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11. 发明授权

US5455241A Polycyclic compounds and processes for the preparation thereof 失效
标题翻译：多环化合物及其制备方法
公开(公告)号：US5455241A
公开(公告)日：1995-10-03
申请号：US309384
申请日：1994-09-20
申请人： Oskar Wacker
发明人： Oskar Wacker
IPC分类号： A61K31/40 , A61K31/55 , A61P9/10 , A61P17/00 , A61P35/00 , A61P43/00 , C07D207/04 , C07D273/06 , C07D309/12 , C07D311/22 , C07D498/22 , C07D273/00
CPC分类号： C07D498/22
摘要： N-(tetrahydropyran-4-yloxy-alkanoyl)-staurosporin derivatives of formula I ##STR1## wherein R.sub.1 is hydrogen, hydroxy, lower alkoxy or oxo,R.sub.2 is hydrogen or C.sub.1-4 alkyl andR.sub.3 is hydrogen or C.sub.1-4 alkyl,processes and novel intermediates for the preparation thereof and processes for the preparation of the intermediates are described. The compounds of formula I inhibit the enzyme protein kinase C with a high degree of selectivity and can be used especially as tumour-inhibiting active ingredients.
摘要翻译：式（I）的N-（四氢吡喃-4-基氧基 - 烷酰基） - 星孢菌素衍生物其中R 1是氢，羟基，低级烷氧基或氧代，R 2是氢或C 1-4烷基，R 3是氢或C 1-4烷基，其制备方法和新型中间体以及制备中间体的方法。式I的化合物以高选择性抑制酶蛋白激酶C，可以特别用作抑制肿瘤的活性成分。

12. 发明授权

US5264431A Polycyclic conjugates 失效
标题翻译：多环共轭物
公开(公告)号：US5264431A
公开(公告)日：1993-11-23
申请号：US973133
申请日：1992-11-06
申请人： Oskar Wacker , Peter Traxler
发明人： Oskar Wacker , Peter Traxler
IPC分类号： A61K31/70 , A61P35/00 , A61P43/00 , C07H9/06 , C07H15/26 , C07H19/02 , C12N9/99 , C07D498/22 , A61K31/55
CPC分类号： C07H19/02 , C07H15/26
摘要： Staurosporin derivatives of the formula I are described, ##STR1## in which R.sub.1 is hydrogen, hydroxyl, lower alkoxy or oxo and R.sub.2 is a radical of the formula II ##STR2## in which the configuration of the sugar moiety is derived from D-glucose, D-galactose or D-mannose, and R.sub.3 -R.sub.7 are as defined below.These compounds have a pronounced and selective inhibitory action on the enzyme proteinkinase C and have, inter alia, an antitumor action.
摘要翻译：描述了式I的星孢菌素衍生物，其中R1是氢，羟基，低级烷氧基或氧代，R2是式II的基团，其中糖部分的构型衍生自D-葡萄糖，D-半乳糖或D-甘露糖，R3-R7如下所定义。这些化合物对酶蛋白酶C具有显着和选择性的抑制作用，并且尤其具有抗肿瘤作用。

13. 发明授权

US4322419A Bicyclomycin derivatives, compositions thereof and process of use thereof 失效
标题翻译：双环霉素衍生物，其组合物及其使用方法
公开(公告)号：US4322419A
公开(公告)日：1982-03-30
申请号：US1996
申请日：1979-01-08
申请人： Beat Muller , Wilhelm Kump , Oskar Wacker
发明人： Beat Muller , Wilhelm Kump , Oskar Wacker
IPC分类号： C07D498/08 , A61K31/505 , A61P31/04 , C07H9/06 , A61K31/495
CPC分类号： C07H9/06
摘要： Derivatives of 5-norbicyclomycin of the formula ##STR1## wherein R represents an unsubstituted or substituted monovalent hydrocarbon radical in which one, two or more carbon atoms can be replaced by heteroatoms, and X represents a bivalent group of the formula --O-- or --N(R')--, wherein R' has one of the meanings assigned to R, whilst R and R', if both have a meaning which is different from hydrogen, can also be linked to each other through a C--C bond or an oxygen, sulphur or nitrogen atom, and corresponding compounds, in which at least one hydroxyl group is protected, and salts of said compounds, provided they contain salt-forming groups, are useful as antibiotics, especially against Enterobacteriaceae, or as intermediates for the production of such antibiotics. They are obtained by condensing a corresponding 5-norbicyclomycin-5-one with a compound of the formula R--X--NH.sub.2 in which X and R have the above meaning.
摘要翻译：其中R表示未被取代或取代的一价烃基，其中一个或两个以上碳原子可被杂原子代替，并且X表示式-O-或 - 的二价基团， N（R'） - ，其中R'具有分配给R的含义之一，而R和R'如果都具有不同于氢的含义，也可以通过CC键或氧相互连接，硫或氮原子，以及其中至少一个羟基被保护的相应化合物和所述化合物的盐，只要它们含有成盐基团，可用作抗生素，特别是对肠杆菌科的抗生素，或作为生产这样的抗生素。它们是通过将相应的5-降胆胺霉素-5-酮与式R-X-NH 2化合物缩合得到的，其中X和R具有上述含义。

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