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433 条记录 (耗时 0.026 秒)

    CYCLOPENTANE HEPTAN(ENE)OIC ACID, 2-HETEROARYLALKENYL DERIVATIVES AS THERAPEUTIC AGENTS
    53.
    发明公开
    CYCLOPENTANE HEPTAN(ENE)OIC ACID, 2-HETEROARYLALKENYL DERIVATIVES AS THERAPEUTIC AGENTS 审中-公开
    环戊烷庚烷（EN）OIC酸，2-杂芳基烯衍生物作为治疗剂的

    公开(公告)号：EP1032395A1

    公开(公告)日：2000-09-06

    申请号：EP98958612.8

    申请日：1998-11-17

    申请人： Allergan Sales, Inc.

    发明人： BURK, Robert, M.

    IPC分类号： A61K31/557 ,  C07D277/30

    CPC分类号： C07D333/28 ,  A61K31/557 ,  A61K31/5575 ,  A61K31/5585 ,  A61K31/559 ,  C07C405/00 ,  C07C405/0016 ,  C07C405/0041 ,  C07C405/0058 ,  C07D333/24 ,  C07D333/38

    摘要： The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The compounds used in accordance with the invention are represented by formula (I), wherein wavy line attachments indicate either the alpha (α) or beta (β) configuration; hatched segments indicate α configuration; the solid triangle is used to indicate β configuration; dashed bonds represent a double bond, or a single bond; R is a substituted heteroaryl radical having at least two pendant substituents selected from the group consisting of C1 to C6 alkyl; halogen; trifluoromethyl; COR1; COCF¿3?; SO2NR?1; NO¿2 and CN or at least one cyano group; R1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of -OR1 and -N(R1)2; Y is = O or represents 2 hydrogen radicals and the 9, 11 or 15 lower alkyl esters thereof; provided, however, when said heteroaryl radical is a dichlorothienyl radical, the compound is not a 1-carboxylic acid or amide thereof. Certain of the compounds represented by Formula (I) are novel and comprise another aspect of the present invention.

    NOVEL AMIDE DERIVATIVES AND MEDICINAL COMPOSITIONS THEREOF
    54.
    发明公开
    NOVEL AMIDE DERIVATIVES AND MEDICINAL COMPOSITIONS THEREOF 失效
    NEUS AMID-DERIVATE UND MEDISINISCHE ZUSAMMENSETZUNGEN DIEE ENTHALTEN

    公开(公告)号：EP0972769A1

    公开(公告)日：2000-01-19

    申请号：EP98900698.6

    申请日：1998-01-22

    申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD.

    发明人： MARUYAMA, Tatsuya ,  ONDA, Kenichi ,  HAYAKAWA, Masahiko ,  TAKAHASHI, Takumi ,  SUZUKI, Takayuki ,  MATSUI, Tetsuo

    IPC分类号： C07D233/64 ,  C07D249/12 ,  C07D257/04 ,  C07D277/40 ,  C07D277/30 ,  A61K31/415 ,  A61K31/41 ,  A61K31/425

    CPC分类号： C07D233/64 ,  C07C217/16 ,  C07C271/16 ,  C07C271/20 ,  C07D235/16 ,  C07D249/12 ,  C07D277/30 ,  C07D277/40 ,  C07D277/42 ,  C07D285/12 ,  C07D471/04

    摘要： An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle.
    (The symbols in the formula have the following meanings. (wherein

    A: heteroarylene;
    X: bond, O, S, -NR 5 -, -NR 5 CO-, -NR 5 CONH-, -NR 5 SO 2 - or -NR 5 C(=NH)NH-;
    R 1 : -H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl;
    R 2a , R 2b : -H or -lower alkyl, which may be the same or different;
    R 3 : -H or -lower alkyl;
    R 4a , R 4b : -H or -OH, which may be the same different, or R 4a and R 4b are taken together to form =O or =N∼O-lower alkyl; and
    R 5 : -H or -lower alkyl.)

    摘要翻译： 由以下通式（I）表示的酰胺衍生物或其盐和含有酰胺衍生物和药学上可接受的载体的药物组合物。 （其中A：亚杂芳基; X：键，O，S，-NR 5 - ，-NR 5 CO - ， - NR 5 CONH- ，-NR 5 SO 2 - 或-NR 5 C（= NH）NH-; R 1：-H， - 取代的低级烷基， - 取代的芳基， - 取代的杂芳基或 - 取代的环烷基 R 2a，R 2b：-H或 - 低级烷基，其可以相同或不同; R 3：-H或 - 低级烷基; R 4a，R 4b：-H 或-OH，其可以是相同的，或者R 4a和R 4b一起形成= O或= N型O-低级烷基;以及R 5：-H或 - 低级烷基。 ）