| US 7,605,152 B2 | ||
| 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators | ||
| William P. Dankulich, Collegeville, Pa. (US); Robert S. Meissner, Schwenksville, Pa. (US); Helen J. Mitchell, Richboro, Pa. (US); and James J. Perkins, Churchville, Pa. (US) | ||
| Assigned to Merck & Co., Inc., Rahway, N.J. (US) | ||
| Appl. No. 10/501,640 PCT Filed Jan. 10, 2003, PCT No. PCT/US03/00874 § 371(c)(1), (2), (4) Date Jul. 15, 2004, PCT Pub. No. WO03/059293, PCT Pub. Date Jul. 24, 2003. |
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| Claims priority of provisional application 60/348808, filed on Jan. 15, 2002. | ||
| Prior Publication US 2005/0107416 A1, May 19, 2005 | ||
| Int. Cl. A61K 31/56 (2006.01); A61K 31/58 (2006.01) | ||
| U.S. Cl. 514—182 [514/176] | 11 Claims |
1. A compound of structural formula II:
 “a” represents a single bond or a double bond;
R1 is hydrogen, hydroxymethyl, or C1-3 alkyl, wherein alkyl is unsubstituted or substituted with one to seven fluorine atoms;
R2 is hydrogen, fluorine, or C1-4 alkyl when “a” represents a double bond; or two R2 substituents are each independently hydrogen, fluorine, or C1-4 alkyl when “a” represents a single bond;
R4 is hydrogen, C1-4 alkyl, C2-4 alkenyl, or C2-4 alkynyl;
one of R5 and R6 is hydrogen and the other is arylmethyl, wherein aryl is selected from the group consisting of phenyl, naphthyl, pyridyl,
furanyl, pyrrolyl, thiazolyl, imidazolyl, benzofuranyl, and 1,3-benzodioxolyl, wherein the aryl group is unsubstituted or
substituted with one to two groups independently selected from halogen, C1-4 alkyl, C1-4 alkoxy, cyano, trifluoromethyl, and trifluoromethoxy.
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