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1. 发明授权

EP0303697B1 DERIVATIVES OF PHYSIOLOGICALLY ACTIVE SUBSTANCE K-252 失效
标题翻译：生理活性剂K-252的衍生物
公开(公告)号：EP0303697B1
公开(公告)日：1997-10-01
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 (I) (wherein W1, W2, R1, R2, R3, R4, 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.

2. 发明公开

EP0383919A1 STAUROSPORIN DERIVATIVES 失效
标题翻译：星孢菌素衍。
公开(公告)号：EP0383919A1
公开(公告)日：1990-08-29
申请号：EP89901739.6
申请日：1989-01-30
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： MURAKATA, Chikara , SATO, Akira , KASAI, Masaji , MORIMOTO, Makoto , AKINAGA, Shiro
IPC分类号： C07D498/22
CPC分类号： C07D498/22 , A61K38/005 , C07D211/46 , C07D417/06 , C07D417/14 , C07K5/0227 , C07K5/06139
摘要： Novel staurosporin derivatives represented by formula (I) (wherein R 1 represents hydrogen, lower alkyl, formyl or amino, R 2 represents hydrogen, formyl, lower alkanoyl or a group formed by removing a hydroxy moiety from the carboxyl group of an a-amino acid whose amino group may optionally be protected, one of X 1 and X 2 represents hydrogen and the other represents hydrogen, hydroxy, lower alkoxy or lower alkylthio, or X' and X 2 are taken together to form oxygen, provided that, when R 1 and R 2 are both hydrogen atoms and one of X 1 and X 2 is hydrogen, the other represents a group other than hydrogen or hydroxy) and their pharmacologically acceptable salts are disclosed. These compounds inhibit protein kinase C and have a cell growth inhibiting activity.
摘要翻译：由式（I）表示的新型星形孢菌素衍生物（其中R 1表示氢，低级烷基，甲酰基或氨基，R 2表示氢，甲酰基，低级烷酰基或通过从羧基的羧基除去羟基而形成的基团其氨基可以任选被保护的α-氨基酸，X 1和X 2之一表示氢，另一个表示氢，羟基，低级烷氧基或低级烷硫基，或X 1和X 2 一起形成氧，条件是当R 1和R 2都是氢原子并且X 1和X 2中的一个是氢时，另一个表示氢或羟基以外的基团）并公开了其药理学上可接受的盐。这些化合物抑制蛋白激酶C并具有细胞生长抑制活性。

3. 发明公开

EP0303697A1 DERIVATIVES OF PHYSIOLOGICALLY ACTIVE SUBSTANCE K-252 失效
标题翻译： 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。

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