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1. 发明申请

WO1997030997A1 TROPANE-DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译： TROPANE-DERIVATIVES，他们的准备和使用
公开(公告)号：WO1997030997A1
公开(公告)日：1997-08-28
申请号：PCT/EP1997000850
申请日：1997-02-21
申请人： NEUROSEARCH A/S , SCHEEL-KRÜGER, Jorgen , MOLDT, Peter , WÄTJEN, Frank
发明人： NEUROSEARCH A/S
IPC分类号： C07D451/02
CPC分类号： C07D451/02 , C07D451/00
摘要： The present invention discloses compounds of formula (a), (b), (c) or (d), or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R is -CH2-X-R', wherein X is O, S or NR", wherein R" is hydrogen, or alkyl and R' is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, or -CO-alkyl; R is phenyl which may be substitued one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; 3,4-methylenedioxyphenyl; benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; heteroaryl which may be substitued one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; or naphthyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl. The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter, i.e. dopamine, serotonin, noradrenaline, reuptake inhibitors.
摘要翻译：本发明公开了式（a），（b），（c）或（d）的化合物或其任何混合物或其药学上可接受的盐; 其中R是氢，烷基，烯基，炔基，环烷基，环烷基烷基或2-羟乙基; R 3是-CH 2 -X-R'，其中X是O，S或NR“，其中R”是氢或烷基，R'是烷基，烯基，炔基，环烷基，环烷基烷基或-CO-烷基 ; R 4是可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的苯基; 3,4-亚甲二氧苯基; 可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的苄基。可以用选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的杂芳基; 或萘基，其可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次。该化合物具有作为单胺神经递质（即多巴胺，5-羟色胺，去甲肾上腺素，再摄取抑制剂）的有价值的药物性质。

2. 发明申请

WO1995028401A1 TROPANE-2-ALDOXINE DERIVATIVES AS NEUROTRANSMITTER REUPTAKE INHIBITORS 审中-公开
标题翻译： TROPANE-2-ALDOXINE DERIVATIVES作为神经递质回收抑制剂
公开(公告)号：WO1995028401A1
公开(公告)日：1995-10-26
申请号：PCT/EP1995001358
申请日：1995-04-12
申请人： NEUROSEARCH A/S , MOLDT, Peter , WÄTJEN, Frank , SCHEEL-KRÜGER, Jorgen
发明人： NEUROSEARCH A/S
IPC分类号： C07D451/02
CPC分类号： C07D451/02
摘要： The present invention discloses compounds of formula (I), (II), (III) or (IV) any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R is CH=NOR', wherein R' is hydrogen or alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, or alkyl all of which may be substituted with COOH, COO-alkyl, COO-cycloalkyl, or phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro; and R is phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; 3,4-methylenedioxyphenyl; benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; heteroaryl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; or naphthyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl. The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter, i.e. dopamine, serotonine, noradrenaline, reuptake inhibitors.
摘要翻译：本发明公开了式（I），（II），（III）或（IV）的任何混合物或其药学上可接受的盐的化合物; 其中R是氢，烷基，烯基，炔基，环烷基，环烷基烷基或2-羟乙基; R 3是CH = NOR'，其中R'是氢或烯基，炔基，环烷基，环烷基烷基，芳基或烷基，其全部可以被COOH，COO-烷基，COO-环烷基或苯基取代，用选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基的取代基取代一次或多次。和R 4是可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的苯基; 3,4-亚甲二氧苯基; 可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的苄基。可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的杂芳基; 或萘基，其可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次。该化合物具有作为单胺神经递质（即多巴胺，5-羟色胺，去甲肾上腺素，再摄取抑制剂）的有价值的药物性质。

3. 发明申请

WO1997013770A1 8-AZABICYCLO[3.2.1]OCT-2-ENE DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译： 8-AZABICYCLO [3.2.1] OCT-2-ENE衍生物，其制备和使用
公开(公告)号：WO1997013770A1
公开(公告)日：1997-04-17
申请号：PCT/EP1996004449
申请日：1996-10-11
申请人： NEUROSEARCH A/S , MOLDT, Peter , SCHEEL-KRÜGER, Jorgen , OLSEN, Gunnar, M. , NIELSEN, Elsebet, Ostergaard
发明人： NEUROSEARCH A/S
IPC分类号： C07D451/06
CPC分类号： C07D451/02 , C07D451/06
摘要： A compound having formula (I) or any of its enantiomers of any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; and R is phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; 3,4-methylenedioxyphenyl; benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; heteroaryl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; or naphtyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl. The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter re-uptake inhibitors.
摘要翻译：具有式（I）的化合物或其任何混合物的任何对映异构体或其药学上可接受的盐; 其中R是氢，烷基，烯基，炔基，环烷基，环烷基烷基或2-羟乙基; 和R 4是可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的苯基; 3,4-亚甲二氧苯基; 可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的苄基。可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的杂芳基; 或可以被选自卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基和芳基的取代基取代一次或多次的萘基。该化合物具有作为单胺神经递质再摄取抑制剂的有价值的药物性质。

4. 发明申请

WO1996008494A1 INDOLE-2,3-DIONE-3-OXIME DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译：吲哚-2,3-二酮-3-氧化物衍生物，其制备和使用
公开(公告)号：WO1996008494A1
公开(公告)日：1996-03-21
申请号：PCT/EP1995003593
申请日：1995-09-12
申请人： NEUROSEARCH A/S , MOLDT, Peter , WÄTJEN, Frank
发明人： NEUROSEARCH A/S
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R , X and R have the meanings set further in the specification. A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders for example.
摘要翻译：本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中R 1，X和R 5具有在说明书中进一步设定的含义。 A是在标记a和b的位置与苯环稠合的5至7个原子的环。该化合物可用于治疗例如脑血管障碍。

5. 发明申请

WO1996008495A1 FUSED INDOLE AND QUINOXALINE DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译：熔融的吲哚和喹啉衍生物，其制备和使用
公开(公告)号：WO1996008495A1
公开(公告)日：1996-03-21
申请号：PCT/EP1995003594
申请日：1995-09-12
申请人： NEUROSEARCH A/S , MOLDT, Peter , WÄTJEN, Frank
发明人： NEUROSEARCH A/S
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein: R is hydrogen, alkyl or benzyl; X is O or NOR , wherein R is hydgrogen, alkyl or benzyl; Y is N-R wherein R is hydrogen, OH or alkyl; n is 0 or 1; R is phenyl which is substituted one or more times with substituents selected from the group consisting of SO2NR'R", CONR'R", and COR''' wherein R' and R" each independently are hydrogen, alkyl, or -(CH2)p-W, wherein p is 0, 1, 2, 3, 4, 5, or 6, and W is hydroxy, amino, alkoxycarbonyl, or phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, NO2, amino, alkyl, alkoxy or methylenedioxy; or wherein R' and R" together are (CH2)rZ(CH2)s wherein r and s each independently are 0, 1, 2, 3, 4, 5, or 6 and Z is O, S, CH2 or NR"" wherein R"" is hydrogen, alkyl, or -(CH2)p-W, wherein p is 0, 1, 2, 3, 4, 5, or 6, and W is hydroxy, amino, alkoxycarbonyl, or phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, NO2, amino, alkyl, alkoxy or methylenedioxy; and wherein R''' is hydrogen, alkyl, alkoxy or phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, NO2, amino, alkyl, alkoxy or methylenedioxy; A is a ring of fixe to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders for example.
摘要翻译：本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中：R 1是氢，烷基或苄基; X是O或NOR 2，其中R 2是氢原子，烷基或苄基; Y是N-R 4，其中R 4是氢，OH或烷基; n为0或1; R 6是被选自SO 2 NR'R“，CONR'R”和COR“的取代基一次或多次的苯基，其中R'和R”各自独立地是氢，烷基或 - （CH 2）p W，其中p是0,1,2,3,4,5或6，并且W是羟基，氨基，烷氧基羰基或苯基，其可以被选自以下的取代基取代一次或多次：卤素，CF 3，NO 2，氨基，烷基，烷氧基或亚甲二氧基;或其中R'和R“一起为（CH 2）rZ（CH 2）s，其中r和s各自独立地为0,1,2,3,4,5 ，或6和Z是O，S，CH 2或NR“”，其中R“”是氢，烷基或 - （CH 2）pW，其中p是0,1,2,3,4,5或6，和 W是可以被选自卤素，CF 3，NO 2，氨基，烷基，烷氧基或亚甲二氧基的取代基取代一次或多次的羟基，氨基，烷氧基羰基或苯基。并且其中R“是氢，烷基，烷氧基或苯基，其可以被选自卤素，CF 3，NO 2，氨基，烷基，烷氧基或亚甲二氧基的取代基取代一次或多次; A是在标记a和b的位置处与苯环稠合的七个原子的固定环。该化合物可用于治疗例如脑血管障碍。

6. 发明申请

WO1998007710A1 DISUBSTITUTED MORPHOLINE, OXAZEPINE OR THIAZEPINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS DOPAMINE D4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：分析的吗啉，氧化氮或噻吩衍生物，其制备及其作为DOPAMINE D4受体拮抗剂的用途
公开(公告)号：WO1998007710A1
公开(公告)日：1998-02-26
申请号：PCT/EP1997004587
申请日：1997-08-22
申请人： NEUROSEARCH A/S , AXELSSON, Oskar , PETERS, Dan , SCHEEL-KRÜGER, Jorgen , OSTERGAARD NIELSEN, Elsebet
发明人： NEUROSEARCH A/S
IPC分类号： C07D265/30
CPC分类号： C07D265/30 , C07D267/10 , C07D413/06
摘要： The present invention relates to compounds of formula (I), any of its enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R , R , R , R , R , R , R , R , and R each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is -CH2-Z-, -Z-CH2-, -NH-CO-, -CO-NH-, or -CH=CH-; wherein Z is O, S, CH2 or NH; Y is O, -CH2-W-, -W-CH2-; wherein W is O, or S; and n is 0, 1, or 2. The compounds are useful in the treatment of psychotic disorders.
摘要翻译：本发明涉及式（I）化合物，其任何对映体或其任何混合物或其药学上可接受的酸加成盐，其中R 1，R 2，R 3，R 4 R 11，R 12，R 13，R 14和R 15各自独立地为氢，烷基，烷氧基，卤素，三氟甲基，硝基，氰基，氨基，酰基，烷基氨基，二烷基氨基，氨基羰基或酰氨基; R 5是氢，烷基，烷氧基烷基或苯基烷基; X是-CH 2 -Z-，-Z-CH 2 - ，-NH-CO-，-CO-NH-或-CH = CH-; 其中Z是O，S，CH 2或NH; Y是O，-CH 2 -W-，-W-CH 2 - ; 其中W是O或S; 并且n为0,1或2.该化合物可用于治疗精神病性疾病。

7. 发明申请

WO1997016451A1 FUSED TROPANE-DERIVATIVES AS NEUROTRANSMITTER REUPTAKE INHIBITORS 审中-公开
标题翻译：作为神经递质回收抑制剂的融合的衍生物
公开(公告)号：WO1997016451A1
公开(公告)日：1997-05-09
申请号：PCT/EP1996004793
申请日：1996-11-04
申请人： NEUROSEARCH A/S , SCHEEL-KRÜGER, Jorgen , OLSEN, Gunnar, M. , NIELSEN, Elsebet, Ostergaard , DAHL, Bjarne, Hugo , JENSEN, Leif, Helth
发明人： NEUROSEARCH A/S
IPC分类号： C07D471/18
CPC分类号： C07D471/18
摘要： The present invention discloses compound of formula (I) or any of its enantiomers or any mixture thereof, a pharmaceutically acceptable addition salt thereof or the N-oxide thereof wherein X and Y together form =O, =S, =NOR , =CR R , =N-CN, =N-NR R , -(CH2)m-, or -W'-(CH2)p-W"-, or one of X and Y is hydrogen and the other is -OR , -SR , or -NR R , Z is hydrogen, -COOR ; R and R are independently hydrogen, halogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alcoxy, aryl, arylalkyl, or -(CH2)q-COOR ; R , R and R are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl, -CO-alkyl, or -SO2-alkyl; R and R are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl or arylalkyl; R is alkyl, alkenyl or alkynyl; R is alkyl, alkenyl, alkynyl, aryl, or arylalkyl; where said aryl groups may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino and nitro; W' and W" are each independently O or S; n is 1, 2, 3 or 4; m is 2, 3, 4 or 5; p is 1, 2, 3, 4, or 5; and q is 0, 1, 2, 3, or 4. The compounds possess valuable properties as monoamine neurotransmitter, i.e dopamine, and serotonine, reuptake inhibitors.
摘要翻译：本发明公开了式（I）化合物或其任何对映体或其任何混合物，其药学上可接受的加成盐或其N-氧化物，其中X和Y一起形成= O，= S，= NOR 2， = CR 3 R 4，= N-CN，= N-NR 7 R 8， - （CH 2）m - 或-W' - （CH 2）p W“ 并且Y是氢，另一个是-OR 5，-SR 5或-NR 5 R 6，Z是氢，-COOR 9; R 3和R 4，独立地是氢，卤素，烷基，环烷基，环烷基烷基，烯基，炔基，烷氧基，芳基，芳基烷基或 - （CH 2）q -COOR 2; R 2，R 5和R 6独立地是氢，烷基，环烷基，环烷基烷基，烯基，炔基，芳基或芳烷基，-CO-烷基或-SO2-烷基; R 7和R 8独立地为氢，烷基，环烷基，环烷基烷基，烯基，炔基，芳基或芳基烷基; R 9是烷基，烯基或炔基; R 1是烷基，烯基，炔基，芳基或芳烷基;其中所述芳基可以被取代基选自以下基团：卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基和硝基的取代基; W'和W“各自独立地为O或S; n为1,2,3或4; m为2,3,4或5; p为1,2,3,4或5; q为0，该化合物具有作为单胺神经递质（即多巴胺和5-羟色胺）再摄取抑制剂的有价值的性质。

8. 发明申请

WO1996033192A1 BENZIMIDAZOLE COMPOUNDS AND THEIR USE AS MODULATORS OF THE GABAA RECEPTOR COMPLEX 审中-公开
标题翻译：苯并咪唑化合物及其作为GABAA受体复合物的调节剂
公开(公告)号：WO1996033192A1
公开(公告)日：1996-10-24
申请号：PCT/EP1996001654
申请日：1996-04-19
申请人： NEUROSEARCH A/S , MEIJI SEIKA KAISHA, Ltd. , TEUBER, Lene , WÄTJEN, Frank
发明人： NEUROSEARCH A/S , MEIJI SEIKA KAISHA, Ltd.
IPC分类号： C07D401/14
CPC分类号： C07D235/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/10 , C07D403/10 , C07D405/10 , C07D405/14 , C07D409/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof or an oxide thereof wherein R is formula (II), wherein A, B and D each is CH, or one or two of A, B and D is N and the others are CH; R is phenyl, benzimidazolyl, or monocyclic heteroaryl all of which may be substituted one or more times with substituents selected from alkyl, halogen, CF3, amino, nitro, cyano, acylamino, alkoxy, acyl, phenyl, and monocyclic heteroaryl, and one of R and R is hydrogen and the other is pyrrolyl which may be substituted one or more times with substituents selected from halogen, alkyl, phenyl, and alkoxy. The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.
摘要翻译：本专利申请公开了具有式（I）化合物或其药学上可接受的盐或其氧化物，其中R 3为式（II），其中A，B和D各自为CH，或A，B中的一种或两种 D为N，其余为CH; R 11是苯基，苯并咪唑基或单环杂芳基，其全部可以被选自烷基，卤素，CF 3，氨基，硝基，氰基，酰氨基，烷氧基，酰基，苯基和单环杂芳基的取代基取代一次或多次。 R 6和R 7中的一个是氢，另一个是可以被选自卤素，烷基，苯基和烷氧基的取代基取代一次或多次的吡咯基。该化合物可用于治疗各种中枢神经系统疾病如癫痫和其他惊厥性疾病，焦虑症，睡眠障碍和记忆障碍。

9. 发明申请

WO1994026747A1 AMPA ANTAGONISTS AND A METHOD OF TREATMENT THEREWITH 审中-公开
标题翻译： AMPA拮抗剂及其治疗方法
公开(公告)号：WO1994026747A1
公开(公告)日：1994-11-24
申请号：PCT/EP1994001492
申请日：1994-05-09
申请人： NEUROSEARCH A/S , WÄTJEN, Frank , DREJER, Jorgen
发明人： NEUROSEARCH A/S
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R is hydrogen, alkyl or benzyl; X is O or NOR , wherein R is hydrogen, alkyl or benzyl; Y is N-R wherein R is hydrogen, OH or alkyl; n is 0 or 1; R is phenyl, naphthyl, thienyl, pyridyl, all of which may be substituted one or more times with substituents selected from the group consisting of halogen; CF3, NO2, amino, alkyl, alkoxy and phenyl; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders for example.
摘要翻译：本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中R 1是氢，烷基或苄基; X是O或NOR 2，其中R 2是氢，烷基或苄基; Y是N-R 4，其中R 4是氢，OH或烷基; n为0或1; R 6是苯基，萘基，噻吩基，吡啶基，它们都可以被选自卤素的取代基取代一次或多次; CF 3，NO 2，氨基，烷基，烷氧基和苯基; A是在标记a和b的位置与苯环稠合的5至7个原子的环。该化合物可用于治疗例如脑血管障碍。

10. 发明申请

WO1996030371A1 METHOD FOR THE PREPARATION OF ESTERS OF ANHYDROECGONINE 审中-公开
标题翻译：制备无机盐的方法
公开(公告)号：WO1996030371A1
公开(公告)日：1996-10-03
申请号：PCT/EP1996001277
申请日：1996-03-22
申请人： NEUROSEARCH A/S , MOLDT, Peter
发明人： NEUROSEARCH A/S
IPC分类号： C07D451/02
CPC分类号： C07D451/02
摘要： A process for the preparation of esters of anhydroecgonine having formula (I), any of its enantiomers or any mixture thereof, or a salt thereof, wherein R is alkyl, or optionally substituted aryl, or arylalkyl; comprising the step of reacting a compound of formula (II), any of its enantiomers or any mixture thereof, or a salt thereof, wherein R is hydrogen, alkyl-CO-, or optionally substituted aryl-CO-, or arylalkyl-CO-; with an alcoholate RO , M wherein R is as defined above and M is a counter ion, followed by isolation of the resulting compound either as the base or, if desired, in the form of a salt thereof.
摘要翻译：一种制备具有式（I）的脱氢莽吉因酯，其任何对映异构体或其任何混合物或其盐的方法，其中R为烷基或任选取代的芳基或芳基烷基; 包括使式（II）化合物，其任何对映体或其任何混合物或其盐反应的步骤，其中R 1是氢，烷基-CO-或任选取代的芳基-CO-或芳基烷基 -CO-; 其中R为如上定义的并且M +为抗衡离子，随后分离所得化合物作为碱或如果需要，以盐的形式分离它们。

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