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11. 发明授权

US06956060B2 Use of R-enantiomer of N-propargyl-1-aminoindan, salts, and compositions thereof 失效
标题翻译： N-炔丙基-1-氨基茚满的R-对映异构体，其盐及其组合物的用途
公开(公告)号：US06956060B2
公开(公告)日：2005-10-18
申请号：US10305478
申请日：2002-11-27
申请人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling , David Lerner , Haim Yellin , Alex Veinberg
发明人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling , David Lerner , Haim Yellin , Alex Veinberg
IPC分类号： A61P9/10 , A61K20060101 , A61K31/135 , A61K31/136 , A61K31/137 , A61K31/195 , A61K31/215 , A61K45/06 , A61P20060101 , A61P9/00 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , C07C20060101 , C07C211/30 , C07C211/38 , C07C211/42
CPC分类号： C07C211/42 , A61K31/135 , A61K31/195 , A61K31/205 , A61K31/215 , A61K45/06 , C07C211/30 , C07C2602/08 , A61K2300/00
摘要： The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an effective illness, a neurodegenerative disease, a neurotoxic injury, stroke, brain ischemia, a head trauma injury, a spinal trauma injury, neurotrauma, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject. Finally, the subject invention provides methods of preparing R(+)-N-propargyl-1-aminoindan, a salt thereof, and racemic N-propargyl-1-aminoindan.
摘要翻译：本发明提供了R（+） - N-炔丙基-1-氨基茚满及其药学上可接受的盐，以及含有它们的药物组合物。本发明还提供了治疗患有帕金森病，记忆障碍，痴呆，抑郁症，多动症综合征，有效疾病，神经变性疾病，神经毒性损伤，中风，脑缺血，头部创伤损伤，脊髓损伤的受试者的方法使用R（+） - N-炔丙基-1-氨基茚满或本发明的药学上可接受的盐，创伤，神经损伤，精神分裂症，注意力缺陷障碍，多发性硬化或戒断症状。本发明进一步提供一种预防受试者的神经损伤的方法。最后，本发明提供了制备R（+） - N-炔丙基-1-氨基茚满其盐和外消旋的N-炔丙基-1-氨基茚满的方法。

12. 发明授权

US06630514B2 Use of R-enantiomer of N-propargyl-1-aminoindan, salts, and compositions thereof 失效
标题翻译： N-炔丙基-1-氨基茚满的R-对映异构体，其盐及其组合物的用途
公开(公告)号：US06630514B2
公开(公告)日：2003-10-07
申请号：US10016268
申请日：2001-10-26
申请人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling
发明人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling
IPC分类号： A61K31135
CPC分类号： C07C211/42 , A61K31/135 , A61K31/195 , A61K31/205 , A61K31/215 , A61K45/06 , C07C211/30 , C07C2602/08 , A61K2300/00
摘要： The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an affective illness, a neurodegenerative disease, a neurotoxic injury, stroke, brain ischemia, a head trauma injury, a spinal trauma injury, neurotrauma, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan, or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject. Finally, the subject invention provides methods of preparing R(+)-N-propargyl-1-aminoindan, a salt thereof, and racemic N-propargyl-1-aminoindan
摘要翻译：本发明提供了R（+） - N-炔丙基-1-氨基茚满及其药学上可接受的盐，以及含有它们的药物组合物。本发明还提供了治疗患有帕金森病，记忆障碍，痴呆，抑郁症，多动症综合征，情感疾病，神经变性疾病，神经毒性损伤，中风，脑缺血，头部外伤损伤，脊髓损伤的受试者的方法使用R（+） - N-炔丙基-1-氨基茚满或本发明的药学上可接受的盐的创伤损伤，神经损伤，精神分裂症，注意力缺陷障碍，多发性硬化或戒断症状。本发明进一步提供一种预防受试者的神经损伤的方法。最后，本发明提供了制备R（+） - N-炔丙基-1-氨基茚满其盐和外消旋N-炔丙基-1-氨基茚满的方法

13. 发明授权

US5668181A Use of the R-enantiomers of N-propargyl-1-aminoindan compounds for the treatment of depression 失效
标题翻译： N-炔丙基-1-氨基茚满化合物的R-对映异构体用于治疗抑郁症的用途
公开(公告)号：US5668181A
公开(公告)日：1997-09-16
申请号：US458645
申请日：1995-06-02
申请人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling , David Lerner , Tirtsah Berger-Paskin , Haim Yellin
发明人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling , David Lerner , Tirtsah Berger-Paskin , Haim Yellin
IPC分类号： C07C211/38 , A61K31/00 , A61K31/13 , A61K31/135 , A61K31/195 , A61K31/215 , A61K45/06 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , C07C209/88 , C07C211/30 , C07C211/42 , C12N9/99
CPC分类号： C07C211/30 , A61K31/135 , A61K31/195 , A61K31/215 , A61K45/06 , C07C211/42 , C07C2102/08
摘要： This invention relates to the use of R(+)-N-propargyl-1-aminoindan.
摘要翻译：本发明涉及R（+） - N-炔丙基-1-氨基茚满的用途。

14. 发明授权

US5599991A Esylate and sulfate salts of R(+)-N-propargyl-1-aminoindan 失效
标题翻译： R（+） - N-炔丙基-1-氨基茚满的盐酸盐和硫酸盐
公开(公告)号：US5599991A
公开(公告)日：1997-02-04
申请号：US465787
申请日：1995-06-06
申请人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling , David Lerner , Haim Yellin , Alex Veinberg
发明人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling , David Lerner , Haim Yellin , Alex Veinberg
IPC分类号： C07C211/38 , A61K31/00 , A61K31/13 , A61K31/135 , A61K31/195 , A61K31/215 , A61K45/06 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , C07C209/88 , C07C211/30 , C07C211/42 , C12N9/99
CPC分类号： C07C211/30 , A61K31/135 , A61K31/195 , A61K31/215 , A61K45/06 , C07C211/42 , C07C2102/08
摘要： The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an affective illness, a neurodegenerative disease, a neurotoxic injury, brain ischemia, a head trauma injury, a spinal trauma injury, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject. Finally, the subject invention provides methods of preparing R(+)-N-propargyl-1-aminoindan, a salt thereof, and racemic N-propargyl-1-aminoindan.
摘要翻译：本发明提供了R（+） - N-炔丙基-1-氨基茚满及其药学上可接受的盐，以及含有它们的药物组合物。本发明还提供了治疗患有帕金森病，记忆障碍，痴呆，抑郁症，多动症综合征，情感疾病，神经变性疾病，神经毒性损伤，脑缺血，头部创伤损伤，脊髓损伤损伤，精神分裂症，注意力缺陷障碍，多发性硬化或戒断症状，使用本发明的R（+） - N-炔丙基-1-氨基茚满或其药学上可接受的盐。本发明进一步提供一种预防受试者的神经损伤的方法。最后，本发明提供了制备R（+） - N-炔丙基-1-氨基茚满其盐和外消旋的N-炔丙基-1-氨基茚满的方法。

15. 发明授权

US5576353A Method of treating memory disorders using R-enantiomers of N-propargyl-aminoindan compounds 失效
标题翻译：使用N-炔丙基 - 氨基茚满化合物的R-对映异构体治疗记忆障碍的方法
公开(公告)号：US5576353A
公开(公告)日：1996-11-19
申请号：US459402
申请日：1995-06-02
申请人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Haim Yellin
发明人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Haim Yellin
IPC分类号： C07C211/38 , A61K31/00 , A61K31/13 , A61K31/135 , A61K31/195 , A61K31/215 , A61K45/06 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , C07C209/88 , C07C211/30 , C07C211/42 , C12N9/99
CPC分类号： C07C211/30 , A61K31/135 , A61K31/195 , A61K31/215 , A61K45/06 , C07C211/42 , C07C2102/08
摘要： R(+)-N-propargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's disease, memory disorders, dementia of the Alzheimer type (DAT), depression and the hyperactive syndrome.
摘要翻译： R（+） - N-炔丙基-1-氨基茚满，其制备和用途以及含有它的药物组合物。发现该新化合物可用于治疗帕金森病，记忆障碍，阿尔茨海默氏型痴呆（DAT），抑郁症和多动症综合征的人类患者。

16. 发明授权

US5457133A R-enantiomers of N-propargyl-aminoindan compounds, their preparation and pharmaceutical compositions containing them 失效
标题翻译： N-炔丙基 - 氨基茚满化合物的R-对映异构体，其制备方法和含有它们的药物组合物
公开(公告)号：US5457133A
公开(公告)日：1995-10-10
申请号：US198205
申请日：1994-02-17
申请人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling , David Lerner , Tirtsah Berger-Paskin , Haim Yellin
发明人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling , David Lerner , Tirtsah Berger-Paskin , Haim Yellin
IPC分类号： C07C211/38 , A61K31/00 , A61K31/13 , A61K31/135 , A61K31/195 , A61K31/215 , A61K45/06 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , C07C209/88 , C07C211/30 , C07C211/42 , C12N9/99
CPC分类号： C07C211/30 , A61K31/135 , A61K31/195 , A61K31/215 , A61K45/06 , C07C211/42 , C07C2102/08
摘要： R(+)-N-propargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's disease, memory disorders, dementia of the Alzheimer type (DAT), depression and the hyperactive syndrome.
摘要翻译： R（+） - N-炔丙基-1-氨基茚满，其制备和用途以及含有它的药物组合物。发现该新化合物可用于治疗帕金森病，记忆障碍，阿尔茨海默氏型痴呆（DAT），抑郁症和多动症综合征的人类患者。

17. 发明授权

US5453446A Use of the R-enantiomers of N-propargyl 1-aminoindan compounds for treating Parkinson's disease. 失效
标题翻译： N-炔丙基1-氨基茚满化合物的R-对映异构体用于治疗帕金森病的用途。
公开(公告)号：US5453446A
公开(公告)日：1995-09-26
申请号：US255046
申请日：1994-06-07
申请人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling , David Lerner , Tirtsah Berger-Paskin , Haim Yellin
发明人： Moussa B. H. Youdim , John P. M. Finberg , Ruth Levy , Jeffrey Sterling , David Lerner , Tirtsah Berger-Paskin , Haim Yellin
IPC分类号： C07C211/38 , A61K31/00 , A61K31/13 , A61K31/135 , A61K31/195 , A61K31/215 , A61K45/06 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , C07C209/88 , C07C211/30 , C07C211/42 , C12N9/99
CPC分类号： C07C211/30 , A61K31/135 , A61K31/195 , A61K31/215 , A61K45/06 , C07C211/42 , C07C2102/08
摘要： R(+)-N-p-opargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's disease, memory disorders, dementia of the Alzheimer type (DAT), depression and the hyperactive syndrome.
摘要翻译： R（+） - N-p-opargyl-1-氨基茚丹，其制备和用途以及含有它的药物组合物。发现该新化合物可用于治疗帕金森病，记忆障碍，阿尔茨海默氏型痴呆（DAT），抑郁症和多动症综合征的人类患者。

18. 发明授权

US5880159A Compositions containing and methods of using 1-aminoindan and derivatives thereof and process for preparing optically active 1-aminoindan derivatives 失效
公开(公告)号：US5880159A
公开(公告)日：1999-03-09
申请号：US948212
申请日：1997-10-09
申请人： Yaacov Herzig , Jeff Sterling , Alex Veinberg , Moussa B. H. Youdim , John P. M. Finberg , Naim Sayag
发明人： Yaacov Herzig , Jeff Sterling , Alex Veinberg , Moussa B. H. Youdim , John P. M. Finberg , Naim Sayag
IPC分类号： A01N37/18 , A01N37/34 , A61K31/135 , A61K31/137 , A61K31/16 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/24 , A61K31/27 , A61K31/275 , A61K31/277 , C07C209/04 , C07C209/88 , C07C211/00 , C07C211/38 , C07C211/42 , C07C213/10 , C07C215/44 , C07C217/74 , C07C231/20 , C07C233/05 , C07C233/06 , C07C233/23 , C07C233/74 , C07C237/04
CPC分类号： C07C237/04 , A61K31/135 , A61K31/136 , A61K31/137 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/24 , A61K31/27 , A61K31/275 , A61K31/277 , C07C209/04 , C07C209/88 , C07C211/38 , C07C211/42 , C07C213/10 , C07C215/44 , C07C217/52 , C07C217/74 , C07C231/20 , C07C233/03 , C07C233/06 , C07C233/11 , C07C233/14 , C07C233/23 , C07C233/52 , C07C233/65 , C07C233/74 , C07C235/54 , C07C237/22 , C07C237/48 , C07C255/24 , C07C255/58 , C07C271/22 , C07C2102/08 , C07C2102/10
摘要： Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid. Parkinson's disease, dementia, epilepsy, convulsions, or seizures are treated by administering a compound of the formula: ##STR1##

19. 发明授权

US06251938B1 Phenylethylamine derivatives 失效
标题翻译：苯乙胺衍生物
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

20. 发明授权

US08802675B2 Neuroprotective multifunctional compounds and pharmaceutical compositions comprising them 有权
标题翻译：神经保护性多功能化合物和包含它们的药物组合物
公开(公告)号：US08802675B2
公开(公告)日：2014-08-12
申请号：US13146975
申请日：2010-01-31
申请人： Moussa B. H. Youdim , Mati Fridkin , Hailin Zheng
发明人： Moussa B. H. Youdim , Mati Fridkin , Hailin Zheng
IPC分类号： A01N43/64 , A61K31/53 , A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , A61K31/497 , A01N43/54 , A61K31/517 , A01N43/42 , A61K31/47 , A01N43/40 , A61K31/445 , A01N47/10 , A61K31/27 , A01N33/02 , A61K31/135 , A61K31/13 , C07D253/08 , C07D487/00 , C07D239/72 , C07D241/36 , C07D401/00 , C07D215/16 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00 , C07C211/00
CPC分类号： C07C259/10 , C07C211/38 , C07C271/40 , C07C2602/08 , C07C2603/74 , C07D215/34 , C07D401/06 , C07D401/12
摘要： Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition. The present invention encompasses compounds of the formulas I to VI.
摘要翻译：提供多官能化合物，其包含两个或多个选自以下的官能部分：（i）赋予铁螯合剂功能的部分; （ii）赋予神经保护功能的部分; （iii）赋予组合的抗细胞凋亡，神经保护和/或神经恢复功能的部分; （iv）赋予脑MAO抑制的部分，优选在肝脏和小肠中几乎没有MAO抑制作用; （v）赋予胆碱酯酶抑制功能的部分; 和（vi）赋予N-甲基-D-天冬氨酸受体（NMDAR）抑制的部分及其药学上可接受的盐和旋光异构体。多官能化合物可用于治疗或预防可通过铁螯合治疗和/或神经保护和/或神经恢复，和/或凋亡抑制和/或MAO抑制和/或MAO抑制和/或治疗的/ 或胆碱酯酶抑制和/或NMADR抑制。本发明包括式I至VI的化合物。

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