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公开(公告)号:US20070135518A1
公开(公告)日:2007-06-14
申请号:US11635922
申请日:2006-12-08
申请人: Marta Weinstock-Rosin , Shai Shoham
发明人: Marta Weinstock-Rosin , Shai Shoham
IPC分类号: A61K31/325
CPC分类号: A61K31/325 , A61K31/27
摘要: The subject invention provides a method of preventing a neurodegenerative disease in a subject or oxidative stress in the brain of a subject, comprising administering to the subject a less than cholinesterase-inhibitory amount or a less than monoamine oxidase-inhibitory amount of R(+)-6-(N-methyl,N-ethyl-carbamoyloxy)-N′-propargyl-1-aminoindan or a salt thereof effective to prevent the neurodegenerative disease or oxidative stress in the subject.
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公开(公告)号:US06251938B1
公开(公告)日:2001-06-26
申请号:US09335555
申请日:1999-06-18
申请人: Michael Chorev , Tamar Goren , Yacov Herzig , Jeffrey Sterling , Marta Weinstock-Rosin , Moussa B. H. Youdim
发明人: Michael Chorev , Tamar Goren , Yacov Herzig , Jeffrey Sterling , Marta Weinstock-Rosin , Moussa B. H. Youdim
IPC分类号: A61K3127
CPC分类号: C07C271/42 , C07C271/56
摘要: This invention is directed to compounds of the following formula: wherein m is from 0-4; X is O or S; Y is halogeno; R1 is hydrogen or C1-4 alkyl; R2 is hydrogen, C1-4 alkyl or optionally substituted propargyl; and R3 and R4 are each independently hydrogen, C1-8 alkyl, C6-12 aryl, C6-12 cycloalkyl or C6-12 aralkyl, R5 is hydrogen or C1-4 alkyl; and pharmaceutically acceptable salts thereof, provided that when X is O, R2 is optionally substituted propargyl. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译: 本发明涉及下式的化合物:其中m为0-4; X是O或S; Y为卤素; R1是氢或C1-4烷基; R2是氢,C1-4烷基或任选取代的炔丙基; 并且R 3和R 4各自独立地为氢,C 1-8烷基,C 6-12芳基,C 6-12环烷基或C 6-12芳烷基,R 5为氢或C 1-4烷基; 其中X为O时,R2为任选取代的炔丙基。本发明还涉及这些化合物用于治疗抑郁症,注意力缺陷症(ADD),注意力缺陷和多动症(ADHD)的用途, Tourette综合征,阿尔茨海默病和其他痴呆症如老年性痴呆,帕金森氏型痴呆,血管性痴呆和路易体痴呆。本发明还涉及一种药物组合物,其包含治疗有效量的上述化合物和药学上可接受的 载体
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3.
公开(公告)号:US08609719B2
公开(公告)日:2013-12-17
申请号:US12582491
申请日:2009-10-20
申请人: Victor Piryatinsky , Bronka Cohen , David Lerner , Dalia Pinkert , Istvan Miskolczi , Yaacov Herzig , Hugo Gottlieb , Marta Weinstock-Rosin
发明人: Victor Piryatinsky , Bronka Cohen , David Lerner , Dalia Pinkert , Istvan Miskolczi , Yaacov Herzig , Hugo Gottlieb , Marta Weinstock-Rosin
IPC分类号: A61K31/13
CPC分类号: C07C271/48 , A61K31/27 , A61K31/325 , C07B2200/07 , C07C271/44 , C07C2602/08
摘要: A method for treating an individual who has been identified as having Alzheimer's disease by administering orally to the individual a therapeutically effective amount of ladostigil or a pharmaceutically active salt thereof, wherein the therapeutically effective amount is 70 mg per day, 140 mg per day, or 200 mg per day. Also, a unit dosage form of ladostigil or a pharmaceutically active salt thereof in an amount of 50 mg, 70 mg, 80 mg or 100 mg.
摘要翻译: 治疗已被鉴定为患有阿尔茨海默病的个体的方法,其通过向个体口服施用治疗有效量的前消炎症或其药物活性盐,其中治疗有效量为每天70mg,每天140mg,或 每天200毫克。 而且,剂量为50mg,70mg,80mg或100mg的地斯达格或其药物活性盐的单位剂型。
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公开(公告)号:US06538025B2
公开(公告)日:2003-03-25
申请号:US09944912
申请日:2001-08-31
申请人: Michael Chorev , Tamar Goren , Yacov Herzig , Jeffrey Sterling , Marta Weinstock-Rosin , Moussa B.H. Youdim
发明人: Michael Chorev , Tamar Goren , Yacov Herzig , Jeffrey Sterling , Marta Weinstock-Rosin , Moussa B.H. Youdim
IPC分类号: A61K3127
CPC分类号: C07C271/56 , C07C271/24 , C07C271/44 , C07C271/58 , C07C333/04 , C07C2601/14 , C07C2602/08 , C07C2602/10
摘要: This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译: 本发明涉及下式的化合物:其中当a为0时,b为1或2; 当a为1时,b为1,m为0-3,X为O或S,Y为卤素,R1为氢C1-4烷基,R2为氢,C1-4烷基或任选取代的炔丙基,R3和 R 4各自独立地为氢,C 1-6烷基,C 6-12芳基,各自任选取代的C 6-12芳烷基。本发明还涉及这些化合物用于治疗抑郁症,注意力缺陷(ADD),注意力缺陷和多动症 疾病(ADHD),Tourette综合征,阿尔茨海默病和其他痴呆症如老年性痴呆,帕金森氏型痴呆,血管性痴呆和路易体痴呆。本发明还涉及包含治疗有效量的上述定义的药物组合物 化合物和药学上可接受的载体。
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公开(公告)号:US06462222B1
公开(公告)日:2002-10-08
申请号:US09944850
申请日:2001-08-31
申请人: Michael Chorev , Tamar Goren , Yacov Herzig , Jeffrey Sterling , Marta Weinstock-Rosin , Moussa B. H. Youdim
发明人: Michael Chorev , Tamar Goren , Yacov Herzig , Jeffrey Sterling , Marta Weinstock-Rosin , Moussa B. H. Youdim
IPC分类号: C07C26100
CPC分类号: C07C271/56 , C07C271/24 , C07C271/44 , C07C271/58 , C07C333/04 , C07C2601/14 , C07C2602/08 , C07C2602/10
摘要: This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is 0 or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R1 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome. Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译: 本发明涉及下式的化合物:其中当a为0时,b为1或2; 当a为1时,b为1,m为0-3,X为0或S,Y为卤素,R1为氢C1-4烷基,R2为氢,C1-4烷基或任选取代的炔丙基,R1和 R 4各自独立地为氢,C 1-6烷基,C 6-12芳基,各自任选取代的C 6-12芳烷基。本发明还涉及这些化合物用于治疗抑郁症,注意力缺陷(ADD),注意力缺陷和多动症 多动症(ADHD),Tourette综合征。 阿尔茨海默病和其他痴呆症如老年性痴呆,帕金森氏型痴呆,血管性痴呆和路易体痴呆。本发明还涉及包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。
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公开(公告)号:US06303650B1
公开(公告)日:2001-10-16
申请号:US09336493
申请日:1999-06-18
申请人: Michael Chorev , Tamar Goren , Yacov Herzig , Jeffrey Sterling , Marta Weinstock-Rosin , Moussa B. H. Youdim
发明人: Michael Chorev , Tamar Goren , Yacov Herzig , Jeffrey Sterling , Marta Weinstock-Rosin , Moussa B. H. Youdim
IPC分类号: A61K3127
CPC分类号: C07C271/56 , C07C271/24 , C07C271/44 , C07C271/58 , C07C333/04 , C07C2601/14 , C07C2602/08 , C07C2602/10
摘要: This invention is directed to compounds of the following formula wherein when a is O, b is 1 or 2; when a is 1, b is 1, m is from 0-3 X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-8 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADC), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译: 本发明涉及当a是O,b是1或2时,下列化合物的化合物: 当a为1时,b为1,m为0-3 X为O或S,Y为卤素,R1为氢C1-4烷基,R2为氢,C1-4烷基或任选取代的炔丙基,R3和R4 各自独立地为氢,C 1-8烷基,C 6-12芳基,各自任选取代的C 6-12芳烷基。本发明还涉及这些化合物用于治疗抑郁症,注意力缺陷(ADC),注意力缺陷和多动障碍 (ADHD),Tourette综合征,阿尔茨海默氏病和其他痴呆症如老年性痴呆,帕金森氏型痴呆,血管性痴呆和路易体痴呆。本发明还涉及一种药物组合物,其包含治疗有效量的上述定义的化合物 和药学上可接受的载体。
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公开(公告)号:US20140349927A1
公开(公告)日:2014-11-27
申请号:US14453187
申请日:2014-08-06
CPC分类号: A61K31/27 , A61K31/325 , A61K45/06 , A61K2300/00
摘要: Methods for treating individuals suffering from inflammation, specifically systemic inflammation including septic shock and inflammatory conditions affecting the gastrointestinal, myocardial and endocrine systems with ladostigil.
摘要翻译: 用于治疗患有炎症的个体的方法,特别是全身性炎症,包括脓毒性休克和影响胃肠道,心肌和内分泌系统的炎性疾病。
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公开(公告)号:US08420696B2
公开(公告)日:2013-04-16
申请号:US11637600
申请日:2006-12-11
申请人: Marta Weinstock-Rosin , Shai Shoham
发明人: Marta Weinstock-Rosin , Shai Shoham
IPC分类号: A61K31/27
CPC分类号: A61K31/27 , A61K31/325
摘要: The subject invention provides a method of preventing a neurodegenerative disease in a subject or oxidative stress in the brain of a subject, comprising administering to the subject a less than cholinesterase-inhibitory amount or a less than monoamine oxidase-inhibitory amount of R(+)-6-(N-methyl,N-ethyl-carbamoyloxy)-N′-propargyl-1-aminoindan or a salt thereof effective to prevent the neurodegenerative disease or oxidative stress in the subject.
摘要翻译: 本发明提供一种预防受试者的神经变性疾病或受试者脑部氧化应激的方法,其包括对受试者施用少于胆碱酯酶抑制量或少于单胺氧化酶抑制量的R(+) -6-(N-甲基,N-乙基 - 氨基甲酰氧基)-N'-炔丙基-1-氨基茚满或其盐,其有效地防止受试者的神经变性疾病或氧化应激。
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9.
公开(公告)号:US20100093848A1
公开(公告)日:2010-04-15
申请号:US12582491
申请日:2009-10-20
申请人: Victor Piryatinsky , Bronka Cohen , David Lerner , Dalia Pinkert , Istvan Miskolczi , Yaacov Herzig , Hugo Gottlieb , Marta Weinstock-Rosin
发明人: Victor Piryatinsky , Bronka Cohen , David Lerner , Dalia Pinkert , Istvan Miskolczi , Yaacov Herzig , Hugo Gottlieb , Marta Weinstock-Rosin
CPC分类号: C07C271/48 , A61K31/27 , A61K31/325 , C07B2200/07 , C07C271/44 , C07C2602/08
摘要: A method for treating an individual who has been identified as having Alzheimer's disease by administering orally to the individual a therapeutically effective amount of ladostigil or a pharmaceutically active salt thereof, wherein the therapeutically effective amount is 70 mg per day, 140 mg per day, or 200 mg per day. Also, a unit dosage form of ladostigil or a pharmaceutically active salt thereof in an amount of 50 mg, 70 mg, 80 mg or 100 mg.
摘要翻译: 治疗已被鉴定为患有阿尔茨海默病的个体的方法,其通过向个体口服施用治疗有效量的前消炎症或其药物活性盐,其中治疗有效量为每天70mg,每天140mg,或 每天200毫克。 而且,剂量为50mg,70mg,80mg或100mg的地斯达格或其药物活性盐的单位剂型。
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公开(公告)号:US20070293583A1
公开(公告)日:2007-12-20
申请号:US11637600
申请日:2006-12-11
申请人: Marta Weinstock-Rosin , Shai Shoham
发明人: Marta Weinstock-Rosin , Shai Shoham
IPC分类号: A61K31/135 , A61P25/16 , A61P25/28 , C07C211/38
CPC分类号: A61K31/27 , A61K31/325
摘要: The subject invention provides a method of preventing a neurodegenerative disease in a subject or oxidative stress in the brain of a subject, comprising administering to the subject a less than cholinesterase-inhibitory amount or a less than monoamine oxidase-inhibitory amount of R(+)-6-(N-methyl,N-ethyl-carbamoyloxy)-N′-propargyl-1-aminoindan or a salt thereof effective to prevent the neurodegenerative disease or oxidative stress in the subject.
摘要翻译: 本发明提供一种预防受试者的神经变性疾病或受试者脑部氧化应激的方法,其包括对受试者施用少于胆碱酯酶抑制量或少于单胺氧化酶抑制量的R(+) -6-(N-甲基,N-乙基 - 氨基甲酰氧基)-N'-炔丙基-1-氨基茚满或其盐,其有效地防止受试者的神经变性疾病或氧化应激。
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