US 7,563,793 B2
Pyrrolo[1,2-a]quinoxalin-5-(4H)-yl)sulfonyls and carbonyls and their use as estrogenic agents
Joseph Peter Sabatucci, Collegeville, Pa. (US); Fei Ye, Audubon, Pa. (US); and Paige Erin Mahaney, Pottstown, Pa. (US)
Assigned to Wyeth, Madison, N.J. (US)
Filed on Dec. 16, 2005, as Appl. No. 11/305,739.
Claims priority of provisional application 60/637556, filed on Dec. 20, 2004.
Prior Publication US 2006/0160815 A1, Jul. 20, 2006
Int. Cl. A61K 31/502 (2006.01); C07D 241/36 (2006.01); A61P 37/08 (2006.01); A61P 37/02 (2006.01); A61P 19/02 (2006.01); A61P 25/28 (2006.01); A61P 9/10 (2006.01)
U.S. Cl. 514—250  [544/344] 13 Claims
 
1. A compound of the formula:

OG Complex Work Unit Drawing
wherein:
G is SO2 or CO;
R1, R4, R8, and R9 are each, independently, H, Cl, Br, F, I, NO2, alkyl, alkoxy, phenyl, OCF3, CF3, or CN;
R2, R3, R5, and R6 are each, independently, hydrogen, hydroxy, alkyl, alkoxy, or halogen;
or R2 and R5 may together form a ring, said ring being a 4 to 8 membered cycloalkane, cycloalkene, cycloalkyne, or aromatic ring optionally containing one or more heteroatoms;
R7 is hydrogen, alkyl, —(C═O)R16, —S(O)2R17, —S(O)2N(R18)(R19), or D-glucuronidate;
R10 and R11 are each, independently, H, alkyl, cycloalkyl, or phenyl;
R16 is alkyl, alkoxy, arylalkyl, or aryl;
R17 is alkyl, aryl, heteroaryl, cycloalkyl, alkenyl, cycloalkenyl, or alkynyl;
R18 and R19 are, independently, hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, monofluoroalkyl, perfluoroalkyl, aryl, arylalkyl, cycloalkenyl, heteroaryl, heteroarylalkyl, hydroxy-(C2-C6)alkyl, alkoxyalkyl, alkylthioalkyl, carbonyl, acyl, alkoxycarbonyl, —C(O)NH2, alkylaminocarbonyl, dialkylaminocarbonyl, alkylaminoalkyl, or dialkylaminoalkyl;
or R18 and R19 are taken together with the nitrogen atom to which they are attached to form a saturated, unsaturated or partially saturated C4-C6 carbon ring;
X is H, alkyl, CN, CHO, F, Br, Cl, CONRXRY, COOH, CO2Rz, or cycloalkyl; and
Rx, Ry, and Rz are each, independently, H or alkyl;
or a pharmaceutically acceptable salt thereof.