	US 7,521,475 B2
	Chondropsin-class antitumor V-ATPase inhibitor compounds, compositions and methods of use thereof
Michael R. Boyd, Mobile, Ala. (US); and Kirk R. Gustafson, Frederick, Md. (US)
Assigned to The United States of America as represented by the Department of Health and Human Services, Washington, D.C. (US)
Filed on Feb. 13, 2007, as Appl. No. 11/674,245.
Application 11/674245 is a division of application No. 10/521930, granted, now 7,205,334, previously published as PCT/US03/23290, filed on Jul. 24, 2003.
Claims priority of provisional application 60/398092, filed on Jul. 24, 2002.
Prior Publication US 2007/0142347 A1, Jun. 21, 2007
Int. Cl. A01N 43/16 (2006.01); A61K 31/35 (2006.01)

U.S. Cl. 514—456

11 Claims

1. A composition comprising a therapeutically effective amount of (i) at least one substantially purified compound of the formula:

wherein:

R¹is H, a straight-chain or branched C_1-30saturated alkyl, a straight-chain or branched C_2-30unsaturated alkyl, or an aryl comprising 6-10 carbon atoms in the ring skeleton thereof, wherein R¹is unsubstituted or substituted with one or more substituents, which are the same or different, selected from the group consisting of a halogen, an oxo, OR^1a, CO₂R^1a, and OC(O)R^1a, wherein R^1ais H, a straight-chain or branched C_1-30saturated alkyl, a straight-chain or branched C_2-30unsaturated alkyl, or an aryl comprising 6-10 carbon atoms in the ring skeleton thereof;

R²-R⁸are the same or different and each is R¹⁰, C(O)R¹⁰, SO₃R¹⁰, or SO₂R¹⁰, wherein R¹⁰is H, a straight-chain or branched C_1-30saturated alkyl, a straight-chain or branched C_2-30unsaturated alkyl, or an aryl comprising 6-10 carbon atoms in the ring skeleton thereof, wherein R¹⁰is unsubstituted or substituted with one or more substituents, which are the same or different, selected from the group consisting of a halogen, an oxo, OR^10a, CO₂R^10aand OC(O)R^10a, wherein R^10ais H, a straight-chain or branched C_1-30saturated alkyl, a straight-chain or branched C_2-30unsaturated alkyl, or an aryl comprising 6-10 carbon atoms in the ring skeleton thereof; and

R⁹is a substituent of the formula:

wherein the R^9asubstituents are the same or different and each is R¹¹, C(O)R¹¹, or SO₂R¹¹, wherein R¹¹is H, a straight-chain or branched C_1-30saturated alkyl, a straight-chain or branched C_2-30unsaturated alkyl, or an aryl comprising 6-10 carbon atoms in the ring skeleton thereof wherein R¹¹is unsubstituted or substituted with one or more substituents, which are the same or different, selected from the group consisting of a halogen, an oxo, OR^11a, CO₂R^11aand OC(O)R^11a, wherein R^11ais H, a straight-chain or branched C_1-30saturated alkyl, a straight-chain or branched C_2-30unsaturated alkyl, or an aryl comprising 6-10 carbon atoms in the ring skeleton thereof;

wherein R^1a, R^10aand R^11aare unsubstituted or substituted with one or more substituents selected from the group consisting of a halogen, an oxo, and a hydroxyl; or a pharmaceutically acceptable salt thereof,

(ii) at least one additional therapeutic agent, and

(iii) a pharmaceutically acceptable carrier.