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22 条记录 (耗时 0.023 秒)

    Treatment of cognitive and behavioral disorders associated with aging and with dementia syndromes
    3.
    发明授权
    Treatment of cognitive and behavioral disorders associated with aging and with dementia syndromes 失效
    治疗与衰老和痴呆综合征相关的认知和行为障碍

    公开(公告)号：US4956363A

    公开(公告)日：1990-09-11

    申请号：US309877

    申请日：1989-08-08

    申请人： Ernst Wulfert ,  Jean Gobert ,  Eric Cossement

    发明人： Ernst Wulfert ,  Jean Gobert ,  Eric Cossement

    IPC分类号： C07D251/18 ,  A61K31/53 ,  A61K31/535 ,  A61P25/04

    CPC分类号： A61K31/53

    摘要： A method for the treatment of cognitive and behavioral disorders associated with aging and with dementia syndromes, for example senile dementia, Alzheimer's type, by administering a 2-amino-4-morpholino-6-propyl-1,3,5-triazine of the formula ##STR1## in which R.sub.1 =hydrogen, alkyl, aralkyl or acetyl, R.sub.2 =hydrogen, hydroxyl, alkyl, hydroxyalkyl, alkoxyalkyl, dialkylamino, aryl-hydroxyalkyl, (hydroxycycloalkyl)alkyl, alkanoyloxyalkyl, benzoyloxyalkyl, phenylacetyloxyalkyl, aminocarbonyloxyalkyl, COR.sub.3, where R.sub.3 =alkyl, aryl, halogenoaryl, alkylaryl, alkoxyaryl, aralkyl or aryloxy, CONR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 =hydrogen or alkyl, or R.sub.1 and R.sub.2 form an alkyleneimino substituted by hydroxyalkyl, and in addition when R.sub.1 =acetyl, R.sub.2 =acetoxyalkyl, or a salt thereof.

    摘要翻译： 一种用于治疗与衰老相关的认知和行为障碍与老年痴呆综合征（例如老年痴呆，阿尔茨海默氏症）的方法，通过施用2-氨基-4-吗啉代-6-丙基-1,3,5-三嗪 式中：R1 =氢，烷基，芳烷基或乙酰基，R2 =氢，羟基，烷基，羟基烷基，烷氧基烷基，二烷基氨基，芳基 - 羟基烷基，（羟基环烷基）烷基，烷酰氧基烷基，苯甲酰氧基烷基，苯基乙酰氧基烷基，氨基羰氧基烷基，COR3， R3 =烷基，芳基，卤代芳基，烷基芳基，烷氧基芳基，芳烷基或芳氧基，CONR4R5，其中R4和R5 =氢或烷基，或R1和R2形成被羟烷基取代的亚烷基亚氨基，此外当R1 =乙酰基时，R2 =乙酰氧基烷基， 或其盐。

    Substituted 1-(1H-imidazol-4-yl)alkyl-benzamides as anti-ischemics and as alpha-2-adrenergic receptor agonists
    6.
    发明授权
    Substituted 1-(1H-imidazol-4-yl)alkyl-benzamides as anti-ischemics and as alpha-2-adrenergic receptor agonists 失效
    取代的1-（1H-咪唑-4-基）烷基 - 苯甲酰胺作为抗缺血剂和作为α-2-肾上腺素能受体激动剂

    公开(公告)号：US4923865A

    公开(公告)日：1990-05-08

    申请号：US334854

    申请日：1989-04-06

    申请人： Eric Cossement ,  Jean-Pierre Geerts ,  Jean Gobert ,  Philippe Michel ,  Ernst Wulfert

    发明人： Eric Cossement ,  Jean-Pierre Geerts ,  Jean Gobert ,  Philippe Michel ,  Ernst Wulfert

    IPC分类号： C07D233/56 ,  A61K31/415 ,  A61K31/4164 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  A61P29/00 ,  C07D233/54 ,  C07D233/64

    CPC分类号： C07D233/64

    摘要： New substituted 1-(1H-imidazol-4-yl)alkyl-benzamides and their salts, processes for the preparation thereof and pharmaceutical compositions.These compounds have the formula ##STR1## wherein R.sub.1, R.sub.2 =hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sub.3 =hydrogen, amino, hydroxyl, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -hydroxyalkyl,R.sub.4 =hydrogen or C.sub.1 -C.sub.4 -alkyl, orR.sub.3 R.sub.4 N=pyrrolidino, piperidino or morpholino,R.sub.5 and R.sub.6 =hydrogen, hydroxyl, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, at least one ofR.sub.5 and R.sub.6 being other than hydrogen.These compounds are prepared either by reacting a nitrogen compound with an alkyl 1-(1H-imidazol-4-yl)alkyl-benzoate or with a 1-(1H-imidazol-4-yl)alkyl-benzoic acid, or by hydrolyzing in an acid medium a 2-hydroxy-3-[1-(1H-imidazol-4-yl)alkyl]-benzonitrile.The compounds have anti-ischemic and .alpha..sub.2 -adrenoceptor agonist activities.

    摘要翻译： 新的取代的1-（1H-咪唑-4-基）烷基 - 苯甲酰胺及其盐，其制备方法和药物组合物。 这些化合物具有下式：其中R1，R2 =氢或C1-C4-烷基，R3 =氢，氨基，羟基，C1-C4-烷基或C1-C4-羟烷基，R4 =氢或C1-C4-烷基 或R3R4N =吡咯烷子基，哌啶子基或吗啉代，R5和R6 =氢，羟基，C1-C4-烷基或C1-C4-烷氧基，R5和R6中的至少一个不是氢。 这些化合物可以通过使氮化合物与1-（1H-咪唑-4-基）烷基 - 苯甲酸烷基酯或1-（1H-咪唑-4-基）烷基 - 苯甲酸烷基酯反应，或通过水解 酸性介质为2-羟基-3- [1-（1H-咪唑-4-基）烷基] - 苄腈。 该化合物具有抗缺血和α2-肾上腺素受体激动剂活性。

    Substituted 1H-imidazoles
    7.
    发明授权
    Substituted 1H-imidazoles 失效
    取代的1H-咪唑

    公开(公告)号：US4814343A

    公开(公告)日：1989-03-21

    申请号：US116325

    申请日：1987-11-02

    申请人： Eric Cossement ,  Jean-Pierre Geerts ,  Jean Gobert ,  Philippe Michel

    发明人： Eric Cossement ,  Jean-Pierre Geerts ,  Jean Gobert ,  Philippe Michel

    IPC分类号： A61K31/415 ,  A61K31/4164 ,  A61K31/495 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D233/54 ,  C07D233/58 ,  C07D233/64 ,  C07D405/06 ,  C07D413/06

    CPC分类号： C07D233/64 ,  C07D405/06

    摘要： New substituted 1H-imidazoles and their salts, processes for the preparation thereof and pharmaceutical compositions.These compounds have the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.5 =hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sub.4 =hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy;Y.sub.1 =hydrogen and Y.sub.2 =OZ.sub.2 or the reverse;Z.sub.1 =Z.sub.2 =hydrogen or C.sub.1 -C.sub.4 -alkyl or Z.sub.1 and Z.sub.2 =--CH.sub.2 -- or --C(CH.sub.3).sub.2 --.These compounds are prepared either by reducing a corresponding imidazole compound having a hydroxyl or alkoxy group on the methyl bridge between the imidazole and phenyl rings, or by hydrolyzing a 4-[[2,2-dimethyl-4H-1,3-benzodioxin-6(or 8)-yl]methyl]-1H-imidazole, or yet by reducing an alkyl 3-[(1H-imidazol-4-yl)methyl]-2-hydroxybenzoate.These compounds have cardiac, cerebral and tissular anti-ischemic activities.

    摘要翻译： 新的取代的1H-咪唑及其盐，其制备方法和药物组合物。 这些化合物具有下式：其中R1，R2，R3和R5 =氢或C1-C4-烷基; R4 =氢，C1-C4-烷基或C1-C4-烷氧基; Y1 =氢，Y2 = OZ2或相反; Z 1 = Z 2 =氢或C 1 -C 4 - 烷基或Z 1和Z 2 = -CH 2 - 或-C（CH 3）2 - 。 这些化合物可以通过在咪唑和苯环之间的甲基桥上还原相应的具有羟基或烷氧基的咪唑化合物，或通过水解4 - [[2,2-二甲基-4H-1,3-苯并二恶英 - 6（或8） - 基]甲基] -1H-咪唑，或还原3 - [（1H-咪唑-4-基）甲基] -2-羟基苯甲酸烷基酯。 这些化合物具有心脏，脑和组织的抗缺血活性。

    Enantjomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl) sulfonyl] piperazine
    10.
    发明申请
    Enantjomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl) sulfonyl] piperazine 审中-公开
    1 - [（4-氯苯基）苯基甲基] -4 - [（4-甲基苯基）磺酰基]哌嗪的内嵌体

    公开(公告)号：US20070142400A1

    公开(公告)日：2007-06-21

    申请号：US11652092

    申请日：2007-01-11

    申请人： Eric Cossement ,  Guy Bodson ,  Jean Gobert

    发明人： Eric Cossement ,  Guy Bodson ,  Jean Gobert

    IPC分类号： A61K31/495

    CPC分类号： A61K31/495 ,  C07D295/073 ,  C07D295/088 ,  C07D295/26

    摘要： The invention provides a method for the treatment of allergic conditions by administering to a patient an effective amount of dextrorotatory dihydrochloride of 2-[2-[4-[(4-chloro-phenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid. The treatment is conducted in the absence of levorotatory dihydrochloride of 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid.

    摘要翻译： 本发明提供了一种通过向患者施用有效量的2- [2- [4 - [（4-氯 - 苯基）苯基甲基] -1-哌嗪基]乙氧基]乙酸的右旋二盐酸盐来治疗过敏症状的方法 。 该处理在不存在2- [2- [4 - [（4-氯苯基）苯基甲基] -1-哌嗪基]乙氧基]乙酸的左旋二盐酸盐的情况下进行。