http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-073677-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_b86ef86a8b00f49ca5a1c9a3bd58f41d http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1c89ce4d9ac03f9acd8ddede1162f94d |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D235-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D235-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 |
| filingDate | 2009-09-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2010-11-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-073677-A1 |
| titleOfInvention | CYCLE DERIVATIVES OF BENZIMIDAZOL PROTEINQUINASA ACTIVATORS OF AMP, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND USE OF THE SAME IN THE TREATMENT OF TYPE II, OBESITY AND OTHER DISEASES. |
| abstract | Claim 1: A compound of structural formula 1: or a pharmaceutically acceptable salt thereof, wherein: X is absent or selected from; (24) -CH2-, (25) -CHF-, (26) -CF2-, (27) -S-, (28) -O-, (29) -O-CH2-, (30) -NH- , (31) -C (O) -, (32) -NHC (O) -, (33) -C (O) NH-, (34) -NHSO2-, (35) -SO2NH-, and (36) -CO2-, where each CH2 is unsubstituted or substituted by 1 or 2 substituents selected from: hydroxy, halogen, NH2, C1-6 alkyl, CO2H, CO2 C1-6 alkyl, CO C1-6 alkyl, phenyl and -CH2phenyl, and where each NH is unsubstituted or substituted by 1 substituent selected from: C1-6 alkyl, CO2H, CO2 C1-6 alkyl, CO C1-6 alkyl, phenyl and -CH2phenyl; And is selected from: (6) C3-10 cycloalkyl, (7) C3-10 cycloalkenyl, (8) C2-10 cycloheteroalkyl, (9) C2-10 cycloheteroalkenyl, (10) aryl, and (11) heteroaryl, where the cycloalkyl , cycloalkenyl, cycloheteroalkyl, cycloheteroalkenyl, aryl and heteroaryl are unsubstituted or substituted by 1, 2, 3 or 4 substituents selected from Rb is selected from: (35) oxo, (36) -CN, (37) - (CH2) nCO2H , (38) - (CH2) nCO2Ri, (39) - (CH2) nOH, (40) - (CH2) nC (O) NHRg, (41) - (CH2) nNHC (O) C1-6 alkyl, (42 ) - (CH2) nNHSO2Ri, (43) - (CH2) nSO2NHRg, (44) (CH2) nSO2NHC (O) Ri, (45) - (CH2) nSO2NHCO2Ri, (46) - (CH2) nSO2NHCON (Rg) 2, (47) - (CH2) nC (O) NHSO2Ri, (48) - (CH2) nNHC (O) N (Rg) 2, (49) - (CH2) C3-10-CO2Recycloalkyl alkyl, (50) heteroaryl, ( 51) -C2-10 cycloheteroalkenyl, and (52) -C2-10 cycloheteroalkyl, where each CH2 is unsubstituted or substituted by 1 or 2 substituents selected from C1-6 alkyl, -OH and -NH2, where each NH is unsubstituted or substituted by 1 substituent selected from Rc , and where each alkyl, cycloalkyl, cycloheteroalkyl, cycloheteroalkenyl, aryl and heteroaryl is unsubstituted or substituted by 1, 2, 3 or 4 substituents selected from Rc; each R1 and R2 is independently selected from: (1) hydrogen, (2) halogen, (3) -CH, (4) -CF3, (5) -C1-6 alkyl, (6) -C2-6 alkenyl, ( 7) C2-6 alkynyl, (8) - (CH2) C3-10 cycloalkyl, (9) (CH2) pcicIoaC3-7-aryl alkyl, (10) - (CH2) C3-7-cycloalkyl-heteroaryl, (11) - (CH2) C4-10 cycloalkenyl, (12) - (CH2) C4-7-aryl cycloalkenyl, (13) - (CH2) C4-7-heteroaryl cycloalkenyl, (14) - (CH2) C2-10 cycloheteroalkyl, (15 ) - (CH2) C2-10 pcicIoheteroaqueniIo, (16) - (CH2) paryl, (17) biphenyl, (18) - (CH2) pheteroaryl, (19) -C2-6 -alkenyl, (20) -C2 alkenyl -6-aryl, (21) -C2-6 alkenyl-heteroaryl, (22) -C2-6-alkenyl C3-7, (23) -C2-alkenyl 6 -6-C3-7 cycloalkenyl, (24) -C2-alkenyl C2-7 6-cycloheteroalkyl, (25) -C2-6 -alkenyl C2-7 cycloheteroalkenyl, (26) -C2-6 -alkynyl-(CH2) 1-3-O-aryl, (27) -C2-6 -alkyl alkyl, (28) -C2-6 -alkyl-aryl, (29) -C2-6 -alkyl-heteroaryl, (30) -C2-6 -alkyl-C3-7 -alkyl, (31) -C2-6 -alkyl-C3- cycloalkenyl 7, (32) -alquin C2-6 -C3-7cycloheteroalkyl, (33) -C2-6 -alkyl-C2-7 cycloheteroalkenyl, and (34) -C (O) NH- (CH2) 0-3phenyl, where each CH2 is unsubstituted or substituted by 1 or 2 substituents selected from: halogen, CF3, -OH, -NH2, -C 1-6 alkyl, -C 1-6 alkyl, -NC 1-6 alkyl and -N (C 1-6 alkyl) 2, where each alkyl , alkenyl and alkynyl is unsubstituted or substituted by 1, 2 or 3 substituents selected from: halogen, CF3, -OH, -NH2, -C1-6 alkyl, -C1-6 alkyl, -N C1-6 alkyl and -N ( alkyl and where each cycloalkyl, cycloalkenyl, cycloheteroalkyl, cycloheteroalkenyl, phenyl, aryl and heteroaryl is unsubstituted or substituted by 1, 2, 3 or 4 substituents independently selected from Ra, with the proviso that at least one of only one of R1 and R2 is selected from the group consisting of: hydrogen, halogen, -CN, -CF3, -C1-6 alkyl, -C2-6 alkenyl and -C2-6 alkynyl, and with the proviso that if R1 or R2 is hydrogen , then at least one of R3 and R4 don't be hydrogen; R3 and R4 are each independently selected from: (5) hydrogen, (6) halogen, (7) -C1-6 alkyl, (8) -C2-6 alkenyl, (9) -C2-6 alkynyl, (10 ) -C3-10 cycloalkyl, (11) -C3-10 cycloalkenyl, (12) aryl, (13) heteroaryl, (14) -CN, (15) -CF3, (16) -OH, (17) -C1 alkyl -6, (18) -NH2, (19) -NH1-6alkyl, (20) -N (C1-6alkyl) 2, (21) -C1-6alkyl, (22) -SO1-6alkyl, ( 23) -SO2 C1-6 alkyl, (24) -NHSO2 C1-6 alkyl, (25) -NHC (O) C1-6 alkyl, (26) -SO2N C1-6 alkyl, and (27) -C (O) NH C1 alkyl -6; R5 is selected from: (7) hydrogen, (8) -C1-6 alkyl, (9) -CH2CO2H, and (10) -CH2CO2C1-6 alkyl; each Ra is independently selected from the group consisting of: (1) halogen, (2) oxo, (3) - (CH2) mOH, (4) (CH2) mN (Rj) 2, (5) (CH2) mNO2 , (6) (CH2) mCN, (7) -C1-6 alkyl, (8) - (CH2) mCF3, (9) - (CH2) mOCF3, (10) -OCH2 or C1-6 alkyl, (11) -OCH2 -aryl, (12) - (CH2) mC (= N-OH) N (Rj) 2, (13) - (CH2) mC 1-6 alkyl, (14) - (CH2) mO-aryl, (15) - OCH2phenyl, (16) (CH2) m C1-6 alkyl, (17) (CH2) mS (O) C1-6 alkyl, (18) - (CH2) mS (O) 2 C1-6 alkyl, (19) - (CH2 ) mNHS (O) 2 C1-6 alkyl, (20) - (CH2) mC (O) Rf, (21) (CH2) mC (O) N (Rj) 2, (22) - (CH2) mN (Rj) C (O) Rf, (23) - (CH2) mN (Rj) C (O) N (Rj) 2, (24) - (CH2) mCO2H, (25) - (CH2) mOC (O) H, ( 26) (CH2) mCO2Rf, (27) - (CH2) mOC (O) Rf, (28) - (CH2) C3-7 cycloalkyl, (29) - (CH2) C3-7 cycloalkenyl, (30) - (CH2 ), C2-6 cycloheteroaIquIo, (31) - (CH2) C2-6 cycloheteroaIquenyl, (32) - (CH2) rnaryl, and (33) - (CH2) mheteroaryl, where each CH2 is unsubstituted or substituted by 1 or 2 substituents selected from: oxo, - (CH2) 0-3OH, -CN, -NH2, -NH (C1-6 alkyl), -N (C1-6 alkyl) 2, -C1 alkyl 6, -C1-6alkyl, halogen, -CH2F, -CHF2, -CF3, -CO2H, -CO2C1-6alkyl, -C3-7cycloalkyl, phenyl, CH2phenyl, heteroaryl and CH2heteroaryl, and where alkyl, cycloalkyl, cycloheteroalkyl , phenyl, aryl and heteroaryl are unsubstituted or substituted by 1, 2, 3 or 4 substituents selected from: oxo, - (CH2) 0-3OH, -CN, -NH2, -NH (C1-6 alkyl), -N (C1-6 alkyl) 2, -C1-6 alkyl, -C1-6 alkyl, halogen, -CH2F, -CHF2, -CF3, -CO2H, -CO2C1-6 alkyl, -C3-7 cycloalkyl, phenyl, CH2phenyl, heteroaryl and CH2heteroaryl; each Rb is independently selected from: (14) hydrogen, (15) -C1-6 alkyl, (16) -C3-6 cycloalkyl, (17) -C3-6 cycloalkenyl, (18) -C3-6 cycloheteroalkyl, (19 ) aryl, (20) heteroaryl, (21) halogen, (22) -OH, (23) -NO2, (24) -NH2, (25) -NH (C1-6 alkyl), (26) -N (alkyl C1-6) 2, (27) -C1-6 alkyl, (28) - (CH2) qCO2H, (29) - (CH2) qCO2C1-6 alkyl, (30) -CF3, (31) -CN (32) -SO2 C1-6alkyl, and (33) - (CH2) qCON (Re) 2, where each CH2 is unsubstituted or substituted by 1 or 2 halogens, and where each alkyl, cycloalkyl, cycloalkenyl, cycloheteroalkyl, aryl and heteroaryl are without substitute or replace with 1, 2 or 3 halogens; each Rc is independently selected from: (21) halogen, (22) oxo, (23) - (CH2) rOH, (24) - (CH2) rN (Re) 2, (25) - (CH2) rCN, (26 ) -C1-6 alkyl, (27) -CF3, (28) -C1-6 alkyl-OH, (29) -OCH2C1-6 alkyl, (30) - (CH2) C1-6 alkyl, (31) -OCH2aryl , (32) - (CH2) r C1-6 alkyl, (33) - (CH2) rC (O) Rf, (34) - (CH2) rC (O) N (Re) 2, (35) - (CH2) rCO2H, (36) - (CH2) rCO2Rf, (37) - (CH2) C3-7cycloalkyl, (38) - (CH2) C2-6cycloheteroalkyl, (39) - (CH2) raryl, and (40) - ( CH2) rheteroaryl, where each CH2 is unsubstituted or substituted by 1 or 2 substituents selected from: oxo, -OH, -CN, -N (Rh) 2, -C1-6 alkyl, -C1-6 alkyl, halogen, - CHF2, -CHF2, -CF3, -CO2H, -CO2C1-6 alkyl, -C3-7cycloalkyl and heteroaryl, and where the alkyl, cycloalkyl, cycloheteroalkyl, aryl and heteroaryl are unsubstituted or substituted by 1, 2, 3 or 4 substituents selected from: oxo, -OH, -CN, -N (Rh) 2, -C1-6 alkyl, -C1-6 alkyl, halogen, -CHF2, -CHF2, -CF3, -CO2H, -CO2C1-6 alkyl , C3-7 cycloalkyl and het eroaryl; each Re, Rg and Rh is independently selected from: (1) hydrogen, and (2) alkyl where the alkyl is unsubstituted or substituted by 1, 2, 3 or 4 substituents selected from: -OH, oxo, halogen, alkyl - C1-6alkyl, -NH2, -NH (C1-6 alkyl) and -N (C1-6 alkyl) 2; each Rj is independently selected from: (1) hydrogen, (2) C1-6 alkyl, (3) C3-6 cycloalkyl, (4) -C (O) Ri, and (5) -SO2Ri, where the alkyl and the Cycloalkyl are unsubstituted or substituted by 1, 2, 3 or 4 substituents selected from: -OH, oxo, halogen, C1-6 alkyl, -C1-6 alkyl, -NH2, -NH (C1-6 alkyl) and -N (C1-6 alkyl) 2; each Rf and Ri is independently selected from: (19) C1-6 alkyl, (20) C4-7 cycloalkyl, (21) C4-7 cycloalkenyl, (22) C3-7 cycloheteroalkyl, (23) C3-7 cycloheteroalkenyl, ( 24) aryl, and (25) heteroaryl, wherein alkyl, cycloalkyl, cycloalkenyl, cycloheteroalkyl, cycloheteroalkenyl, aryl and heteroaryl are unsubstituted or substituted by 1, 2, 3 or 4 substituents selected from: oxo, -OH, -CN, -NH2, -C1-6alkyl, -C1-6alkyl, halogen, -CH2F, -CHF2, -CF3, -CO2H, -CO2C1-6alkyl, -C3-7cycloalkyl and heteroaryl; n is 0, 1, 2, 3 or 4; m is 0, 1, 2, 3 or 4; p is 0, 1, 2 or 3; q is 0, 1, 2, 3 or 4; and r is 0, 1 or 2. |
| priorityDate | 2008-09-26-04:00^^<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: 31.