Pharmaceutical compositions 3
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. Th...
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| Main Authors | , , |
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| Format | Patent |
| Language | English |
| Published |
25.05.2010
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| Online Access | Get full text |
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| Abstract | 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. |
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| AbstractList | 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. |
| Author | Reading, Christopher L Ahlem, Clarence N Frincke, James M |
| Author_xml | – sequence: 1 givenname: James M surname: Frincke fullname: Frincke, James M – sequence: 2 givenname: Christopher L surname: Reading fullname: Reading, Christopher L – sequence: 3 givenname: Clarence N surname: Ahlem fullname: Ahlem, Clarence N |
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| References | Garsd et al. (2007/0077203) 20070400 Flores-Riveros et al. (2008/0221074) 20080900 Horn, Y., The effect of androgenic hormones on bone marrow of rats receiving chemotherapy, Oncology 25:512-519 (1971). (WO 00/32176) 20000600 (WO 00/32201) 20000600 Flores-Riveros et al. (2008/0146532) 20080600 Lardy et al. (2008/0058301) 20080300 Frincke et al. (2008/0153797) 20080600 Waskiewicz et al, Induction of "male-specific" cytochrome P450 isozymes in female rast by oxandrolone, Drug Metab. Dispo. 23(11):1291-1296 (1995). (0289327) 19881100 Jung et al. (3280149) 19661000 Frincke et al. (2008/0045490) 20080200 Bebo et al, Androgens alter the cytokine profile and reduce encephalitogenicity of myelin-reactive T cells, J. Immunol, 162(1): 35-40 (1999). Fennessey et al, Anabolic steroids in body builders: use, metabolic disposition and physiological effects, J. Pharmaceutical and Biomed. Analysis, 6(6-8):999-1002 (1988). Pappo (3128283) 19640400 Ahlem et al. (2004/0220114) 20041100 Ahlem et al. (2007/0129282) 20070600 Xia et al, Anti-AIDS agents. Part 36:1 17-carboxylated steroids as potential anti-HIV agents, Bioorganic & Medicinal Chem. 7(9):1907-1911 (1999). Yang et al, Inhibition of HIV-1 Latency Reactivation by Dehydroepiandrosterone (DHEA) and an Analog of DHEA, Aids Research and Human Retroviruses 9(8):747-754 (1993). Lardy et al. (2008/0176823) 20080700 Henderson et al, Dehydroepiandrosterone and 16α-bromoepiandrosterone: inhibitors of Epstein-Barr virus induced transformation of human lymphocytes, Carcinogenesis, 2(7):683-686 (1981). Dowell et al. (5859000) 19990100 Ahlem et al. (6667299) 20031200 Lardy et al. (2008/0004250) 20080100 (3812595) 19970700 Daynes et al. (5635496) 19970600 (0133995) 19950300 Schwartz et al. (4898694) 19900200 Reading et al. (2007/0275937) 20071100 Pappo et al, 2-Oxasteroids: A new class of biologically active compounds, Tetrahedron Letters, 9:365-371 (1962). Kang et al, Dehydroepiandrosterone and β-endorphin enhance IL-12 gene expression, Chemical Abstracts 126(9):99 (1997). Pappo (3101350) 19630800 Frincke et al. (2006/0073099) 20060400 Reading et al. (2007/0014719) 20070100 Frincke et al. (2008/0153792) 20080600 Lardy et al. (7462610) 20081200 Ahlem et al. (2007/0275936) 20071100 Hernandez-Pando et al, The effects of androstenediol and dehydroepiandrosterone on the course and cytokine profile of tuberculosis in BALB/c mice, Immunology, 95(2):234-241 (1998). Manz et al, Methyl 17β-Carboxyester Derivatives of Natural and Synthetic Glucocorticoids: Correlation Between Receptor Binding and Inhibition of in vitro Phytohaemagglutinin-Induced Lymphocyte Blastogenesis, J. Clin. Chem. Clin. Biochem. 21(2):69-75 (1983). Kang et al, Dehydroepiandrosterone and β-endorphin enhance IL-12 gene expression, Taehan Misaengmulhak Hoechi (J. Korean Soc. Microbiology) 31(4):399-404 (1996) (translation from Korean). Ahlem et al. (2006/0079492) 20060400 Araghi-Niknam et al, Modulation of immune dysfunction during murine leukaemia retrovirus infection of old mice by dehyroepiandrosterone sulphate (DHEAS), Immunology 90(3):344-349 (1997). Zhang et al, Prevention of immune dysfunction and vitamin E loss by dehydroepiandrosterone and melatonin supplementation during murine retrovirus infection, Immunology, 96(2):291-297 (1999). (WO 00/32177) 20000600 Sigg et al, 3α-Acetoxyätien-(8:9 oder 8:14)-säure-methylester, Helvetica Chimica Acta, 39(6):1507-1525 (1956) (translation from German). Araghi-Niknam et al, Cytokine dysregulation and increased oxidation is prevented by dehydroepiandrosterone in mice infected with murine leukemia retrovirus, Proc. Soc. Exp. Biol. Med., 216(3):386-391 (1997). Loria (5461042) 19951000 Lardy (5292730) 19940300 Lardy et al. (5424463) 19950600 Loria (5478566) 19951200 Loria (5387583) 19950200 Jung et al. (3246014) 19660400 Inserra et al, Modulation of cytokine production by dehydroepiandrosterone (DHEA) plus melatonin (MLT) supplementation of old mice, Proc. Soc. Exp. Biol. Med., 218(1):76-82 (1998). Daynes et al. (5837269) 19981100 Ahlem et al. (7396827) 20080700 (WO 01/30802) 20010500 Lardy et al. (2008/0021006) 20080100 Das et al, 18-Substituted Steroids. Part 11. Synthesis of 3β,16α,18-trihydroxyandrost-5-en-17-one, a neonatal urinary metabolite, and the 3,16,18-triacetate of its 16β-epimer, J. Chem. Soc. Perkin Trans. I pp. 1821-1831, 1984. Reading et al. (2008/0015174) 20080100 (WO 01/23405) 20010400 |
| References_xml | – year: 20080100 ident: 2008/0021006 – reference: Kang et al, Dehydroepiandrosterone and β-endorphin enhance IL-12 gene expression, Chemical Abstracts 126(9):99 (1997). – reference: Bebo et al, Androgens alter the cytokine profile and reduce encephalitogenicity of myelin-reactive T cells, J. Immunol, 162(1): 35-40 (1999). – year: 20071100 ident: 2007/0275937 – year: 20000600 ident: WO 00/32201 – year: 20010500 ident: WO 01/30802 – year: 19630800 ident: 3101350 – reference: Yang et al, Inhibition of HIV-1 Latency Reactivation by Dehydroepiandrosterone (DHEA) and an Analog of DHEA, Aids Research and Human Retroviruses 9(8):747-754 (1993). – year: 20060400 ident: 2006/0079492 – reference: Inserra et al, Modulation of cytokine production by dehydroepiandrosterone (DHEA) plus melatonin (MLT) supplementation of old mice, Proc. Soc. Exp. Biol. Med., 218(1):76-82 (1998). – year: 20070100 ident: 2007/0014719 – year: 20000600 ident: WO 00/32176 – reference: Araghi-Niknam et al, Cytokine dysregulation and increased oxidation is prevented by dehydroepiandrosterone in mice infected with murine leukemia retrovirus, Proc. Soc. Exp. Biol. Med., 216(3):386-391 (1997). – reference: Araghi-Niknam et al, Modulation of immune dysfunction during murine leukaemia retrovirus infection of old mice by dehyroepiandrosterone sulphate (DHEAS), Immunology 90(3):344-349 (1997). – reference: Fennessey et al, Anabolic steroids in body builders: use, metabolic disposition and physiological effects, J. Pharmaceutical and Biomed. Analysis, 6(6-8):999-1002 (1988). – reference: Waskiewicz et al, Induction of "male-specific" cytochrome P450 isozymes in female rast by oxandrolone, Drug Metab. Dispo. 23(11):1291-1296 (1995). – year: 20031200 ident: 6667299 – reference: Xia et al, Anti-AIDS agents. Part 36:1 17-carboxylated steroids as potential anti-HIV agents, Bioorganic & Medicinal Chem. 7(9):1907-1911 (1999). – year: 19660400 ident: 3246014 – year: 19881100 ident: 0289327 – year: 19970600 ident: 5635496 – reference: Horn, Y., The effect of androgenic hormones on bone marrow of rats receiving chemotherapy, Oncology 25:512-519 (1971). – year: 19661000 ident: 3280149 – year: 20060400 ident: 2006/0073099 – year: 19951000 ident: 5461042 – year: 20070600 ident: 2007/0129282 – year: 20080600 ident: 2008/0153792 – reference: Manz et al, Methyl 17β-Carboxyester Derivatives of Natural and Synthetic Glucocorticoids: Correlation Between Receptor Binding and Inhibition of in vitro Phytohaemagglutinin-Induced Lymphocyte Blastogenesis, J. Clin. Chem. Clin. Biochem. 21(2):69-75 (1983). – reference: Kang et al, Dehydroepiandrosterone and β-endorphin enhance IL-12 gene expression, Taehan Misaengmulhak Hoechi (J. Korean Soc. Microbiology) 31(4):399-404 (1996) (translation from Korean). – year: 20010400 ident: WO 01/23405 – reference: Henderson et al, Dehydroepiandrosterone and 16α-bromoepiandrosterone: inhibitors of Epstein-Barr virus induced transformation of human lymphocytes, Carcinogenesis, 2(7):683-686 (1981). – reference: Pappo et al, 2-Oxasteroids: A new class of biologically active compounds, Tetrahedron Letters, 9:365-371 (1962). – year: 20080600 ident: 2008/0146532 – year: 19970700 ident: 3812595 – year: 20080100 ident: 2008/0004250 – year: 19950300 ident: 0133995 – year: 20081200 ident: 7462610 – year: 19940300 ident: 5292730 – year: 19640400 ident: 3128283 – year: 19951200 ident: 5478566 – year: 20070400 ident: 2007/0077203 – year: 19981100 ident: 5837269 – year: 19950600 ident: 5424463 – reference: Sigg et al, 3α-Acetoxyätien-(8:9 oder 8:14)-säure-methylester, Helvetica Chimica Acta, 39(6):1507-1525 (1956) (translation from German). – year: 20071100 ident: 2007/0275936 – year: 20080700 ident: 7396827 – year: 20080100 ident: 2008/0015174 – reference: Das et al, 18-Substituted Steroids. Part 11. Synthesis of 3β,16α,18-trihydroxyandrost-5-en-17-one, a neonatal urinary metabolite, and the 3,16,18-triacetate of its 16β-epimer, J. Chem. Soc. Perkin Trans. I pp. 1821-1831, 1984. – year: 20000600 ident: WO 00/32177 – year: 19990100 ident: 5859000 – year: 20080700 ident: 2008/0176823 – year: 20080300 ident: 2008/0058301 – year: 20080600 ident: 2008/0153797 – year: 20041100 ident: 2004/0220114 – year: 19950200 ident: 5387583 – reference: Hernandez-Pando et al, The effects of androstenediol and dehydroepiandrosterone on the course and cytokine profile of tuberculosis in BALB/c mice, Immunology, 95(2):234-241 (1998). – year: 20080200 ident: 2008/0045490 – reference: Zhang et al, Prevention of immune dysfunction and vitamin E loss by dehydroepiandrosterone and melatonin supplementation during murine retrovirus infection, Immunology, 96(2):291-297 (1999). – year: 19900200 ident: 4898694 – year: 20080900 ident: 2008/0221074 |
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