公开(公告)号：WO1994013656A1

公开(公告)日：1994-06-23

申请号：PCT/GB1993002512

申请日：1993-12-08

Applicant: SMITHKLINE BEECHAM PLC ,  SMITHKLINE BEECHAM CORPORATION ,  THOMPSON, Mervyn ,  EVANS, John, Morris ,  UPTON, Neil ,  CHAN, Wai, Ngor ,  VONG, Kuok, Keong ,  WILLETTE, Robert, Nicholas

Inventor： SMITHKLINE BEECHAM PLC ,  SMITHKLINE BEECHAM CORPORATION

IPC: C07D311/68

CPC classification number: C07D405/12 ,  C07D311/68 ,  C07D407/12 ,  C07D409/12

Abstract: A method of treatment and/or prophylaxis of disorders resulting from subarachnoid haemorrhage, neural shock, cerebral ischaemia, Parkinson's Disease, migraine and/or psychosis, in mammals, especially humans which comprises administering to the sufferer in need thereof an effective or prophylactic amount of a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein either Y is N and R2 is hydrogen, or Y is C-R1 where either one of R1 and R2 is hydrogen and the other is selected from the class of hydrogen, C3-8 cycloalkyl, C1-6 alkyl optionally interrupted by oxygen or substituted by hydroxy, C1-6 alkoxy or substituted aminocarbonyl, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkoxy, nitro, cyano, halo, trifluoromethyl, CF3S, or a group CF3-A-, or a group CF2H-A'-; trifluoromethoxy, C1-6 alkylsulphinyl, perfluoro C2-6 alkylsulphonyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 alkoxysulphonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, phosphono, arylcarbonyloxy, heteroarylcarbonyloxy, arylsulphinyl, heteroarylsulphinyl, arylsulphonyl, heteroarylsulphonyl in which any aromatic moiety is optionally substituted, C1-6 alkylcarbonylamino, C1-6 alkoxycarbonylamino, C1-6 alkyl-thiocarbonyl, C1-6 alkoxy-thiocarbonyl, C1-6 alkyl-thiocarbonyloxy, 1-mercapto C2-7 alkyl, formyl, or aminosulphinyl, aminosulphonyl or aminocarbonyl, any amino moiety being optionally substituted by one or two C1-6 alkyl groups, or C1-6 alkylsulphinylamino, C1-6 alkylsulphonylamino, C1-6 alkoxysulphinylamino or C1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C1-6 alkylcarbonyl, nitro or cyano, or -C(C1-6 alkyl)NOH or -C(C1-6 alkyl)NNH2, or one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is methoxy or amino group; or R1 and R2 together are -(CH2)4- or -CH CH-CH CH-, or form an optionally substituted triazole or oxadiazole ring; and X is oxygen or NR10.

Abstract translation: 一种治疗和/或预防哺乳动物，特别是人的蛛网膜下腔出血，神经性休克，脑局部缺血，帕金森病，偏头痛和/或精神病引起的疾病的方法，包括向有需要的患者施用有效或预防量的 式（I）化合物或其药学上可接受的盐，其中Y为N且R 2为氢，或Y为C-R 1，其中R 1和R 2中的任一个为氢，另一个选自氢，C 3 -8环烷基，任选被氧中断或被羟基取代的C 1-6烷基，C 1-6烷氧基或取代的氨基羰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰氧基，C 1-6烷氧基，硝基，氰基，卤素 ，三氟甲基，CF 3 S或CF 3 -A-或CF 2 H-A'-基团; 三氟甲氧基，C 1-6烷基亚磺酰基，全氟C 2-6烷基磺酰基，C 1-6烷基磺酰基，C 1-6烷氧基亚磺酰基，C 1-6烷氧基磺酰基，芳基，杂芳基，芳基羰基，杂芳基羰基，膦酰基，芳基羰基氧基，杂芳基羰氧基，芳基亚磺酰基，杂芳基亚磺酰基，芳基磺酰基，杂芳基磺酰基 任何芳族部分任选被取代，C 1-6烷基羰基氨基，C 1-6烷氧基羰基氨基，C 1-6烷基 - 硫代羰基，C 1-6烷氧基 - 硫代羰基，C 1-6烷基 - 硫代羰基氧基，1-巯基C 2-7烷基，甲酰基或 氨基亚磺酰基，氨基磺酰基或氨基羰基，任选被一个或两个C 1-6烷基取代的氨基部分，或C 1-6烷基亚磺酰氨基，C 1-6烷基磺酰基氨基，C 1-6烷氧基亚磺酰氨基或C 1-6烷氧基磺酰基氨基，或被C 1 -C 6末端取代的亚乙基， 6烷基羰基，硝基或氰基或-C（C 1-6烷基）NOH或-C（C 1-6烷基）NNH 2，或R 1和R 2之一是硝基，氰基或C 1-3烷基羰基，另一个是甲氧基或氨基 组; 或者R 1和R 2一起是 - （CH 2）4 - 或-CH 3 CH-CH，或形成任选取代的三唑或恶二唑环; X是氧或NR 10。

公开(公告)号：WO1994013292A1

公开(公告)日：1994-06-23

申请号：PCT/GB1993002514

申请日：1993-12-08

Applicant: SMITHKLINE BEECHAM PLC ,  SMITHKLINE BEECHAM CORPORATION ,  VONG, Kuok, Keong ,  EVANS, John, Morris ,  NADLER, Guy, Marguerite, Marie, Gérard ,  WILLETTE, Robert, Nicholas

Inventor： SMITHKLINE BEECHAM PLC ,  SMITHKLINE BEECHAM CORPORATION

IPC: A61K31/47

CPC classification number: A61K31/335 ,  A61K31/00 ,  A61K31/275 ,  A61K31/38

Abstract: A method of treatment and/or prophylaxis of anxiety, mania, depression, the effects associated with withdrawal from substances of abuse such as cocaine, nicotine, alcohol and benzodiazepines; disorders treatable and/or preventable with anticonvulsive agents, such as epilepsy; and in the treatment or prevention of cerebral ischaemia, disorders resulting from sub-arachnoid haemorrhage, Parkinson's disease, migraine and/or psychosis, comprising administering to the sufferer in need thereof an effective or prophylactic amount of a potassium channel activator.

Abstract translation: 治疗和/或预防焦虑症，躁狂症，抑郁症，与可卡因，尼古丁，酒精和苯并二氮杂类药物滥用物质相关的作用的方法; 可用抗惊厥药治疗和/或预防的疾病如癫痫; 以及治疗或预防脑缺血，由蛛网膜下出血，帕金森病，偏头痛和/或精神病引起的疾病，包括向有需要的患者施用有效或预防量的钾通道活化剂。

公开(公告)号：WO1994013297A1

公开(公告)日：1994-06-23

申请号：PCT/GB1993002515

申请日：1993-12-08

Applicant: SMITHKLINE BEECHAM PLC . ,  SMITHKLINE BEECHAM CORPORATION ,  EVANS, John, Morris ,  VONG, Kuok, Keong ,  WILLETTE, Robert, Nicholas

Inventor： SMITHKLINE BEECHAM PLC . ,  SMITHKLINE BEECHAM CORPORATION

IPC: A61K31/535

CPC classification number: A61K31/47 ,  A61K31/00 ,  A61K31/40 ,  A61K31/475 ,  A61K31/535

Abstract: A method of treatment and/or prophylaxis of anxiety, mania, depression, the effects associated with withdrawal from substances of abuse such as cocaine, nicotine, alcohol and benzodiazepines; disorders treatable and/or preventable with anti-convulsive agents, such as epilepsy; and in the treatment or prevention of cerebral ischaemia, disorders resulting from sub-arrachnoid haemorrhage, Parkinson's disease, migraine and/or psychosis, comprising administering to the sufferer in need thereof an effective or prophylactic amount of a potassium channel activator.

Abstract translation: 治疗和/或预防焦虑症，躁狂症，抑郁症，与可卡因，尼古丁，酒精和苯并二氮杂类药物滥用物质相关的作用的方法; 可用抗惊厥药治疗和/或预防的疾病如癫痫; 以及治疗或预防脑缺血，由蛛网膜下腔出血，帕金森病，偏头痛和/或精神病引起的疾病，包括向有需要的患者施用有效或预防量的钾通道活化剂。