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US 2004/0176425 A1Published application
Cycloalkyl containing anilide ligands for the thyroid receptor
OwnerWilliam N. Washburn, Wei Menginventors
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Abstract
Novel thyroid receptor ligands are provided having the general formula I 1 wherein X, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
Claims24
A compound of formula I
- 48
- wherein
- X is selected from oxygen (—O—), selenium (—Se—), sulfur (—S—), sulfenyl (SO), sulfonyl (SO2), carbonyl (—CO), methylene (—CH2—) and —NH—;
- R1 is selected from hydrogen, halogen, CF3 and C1 to C6 alkyl;
- R2 is selected from halogen, CF3, C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C7 cycloalkyl, C4 to C7 cycloalkenyl, aryl, heteroaryl, alkoxy, aryloxy, heteroaryloxy, arylalkoxy, cycloalkoxy, N(R12)COR13, CO(NR12R13), N(R12)SO2R13, SO2(NR12R13), SR14, SOR14, SO2R14, COR14, CR12(OR5)R13 and CH2NR12R13;
- R3 is selected from hydrogen, alkyl, benzyl, aroyl and alkanoyl;
- R4 and R5 are each independently selected from hydrogen, halogen and alkyl;
- R6 and R7 are each independently selected hydrogen, halogen, cyano, C1 to C4 alkyl and C3 to C6 cycloalkyl, where at least one of R6 and R7 is other than hydrogen;
- R8 and R9 are each independently selected from hydrogen, halogen, alkoxy, hydroxy, cyano, CF3 and alkyl;
- R10 is hydrogen or alkyl;
- R11 is CO2R13 or tetrazole;
- R12 and R13 for each occurrence are each independently selected from hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl;
- R14 is selected from alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl;
- and
- n is an integer from 1 to 4,
- including all prodrugs, stereoisomers and pharmaceutically acceptable salts thereof.
13 more elements
Dependencies are inferred from the claim text.