7-[(4′-trifluoromethyl-biphenyl-2-carbonyl)amino]-quinoline-3-carboxylic acid amides, and methods of inhibiting the secretion of apolipoprotein B
AssigneePfizer Inc.
InventorsRoger Ruggeri, Douglas Wilson
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Abstract
This invention relates to compounds of Formula I: that inhibit the secretion of apolipoprotein B, to pharmaceutical compositions comprising the compounds, and to methods of treating and/or preventing atherosclerosis, obesity, diabetes, hyperlipidemia, hyperliproproteinemia, hypercholesterolemia, hypertriglyceridemia, hypoalphalipoproteinemia, pancreatitis, myocardial infarction, stroke, restenosis, or Syndrome X. This invention also relates to methods of reducing the secretion of apolipoprotein B and/or inhibiting microsomal triglyceride transfer protein.
Claims2
A method of treating a disease selected from atherosclerosis, obesity, hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, hypoalphalipoproteinemia, pancreatitis and diabetes, the method comprising the step of administering to a patient having such disease a therapeutically effective amount of a compound of Formula I
- or a stereoisomer, pharmaceutically acceptable salt or prodrug thereof, or a pharmaceutically acceptable salt of the prodrug,
- wherein
- each Ra and Rb is independently hydrogen or C1-C8alkyl;
- each n is independently 0, 1, 2 or 3;
- each X is independently aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl;
- R1 is hydrogen or C1-C8alkyl;
- and
- R2 hydrogen, —(CRaRa)n—X, C1-C8alkyl, C1-C8substituted alkyl,
- or R1 and R2 together with the nitrogen atom to which they are bonded form a 3 to 7 membered heterocycloalkyl ring comprising from 1 to 3 heteroatoms.
A method of treating a disease selected from atherosclerosis, obesity, hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, hypoalphalipoproteinemia, pancreatitis and diabetes, the method comprising the step of administering to a patient having such disease a therapeutically effective amount of a compound of Formula II
- or a stereoisomer, pharmaceutically acceptable salt or prodrug thereof, or a pharmaceutically acceptable salt of the prodrug,
- wherein
- each R3 is independently hydrogen or C1-C6alkyl;
- each RQ is independently hydrogen or C1-C6alkyl;
- A is
- X is O or S;
- n is 0 to 6;
- each Rb is independently hydrogen, —CF3, —OC1-C6alkyl, halo, —SH, —SC1-C6-alkyl, phenyl, or —C1-C6alkyl;
- B is hydrogen,
- or B and RQ together with the nitrogen atom to which they are bonded form a heterocycloalkyl ring comprising from 1 to 3 heteroatoms;
- each R is independently hydrogen or C1-C6alkyl;
- each Y is independently phenyl, substituted phenyl, pyridyl or substituted pyridyl, wherein any substituents are independently selected from —CF3, halo, —OC1-C6alkyl, or —C1-C6alkyl;
- and
- m is 0 to 5.
Dependencies are inferred from the claim text.