http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-043184-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_e9c55cbd632f124625c19c848aaffd9c |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 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/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D407-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4965 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-495 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-50 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-501 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D407-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A01N43-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-47 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D- http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A01N43-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A01N43-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A01N43-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-497 |
| filingDate | 2004-02-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-07-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-043184-A1 |
| titleOfInvention | PIRAZOLES AND METHODS OF ELABORATION AND USE OF THESE |
| abstract | This is based on the discovery that the compounds of formula (1) unexpectedly possess high affinity for Alk5 and / or Alk4, and may be useful as antagonists of these to prevent and / or treat numerous diseases, including fibrotic disorders, and inhibition of T 6 Fbeta receptors Claim 1: A compound of formula (1) or an N-oxide, or a pharmaceutically acceptable salt of said compound; wherein each Ra is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocicloalquilsulfanilo, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl or heteroaroyl; R1 is a bond, alkylene, alkenylene, alkynylene, or - (CH2) r1-O- (CH2) r2-, where each of r1 and r2 is independently 2 or 3; R2 is cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl or a bond; R3 is -C (O) -, -C (O) O-, -OC (O) -, -C (O) -N (Rb), -N (Rb) -C (O) -, -OC ( O) -N (Rb) -, -N (Rb) -C (O) -O-, -OS (O) pN (Rb), -N (Rb) -S (O) pO-, -N (Rb ) -C (O) -N (Rc) -, -N (Rb) -S (O) pN (Rb) -, -C (O) -N (Rb) -S (O) p-, -S ( O) pN (Rb) -C (O) -, -S (O) pN (Rb) -, -N (Rb) -S (O) p-, -N (Rb) -, -S (O) p -, -O-, -S-, or - (C (Rb) (Rc)) q-, or a bond; wherein each of Rb and Rc is independently H, hydroxy, alkyl, aryl, .aralkyl, heterocycloalkyl, heteroaryl or heteroaralkyl, p is 1 or 2; and q is 1-4; R4 is H, alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl) alkyl, heterocycloalkyl, (heterocycloalkyl) alkyl, cycloalkenyl, (cycloalkenyl) alkyl, heterocycloalkenyl, (heterocycloalkenyl) alkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; R5 is H, unsubstituted alkyl, halo-substituted alkyl, alkoxy, alkylsulfinyl, amino, alkenyl, alkynyl, cycloalkyl, cycloalkoxy, cycloalkylsulfinyl, heterocycloalkyl, heterocycloalkoxy, heterocycloalkylsulfinyl, aryl, aryloxy, arylsulfinyl, heteroaryl, heteroaryl, heteroaryl, heteroaryl; R6 is (1) a heterocyclyl of 5 to 6 members containing 1 to 3 ring heteroatoms selected from the group consisting of -O-; -S-, -N = and -NRd-, where Rd is H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl or heteroaralkyl; said heterocyclyl is substituted with Re and optionally substituted with one or two Rf; where Re is oxo, thioxo, alkoxy, alkylsulfinyl, -NH2-, -NH (unsubstituted alkyl), or -N (unsubstituted alkyl) 2 and Rf is alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino , nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, alkylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, cycloalkylsulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfyl, cycloalkyl sulfoyl, cycloalkyl, cycloalkyl, cycloalkyl sulfyl, cycloalkyl, cycloalkyl, cycloalkyl, cycloalkyl; , heterocycloalkyl, heterocycloalkyloxy, heterocycloalkylsulfanyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; or (2) a fused heteroaryl ring selected from the group consisting of the moieties of formulas (2) where ring A is an aromatic ring containing 0 to 4 ring heteroatoms, and ring B is an aromatic or non-aromatic ring of 5 to 7 members, containing 0 to 4 ring heteroatoms, provided that at least one of ring A and ring B contains one or more ring heteroatoms; ring A´ is an aromatic ring containing 0 to 4 ring heteroatoms, and ring B´ is a saturated or unsaturated ring, with 5 to 7 members, containing 0 to 4 ring heteroatoms, provided that at least one of ring A 'and ring B' contain one or more ring heteroatoms; each ring heteroatom is -O-, -S-, -N =, or NRg-; each X1 is independently N or C; each X2 is independently -O-; -S-; -N =, -NRg-, or -CHRh-; where Rg is H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl or heteroaralkyl; each of Rh and Ri is independently alkyl, alkenyl, alkynyl, alkoxy, acyl, halo, hydroxy, amino, nitro, oxo, thioxo, cyano, guanadino, amidino, carboxy, sulfo, mercapto, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, aminocarbonyl, alkylcarbonylamino, arylcarbonylamino, heteroarylcarbonylamino, alkylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkoxycarbonyl, alkylcarbonyloxy, urea, thiourea, sulfamoyl, sulfamide, carbamoyl, cycloalkyl, cycloalkyloxy, cycloalkylsulfanyl, cycloalkylcarbonyl, heterocycloalkyl, heterocycloalkyloxy, heterocicloalquilsulfanilo, heterocycloalkylcarbonyl, aryl, aryloxy, arylsulfanyl, aroyl, heteroaryl, heteroaryloxy, heteroarylsulfanyl, or heteroaroyl; n is 0 to 2; and m is 0 to 3; provided that when m is 2, two adjacent Ra groups can be joined to form an optionally substituted cyclic portion, of 4 to 8 members; provided that if R6 is 2-naphthyridinyl, 4-quinolinyl, imidazo [1,2-a] pyridyl, or benzimidazolyl, then -R1-R2-R3-R4 is not H, unsubstituted alkyl, -CH2-C (O) -N (H) -alkyl, -CH2-C (O) -N (alkyl) 2 or benzyl. |
| priorityDate | 2003-02-12-04:00^^<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: 69.