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1. 发明授权

US4092335A Desalanyltetaine derivatives and the method for their preparation 失效
标题翻译：脱氨基甜菜碱衍生物及其制备方法
公开(公告)号：US4092335A
公开(公告)日：1978-05-30
申请号：US739347
申请日：1976-11-05
申请人： Wojciech Gruszecki , Edward Bordwski , Jerzy Gumieniak , Malgorzata Gumieniak , Maciej Smulkowski , Hanna Wojciechowska , Miroslaw Bobrowski
发明人： Wojciech Gruszecki , Edward Bordwski , Jerzy Gumieniak , Malgorzata Gumieniak , Maciej Smulkowski , Hanna Wojciechowska , Miroslaw Bobrowski
IPC分类号： A01N43/20 , C07D303/36 , C07D301/00 , A01N9/00
CPC分类号： C07D303/36 , A01N43/20
摘要： The subject of this invention are the desalanyltetaine derivatives of the formula 1, wherein R.sup.1 is a hydroxyl group or an arrangement of the formula 2, wherein R.sup.3 is a hydrogen atom or an alkyl, aryl, aralkyl group and X is an acyl or alkyl group, R.sup.2 is a hydrogen atom or an acyl group, and Z is an oxygen atom, hydroxylamine or hydrazine radical or their alkyl, aryl or aralkyl derivatives.The method of the preparation of the derivatives according to the invention consists in treating the desalanyltetaine derivatives of the formula 1, where R.sup.1 and R.sup.2 have the above mentioned significance, and Z is an oxygen atom with hydroxylamine, hydrazine or their derivatives. A modification of the method consists in treating the desalanyltetaine of the formula 1, where R.sup.2 and Z have the above mentioned significance, and R.sup.1 is a hydroxyl group with the chloroethers.Another modification of the method consists in the fact that the desalanyltetaine derivatives of the formula 1 where R.sup.1 and Z have the above mentioned significance and R.sup.2 is a hydrogen atom, are acylized by the proper carboxylic acids derivatives.The advantage of the derivatives according to the invention is a wide spectrum of their activity as well as their low toxity.
摘要翻译：本发明的主题是式1的脱烷基甜菜碱衍生物，其中R 1是羟基或式2的排列，其中R 3是氢原子或烷基，芳基，芳烷基，X是酰基或烷基 R2是氢原子或酰基，Z是氧原子，羟胺或肼基或它们的烷基，芳基或芳烷基衍生物。

2. 发明授权

US5942495A Antibiotics 失效
标题翻译：抗生素
公开(公告)号：US5942495A
公开(公告)日：1999-08-24
申请号：US857281
申请日：1997-05-16
申请人： Edward Borowski , Jolanta Grzybowska , Pawel Sowinski , Jerzy Gumieniak , Andrzej Czerwinski
发明人： Edward Borowski , Jolanta Grzybowska , Pawel Sowinski , Jerzy Gumieniak , Andrzej Czerwinski
IPC分类号： C07H17/08 , A61K31/71
CPC分类号： C07H17/08
摘要： The invention relates to an N-alkyl-N-glycosyl derivative of antifungal antibiotics of the polyene macrolide group of general formula 1(a), wherein M represents polyene macrolide antibiotics residues, R represents a variable part of sugar residue, R.sup.1 represents a C.sub.1-4 alkyl group and R.sup.2 represents hydrogen or a C.sub.1-4 alkyl group; their salts of general formula 2(a), wherein R, R.sup.1, R.sup.2 and M are as herein defined and A represents an anion of organic or inorganic acid. Compounds of formula 1(b) and 2(b) wherein the N-alkyl and alkyl ester groups are represented by methyl are of particular interest.The invention relates also to processes for preparation of the compounds, to compositions containing these compounds and to their use in therapy and the treatment of external and internal fungal infections in humans and animals. ##STR1##
摘要翻译：本发明涉及通式1（a）的多烯大环内酯类抗真菌抗生素的N-烷基-N-糖基衍生物，其中M表示多烯大环内酯抗生素残基，R表示糖残基的可变部分，R1表示C1 -4-烷基，R 2表示氢或C 1-4烷基; 其通式2（a）的盐，其中R，R 1，R 2和M如本文所定义，A代表有机或无机酸的阴离子。特别令人感兴趣的是其中N-烷基和烷基酯基由甲基表示的式1（b）和2（b）的化合物。本发明还涉及制备化合物的方法，含有这些化合物的组合物及其在治疗和治疗人和动物中的外部和内部真菌感染中的用途。

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