a phenyl
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） - 酰胺衍生物的用途，其中X选自：式（A）或（B）的吲哚，分别键合在 2或3： - 在3位键合的式（C）吲唑： - 在任何2至6位键合的吡啶; 和 - 用于治疗和/或预防其中涉及糖原合酶激酶3（GSK-3）的疾病的苯基，特别是诸如阿尔茨海默病或非胰岛素依赖性糖尿病的神经变性疾病。

公开(公告)号：EP1798220A1

公开(公告)日：2007-06-20

申请号：EP05077910.7

申请日：2005-12-16

申请人： Neuropharma S.A.

发明人： Martínez Gil, Ana ,  Castro Morera, Ana ,  Medina Padilla, Miguel ,  Muñoz Ruiz, Pilar ,  Rubio Arrieta, Laura ,  García Palomero, Esther ,  De Austria, Celia

IPC分类号： C07C255/60 ,  A61K31/166 ,  A61P25/28

CPC分类号： C07C235/60

摘要： The invention is directed to a compound of formula (I)

Having VDCC blocking activity. These compounds are useful for the treatment of a series of human diseases and conditions, especially cognitive or neurodegenerative diseases or conditions.

摘要翻译： 本发明涉及具有VDCC封闭活性的式（I）化合物。 这些化合物可用于治疗一系列人类疾病和病症，特别是认知或神经变性疾病或病症。

公开(公告)号：EP1749523A1

公开(公告)日：2007-02-07

申请号：EP05380176.7

申请日：2005-07-29

申请人： Neuropharma, S.A.

发明人： Martinez Gil, Ana ,  Medina Padilla, Miguel ,  Castro Morera, Ana ,  Alonso Cascón, Mercedes ,  Martin Aparicio, Ester ,  Fuertes Huerta, Ana ,  Navarro Rico, Maria Luisa ,  Pérez Puerto, Maria Jose

IPC分类号： A61K31/17 ,  A61K31/36 ,  A61P25/28 ,  A61P3/10 ,  A61P25/24 ,  A61P25/00 ,  A61P9/10 ,  C07D317/66

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 synthasc 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 2，GSK-3的抑制剂，制备这些化合物的方法，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。

公开(公告)号：EP1939191A1

公开(公告)日：2008-07-02

申请号：EP06127276.1

申请日：2006-12-28

申请人： Neuropharma S.A.

发明人： Martinez Gil, Ana ,  Medina Padilla, Miguel ,  Fall Diop, Yagamare ,  Gomez Pacios, Generosa ,  Pérez Vazquez, Manuel ,  Martin Aparicio, Ester ,  Fuertes Huerta, Ana ,  Del Monte Millan, Maria ,  Navarro Rico, Maria Luisa ,  Pérez Puerto, Maria, José

IPC分类号： C07D307/42 ,  C07D307/54 ,  A61K31/341 ,  A61P25/28

CPC分类号： C07D307/42 ,  C07D307/54

摘要： The present invention relates to furan derivatives of formula (I), their method of synthesis and uses thereof. Concretely, the compounds disclosed have proved to be inhibitors of glycogen synthase kinase 3β, GSK-3 β, which is known to be involved in different disease and conditions, such as Alzheimer's disease or non-insulin dependent diabetes mellitus. 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 GSK-3 mediated disease or condition.

摘要翻译： 本发明涉及式（I）的呋喃衍生物及其合成方法及用途。 具体地说，所公开的化合物已被证明是糖原合成酶激酶3 2，GSK-3 2的抑制剂，其已知涉及不同的疾病和病症如阿尔茨海默病或非胰岛素依赖性糖尿病。 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GSK-3介导的疾病或病症的药物中的用途。

公开(公告)号：EP1586319A1

公开(公告)日：2005-10-19

申请号：EP05075779.8

申请日：2005-04-04

申请人： Neuropharma S.A.

发明人： Martinez, Gil ,  Dorronsoro Diaz, Isabel ,  Alonso Cascon, Mercedes ,  Panizodel Pliego, Gema ,  Fuertes Huerta, Ana ,  Perez Puerto, Maria José ,  Medina Padilla, Miguel

IPC分类号： A61K31/433 ,  C07D285/08 ,  C07D417/04 ,  A61P25/28 ,  A61P3/10

CPC分类号： C07D285/08 ,  C07D417/04

摘要： Provided arc thiadiazolidinc compounds of formula I
wherein R 1 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，其不直接通过-C（O）直接与N连接，并且至少包含芳环 ，及其药物组合物。 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，包括阿尔茨海默病，II型糖尿病，抑郁症和脑损伤。