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132 条记录 (耗时 0.016 秒)

    VITAMIN D ANALOGS AND METHODS OF PREPARING THESE COMPOUNDS
    1.
    发明授权
    VITAMIN D ANALOGS AND METHODS OF PREPARING THESE COMPOUNDS 失效
    VITAMIN D ANALOGA UND VERFAHREN ZU IHRER HERSTELLUNG

    公开(公告)号：EP0900185B1

    公开(公告)日：2001-03-14

    申请号：EP97923877.1

    申请日：1997-05-02

    申请人： DUPHAR INTERNATIONAL RESEARCH B.V

    发明人： HALKES, Sebastian ,  VAN DE VELDE, Jan, Paul ,  KANZLER, Silvia ,  REISCHL, Wolfgang

    IPC分类号： C07C33/38 ,  A61K31/045 ,  C07C39/23

    CPC分类号： C07C33/38 ,  C07C2602/08

    摘要： The invention relates to vitamin D analogs of general formula (I) wherein: R1 is a hydrogen atom or a substituent selected from the group consisting of hydroxy, CH2OH, CH2CH2OH, CH2CH2CH2OH, OCH3, OCH2OH, OCH2CH2OH and OCH2CH2CH2OH; R2 is a hydrogen atom or a substituent selected from the group consisting of OCH3, OCH2OH, CHm(CH2OH)n(CH2CH2OH)p, (CH2)qOH and O(CH2)rOH; wherein: m is 0 or 1, p, q and n are 0-3, r is 1-3 and m+n+p=3; with the proviso that R1 and/or R2 contain at least one OH group; R3 is a straight or branched, saturated or unsaturated aliphatic hydrocarbon of 6-13 C atoms which may be substituted with one or more substituents from the group hydroxy or fluoro. The invention further relates to methods of preparing these compounds, a pharmaceutical composition containing these compounds and to their use in pharmacotherapy and cosmetics.

    摘要翻译： 本发明涉及通式（I）的维生素D类似物，其中：R 1是氢原子或选自羟基，CH 2 OH，CH 2 CH 2 OH，CH 2 CH 2 CH 2 OH，OCH 3，OCH 2 OH，OCH 2 CH 2 OH和OCH 2 CH 2 CH 2 OH的取代基; R2是氢原子或选自OCH3，OCH2OH，CHm（CH2OH）n（CH2CH2OH）p，（CH2）qOH和O（CH2）rOH的取代基; 其中：m为0或1，p，q和n为0-3，r为1-3，m + n + p = 3; 条件是R1和/或R2含有至少一个OH基团; R3是6-13个碳原子的直链或支链饱和或不饱和脂族烃基，其可以被一个或多个羟基或氟取代基取代。 本发明还涉及制备这些化合物的方法，含有这些化合物的药物组合物及其在药物治疗和化妆品中的用途。

    N-oxotetrahydro-beta-carbolines
    3.
    发明公开
    N-oxotetrahydro-beta-carbolines 失效
    的N-氧代四氢β-咔啉

    公开(公告)号：EP0719777A2

    公开(公告)日：1996-07-03

    申请号：EP96200625.0

    申请日：1990-06-05

    申请人： DUPHAR INTERNATIONAL RESEARCH B.V

    发明人： Hermkens, Peter Harold Han ,  van Maarseveen, Jan Herman ,  Scheeren, Johan Wilhelm ,  Kruse, Cornelis Gerrit

    IPC分类号： C07D498/14 ,  C07D515/14

    CPC分类号： C07D515/14

    摘要： The invention relates to a method of preparing N-oxo-tetrahydro-β-carbolines having formula 1.

    wherein

    R 1 is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino,
    n has the value 0, 1 or 2,
    R 2 is hydrogen, lower alkyl or acyl,
    R 3 is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R 1 , and
    A together with the group -C-N-O-, forms a saturated heterocyclic ring system consisting of 6-8 ring atoms, wherein, in addition to the already present oxygen atom and nitrogen atom, an extra hetero atom from the group O, S and N may be present, which ring system may he substituted with one or more of the substituents alkyl,alkoxycarbonyl, alkanoyl, alkoxy, hydroxy, oxo, amino, mono- or dialkylamino, alkanoyl-or alkoxycarbonylamino, which ring system may be annelated with a saturated carbocyclic group of 5 or 6 ring atoms, by an intramolecular ringclosure reaction of compounds of formula 2

    wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a function during the ringclosure reaction.
    The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumour activity.

    摘要翻译： 其中R 1为低级烷基或烷氧基，卤素，三氟甲基，低级烷硫基，羟基，氨基，低级单或二烷基 - 或酰氨基，n为0,1或2，R 2为氢，低级烷基 或酰基，R 3为氢，低级烷基或烷氧基羰基，或任选被基团R 1取代的苯基，A与基团-CNO-一起形成由6-8个环原子组成的饱和杂环系统，其中， 除了已经存在的氧原子和氮原子之外，可以存在来自O，S和N基团的额外的杂原子，该环系可以被一个或多个取代基取代，烷基，烷氧基羰基，烷酰基，烷氧基，羟基， 氧代，氨基，一或二烷基氨基，烷酰基或烷氧基羰基氨基，该环系可用5或6个环原子的饱和碳环基团取代。 具有式1的化合物组中的雌激素衍生物具有强的抗病毒和抗肿瘤活性。

    2-Phenyl-7-azabicycloheptanes and 6-phenyl-8-azabicyclo
    6.
    发明公开
    2-Phenyl-7-azabicycloheptanes and 6-phenyl-8-azabicyclo 失效
    2-苯基-7-氮杂双环庚烷和6-苯基-8-氮杂双环辛烷。

    公开(公告)号：EP0664293A1

    公开(公告)日：1995-07-26

    申请号：EP94203482.8

    申请日：1994-11-30

    申请人： DUPHAR INTERNATIONAL RESEARCH B.V

    发明人： Scheeren, Johannes, Octrooibureau Zoan B.V. ,  Aben, René W.M., Octrooibureau Zoan B.V. ,  Kruse, Cornelis, Octrooibureau Zoan B.V.

    IPC分类号： C07D451/02 ,  C07D487/08 ,  A61K31/40 ,  A61K31/46

    CPC分类号： C07D451/02 ,  C07D487/08

    摘要： The invention relates to a group of novel 2-phenyl-7-azabicyclo [2,2,1] heptane and 6-phenyl-8-azabicyclo [3,2,1] octane derivatives having central nervous system, in particular analgesic activity, and to a method for the preparation of these compounds.
    The compounds have the general formula (1)

    wherein R is hydrogen or alkyl (1-3C), R₁ is alkyl (1-3C), alkoxy (1-3C), halogen, hydroxy or esterified hydroxy, amino or acetylated amino, or methylenedioxy, n has the value 0-3, and p is 1 or 2.

    摘要翻译： 本发明涉及一组具有中枢神经系统，特别是止痛活性的2-苯基-7-氮杂双环[2,2,1]庚烷和6-苯基-8-氮杂双环[3,2,1]辛烷衍生物， 以及制备这些化合物的方法。 化合物具有通式（1）其中R为氢或烷基（1-3C），R1为烷基（1-3C），烷氧基（1-3C），卤素，羟基或酯化羟基，氨基或乙酰化 氨基或亚甲二氧基，n的值为0-3，p为1或2。

    New antigenically active proteins/peptides, and feline infectious virus (FIPV)-vaccines
    9.
    发明公开
    New antigenically active proteins/peptides, and feline infectious virus (FIPV)-vaccines 失效
    新的抗原活性蛋白/肽，和感染性病毒（FIPV）-VACCINES

    公开(公告)号：EP0411684A3

    公开(公告)日：1991-02-27

    申请号：EP90201852.2

    申请日：1990-07-10

    申请人： DUPHAR INTERNATIONAL RESEARCH B.V

    发明人： Vennema, Harry ,  Rottier, Peter J.

    IPC分类号： C12N15/50 ,  C07K15/00 ,  A61K39/215

    CPC分类号： C07K14/005 ,  A61K39/00 ,  C12N2770/20022

    摘要： The invention relates to two new antigenic proteins/pepti­des which can be used to stimulate the immunity of cats (Felidae) against feline infectious peritonitis virus (FIPV), i.e. the M-protein and the N-protein. The invention also relates to vaccines which comprise such antigenic proteins or peptides. The nucleotide sequence and amino acid sequence of the M-­protein and the N-protein are indicated in figure 1.

    摘要翻译： 本发明涉及可用于刺激猫（Felidae）对猫传染性腹膜炎病毒（FIPV）即M蛋白和N-蛋白的免疫力的两种新的抗原蛋白/肽。 本发明还涉及包含这种抗原蛋白或肽的疫苗。 M蛋白和N-蛋白的核苷酸序列和氨基酸序列如图1所示。