Substituted heteroaryl- and phenylsulfamoyl compounds
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A technology of phenylsulfamoyl and compound, applied in the field of peroxisome proliferator-activated receptor agonists, can solve problems such as low ability and increased esterification
Inactive Publication Date: 2007-03-14
PFIZER PRODS ETAT DE CONNECTICUT
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This is usually caused by increased esterification of NEFA absorbed from the blood, accompanied...
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Embodiment 1
[0516] Example 1: 5-(4-Benzyloxy-phenylsulfamoyl)-2-methyl-benzoic acid
[0517]
[0518] Sodium bicarbonate (215 mg, 0.56mmol) in 2ml of aqueous solution. The resulting mixture was stirred overnight at room temperature. Acetone was then removed under reduced pressure and the residual mixture was partitioned between 25 ml of 1N aqueous hydrochloric acid and 25 ml of ethyl acetate. The aqueous phase was separated and extracted with 2 x 25 ml ethyl acetate. The ethyl acetate extracts were combined, dried (anhydrous sodium sulfate), and concentrated under reduced pressure. The residue was purified by flash column chromatography (silica gel, 15 gm) eluting with 9:1 chloroform / methanol to give a white solid (154 mg). The solid was triturated with dichloromethane to afford the title compound (93 mg, 28% yield) as a white solid.
[0519] MS: 395.6(M-1); 1 H NMR (400MHz, CD 3 OD): δ2.57(s, 3H), 4.96(s, 2H),...
Embodiment 2
[0521] Example 2: 2-methyl-5-[4-(6-methyl-benzothiazol-2-yl)-phenylsulfamoyl]benzoic acid
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Abstract
The present invention relates to substituted heteroaryl- and phenyl-sulfamoyl compounds, pharmaceutical compositions containing such compounds and the use of such compounds as agonists of the peroxisome proliferator-activated receptor (PPAR), which activates Agents, pharmaceutical compositions containing such compounds and uses of such compounds to raise certain plasma lipid levels, including HDL-cholesterol, and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides , thus treating diseases such as atherosclerosis and cardiovascular disease in mammals, including humans, that are exacerbated by low levels of HDL-cholesterol and/or high levels of LDL-cholesterol and triglycerides. These compounds are also useful in the treatment of negative energy balance (NEB) and related diseases in ruminants.
Description
Background of the invention [0001] The present invention relates to substituted heteroaryl- and phenyl-sulfamoyl compounds, pharmaceutical compositions containing such compounds and the use of such compounds as peroxisome proliferator-activated receptor (PPAR) agonists. These compounds are particularly useful as PPARα agonists for the treatment of atherosclerosis, hypercholesterolemia, hypertriglyceridemia, diabetes, obesity, osteoporosis and Syndrome X (also known as metabolic syndrome) in mammals, including humans. ). These compounds are also useful in the treatment of negative energy balance (NEB) and related diseases in ruminants. [0002] Atherosclerosis, a disease of the arteries, is considered the leading cause of death in the United States and Western Europe. The pathological sequences leading to atherosclerosis and obstructive heart disease are well known. Early in this sequence is the formation of "fatty streaks" in the carotid, coronary, and cerebral arteries and...
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