http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-056884-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_aeeae3a1e9c2f6b4db133adad89691b1 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5025 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D253-07 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4985 |
| filingDate | 2006-11-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2007-10-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-056884-A1 |
| titleOfInvention | MTOR INHIBITING FUSIONED BICYCLE COMPOUNDS |
| abstract | They are mTOR inhibitors and are useful in the treatment of cancer. Claim 1: A compound represented by formula (1), or a salt acceptable for pharmaceutical use thereof, wherein, X1, and X2 are each independently N or C- (E1) aa; X5 is N, C- (E1) aa, or N- (E1) aa; X3, X4, X6, and X7 are each independently N or C; where at least one of X3, X4, X5, X6 and X7 is independently N or N- (E1) aa; it is C0-10 alkyl, C3-10 cycloalkyl, C3-10 aminomethylcycloalkyl, C5-10 cycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, heterocyclyl or heterobicycloalkyl, any of which is optionally substituted with one or more independent G11 substituents; Q1 is A (R1) mB (W) n or B (G11) nA (Y) m; A and B are respectively, aromatic or heteroaromatic rings of 5 and 6 members, fused to form a 9-membered heteroaromatic system with the exception of 5-benzo [b] furyl and 3-indolyl; and with the proviso of 2-indolyl, 2-benzoxazol, 2-benzothiazol, 2-benzimidazolyl, 4-aminopyrrolpyrimidin-5-yl, 4-aminopyrrolpyrimidin-6-yl and derivatives of 7-deaza-7-adenosinyl when X1 and X5 they are CH, X3, X6 and X7 are C, and X2 and X4 are N; or Q1 is A (R1) mA (Y) m, where each A is the same ring or a different 5-membered aromatic or heteroaromatic ring and the two merge to form an 8-membered heteroaromatic system; R1 is independently, hydrogen, -N (C0-8 alkyl) (C0-8 alkyl), hydroxyl, halogen, oxo, aryl (optionally substituted by 1 or more R31 groups), hetaryl (optionally substituted by 1 or more R31 groups) , C1-6 alkyl, -C0-8 alkyl-C3-8 cycloalkyl, -C0-8-NR311S alkyl (O) 0-2R321, -C0-8-NR311S (O) 0-2NR321R331, -C0-8 alkyl -S (O) 0-2NR311R321, -alkyl C0-8-NR311COR321, - alkyl C0-8-NR311CO2R321, -alkyl C0-8-NR311CONR321R331, -alkyl C0-8-CONR311R321, -alkyl C0-8CON (R311) (O) 0-2R321, -C0-8-CO2R311 alkyl, -C0-8-S alkyl (O) 0-2R311, -C0-8-O-C1-8 alkyl, -C0-8-O-alkyl C0-8-alkyl C3-8 alkyl, -C0-8-O-alkyl C0-8 alkylhetero-C0-8-O-C0-8 alkyl, -C0-8-aryl alkyl, -C0-8 alkyl Hetaryl, -C0-8-heterocyclyl alkyl, -C0-8-O-C0-8 alkylheteroyl, -C0-8-S-alkyl-C0-8, -C0-8-S-alkyl-C0-8-cycloalkyl C3-8, - alkyl C0-8-S-alkylheterocyclyl C0-8, -alkyl C0-8-S-alkylaryl C0-8, -alkyl C0-8-S-alkylheteroyl C0-8, -alkyl C0-8-N (R311) -C0-8 alkyl, -C0-8-N alkyl (R311) -C0-8 alkyl-C3-8 alkyl, -C0-8-N alkyl (R311) -C0-8 alkylheterocyclyl , - C0-8-N (R311) -C0-8 -alkylaryl, -C0-8-N-alkyl (R311) -C0-8 alkylhetaryl, -C0-8-NR311R321 -alkyl, -C2-8 -alkenyl, -C2 -alkyl -8, NO2, CN, CF3, OCF3, OCHF2 provided that Q1 is not N-methyl-2-indolyl, N (phenylsulfonyl) -2-indolyl or N-tert-butoxycarbonyl; W is independently hydrogen, -N (C0-8 alkyl) (C0-8 alkyl), hydroxyl, halogen, oxo, aryl (optionally substituted by 1 or more R31 groups), heteroaryl (optionally substituted by 1 or more R31 groups), C1-6 alkyl, -C0-8 alkyl-C3-8 cycloalkyl, -C0-8-NR312S alkyl (O) 0-2R322, -C0-8-NR311S (O) 0-2NR321R331, -C0-8 alkyl NR311CO2R321, -alkyl C0-8-CON (R311) S (O) 0-2R321, -alkyl C0-8-S (O) 0-2NR312R322, -alkyl C0-8-NR312COR322, -alkyl C0-8-NR312CONR322R332, -C0-8-CONR312R322 alkyl, -C0-8-CO2R312 alkyl, -C0-8-S alkyl (0) 0-2R312, -C0-8-O-C1-8 alkyl, -C0-8-O alkyl -C0-8 alkylcyclyl, -C0-8-O-alkyl-C0-8 alkylheterocycloalkyl, -C0-8 alkyl-O-C0-8 alkylaryl, C0-8 -alkylaryl, -C0-8 alkylhetaryl, -C0-8 -alkylheterocyclyl, -O-aryl, -C0-8-O-alkyl C0-8 alkyl, -C0-8-S-alkyl C0-8, -C0-8-S-alkyl C0-8-C3-8 cycloalkyl, - C0-8-S-alkyl-heterocycI-C0-8 alkyl, -C0-8-S-C0-8 alkyl, -C0-8-S-alkyl C0-8 alkylhetero, -alq C0-8-N (R312) -C0-8 alkyl, -C0-8-N-alkyl (R312) -C0-8-alkyl-C3-8 alkyl, -C0-8-N-alkyl (R312) -C0-alkyl-alkylcycloalkyl 8, -C0-8-N-alkyl (R312) -C0-8 -alkylaryl, -C0-8-N -alkyl (R312) -C0-8 -alkylhetaryl, C0-8-NR312R322 -alkyl, -C2-8 -alkenyl, -C2 -alkyl -8, NO2, CN, CF3, OCF3, OCHF2 as long as it is not 4-benzyloxy-2-indolyl; Y is independently hydrogen, -N (C0-8 alkyl) (C0-8 alkyl), hydroxyl, halogen, oxo, aryl (optionally substituted by 1 or more R31 groups), heteroaryl (optionally substituted by 1 or more R31 groups), C0-6 alkyl, -C0-8 alkyl-C3-8 cycloalkyl, -C0-8-NR311S alkyl (O) 0-2R321, -C0-8-NR311S (O) 0-2NR321R331, -C0-8 alkyl NR311CO2R321, -alkyl C0-8-CON (R311) S (O) 0- 2R321, -alkyl C0-8-S (O) 0-2NR311R321, -alkyl C0-8-NR311COR321, -alkyl C0-8-NR311CONR321R331, -C0-8-CONR311R321 alkyl, -C0-8-CO2R311 alkyl, -C0-8-S alkyl (0) 0-2R311, -C0-8-O-C1-8 alkyl, -C0-8-O alkyl -C0-8 alkyl-C3-8 cycloalkyl, - C0-8-O-alkyl C0-8 alkylheterocycloalkyl, -C0-8 -alkyl-C0-8 alkyl, -C0-8 -alkylaryl, -C0-8 -alkylheteroyl, - C0-8 alkylheterocyclyl, -C0-8-O-alkyl C0-8 alkyl, -C0-8-S-alkyl C0-8, -C0-8-S-alkyl C0-8- cycloalkyl C3-8, - C0-8-S-C0-8 alkylheterocycloalkyl, C0-8-S-C0-8 alkyl, -C0-8-S-C0-8 alkylheteroyl, - C0-8-N (R311) alkyl-C0-8 alkyl, -C0-8-N-alkyl (R311) -C0-8 alkyl-C3-8 alkyl, -C0-8-N alkyl (R311) - C0- alkylcycloalkyl alkyl 8, -C0-8-N-alkyl (R311) -C0-8 -alkylaryl, -C0-8N-alkyl (R311) -C0-8 -alkylhetaryl, -C0-8 -N-NR311R321 -alkyl, -C2-8 -alkenyl, -C2 -alkyl 8, NO2, CN, CF3, OCF3, OCHF2 as long as it is not 2-carboxy-5- benzo [b] thiophenyl; G11 is halo, oxo, -CF3, -OCF3, -OR312, -NR312R322, -C (O) R312, - (O) C3-8 cycloalkyl, -CO2-C3-8 cycloalkyl, -CO2R312, -C (= O ) NR312R322, -NO2, -CN, -S (O) 0-2R312, -SO2NR312R322, NR312 (C = O) R322, NR312C (= O) OR322, NR312C (= O) NR322R332, NR312S (O) 0-2R322 , - C (= S) OR312, -C (= O) SR312, -NR312C (= NR322) NR332R341, -NR312C (= NR322) OR332, -NR312C (= NR322) SR332, -OC (= O) OR312, - OC (= O) NR312R322, -OC (= O) SR312, -SC (= O) OR312, -SC (= O) NR312R322, -P (O) OR312OR322, C1-10 alkylidene, C0-10 alkyl, C2 alkenyl -10, C2-10 alkynyl, -C1-10 alkoxy-C1-10 alkyl, -C1-10 alkoxy-C2-10 alkenyl, -C1-10 alkoxy-C2-10 alkynyl, -C1-10 alkylthio-C1-alkyl 10, -C1-10 alkylthio-C2-10 alkenyl, -C1-10 alkylthio-C2-10 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, - C3-8 cycloalkyl-C1-10 alkyl, -C3-8 cycloalkenyl C 1-10 alkyl, C 3-8 cycloalkyl C 2-10 alkenyl, C 3-10 cycloalkenyl, C 3-10 alkynyl, C 3-10 cycloalkyl, C 3-8 cycloalkenyl, C 2-10 alkynyl, -heterocyclyl-C0-10 alkyl, - heterocyclyl-alkyl C2-10 enyl or -C2-10 heterocyclyl-alkynyl, any of which is optionally substituted by one or more independent substituents halo, oxo, -CF3, -OCF3, -OR313, -NR313R323, -C (O) R313, - CO2R313, -C (= O) NR313R323, -NO2, - CN, -S (O) 0-2R313, -SO2NR313R323, -NR313C (= O) R323, -NR313C (= O) OR323, -NR313C (= O) NR323R333, -NR313S (O) 0-2R323, -C (= S) OR313, -C (= O) SR313, -NR313C (= NR323) NR333R342, -NR313C (= NR323) OR333, -NR313C (= NR323) SR333 , -OC (= O) OR333, -OC (= O) NR313R323, - OC (= O) SR313, -SC (= O) OR313, -P (O) OR313OR323 or -SC (= O) R313R323; or G11 is C0-10 aryl-alkyl, C2-10 aryl-alkenyl, C2-10 aryl-alkynyl, C0-10 heteroaryl, C2-10 -henyl-alkenyl, or C2-10 -henyl-alkynyl, where the point of attachment is from the left or right as written, where any of which is optionally substituted by one or more independent substituents halo, -CF3, -OCF3, -OR313, -NR313R323, -C (O) R313, -CO2R313, -C (= O) NR313R323, -NO2, -CN, -S (O) 0-2R313, - SO2NR313R323, -NR313C (= O) R323, -NR313C (= O) OR323, -NR313C (= O) NR323R333, -NR313S (O) 0-2R323, -C (S) OR313, -C (O) SR313, -NR323C (= NR313) NR333R342, -NR313C (= NR323) OR333, -NR313C (= NR323) SR333, -OC (= O ) OR313, -OC (= O) NR313R323, -OC (= O) SR313, -P (O) OR313OR323, or - SC (= O) NR313R323 provided that G11 is not N-CH2CO2H when R3 is 4-piperidinyl; R31, R32, R33, R311, R321, R331, R312, R322, R332, R341, R313, R323, R333, and R342, in each case, is independently C0-8 alkyl optionally substituted by an aryl, heterocyclyl or heteroaryl substituent or C0-8 alkyl optionally substituted by 1-6 independent substituents halo, -CON (C0-8 alkyl) (C0-8 alkyl), -CO (C0-8 alkyl), -O-C0-8 alkyl, -O-aryl , -O-heteroaryl, -O-heterocyclyl, -S (O) 0-2 -aryl, -S (O) 0-2hetaryl, -S (O) 0-2heterocyclyl, -S (O) 0-2C0-8 alkyl, -N (C0-8 alkyl) (C0-8 alkyl), -N (C0-8 alkyl) CON (C0-8 alkyl) (C0-8 alkyl), -N (C0-8 alkyl) CO (C1- alkyl 8), -N (C0-8 alkyl) CO (C3-8 cycloalkyl), -N (C0-8 alkyl) CO2 (C1-8 alkyl), S (O) 1-2N (C0-8 alkyl) (alkyl C0-8), -NR11S (O) 1-2 (C0-8 alkyl), -CON (C3-8 cycloalkyl), -CON (C0-8 alkyl) (C3-8 cycloalkyl), -N (C3-8 cycloalkyl) CON (C0-8 alkyl) (C0-8 alkyl), -N (C3-8 cycloalkyl) CON (C3-8 cycloalkyl) (C0-8 alkyl), -N (C0- alkyl 8) CON (C3-8 cycloalkyl) (C0-8 alkyl), -N (C0-8 alkyl) CO2 (cycloalk C3-8 uyl), -N (C3-8 cycloalkyl) CO2 (C3-8 cycloalkyl), S (O) 1-2N (C0-8 alkyl) (C3-8 cycloalkyl), -NR11S (O) 1-2 (C3-8 cycloalkyl), C2-8 alkenyl, C2-8 alkynyl, CN, CF3, OH, or optionally substituted aryl; so that one of the foregoing aryl, heterocyclyl, heteroaryl, alkyl or cycloalkyl groups can be optionally and independently substituted by -N (C0-8 alkyl) (C0-8 alkyl), hydroxyl, halogen, oxo, aryl, heteroaryl, alkyl C0-6, -C0-8 alkylcyclyl, -C0-8-N alkyl (C0-8 alkyl) -S (O) 0-2- (C0-8 alkyl), -C0-8-S alkyl (O) 0 -2-N (C0-8 alkyl) (C0-8 alkyl), -C0-8-N alkyl (C0-8 alkyl) CO (C0-8 alkyl), -C0-8-N alkyl (C0-8 alkyl ) CO-N (C0-8 alkyl) (C0-8 alkyl), -C0-8-CO-N alkyl (C0-8 alkyl) (C0-8 alkyl), -C1-8-CO2 alkyl (C0 alkyl -8), -C0-8-S (O) 0-2- (C0-8 alkyl), -C0-8-O-C1-8 alkyl, -C0-8-O-C0-8 alkylcyclyl , -C0-8-O-alkyl C0-8 alkylheterocyclyl, -C0-8-O-C0-8 alkyl, -C0-8-O-alkyl C0-8, -C0-8-S-C0 alkyl -8, -C0-8-S-C0-8 alkylcyclyl, -C0-8-S-C0-8 alkylheterocyclyl, -C0-8-S-C0-8-alkyl-alkyl, C0-8-S-alkyl C0-8 alkylhetaryl, -C0-8-N alkyl (C0-8 alkyl) -C0-8 alkyl, -C0-8N alkyl (C0 alkyl -8) -C0-8 alkylcyclyl, -C0-8-N alkyl (C0-8 alkyl) -alkyl heterocyclic |
| priorityDate | 2005-11-17-04:00^^<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: 34.