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    • 76. 发明申请
    • CARBOXYLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS
    • 羧酸衍生物和药物组合物
    • WO1997015546A1
    • 1997-05-01
    • PCT/JP1996003056
    • 1996-10-21
    • NIPPON SHINYAKU CO., LTD.AOKI, TomiyoshiKUWABARA, Kenji
    • NIPPON SHINYAKU CO., LTD.
    • C07C59/68
    • C07C59/68C07C59/84
    • Carboxylic acid derivatives of general formula (1); pharmaceutically acceptable salts thereof; and solvates of these (wherein R , R , R and R are each independently hydrogen, alkyl, halogeno, hydroxy or alkoxy; R and R are each independently alkyl; R is hydrogen or alkyl; -X- is -O- or -S-; Y is hydrogen, alkyl, halogeno, hydroxy or alkoxy, and Z and Z are each hydrogen, or alternatively Y, Z and Z are joined together to represent -CH=; -A- is >CH-OH, >C=O, >CH-OR or >CH-OCOR wherein R is alkyl and R is alkyl or aryl; and T is alkylene optionally containing a multiple bond or the like). The above compounds are efficacious in preventing and treating arterial sclerosis, ischemic heart diseases, cerebral infarction, post-PTCA restenosis, and so on.
    • 通式(1)的羧酸衍生物; 其药学上可接受的盐; 和这些的溶剂合物(其中R 1,R 2,R 3和R 4各自独立地为氢,烷基,卤代,羟基或烷氧基; R 5和R 6各自独立地为 烷基; R 7是氢或烷基; -X-是-O-或-S-; Y是氢,烷基,卤代,羟基或烷氧基,Z 1和Z 2分别是氢或 或者Y,Z 1和Z 2连接在一起以表示-CH =; -A-是> CH-OH,> C = O,> CH-OR 8或> CH-OCOR 9 其中R 8为烷基,R 9为烷基或芳基; T为任选含有多重键的亚烷基等)。 上述化合物在预防和治疗动脉硬化,缺血性心脏病,脑梗死,PTCA后再狭窄等方面是有效的。
    • 80. 发明申请
    • ANTISENSE NUCLEIC ACID HOMOLOG
    • 抗原核酸同源异构体
    • WO1996018640A1
    • 1996-06-20
    • PCT/JP1995002584
    • 1995-12-15
    • NIPPON SHINYAKU CO., LTD.OHGI, TadaakiISHIYAMA, Kouichi
    • NIPPON SHINYAKU CO., LTD.
    • C07H21/02
    • C12N15/113A61K38/00C07H21/00C12N2310/321C12N2310/322C12N2310/3527C12N2310/3531C12N2310/3533
    • An antisense nucleic acid homolog having at least one nucleoside represented by general formula (1) in the same chain of a nucleic acid homolog having been modified or replaced at DNA, RNA or a phosphoric acid diester bond, wherein B represents adenin-9-yl, guanin-9-yl, hypoxanthin-9-yl, thymin-1-yl, uracil-1-yl or cytosin-1-yl; and X and Y are the same or different and each represents hydrogen, hydroxy, halogeno or lower alkoxy. Examples of the modified phosphoric acid diester bond of this antisense nucleic acid derivative include phosphorothioate, alkylphosphorothiate, N-alkylphosphoamidate, phosphorodithioate and alkylphosphonate bonds. Thus it is possible to provide an antisense molecular drug having a low toxicity and suppressing infection with herpesvirus, influenza virus, human immunodeficiency virus, etc., or the action of oncogenes.
    • 在具有在DNA,RNA或磷酸二酯键被修饰或替换的核酸同系物的同一链中具有至少一个由通式(1)表示的核苷酸的反义核酸同源物,其中B代表腺嘌呤-9-基 胍胺-9-基,次黄嘌呤-9-基,甲氨基-1-基,尿嘧啶-1-基或细胞蛋白-1-基; X和Y相同或不同,各自表示氢,羟基,卤代或低级烷氧基。 该反义核酸衍生物的改性磷酸二酯键的实例包括硫代磷酸酯,磷酸烷基酯,N-烷基磷酸酯,二硫代磷酸酯和烷基膦酸酯键。 因此,可以提供具有低毒性并抑制疱疹病毒,流感病毒,人类免疫缺陷病毒等感染或癌基因作用的反义分子药物。