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公开(公告)号：US06329345B1
公开(公告)日：2001-12-11
申请号：US09442530
申请日：1999-11-18
申请人： Robert J. Rafka , Barry J. Morton , Colman B. Ragan , Peter Bertinato , John P. Dirlam , Alan E. Blize , Carl B. Ziegler
发明人： Robert J. Rafka , Barry J. Morton , Colman B. Ragan , Peter Bertinato , John P. Dirlam , Alan E. Blize , Carl B. Ziegler
IPC分类号： A61K3170
CPC分类号： C07H17/08 , A61K31/7052 , C07H17/00
摘要： The invention relates to a method of preparing compounds of the formula 1 and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial protozoa infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.
摘要翻译： 本发明涉及制备式1化合物及其药学上可接受的盐的方法。 式1的化合物是可用于治疗各种细菌和原生动物感染的抗菌剂。 本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物来治疗细菌原生动物感染的方法。本发明还涉及制备式1化合物的方法和用于此类制备的中间体。
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公开(公告)号：US06583274B1
公开(公告)日：2003-06-24
申请号：US09563792
申请日：2000-05-02
IPC分类号： C07H1708
摘要： Novel crystalline forms of a compound of Formula 1 are disclosed: Also disclosed are pharmaceutical compositions comprising these forms, and methods of their preparation and use.
摘要翻译： 公开了式1化合物的新型结晶形式：还公开了包含这些形式的药物组合物及其制备和使用方法。
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3.发明授权Diphosphate salt of A 4″-substituted-9-deoxo-9A-AZA-9A-homoerythromycin derivative and its pharmaceutical composition 失效A 4“ - 取代-9-脱氧-9A-AZA-9A-高红霉素衍生物的二磷酸盐及其药物组合物公开(公告)号：US06861412B2
公开(公告)日：2005-03-01
申请号：US10218154
申请日：2002-08-12
IPC分类号： C07H17/00 , A61K31/439 , A61K31/7052 , A61P1/08 , A61P31/04 , A61P33/02 , C07D453/02 , C07H17/08 , A01N43/04 , A61K31/70
摘要： This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[[2,6-dideoxy-3-C-methyl-3-o-methyl-4-C-[(propylamino)methyl]-α-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.
摘要翻译： 本发明涉及（2R，3S，4R，5R，8R，10R，11R，12S，13S，14R）-13 - [[2,6-二脱氧-3-C-甲基-3- 邻 - 甲基-4-C - [（丙基氨基）甲基]-α-L-核 - 六氢肉豆蔻酰基]氧基] -2-乙基-3,4,10-三羟基-3,5,8,10,12,14- 六甲基-11 - [[3,4,6-三脱氧-3-（二甲基氨基） - D-xylo-hexopyranosyl]氧基] -1-氧杂-6-氮杂环十五烷-15-可用作抗菌和抗原生动物 哺乳动物代理。 本发明还涉及含有二磷酸盐的游离碱的药物组合物和通过向需要这种治疗的哺乳动物施用二磷酸的游离碱来治疗哺乳动物的细菌和原生动物感染的方法。 本发明的二磷酸盐的游离碱在通过胃肠外施用于哺乳动物时具有针对各种细菌和原生动物感染的有效活性。
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4.发明授权Diphosphate salt of a 4″-substituted-9-deoxo-9A-AZA-9A- homoerythromycin derivative and its pharmaceutical composition 失效4“ - 取代-9-脱氧-9A-AZA-9A-高红霉素衍生物的二磷酸盐及其药物组合物公开(公告)号：US06465437B1
公开(公告)日：2002-10-15
申请号：US09574160
申请日：2000-05-18
IPC分类号： A01N4304
摘要： This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[[2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(propylamino)methyl]-&agr;-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-&bgr;-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.
摘要翻译： 本发明涉及（2R，3S，4R，5R，8R，10R，11R，12S，13S，14R）-13 - [[2,6-二脱氧-3-C-甲基-3- O-甲基-4-C - [（丙基氨基）甲基]-α-L-核 - 六羟基甲硅烷基]氧基] -2-乙基-3,4,10-三羟基-3,5,8,10,12,14- 六甲基-11 - [[3,4,6-三脱氧-3-（二甲基氨基） - D-xylo-hexopyranosyl]氧基] -1-氧杂-6-氮杂环十五烷-15-可用作抗细菌和抗原生动物 哺乳动物代理。 本发明还涉及含有二磷酸盐的游离碱的药物组合物和通过向需要这种治疗的哺乳动物施用二磷酸的游离碱来治疗哺乳动物的细菌和原生动物感染的方法。 本发明的二磷酸盐的游离碱在通过胃肠外施用于哺乳动物时具有针对各种细菌和原生动物感染的有效活性。
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5.发明授权Diphosphate salt of a 4″—substituted-9-deoxo-9 A—AZA—homoerythromycin derivatives and its pharmaceutical composition 失效4“ - 取代-9-脱氧-9A-AZA-高红霉素衍生物的二磷酸盐及其药物组合物公开(公告)号：US07297682B2
公开(公告)日：2007-11-20
申请号：US10840529
申请日：2004-05-06
摘要： This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[[2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(propylamino)methyl]-α-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.
摘要翻译： 本发明涉及（2R，3S，4R，5R，8R，10R，11R，12S，13S，14R）-13 - [[2,6-二脱氧-3-C-甲基-3- O-甲基-4-C - [（丙基氨基）甲基]-α-L-核 - 六羟基甲硅烷基]氧基] -2-乙基-3,4,10-三羟基-3,5,8,10,12,14- 六甲基-11 - [[3,4,6-三脱氧-3-（二甲基氨基） - D-xylo-hexopyranosyl]氧基] -1-氧杂-6-氮杂环十五烷-15-可用作抗菌和抗原生动物 哺乳动物代理。 本发明还涉及含有二磷酸盐的游离碱的药物组合物和通过向需要这种治疗的哺乳动物施用二磷酸的游离碱来治疗哺乳动物的细菌和原生动物感染的方法。 本发明的二磷酸盐的游离碱在通过胃肠外施用于哺乳动物时具有针对各种细菌和原生动物感染的有效活性。
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