Polyarylcarboxamide useful as lipid lowering agent

PK140593AUndetermined Publication Date: 2010-04-08JANSSEN PHARMA NV
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Patent Information

Application Number
PK200100853
Authority / Receiving Office
PK · PK
Patent Type
Applications
Current Assignee / Owner
Publication Date
2010-04-08
Patent Text Reader

Abstract

Polyarylcarboxamide compound of formula (I) Are useful as lipid lowering agents. Wherein - Z1 is selected from (CH2)n wherein n is 1 to 3, CH2CH2O and OCH2CH2; - Z2 is (CH2)m wherein m is 1 or 2; - X1 represents O, CH2, CO, NH, CH2O, OCH2, CH2S, SCH2 and OCH2CH2; - X2 and X3 are each independently selected from CH, N and a sp2 carbon atom; - R1 is hydrogen or C1-4 alkyl; - Ar1 is an aromatic ring selected from phenyl, naphthalenyl, pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, triazinyl, triazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, pyrrolyl, furanyl and thienyl, optionally substituted with one or two R3 substituents; - Ar2 is an aromatic ring selected from phenyl, naphthalenyl, pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, triazinyl, triazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, pyrrolyl, furanyl and thienyl, optionally substituted with one or two or three R4 substituents; - Each R2 and R3 is independently selected from C1-4alkyl, C1-4alkyloxy, halo and trifluoromethyl; - Each R4 is independently selected from C1-4alkyl, C1-4alkyloxy, halo, hydroxyl, mercapto, cyano, nitro, C1-4alkylthio or polyhaloC1-6alkyl, amino C1-4alkylamino and di(C1-4alkyl)amino; - P1 and p2 are each 0 to 2; - P3 is 0 to 3; - X1 and R4 taken together with the aromatic rings Ar1 and Ar2 to which they are attached may form a fluoren-1-yl or a fluoren-4-yl group; - A represents a C1-6alkyanediyl substituted with one or two groups selected from aryl, heterorayl and C3-10cycloalkyl; when X3 is CH, A may also represents a nitrogen atom substituted with hydrogen, C1-10alkyl, aryl, heteroaryl, arylC1-10alkyl, heteroarylC1-10alkyl or C3-10; - B represents hydrogen; C1-10alkyl; aryl or heteroaryl each optionally substituted with agroup selected from halo, cyano, nitro, C1-4alkyloxy, amino, C1-10alkylamino, di(C1-10alkyl)amino, C1-10acyl, C1-10alkylthio, C1-10alkyloxycarbonyl, C1-10alkylaminocarbonyl and di(C1-10alkyl)aminocarbonyll arylC1-10alkyl; heteroarylC1-10alkyl; C3-10cycloalkyl; polyhaloC-6alkyl; C3-6Alkenyl; C3-6alkylnyl; NR6R7; or OR8; - R6 and R7 each independently represent hydrogen C1-10alkyl, aryl or heteroaryl each optionally substituted with a group selected from halo, cyano, C1-4alkyloxy, amino, C1-10alkylamino, di(C1-10alkyl)amino, C1-10acyl, C1-10alkylthio, C1-10alkylaminocarbonyl and di(C1-10alkyl)aminocarbonyl; arylC1-10alkyl, heteroarylC1-10alkyl, C3-10cycloalkyl, C7-10polycycloalkyl, polyhaloC1-6alkyl, C3-8alkenyl, C3-8alkynyl, fused benzo-C5-6cycloalkyl, and wherein R6 and R7 taken together with the nitrogen atom to which they are attached may form a C4-8 saturated heterocyclic radical; - R8 represents C1-10alkyl, aryl or heteroary each optionally substituted with a group selected from hal, cyano, nitro, C1-4alkyloxy, amino, C1-10alkylamino, di(C1-10alkyl)amino, C1-10acyl, C1-10alkylthio, C1-10alkylaminocarbonyl and di(C1-10alkyl)aminocarbonyl; arylC1-10alkyl, heteroarylC1-10alkyl, C3-8alkyenyl, C3-8alkylnyl or fused benzo-C5-8cycloalkyl.
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