公开(公告)号：US09266832B2

公开(公告)日：2016-02-23

申请号：US13993723

申请日：2011-12-13

申请人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Sara Allasia ,  Arnaud Marchand ,  Amuri Kilonda ,  Patrick Chaltin

发明人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Sara Allasia ,  Arnaud Marchand ,  Amuri Kilonda ,  Patrick Chaltin

IPC分类号： C07D409/12 ,  C07D401/12 ,  C07D403/12 ,  C07D209/14 ,  C07D405/12 ,  C07D471/04

CPC分类号： C07D209/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.

摘要翻译： 本发明提供了新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地，某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症 。 本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。 本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。 该化合物具有式（A1），其中R1，R2，R4，R6，E，n，Y1，Y2，Y3，Y4，Y5，L，B，R8和m如权利要求中所定义。

公开(公告)号：US20130274260A1

公开(公告)日：2013-10-17

申请号：US13993723

申请日：2011-12-13

申请人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Sara Allasia ,  Arnaud Marchand ,  Amuri Kilonda ,  Patrick Chaltin

发明人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Sara Allasia ,  Arnaud Marchand ,  Amuri Kilonda ,  Patrick Chaltin

IPC分类号： C07D209/14 ,  C07D471/04 ,  C07D409/12 ,  C07D405/12 ,  C07D403/12 ,  C07D401/12

CPC分类号： C07D209/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.

摘要翻译： 本发明提供新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地说是某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症 。 本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。 本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。 该化合物具有式（A1），其中R1，R2，R4，R6，E，n，Y1，Y2，Y3，Y4，Y5，L，B，R8和m如权利要求中所定义。

公开(公告)号：US20130289033A1

公开(公告)日：2013-10-31

申请号：US13993756

申请日：2011-12-13

申请人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Arnaud Marchand ,  Sara Alassia ,  Amuri Kilonda ,  Patrick Chaltin

发明人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Arnaud Marchand ,  Sara Alassia ,  Amuri Kilonda ,  Patrick Chaltin

IPC分类号： C07D209/18 ,  C07D409/12 ,  C07D401/12

CPC分类号： C07D209/18 ,  C07D209/14 ,  C07D401/12 ,  C07D409/12 ,  C07D471/04

摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1), wherein R1, R2, R4, R5, R6, E, n, Y1, Y2, Y3, Y4, Y5, B, R8, and m are as defined in the claims.

摘要翻译： 本发明提供新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地说是某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症 。 本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。 本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。 化合物具有式（A1），其中R1，R2，R4，R5，R6，E，n，Y1，Y2，Y3，Y4，Y5，B，R8和m如权利要求中所定义。

公开(公告)号：US09284271B2

公开(公告)日：2016-03-15

申请号：US13993756

申请日：2011-12-13

申请人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Arnaud Marchand ,  Sara Alassia ,  Amuri Kilonda ,  Patrick Chaltin

发明人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Arnaud Marchand ,  Sara Alassia ,  Amuri Kilonda ,  Patrick Chaltin

IPC分类号： C07D209/14 ,  C07D209/18 ,  C07D401/12 ,  C07D409/12 ,  C07D471/04

CPC分类号： C07D209/18 ,  C07D209/14 ,  C07D401/12 ,  C07D409/12 ,  C07D471/04

摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1), wherein R1, R2, R4, R5, R6, E, n, Y1, Y2, Y3, Y4, Y5, B, R8, and m are as defined in the claims.

摘要翻译： 本发明提供了新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地，某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症 。 本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。 本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。 化合物具有式（A1），其中R1，R2，R4，R5，R6，E，n，Y1，Y2，Y3，Y4，Y5，B，R8和m如权利要求中所定义。

公开(公告)号：US08618138B2

公开(公告)日：2013-12-31

申请号：US13377505

申请日：2010-06-11

申请人： Gerard Griffioen ,  Tom Van Dooren ,  Veronica Rojas De La Parra ,  Arnaud Marchand ,  Sara Allasia ,  Amuri Kilonda ,  Patrick Chaltin

发明人： Gerard Griffioen ,  Tom Van Dooren ,  Veronica Rojas De La Parra ,  Arnaud Marchand ,  Sara Allasia ,  Amuri Kilonda ,  Patrick Chaltin

IPC分类号： A61K31/4439 ,  A61K31/422 ,  C07D413/14 ,  C07D261/18

CPC分类号： A61K31/4045 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/635 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

摘要翻译： 本发明提供新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地说是某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症 。 本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。 本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。

公开(公告)号：US20120083475A1

公开(公告)日：2012-04-05

申请号：US13377505

申请日：2010-06-11

申请人： Gerard Griffioen ,  Tom Van Dooren ,  Veronica Rojas De La Parra ,  Arnaud Marchand ,  Sara Allasia ,  Amuri Kilonda ,  Patrick Chaltin

发明人： Gerard Griffioen ,  Tom Van Dooren ,  Veronica Rojas De La Parra ,  Arnaud Marchand ,  Sara Allasia ,  Amuri Kilonda ,  Patrick Chaltin

IPC分类号： A61K31/635 ,  C07D413/14 ,  C07D409/14 ,  C07D405/14 ,  C07D417/12 ,  C07D403/12 ,  C07D417/14 ,  A61K31/422 ,  A61K31/4155 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4192 ,  A61K31/4045 ,  A61K31/497 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  C07D413/12

CPC分类号： A61K31/4045 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/635 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

摘要翻译： 本发明提供了新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地，某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症 。 本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。 本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。

公开(公告)号：US08541406B2

公开(公告)日：2013-09-24

申请号：US12187115

申请日：2008-08-06

申请人： Gerard Griffioen ,  Kristel Marie Edith Coupet ,  Hein Roger Duhamel ,  Stefaan Wera ,  Ellen Gommé ,  Nele Van Damme ,  Ingrid Van Der Auwera ,  Marleen Lox ,  Tom Van Dooren ,  Tine Decruy

发明人： Gerard Griffioen ,  Kristel Marie Edith Coupet ,  Hein Roger Duhamel ,  Stefaan Wera ,  Ellen Gommé ,  Nele Van Damme ,  Ingrid Van Der Auwera ,  Marleen Lox ,  Tom Van Dooren ,  Tine Decruy

IPC分类号： A61K31/55 ,  C07D241/02

CPC分类号： A61K31/497 ,  A61K31/55

摘要： This invention provides specifically substituted 1,2,4-thiadiazole derivatives for use in the treatment of an α-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides various methods for producing such substituted 1,2,4-thiadiazole derivatives.

摘要翻译： 本发明提供了特异性取代的1,2,4-噻二唑衍生物，用于治疗α-突触核蛋白病如帕金森病，弥漫性路易体病，创伤性脑损伤，肌萎缩性侧索硬化，尼曼 - 皮克病，哈勒沃登 - 斯皮茨综合征 ，唐氏综合征，神经性营养不良，多系统萎缩和阿尔茨海默病。 本发明还提供了制备这种取代的1,2,4-噻二唑衍生物的各种方法。