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    DERIVATIVES OF PHYSIOLOGICALLY ACTIVE SUBSTANCE K-252
    2.
    发明公开
    DERIVATIVES OF PHYSIOLOGICALLY ACTIVE SUBSTANCE K-252 失效
    DERIVATE DES PHYSIOLOGISCH AKTIVEN MITTELS K-252。

    公开(公告)号：EP0303697A1

    公开(公告)日：1989-02-22

    申请号：EP87901672.3

    申请日：1987-03-09

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： MURAKATA, Chikara ,  SATO, Akira ,  TAKAHASHI, Mitsuru ,  KOBAYASHI, Eiji ,  MORIMOTO, Makoto ,  AKINAGA, Shiro ,  HIRATA, Tadashi ,  MOCHIDA, Kenichi ,  KASE, Hiroshi ,  YAMADA, Koji ,  IWAHASHI, Kazuyuki

    IPC分类号： C07D498/22 ,  A61K31/55

    CPC分类号： C07D498/22

    摘要： Novel derivatives of K-252 ((8R', 9S*, 11S')-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8,11-epoxy-1H,8H,11H-2,7b,11a-triazadibenzo[a,g]cycloocta[cde]trinden-1-one) represented by formula (l) (wherein W 1 , W 2 , R 1 , R 2 , R 3 , R 4 , X, and Y represent various substituents) are disclosed. These compounds are physiologically active substances having a protein kinase C-inhibiting activity and an oncostatic activity, thus being useful as medicines.

    摘要翻译： 抗生素K-252衍生物。 式（I）的化合物是新的：在（I）中，R 1和R 3是OH，低级烷氧基或氨基，或R 3是H，R 1是H，Me，OH，Br，Cl，羟甲基，NR 5 R 6等; R2是H或氨基; 一个或R 5 / R 6是H，另一个是H，氨基甲酰基或低级烷基氨基羰基，或者R 5和R 6都是低级烷基; R4是H，C1，氨基甲酰基，低级烷基，氨基或-CH2CH2R7; R7是Br，氨基，羟基，二（低级烷基）氨基或羟基。 低级烷基氨基; W1和W2为H或一起为= O; X是H，甲酰基，低级烷氧基羰基，-CONR 8 R 9，-CH 2 A或-CH = NR 12; R8和R9是H，低级烷基，羟基。 低级烷基或R8是H，R9是OH; A是OH，叠氮基，低级烷硫基，低级烷基磺酰基，-NR10R11，-N = CHNMe2，-OCOCH2CH2COOH或2-四氢吡喃基氧基; R10和R11都是H或一个是H，低级烷基，芳基，羧基 - 低级烷基等，xycar，另一个是低级烷基（选择C1-substd）。 或R 10和R 11一起为-CH 2 CH 2 -B-CH 2 CH 2 - ; B是亚甲基，-NH-，S或O; R 12是OH，氨基，胍基或2-咪唑基氨基; Y是OH或氨基甲酰氧基; X和Y可以是（-XY-）-O-，-CH2O-，-CH2OCOO-，-CH2-O-CS-O-，-CH2-NR13-COO-，-CH2-N = CR14-O- 或-CH 2 -NH-CS-O-CH 2 -O-SO-O-; R 13是H，低级烷基，芳基，甲酰基甲基，-CH 2 CHOH-CH 2 OH或-CH 2 CH = N-NH-C（= NH）-NH 2; R 14是低级烷基或低级烷硫基。 当W1 / W2 = 0时，R1 = R2 = R3 = H; 当R 4为低级烷基时，氨基或-CH 2 CH 2 R 7，则W1 / W2为= O。 当Y是氨基甲酰氧基时，R1 = R2 = R3 = W1 = W2 = H，R4是氨基甲酰基，X是低级烷氧基羰基。 当R4为C1时，R1 = R2 = R3 = W1 = W2 = H，X为低级烷氧基羰基。 当X是H，甲酰基，-CONR 8 R 9，-CH 2 A或-CH = NR 12时，则R1 = R2 = R3 = W1 = W2 = R4 = H。 当X是-CONHOH时，则R1 = R2 = R3 = R4 = H。 = R4 = H。

    ENDOTHELIN-ANTAGONIZING PEPTIDE
    3.
    发明公开
    ENDOTHELIN-ANTAGONIZING PEPTIDE 失效
    内皮素增生肽。

    公开(公告)号：EP0679658A1

    公开(公告)日：1995-11-02

    申请号：EP95904339.9

    申请日：1994-06-23

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： SHIBATA, Kenji ,  SUZAWA, Toshiyuki ,  YAMASAKI, Motoo ,  TANAKA, Takeo ,  TSUKUDA, Eiji ,  YAMADA, Koji ,  OHNO, Tetsuji

    IPC分类号： C07K7/08 ,  C07K7/06

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K14/57536

    摘要： An endothelin-antagonizing peptide compound represented by general formula (I) and a pharmacologically acceptable salt thereof: R¹-R²-R³-R⁴-R⁵-R⁶-R⁷-R⁸-R⁹-R¹⁰-R¹¹-R¹²-Phe-R¹⁴-R¹⁵-R¹⁶-R¹⁷-R¹⁸-Ile-R²⁰-Z wherein R¹ is X¹-Gly, X³(a), X²-SCH₂CO or hydrogen; R² is Asn, Asp, Phe, Tyr, Ser or a single bond; R³ is Trp, Ile, Pro, Ala or a single bond; R⁴ is His, Lys, Gly, Trp, Ala or a single bond; R⁵ is Gly, Thr, Trp, Val or a single bond; R⁶ is Gly, Thr, Asn, Tyr, Asp or a single bond; R⁷ is Ala, Ser, Asn, Asp, Tyr, Phe or a single bond; R⁸ is Pro, Ala, Arg or a single bond; R⁹ is (b), (c) or a single bond; R¹⁰ is Trp or Ala; R¹¹ is Val, Pro or a single bond; R¹² is Tyr or a single bond; R¹⁴ is Ala, MeAla, Ser or Cys; R¹⁵ is His or Trp; R¹⁶ is Leu or Nva; R¹⁷ is Asp, Thr, Asn, Ser, Gly or Glu; R¹⁸ is Ile, Leu, Cha, Abu, Thi, Met, Tyr, MeLeu, MeIle, Phg or Nle; R²⁰ is Trp, Phe or Tyr; and Z is hydroxy, lower alkoxy or amino.

    摘要翻译： 由通式（I）表示的内皮素拮抗肽化合物及其药理学上可接受的盐：R 1 -R 2 -R 3 -R 4 -R 5 -R 6 - R 7 -R 8 -R 9 -R 1 -R 1 1 -R 1 -P-R 1 - 4 - R 1 -R 5 -R 6 -R 1 -R 7 -R 8 -Ile-R 2 -Z其中R 1是X X 3（a），X 2 -SCH 2 CO或氢; R 2是Asn，Asp，Phe，Tyr，Ser或单键; R 3是Trp，Ile，Pro，Ala或单键; R 4是His，Lys，Gly，Trp，Ala或单键; R 5是Gly，Thr，Trp，Val或单键; R 6是Gly，Thr，Asn，Tyr，Asp或单键; R 7是Ala，Ser，Asn，Asp，Tyr，Phe或单键; Pro，Ala，Arg或单键; R 9为（b），（c）或单键; R 1是Trp或Ala; R 1是Val，Pro或单键; R 1是Tyr或单键; R 1是Ala，MeAla，Ser或Cys; R 1 <5>是His或Trp; R 1是Leu或Nva; R 1是Asp，Thr，Asn，Ser，Gly或Glu; R 1是Ile，Leu，Cha，Abu，Thi，Met，Tyr，MeLeu，MeIle，Phg或Nle; R 2是Trp，Phe或Tyr; Z是羟基，低级烷氧基或氨基。

    IMIDAZOQUINAZOLINE DERIVATIVE
    4.
    发明公开
    IMIDAZOQUINAZOLINE DERIVATIVE 失效
    咪唑中和唑衍生物

    公开(公告)号：EP0668280A1

    公开(公告)日：1995-08-23

    申请号：EP94925621.8

    申请日：1994-09-02

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： MACHII, Daisuke ,  MATSUNO, Kenji ,  KINOSHITA, Iwao ,  NOMOTO, Yuji ,  TAKAI, Haruki ,  OHNO, Tetsuji ,  NAGASHIMA, Ken ,  ISHIKAWA, Tomoko ,  YAMADA, Koji ,  ICHIMURA, Michio ,  KASE, Kiroshi

    IPC分类号： C07D487/04 ,  A61K31/505

    CPC分类号： C07D487/04

    摘要： An imidazoquinazoline derivative represented by formula (I) or a pharmacologically acceptable salt thereof, wherein R 1 andR 2 may be the same or different from each other and each represents hydrogen, lower alkyl, lower alkenyl, aryl, etc.; R 3 represents hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aryl, etc.; and X represents O or S. This compound has a potent and selective cCMP-specific PDE inhibitor activity and is useful for treating or mitigating cardiovascular diseases such as thrombosis, angina pectoris, hypertension and arteriosclerosis, asthma, and so forth.

    摘要翻译： 由式（I）表示的咪唑并喹唑啉衍生物或其药学上可接受的盐，其中R 1和R 2可以相同或不同，各自表示氢，低级烷基，低级烯基，芳基等; R 3表示氢，低级烷基，环烷基，低级烯基，芳基等; X表示O或S.该化合物具有有效和选择性的cCMP特异性PDE抑制剂活性，可用于治疗或缓解心血管疾病如血栓形成，心绞痛，高血压和动脉硬化，哮喘等。

    IMIDAZOQUINAZOLINE DERIVATIVES
    6.
    发明公开
    IMIDAZOQUINAZOLINE DERIVATIVES 失效
    咪唑喹唑啉衍生物

    公开(公告)号：EP0758653A1

    公开(公告)日：1997-02-19

    申请号：EP96904302.5

    申请日：1996-03-01

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： ONODA, Yasuo ,  SASAKI, Shin-ichi ,  MACHII, Daisuke ,  TAKAI, Haruki ,  OHNO, Tetsuji ,  YAMADA, Koji ,  ICHIMURA, Michio ,  KASE, Hiroshi

    IPC分类号： C07D487/04 ,  A61K31/505

    CPC分类号： C07D487/04

    摘要： Imidazoquinazoline derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R 1 represents hydrogen, optionally substituted lower alkyl, etc.; R 2 and R 3 are the same or different and each represents hydrogen, optionally substituted lower alkyl, optionally substituted aralkyl, optionally substituted aryl, etc., or R 2 and R 3 together form an optionally substituted nitrogenous heterocycle; R 4 represents hydrogen or optionally substituted lower alkyl; X represents O or S; Y represents a single bond or O; and n is 0, 1, 2 or 3.

    摘要翻译： 由通式（I）表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐，其中R1代表氢，任选取代的低级烷基等; R2和R3相同或不同，并且各自代表氢，任选取代的低级烷基，任选取代的芳烷基，任选取代的芳基等，或者R2和R3一起形成任选取代的含氮杂环; R4代表氢或任选取代的低级烷基; X代表O或S; Y代表单键或O; 并且n是0,1,2或3。