http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-035056-A1
Outgoing Links
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|---|---|
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| filingDate | 2001-08-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2004-04-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-035056-A1 |
| titleOfInvention | POLYARYL CARBOXAMIDE COMPOUNDS, PROCESSES FOR THEIR PREPARATION, USEFUL INTERMEDIARIES FOR THE PREPARATION OF SUCH COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE SUCH COMPOUNDS, AND, THE USE OF SUCH COMPOUNDS IN THE MANUFACTURE OF MEDICINES |
| abstract | Polyarylcarboxamide compounds of formula (1), N-oxides, pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein: Z1 is selected from (CH2) n where n is 1 to 3, CH2CH2O and OCH2CH2; Z2 is (CH2) m where m is 1 or 2; X1 represents O, CH2, CO, NH, CH2O, OCH2, CH2S, SCH2 or a direct link; X2 and X3 are individually 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, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, pyrrolyl, furanyl and thienyl optionally substituted with one or two R3; Ar2 is an aromatic ring selected from phenyl, naphthalenyl, pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, triazinyl, triazolyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, irrolyl, furanyl and thienyl, optionally substituted with one, two, substituted with one, two, or three, substituted with R4; each R2 and R3 is independently selected from C1-4 alkyl, C1-4 alkyloxy, halo, trifluoromethyl; each R4 is independently selected from C1-4 alkyl, C1-4 alkyloxy, halo, hydroxy, mercapto, cyano, nitro, C1-4 alkylthio or C1-4 polyhaloalkyl, amino, C1-4 alkylamino and di (C1-4 alkyl) Not me; 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 can form a fluoren-1-yl group or a fluoren-4-yl group; A represents a C1-6 alkanediyl substituted with one or two groups selected from aryl, heteroaryl and C3-10 cycloalkyl; or when X3 is CH, A may also represent a nitrogen atom substituted with hydrogen, C1-10 alkyl, aryl, heteroaryl, aryl-C1-10 alkyl, C1-10 heteroarylalkyl or C3-10 cycloalkyl; B represents hydrogen, C1-10 alkyl, aryl or heteroaryl each optionally substituted with a group selected from halo, cyano, nitro, C1-4 alkyloxy, amino, C1-10 alkylamino, di (C1-10 alkyl) amino, C1 acyl -10, C1-10 alkylthio, C1-10 alkoxycarbonyl, C1-10 alkylaminocarbonyl and di (C1-10 alkyl) aminocarbonyl, C1-10 arylalkyl, C1-10 heteroarylalkyl, C3-10 cycloalkyl, C1-6 polyhaloalkyl, C3- alkenyl 6, C3-6 alkynyl, NR6R7, or OR8; R6 and R7 each independently represent hydrogen, C1-10 alkyl, aryl or heteroaryl each optionally substituted with a group selected from halo, cyano, C1-4 alkyloxy, amino, C1-10 alkylamino, di (C1-10 alkyl) amino , C1-10 acyl, C1-10 alkylthio, C1-10 alkylaminocarbonyl and di (C1-10 alkyl) aminocarbonyl, C1-10 arylalkyl, C1-10 heteroarylalkyl, C3-10 cycloalkyl, C7-10 polycycloalkyl, C1-6 polyhaloalkyl, C3-8 alkenyl, C3-8 alkynyl, fused benzo-cycloalkyl-C5-8, and wherein R6 and R7 taken together with the nitrogen atom to which they are attached can form a C4-8 saturated heterocyclic radical; R8 represents C1-10 alkyl, aryl or heteroaryl each optionally substituted with a group selected from halo, cyano, nitro, C1-4 alkyloxy, amino, C1-10 alkylamino, di (C1-10 alkyl) amino, C1-10 acyl , C1-10 alkylthio, C1-10 alkylaminocarbonyl and di (C1-10 alkyl) aminocarbonyl, C1-10 arylalkyl, C1-10 heteroarylalkyl, C3-10 cycloalkyl, C7-10 polycycloalkyl, C1-6 polyhaloalkyl, C3-8 alkenyl, C3-8 alkynyl or fused C5-8 benzocycloalkyl. Such polyarylcarboxamide compounds are useful as lipid reducing agents. Also disclosed are: processes for their preparation, useful intermediates for the preparation of such compounds, pharmaceutical compositions comprising said compounds, and the use of such compounds in the manufacture of medicaments. |
| priorityDate | 2000-09-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 66.