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US 8,772,494 B2Granted
N-aryl piperidine substituted biphenylcarboxamides as inhibitors of apolipoprotein b
AssigneeJanssen Pharmaceutica NV
InventorsLieven Meerpoel, Marcel Viellevoye, Joannes Theodorus Maria Linders
Life of this patent
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Abstract
N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.
Claims8
A compound of formula (I)
- the N-oxides, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein
- R1 is hydrogen, C1-4alkyl, halo, or polyhaloC1-4alkyl;
- R2 is hydrogen, C1-4alkyl, halo, or polyhaloC1-4alkyl;
- R3 is hydrogen or C1-4alkyl;
- R4 is hydrogen, C1-4alkyl, or halo;
- n is an integer 0, or 1;
- X1 is carbon and X2 is carbon;
- or X1 is nitrogen and X2 is carbon;
- or X1 is carbon and X2 is nitrogen;
- X3 is carbon or nitrogen;
- Y represents O, or NR6 wherein R6 is hydrogen or C1-4alkyl;
- R5 represents a radical of formula
- wherein
- m is an integer 0, 1, or 2;
- Z is O or NH;
- R7 is hydrogen,
- C1-6alkyl;
- C1-6alkyl substituted with hydroxy, amino, mono- or di(C1-4alkyl)amino, C1-4alkyloxycarbonyl, aminocarbonyl, aryl or heteroaryl;
- C1-4alkyl-O—C1-4alkyl;
- C1-4alkyl-S—C1-4alkyl;
- or
- aryl;
- R8 is hydrogen or C1-6alkyl;
- R9 is C1-4alkyl;
- or when Y represents NR6 the radicals R5 and R6 may be taken together with the nitrogen to which they are attached to form pyrrolidinyl substituted with C1-4alkyloxycarbonyl and optionally further substituted with hydroxy;
- or piperidinyl substituted with C1-4alkyloxycarbonyl;
- aryl is phenyl;
- phenyl substituted with one, two or three substituents each independently selected from C1-4alkyl, C1-4alkyloxy, halo, hydroxy, nitro, cyano, C1-4alkyloxycarbonyl, trifluoromethyl, or trifluoromethoxy;
- or benzo[1,3]dioxolyl;
- and
- heteroaryl is imidazolyl, thiazolyl, indolyl, or pyridinyl.
28 more elements
Dependencies are inferred from the claim text.