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。

公开(公告)号：WO1992022293A1

公开(公告)日：1992-12-23

申请号：PCT/GB1992001045

申请日：1992-06-11

Applicant: SMITHKLINE BEECHAM P.L.C. ,  EVANS, John, Morris ,  THOMPSON, Mervyn ,  UPTON, Neil

Inventor： SMITHKLINE BEECHAM P.L.C.

IPC: A61K31/35

CPC classification number: C07D491/04 ,  C07D215/48 ,  C07D311/68 ,  C07D311/70 ,  C07D311/72

Abstract: A method of treatment and/or prophylaxis of anxiety and/or mania, and/or depression and/or the effects associated with withdrawal from substances of abuse, and/or disorders treatable and/or preventable with anticonvulsive agents, comprising 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-, where A is -CF2-, -CO-, -CH2- or CH(OH), trifluoromethoxy, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 alkoxysulphonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, 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 optionally substituted by one or two C1-6 alkyl or by C2-7 alkanoyl; one or R3 and R4 is hydrogen or C1-4 alkyl and the other is C1-4 alkyl or R3 and R4 together are C2-5 polymethylene; R5 is C1-6 alkylcarbonyloxy, benzoyloxy, ONO2, benzyloxy, phenyloxy or C1-6 alkoxy and R6 and R9 are hydrogen or R5 is hydroxy and R6 is hydrogen or C1-2 alkyl and R9 is hydrogen; R7 is fluorophenyl; R8 is hydrogen or C1-6 alkyl; the R8-N-CO-R7 group being trans to the R5 group; and X is oxygen or NR10 where R10 is hydrogen or C1-6 alkyl.

Abstract translation: 治疗和/或预防焦虑和/或躁狂症和/或抑郁症和/或与滥用物质的戒断有关的作用的方法，和/或可用抗惊厥药治疗和/或预防的病症的方法，包括对患者施用 需要其有效或预防量的式（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，并且 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烷基羰基氧基， C 1-6烷氧基，硝基，氰基，卤素，三氟甲基，CF 3 S或基团CF 3 -A，其中A是-CF 2 - ， - CO - ， - CH 2 - 或CH（OH），三氟甲氧基，C 1-6烷基亚磺酰基， 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，杂环 芳基羰基，芳基亚磺酰基，杂芳基亚磺酰基，芳基磺酰基，芳基部分任选取代的杂芳基磺酰基，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， - 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烷氧基亚磺酰基氨基或C 1-6烷基磺酰基氨基， 6个烷氧基磺酰基氨基或被C 1-6烷基羰基，硝基或氰基末端取代的亚乙基，或-C（C 1-6烷基）NOH或-C（C 1-6烷基）NNH 2，或者R 1和R 2之一是硝基，氰基或C 1 -3烷基羰基，另一个是任选被一个或两个C 1-6烷基或C 2-7烷酰基取代的甲氧基或氨基; 一个或R 3和R 4是氢或C 1-4烷基，而另一个是C 1-4烷基或者R 3和R 4一起是C 2-5的聚亚甲基; R5是C1-6烷基羰基氧基，苯甲酰氧基，ONO2，苄氧基，苯氧基或C1-6烷氧基，R6和R9是氢或R5是羟基，R6是氢或C1-2烷基，R9是氢; R7是氟苯基; R8是氢或C1-6烷基; R8-N-CO-R7基团转变为R5基团; 并且X是氧或NR 10，其中R 10是氢或C 1-6烷基。

公开(公告)号：WO1991009031A1

公开(公告)日：1991-06-27

申请号：PCT/GB1990001935

申请日：1990-12-11

Applicant: BEECHAM GROUP P.L.C. ,  EVANS, John, Morris ,  STEMP, Geoffrey ,  TEDDER, John, Martin

Inventor： BEECHAM GROUP P.L.C.

IPC: C07D405/04

CPC classification number: C07D405/04 ,  C07D311/22 ,  C07D311/58 ,  C07D311/68 ,  C07D493/04

Abstract: A compound of formula (I) or, where appropriate, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein A1, A2, A3, A4, R1, R2, R3, R4 and Y are as defined herein; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound and composition in medicine.

Abstract translation: 式（I）化合物或其合适的药学上可接受的盐或其药学上可接受的溶剂合物，其中A1，A2，A3，A4，R1，R2，R3，R4和Y如本文所定义; 制备这种化合物的方法，含有这种化合物的药物组合物以及这种化合物和组合物在医药中的用途。

公开(公告)号：WO1985000602A1

公开(公告)日：1985-02-14

申请号：PCT/GB1984000252

申请日：1984-07-18

Applicant: BEECHAM GROUP P.L.C. ,  EVANS, John, Morris ,  STEMP, Geoffrey

Inventor： BEECHAM GROUP P.L.C.

IPC: C07D401/04

CPC classification number: C07D215/233 ,  C07D215/18 ,  C07D401/04 ,  C07D491/04

Abstract: Compounds of formula (I), wherein: n is 1 or 2; R1 is chloro, bromo, C1-6 alkylcarbonyl or cyano; one of R3 and R4 is hydrogen or C1-4 alkyl and the other is C1-4 alkyl or R3 and R4 together are C2-5 polymethylene; and either; R5 is hydroxy, C1-3 alkoxy or C1-8 acyloxy; and R2 is hydrogen and the cyclic amide moiety and R5 are trans; or R5 and R2 together form a bond; having anti-hypertensive activity, and process for their preparation and their use as pharmaceuticals.

Abstract translation: 式（I）的化合物，其中：n为1或2; R1是氯，溴，C1-6烷基羰基或氰基; R3和R4之一是氢或C1-4烷基，另一个是C1-4烷基或R3和R4一起是C2-5聚亚甲基; 和 R5是羟基，C1-3烷氧基或C1-8酰氧基; 并且R 2是氢，环酰胺部分和R 5是反式; 或R 5和R 2一起形成键; 具有抗高血压活性，其制备方法及其作为药物的用途。

公开(公告)号：WO9825594A3

公开(公告)日：1998-09-17

申请号：PCT/EP9706971

申请日：1997-12-09

Applicant: SMITHKLINE BEECHAM PLC ,  EVANS JOHN MORRIS ,  PARSONS ANDREW

Inventor： EVANS JOHN MORRIS ,  PARSONS ANDREW

IPC: A61K31/53 ,  A61P25/06 ,  A61K31/00

CPC classification number: A61K31/53

Abstract: A method of treating or preventing migraine in humans comprises administering to a patient in need thereof an effective amount of lamotrigine or a pharmaceutically acceptable salt thereof. 00000

Abstract translation: 治疗或预防人类偏头痛的方法包括向有需要的患者施用有效量的拉莫三嗪或其药学上可接受的盐。 00000

公开(公告)号：WO1998011890A1

公开(公告)日：1998-03-26

申请号：PCT/EP1997005168

申请日：1997-09-15

Applicant: SMITHKLINE BEECHAM PLC ,  PARSONS, Andrew, A. ,  THOMPSON, Mervyn ,  UPTON, Neil ,  EVANS, John, Morris

Inventor： SMITHKLINE BEECHAM PLC

IPC: A61K31/35

CPC classification number: A61K31/353

Abstract: Benzopyran derivatives and analogs are disclosed as useful for the treatment and/or prophylaxis of degenerative diseases such as Huntingdon's chorea, schizophrenia, neurological deficits associated with AIDS, sleep disorders (including circadian rhythm disorders, insomnia and narcolepsy), tics (e.g. Gilles de la Tourette's syndrome), traumatic brain injury, tinnitus, neuralgia, especially trigeminal neuralgia, neuropathic pain, dental pain, cancer pain, inappropriate neuronal activity resulting in neurodysthesias in diseases such as diabetes, MS and motor neurone disease, ataxias, muscular rigidity (spasticity), temporomandibular joint dysfunction.

Abstract translation: 公开了苯并吡喃衍生物和类似物用于治疗和/或预防退行性疾病如亨廷顿氏舞蹈病，精神分裂症，与AIDS相关的神经功能障碍，睡眠障碍（包括昼夜节律紊乱，失眠和发作性睡病），抽搐（例如Gilles de la Tourette综合征），创伤性脑损伤，耳鸣，神经痛，特别是三叉神经痛，神经性疼痛，牙痛，癌症疼痛，导致糖尿病，运动神经元疾病，共济失调，肌肉僵直（痉挛）等疾病中的神经损伤的不适当的神经元活动 ，颞下颌关节功能障碍。

公开(公告)号：WO1995034547A1

公开(公告)日：1995-12-21

申请号：PCT/EP1995002249

申请日：1995-06-09

Applicant: SMITHKLINE BEECHAM PLC ,  VONG, Antonio, Kuok, Keong ,  THOMPSON, Mervyn ,  EVANS, John, Morris ,  MORGAN, Helen, Kate, Anne

Inventor： SMITHKLINE BEECHAM PLC

IPC: C07D311/68

CPC classification number: C07D491/04 ,  C07D311/68

Abstract: The invention provides certain 5 and/or 8 substituted benzopyran, pyranopyridine or tetrahydroquinaline compounds having a C-4 amide substituent and processes for making them. The compounds described are useful in treating and/or preventing certain disorders.

Abstract translation: 本发明提供具有C-4酰胺取代基的某些5和/或8取代的苯并吡喃，吡喃并吡啶或四氢金刚碱化合物及其制备方法。 所描述的化合物可用于治疗和/或预防某些疾病。

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：WO1986006960A2

公开(公告)日：1986-12-04

申请号：PCT/GB1986000282

申请日：1986-05-20

Applicant: BEECHAM GROUP P.L.C. ,  BEECHAM-WUELFING GMBH & CO. KG. ,  NICHOLSON, Charles, David ,  ANGERSBACH, Dieter ,  EVANS, John, Morris

Inventor： BEECHAM GROUP P.L.C. ,  BEECHAM-WUELFING GMBH & CO. KG.

IPC: A61K31/44

CPC classification number: A61K31/455 ,  A61K31/44

Abstract: The use of nicorandil or pinacidil or a pharmaceutically acceptable salt or a hydrate thereof in the preparation of a medicament for the treatment of peripheral vascular disease.

Abstract translation: 尼可地尔或pinacidil或其药学上可接受的盐或其水合物在制备用于治疗外周血管疾病的药物中的用途。

公开(公告)号：WO1998025594A2

公开(公告)日：1998-06-18

申请号：PCT/EP1997006971

申请日：1997-12-09

Applicant: SMITHKLINE BEECHAM PLC ,  EVANS, John, Morris ,  PARSONS, Andrew

Inventor： SMITHKLINE BEECHAM PLC

IPC: A61K31/00

CPC classification number: A61K31/53

Abstract: A method of treating or preventing migraine in humans comprises administering to a patient in need thereof an effective amount of lamotrigine or a pharmaceutically acceptable salt thereof.

Abstract translation: 治疗或预防人类偏头痛的方法包括向有需要的患者施用有效量的拉莫三嗪或其药学上可接受的盐。