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US 8,263,630 B2Granted
1,2,3-triazoles as 11-beta hydroxysteroid dehydrogenase type I inhibitors
AssigneeBristol-Myers Squibb Company
InventorJames J. Li
Life of this patent
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Abstract
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are defined herein.
Claims13
A compound of formula (I)
- or salts thereof wherein:
- R1 is aryl or bicycloalkyl, both of which may be optionally substituted with one or more R1as;
- R1a, at each occurrence, is independently selected from alkyl, haloalkyl, aryl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, halo, —NH2, —CN, —C(═O)OH, —C(═O)OR14, —OCF3, —OR10, —OH, —OCF3, —SH, —SR14, —C(═O)NR14R14, —NR14R14, —C(═O)R14, —NR14C(═O)R14, —OC(═O)R14, —C(═NR14)NR14R14, —NHC(═NR14)NR14R14, —S(═O)R14, —NR14C(═O)OR10, —OC(═O)NR14R14, —NR14C(═O)NR14R14 or arylalkyl, wherein the alkyl, aryl, cycloalkyl, cycloalkylalkyl, heterocyclyl, and heterocyclylalkyl may be optionally substituted with 0-3 R10a;
- R2 is unsubstituted C1-4 alkyl;
- R3 is bicycloalkyl, which may be optionally substituted with one or more R3a's;
- R3a, at each occurrence, is independently selected from alkyl, haloalkyl, aryl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, halo, —NH2, —CN, —NO2, —C(═O)OH, —C(═O)OR14, —OCF3, —OR10, —OH, —OCF3, —SH, —SR14, —C(═O)NR14R14, —NR14R14, —S(O)2NR14R14, —NR14S(O)2CF3, —C(═O)NR14S(O)2R10, —S(O)2NR14C(═O)OR10, —S(O)2NR14C(═O)NR14R14, —C(═O)NR14S(O)2R14, —C(═O)R14, —NR14C(═O)R14, —OC(═O)R14, —C(═NR14)NR14R14, —NHC(═NR14)NR14R14, —S(═O)R14, —S(O)2R14, —OS(O)2R14, —NR14C(═O)OR10, —NR14S(O2)R8, —OC(═O)NR14R14, —NR14C(═O)NR14R14 or arylalkyl, wherein the alkyl, aryl, cycloalkyl, cycloalkylalkyl, heterocyclyl, and heterocyclylalkyl may be optionally substituted with 0-3 R10a;
- R8, at each occurrence, is independently alkyl, aryl or heterocyclyl;
- R10, at each occurrence, is independently selected from alkyl, cycloalkyl, alkenyl, alkynyl, aryl, arylalkyl or heterocyclyl, wherein the alkyl, cycloalkyl, aryl, arylalkyl or heterocyclyl may be optionally substituted with 0-3 R10a, and the heterocyclyl contains 1-4 heteroatoms selected from N, O, and S;
- R10a, at each occurrence, is independently selected from alkyl, haloalkyl, aryl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, halo, —NH2, —CN, —NO2, —OCF3, —OR14, —OH, —SH, —SR14, —C(═O)NR14R14, —NR14R14, —S(O)2NR14R14, —NR14S(O)2CF3, —C(═O)NR14S(O)2R14, —S(O)2NR14C(═O)OR14, —S(O)2NR14C(═O)NR14R14, —C(═O)NR14S(O)2CF3, —C(═O)R14, —NR14C(═O)R14, —OC(═O)R14, —C(═NR14)NR14R14, —NHC(═NR14)NR14R14, —S(═O)R14, —S(O)2R14, —NR14C(═O)OR8, —NR14S(O2)R8 or arylalkyl;
- R14, at each occurrence, is independently selected from hydrogen, alkyl, cycloalkyl, aryl or arylalkyl, wherein the alkyl, cycloalkyl, aryl or arylalkyl may be optionally substituted with 0-3 R14a;
- R14a, at each occurrence, is independently selected from alkyl, haloalkyl, aryl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, halo, —NH2, —NO2, —C(═O)OH, —C(═O)OR15, —OCF3, —OR15, —OH, —SH, —SR15, —C(═O)NR15R15, —NR15R15, —S(O)2NR15R15, —NR15S(O)2CF3, —C(═O)NR15S(O)2R15, —S(O)2NR15C(═O)OR15, —S(O)2NR15C(═O)NR15R15, —C(═O)NR15S(O)2CF3, —C(═O)R15, —NR15C(═O)R15, —OC(═O)R15, —C(═)R15, —NR15R15, —NHC(═NR15)NR15R15, —S(═O)R15, —S(O)2R15, —NR15C(═O)OR8, —NR15S(O2)R8 or arylalkyl;
- and
- R15, at each occurrence, is independently selected from hydrogen, alkyl, cycloalkyl, aryl or arylalkyl;
- provided that:
- the compound is not a compound of the following structure:
12 more elements
A compound selected from the group consisting of:
Dependencies are inferred from the claim text.