公开(公告)号：WO1995018617A1

公开(公告)日：1995-07-13

申请号：PCT/US1995000245

申请日：1995-01-09

Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD. ,  TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD. ,  COHEN, Sasson ,  HERZIG, Yaacov ,  LEVY, Ruth ,  SPEISER, Tzipora ,  SHIRVAN, Mitchell ,  STERLING, Jeff ,  VEINBERG, Alex ,  YOUDIM, Moussa, B., H. ,  FINBERG, John, P., M. ,  SKLARZ, Benjamin ,  SAYAG, Naim

Inventor： TEVA PHARMACEUTICAL INDUSTRIES LTD. ,  TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD.

IPC: A61K31/495

CPC classification number: C07C237/04 ,  A61K31/135 ,  A61K31/137 ,  A61K31/165 ,  A61K31/166 ,  A61K31/167 ,  A61K31/18 ,  A61K31/195 ,  A61K31/215 ,  A61K31/216 ,  A61K31/24 ,  A61K31/27 ,  A61K31/275 ,  A61K31/277 ,  C07C209/88 ,  C07C211/42 ,  C07C213/10 ,  C07C215/44 ,  C07C217/74 ,  C07C233/06 ,  C07C233/23 ,  C07C233/74 ,  C07C2602/08 ,  C07C2602/10 ,  A61K2300/00

Abstract: Novel derivatives of 1-aminoindan and their salts are described. Parkinson's disease, dementia, epilepsy, convulsions, seizures, acute neurological traumatic disorder or neurotrauma are treated by administering a compound of formula (I).

Abstract translation: 描述了1-氨基茚满及其盐的新型衍生物。 通过施用式（I）化合物治疗帕金森病，痴呆，癫痫，抽搐，癫痫发作，急性神经外伤性疾病或神经损伤。

公开(公告)号：WO9637199A8

公开(公告)日：1999-08-12

申请号：PCT/US9607465

申请日：1996-05-22

Applicant: TEVA PHARMA ,  TECHNION RES & DEV FOUNDATION ,  YOUDIM MOUSSA B H ,  FINBERG JOHN P M ,  LEVY RUTH ,  STERLING JEFFREY ,  LERNER DAVID ,  YELLIN HAIM ,  VEINBERG ALEX

Inventor： YOUDIM MOUSSA B H ,  FINBERG JOHN P M ,  LEVY RUTH ,  STERLING JEFFREY ,  LERNER DAVID ,  YELLIN HAIM ,  VEINBERD ALEX

IPC: 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 classification number: C07C211/42 ,  A61K31/135 ,  A61K31/195 ,  A61K31/205 ,  A61K31/215 ,  A61K45/06 ,  C07C211/30 ,  C07C2602/08 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO1996037199A1

公开(公告)日：1996-11-28

申请号：PCT/US1996007465

申请日：1996-05-22

Applicant: TEVA PHARMACEUTICAL INDUSTRIES, INC. ,  TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD. ,  YOUDIM, Moussa, B., H. ,  FINBERG, John, P., M. ,  LEVY, Ruth ,  STERLING, Jeffrey ,  LERNER, David ,  YELLIN, Haim ,  VEINBERG, Alex

Inventor： TEVA PHARMACEUTICAL INDUSTRIES, INC. ,  TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD.

IPC: A61K31/135

CPC classification number: C07C211/42 ,  A61K31/135 ,  A61K31/195 ,  A61K31/205 ,  A61K31/215 ,  A61K45/06 ,  C07C211/30 ,  C07C2602/08 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO1997002027A1

公开(公告)日：1997-01-23

申请号：PCT/US1996011318

申请日：1996-07-05

Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD. ,  GILAD, Gad ,  GILAD, Varda ,  STERLING, Jeffrey ,  HERZIG, Yaacov ,  LERNER, David ,  VEINBERG, Alex ,  MILMAN, Isaac ,  FINKELSTEIN, Nina

Inventor： TEVA PHARMACEUTICAL INDUSTRIES, LTD.

IPC: A61K31/15

CPC classification number: C07C279/12 ,  A61K31/135 ,  A61K31/155 ,  C07C211/42 ,  C07C233/41 ,  C07C2602/24

Abstract: A compound of general formula (I), wherein n is 1 or 2; R1 and R2 are each independently hydrogen, hydroxy, substituted or unsubstituted C1-4 alkyl, substituted or unsubstituted C1-4 alkoxy or halogeno; R5 is hydrogen, substituted or unsubstituted C1-4 alkyl, amino or NR6R7; R3, R4, R6 and R7 are each independently hydrogen or (CH2)m-[NH(CH2)x]y-NHR11 wherein m is from 0-5, y is from 0-5 and each x is independently from 1-5 and R11 is hydrogen or C(NH)NH2; provided that when R3 and R4 are both hydrogen, R5 is amino or NR6R7; pharmaceutically acceptable salts and optically active isomers thereof.

Abstract translation: 通式（I）的化合物，其中n为1或2; R 1和R 2各自独立地为氢，羟基，取代或未取代的C 1-4烷基，取代或未取代的C 1-4烷氧基或卤素; R5是氢，取代或未取代的C1-4烷基，氨基或NR6R7; R3，R4，R6和R7各自独立地为氢或（CH2）m- [NH（CH2）x] y-NHR11，其中m为0-5，y为0-5，并且各x独立地为1-5 和R 11是氢或C（NH）NH 2; 条件是当R3和R4都是氢时，R5是氨基或NR6R7; 其药学上可接受的盐和旋光异构体。

公开(公告)号：WO1995011016A1

公开(公告)日：1995-04-27

申请号：PCT/US1994011567

申请日：1994-10-12

Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD. ,  TECHNION RESEARCH AND DEVELOPMENT FOUNDATION, LTD. ,  YOUDIM, Moussa, B., H. ,  FINBERG, John, P., M. ,  LEVY, Ruth ,  STERLING, Jeffrey ,  LERNER, David ,  BERGER-PASKIN, Tirtsah ,  YELLIN, Haim ,  VEINBERG, Alex

Inventor： TEVA PHARMACEUTICAL INDUSTRIES LTD. ,  TECHNION RESEARCH AND DEVELOPMENT FOUNDATION, LTD.

IPC: A61K31/135

CPC classification number: C07C211/30 ,  A61K31/195 ,  A61K31/215 ,  A61K45/06 ,  C07C2602/08 ,  Y02A50/395 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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。