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1. 发明授权

US4044123A 6'-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their use as antibacterial agents and compositions useful therefor 失效
标题翻译： 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
申请人： Peter J. L. Daniels , William N. Turner
发明人： Peter J. L. Daniels , William N. Turner
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。

2. 发明授权

US4284764A Process for the preparation of 5-fluoro-5-deoxy and 5-epi-fluoro-5-deoxy-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols and novel 5-fluoro-5-deoxy and 5-epi-fluoro-5-deoxy derivatives produced thereby 失效
标题翻译：制备5-氟-5-脱氧和5-表氟-5-脱氧-4,6-二-O-（氨基糖基）-1,3-二氨基二醇的方法和新的5-氟-5-脱氧和由此制备的5-表氟-5-脱氧衍生物
公开(公告)号：US4284764A
公开(公告)日：1981-08-18
申请号：US122097
申请日：1980-02-19
申请人： Peter J. L. Daniels , Dinanath Rane
发明人： Peter J. L. Daniels , Dinanath Rane
IPC分类号： C07H15/234 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234
摘要： A novel process whereby 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols are reacted with a dialkylaminosulfur trifluoride to produce novel 5-fluoro-5-deoxy and 5-epi-fluoro-5-deoxy-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitol antibacterial agents.
摘要翻译：将4,6-二-O-（氨基糖基）-1,3-二氨基环糊精与二烷基氨基三氟化硫反应以制备新的5-氟-5-脱氧和5-表氟-5-脱氧-4的新方法， 6-二-O-（氨基糖基）-1,3-二氨基环糊精抗菌剂。

3. 发明授权

US4283528A 1-N-aminohydroxyacyl derivatives of gentamicin B 失效
标题翻译：庆大霉素B的1-N-氨基羟基酰基衍生物
公开(公告)号：US4283528A
公开(公告)日：1981-08-11
申请号：US32808
申请日：1979-04-24
申请人： Peter J. L. Daniels , Tattanahalli L. Nagabhushan
发明人： Peter J. L. Daniels , Tattanahalli L. Nagabhushan
IPC分类号： C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/236
摘要： 1-N-(R-.beta.-amino-.alpha.-hydroxypropionyl) gentamicin B, 1-N-(R-.gamma.-amino-.alpha.-hydroxybutyryl) gentamicin B, 1-N-(R-.delta.-amino-.alpha.-hydroxyvaleryl) gentamicin B and the corresponding diastereoisomers derived from the respective S-aminohydroxy acids and the acid addition salts thereof exhibit substantial antibacterial activity, especially against strains of bacteria which are resistant to gentamicin B and acid addition salts thereof.
摘要翻译： 1-N-（R-β-氨基-α-羟基丙酰基）庆大霉素B，1-N-（R-γ-氨基-α-羟基丁酰基）庆大霉素B，1-N-（R-α-氨基-α-羟基戊酰基）庆大霉素B和衍生自相应的S-氨基羟酸及其酸加成盐的相应的非对映异构体表现出显着的抗菌活性，特别是抗庆大霉素B及其酸加成盐的细菌菌株。

4. 发明授权

US4234685A Microbiological methylation of aminoglycosyl-aminoglycosides 失效
标题翻译：氨基糖基 - 氨基糖苷类的微生物甲基化
公开(公告)号：US4234685A
公开(公告)日：1980-11-18
申请号：US51790
申请日：1979-06-25
申请人： Bong K. Lee , Gerald H. Wagman , Dinanath F. Rane , Joseph A. Marquez , Peter J. L. Daniels
发明人： Bong K. Lee , Gerald H. Wagman , Dinanath F. Rane , Joseph A. Marquez , Peter J. L. Daniels
IPC分类号： C12P19/48
CPC分类号： C12R1/29 , C12P19/485 , Y10S435/862 , Y10S435/867
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。

5. 发明授权

US4011390A Semi-synthetic aminocyclitol aminoglycoside antibiotics and methods for the preparation thereof 失效
标题翻译：半合成氨基磺酰胺氨基酰胺抗生素及其制备方法
公开(公告)号：US4011390A
公开(公告)日：1977-03-08
申请号：US476638
申请日：1974-06-05
申请人： Marvin J. Weinstein , Peter J. L. Daniels , Gerald H. Wagman , Raymond Testa
发明人： Marvin J. Weinstein , Peter J. L. Daniels , Gerald H. Wagman , Raymond Testa
IPC分类号： C07H15/236 , C07H15/22
CPC分类号： C07H15/236 , Y10S435/863
摘要： Micromonospora inyoensis strain 1550F-1G NRRL 5742 is incapable of producing antibiotics unless an aminocyclitol is added to the fermentation medium. When such a compound is added, mutamicins are produced, said mutamicins being analogs of known aminoglycoside antibiotics differing therefrom with respect to the aminocyclitol subunit.

6. 发明授权

US4000262A 5-Epi-amino and 5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines 1-N-alkyl-5-epi-amino and 1-N-alkyl-5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines 失效
标题翻译： 5-EPI-氨基和5-EPI-AZIDO-4,6-DI-O-（氨基甲酰基）-2,5-二羧基甲苯胺1-N-烷基-5-丙烯酰胺和1-N-烷基-5-EPI -AZIDO-4,6-DI-O-（氨基甲酰基）-2,5-二脱氧酪氨酸
公开(公告)号：US4000262A
公开(公告)日：1976-12-28
申请号：US611290
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： C07H15/234 , C07H15/22 , C07H15/236
摘要： 5-Epi-azido- and 5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines and 1-N-alkyl derivatives thereof, valuable as antibacterial agents, are prepared from the corresponding 5-O-hydrocarbonsulfonyl (or substituted hydrocarbonsulfonyl)-4,6-di-O-(aminoglycosyl)-2-deoxystreptamine wherein all other hydroxyl functions and all amino functions are protected, by the reaction thereof with an alkali metal azide in an organic solvent followed by the reaction of the resulting 5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamine with base to remove the protecting groups, or with hydrogen in the presence of a catalyst or with an alkali metal in liquid ammonia, and thence cleavage of any remaining hydroxyl and amino protecting groups in the thereby formed 5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamine or 1-N-alkyl derivative thereof.In addition to the foregoing, methods are described whereby the 1-N-alkyl-5-epi-azido and 1-N-alkyl-5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines are prepared from the corresponding 1-N-unsubstituted-5-epi-azido and 1-N-unsubstituted-5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines.Pharmaceutical compositions comprising 5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines, 1-N-alkyl-5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines, 5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines and 1-N-alkyl-5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines elicit an antibacterial response in a warm blooded animal having a susceptible bacterial infection.

7. 发明授权

US3984395A Method of isolating gentamicin C.sub.2a 失效
标题翻译：分离庆大霉素C（HD 2a
公开(公告)号：US3984395A
公开(公告)日：1976-10-05
申请号：US498495
申请日：1974-08-19
申请人： Peter J. L. Daniels , Joseph A. Marquez
发明人： Peter J. L. Daniels , Joseph A. Marquez
IPC分类号： C07H15/236 , C07H15/22
CPC分类号： C07H15/236 , Y10S435/863 , Y10S435/865
摘要： Fermentation of Micromono spora purpurea NRRL 2953 under controlled aerobic conditions produces a plurality of antibiotic substances including gentamicin C.sub.2a which has been heretofore unknown and unrecognized. A method of isolating said antibiotic is described as are the chemical and biological properties of the same.
摘要翻译：在受控的有氧条件下发酵微生物紫草NRRL 2953产生了许多抗生素物质，包括迄今为止未知和未被认识的庆大霉素C2a。描述了分离所述抗生素的方法是其化学和生物学特性。

8. 发明授权

US4178453A Process for the preparation of 2,5-dideoxystreptamine and of a novel intermediate therefor 失效
标题翻译：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
申请人： Peter J. L. Daniels , Mohammed M. N. Varchei
发明人： Peter J. L. Daniels , Mohammed M. N. Varchei
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。

9. 发明授权

US4053591A 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
标题翻译： 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
申请人： Peter J. L. Daniels , Stuart W. McCombie
发明人： Peter J. L. Daniels , Stuart W. McCombie
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.

10. 发明授权

US4002742A 1-N-alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, methods for their use as antibacterial agents, and compositions useful therefor 失效
标题翻译： 1-N-烷基-4,6-二 - （氨基糖基）-1,3-二氨基二醇，其制备方法，用作抗菌剂的方法及其用途
公开(公告)号：US4002742A
公开(公告)日：1977-01-11
申请号：US492998
申请日：1974-07-30
申请人： John J. Wright , Peter J. L. Daniels , Alan K. Mallams , Tattanahalli L. Nagabhushan
发明人： John J. Wright , Peter J. L. Daniels , Alan K. Mallams , Tattanahalli L. Nagabhushan
IPC分类号： C07H15/236 , A61K31/70
CPC分类号： C07H15/236
摘要： 1-N-Alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols, valuable as antibacterial agents, are prepared by treating an acid addition salt of a 4,6-di-(aminoglycosyl)-1,3-diamonocyclitol antibacterial agent in an inert solvent, preferably a protic solvent containing water, with one equivalent of a hydride donor reducing agent and with at least one equivalent of an aldehyde.The 1-N-alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols are also prepared by treating the corresponding 1-N-acyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitol with an amide-reducing hydride reagent in an inert organic solvent.Other methods of preparing 1-N-alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols include carrying out the foregoing processes with partially N-protected intermediates. Another useful process involves preparing a Schiff base of the 1-amino function of a partially N-protected 4,6-di-(aminoglycosyl)-1,3-diaminocyclitol followed by reduction of said Schiff base and removal of the N-protecting groups.Pharmaceutical compositions comprising 1-N-alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols are described as well as the method of using said compositions to elicit an antibacterial response in a warm blooded animal having a susceptible bacterial infection.
摘要翻译：通过将4,6-二（氨基糖基）-1,3-二氨基二（氨基糖基）-1,3-二氨基环己烷酸的酸加成盐处理，制备作为抗菌剂有价值的1-N-烷基-4,6-二（氨基糖基） - 二氨基环醇醇抗菌剂在惰性溶剂中，优选含有水的质子溶剂，与一当量的氢化物供体还原剂和至少一当量的醛。

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