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    • 1. 发明授权
    • Anti-convulsant isoquinolyl-benzamide derivatives
    • 抗惊厥异喹啉基 - 苯甲酰胺衍生物
    • US06277861B1
    • 2001-08-21
    • US09381369
    • 1999-12-21
    • John David HarlingBarry Sidney OrlekMervyn Thompson
    • John David HarlingBarry Sidney OrlekMervyn Thompson
    • A61K3147
    • C07D217/04
    • Compounds of formula (I) and pharmaceutically acceptable salts thereof, where R1 is hydrogen, C1-6alkyl (optionally substituted by hydroxy or C1-4alkoxy), C1-6alkenyl, C1-6alkynyl, C1-6alkylCO—, formyl, CF3CO— or C1-6alkylSO2—; R2 is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, CF3O—, CF3S—, CF3CO—, trifluoromethyldiazirinyl, C 1-6?alkyl, C1-6alkenyl, C1-6alkynyl, C1-6perfluoroalkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkylO—, C1-6alkylCO—, C3-6cycloalkylO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4alkylO—, C3-6cycloalkyl-C1-4alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, C1-6alkylS—, C1-6alkylSO2—, (C1-4alkyl)2NSO2—, (C1-4alkyl)NHSO2—, (C1-4alkyl)2NCO—, (C1-4alkyl)NHCO— or CONH2; or —NR5R6 where R5 is hydrogen or C1-4alkyl, and R6 is hydrogen, C1-4alkyl, formyl, —CO2C1-4alkyl or —COC1-4alkyl; or two R2 groups together form a carbocyclic ring that is saturated or unsaturated and unsubstituted or substituted by —OH or ═O; and the two R3 groups and the two R4 groups are each independently hydrogen or C1-6alkyl or the two R3 groups and/or the two R4 groups together form a C3-6spiroalkyl group provided that at least one R3 and R4 group is not hydrogen, are useful in the treatment and prophylaxis of epilepsy and other disorders.
    • 式(I)化合物及其药学上可接受的盐,其中R 1为氢,C 1-6烷基(任选被羟基或C 1-4烷氧基取代),C 1-6烯基,C 1-6炔基,C 1-6烷基CO-,甲酰基,CF 3 CO-或C 1 烷基SO2-; R 2是氢或至多三个选自卤素,NO 2,CN,N 3,CF 3 O-,CF 3 S-,CF 3 CO-,三氟甲基二氮丙烯基,C 1-6烷基,C 1-6烯基,C 1-6炔基,C 1-6全氟烷基, C 1-6烷基,C 3-6环烷基-C 1-4烷基 - ,C 1-6烷基O - ,C 1-6烷基CO-,C 3-6环烷基O-,C 3-6环烷基CO-,C 3-6环烷基-C 1-4烷基O - ,C 3-6环烷基-C 1-4烷基CO-,苯基 ,苯氧基,苄氧基,苯甲酰基,苯基-C 1-4烷基 - ,C 1-6烷基-S-,C 1-6烷基SO 2 - ,(C 1-4烷基)2NSO 2 - ,(C 1-4烷基)NHSO 2 - ,(C 1-4烷基)2 CO-, -4-烷基)NHCO-或CONH 2; 或-NR5R6,其中R5是氢或C1-4烷基,R6是氢,C1-4烷基,甲酰基,-CO2C1-4烷基或-COC1-4烷基; 或两个R 2基团一起形成饱和或不饱和且未被取代或被-OH或= O取代的碳环; 并且两个R 3基团和两个R 4基团各自独立地为氢或C 1-6烷基,或者两个R 3基团和/或两个R 4基团一起形成C 3-6螺环烷基,条件是至少一个R 3和R 4
    • 5. 发明授权
    • Substituted cycloalkylamine derivatives and their use as calcium channel
antagonists
    • 取代的环烷基胺衍生物及其作为钙通道拮抗剂的用途
    • US5817698A
    • 1998-10-06
    • US704585
    • 1996-09-20
    • Thomas Henry BrownJohn David HarlingBarry Sidney Orlek
    • Thomas Henry BrownJohn David HarlingBarry Sidney Orlek
    • A61K31/135A61P9/10A61P25/00A61P25/28A61P43/00C07C211/35C07C211/37C07C217/52C07C225/20C07C255/49C07C323/26C07C323/30C07C323/50
    • C07C225/20C07C217/52C07C323/26C07C2101/08
    • A method of treatment of a condition or disease related to the accumulation of calcium in the brain cells of a mammal which comprises administering to a subject in need thereof an effective amount of a compound of formula (I), wherein X is O, S, C.dbd.O or a bond; p and q are independently 0-4; R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkylC.sub.1-4 alkyl; n is 1, 2, 3 or 4; and Ar is phenyl optionally substituted by 1 to 3 substituents selected from; halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-2 alkylenedioxy, trifluoromethyl, trifluoromethoxy, CN, NO.sub.2, amino, mono- or di- alkylamino and Ph(Alk.sup.1).sub.r Y(Alk.sup.2).sub.s -- where Ph is optionally substituted phenyl, Y is a bond, oxygen or a carbonyl group, Alk.sup.1 and Alk.sup.2 are independently C.sub.1-4 alkyl which may be straight or branched and r and s are independently 0 or 1, provided that the length of (Alk.sup.1).sub.r Y(Alk.sup.2).sub.s does not exceed 5 atoms, and pharmaceutically acceptable salts thereof; in the manufacture of a medicament for the treatment of a disorder wherein a calcium channel antagonist is indicated, e.g. ischaemic stroke. Certain novel compounds within formula (I) are also claimed.
    • PCT No.PCT / EP95 / 00964 Sec。 371日期:1996年9月20日 102(e)1996年9月20日PCT PCT 1995年3月14日PCT公布。 公开号WO95 / 26327 日期1995年10月5日式(I)治疗与哺乳动物脑细胞中钙累积相关的病症或疾病的方法,其包括向有需要的受试者施用有效量的化合物 式(I)的化合物,其中X为O,S,C = O或键; p和q独立地为0-4; R 1和R 2各自独立地选自氢,C 1-6烷基,C 3-6环烷基或C 3-6环烷基C 1-4烷基; n为1,2,3或4; 并且Ar是任选被1至3个选自下列的取代基取代的苯基; 卤素,C 1-4烷基,C 1-4烷氧基,C 1-2亚烷基二氧基,三氟甲基,三氟甲氧基,CN,NO 2,氨基,单 - 或二 - 烷基氨基和Ph(Alk 1)rY(Alk 2)s-,其中Ph是任选取代的苯基,Y是 键,氧或羰基,Alk1和Alk2独立地为可以是直链或支链的C 1-4烷基,r和s独立地为0或1,条件是(Alk1)rY(Alk2)s的长度不超过5 原子及其药学上可接受的盐; 在制备用于治疗其中指示钙通道拮抗剂的病症的药物中,例如, 缺血性中风。 还要求公式(I)中的某些新化合物。
    • 8. 发明授权
    • 1,6-naphthyridine anti-convulsants
    • 1,6-萘啶抗惊厥药
    • US06245778B1
    • 2001-06-12
    • US09424399
    • 1999-11-23
    • Michael Stewart HadleyJohn David HarlingFrank Peter HarringtonMervyn ThompsonRobert William Ward
    • Michael Stewart HadleyJohn David HarlingFrank Peter HarringtonMervyn ThompsonRobert William Ward
    • A61K314375
    • C07D471/04
    • Compounds of formula (I) and pharmaceutically acceptable salts thereof: where R1 is hydrogen, C1-6 alkyl optionally substituted by hydroxy or C1-4alkoxy, or C1-6 alkylphenyl; R2 is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, C1-6 alkylO-, C1-6 alkylS-, C1-6 alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl, CF3, CF3O, CF3CO—, C1-6alkylCO-, C3-6cycloalkylCO-, C3-6cycloalkyl-C1-4alkylCO-, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, or —NR3R4 where R3 is hydrogen or C1-4 alkyl, and R4 is hydrogen, C1-4alkyl, —CHO, —CO2C1-4alkyl or —COC1-4alkyl; or two R2 groups form a saturated carbocyclic ring optionally interrupted by oxygen; and X is selected from hydrogen, halogen, cyano, alkyl and alkoxy; are useful in the treatment and prophylaxis of inter alia epilepsy.
    • 式(I)化合物及其药学上可接受的盐:其中R 1是氢,任选被羟基或C 1-4烷氧基取代的C 1-6烷基或C 1-6烷基苯基; R 2是氢或至多三个选自卤素,NO 2,CN的取代基 ,N 3,C 1-6烷基,C 1-6烷基,C 1-6烷基,C 3-6环烷基,C 3-6环烷基-C 1-4烷基 - ,C 1-6烯基,C 1-6炔基,CF 3,CF 3 O,CF 3 CO-, C 3-6烷基CO-,C 3-6环烷基CO-,C 3-6环烷基-C 1-4烷基CO-,苯基,苯氧基,苄氧基,苯甲酰基,苯基-C 1-4烷基 - 或-NR 3 R 4,其中R 3是氢或C 1-4烷基,R 4是氢, 4个烷基,-CHO,-CO 2 C 1-4烷基或-COC 1-4烷基;或两个R 2基团形成任选被氧中断的饱和碳环; X选自氢,卤素,氰基,烷基和烷氧基;可用于处理和 特别是癫痫预防。
    • 10. 发明授权
    • Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity
    • 具有抗惊厥活性的四氢萘并吡喃基甲酰胺
    • US06410555B1
    • 2002-06-25
    • US09719335
    • 2001-02-16
    • John David HarlingFrank Peter HarringtonMervyn Thompson
    • John David HarlingFrank Peter HarringtonMervyn Thompson
    • A61K31435
    • C07D471/04C07D471/10
    • Compounds of formula (I) and pharmaceutically acceptable salts and solvates: where R1 is hydrogen, C1-6alkyl (optionally substituted by hydroxy or C1-4alkoxy), phenyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl; R2 is hydrogen or, up to three substituents selected from halogen, NO2, CN, N3, CF3O—, CF3S—, CF3SO2—, CF3CO—, C1-6alkyl, C1-6alkenyl, C1-6alkynyl, C1-6perfluoroalkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkyl, C1-6alkylCO—, C3-6cycloalkylO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4alkylO—, C3-6cycloalkyl-C1-4alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, C1-6alkylS—, C1-6alkylSO2—, (C1-4alkyl)2NSO2—, (C1-4alkyl)NHSO2—, (C1-4alkyl)2NCO—, (C1-4alkyl)NHCO— or CONH2; or —NR5R6 where R5 is hydrogen or C1-4alkyl, and R6 is hydrogen, C1-4alkyl, formyl, —CO2C1-4alkyl or —COC1-4alkyl; or two R2 groups together form a carbocyclic ring that is saturated or unsaturated, optionally interrupted by O or NH; R3 groups and R4 groups are each independently hydrogen or C1-6alkyl and/or the two R3 groups and/or the two R4 groups together form a C3-6spiroalkyl group, provided that at least one R3 or R4 group is not hydrogen; and X is selected from hydrogen, halogen, cyano, alkyl and alkoxy, are useful in the treatment and prophylaxis of epilepsy, migraine, and other disorders.
    • 式(I)化合物及其药学上可接受的盐和溶剂化物:其中R 1是氢,C 1-6烷基(任选被羟基或C 1-4烷氧基取代),苯基-C 1-4烷基 - ,C 1-6烯基,C 1-6炔基; R2是氢或最多三个选自卤素,NO 2,CN,N 3,CF 3 O-,CF 3 S-,CF 3 SO 2 - ,CF 3 CO-,C 1-6烷基,C 1-6烯基,C 1-6炔基,C 1-6全氟烷基,C 3-6环烷基 ,C 3-6环烷基-C 1-4烷基 - ,C 1-6烷基,C 1-6烷基CO-,C 3-6环烷基O-,C 3-6环烷基CO-,C 3-6环烷基-C 1-4烷基O - ,C 3-6环烷基-C 1-4烷基CO-,苯基,苯氧基 ,(C 1-4烷基)2 NSO 2 - ,(C 1-4烷基)NHSO 2 - ,(C 1-4烷基)2 NCO - ,(C 1-4烷基),C 1-4烷基 )NHCO-或CONH 2; 或-NR5R6,其中R5是氢或C1-4烷基,R6是氢,C1-4烷基,甲酰基,-CO2C1-4烷基或-COC1-4烷基; 或两个R 2基团一起形成饱和或不饱和的碳环,任选被O或NH中断; R 3基团和R 4基团各自独立地为氢或C 1-6烷基和/或两个R 3基团和/或两个R 4基团一起形成C 3-6螺环烷基,条件是至少一个R 3或R 4基团不是氢; X选自氢,卤素,氰基,烷基和烷氧基