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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

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。

3. 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。

4. 发明申请

WO1997040035A1 1-(4-PIPERIDYL)-BENZIMIDAZOLES HAVING NEUROTROPHIC ACTIVITY 审中-公开
标题翻译：具有神经营养活性的1-（4-哌啶基） - 苯并咪唑
公开(公告)号：WO1997040035A1
公开(公告)日：1997-10-30
申请号：PCT/EP1997002011
申请日：1997-04-21
申请人： NEUROSEARCH A/S , MOLDT, Peter , DAHL, Bjarne, Hugo , DREJER, Jorgen , AXELSSON, Oskar
发明人： NEUROSEARCH A/S
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The present invention discloses compounds of formula (I) wherein the dotted bonds are optional extra bonds allowing any tautomeric isomers compatible with substituents X and R ; R is non-existing, hydrogen, or alkyl; X is O, S, imino, alkoxy, alkylthio, or amino; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, acyl, acylalkyl, alkoxyalkyl, dialkoxyalkyl, or phenylalkyl which may be substituted with alkyl, halogen, amino, nitro or cyano; and R , R , R and R independently of each other are hydrogen, halogen, amino, nitro, CN, CF3, COOH, COO-alkyl, alkyl, acyl, alcoxy, -(CH2)n, -OH wherein n is 0, 1, 2 or 3; -(CH2)m-O-alkyl wherein m is 0, 1, 2 or 3; -(CH2)p-O-acyl wherein p is 0, 1, 2 or 3; or a pharmaceutically acceptable addition salt thereof. The compounds are useful as pharmaceuticals, for example, in the treatment of traumatic lesions of peripheral nerves, the medulla, and/or the spinal cord, cerebral ischaemic neuronal damage, neuropathy and especially peripheral neuropathy, dementia, Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, or any other neurodegenerative disease.
摘要翻译：本发明公开了式（I）的化合物，其中虚线键是任选的额外键，允许任何与取代基X和R 3相容的互变异构体; R 3不存在，氢或烷基; X是O，S，亚氨基，烷氧基，烷硫基或氨基; R 1是氢，烷基，烯基，炔基，环烷基，环烷基烷基，酰基，酰基烷基，烷氧基烷基，二烷氧基烷基或可被烷基，卤素，氨基，硝基或氰基取代的苯基烷基; R 4，R 5，R 6和R 7彼此独立地为氢，卤素，氨基，硝基，CN，CF 3，COOH，COO-烷基，烷基，酰基，烷氧基，（CH 2）n，-OH，其中n为0,1,2或3; - （CH 2）m -O-烷基，其中m为0,1,2或3; - （CH 2）p -O-酰基，其中p为0,1,2或3; 或其药学上可接受的加成盐。该化合物可用作药物，例如用于治疗周围神经，髓质和/或脊髓的创伤性损伤，脑缺血性神经元损伤，神经病变，特别是周围神经病变，痴呆，阿尔茨海默病，亨廷顿病，帕金森病疾病，肌萎缩性侧索硬化或任何其他神经变性疾病。

5. 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。

6. 发明申请

WO1996023420A1 ASTAXANTHIN SUSPENSION 审中-公开
标题翻译： ASTAXANTHIN暂停
公开(公告)号：WO1996023420A1
公开(公告)日：1996-08-08
申请号：PCT/EP1996000373
申请日：1996-01-30
申请人： NEUROSEARCH A/S , MOLDT, Peter
发明人： NEUROSEARCH A/S
IPC分类号： A23K01/16
CPC分类号： C07C403/24 , A23K20/179 , A23K50/80 , A23L5/44
摘要： A suspension of astaxanthin in oil and use thereof in the manufacture of feed for aquatic animals.
摘要翻译：虾青素在油中的悬浮液，并用于生产水生动物饲料。

7. 发明申请

WO1994022807A1 UREA AND AMIDE DERIVATIVES AND THEIR USE IN THE CONTROL OF CELL MEMBRANE POTASSIUM CHANNELS 审中-公开
标题翻译：尿素和酰胺衍生物及其在控制细胞膜蛋白通道中的用途
公开(公告)号：WO1994022807A1
公开(公告)日：1994-10-13
申请号：PCT/EP1994001008
申请日：1994-03-30
申请人： NEUROSEARCH A/S , OLESEN, Soren-Peter , MOLDT, Peter , PEDERSEN, Ove
发明人： NEUROSEARCH A/S
IPC分类号： C07C233/29
CPC分类号： C07D213/75 , A61K31/165 , A61K31/17 , A61K31/195 , A61K31/24 , A61K31/44 , C07C233/29 , C07C235/38 , C07C275/30 , C07C275/32 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C279/18 , C07C335/18
摘要： A compound having formula (I) or a pharmaceutically acceptable salt thereof, wherein X and Z each independently are NH or CH2, at least one of X and Z being NH; Y is O, S, NCN, or NH; B, D, E and F each independently are C or N, at least three of B, D, E, and F being C; and R , R , R , R , R , R have the meanings set forth in the specification, pharmaceutical compositions comprising the same, and a method of treating therewith. The compounds are useful as potassium channel openers.
摘要翻译：具有式（I）的化合物或其药学上可接受的盐，其中X和Z各自独立地为NH或CH 2，X和Z中的至少一个为NH; Y是O，S，NCN或NH; B，D，E和F各自独立地为C或N，B，D，E和F中的至少三个为C; 和R 1，R 2，R 3，R 4，R 11，R 12具有说明书中所述的含义，包含它们的药物组合物和治疗方法与之。这些化合物可用作钾通道开放剂。

8. 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。

9. 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。

10. 发明申请

WO1997045400A1 PHENYL DERIVATIVES CONTAINING AN ACIDIC GROUP, THEIR PREPARATION AND THEIR USE AS CHLORIDE CHANNEL BLOCKERS 审中-公开
标题翻译：含有酸性基团的苯甲衍生物，其制备及其作为氯离子通道阻断剂的使用
公开(公告)号：WO1997045400A1
公开(公告)日：1997-12-04
申请号：PCT/EP1997002723
申请日：1997-05-26
申请人： NEUROSEARCH A/S , CHRISTOPHERSEN, Palle , PEDERSEN, Ove
发明人： NEUROSEARCH A/S
IPC分类号： C07C275/42
CPC分类号： C07C311/47 , A61K31/155 , A61K31/17 , C07C233/55 , C07C271/58 , C07C275/40 , C07C275/42 , C07C309/51 , C07C311/08 , C07C311/21 , C07C311/60 , C07C335/22
摘要： The present patent application relates to compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein one of R , R and R is a non-cyclic acidic group having a pKa value below 8 or a group which is in vivo convertible to such a group; R , R and the other two of the substituents R , R and R are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, and aryl, aralkyl, arylamino, aryloxy, aryl-CO-, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or R and R or R and R together form a fused 4- to 7-membered carbocyclic ring which may be unsaturated, or partially or fully saturated, while the other substituents R , R , R , R and R are as defined above; Y is -CO-, -CS-, -SO2-, or -C(=N-R )-, wherein R is hydrogen, alkyl, or cyano; X is -NH-, -CH2-NH-, or -SO2-NH-; Z is NR , O, -CH=CH-, -C=C-, -N=CH-, or -CH=N-; wherein R is hydrogen, or alkyl; R , R , R , R and R are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, -NHSO2-R , -COOR , -SO2N(R )2, -SO2OR and -CO-R , wherein R is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl or aralkyl; and aryl, aralkyl, arylamino, aryloxy, aryl-CO-, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or one of R and R , R and R , R and R or R and R together form a fused 4- to 7-membered carbocyclic ring which may be unsaturated, or partially or fully saturated, while the other substituents R , R , R , R and R are as defined above. The compounds are useful for the treatment of diseases and disorders responsive to the blockage of chloride channels.
摘要翻译：本发明涉及具有式（I）化合物或其药学上可接受的盐，其中R 1，R 2和R 3之一是pKa值低于8的非环状酸性基团或可体内转化为该组的组; R 4，R 5和另外两个取代基R 1，R 2和R 3各自独立地选自氢，烷基，环烷基，环烷基烷基，烯基，炔基，烷氧基，羟基，卤素，三氟甲基，三氟甲氧基，氰基，硝基，氨基和芳基，芳烷基，芳基氨基，芳氧基，芳基-CO-或杂芳基，其中芳基和杂芳基可以被取代基取代一次或多次，，环烷基烷基，烯基，炔基，羟基，烷氧基，卤素，三氟甲基，三氟甲氧基，氰基，硝基和氨基; 或R 3和R 4或R 4和R 5一起形成稠合的4-至7-元碳环，其可以是不饱和的或部分或完全饱和的，而其它取代基R 1 R 2，R 3，R 4和R 5如上定义; Y是-CO - ， - CS-，-SO 2 - 或-C（= N-R 8） - ，其中R 8是氢，烷基或氰基; X是-NH-，-CH 2 -NH-或-SO 2 -NH-; Z是NR 6，O，-CH = CH-，-C = C-，-N = CH-或-CH = N-; 其中R 6是氢或烷基; R 11，R 12，R 13，R 14和R 15各自独立地选自氢，烷基，环烷基，环烷基烷基，烯基，炔基，烷氧基，羟基，卤素，三氟甲基，三氟甲氧基，氰基，硝基，氨基，-NHSO 2 -R 7，-COOR 7，-SO 2 N（R 7）2，-SO 2 OR 7和-CO-R 7，其中R 7，是氢，烷基，环烷基，环烷基烷基，烯基，炔基，芳基或芳烷基; 芳基，芳烷基，芳基氨基，芳氧基，芳基-CO-或杂芳基，其中芳基和杂芳基可以被选自烷基，环烷基，环烷基烷基，烯基，炔基，羟基，烷氧基，卤素，三氟甲基，三氟甲氧基，氰基，硝基和氨基; 或R 11和R 12之一，R 12和R 13，R 13和R 14或R 14和R 15一起形成稠合的4-至7 其中R 11，R 12，R 13，R 14和R 15如上所定义，其可以是不饱和的，或部分或完全饱和的。该化合物可用于治疗对氯通道阻塞作出反应的疾病和病症。

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