| US 7,468,446 B2 | ||
| Substituted heterocyclic compounds and uses thereof | ||
| George W. Muller, Bridgewater, N.J. (US); and Hon-Wah Man, Princeton, N.J. (US) | ||
| Assigned to Celgene Corporation, Summit, N.J. (US) | ||
| Filed on Sep. 01, 2005, as Appl. No. 11/219,592. | ||
| Claims priority of provisional application 60/607408, filed on Sep. 03, 2004. | ||
| Prior Publication US 2006/0052596 A1, Mar. 09, 2006 | ||
| Int. Cl. C07C 307/00 (2006.01) | ||
| U.S. Cl. 549—429 [514/520; 514/576; 558/402] | 7 Claims |
1. A compound having the formula:
 wherein:
X is substituted or unsubstituted benzofuran;
R1 is H and R2 is —CN;
each occurrence of Ra and Rb is independently —H, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted
heterocycle, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, halogen, cyano, —NO2, —OH, —OPO(OH)2, —N(R9)2, —OC(O)—R10, —OC(O)—R10—N(R10)2, —C(O)N(R10)2, —NHC(O)—R10, —NHS(O)2—R10, —S(O)2—R10, —S(O)2—NH2, —S(O)2—N(R10)2, —NHC(O)NH—R10, —NHC(O)N(R10)2, —NHC(O)NHSO2—R10, —NHC(O)—R10—N(R10)2, —NHC(O)CH(R10)(N(R9)2) or —NHC(O)—R10—NH2;
R3 is —H, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocycle,
substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, halogen, cyano, —NO2, —OH, —OPO(OH)2, —N(R9)2, —OC(O)—R10, —OC(O)—R10—N(R10)2, —OC(O)—R10—NH2, —C(O)N(R10)2, —NHC(O)—R10, —NHS(O)2—R10, —S(O)2—R10, —OS(O)2—R10, —S(O)2—NH2, —S(O)2—N(R10)2, —OS(O)2—NH2, —OS(O)2—N(R10)2, —NHC(O)O—R10, —NHC(O)NH—R10, —NHC(O)N(R10)2, —NHC(O)NHSO2—R10, —NHC(O)—R10—N(R10)2, —NHC(O)CH(R10)(N(R9)2) or —NHC(O)—R10—NH2, or R3 with either Ra or with R4, together form —O—C(R16R17)—O—, —O—(C(R16R17))2—O— or —O—(C(R16R17))3—O—;
R4 is —H, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocycle,
substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, halogen, cyano, —NO2, —OH, —OPO(OH)2, —N(R9)2, —OC(O)—R10, —OC(O)—R10—N(R10)2, —OC(O)—R10—NH2, —C(O)N(R10)2, —NHC(O)—R10, —NHS(O)2—R10, —S(O)2—R10, —OS(O)2—R10, —S(O)2—NH2, —S(O)2—N(R10)2, —OS(O)2—NH2, —OS(O)2—N(R10)2, —NHC(O)O—R10, —NHC(O)NH—R10, —NHC(O)N(R10)2, —NHC(O)NHSO2—R10, —NHC(O)—R10—N(R10)2, —NHC(O)CH(R10)(N(R9)2) or —NHC(O)—R10—NH2;
R5 is —H, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocycle,
substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, halogen, cyano, —NO2, —OH, —OPO(OH)2, —N(R9)2, —OC(O)—R10, —OC(O)—R10—N(R10)2, —OC(O)—R10—NH2, —C(O)N(R10)2, —NHC(O)—R10, —NHS(O)2—R10, —S(O)2—R10, —OS(O)2—R10, —S(O)2—NH2, —S(O)2—N(R10)2, —OS(O)2—NH2, —OS(O)2—N(R10)2, —NHC(O)O—R10, —NHC(O)NH—R10, —NHC(O)N(R10)2, —NHC(O)NHSO2—R10, —NHC(O)—R10—N(R10)2, —NHC(O)CH(R10)(N(R9)2) or —NHC(O)—R10—NH2;
each occurrence of R9 is independently —H, substituted or unsubstituted lower alkyl, or substituted or unsubstituted cycloalkyl;
each occurrence of R10 is independently substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted
aryl, substituted or unsubstituted lower hydroxyalkyl, or R10 and a nitrogen to which it is attached form a substituted or unsubstituted heterocycle, or R10 is —H where appropriate;
each occurrence of R16 and R17 is independently —H or halogen.
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