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11.发明授权Process for the preparation of 2,5-dideoxystreptamine and of a novel intermediate therefor 失效制备2,5-二隐球菌胺及其新型中间体的方法
公开(公告)号：US4178453A
公开(公告)日：1979-12-11
申请号：US869207
申请日：1978-01-13
IPC分类号： C07D231/54 , C07D231/00
CPC分类号： C07D231/54
摘要： The aminocyclitol 2,5-dideoxystreptamine may be prepared by a novel two-step synthesis from cis-4,8-dioxatricyclo [5.1.0.0.sup.3,5 ]octane. The aminocyclitol and a novel intermediate in the synthesis thereof are utilized by a Micromonospora inyoensis (M. inoyensis strain 1550F-1G NRRL 5742) for the elaboration of a novel antibacterial agent designated Mutamicin 2.
摘要翻译： 氨基环糊精2,5-二去甲卡必思胺可以通过从顺式-4,8-二氧杂三环[5.1.0.03,5]辛烷的新型两步合成制备。 氨基环醇和其合成中的新型中间体由微单孢菌（M.inoyensis菌株1550F-1G NRRL 5742）用于制备名为Mutamicin 2的新型抗菌剂。
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12.发明授权5-Deoxy-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, method for their use as antibacterial agents and compositions useful therefor 失效5-去氧-4,6-二-O-（氨基甲酰基）-1,3-二氨基胆碱酯，其制备方法，用作抗菌剂及其组合物的方法
公开(公告)号：US4053591A
公开(公告)日：1977-10-11
申请号：US701387
申请日：1976-06-30
IPC分类号： C07H15/234 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234 , Y10S435/863
摘要： 5-Deoxy-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, useful antibacterial agents, are prepared by the reaction of the corresponding 5-O-thioformyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitol having all amino functions and all primary and secondary hydroxyl groups protected, with an organotin hydride (preferably tri-n-butylstannane) in an inert aprotic solvent under an inert atmosphere at temperatures of at least about 100.degree. C, followed by removal of said hydroxyl and amino protecting groups.
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公开(公告)号：US4348516A
公开(公告)日：1982-09-07
申请号：US158850
申请日：1980-06-12
CPC分类号： C12R1/29 , C12P19/485
摘要： The microorganisms Micromonospora inyoensis 1550F-1G and M. purpurea strain 1124 each microbiologically convert tobramycin, kanamycin A, kanamycin B and dibekacin to their respective 3"-N-methyl and 3"-N-methyl-4"-C-methyl derivatives. The derivatives exhibit significant activity against representative gram positive and gram negative bacteria and may also be converted to other derivatives which have significant antibacterial activity.
摘要翻译： 微生物Micromonospora inyoensis 1550F-1G和M.peppurea菌株1124每个微生物转化妥布霉素，卡那霉素A，卡那霉素B和二卡西汀至其相应的3' - N-甲基和3“ - N-甲基-4'-C- 甲基衍生物。 该衍生物对代表性的革兰氏阳性细菌和革兰氏阴性细菌表现出显着的活性，并且还可以转化为具有显着抗菌活性的其它衍生物。
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公开(公告)号：US4117221A
公开(公告)日：1978-09-26
申请号：US734166
申请日：1976-10-20
申请人： Peter J. L. Daniels
发明人： Peter J. L. Daniels
IPC分类号： C07H15/234 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： Disclosed herein are novel 1-N-X-aminoglycoside anti-bacterial agents produced from antibiotics elaborated by species of the genus Micromonospora wherein X is a member selected from the group consisting of S-3-amino-2-hydroxypropionyl and S-4-amino-2-hydroxybutyryl and S-5-amino-2-hydroxypentanoyl. Also disclosed are novel intermediates in the production of the foregoing.
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15.发明授权5-Epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines, methods for their manufacture and intermediates useful therein, methods for their use as antibacterial agents and compositions useful therefor 失效5-EPI-4,6-DI-O-（氨基甲酰基）-2-脱氧酪氨酸蛋白酶，其制备方法及其有用的中间体，其用作抗细菌剂及其组合物的方法
公开(公告)号：US4000261A
公开(公告)日：1976-12-28
申请号：US611289
申请日：1975-09-08
申请人： Peter J. L. Daniels
发明人： Peter J. L. Daniels
IPC分类号： C07H15/234 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/22 , C07H15/234 , C07H15/236
摘要： 5-Epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines and 1-N-alkyl-5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines, valuable as antibacterial agents, are prepared from the corresponding 5-O-hydrocarbonsulfonyl (or substituted hydrocarbonsulfonyl)-4,6-di-O-(aminoglycosyl)-2-deoxystreptamine wherein amino and hydroxyl functions are protected by groups susceptible to reductive cleavage or to basic or mild acid hydrolysis, by the reaction thereof with dimethylformamide at elevated temperatures, followed by removal of the protecting groups. Alternatively, 5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines and their 1-N-alkyl derivatives are prepared by oxidation of the corresponding 4,6-di-O-(aminoglycosyl)-2-deoxystreptamine wherein the amino and hydroxyl functions other than the 5-hydroxyl function are protected by groups susceptible to reductive cleavage or to basic or mild acid hydrolysis, with ruthenium tetroxide, chromic acid in acetone or chromium trioxide-pyridine complex in methylene chloride, thence reaction of the thereby produced 5-dehydro-4,6-di-O-(aminoglycosyl)-2-deoxystreptamine or 1-N-alkyl derivative thereof (novel intermediates) with an alkali metal borohydride followed by removal of the amino and hydroxyl protecting groups.In addition to the foregoing, methods are described whereby the 1-N-alkyl-5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines are prepared from the corresponding 1-N-unsubstituted-5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines.Pharmaceutical compositions comprising 5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines or 1-N-alkyl-5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines elicit an antibacterial response in a warm blooded animal having a susceptible bacterial infection.
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16.发明授权Process for the preparation of 2,5-dideoxystreptamine and of a novel intermediate therefor 失效制备2,5-二隐球菌胺及其新型中间体的方法
公开(公告)号：US4092359A
公开(公告)日：1978-05-30
申请号：US443051
申请日：1974-02-15
IPC分类号： C07D231/54 , C07C91/14
CPC分类号： C07D231/54
摘要： The aminocyclitol 2,5-dideoxystreptamine may be prepared by a novel two-step synthesis from cis-4,8-dioxatricyclo [5.1.0.0.sup.3,5 ]octane. The aminocyclitol and a novel intermediate in the synthesis thereof are utilized by a Micromonospora inyoensis (M. inoyensis strain 155OF-1G NRRL 5742) for the elaboration of a novel antibacterial agent designated Mutamicin 2.
摘要翻译： 氨基环糊精2,5-二去甲卡必思胺可以通过从顺式-4,8-二氧杂三环[5.1.0.03,5]辛烷的新型两步合成制备。 氨基环醇和其合成中的新型中间体由微单孢菌（M.inoyensis菌株155F-1G NRRL 5742）用于制备称为Mutamicin 2的新型抗菌剂。
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17.发明授权6'-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their use as antibacterial agents and compositions useful therefor 失效6 {40-烷基-4,6-二-O-（氨基糖基）-1,3-二氨基二醇，其用作抗菌剂的方法及其用途
公开(公告)号：US4044123A
公开(公告)日：1977-08-23
申请号：US666715
申请日：1976-03-15
IPC分类号： C07H15/234 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234 , C07H15/236
摘要： Described are 6'-N-alkyl derivatives of antibacterially active 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols having a primary carbinamine at C-5' of which a preferred group are 6'-N-alkyl derivatives having 2 to 4 carbon atoms of 4-O-aminoglycosyl-6-O-garosaminyl-2-deoxystreptamines having a primary carbinamine at C-5', a particularly preferred compound being 6'-N-ethylsisomicin.The 6'-N-alkyl derivatives are prepared by the reaction of the corresponding 6'-N-unsubstituted aminoglycoside having protecting groups on all other amino functions with an aldehyde or a ketone, followed by the reaction in situ of the 6'-N-substituted intermediate thereby formed with a hydride reducing agent, then removal of any N-protecting groups.Pharmaceutical formulations comprising 6'-N-alkylaminoglycosides of the invention are described and the method for their use in treating bacterial infections.
摘要翻译： 描述了在C-5'具有主要元素的抗菌活性4,6-二-O-（氨基糖基）-1,3-二氨基二醇的6'-N-烷基衍生物，其中优选的基团是6'-N-烷基 具有C-5'的初级甲胺胺的4-O-氨基糖基-6-0-高酰胺基-2-脱氧神经胺具有2至4个碳原子的衍生物，特别优选的化合物是6'-N-乙基丙基肌氨酸。
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公开(公告)号：US3985727A
公开(公告)日：1976-10-12
申请号：US563046
申请日：1975-03-28
申请人： Peter J. L. Daniels
发明人： Peter J. L. Daniels
IPC分类号： C07H15/04 , C07H15/18 , C07H15/234 , C07H15/236 , C07H15/22
CPC分类号： C07H15/18 , C07H15/04 , C07H15/234
摘要： This disclosure relates to the preparation of certain gentamine derivatives, to their use as intermediates in the preparation of certain novel pseudotrisaccharides containing a gentamine moiety, and to the use of these pseudotrisaccharides as antibacterial agents.
摘要翻译： 本公开内容涉及某些香叶胺衍生物的制备，用作制备含有万古胺部分的某些新型假三糖的中间体以及将这些假三糖用作抗菌剂的用途。
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