US 6,982,258 B2 | ||
Low-calcemic oxime analogs of 1α,25-dihydroxy vitamin D3 | ||
Gary Posner, Baltimore, Md. (US); Mehmet Kahraman, Baltimore, Md. (US); Heung Bae Jeon, Baltimore, Md. (US); Jay A. White, Ontario (Canada); Glenville Jones, Ontario (Canada); and Bethany Halford, Baltimore, Md. (US) | ||
Assigned to Cytochroma Inc., Markham (Canada); and Johns Hopkins University, Baltimore, Md. (US) | ||
Filed on Oct. 15, 2002, as Appl. No. 10/270,158. | ||
Claims priority of provisional application 60/328428, filed on Oct. 12, 2001. | ||
Prior Publication US 2003/0171342 A1, Sep. 11, 2003 | ||
Int. Cl. A61K 31/593 (2006.01); C07C 401/00 (2006.01) |
U.S. Cl. 514—167 | 42 Claims |
1. A compound of Formula I, and pharmaceutically acceptable salts, hydrates, solvates, and prodrugs thereof: ![]() wherein R1 and R2 are independently selected from the group consisting of OH, OC1-6alkyl, and halo;
R3 is C1-6alkyl;
R4 is selected from the group consisting of H, C1-6alkyl, aryl and heteroaryl, with C1-6alkyl being unsubstituted or substituted with 1-4 groups independently selected from C1-4alkyl, OC1-4alkyl, OH, halo, NH2, NHC1-4alkyl and N(C1-4alkyl)(C1-4alkyl), and with aryl and heteroaryl being unsubstituted or substituted with 1-5 groups independently selected from C1-4alkyl, OC1-4alkyl, OH, CF3, OCF3, halo, SH, SC1-4alkyl, NH2, NHC1-4alkyl, N(C1-4alkyl)(C1-4alkyl), CN, C(O)OH, C(O)OC1-4alkyl, C(O)NHC1-4alkyl, NHC(O)C1-4alkyl, OC(O)C1-4alkyl, SOC1-4alkyl, SO2C1-4alkyl, SO2NHC1-4alkyl and SO2NH2;
R5 is selected from the group consisting of C1-6alkyl, cyclo(C3-C6)alkyl, aryl and heteroaryl, aryl-C1-6alkyl and heteroaryl-C1-6alkyl, with C1-6alkyl being unsubstituted or substituted with 1-4 groups independently selected from C1-4alkyl, OC1-4alkyl, OH, halo, NH2, NHC1-4alkyl and N(C1-4alkyl)(C1-4alkyl), and with cyclo(C3-C6)alkyl, aryl, heteroaryl, aryl-C1-6alkyl and heteroaryl-C1-6alkyl, being unsubstituted or substituted with 1-5 groups independently selected from C1-4alkyl, OC1-4alkyl, OH, CF3, OCF3, halo, SH, SC1-4alkyl, NH2, NHC1-4alkyl, N(C1-4alkyl)(C1-4alkyl), CN, C(O))OH, C(O)OC1-4alkyl, C(O)NHC1-4alkyl, NHC(O)C1-4alkyl, OC(O)C1-4alkyl, SOC1-4alkyl, SO2C1-4alkyl, SO2NHC1-4alkyl and SO2NH2; and
R6 are either both H or together from ═CH2.
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