http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-066386-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_7fed2b7de0f46aff7b08dd465a2841e2 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-048 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4355 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5025 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D495-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 |
filingDate | 2005-12-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e05276a17f4646e23190939f3a0adb09 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e49e9f41db29d4a6def2df10d1c20302 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5b7b7c219efc28aa9226df06ffaf1e40 |
publicationDate | 2009-08-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AR-066386-A1 |
titleOfInvention | CONDENSED HETEROCICLICAL COMPOUNDS, METHODS AND INTERMEDIARIES FOR THEIR PREPARATION, A PHARMACEUTICAL COMPOSITION THAT INCLUDES THEM AND THEIR USE IN THE TREATMENT OF DISEASES MEDIATED BY THE INHIBITION OF PDE-4 |
abstract | Pharmaceutical compositions containing them, which are useful in the treatment of allergic and inflammatory diseases including asthma, chronic bronchitis, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, eosinophilic granuloma, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis , Crohn's disease, reperfusion myocardial damage, reperfusion brain damage, chronic glomerulonephritis, endotoxic shock and respiratory distress syndrome in adults. Claim 1: A compound of formula (1) in which; in each case R1, R2 and R3 may be identical or different, and are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkyl , substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclyl group , -NR5R6, -C (= L) -R5, -C (O) -R5, -C (O) O-R5, -C (O) NR5R6, -S (O) m-R5, -S (O ) m-NR5R6, nitro, -OH, cyano, oxo, formyl, acetyl, halogen, -OR5, -SR5, or a protecting group, or when two R2 substituents or two R3 substituents are in ortho position with each other, the two substituents can be attached to form an anil the 3-7-membered cyclic optionally substituted, saturated or unsaturated, which may optionally include up to two heteroatoms selected from O, NR5 or S; in each case, R5 and R6 may be identical or different and are, independently, hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkyl , substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, a substituted or unsubstituted heterocyclic group, heterocyclyl substituted , nitro, halo, -OH, cyano, -C (O) -Ra, -C (O) O-Ra, -C (O) NRaRb, -S (O) m-Ra, -S (O) m- NRaRb, -C (= NRa) -Rb, -C (= NRa) -NRaRb, -C (= S) -NRaRb, -C (= S) -Ra, -N = C (RaRb), -NRaRb, - ORa, -SRa, or a protecting group, or R5 and R6 may be linked together with the atom to which they are linked to form a 3-7 membered cyclic ring optionally substituted, saturated or unsaturated, which may optionally include up to two heteroatoms selected from O, NRa or S; in each case, Ra and Rb may be identical or different, and are, independently, hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl substituted, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenyl alkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroaryl, a substituted or unsubstituted heterocyclyl group substituted, nitro, -OH, cyano, formyl, acetyl, halogen, a protecting group, -C (O) -Ra, -C (O) O-Ra, -C (O) NRaRb, -S (O) m- Ra, -S (O) m-NRaRb, NRaRb, -ORa, or -SRa; Ar is substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocycloalkyl, a substituted or unsubstituted heteroaryl ring, or substituted or unsubstituted heteroarylalkyl; L is O, S or NRa, where Ra is as defined above; n is an integer from 0 to 2; p is an integer from 0 to 8; T, U, V and W are each, independently, C, C = O, N, NRa, O or S, provided that at least one of T, U, V and W is N, NRa, O or S , and where Ra is as defined above; each broken line [-----] in the ring represents an optionally double bond; X is O, S (O) m or NRb, where Rb is as defined above; in each case, m is independently 0, 1 or 2; Y is -C (O) NR4-, -NR4SO2-, -SO2NR4- or -NR4C (O) -; R4 is hydrogen, substituted or unsubstituted alkyl, hydroxyl, -ORa (wherein Ra is as defined above), substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryl alkyl, a substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocycloalkyl, a substituted or unsubstituted heteroaryl or substituted or unsubstituted heteroarylalkyl ring, or an analogue, tautomer, regioisomer, stereoisomer, enantiomer, diasteromer, polymorph, pharmaceutically acceptable salt, N- oxide, or a pharmaceutically acceptable solvate thereof. Claim 56: A compound that is: ethyl 4-formyl-7-methoxy-3-methylbenzo [b] furan-2-carboxylate; 2-ethoxycarbonyl-7-methoxy-3-methylbenzo [b] furan-4-carboxylic acid; 2-ethyl-4-methyl-7-methoxy-3-methylbenzo [b] furan-2,4-dicarboxylate; 2-ethyl-4-methyl-3-bromomethyl-7-methoxybenzo [b] furan-2,4-dicarboxylate; 2-ethyl-4-methyl 3-formyl-7-methylbenzo [b) furan-2,4-dicarboxylate; methyl-7-methoxy-2-methylbenzo [b] furan-4-carboxylate; methyl-2-bromomethyl-7-methoxybenzo [b] furan-4-carboxylate; methyl-2-formyl-7-methoxybenzo [b] furan-4-carboxylate; (Z) -3- (7-Methoxy-4-methyloxycarbonylbenzo [b] furan-2-yl) -2-propenoic acid; methyl-2 - [(Z) -2-azidocarbonyl) -1-ethenyl] -7-methoxybenzo [b] furan-4-carboxylate; 2-ethoxycarbonyl-7-hydroxy-3-methylbenzo [b] furan-4-carboxylic acid; 2,4-diethyl-7-hydroxy-3-methylbenzo [b] furan-2,4-dicarboxylate, 2,4-diethyl-7-difluoromethoxy-3-methylbenzo [b] furan-2,4-dicarboxylate; diethyl 3-bromomethyl-7-difluoromethoxybenzo [b] furan-2,4-dicarboxylate; diethyl 7-difluoromethoxy-3-formylbenzo [b] furan-2,4-dicarboxylate; 2- (7-methoxy-1-benzofuran-2-yl) ethanamine; ethyl 2- (7-methoxy-1-benzofuran-2-yl) ethylcarbamate; 7-hydroxy-2-methylbenzo [b] furan-4-carbaldehyde; 7-cyclopentyloxy-2-methylbenzo [b) furan-4-carboxaldehyde; 7-cyclopentyloxy-2-methylbenzo [b] furan-4-carboxylic acid; methyl-7-cyclopentyloxy-2-methylbenzo [b] furan-4-carboxylate; methyl-7-cyclopentyloxy-2-bromomethylbenzo [b] furan-4-carboxylate; methyl-2-formyl-7-cyclopentyloxybenzo [b] furan-4-carboxylate; (Z) -3- (7-Cyclopentyloxy-4-methyloxycarbonylbenzo [b] furan-2-yl) -2-propenoic acid; methyl-2 - [(Z) -2-azidocarbonyl) -1-ethenyl] -7-methoxybenzo [b] furan-4-carboxylate; 2- (7-methoxybenzene [b] thiophene-3-yl) acetamide; 2- (7-methoxybenzene [b] thiophene-3-yl) ethylamine; ethyl 2- (7-methoxybenzene [b] thiophene-3-yl) ethylcarbamate; ethyl-2- (7-methoxy-1-benzofuran-3-yl) ethylcarbamate; or 1-methyl-3- (2-methoxy-5-carbmethoxy-phenyl-hydrazono) -piperidin-2-one. Claim 57 A compound that is methyl (6-methoxy-4-oxo-3,4-dihydrobenzo [4,5] furo [2,3-d] pyridazine-9-carboxylate; methyl (4-chloro-6-methoxybenzo [ 4,5] furo [2,3-d] pyridazine) -9-carboxylate; methyl (6-methoxybenzo [4,5] furo [2,3-d] pyridazin) -9-carboxylate; 6-methoxybenzo [4, 5] furo [2,3-d] pyridazin-9-carboxylic acid; 4-nitrophenyl 6-methoxybenzo [4,5] furo [2,3-d] pyridazin-9-carboxylate, 6-methoxy-3,4- dihydrobenzo [4,5] furo [3,2-d] pyrimidin-4-one; 6-methoxybenzo [4,5] furo [3,2-d] pyrimidine; 9-bromo-6-methoxybenzo [4,5] furo [3,2-d] pyrimidine; 6-methoxybenzo [4,5] furo [3,2-d] pyrimidin-9-yl cyanide; 6-methoxybenzo [4,5] furo [3,2-d] pyrimidin-9-carboxylic acid; 4-nitrophenyl 6-methoxybenzo [4,5] furo [3,2-d] pyrimidin-9-carboxylate; ethyl-8-methoxy-1,2,3,4-tetrahydrobenzo [4,5 ] thieno [2,3-c] pyridin-2-carboxylate; ethyl-5-formyl-8-methoxy-1,2,3,4-tetrahydrobenzo [4,5] thieno [2,3-c] pyridin-2 -carboxylate; 2-ethoxycarbonyl-8-methoxy-1,2,3,4-tetrahydrobenzo [4,5] thieno [2,3-] pyridine-5-carbox acid Ilic; 2-ethyl-5- (4-nitrophenyl) -8-methoxy-1,2,3,4-tetrahydrobenzo [4,5] thieno [2,3-c] pyridine-2,5-dicarboxylate; 2-ethyl-5- (4-nitrophenyl) -8-methoxy-1,2,3,4-tetrahydrobenzo [4,5] thieno [2,3-c] pyridine-2,5-dicarboxylate; ethyl-6-difluoromethoxy-4-oxo-3,4-dihydrobenzo [4,5] furo [2,3-d] pyridazine-9-carboxylate; ethyl-4-chloro-6-difluoromethoxybenzo [4,5] furo [2,3-d] pyridazine-9-carboxylate; ethyl-6-difluoromethoxybenzo [4,5] furo [2,3-d] pyridazine-9-carboxylate; 6-Difluoromethoxybenzo [4,5] furo [2,3-d] pyridazine-9-carboxylic acid; 4-nitrophenyl 6-difluoromethoxybenzo [4,5] furo [2,3-d] pyridazine-9-carboxylate; 2-tert-Butyloxycarbonyl-8-methoxy-1,2,3,4-tetrahydrobenzo [4,5] thieno [2,3-c] pyridine-5-carboxylic acid; 2 (tert-butyl) -5- (4-nitrophenyl) -8-methoxy-1,2,3,4-tetrahydrobenzo [4,5] thieno [2,3-c] pyridine-2,5-dicarboxylate; tert-butyl-5- (3,5-dichloro-4-pyridylcarbamoyl) -8-methoxy-1,2,3,4-tetrahydrobenzo [4,5] thieno [2,3-c) pyridine-2-carboxylate; 2-ethoxycarbonyl-6-methoxy-1,2,3,4-tetrahydro [1] benzofuro [3,2-c] pyridine; 2-ethoxycarbonyl-6-methoxy-1,2,3,4-tetrahydro [1] benzofide (3,2-c] pyridin-9-carbaldehyde; 2-ethoxycarbonyl-6-methoxy-1,2,3,4 -tetrahydro [12] benzofide (3,2-c] pyridine-9-carboxylic acid; 4-nitrophenyl- (2-ethoxycarbonyl] -6-methoxy-1,2,3,4-tetrahydro [1] benzofide [3,2 -c] pyridin) -9-carboxylate; methyl-1-hydroxy-6-methoxybenzo [4,5] furo [3,2-c] pyridin-9-carboxylate; methyl-1-chloro-6-methoxybenzo [4, 5] furo [3,2-c] pyridin-9-carboxylate; metho-6-methoxybenzo [4,5] furo [3,2-c) pyridin-9-carboxylate; 6-methoxybenzo [4,5] furo [3, 2-c] pyridin-9-carboxylic acid; 4-nitrophenyl-6-methoxybenzo [4.5] furo [3,2-c] pyridin-9-carboxylate; ethyl 8-methoxy-3,4-dihydro [1] benzofide [ 2,3-c] pyridin-2 (1H) -carboxylate; ethyl 5-formyl-8-methoxy-3,4-dihydro [1] -benzofuro [2,3-c] pyridin-2 (1H) -carboxylate; 2- (ethoxycarbonyl) -8-methoxy-1,2,3,4-tetrahydro [1] benzofuro [2,3-c] pyridine-5-carbox acid |
priorityDate | 2004-12-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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