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    Derivatives of acyl-piperazinyl-pyrimidines, preparation thereof and application as medicaments
    1.
    发明授权
    Derivatives of acyl-piperazinyl-pyrimidines, preparation thereof and application as medicaments 失效
    酰基 - 哌嗪基 - 嘧啶的衍生物，其制备和作为药物的应用

    公开(公告)号：US06372746B1

    公开(公告)日：2002-04-16

    申请号：US09462880

    申请日：2000-02-24

    申请人： Jordi Corbera-Arjona ,  David Vaño-Domenech ,  Jordi Frigola-Constansa

    发明人： Jordi Corbera-Arjona ,  David Vaño-Domenech ,  Jordi Frigola-Constansa

    IPC分类号： C07D40304

    CPC分类号： C07D405/12 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

    摘要： The derivatives of acyl-piperazinyl-pyrimidines of general formula (I), where X is O or S; R1 is alkoxy or trifluoromethyl; R2 is alkyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, show activity in the central nervous system. Compounds of general formula (I) in which X is O can be obtained by reacting a derivative of pyrimidine with a derivative of piperazine or by reacting a derivative of piperazinyl-pyrimidine with a carboxylic acid or a salt or derivative thereof. Compounds of general formula (I) in which X is S can be obtained by reacting (I) in which X is O with Lawesson's reagent or with phosphorous pentasulphide. The compounds (I) show sedative activity, anticonvulsant, sleep-inducing or general anaesthetic activity and can be applied in human or veterinary medicine

    摘要翻译： 通式（I）的酰基哌嗪基 - 嘧啶衍生物，其中X为O或S; R1是烷氧基或三氟甲基; R2是烷基，环烷基，杂环烷基，芳基，芳基烷基，杂芳基或杂芳基烷基，在中枢神经系统中显示活性。 其中X为O的通式（I）化合物可以通过使嘧啶衍生物与哌嗪的衍生物反应或通过使哌嗪基 - 嘧啶的衍生物与羧酸或其盐或衍生物反应来获得。 其中X为S的通式（I）的化合物可以通过（I）其中X为O与Lawesson's试剂或五硫化磷反应而获得。 化合物（I）显示镇静活性，抗惊厥，睡眠诱导或全身麻醉活性，可应用于人或兽药

    Topical ophthalmic composition comprising a 2-[4-(azolylbutyl)piperazinylmethyl]benzimidazole derivative, in particular for the treatment of allergic conjunctivitis
    6.
    发明授权
    Topical ophthalmic composition comprising a 2-[4-(azolylbutyl)piperazinylmethyl]benzimidazole derivative, in particular for the treatment of allergic conjunctivitis 失效
    包含2- [4-（唑基丁基）哌嗪基甲基]苯并咪唑衍生物的局部眼用组合物，特别是用于治疗过敏性结膜炎

    公开(公告)号：US5641781A

    公开(公告)日：1997-06-24

    申请号：US613843

    申请日：1996-03-11

    申请人： Maria Rosa Cuberes-Altisent ,  Jordi Frigola-Constansa

    发明人： Maria Rosa Cuberes-Altisent ,  Jordi Frigola-Constansa

    IPC分类号： C07D403/12 ,  A61K31/495 ,  A61K31/496 ,  A61K31/55 ,  A61K31/551 ,  A61P27/02

    CPC分类号： A61K31/551 ,  A61K31/496

    摘要： The present invention relates to a topical ophthalmic composition comprising at least one compound of general formula I ##STR1## in which n may have the values 0 or 1,m may have the values 2 or 3,and Het represents a heteroaromatic radical of formula ##STR2## in which X, Y, Z and W, which may be the same or different, represent a nitrogen atom or a carbon atom linked to a hydrogen atom, a halogen atom, a methyl radical, an ethyl carboxylate radical, a carboxylic radical or a sulphonic radical, and the pharmaceutically acceptable salts thereof, combined with an ophthalmically acceptable vehicle, in particular for the treatment of allergic conjunctivitis.

    摘要翻译： 本发明涉及包含至少一种通式I的化合物（I）的局部眼用组合物，其中n可以具有0或1的数值，m可以具有2或3的值，并且Het表示杂芳族基团 其中X，Y，Z和W可以相同或不同，表示与氢原子，卤素原子，甲基，羧酸乙酯基团连接的氮原子或碳原子， 羧基或磺酰基及其药学上可接受的盐，与眼科可接受的载体组合，特别是用于治疗过敏性结膜炎。