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    Novel acrylic amide derivatives, a process for their preparation, pharmaceutical compositions containing the same and their use in medicine
    3.
    发明公开
    Novel acrylic amide derivatives, a process for their preparation, pharmaceutical compositions containing the same and their use in medicine 失效
    丙烯酰胺衍生物，它们的制备方法，含有它们和它们在医学中使用的药物组合物。

    公开(公告)号：EP0408106A2

    公开(公告)日：1991-01-16

    申请号：EP90201742.5

    申请日：1990-06-29

    申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.

    发明人： Fodor, Tamas ,  Fischer, Janos ,  Dobay, Laszlo ,  Ezer, Elemér ,  Matuz, Judit ,  Saghy, Katalin ,  Szporny, Laszlo ,  Hajos, György

    IPC分类号： C07C323/60 ,  C07C317/24 ,  A61K31/10 ,  C07C315/04 ,  C07C319/20 ,  C07D295/18 ,  C07D277/06

    CPC分类号： C07D295/185 ,  C07C317/44 ,  C07C323/54 ,  C07D207/16

    摘要： Novel acrylic amide derivative of the formula
    wherein
    R¹ represents a hydrogen or a halogen atom or a C₁₋₄alkyl, a C₁₋₄alkoxy or a nitro group.
    n is an integer of 0 to 2,
    A represents an amino acid residue derived from a naturally occuring amino acid or an antipode there­of which is connected to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid connected to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C₁₋₄alkyl group or is amidated; or A represents a group of formula
    wherein
    R₂ is a hydrogen atom or a phenyl, a C₁₋₄alkyl or a C₁₋₄alkoxycarbonyl group,
    and their salts which have interesting cytoprotective and antiulcer activities are provided. A process is also described for the preparation of said compounds.

    摘要翻译： 式 worin的R新颖丙烯酰胺衍生物<1> darstellt氢或卤素原子或C 1-4烷基，C 1-4烷氧基一个或硝基。 n是0〜2的整数，在氨基酸残基甲darstellt从天然存在的氨基酸或在它们的对映体的所有其连接到通过其氨基团的丙烯酸酰基残基衍生的; 或通过其氮连接到所述丙烯酸类酰基噻唑烷羧酸的残基，或上述残基的衍生物worin任何游离羧基被酯化被C 1-4烷基或酰胺化; 或甲darstellt式的基团的worin R2是氢原子或苯基，C 1-4烷基或一组C1-4alkoxycarbonyl，并且提供它们的盐其中具有令人感兴趣的细胞保护和抗溃疡活性。 因此，一个过程被描述为所述化合物的制备。

    Alkylaminofuranone derivatives
    9.
    发明公开
    Alkylaminofuranone derivatives 失效
    烷基氨基呋喃酮衍生物

    公开(公告)号：EP0192393A2

    公开(公告)日：1986-08-27

    申请号：EP86300895.9

    申请日：1986-02-10

    申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.

    发明人： Fodor, Tamas ,  Dobay, Laszlo ,  Fischer, Janos ,  Stefko, Bela ,  Kiss, Bela ,  Szombathelyi, Zsolt ,  Karpati, Egon ,  Laszlovszky, Istavan ,  Szporny, Laszlo

    IPC分类号： C07K5/06 ,  A61K37/02

    CPC分类号： C07K5/0222 ,  A61K38/00 ,  Y02P20/55

    摘要： The present invention relates to a compound of formula (I)
    wherein

    R' represents methyl or a group of the formula R 3 -NH-/CH 2 ) 4 - wherein R 3 is hydrogen or a protective group compatible with the peptide bond,
    R 2 represents hydrogen, a protective group compatible with the peptide bond or a cation derived from an organic or inorganic base; pharmaceutically acceptable salts and diastereomers thereof.

    The compounds of the invention are useful for inhibiting the effect of the angiotensin-converting enzyme and they can be used in therapy as blood pressure reducing agents and for the treatment of cardiac failure and glaucoma.

    摘要翻译： 本发明涉及式（I）化合物，其中R'代表甲基或式R3-NH- / CH2）4-基团，其中R3是氢或与该肽键相容的保护基，R2代表氢， 与肽键相容的保护基或衍生自有机或无机碱的阳离子; 其药学上可接受的盐和非对映体。 本发明化合物可用于抑制血管紧张素转化酶的作用，它们可用作降血压药物的治疗剂和治疗心力衰竭和青光眼。