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1. 发明授权

US5593970A Heterocyclic anthracycline analogs 失效
标题翻译：杂环蒽环类似物
公开(公告)号：US5593970A
公开(公告)日：1997-01-14
申请号：US263925
申请日：1994-06-20
申请人： Giorgio Attardo , Jean-Louis Kraus , Marc Courchesne , Serge Lamonthe , Jean-Fran.cedilla.ois Lavall ee , Elaine Lebeau , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Bernard Belleau, deceased
发明人： Giorgio Attardo , Jean-Louis Kraus , Marc Courchesne , Serge Lamonthe , Jean-Fran.cedilla.ois Lavall ee , Elaine Lebeau , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Bernard Belleau, deceased
IPC分类号： C07H3/06 , C07H15/244 , C07M15/24 , A61K31/70
CPC分类号： C07H15/244 , C07H3/06
摘要： Novel pyrano heterocyclic anthracycline derivatives are described, which are useful in the treatment of cancer and tumors, such as breast cancer, leukemia, lung cancer, colon cancer, ovarian cancer, renal cancer, and melanoma. As well, these compounds may be used ex vivo for the treatment of cancerous bone marrow before retransplanting said marrow in a patient. Pharmaceutical compositions and methods of preparing the compounds are also described.
摘要翻译：描述了新的吡喃杂环蒽环类衍生物，其可用于治疗癌症和肿瘤，例如乳腺癌，白血病，肺癌，结肠癌，卵巢癌，肾癌和黑素瘤。同样，这些化合物也可以离体用于治疗癌性骨髓，然后再将患者骨髓再次移植。还描述了制备化合物的药物组合物和方法。

2. 发明授权

US5625043A Anthracyclines with unusually high activity against cells resistant to doxorubicin and its analogs 失效
标题翻译：蒽环类药物对抗多柔比星及其类似物的细胞具有异常高的活性
公开(公告)号：US5625043A
公开(公告)日：1997-04-29
申请号：US396290
申请日：1995-02-27
申请人： Waldemar Priebe , Piotr Skibicki , Roman Perez-Soler
发明人： Waldemar Priebe , Piotr Skibicki , Roman Perez-Soler
IPC分类号： C07H15/252 , C07M15/24
CPC分类号： C07H15/252
摘要： The present disclosure details novel modified anthracyclines, the synthesis thereof, and their use in treating patients with tumors. Preferred aspects of the disclosure involve modified anthracyclines which have an O-substituted aromatic ring on their sugar moiety. Other preferred aspects of the disclosure involve synthesis steps wherein a hydroxyl group on a sugar moiety to be added is blocked with a halo-substituted alkyl group during the process of adding it to an anthracycline ring compound.
摘要翻译：本发明详述了新型改性蒽环类药物的合成及其在治疗肿瘤患者中的用途。本公开的优选方面涉及在其糖部分上具有O-取代的芳环的修饰的蒽环类。本公开的其它优选方面涉及其中待添加的糖部分上的羟基在其加入蒽环类化合物的过程中被卤代烷基取代的合成步骤。

3. 发明授权

US5602108A Semisynthetic diastereomerically pure N-glycidylanthracyclines, a process for the stereoselective preparation thereof as the use thereof as cytostatics 失效
标题翻译：半合成非对映异构体纯的N-缩水甘油环内酯，其作为细胞抑制剂的用途的立体选择性制备方法
公开(公告)号：US5602108A
公开(公告)日：1997-02-11
申请号：US464468
申请日：1995-06-05
申请人： Manfred Gerken , Monika Grimm , Ernst Raab , Dieter Hoffmann , Reiner Straub
发明人： Manfred Gerken , Monika Grimm , Ernst Raab , Dieter Hoffmann , Reiner Straub
IPC分类号： A61K31/65 , A61K31/70 , A61K31/704 , A61P35/00 , C07B53/00 , C07C15/62 , C07C50/36 , C07H15/252 , C07H15/26 , A61K37/00 , C07M15/24
CPC分类号： C07H15/26 , C07H15/252
摘要： Semisynthetic diastereomerically pure N-glycidylanthracyclines, a process for the stereoselective preparation thereof and the use thereof as cytostatics. The invention relates to anthracyclines having cytostatic activity and the formula I, which are, where appropriate, in the form of a salt with an inorganic or organic acid, ##STR1## in which R.sup.1 is hydrogen or a hydroxyl group,R.sup.2 is hydrogen, a hydroxyl group or an alkyloxy group (C.sub.1 -C.sub.4),R.sup.3 is hydrogen, a hydroxyl group or a structure of the formula II ##STR2## R.sup.4 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH,R.sup.5 is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula II,R.sup.6 is hydrogen, an alkyl group (C.sub.1 -C.sub.4), an allyl group, a benzyl group or mono- or di-methyloxy-substituted benzyl group, a tetrahydropyranyl group,R.sup.7 is hydrogen, an alkyl group (C.sub.1 -C.sub.4), an allyl group, a benzyl group or mono- or di-methyloxy-substituted benzyl group andR.sup.8 is a structure of the formula III or IV ##STR3## and to a process for the preparation of these compounds, which comprises reacting an anthracycline derivative of the structure I in whichR.sup.1, R.sup.2 and R.sup.4 are as defined above, andR.sup.3 is hydrogen, a hydroxyl group or a structure of the formula V ##STR4## R.sup.5 is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula V andR.sup.6 and R.sup.7 are as defined above, with (R)- or (S)-glycidyl sulfonate.
摘要翻译：半合成非对映体纯N-缩水甘油环素，其立体选择性制备方法及其作为细胞抑制剂的用途。本发明涉及具有细胞抑制活性的蒽环类抗生素和式I，它们在适当的情况下为无机或有机酸形式的盐，其中R 1为氢或羟基，R 2为氢，羟基或烷氧基（C 1 -C 4），R 3是氢，羟基或式II的结构。R 4是CH 2 CH 3，COCH 3，COCH 2 OH，CHOHCH 3或CHOHCH 2 OH，R 5是氢，羟基，甲氧基羰基或式II的结构，R6是氢，烷基（C1-C4），烯丙基，苄基或单 - 或二 - 甲氧基取代的苄基，四氢吡喃基，R7是氢，烷基（C1-C4），烯丙基，苄基或单 - 或二 - 甲氧基取代的苄基，R8是式III或IV的结构，IV和一种制备这些化合物的方法，其包括使结构I的蒽环衍生物与其中R 1，R 2和/ R 4如上定义，并且R 3是氢，羟基或式V R 5的结构是氢，羟基，甲氧基羰基或式V和R 6和R 7的结构如上定义（R） - 或（S） - 磺酰基磺酰基。

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