Isatineoxime derivatives and their use
    31.
    发明授权
    Isatineoxime derivatives and their use 失效
    伊马替尼肟衍生物及其用途

    公开(公告)号:US5223527A

    公开(公告)日:1993-06-29

    申请号:US899620

    申请日:1992-06-16

    IPC分类号: C07D209/60

    CPC分类号: C07D209/60

    摘要: A compound having the formula ##STR1## wherein R.sup.1 is C.sub.1-6 -alkyl which may be branched or cyclic;R.sup.2 is C.sub.1-6 -alkyl which may be branched or cyclic; or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --, wherein n is 3, 4, 5.and a method of treating disorders of a mammal, including a human, responsive to the blockade of glutamic and aspartic acid receptors, with the same.

    摘要翻译: 具有式“IMAGE”的化合物,其中R 1是可以是支链或环状的C 1-6 - 烷基; R2是可以是支链或环状的C 1-6 - 烷基; 或其中R 1和R 2一起表示 - (CH 2)n - ,其中n为3,4,5。以及治疗对谷氨酸和天冬氨酸受体的封闭反应的哺乳动物(包括人)的病症的方法,其中 相同。

    Isatine derivatives, their preparation and use
    32.
    发明授权
    Isatine derivatives, their preparation and use 失效
    伊马替尼衍生物,其制备和用途

    公开(公告)号:US5198461A

    公开(公告)日:1993-03-30

    申请号:US710790

    申请日:1991-06-05

    IPC分类号: C07D209/40

    CPC分类号: C07D209/40

    摘要: A method of treatment with compounds having the formula ##STR1## R.sup.1 is hydrogen, C.sub.1-6 -alkyl which may be branched, C.sub.3-7 -cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C.sub.1-6 -alkoxy, CH.sub.2 CO.sub.2 R' wherein R' is hydrogen or C.sub.1-6 -alkyl which may be branched, CH.sub.2 CN, CH.sub.2 CONR.sup.IV R.sup.V wherein R.sup.IV and R.sup.V independently are hydrogen or C.sub.1-6 -alkyl, or CH.sub.2 C(.dbd.NOH)NH.sub.2 ; R.sup.2 is hydrogen, benzyl, C.sub.1-6 -alkyl which may be branched, or C.sub.3-7 -cycloalkyl; R.sup.4, R.sup.5, R.sup.6, R.sup.7 independently are hydrogen, C.sub.1-6 -alkyl which may be branched, phenyl, halogen, C.sub.1-6 -alkoxy, NO.sub.2, CN, CF.sub.3, OCF.sub.3, or SO.sub.2 NR"R'" wherein R" and R'" independently are hydrogen, aralkoxy, aralkyl, or C.sub.1-6 -alkyl; or R.sup.6 and R.sup.7 together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO.sub.2, CF.sub.3, CN, OCF.sub.3, SO.sub.2 NR" R"' wherein R" and R"' independently are hydrogen, aralkoxy, aralkyl, or C.sub.1-6 -alkyl, and R.sup.4 and R.sup.5 have the meanings set forth above, are disclosed, as well as pharmaceutical compositions thereof. Certain of the compounds are novel.The compounds and pharmaceutical compositions containing the compounds are useful in the treatment of central nervous system disorders and especially conditions sensitive to excitatory amino acids.

    摘要翻译: 具有下式的化合物的方法是氢,可以是支链的C 1-6 - 烷基,C 3-7 - 环烷基,苄基,可被取代的苯基,酰基,羟基,C 1-6 - 烷氧基, CH2CO2R'其中R'是氢或可以是支链的C 1-6 - 烷基,CH 2 CN,CH 2 CONRIVRV其中RIV和RV独立地是氢或C 1-6 - 烷基或CH 2 C(= NOH)NH 2; R2是氢,苄基,可以是支链的C 1-6 - 烷基或C 3-7 - 环烷基; R4,R5,R6,R7独立地是氢,可以是支链的C1-6烷基,苯基,卤素,C1-6烷氧基,NO2,CN,CF3,OCF3或SO2NR''R“ '和R“独立地是氢,芳烷氧基,芳烷基或C 1-6 - 烷基; 或R6和R7一起形成另外的4至7元环,其可以是芳族或部分饱和的并且可以被卤素,NO 2,CF 3,CN,OCF 3,SO 2 NR“R”取代,其中R“和R' 独立地是氢,芳烷氧基,芳烷基或C 1-6 - 烷基,并且R 4和R 5具有上述含义,以及其药物组合物。 某些化合物是新颖的。 含有这些化合物的化合物和药物组合物可用于治疗中枢神经系统疾病,特别是对兴奋性氨基酸敏感的病症。

    4-phenylpiperidine compounds and their use
    36.
    发明授权
    4-phenylpiperidine compounds and their use 失效
    4-苯基哌啶化合物及其用途

    公开(公告)号:US4845095A

    公开(公告)日:1989-07-04

    申请号:US172197

    申请日:1988-03-23

    申请人: Frank Watjen

    发明人: Frank Watjen

    CPC分类号: C07D413/04 C07D211/28

    摘要: Piperidine compounds having the formula ##STR1## wherein R.sup.1 is hydrogen, (C.sub.1-6 -alkoxyaryl)alkyl, diphenylmethozy-C.sub.1-6 -alkyl, C.sub.1-8 -alkyl, C.sub.4-10 -cycloalkylalkyl, phenoxy-C.sub.1-8 -alkyl, or C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl; andR is ##STR2## or CH.dbd.NOR' wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl, aryl-C.sub.0-6 -alkyl, which may optionally be substituted with one or more halogen and (.sub.1-5 -alkoxy, thienyl, or C.sub.4-7 -cycloalkylalkyl.The novel compounds are useful for the treatment of pain conditions and as neuroleptics.

    Imidazoquinoxaline compounds
    37.
    发明授权
    Imidazoquinoxaline compounds 失效
    咪唑喹喔啉化合物

    公开(公告)号:US4774245A

    公开(公告)日:1988-09-27

    申请号:US912776

    申请日:1986-09-26

    摘要: New heterocyclic compounds having the general formula ##STR1## wherein X is ##STR2## wherein R.sup.1 is C.sub.1-6 -alkyl, Cphd 3-7-cycloalkyl, phenyl, thienyl, or C.sub.1-3 -alkoxymethyl,R.sup.6 and R.sup.7 independently are hydrogen or halogen, and--A--is --N(R")--C(O)--, --N(R")--CH.sub.2 --, or ##STR3## wherein R" is hydrogen, C.sub.3.differential. -cycloalkyl, or C.sub.1-6 -alkyl The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.

    摘要翻译: 具有通式的新的杂环化合物,其中X为X,其中R 1为C 1-6 - 烷基,C 3-10 - 环烷基,苯基,噻吩基或C 1-3 - 烷氧基甲基,R 6和R 7独立地为氢或 卤素和-A是-N(R“)-C(O) - , - N(R”') - CH 2 - 或其中R“是氢,C 3不同 - 环烷基或C 1 -6-烷基该化合物可用作精神药物制剂,如抗惊厥药,抗焦虑药,催眠药和精神分裂药。

    Hydrochloride salt of an azabicyclo[3.2.1]octane derivative
    38.
    发明授权
    Hydrochloride salt of an azabicyclo[3.2.1]octane derivative 有权
    氮杂双环[3.2.1]辛烷衍生物的盐酸盐

    公开(公告)号:US08263611B2

    公开(公告)日:2012-09-11

    申请号:US12529502

    申请日:2008-02-28

    CPC分类号: C07D451/02

    摘要: The invention relates to a hydrochloride salt of (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-[(methyloxy)methyl]-8-azabicyclo[3.2.1]octane, uses of the salt as a medicament in the treatment inter alia of disorders of the central nervous system and pharmaceutical compositions and dosage forms comprising the salt.

    摘要翻译: 本发明涉及(1R,2R,3S,5S)-3-(3,4-二氯苯基)-2 - [(甲氧基)甲基] -8-氮杂双环[3.2.1]辛烷的盐酸盐, 盐作为治疗特别是中枢神经系统病症的药物以及包含该盐的药物组合物和剂型。