| US 7,482,356 B2 | ||
| Bicyclic pyrazolone cytokine inhibitors | ||
| Michael Philip Clark, Maineville, Ohio (US); Steven Karl Laughlin, Taylor Mill, Ky. (US); Adam Golebiowski, Loveland, Ohio (US); Todd Andrew Brugel, West Chester, Ohio (US); and Mark Sabat, Loveland, Ohio (US) | ||
| Assigned to The Procter & Gamble Company, Cincinnati, Ohio (US) | ||
| Filed on Nov. 05, 2004, as Appl. No. 10/983,114. | ||
| Claims priority of provisional application 60/518886, filed on Nov. 10, 2003. | ||
| Prior Publication US 2005/0113392 A1, May 26, 2005 | ||
| Int. Cl. C07D 487/04 (2006.01); A61K 31/4162 (2006.01) | ||
| U.S. Cl. 514—274 [514/275; 544/315; 544/330] | 29 Claims |
1. A compound or enantiomeric and diasteriomeric forms or pharmaceutically acceptable salts thereof, said compound having
the formula:
 wherein R is:
a) —O[CH2]kR3; or
b) —NR4aR4b;
R3 is substituted or unsubstituted C1-C4 alkyl, substituted or unsubstituted carbocyclic, substituted or unsubstituted heterocyclic, substituted or unsubstituted aryl
or alkylenearyl, substituted or unsubstituted heteroaryl or alkyleneheteroaryl;
the index k is from 0 to 5;
R4a and R4b are each, independently:
a) hydrogen; or
b) —[C(R5aR5b)]mR6;
R5a and R5b are each; independently, hydrogen, —OR7, —N(R7)2, —CO2R7, —CON(R7)2; C1-C4 liner, branched, or cyclic alkyl; R6 is hydrogen, —OR7, —N(R7)2, —CO2R7, —CON(R7)2; substituted or unsubstituted C1-C4 alkyl, substituted or unsubstituted heterocyclic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
R7 is hydrogen, C1-C4 alkyl, or substituted or unsubstituted aryl; the index m is from 0 to 5;
and wherein R1 is:
a) substituted or unsubstituted aryl; or
b) substituted or unsubstituted heteroaryl.
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