Patent
Therapeutic treatment methods
| العنوان: | Therapeutic treatment methods |
|---|---|
| Patent Number: | 7,547,687 |
| تاريخ النشر: | June 16, 2009 |
| Appl. No: | 11/674128 |
| Application Filed: | February 12, 2007 |
| مستخلص: | 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. |
| Inventors: | Reading, Christopher L. (San Diego, CA, US); Ahlem, Clarence N. (San Diego, CA, US); Auci, Dominick L. (San Diego, CA, US); Dowding, Charles (San Diego, CA, US); Frincke, James M. (Carlsbad, CA, US); Li, Mei (San Diego, CA, US); Page, Theodore M. (Carlsbad, CA, US); Stickney, Dwight R. (Granite Bay, CA, US); Trauger, Richard J. (Leucadia, CA, US); White, Steven K. (San Diego, CA, US) |
| Assignees: | Hollis-Eden Pharmaceuticals, Inc. (San Diego, CA, US) |
| Claim: | 1. A composition comprising one or more excipients and a compound having the structure [chemical expression included] wherein the dotted lines are optional double bonds; R 1 is —OH or an ester; R 2 is —H, —OH or an ester; R 3 is —H, —OH, a halogen or an ester; R 4 in the β-configuration is —OH, an ester or an amino acid and R 4 in the α-configuration is —H or optionally substituted alkynyl; R 5 is —CH 3 or —C 2 H 5 ; R 10A is —OH or R 10A is —H or —OH when R 2 is —OH or an ester; and R 10B is a halogen. |
| Claim: | 2. The composition of claim 1 wherein R 3 is —OH, a halogen or an ester and the compound has the structure [chemical expression included] |
| Claim: | 3. The composition of claim 2 wherein R 5 is —CH 3 . |
| Claim: | 4. The composition of claim 3 wherein R 10B is —F. |
| Claim: | 5. The composition of claim 4 having the structure [chemical expression included] |
| Claim: | 6. The composition of claim 2 wherein R 4 in the α-configuration is alkynyl. |
| Claim: | 7. The composition of claim 2 wherein the composition is a pharmaceutical formulation. |
| Claim: | 8. The composition of claim 1 wherein the compound has the structure [chemical expression included] |
| Claim: | 9. The composition of claim 8 wherein the compound has the structure [chemical expression included] |
| Claim: | 10. The composition of claim 9 wherein R 10B is —F. |
| Claim: | 11. The composition of claim 10 wherein R 5 is —CH 3 . |
| Claim: | 12. The composition of claim 11 having the structure [chemical expression included] |
| Claim: | 13. The composition of claim 12 having the structure [chemical expression included] |
| Claim: | 14. The composition of claim 12 wherein R 4 in the α-configuration is alkynyl. |
| Claim: | 15. The composition of claim 12 wherein R 4 in the α-configuration is —H. |
| Claim: | 16. The composition of claim 15 wherein R 4 in the β-configuration is —OH. |
| Claim: | 17. The composition of claim 16 wherein R 2 is —H or —OH. |
| Claim: | 18. The composition of claim 17 wherein the compound is 1 α,3β17β-trihydroxy-4α-fluoroandrost-5-ene. |
| Claim: | 19. The composition of claim 8 wherein the composition is a pharmaceutical formulation. |
| Current U.S. Class: | 514/169 |
| Patent References Cited: | 3001988 September 1961 Nysted 3001991 September 1961 Allen et al. 4868167 September 1989 Mokotoff 4898694 February 1990 Schwartz et al. 4908358 March 1990 Schreiber 5206008 April 1993 Loria 5387583 February 1995 Loria 5461042 October 1995 Loria 5635496 June 1997 Daynes et al. 5811418 September 1998 Daynes et al. 5859000 January 1999 Dowell et al. 6187767 February 2001 Araneo et al. 6667299 December 2003 Ahlem et al. 7396827 July 2008 Ahlem et al. 2002/0107233 August 2002 Liao et al. 2006/0063749 March 2006 Ahlem et al. 2006/0079492 April 2006 Ahlem et al. 2007/0129282 June 2007 Ahlem et al. 2007/0275937 November 2007 Reading et al. 2008/0015174 January 2008 Reading et al. 2008/0021006 January 2008 Lardy et al. 2008/0058301 March 2008 Lardy et al. WO 00/32201 June 2000 WO 01/23405 April 2001 WO 01/30802 May 2001 WO 02/069977 September 2002 WO 2004/019953 March 2004 WO 2004/089304 October 2004 |
| Other References: | Pettit et al., Antimicrobial and cancer cell growth inhibitory activities of 3β-acetoxy-17β-(L-prolyl)amino-5α-androstane in vitro, Int. J. Antimicrob. Agents vol. 15 (2000) pp. 299-304. cited by examiner U.S. Appl. No. 11/835,394, filed Aug. 7, 2007, Lardy et al. cited by other U.S. Appl. No. 11/835,397, filed Aug. 7, 2007, Lardy et al. cited by other Flouret et al, “17-aminoacylamido-5-androsten-3β-ols” J. Med. Chem. 11: 880-882 (1968). cited by other Flouret et al, “17-aminoacylamido steroid antidepressants” J. Med. Chem. 15: 1281-1283 (1972). cited by other Kwiatkowski et al, “A syhthesis of N-substituted β-alanines: Michael addition of amines to trimethylsilyl acrylate” Synthesis 946-949 (1989). cited by other Mokotoff et al, “Peptidyl aminosteroids as potential new antiarrhythmic agents” Steroids 55: 399-404 (1990). cited by other Pettit et al, “Synthesis of 3β-acetoxy-17β-(L-arginyl-L-arginyl-L-prolyl)-amino-5α-androstane” J. Med. Chem. 10: 145-148 (1967). cited by other Pettit et al, “Structural biochemistry IV. 3β-hydroxy-17β-(L-prolyl)amino-androst-5-ene” Can. J. Chem. 45: 501-507 (1967). cited by other Pettit et al, “Structural biochemistry II. Synthesis of 3β-hydroxy-17β-(L-prolyl)amino-5α-androstane” Can. J. Chem. 44: 2023-2029 (1967). cited by other Vincze et al, “Steroids 54. Aminoacylamidosteroids” Steroids 61: 697-702 (1996). cited by other Wheeler et al, “Steroid derivatives of cysteamine and cysteine” Can. J. Chem. 47 160-162 (1969). cited by other |
| Assistant Examiner: | Jagoe, Donna |
| Primary Examiner: | Marschel, Ardin |
| Attorney, Agent or Firm: | Muenchau, Daryl D. |
| رقم الانضمام: | edspgr.07547687 |
| قاعدة البيانات: | USPTO Patent Grants |
| الوصف غير متاح. |