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    Pharmaceutical compositions and methods for use
    4.
    发明授权
    Pharmaceutical compositions and methods for use 失效
    药物组合物和使用方法

    公开(公告)号：US06432954B1

    公开(公告)日：2002-08-13

    申请号：US09616743

    申请日：2000-07-14

    申请人： Gary M. Dull ,  Jean-Pierre LeConte ,  Humayun Kabir

    发明人： Gary M. Dull ,  Jean-Pierre LeConte ,  Humayun Kabir

    IPC分类号： A61K3153

    CPC分类号： A61K31/435 ,  A61K31/505 ,  A61K2300/00

    摘要： Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are 2,3-diacyltartaric acid salts of nicotinic compounds, and particularly, nicotinic compounds that are characterized as aryl substituted amines (e.g., aryl substituted olefinic amines).

    摘要翻译： 通过向有需要的患者施用作为烟碱化合物的2,3-二酰基酒石酸盐的组合物，特别是以烟酸化合物为特征的烟碱化合物治疗易患或患有病症和障碍的患者，例如中枢神经系统疾病， 芳基取代的胺（例如，芳基取代的烯属胺）。

    Use of agonists or antagonists of P2 purinoceptors for the prevention of glutamate-evoked cytotoxicity
    6.
    发明授权
    Use of agonists or antagonists of P2 purinoceptors for the prevention of glutamate-evoked cytotoxicity 失效
    使用P2嘌呤受体的激动剂或拮抗剂来预防谷氨酸诱发的细胞毒性

    公开(公告)号：US06326370B1

    公开(公告)日：2001-12-04

    申请号：US09000403

    申请日：1998-03-18

    申请人： Cinzia Volonte' ,  Daniela Merlo

    发明人： Cinzia Volonte' ,  Daniela Merlo

    IPC分类号： A61K3153

    CPC分类号： A61K31/7076 ,  A61K31/53

    摘要： This invention relates to the use of agonists or antagonists of P2 purinoceptors for the prevention of glutamate-evoked cytotoxicity and in particular use of Basilen Blue D-3G (Reactive Blue 2), Cibacron Blue 3GA and 5-adenylylimidodiphosphate (AMPPNP). In the presence of cytotoxic concentrations of glutamate, these compounds sustain cellular survival of central nervous system (CNS) neurons, such as for example postnatal rat cerebellar granule neurons.

    摘要翻译： 本发明涉及P2嘌呤受体的激动剂或拮抗剂用于预防谷氨酸诱发的细胞毒性，特别是使用Basilen Blue D-3G（活性蓝2），Cibacron Blue 3GA和5-腺苷二磷酸（AMPPNP）。 在存在谷氨酸的细胞毒性浓度的情况下，这些化合物维持中枢神经系统（CNS）神经元的细胞存活，例如产后大鼠小脑颗粒神经元。

    3-oxo-2(H)-1,2,4-triazine derivatives as ligands of 5 HT1A receptors
    7.
    发明授权
    3-oxo-2(H)-1,2,4-triazine derivatives as ligands of 5 HT1A receptors 有权
    3-羟基-2（H）-1,2,4-三嗪衍生物作为5个HT1A受体的配体

    公开(公告)号：US06303603B1

    公开(公告)日：2001-10-16

    申请号：US09529728

    申请日：2000-04-14

    申请人： Jean-Francois Patoiseau ,  Elisabeth Dupont-Passelaigue ,  Wouter Koek

    发明人： Jean-Francois Patoiseau ,  Elisabeth Dupont-Passelaigue ,  Wouter Koek

    IPC分类号： A61K3153

    CPC分类号： C07D253/075 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

    摘要： The invention concerns novel 3-oxo-(2H)-1,2,4-triazine derivatives of general formula (I) in which R1 represents: hydrogen, when A is an optionally substituted nitrogen atom; a linear or branched 1-C4 alkyl group; a C1-C4phenyl alkyl group, the phenyl ring being optionally substituted by one or several groups such as C1-C4 alkyl, C1-C3 alkoxy, halogen, trifluoromethyl. R2 represents: hydrogen; a linear or branched C1-C4 alkyl radical; a C1-C4 phenyl or phenylalkyl group, the phenyl ring being optionally substituted by one or several groups such as C1-C4 alkyl, C1-C3 alkoxy, halogen, trifluoromethyl. A represents an oxygen atom or a nitrogen atom optionally NR3 substituted. R3 represents hydrogen or a methyl group. B represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl, pyridyl or pyrimidyl, optionally substituted by one or several groups such as C1-C3 alkyl, C1-C3 alkoxy, hydroxy, trifluoromethyl or halogen and n can be whole numbers ranging between 3 and 5; (IIb) in which Ar is as defined in formula (IIa) and m can be a whole number ranging between 1 and 2; (IIc) in which R4 represents hydrogen or a C1-C3 alkyl group and n can be whole numbers ranging between 3 and 5.

    摘要翻译： 本发明涉及通式（I）的新的3-氧代 - （2H）-1,2,4-三嗪衍生物，其中当R1是任意取代的氮原子时，R 1表示：氢; 直链或支链的1-C4烷基; C1-C4苯基烷基，苯环任选被一个或多个基团取代，例如C 1 -C 4烷基，C 1 -C 3烷氧基，卤素，三氟甲基。 R2表示：氢; 直链或支链C 1 -C 4烷基; C 1 -C 4苯基或苯基烷基，苯环任选被一个或几个基团例如C 1 -C 4烷基，C 1 -C 3烷氧基，卤素，三氟甲基取代。 A表示氧原子或任选被NR 3取代的氮原子。 R3表示氢或甲基。 B表示其中Ar本身表示芳族结构的基团，例如苯基，吡啶基或嘧啶基，任选被一个或多个基团例如C 1 -C 3烷基，C 1 -C 3烷氧基，羟基，三氟甲基或卤素取代， n可以是3到5之间的整数; （IIb）其中Ar如式（IIa）中所定义，m可以是1和2之间的整数; （IIc）其中R4表示氢或C1-C3烷基，n可以是3至5的整数。

    Preventive/remedies for liver diseases
    9.
    发明授权
    Preventive/remedies for liver diseases 有权
    预防/治疗肝病

    公开(公告)号：US06794398B1

    公开(公告)日：2004-09-21

    申请号：US09959441

    申请日：2002-03-06

    申请人： Makoto Nakamuta ,  Hajime Nawata ,  Masayoshi Uehata

    发明人： Makoto Nakamuta ,  Hajime Nawata ,  Masayoshi Uehata

    IPC分类号： A61K3153

    CPC分类号： C07D471/04 ,  A61K31/16 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4409 ,  C07D213/75

    摘要： The invention provides an agent for the prophylaxis and treatment of liver disease and an activation inhibitor of hepatic stellate cells, which contains a compound having a Rho kinase inhibitory activity. The compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)cyclohexane, is useful for the prophylaxis and treatment of liver diseases, such as hepatitis, hepatic fibrosis, hepatic cirrhosis, hepatic cancer and the like, because it has various actions, such as a superior inhibitory action on the activation of hepatic stellate cell, suppressive action on hepatic fibrogenesis in liver tissues and the like.

    摘要翻译： 本发明提供了预防和治疗肝脏疾病的药剂和肝星状细胞的活化抑制剂，其含有具有Rho激酶抑制活性的化合物。 具有Rho激酶抑制活性的化合物如（+） - 反式-4-（1-氨基乙基）-1-（4-吡啶基氨基甲酰基）环己烷可用于预防和治疗肝脏疾病如肝炎，肝脏 纤维化，肝硬化，肝癌等，因为具有对肝星状细胞活化的优异抑制作用，对肝组织中肝纤维发生的抑制作用等各种作用。