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1.发明授权INDOLE AMIDE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES 有权维生素D VERBINDUNGEN ZUR BEHANDLUNG VON NEURODEGENERATIVEN ERKRANKUNGEN INDOLAMIDDERIVATE
公开(公告)号：EP2440550B1
公开(公告)日：2017-03-15
申请号：EP10728150.3
申请日：2010-06-11
发明人： GRIFFIOEN, Gerard , VAN DOOREN, Tom , ROJAS DE LA PARRA, Veronica , MARCHAND, Arnaud , ALLASIA, Sara , KILONDA, Amuri , CHALTIN, Patrick
IPC分类号： C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/4045 , A61P25/28
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
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2.发明公开NEW COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 有权N - （（1H-吲哚-3-基）烷基）-4-苄基）苯甲酰胺，和N - （（1H-吡咯并[2,3-b]吡啶-3-基）烷基）-4-苄基） 苯甲酰胺衍生物作为α-突触核蛋白聚集抑制剂用于治疗神经变性疾病的治疗
公开(公告)号：EP2651888A1
公开(公告)日：2013-10-23
申请号：EP11805450.1
申请日：2011-12-13
发明人： GRIFFIOEN, Gerard , VAN DOOREN, Tom , ROJAS DE LA PARRA, Verónica , ALLASIA, Sara , MARCHAND, Arnaud , KILONDA, Amuri , CHALTIN, Patrick
IPC分类号： C07D209/14 , C07D471/04 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/4045 , A61P25/28 , A61P25/16
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 R
1 , R
2 , R
4 , R
6 , E, n, Y
1 , Y
2 , Y
3 , Y
4 , Y
5 , L, B, R
8 , and m are as defined in the claims.-
3.发明公开NOVEL COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 有权N-（2-（5-取代的-1H-吲哚-3-基）乙基）联苯-4-甲酰胺衍生物和相关化合物作为τ聚集诱导的毒性抑制剂的神经变性疾病的治疗
公开(公告)号：EP2651887A1
公开(公告)日：2013-10-23
申请号：EP11804532.7
申请日：2011-12-13
发明人： GRIFFIOEN, Gerard , VAN DOOREN, Tom , ROJAS DE LA PARRA, Verónica , MARCHAND, Arnaud , ALLASIA, Sara , KILONDA, Amuri , CHALTIN, Patrick
IPC分类号： C07D209/14 , C07D471/04 , A61K31/4045 , A61P25/28 , A61P25/16
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 R
1 , R
2 , R
4 , R
5 , R
6 , E, n, Y
1 , Y
2 , Y
3 , Y
4 , Y
5 , B, R
8 , and m are as defined in the claims.-
4.发明公开INDOLE AMIDE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES 有权INDOLAMIDDERIVATE和神经退行性疾病的治疗相关的化合物
公开(公告)号：EP2440550A1
公开(公告)日：2012-04-18
申请号：EP10728150.3
申请日：2010-06-11
发明人： GRIFFIOEN, Gerard , VAN DOOREN, Tom , ROJAS DE LA PARRA, Veronica , MARCHAND, Arnaud , ALLASIA, Sara , KILONDA, Amuri , CHALTIN, Patrick
IPC分类号： C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/4045 , A61P25/28
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.
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5.发明授权PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE 有权PIPERAZINTHIAZOLDERIVATE阿尔茨海默病作为Tau蛋白病的治疗
公开(公告)号：EP2744798B1
公开(公告)日：2016-03-30
申请号：EP12756402.9
申请日：2012-08-17
申请人： reMYND NV
发明人： GRIFFIOEN, Gerard , CECERE, Giuseppe , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , ROGERS-EVANS, Mark , VIFIAN, Walter
IPC分类号： C07D417/14 , C07D285/08 , C07D417/04 , C07D417/12 , A61K31/433 , A61P25/28
CPC分类号： A61K31/496 , C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to a compound of formula (IA), wherein G1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is —NR2R3; R2 is hydrogen or lower alkyl; R3 is lower alkyl; tetrahydropyran-4-yl; —CH2-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is —CH2—or —(CH2)2—; Ar is phenyl or pyridinyl; R4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
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6.发明授权1,2,4-THIADIAZOL-5-YLPIPERAZINE DERIVATIVES USEFUL IN THE TREATMENT OF NEURODEGENERATIVE DISEASES 有权用于治疗神经变性疾病的1，2，4 -THIADIAZOL- -5-基哌嗪衍生物
公开(公告)号：EP2726470B1
公开(公告)日：2015-04-29
申请号：EP12737238.1
申请日：2012-06-29
申请人： reMYND NV
IPC分类号： C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14 , A61K31/433 , A61P25/28
CPC分类号： C07D285/135 , C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14
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公开(公告)号：EP1644505B1
公开(公告)日：2008-04-23
申请号：EP04737685.0
申请日：2004-07-09
申请人： reMynd NV
IPC分类号： C12N15/81 , C12N9/64 , C07K14/395 , C07K14/47 , G01N33/68
CPC分类号： C12N15/81 , C07K14/395
摘要： The present invention relates to an engineered yeast strain, comprising a transgene encoding one or more amyloidogenic proteins or mutant(s) thereof, characterised in that it lacks one or more functional genes responsive to oxidative stress. The invention further relates to the use of this yeast strain for pharmaceutical screening, for modelling of neurodegenerative diseases and for cellular modelling of biochemistry of the amyloidogenic proteins involved therein.
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公开(公告)号：EP3119782B1
公开(公告)日：2018-01-31
申请号：EP15710486.0
申请日：2015-03-17
申请人： reMYND NV
发明人： GRIFFIOEN, Gerard , DE TAEYE, Bart , PRINCEN, Katrien , DE WITTE, Koen , BLANCHE, Emilie , RATNI, Hasane , ROGERS-EVANS, Mark
IPC分类号： C07D471/10 , A61P3/10 , A61K31/438
CPC分类号： A61K31/5377 , A61K31/435 , A61K31/444 , C07D471/10
摘要： The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, Formula (I), wherein R1, R3, R4, L1, L2, L3, L4, and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.
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9.发明授权N-((1H-indol-3-yl)-alkyl)-4-benzyl)benzamide and N-((1H-pyrrolo[2,3-b]pyridin-3-yl)-alkyl)-4-benzyl)benzamide derivatives as alpha synuclein aggregation inhibitors for the treatment of neurodegenerative disorders 有权N-（（1H-吲哚-3-基） - 烷基）-4-苄基）苯甲酰胺和N - （（1H-吡咯并[2,3-b]吡啶-3-基） - 烷基）-4-苄基） 苯甲酰胺衍生物α-突触核蛋白聚集抑制剂zur Behandlung von neurodegenerativen Erkrankungen
公开(公告)号：EP2651888B1
公开(公告)日：2017-05-17
申请号：EP11805450.1
申请日：2011-12-13
发明人： GRIFFIOEN, Gerard , VAN DOOREN, Tom , ROJAS DE LA PARRA, Verónica , ALLASIA, Sara , MARCHAND, Arnaud , KILONDA, Amuri , CHALTIN, Patrick
IPC分类号： C07D209/14 , C07D471/04 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/4045 , A61P25/28 , A61P25/16
CPC分类号： C07D209/14 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04
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10.发明公开PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE 有权PIPERAZINTHIAZOLDERIVATE阿尔茨海默病作为Tau蛋白病的治疗
公开(公告)号：EP2744798A1
公开(公告)日：2014-06-25
申请号：EP12756402.9
申请日：2012-08-17
申请人： reMYND NV
发明人： GRIFFIOEN, Gerard , CECERE, Giuseppe , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , ROGERS-EVANS, Mark , VIFIAN, Walter
IPC分类号： C07D285/08 , C07D417/04 , C07D417/12 , A61K31/433 , A61P25/28
CPC分类号： A61K31/496 , C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to a compound of formula (IA), wherein G1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is —NR2R3; R2 is hydrogen or lower alkyl; R3 is lower alkyl; tetrahydropyran-4-yl; —CH2-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is —CH2—or —(CH2)2—; Ar is phenyl or pyridinyl; R4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
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