http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-044514-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_05a203d85ee01909eaf728dc16f0f6cb |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2601-04 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D263-32 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C62-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-66 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C311-29 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C59-68 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C311-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D249-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C271-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C271-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D307-79 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C317-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-08 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C249-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D263-32 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C271-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C62-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D249-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-66 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C311-29 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C61-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C59-68 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C59-125 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C271-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C311-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D307-79 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C317-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 |
| filingDate | 2004-04-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-09-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-044514-A1 |
| titleOfInvention | ALFA CARBOXYLIC ACIDS REPLACED AS PPAR MODULATORS |
| abstract | A-substituted carboxylic acids, pharmaceutical compositions containing effective amounts of said compounds or their salts, are useful for treating PPAR, specifically disorders related to PPAR a / g such as diabetes, dyslipidemia, obesity and inflammatory disorders. Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt or solvate thereof, wherein, the Q ring is C6-10 aryl or heterocyclyl of (4-10) links; R1 is H, halo, C1-8 alkyl, C1-8 alkoxy, CN, CF3, -O-CF3, -O-SO2-C1-8 alkyl, -O-SO2- (CR11R12) C6-10 taryl, - ( CR11R12) t-cycloalkyl C3-10- (CR11R12) t, - (CR11R12) t-cycloalkyl C3-10- (CR11R12) tO-, - (CR11R12) taril C6-10- (CR11R12) t, - (CR11R12) t-aryl C6-10- (CR11R12) t- O-, - (CR11R12) t-heterocyclyl of (4-10) links- (CR11R12) t, or - (CR11R12) t- heterocyclyl of (4-10) links- (CR11R12 ) tO-; wherein the carbon atoms of the R1 ring are optionally substituted with 1 to 3 R13 groups; and the nitrogen atoms in the ring of R1 are optionally substituted with 1 to 3 C1-8 alkyl; R2 is H, C1-8 alkyl, - (CR11R12) t-C3-10 cycloalkyl, - (CR11R12) t-aryl C6-10, or - (CR11R12) t heterocyclyl of (4-10) links; and wherein the carbon atoms of R2 are optionally substituted with 1 to 3 R13 groups; and the nitrogen atoms in the R2 ring are optionally substituted with 1 to 3 C1-8 alkyl; R3 is selected from the group consisting of formulas (2), (3), (4) and (5); Y is - (C = O) - or -SO2-; Y "is NR10 or -O-; p is 0, 1 or 2; each q, r, and t are independently 0, 1, 2, 3, 4 or 5; each n is independently 0, 1, 2, 3 or 4 ; each k is independently 1, 2, or 3; each mys are independently 0, 1, 2 or 3; each j is 0, 1 or 2; each R4 is - (CR11R12) n-, - (CR11R12) nS- ( CR11R12) n-, - (CR11R12) n-NR10-, - (CR11R12) n-NR10- (CR11R12) nO-, - (CR11R12) nO- (CR11R12) k-NR10-, - (CR11R12) nO- (CR11R12 ) n-, - (CR11R12) nO- (CR11R12) kO- (CR11R12) n-, - (CR11R12) n-CR11 = CR12- (CR11R12) n-, or -CH = CH- (CR11R12) -O- ( CH2) n-; each R5 is a bond or - (CR11R12) mZ- (CR11R12) s; where Z is -CR11R12-, -O-NR10a-, or -S (O) j-; each R6 is - (C = O) -OH, - (C = O) -OM +, - (C = O) -C 1-8 alkyl, - (C = O) -O-C 1-8 alkyl, - (C = O) - NR10R11, - (C = O) -NR10-SO2-R11, -SO2-NH- R10, -NH-SO2-R10, - (C = O) -NH-CºN, or R6 has a formula (6) or ( 7); M + is an alkali metal cation or an alkaline earth metal cation; each R7 and R8 is independently H, C1-8 alkyl, C1-8 alkoxy, - (CR11R12) C3-10 tcycloalkyl, - (CR11R12) C6 taryl -10, - (CR11R12) C6-10-O- taryl, - (CR11R12) t heterocyclyl of (4-10) links or - (CR11R12) t heterocyclyl of (4-10) links-O-; or R7 and R8 can optionally be taken together with the carbon to which they are attached to form a C3-10 cycloalkyl or a heterocyclyl of (3-10) links; each Ar1, Ar2, Ar3, and Ar4 represents C6-10 aryl or heterocyclyl of (5-10) links; wherein the carbon atoms in the ring of each Ar1, Ar2, Ar3, and Ar4 are optionally substituted with one to three R13 groups; Ring A represents a ring of 3, 4, 5, 6 or 7 links optionally containing 1 to 4 heteroatoms that can be the same or different and are selected from -N (R10a) -, O, and S (O) j , in which j is 0, 1 or 2, with the proviso that the ring does not contain two adjacent O or S (O) j atoms, and in which the carbon atoms of residue A in the ring are optionally substituted with one to three R13 groups; R9 is C1-8 alkyl, - (CR11R12) C6-10 taryl or - (CR11R12) t heterocyclyl of (4-10) links, in which t are independently 0, 1, 2, 3, 4, or 5, in wherein said R9 groups are substituted with 1 to 3 groups independently selected from - (CR11R12) qNR10R11, - (CR11R12) qNR10alkanoyl C1-6, - (CR11R12) qO (CR11R12) rR10, and - (CR11R12) qR10; and wherein the heterocyclyl, aryl and alkyl moieties of the above groups are optionally substituted with one to three R13 groups; R9a and R10 are independently H or C1-8 alkyl; R11 and R12 are independently H, C1-8 alkyl, hydroxy, or C1-6 alkoxy; R10a is selected from H, C1-8 alkyl, - (C = O) -R14, -SO2NR15R16, or -S (O) C1-6alkyl; each R13 and R13a are independently selected from the group consisting of halo, cyano, nitro, trifluoromethoxy, trifluoromethyl, azido, hydroxy, C1-6 alkoxy, C1-10 alkyl, C2-6 alkenyl, C2-6 alkynyl, -O- ( CR11R12) kO- (CR11R12) n-, - (C = O) -R14, - (C = O) -O-R15, -O- (C = O) -R15, -NR15 (C = O) -R16 , -NR15 (C = O) -O-R16, - (C = O) -NR15R16, -NR15R16, -NR15OR16, -SO2NR15R16, -S (O) C1-6 jalkyl, -O-SO2-R14, -NR15 -SO2-R16, R15- (CR11R12) C6-10 taryl, - (CR11R12) t heterocyclyl of (4-10) links, - (CR11R12) q (C = O) (CR11R12) C6-10 taryl, -CR11R12) q (C = O) (CR11R12) t heterocyclyl of (4-10) links, - (CR11R12) tO (CR11R12) qaryl C6-10, - (CR11R12) tO (CR11R12) qheterocyclyl of (4-10) links, - (CR11R12) qSO2 (CR11R12) C6-10 taryl, and - (CR11R12) qSO2 (CR11R12) t heterocyclyl of (4-10) links; 1 or 2 carbon atoms in the ring of the heterocyclic moieties of the above groups R13 and R13a are optionally substituted with 1 to 3 substituents independently selected from halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, azido, -OR15, - (C = O) -R15, - (C = O) - O-R15, -O- (C = O) -R15, -NR15 (C = O) -R16, - (C = O) -NR15R16, -NR15R16, - NR15OR16, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, - (CR11R12) C6-10 taryl, and - (CR11R12) t heterocyclyl of (4-10) links; each R14, R15, and R16 is independently selected from H, C1-6 alkyl, - (CR11R12) t C6-10 aryl, and - (CR11R12) t heterocyclyl of (4-10) links; 1 or 2 carbon atoms in the ring of the heterocyclic group are optionally substituted with an oxo (= O) moiety, and the alkyl, aryl and heterocyclic moieties of the above groups R14, R15 and R16 are optionally substituted with 1 to 3 selected substituents independently between halo, cyano, nitro, -NR11R12, trifluoromethyl, trifluoromethoxy, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, hydroxy, and C1-6 alkoxy; R17 is H, C1-8 alkyl, -O-C1-8 alkyl, halo, CN, OH, CF3, or -O-CF3; and wherein any of the above-mentioned substituents comprise a CH3 (methyl), CH2 (methylene), or CH (methine) group that is not attached to a halo, SO or SO2 group or to an optionally N, O or S atom a substituent selected from hydroxy, halo, C1-4 alkyl, C1-4 alkoxy, -NH2, -NH C1-8 alkyl, and -N (C1-8 alkyl) 2 is supported on said group. |
| priorityDate | 2003-04-15-04:00^^<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: 67.