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    • 2. 发明公开
    • LK6-A DERIVATIVES
    • LK6-A-衍生物
    • EP1097934A1
    • 2001-05-09
    • EP99929753.4
    • 1999-07-08
    • KYOWA HAKKO KOGYO CO., LTD.
    • AKAMA, TsutomuNAGATA, HiroyukiHASEGAWA, AtsuhiroUE, HarumiTAKAHASHI, IsamiSAITOH, YutakaMOCHIDA, KenichiIKEDA, Shun-ichiKANDA, Yutaka
    • C07D471/06A61K31/47
    • C07D471/06
    • LK6-A derivatives represented by general formula (I) and pharmacologically acceptable salts thereof, which exhibit immunosuppressive, cytostatic and antitumor effects and so on, wherein R 1 is a lower alkanoyl or acryloyl group which may be substituted with, e.g., lower alkoxy, or the like; R 2 is hydrogen, halogeno or the like; R 2' is hydrogen, or R 2' together with R 3 forms a bond; R 3 is optionally substituted lower alkanoyl, or R 3 together with R 2' forms a bond; R 4 and R 5 are each hydrogen, optionally substituted lower alkanoyl or the like; R 6 is hydrogen or the like; and R 7 and R 8 are each hydrogen, optionally substituted lower alkanoyl or the like, with the proviso that LK6-A corresponding to a compound of general formula (I) where R 1 is (E)-methoxyacryloyl; R 2 , R 4 , R 5 , R 6 and R 7 are each hydrogen; R 8 is acetyl; and R 2' and R 3 together form a bond is excepted.
    • 具有通式(I)表示的LK6-A衍生物及其药理学上可接受的盐,其具有免疫抑制,细胞抑制和抗肿瘤作用等,其中R 1为低级烷酰基或丙烯酰基,其可被例如较低级 烷氧基等; R 2是氢,卤素等; R 2是氢,或R 2与R 3一起形成键; R 3是任选取代的低级烷酰基,或R 3与R 2'一起形成键; R 4和R 5各自为氢,任选取代的低级烷酰基等; R 6是氢等; R 7和R 8各自为氢,任选取代的低级烷酰基等,条件是对应于通式(I)的化合物的LK6-A,其中R 1为(E) - 甲氧基丙烯酰基 ; R 2,R 4,R 5,R 6和R 7各自为氢; R 8是乙酰基; 和R 2'和R 3一起形成键。
    • 3. 发明公开
    • DC 107 DERIVATIVES (2)
    • DC 107-DERIVATE
    • EP0887351A1
    • 1998-12-30
    • EP97947917.7
    • 1997-12-12
    • Kyowa Hakko Kogyo Co., Ltd.
    • KANDA, YutakaARAI, HitoshiYAMAGUCHI, HiroyukiASHIZAWA, TadashiIKEDA, Shun-ichiMURAKATA, ChikaraTAMAOKI, Tatsuya
    • C07D513/18C07D513/20C07D519/00C07H15/26C07H17/00A61K31/425A61K31/70
    • C07D513/08C07H15/26C07H17/02
    • DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided:
      wherein R 1 represents CO(CR 4A R 4B ) n1 (O(CH 2 ) p1 ) n2 OR 5 {wherein n1 represents an integer of 1 or 2; R 4A and R 4B are the same or different, and each represents hydrogen or lower alkyl; p1 and n2 each represents an integer of 1 to 10; and R 5 represents hydrogen, lower alkyl, or the like), or
      (wherein A 1 , A 2 , A 3 , and A 4 are the same or different, and each represents hydrogen, hydroxy, or the like); R 2 represents hydrogen or COR 6 (wherein R 6 represents lower alkyl, aralkyl, substituted or unsubstituted aryl, or the like); R 3 represents lower alkyl, lower alkenyl, aralkyl having substituted or unsubstituted aryl, alicyclic alkanoyloxyalkyl, -CH 2 OCOR 7 , or the like, or is combined with Y to represent a bond; Y is combined together with R 3 to represent a bond or is combined together with Z to represent a bond; Z represents hydrogen, or is combined together with Y to represent a bond; and W represents oxygen, or NR 8 .
    • 提供了具有抗微生物活性和抗肿瘤活性的由式​​(I)表示的DC107衍生物或其药学上可接受的盐:其中R 1表示CO(CR 4 R 4)n1(O(CH 2)p1) )n2OR <5>其中n1表示1或2的整数; R 4A和R 4B相同或不同,各自表示氢或低级烷基; p1和n2各自表示1〜10的整数, R 5表示氢,低级烷基等)或(其中A 1,A 2,A 3和A 4相同或不同,各自 表示氢,羟基等); R 2表示氢或COR 6(其中R 6表示低级烷基,芳烷基,取代或未取代的芳基等); R 3表示低级烷基,低级烯基,具有取代或未取代的芳基的芳烷基,脂环族烷酰氧基烷基,-CH 2 OCOR 7等,或与Y结合以表示键; Y与R 3结合以表示键或与Z结合以表示键; Z表示氢,或与Y结合表示键; W表示氧,或NR 8。