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US 6,723,744 B2Granted
Indole carboxylic acids as thyroid receptor ligands
AssigneePfizer Inc.
InventorsGary E. Aspnes, Yuan-Ching P. Chiang
Life of this patent
Estimating the term…
Abstract
A compound of the formula wherein W, R1, R2, R3, R4, R5, R6, R7, R8 and R13 are as defined herein, useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss.
Claims23
A compound of the formula
- or the pharmaceutically acceptable salt thereof;
- wherein
- W is oxygen, CH2, CF2, NR12, S(O)m wherein m is 0, 1 or 2;
- R1, R2, and R3 are each independently selected from the group consisting of hydrogen, halo, cyano, trifluoromethyl, trifluomethoxy and (C1-C6)alkyl;
- R4 is hydrogen, halo, cyano, (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, (C3-C10)cycloalkyl, (C3-C10)cycloalkyl(C1-C6)alkyl, —OR9, —S(O)2NR10R11, —C(O)NR10R11, —C(O)R10, —CH(OH)R10, —NR12C(O)R10, —NR12C(O)NR10R11, —NR12S(O)2R10 or —S(O)nR10 wherein n is 0, 1 or 2;
- R5 is hydroxy, or, (C1-C4)alkoxy;
- R6 is hydrogen, —C(O)CH3, (C1-C6)alkyl, or phenyl(C1-C6)alkyl;
- R7 is hydrogen or (C1-C6)alkyl;
- R8 is OR12 or NR9R12;
- R9 for each occurrence is independently hydrogen, (C1-C12)alkyl, (C3-C10)cycloalkyl;
- R10 for each occurrence is independently hydrogen, (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, (C3-C10)cycloalkyl, (C3-C9)cycloalkyl(C1-C6)alkyl;
- R11 for each occurrence is independently hydrogen, (C1-C6)alkyl, (C3-C10) cycloalkyl or (C3-C9)cycloalkyl(C1-C6)alkyl;
- R12 for each occurrence is independently hydrogen or (C1-C6)alkyl;
- and
- R13 is hydrogen, halo or (C1-C6)alkyl.
12 more elements
Dependencies are inferred from the claim text.