http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-037090-A1
Outgoing Links
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| filingDate | 2002-09-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
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| publicationDate | 2004-10-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-037090-A1 |
| titleOfInvention | PIRAZOLILO SUBSTITUTED COMPOUNDS FOR THE TREATMENT OF INFLAMMATIONS |
| abstract | A compound to treat cancer, inflammation and inflammation-related disorders, for example arthritis. Claim 1: A compound characterized in that it responds to formula (1) wherein A is (CH2) m; where each CH2 can be independently substituted with one or more substitutions selected from the group consisting of: hydroxy, halogen, alkoxy, lower alkyl, amino, aminoalkyl, alkylamino, alkenyl, and alkynyl; m is between 1 and 4; B is a 5- or 6-membered heteroaryl, aryl, saturated or unsaturated heterocyclic wherein said aryl, heteroaryl, or heterocyclic is optionally substituted with R1, R2, and R12; X is selected from the group consisting of: N and C; Y and Z are independently selected from the group consisting of: N, CH, CR3, S, and O; R1 is selected from the group consisting of: hydride, halogen, alkyl, aryl, heteroaryl, alkenyl, alkynyl, haloalkyl, CN, NO2, OR5, OCOOR5, CO2R7, CON (R6) R7, COR6, SR6, SOR6, SO2R6, NR6R7, NR6COR7, NR6CONHR7, NR6SO2R7, NR6SO2NHR7, and SO2N (R6) R7 where R6 and R7 can be taken together to form a 3-7 membered carbocyclic ring with between 1 and 3 substituted or unsubstituted heteroatoms selected from the group consisting of: S, SO , SO2, O, and NR6; wherein said alkenyl, alkynyl, alkyl, aryl, heteroaryl or OR5 are optionally substituted with, hydride, halogen, alkyl, hydroxyalkyl, aryl, heteroaryl, haloalkyl, COCF3, CN, NO2, OR5, OCOOR5, CO2R7, CON (R6) R7, COR6, SR6, SOR6, SO2R6, NR6R7, NR6COR7, NR6CONHR7, NR6SO2R7, NR6SO2NHR7, and SO2N (R6) R7 where R6 and R7 can be taken together to form a 3-7 membered carbocyclic ring with between 1 and 3 substituted heteroatoms or unsubstituted selected from the group consisting of: S, SO, SO2, O, and NR6; R2 is selected from the group consisting of: halogen, hydride, hydroxyalkyl, alkyl, OR6, CN, NO2, SR6, NHR6, CON (R6) R7, NHCONHR6, CO2H, and haloalkyl; R1 and R2 can be taken together to form a saturated 5- or 7-membered carbocyclic ring that optionally contains between 0 and 3 heteroatoms selected from the group consisting of N, O, or S, and where said ring is optionally substituted with R1; R3 is selected from the group consisting of: substituted or unsubstituted amide, alkylamino, aminoalkyl, CONHR7, NH2, NHCOR6, and CH2NHCOR6 with the proviso that when R3 is NH2 or NHCH3, then R1, R2, R4, R11, and R12 are not hydride; R4 is selected from the group consisting of: halogen, alkylsulfinyl, alkylsulfonyl, cyano, alkoxycarbonyl, alkyl, haloalkyl, hydride, hydroxyalkyl, haloalkoxy, heterocyclic, nitro, acylamino, aryl, heteroaryl, and alkenyl, OR13, SR8, SO2N (R8) R8 ', NHR9, NHCOR9, NR9COR9, NHCO (OR9), NR9CO (OR9), NR8SO2R10, NHSO2N (R10) R10', NR6CON (R10) R10 ', COR9, CO2R8, CON (R8) R8', where R8 and R8 ' they can be taken together to form a 3-7 membered carbocyclic ring with between 1 and 3 substituted or unsubstituted heteroatoms selected from S, SO, SO2, O, N, and NR6, and where R10 and R10 'can be taken together to form a 3-7 membered carbocyclic ring with between 1 and 3 substituted or unsubstituted heteroatoms selected from S, SO, SO2, O, N, and NR6 where said aryl, heterocyclic, heteroaryl, or alkenyl is optionally substituted with R9; R5 is selected from the group consisting of: hydride, alkyl, aryl, arylalkyl, heteroaryl, heterocyclicalkyl, and heteroarylalkyl, where aryl, alkyl, arylalkyl, heteroaryl, heterocyclicalkyl, or heteroarylalkyl are optionally substituted with one or more radicals selected from the group consisting of OR14 , N (R14) R14 ', and glycols; R6 is independently selected from the group consisting of: hydride, aryl, heteroaryl, lower alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxy, alkoxyalkyl, heterocyclicalkyl, and heterocyclic; R7 is independently selected from the group consisting of: hydride, aryl, heteroaryl, lower alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxy, alkoxyalkyl, heterocyclicalkyl, and heterocyclic; R8 is independently selected from the group consisting of: hydride, aryl, heteroaryl, arylalkyl, heterocyclic, haloalkyl, arylalkyl amino, alkylaminoalkyl, dialkylaminoalkyl, alkyl, alkenyl, alkynyl, heteroarylalkyl, and heterocyclicalkyl; R8 'is independently selected from the group consisting of: hydride, aryl, heteroaryl, arylalkyl, heterocyclic, haloalkyl, arylalkylamino, alkylaminoalkyl, dialkylaminoalkyl, alkyl, alkenyl, alkynyl, heteroarylalkyl, and heterocyclicalkyl; R9 is independently selected from the group consisting of: hydride, lower alkyl, aryl, heteroaryl, arylalkyl, heterocyclic, cycloalkyl, heterocyclicalkyl, haloalkyl, arylalkyl amino, amino, aminoalkyl, aminoacyl, nitro, azido, and heteroarylalkyl, where alkyl, aryl, heteroaryl, aminoalkyl, or arylalkyl are optionally substituted with one or more radicals selected from the group consisting of: alkylsulfonamide, sulfamyl, alkyl, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, aminoalkyl, alkylaminoalkyl, alkoxy, halogen, acyloxy, oxy, formyl, haloalkyl, cyano, haloalkoxy, acyl, carboxyl, hydroxy, hydroxyalkyloxy, phenoxy, nitro, azido, benzyloxy, dialkylaminoacyl, thioalkyl, aminoacyloxy, thiocyanate, isothiocyanate, alquildioxi, hydroxyalkyl, alkylamino, alkyloxycarbonyl, alkoxyalkyl, alkenylamino, alkynylamino, alkenyl, alkynyl, dialkylaminoalkyloxy, and heterocyclic optionally substituted with alkyl, alkylamino, aminoalkyl, hydroxyalkyl, and alkylaminoalkyl; R10 is independently selected from the group consisting of: hydride, lower alkyl, heteroaryl, heterocyclic, haloalkyl, arylalkyl amino, heteroarylalkyl, aryl, and arylalkyl, where aryl, heteroaryl, heterocyclic, or arylalkyl are optionally substituted with one or more radicals selected from alkyl, alkoxy, halogen, haloalkyl, cyano, haloalkoxy, acyl, carboxyl, hydroxy, hydroxyalkyloxy, phenoxy, benzyloxy, dialkylaminoalkyloxy, and heterocyclic; R10 'is independently selected from the group consisting of: hydride, lower alkyl, heteroaryl, heterocyclic, haloalkyl, arylalkyl amino, heteroarylalkyl, aryl, and arylalkyl, where aryl, heteroaryl, heterocyclic, or arylalkyl are optionally substituted with one or more radicals selected from alkyl , alkoxy, halogen, haloalkyl, cyano, haloalkoxy, acyl, carboxyl, hydroxy, hydroxyalkyloxy, phenoxy, benzyloxy, dialkylaminoalkyloxy, and heterocyclic, R11 is selected from the group consisting of: hydride, halogen, haloalkyl, CN, CO2R5, lower alkyl, alkenyl lower, lower alkynyl, alkoxy, and CONH2; R12 is selected from the group consisting of: hydride, halogen, alkyl, and alkoxy; R13 is selected from the group consisting of: hydride, alkyl, aryl, arylalkyl, heteroaryl, heterocyclicalkyl, and heteroarylalkyl, where aryl, alkyl, arylalkyl, heteroaryl, heterocyclicalkyl, or heteroarylalkyl are optionally substituted with one or more radicals selected from the group consisting of OR14 , N (R14) R14 ', and glycols; R14 is independently selected from the group consisting of hydride, and lower alkyl; and R14 'is independently selected from the group consisting of hydride, and lower alkyl; with the proviso that when R1 is sulfamyl, then R4 is not halogen, alkylthio, alkylsulfinyl, alkylsulfonyl, cyano, carboxyl, alkoxycarbonyl, amido, N-monoalkylamido, N-monoarylamido, alkyl, N, N-dialkylamido, N-alkyl- N-arylamido, haloalkyl, hydride, hydroxyl, alkoxy, hydroxyalkyl, haloalkoxy, sulfamyl, N-alkylsulfamyl, amino, alkylamino, heterocyclic, nitro, and acylamino, and / or when R4 is sulfamyl, then R1 is not sulfamyl, halogen, alkyl , alkoxy, hydroxyl and haloalkyl; or isomers, vehicles, esters, prodrugs, salts acceptable for pharmaceutical use thereof. |
| priorityDate | 2001-09-19-04:00^^<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: 103.