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公开(公告)号：US20070129282A1
公开(公告)日：2007-06-07
申请号：US10877911
申请日：2004-06-24
申请人： Clarence Ahlem , James Frincke , Luis Daniel Carvalho , William Heggie , Patrick Prendergast , Christopher Reading , Krupakar Thadikonda , Russell Vernon
发明人： Clarence Ahlem , James Frincke , Luis Daniel Carvalho , William Heggie , Patrick Prendergast , Christopher Reading , Krupakar Thadikonda , Russell Vernon
IPC分类号： A61K38/22 , A61K31/704 , A61K31/58 , A61K31/66 , A61K31/56
CPC分类号： C07J1/0011 , A61K31/56 , C07J1/0025 , C07J31/003 , C07J31/006 , Y02A50/411
摘要： The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
摘要翻译： 本发明提供包含式1类固醇的组合物，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮半水合物和一种或多种赋形剂，包括包含低于约3％v / v水的液体制剂的组合物 。 该组合物可用于制备改进的药物制剂。 本发明还提供了间歇给药类固醇化合物的方法，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮的类似物和可用于这种给药方案的组合物。 本发明进一步提供抑制病原体复制，改善与免疫调节异常有关的症状并使用该化合物调节受试者的免疫应答的组合物和方法。 本发明还提供了制备和使用这些免疫调节组合物和制剂的方法。
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公开(公告)号：US20070275936A1
公开(公告)日：2007-11-29
申请号：US11564026
申请日：2006-11-28
申请人： Clarence Ahlem , James Frincke , Luis Carvalho , William Heggie , Patrick Prendergast , Christopher Reading , Krupakar Thadikonda , Russell Vernon
发明人： Clarence Ahlem , James Frincke , Luis Carvalho , William Heggie , Patrick Prendergast , Christopher Reading , Krupakar Thadikonda , Russell Vernon
CPC分类号： C07J1/0011 , A61K31/56 , C07J1/0025 , C07J31/003 , C07J31/006 , Y02A50/411
摘要： The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
摘要翻译： 本发明提供包含式1类固醇的组合物，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮半水合物和一种或多种赋形剂，包括包含低于约3％v / v水的液体制剂的组合物 。 该组合物可用于制备改进的药物制剂。 本发明还提供了间歇给药类固醇化合物的方法，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮的类似物和可用于这种给药方案的组合物。 本发明进一步提供抑制病原体复制，改善与免疫调节异常有关的症状并使用该化合物调节受试者的免疫应答的组合物和方法。 本发明还提供了制备和使用这些免疫调节组合物和制剂的方法。
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公开(公告)号：US20060079492A1
公开(公告)日：2006-04-13
申请号：US11234675
申请日：2005-09-23
申请人： Clarence Ahlem , Christopher Reading , James Frincke , Dwight Stickney , Henry Lardy , Padma Marwah , Ashok Marwah , Patrick Prendergast
发明人： Clarence Ahlem , Christopher Reading , James Frincke , Dwight Stickney , Henry Lardy , Padma Marwah , Ashok Marwah , Patrick Prendergast
IPC分类号： A61K31/57
CPC分类号： A61K31/57 , A61K9/0019 , A61K31/343 , A61K47/34 , A61K47/44
摘要： The invention relates to the use of compounds to treat a number of conditions, such as thrombocytopenia, neutropenia or the delayed effects of radiation therapy. Compounds that can be used in the invention include methyl-2,3,4-trihydroxy-1-O-(7,17-dioxoandrost-5-ene-3β-yl)-β-D-glucopyranosiduronate, 16α,3α-dihydroxy-5α-androstan-17-one or 3,7,16,17-tetrahydroxyandrost-5-ene, 3,7,16,17-tetrahydroxyandrost-4-ene, 3,7,16,17-tetrahydroxyandrost-1-ene or 3,7,16,17-tetrahydroxyandrostane that can be used in the treatment method.
摘要翻译： 本发明涉及化合物用于治疗诸如血小板减少症，中性粒细胞减少症或辐射治疗的延迟作用的许多病症的用途。 可用于本发明的化合物包括甲基-2,3,4-三羟基-1-O-（7,17-二氧雄甾-5-烯-3β-基）-β-D-吡喃葡萄糖醛酸呃酯，16α，3α-二羟基 -5α-雄甾烷-17-酮或3,7,16,17-四羟基雄甾-5-烯，3,7,16,17-四羟基雄甾-4-烯，3,7,16,17-四羟基雄甾-1-烯 或可用于治疗方法的3,7,16,17-四羟基雄甾烷。
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公开(公告)号：US20050159366A1
公开(公告)日：2005-07-21
申请号：US10890490
申请日：2004-07-13
IPC分类号： A61K31/56 , A61K31/565 , C07J1/00 , C07J3/00 , A61K38/04 , A61K31/704 , A61K31/695 , A61K31/66
CPC分类号： A61K31/565 , A61K9/0019 , A61K9/0031 , A61K9/127 , A61K31/56 , A61K31/568 , A61K31/5685 , C07J1/00 , C07J1/0011 , C07J3/005 , Y02A50/402 , Y02A50/409 , Y02A50/411 , Y02A50/415 , Y02A50/423 , Y02A50/475 , Y02A50/478 , Y02A50/481 , A61K2300/00
摘要： The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
摘要翻译： 本发明提供包含式1类固醇的组合物，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮半水合物和一种或多种赋形剂，通常其中组合物包含少于约3％的水。 该组合物可用于制备改进的药物制剂。 本发明还提供了间歇给药类固醇化合物的方法，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮的类似物和可用于这种给药方案的组合物。 本发明进一步提供抑制病原体（病毒）复制，改善与免疫失调相关的症状并使用某些类固醇和类固醇类似物调节受试者的免疫应答的组合物和方法。 本发明还提供了制备和使用这些免疫调节组合物和制剂的方法。
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公开(公告)号：US20050282732A1
公开(公告)日：2005-12-22
申请号：US10876957
申请日：2004-06-24
CPC分类号： A61K31/565 , A61K9/0019 , A61K9/0031 , A61K9/127 , A61K31/56 , A61K31/568 , A61K31/5685 , C07J1/00 , C07J1/0011 , C07J3/005 , Y02A50/402 , Y02A50/409 , Y02A50/411 , Y02A50/415 , Y02A50/423 , Y02A50/475 , Y02A50/478 , Y02A50/481 , A61K2300/00
摘要： The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
摘要翻译： 本发明提供包含式1类固醇的组合物，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮半水合物和一种或多种赋形剂，通常其中组合物包含少于约3％的水。 该组合物可用于制备改进的药物制剂。 本发明还提供了间歇给药类固醇化合物的方法，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮的类似物和可用于这种给药方案的组合物。 本发明进一步提供抑制病原体（病毒）复制，改善与免疫失调相关的症状并使用某些类固醇和类固醇类似物调节受试者的免疫应答的组合物和方法。 本发明还提供了制备和使用这些免疫调节组合物和制剂的方法。
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公开(公告)号：US20060063749A1
公开(公告)日：2006-03-23
申请号：US10607415
申请日：2003-06-25
CPC分类号： A61K31/565 , A61K9/0019 , A61K9/0031 , A61K9/127 , A61K31/56 , A61K31/568 , A61K31/5685 , C07J1/00 , C07J1/0011 , C07J3/005 , Y02A50/402 , Y02A50/409 , Y02A50/411 , Y02A50/415 , Y02A50/423 , Y02A50/475 , Y02A50/478 , Y02A50/481 , A61K2300/00
摘要： The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
摘要翻译： 本发明提供包含式1类固醇的组合物，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮半水合物和一种或多种赋形剂，通常其中组合物包含少于约3％的水。 该组合物可用于制备改进的药物制剂。 本发明还提供了间歇给药类固醇化合物的方法，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮的类似物和可用于这种给药方案的组合物。 本发明进一步提供抑制病原体（病毒）复制，改善与免疫失调相关的症状并使用某些类固醇和类固醇类似物调节受试者的免疫应答的组合物和方法。 本发明还提供了制备和使用这些免疫调节组合物和制剂的方法。
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公开(公告)号：US20070275938A1
公开(公告)日：2007-11-29
申请号：US11674128
申请日：2007-02-12
申请人： Christopher Reading , Clarence Ahlem , Dominick Auci , Charles Dowding , James Frincke , Mei Li , Theodore Page , Dwight Stickney , Richard Trauger , Steven White
发明人： Christopher Reading , Clarence Ahlem , Dominick Auci , Charles Dowding , James Frincke , Mei Li , Theodore Page , Dwight Stickney , Richard Trauger , Steven White
摘要： The invention relates to the use of compounds to ameliorate or treat a condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3β-hydroxy-17β-aminoandrost-5-ene, 3β-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3α-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3β-hydroxy-16β-fluoro-17β-aminoandrost-5-ene, 1α,3β-dihydroxy-4α-fluoroandrost-5-ene-17-one, 1α,3β,17β-trihydroxy-4α-fluoroandrost-5-ene, 1β,3β-dihydroxy-6α-bromoandrost-5-ene, 1α-fluoro-3β,12α-dihydroxyandrost-5-ene-17-one, 1α-fluoro-3β,4α-dihydroxyandrost-5-ene and 4α-fluoro-3β,6α,17β-trihydroxyandrostane.
摘要翻译： 本发明涉及化合物用于改善或治疗诸如囊性纤维化，中性粒细胞减少症或其它示例性病症的病症的用途。 可以使用的示例性化合物包括3β-羟基-17β-氨基雄甾-5-烯，3β-羟基-16α-氟-17β-氨基雄甾-5-烯，3α-羟基-16α-氟-17β-氨基雄甾-5-烯 ，3β-羟基-16β-氟-17β-氨基雄甾-5-烯，1α，3β-二羟基-4α-氟代雄甾-5-烯-17-酮，1α，3β，17β-三羟基-4α-氟代雄甾-5-烯 ，1beta，3β-二羟基-6α-溴代雄甾-5-烯，1α-氟-3β，12α-二羟基雄甾-5-烯-17-酮，1α-氟-3β，4α-二羟基雄甾-5-烯和4α-氟 -3β，6α，17β-三羟基雄甾烷。
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公开(公告)号：US20080015174A1
公开(公告)日：2008-01-17
申请号：US11696637
申请日：2007-04-04
CPC分类号： A61K31/56 , A61K31/566
摘要： The invention relates to the use of compounds to treat a number of conditions, such as a pre-diabetes condition, type 1 diabetes, type 2 diabetes, hyperglycemia, insulin resistance and glucose intolerance. Compounds that can be used in one or more of the treatment methods include 3β,7β,16α,17β-tetrahydroxyandrost-5-ene, 3α,7β,16α,17β-tetrahydroxyandrost-5-ene, 3β,7β,16α,17β-tetrahydroxyandrost-5-ene, 3β,16α,17β-trihydroxyandrost-5-ene-7-one, 3β,7β,17β-trihydroxy-17α-ethynylandrost-5-ene, 3β,17β-dihydroxy-17α-ethynylandrost-5-ene-7-one and 3β,7α,17β-trihydroxy-17α-ethynylandrost-5-ene.
摘要翻译： 本发明涉及化合物用于治疗诸如前期糖尿病，1型糖尿病，2型糖尿病，高血糖症，胰岛素抵抗和葡萄糖耐受不良的许多病症的用途。 可用于一种或多种治疗方法的化合物包括3β，7beta，16α，17β-四羟基雄甾-5-烯，3α，7beta，16α，17β-四羟基雄甾-5-烯，3β，7beta，16α，17β- 三羟基雄甾-5-烯，3β，16α，17β-三羟基雄甾-5-烯-7-酮，3β，7β，17β-三羟基-17α-乙炔基雄甾-5-烯，3β，17β-二羟基-17α-乙炔基雄甾-5- 烯-7和3β，7α，17β-三羟基-17α-乙炔基雄甾-5-烯。
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公开(公告)号：US20070275937A1
公开(公告)日：2007-11-29
申请号：US11674126
申请日：2007-02-12
申请人： Christopher Reading , Clarence Ahlem , Dominick Auci , Charles Dowding , James Frincke , Mei Li , Theodore Page , Dwight Stickney , Richard Trauger , Steven White
发明人： Christopher Reading , Clarence Ahlem , Dominick Auci , Charles Dowding , James Frincke , Mei Li , Theodore Page , Dwight Stickney , Richard Trauger , Steven White
摘要： The invention relates to the use of compounds to ameliorate or treat a condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3β-hydroxy-17β-aminoandrost-5-ene, 3β-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3α-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3β-hydroxy-16β-fluoro-17β-aminoandrost-5-ene, 1α,3β-dihydroxy-4α-fluoroandrost-5-ene-17-one, 1α,3β,17β-trihydroxy-4α-fluoroandrost-5-ene, 1β,3β-dihydroxy-6α-bromoandrost-5-ene, 1α-fluoro-3β,12α-dihydroxyandrost-5-ene-17-one, 1α-fluoro-3β,4α-dihydroxyandrost-5-ene and 4α-fluoro-3β,6α,17β-trihydroxyandrostane.
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公开(公告)号：US20050256095A1
公开(公告)日：2005-11-17
申请号：US10949694
申请日：2004-09-23
IPC分类号： A61K31/56 , A61K31/565 , C07J1/00 , C07J3/00 , A61K31/57
CPC分类号： A61K31/565 , A61K9/0019 , A61K9/0031 , A61K9/127 , A61K31/56 , A61K31/568 , A61K31/5685 , C07J1/00 , C07J1/0011 , C07J3/005 , Y02A50/402 , Y02A50/409 , Y02A50/411 , Y02A50/415 , Y02A50/423 , Y02A50/475 , Y02A50/478 , Y02A50/481 , A61K2300/00
摘要： The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
摘要翻译： 本发明提供包含式1类固醇的组合物，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮半水合物和一种或多种赋形剂，通常其中组合物包含少于约3％的水。 该组合物可用于制备改进的药物制剂。 本发明还提供了间歇给药类固醇化合物的方法，例如16α-溴-3β-羟基-5α-雄甾烷-17-酮的类似物和可用于这种给药方案的组合物。 本发明进一步提供抑制病原体（病毒）复制，改善与免疫失调相关的症状并使用某些类固醇和类固醇类似物调节受试者的免疫应答的组合物和方法。 本发明还提供了制备和使用这些免疫调节组合物和制剂的方法。
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