专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US09273049B2 Method for increasing the solubility of nevirapine 有权
标题翻译：增加奈韦拉平溶解度的方法
公开(公告)号：US09273049B2
公开(公告)日：2016-03-01
申请号：US13509216
申请日：2010-11-09
申请人： Wilna Liebenberg , Nicole Stieger
发明人： Wilna Liebenberg , Nicole Stieger
IPC分类号： A61K9/00 , C07D471/14
CPC分类号： C07D471/14 , Y10T428/2982
摘要： The invention provides a method for increasing the solubility of nevirapine, including the steps of rendering nevirapine in a gaseous phase; and rendering the gaseous phase in a relatively more soluble solid particulate form. The invention further provides for a crystalline Form-VI (36) of nevirapine having an X-ray diffraction pattern of (2-theta values in degrees) 9.2953, 11.2023, 12.7019, 12.9796, 13.5273, 15.4670, 17.2597, 19.1038, 19.7267, 21.1303, 22.9381, 25.5589, 26.4913, 27.2150, 27.7283, 29.7134, and 33.8343 degrees two theta. The invention further provides for the preparation of microspherical and/or nanospherical Form-V (34) and crystalline Form-VI (36) of nevirapine as well as novel dosage forms including parenteral-, inhalant-, transdermal- and oral dosage forms.
摘要翻译：本发明提供了增加奈韦拉平的溶解度的方法，包括使奈韦拉平呈气相的步骤; 并使气相呈相对更可溶的固体颗粒形式。本发明进一步提供奈韦拉平的结晶形式VI（36），其具有（2-theta值，度）为9.2953,11.2023,12.7019,129.796,13.5273,15.4670,17.2597,9.1038,19.7267,21.1303的X射线衍射图，22.9381,25.5589,26.4913,27.2150,27.7283,29.7134和33.8343度2θ。本发明进一步提供了奈韦拉平的微球和/或纳米球形形式V（34）和晶型VI（36）的制备，以及包括肠胃外，吸入，经皮和口服剂型的新型剂型。

2. 发明申请

US20130102550A1 AMORPHOUS ROXITHROMYCIN COMPOSITION 有权
标题翻译：不规则的ROXITHROMYCIN组合物
公开(公告)号：US20130102550A1
公开(公告)日：2013-04-25
申请号：US13640643
申请日：2011-04-14
申请人： Wilna Liebenberg , Marique Aucamp
发明人： Wilna Liebenberg , Marique Aucamp
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： This invention relates to a macrolide composition, more particularly an amorphous form (Form-III) of 3R, 4S, 5S, 6R, 7R, 9R, 11S, 12R, 13S, 14R-6-[(2S, 3R, 4S, 6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7, 12, 13-trihydroxy-4-[(2R, 4R, 5S, 6S)-5-hydroxy-4-methoxy-4, 6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxy-imino)-3, 5, 7, 9, 11, 13-hexamethyl-1-oxacyclotetradecan-2-one or roxithromycin characterised by the absence of peaks in the infra-red spectrum of amorphous (Form-III) of roxithromycin at 3577.15; 3526.03; 3465.27 and 3276.24 cm-1 relative to the infra-red spectrum of the prior art roxithromycin raw material displaying peaks at 3577.15; 3526.03; 3465.27 and 3276.24 cm-1 and further characterised by an increased solubility of at least 50% over prior art anhydrous and monohydrated roxithromycin in acetate buffer (pH 4.5), phosphate buffer (pH 6.8) and water.
摘要翻译：本发明涉及大环内酯类组合物，更具体地说是3R，4S，5S，6R，7R，9R，11S，12R，13S，14R-6 - [（2S，3R，4S，6R ）-4-二甲基氨基-3-羟基-6-甲基恶唑-2-基]氧基-4-乙基-7,12,13-三羟基-4 - [（2R，4R，5S，6S）-5-羟基-4 （2-甲氧基乙氧基甲氧基 - 亚氨基）-3,5,7,9,11,11-六甲基-1-氧杂环十四烷-2-酮或罗红霉素，其特征在于在3577.15的罗红霉素的无定形（III型）的红外光谱中没有峰; 3526.03; 3465.27和3276.24cm-1相对于现有技术的罗红霉素原料的红外光谱在3577.15显示峰; 3526.03; 3465.27和3276.24cm-1，并且进一步的特征在于比现有技术的无水和一水合罗红霉素在乙酸盐缓冲液（pH 4.5），磷酸盐缓冲液（pH6.8）和水中的溶解度增加至少50％。

3. 发明授权

US08901089B2 Composition comprising an amorphous non-crystalline glass form of roxithromycin 有权
标题翻译：包含无定形非晶玻璃形式的罗红霉素的组合物
公开(公告)号：US08901089B2
公开(公告)日：2014-12-02
申请号：US13516864
申请日：2010-12-15
申请人： Wilna Liebenberg , Marique Aucamp , Melgardt M De Villiers
发明人： Wilna Liebenberg , Marique Aucamp , Melgardt M De Villiers
IPC分类号： A61K31/70 , C07H17/08 , C07H1/00
CPC分类号： C07H17/08 , C07H1/00
摘要： The invention relates to an amorphous non-crystalline glass form (Form-II) of 3R,4S,5S,6R,7R,9R,11S,12R,13S,14R-6-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-1-oxa-cyclotetradecan-2-one or roxithromycin having at least one characteristic infra-red spectrum peak at approximately 3580 to 3464 cm−1. The invention further relates to a preparation method of increasing the solubility of roxithromycin including the steps of selecting anhydrous roxithromycin or monohydrated roxithromycin; elevating the temperature of the roxithromycin to above the melting point thereof; and reducing the temperature of the melt sufficiently to allow it to set into an amorphous non-crystalline glass form (Form-II) of roxithromycin having relatively increased solubility without decreasing the stability of thereof.
摘要翻译：本发明涉及3R，4S，5S，6R，7R，9R，11S，12R，13S，14R-6 - [（2S，3R，4S，6R） - 4-二甲基氨基-3-羟基-6-甲基氧基-2-基]氧基-14-乙基-7,12,13-三羟基-4 - [（2R，4R，5S，6S）-5-羟基-4-甲氧基 -4,6-二甲基氧基-2-基]氧基-10-（2-甲氧基乙氧基甲氧基亚氨基）-3,5,7,9,11,13-六甲基-1-氧杂环十四烷-2-酮或具有至少一个特征红外光谱峰在约3580至3464厘米-1。本发明还涉及增加罗红霉素溶解度的制备方法，包括选择无水罗红霉素或一水合罗红霉素的步骤; 将罗红霉素的温度升高到其熔点以上; 并充分降低熔体的温度，使其能够固化成具有相对增加的溶解度而不降低其稳定性的罗红霉素的无定形非晶玻璃形式（II型）。

4. 发明申请

US20130059805A1 COMPOSITION COMPRISING AN AMORPHOUS NON-CRYSTALLINE GLASS FORM OF AZITHROMYCIN 审中-公开
标题翻译：包含无定形非结晶玻璃形式的组合物
公开(公告)号：US20130059805A1
公开(公告)日：2013-03-07
申请号：US13516942
申请日：2010-12-15
申请人： Roelf Willem Odendaal , Wilna Liebenberg , Marique Aucamp
发明人： Roelf Willem Odendaal , Wilna Liebenberg , Marique Aucamp
IPC分类号： C07H17/08 , A61P31/04 , A61K31/7052
CPC分类号： C07H17/08 , C07H1/00
摘要： The invention relates to an amorphous non-crystalline glass form (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-15-oxo-11-{[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy}-1-oxa-6-azacyclopentadec-13-yl 2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranoside or azithromycin having an infra-red pattern displaying characteristic relatively broad peaks at approximately 3500 and 1727 cm−1 and characteristic peaks at approximately 2970 and 2938 cm−1. The invention further relates to a preparation method of increasing the solubility of azithromycin including the steps of selecting anhydrous, monohydrated or dihydrated azithromycin; elevating the temperature of the azithromycin to above the melting point thereof; and reducing the temperature of the melt sufficiently to allow it to set into an amorphous non-crystalline glass form (Form-II) of azithromycin having relatively increased solubility without decreasing the structural stability thereof.
摘要翻译：本发明涉及无定形非结晶玻璃形式（2R，3S，4R，5R，8R，10R，11R，12S，13S，14R）-2-乙基-3,4,10-三羟基-3,5,6 ，8,10,12,14-七甲基-15-氧代-11 - {[3,4,6-三脱氧-3-（二甲基氨基） - 乙酸-D-木糖 - 六吡喃糖基]氧基} -1-氧杂-6 - 十八烷基十六烷基-13-基-2,6-二脱氧-3-C-甲基-3-O-甲基-α-L-核糖 - 六吡喃糖苷或阿奇霉素，其具有在大约3500和1727cm处显示特征相对宽峰的红外图案 -1和特征峰在约2970和2938厘米-1。本发明还涉及增加阿奇霉素的溶解度的制备方法，包括选择无水，一水合或二水合阿奇霉素的步骤; 将阿奇霉素的温度升高到其高于其熔点的温度; 并充分降低熔体的温度，使其能够固化成具有相对增加的溶解度的阿奇霉素的无定形非晶玻璃形式（II型），而不降低其结构稳定性。

5. 发明申请

US20130143872A1 INJECTABLE FORMULATION OF A REVERSE TRANSCRIPTASE INHIBITOR FOR THE TREATMENT CANCER 审中-公开
标题翻译：用于治疗癌症的逆转录酶抑制剂的注射剂配方
公开(公告)号：US20130143872A1
公开(公告)日：2013-06-06
申请号：US13696472
申请日：2011-05-31
申请人： Nicole Stieger , Wilna Liebenberg , Melgardt Melvin De Villiers , Mino Rodolfo Caira
发明人： Nicole Stieger , Wilna Liebenberg , Melgardt Melvin De Villiers , Mino Rodolfo Caira
IPC分类号： A61K9/00
CPC分类号： A61K9/0019 , A61K31/551 , A61K31/7072 , A61K47/10
摘要： This invention relates to a composition formulated into a parenteral or injectable dosage form for the treatment of cancer, more particularly, this invention relates to a composition formulated into a parenteral dosage form suitable for administration in and around cancerous tissue, the composition including: a pharmaceutically acceptable solvent including from 20% to 100% ethanol (V/V); and a reverse transcriptase inhibitor exhibiting an anti-cancer effect, dissolved in the solvent.
摘要翻译：本发明涉及配制成用于治疗癌症的胃肠外或可注射剂型的组合物，更具体地说，本发明涉及配制成适于在癌组织内和周围施用的肠胃外剂型的组合物，所述组合物包括：药学上包括20％至100％乙醇（V / V）的可接受溶剂; 和表现出抗癌作用的逆转录酶抑制剂，溶解在溶剂中。

6. 发明授权

US08951977B2 Amorphous roxithromycin composition 有权
标题翻译：无定形罗红霉素组合物
公开(公告)号：US08951977B2
公开(公告)日：2015-02-10
申请号：US13640643
申请日：2011-04-14
申请人： Wilna Liebenberg , Marique Aucamp
发明人： Wilna Liebenberg , Marique Aucamp
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/08
摘要： This invention relates to a macrolide composition, more particularly an amorphous form (Form-III) of 3R, 4S, 5S, 6R, 7R, 9R, 11S, 12R, 13S, 14R-6-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecan-2-one or roxithromycin characterized by the absence of peaks in the infra-red spectrum of amorphous (Form-I11) of roxithromycin at 3577.15; 3526.03; 3465.27 and 3276.24 cm-1 relative to the infra-red spectrum of the prior art roxithromycin raw material displaying peaks at 3577.15; 3526.03; 3465.27 and 3276.24 cm-1 and further characterized by an increased solubility of at least 50% over prior art anhydrous and monohydrated roxithromycin in acetate buffer (pH 4.5), phosphate buffer (pH 6.8) and water.
摘要翻译：本发明涉及大环内酯类组合物，更具体地说是3R，4S，5S，6R，7R，9R，11S，12R，13S，14R-6 - [（2S，3R，4S，6R ）-4-二甲基氨基-3-羟基-6-甲基氧基-2-基]氧基-14-乙基-7,12,13-三羟基-4 - [（2R，4R，5S，6S）-5-羟基-4 - 甲氧基-4,6-二甲基氧基-2-基]氧基-10-（2-甲氧基乙氧基甲氧基亚氨基）-3,5,7,9,11,13-六甲基-1-氧杂环十四烷-2-酮或罗红霉素，其特征在于不存在在3577.15的罗红霉素的无定形（Form-I11）的红外光谱中的峰值; 3526.03; 3465.27和3276.24cm-1相对于现有技术的罗红霉素原料的红外光谱在3577.15显示峰; 3526.03; 3465.27和3276.24cm-1，并且进一步的特征在于比现有技术的无水和一水合罗红霉素在乙酸盐缓冲液（pH 4.5），磷酸盐缓冲液（pH6.8）和水中的溶解度增加至少50％。

7. 发明申请

US20130039987A1 METHOD FOR INCREASING THE SOLUBILITY OF A TRANSCRIPTASE INHIBITOR COMPOSITION 有权
标题翻译：增加转录酶抑制剂组合物溶解性的方法
公开(公告)号：US20130039987A1
公开(公告)日：2013-02-14
申请号：US13509216
申请日：2010-11-09
申请人： Wilna Liebenberg , Nicole Stieger
发明人： Wilna Liebenberg , Nicole Stieger
IPC分类号： C07D471/14 , C23C16/44 , A61P37/00 , A61K9/14 , A61K31/551
CPC分类号： C07D471/14 , Y10T428/2982
摘要： The invention provides a method for increasing the solubility of nevirapine, including the steps of rendering nevirapine in a gaseous phase; and rendering the gaseous phase in a relatively more soluble solid particulate form. The invention further provides for a crystalline Form-VI (36) of nevirapine having an X-ray diffraction pattern of (2-theta values in degrees) 9.2953, 11.2023, 12.7019, 12.9796, 13.5273, 15.4670, 17.2597, 19.1038, 19.7267, 21.1303, 22.9381, 25.5589, 26.4913, 27.2150, 27.7283, 29.7134, and 33.8343 degrees two theta. The invention further provides for the preparation of microspherical and/or nanospherical Form-V (34) and crystalline Form-VI (36) of nevirapine as well as novel dosage forms including parenteral-, inhalant-, transdermal- and oral dosage forms.
摘要翻译：本发明提供了增加奈韦拉平的溶解度的方法，包括使奈韦拉平呈气相的步骤; 并使气相呈相对更可溶的固体颗粒形式。本发明进一步提供奈韦拉平的结晶形式VI（36），其具有（2-theta值，度）为9.2953,11.2023,12.7019,129.796,13.5273,15.4670,17.2597,9.1038,19.7267,21.1303的X射线衍射图，22.9381,25.5589,26.4913,27.2150,27.7283,29.7134和33.8343度2θ。本发明进一步提供奈韦拉平的微球和/或纳米球形形式V（34）和晶型VI（36）的制备，以及包括肠胃外，吸入，经皮和口服剂型的新型剂型。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式