公开(公告)号：US06500936B2

公开(公告)日：2002-12-31

申请号：US09784035

申请日：2001-02-16

申请人： Laszlo Vertesy ,  Klaus Ehrlich ,  Martin Knauf ,  Joachim Wink ,  Francis P. Barbone ,  Elaine A. Powers ,  Elizabeth A. Cashman

发明人： Laszlo Vertesy ,  Klaus Ehrlich ,  Martin Knauf ,  Joachim Wink ,  Francis P. Barbone ,  Elaine A. Powers ,  Elizabeth A. Cashman

IPC分类号： A61K3135

CPC分类号： C12R1/01 ,  C07H17/04 ,  C12P19/26 ,  C12P19/60

摘要： The invention relates to a compound of formula (I) wherein R1 is a sugar; R2 is —CH2—O—(R7)m, R7 representing a sugar, or is —COOH; R3 is an epoxide-comprising group, or is C1-C6-alkyl or C2-C6-alkenyl, unsubstituted or substituted by at least one OH; R5 is H, C1-C6-alkyl, C2-C6-alkenyl or C2-C6-alkynyl; R4R6, R8 and R10 independently of one another are H; C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, —X2H, or —X2R12, or R4 and R6 together and/or R8 and R10 together are =X2; X2 is O, NH, N—C1-C6-alkyl, N—C2-C6-alkenyl, N-C2-C6-alkynyl or S; R12 is C1-C6-alkyl, C2-C6—alkenyl, C2-C6-alkynyl, aryl or acyl; and m and n are 1 or 2; in any of its stereochemical forms and mixtures of these forms in any ratio, and a physiologically acceptable salt or derivative thereof. The compounds are obtainable from a culture of the microorganism Actinomycetales species HAG 003959, DSM 12931, by fermentation. Accordingly, the invention relates to a process for their preparation and to the use of the compounds as pharmaceuticals, for example as antitumor agents.

摘要翻译： 本发明涉及式（I）化合物，其中R1是糖; R2是-CH2-O-（R7）m，R7代表糖，或是-COOH; R3是含环氧化物的基团，或是未被取代或被至少一个OH取代的C1-C6-烷基或C2-C6-烯基; R5是H，C1-C6-烷基，C2-C6-烯基或C2-C6-炔基; R4R6，R8和R10彼此独立地为H; C1-C6-烷基，C2-C6-烯基，C2-C6-炔基，-X2H或-X2R12或R4和R6一起和/或R8和R10一起为= X2; X 2是O，NH，N-C 1 -C 6 - 烷基，N-C 2 -C 6 - 烯基，N-C 2 -C 6 - 炔基或S; R 12是C 1 -C 6烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基，芳基或酰基; m和n为1或2; 其任何立体化学形式和这些形式的任何比例的混合物及其生理上可接受的盐或其衍生物。 这些化合物可通过发酵从放线菌种类HAG 003959，DSM 12931的培养物中获得。 因此，本发明涉及其制备和使用化合物作为药物的方法，例如作为抗肿瘤剂。