http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-046337-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_aeeae3a1e9c2f6b4db133adad89691b1 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4985 |
| filingDate | 2004-10-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-12-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-046337-A1 |
| titleOfInvention | IMIDAZOPIRAZINE INHIBITORS OF THIROSINQUINASES |
| abstract | They inhibit the IGF-1R enzyme and are useful for the treatment and / or prevention of different diseases and conditions that respond to treatment by tyrosine kinase inhibition. Claim 1: A compound represented by the formula (1), or a salt thereof acceptable for pharmaceutical use, wherein Q1 is aryl1, heteroaryl1, cycloalkyl, heterocyclyl, cycloalkenyl, or heterocycloalkenyl, any of which is optionally substituted with one and five independent G1 substituents; R1 is alkyl, cycloalkyl, bicycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, heterocyclyl, or heterobicycloalkyl, any of which is optionally substituted with one or more independent G11 substituents; G1 and G41 are independently halo, oxo, -CF3, -OCF3, -OR2, -NR2R3 (R3a) j1, -C (O) R2, -CO2R, -CONRaR3, -NO2, -CN, -S (O) j1R2 , -SO2NR2R3, NR2 (C = O) R3, NR2 (C = O) OR3, NR2 (C = O) NR2R3, NR2S (O) j1R3, - (C = S) OR2, - (C = O) SR2, - NR2 (C = NR3) NR2aR3a, -NR2 (C = NR3) OR2a, -NR2 (C = NR3) SR3a, -O (C = O) OR2, -O (C = O) NR2R3, -O (C = O) SR2, -S (C = O) OR2, -S (C = O) NR2R3, C0-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy C1-10 alkyl, C1-10 alkoxyC2 alkenyl -10, C1-10 alkoxyC2-10 alkynyl, C1-10 alkylthioC1-10 alkyl, C1-10 alkylthioC2-10 alkynyl, C1-10 alkylthioC2-10 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, C3-8alkyl C1 -10, C3-8 cycloalkenyl C1-10 alkyl, C3-8 cycloalkyl C1-10, cycloalkenyl C3-8alkenyl C2-10, cycloalkyl C3-8alkynyl C2-10, cycloalkenyl C3-10 alkyl heterocyclyl-C0-10 alkyl, C2-10 heterocyclyl-alkenyl, or C2-10 heterocyclyl-alkynyl, any of which is optionally substituted with one or more independent substituents halo, oxo -CF3, -OCF3, -OR222, -NR222R333 (R333a) j1a, -C (O) R222, -CO2R222, -CONR222R333, -NO2, -CN, -S (O) j1aR222, -SO2NR222R333, NR222 (C = O ) R333, NR222 (C = O) OR333, NR222 (C = O) NR222R333, NR222S (O) j1aR333, - (C = S) OR222, - (C = O) R222, -NR222 (C = NR333) NR222aR333a, -NR222 (C = NR333) OR222a, -NR222 (C = NR333) SR333a, -O (C = O) OR222, -O (C = O) NR222R333, -O (C = O) SR222, -S (C = O) OR222, or -S (C = O) NR222R333; or - (X1) n- (Y1) m-R4; or C0-10 aryl-alkyl, C2-10 aryl-alkenyl, or C2-10 aryl-alkynyl, any of which is optionally substituted with one or more independent substituents, -CF3, -OCF3, -OR222, -NR222R333 (R333a ) j2a, -C (O) R222, -CO2R222, -CONR222R333, -NO2, -CN, -S (O) j2aR222, -SO2NR222R333, NR222 (C = O) R333, NR222 (C = O) OR333, NR222 ( C = O) NR222R333, NR222S (O) j2aR333, - (C = S) OR222, - (C = O) SR222, -NR222 (C = NR333) NR222aR333a, -NR222 (C = NR333) OR222a, -NR222 (C = NR333) SR333a, -O (C = O) OR222, -O (C = O) NR222R333, -O (C = O) SR222, -S (C = O) OR222, or -S (C = O) NR222R333 ; or C 0-10 alkyl, C 2-10 heteroaryl, or C 2-10 alkynyl, any of which is optionally substituted with one or more independent halo substituents, -CF3, -OCF3, -OR222, -NR222R333 ( R333a) j3a, -C (O) R222, -CO2R222, - CONR222R333, -NO2, -CN, -S (O) j3aR222, -SO2NR222R333, NR222 (C = O) R333, NR222 (C = O) OR333, NR222 (C = O) NR222R333, NR222S (O) j3aR333, - (C = S) OR222, - (C = O) SR222, -NR222 (C = NR333) NR222aR333a, -NR222 (C = NR333) OR222a, -NR222 ( C = NR333) SR333a, -O (C = O) OR222, - O (C = O) NR222R333, -O (C = O) SR222, -S (C = O) OR222, or -S (C = O) NR222R333; G11 is halo, oxo, -CF3, -OCF3, -OR21, -NR21R31 (R3a1) j4, -C (O) R21, -CO2R21, -CONR21R31, -NO2, -CN, -S (O) j4R21, -SO2NR21R31 , NR21 (C = O) R31, NR21 (C = O) OR31, NR21 (C = O) NR21R31, NR21S (O) j4R31, - (C = S) OR21, - (C = O) SR21, -NR21 ( C = NR31) NR2a1R3a1, -NR21 (C = NR31) OR2a1, -NR21 (C = NR31) SR3a1, -O (C = O) OR21, -O (C = O) NR21R31, -O (C = O) SR21 , -S (C = O) OR21, -S (C = O) NR21R31, -P (O) OR21OR31, C0-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy C1-10 alkyl, alkoxy C1-10 C2-10 alkenyl, C1-10 alkoxy C2-10 alkynyl, C1-10 alkylthio C1-10 alkyl, C1-10 alkylthio C2-10 alkenyl, C1-10 alkylthio C2-10 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, cycloalkyl C3-8 C1-10 alkyl, C3-8 cycloalkenyl C1-10 alkyl, C3-8 cycloalkyl C2-10 alkynyl, C3-8 cycloalkenyl C2-10 cycloalkyl C3-8alkynyl C2-10, cycloalkenyl C3-8alkynyl C2-10, heterocyclyl-alkyl C0-10, C2-10 heterocyclyl-alkenyl, or C2-10 heterocyclyl-alkynyl, any of which is optionally substituted with one or more substitutes independent tes halo, oxo, -CF3, -OCF3, -OR2221, -NR2221R3331 (R333a1) j4a, -C (O) R2221, -CO2R2221, -CONR2221R3331, -NO2, -CN, -S (O) j4aR2221, -SO2NR2221R3331 , NR2221 (C = O) R3331, NR2221 (C = O) OR3331, NR2221 (C = O) NR2221R3331, NR2221S (O) j4aR3331, - (C = S) OR2221, - (C = O) SR2221, -NR2221 ( C = NR3331) NR222a1R333a1, -NR2221 (C = NR3331) OR222a1, -NR2221 (C = NR3331) SR333a1, -O (C = O) OR2221, -O (C = O) NR2221R3331, -O (C = O) SR2221 , -S (C = O) OR2221, - P (O) OR2221OR3331, or -S (C = O) NR2221R3331; or C0-10 aryl-alkyl, C2-10 aryl-alkenyl, or C2-10 aryl-alkynyl, any of which is optionally substituted with one or more independent halo substituents, -CF3, -OCF3, -OR2221, - NR2221R3331 ( R333a1) j5a, -C (O) R2221, -CO2R2221, -CONR2221R3331, -NO2, -CN, -S (O) j5aR2221, -SO2NR2221R3331, NR2221 (C = O) R3331, NR2221 (C = O) OR3331, NR2221 (C = O) NR2221R3331, NR2221S (O) j5aR3331, - (C = S) OR2221, - (C = O) SR2221, -NR2221 (C = NR3331) NR222a1R333a1, - NR2221 (C = NR3331) OR222a1, -NR2221 ( C = NR3331) SR333a1, -O (C = O) OR2221, -O (C = O) NR2221R3331, -O (C = O) SR2221, -S (C = O) OR2221, -P (O) OR2221OR3331, or -S (C = O) NR2221R3331; or C0-10 -alkyl-alkyl, C2-10 -heteroyl-alkenyl, or C2-10 -alkylaryl-alkynyl, any of which is optionally substituted with one or more independent halo, -CF3, -OCF3, -OR2221, -NR2221R3331 (R333a1 ) j6a, -C (O) R2221, -CO2R2221, -CONR2221R3331, -NO2, -CN, -S (O) j6aR2221, -SO2NR2221R3331, NR2221 (C = O) R3331, NR2221 (C = O) OR3331, NR2221 ( C = O) NR2221R3331, NR2221S (O) j6aR3331, - (C = S) OR2221, - (C = O) SR2221, -NR2221 (C = NR3331) NR222a1R333a1, -NR2221 (C = NR3331) OR222a1, -NR2221 (C = NR3331) SR333a1, -O (C = O) OR2221, -O (C = O) NR2221R3331, -O (C = O) SR2221, -S (C = O) OR2221, -P (O) OR2221OR3331, or - S (C = O) NR2221R3331; or G11 is taken together with the carbon to which it is attached to form a double bond that is substituted with R5 and G111; R2, R2a, R3, R3a, R222, R222a, R333, R333a, R21, R2a1, R31, R3a1, R2221, R222a1, R3331, and R333a1 are each independently equal to C0-10 alkyl, C2-10 alkenyl, C2 alkynyl -10, C1-10 alkoxy C1-10 alkyl, C1-10 alkoxyC2-10 alkenyl, C1-10 alkoxyC2-10 alkynyl, C1-10 alkylthio C1-10 alkyl, C1-10 alkylthio C2-10 alkenyl, C1-10 alkylthioC2-10 , C3-8 cycloalkyl, C3-8 cycloalkenyl, C3-8 cycloalkyl C1-10 alkyl, C3-8 cycloalkenyl C1-10 alkyl, C3-8 cycloalkyl C2-10 alkenyl, C3-8 cycloalkenyl C2-10 cycloalkenyl , C3-8 cycloalkenyl C2-10 alkynyl, heterocyclylC0-10 alkyl, heterocyclylC2-10 alkenyl, or heterocyclylC2-10 alkynyl, any of which is optionally substituted with one or more G111 substituents; or C0-10 aryl-alkyl, C2-10 aryl-alkenyl, or C2-10 aryl-alkynyl, C0-10 -heteroyl-alkyl, C2-10 -heteroyl-alkenyl, or C2-10 -henyl-alkynyl, each of which it is optionally substituted with one or more G111 substituents; or in the case of -NR2R3 (R3a) j1 or -NR222R333 (R333a) j1a or -NR222R333 (R333a) j2a or - NR2221R3331 (R333a1) j3a or -NR2221R3331 (R333a1) j4a or -NR2221a1 -NR222133 (31) R333a1) j6a, R2 and R3 or R222 and R333 or R2221 and R3331 taken together with the nitrogen to which they are attached form a ring of 3-10 saturated cyclic, unsaturated cyclic, heterocyclic saturated cyclic, or heterocyclic unsaturated cyclic, wherein said ring is optionally substituted with one or more G111 substituents; X1 and Y1 are each independently -O-, -NR7-, -S (O) J7-, -CR5R6-, -N (C (O) OR7) -, -N (C (O) R7) -, -N (SO2R7) -, -CH2O-, -CH2S-, -CH2N (R7) -, -CH (NR7) -, -CH2N (C (O) R7) -, -CH2N (C (O) OR7) - , -CH2N (SO2R7) -, -CH (NHR7) -, -CH (NHC (O) R7) -, -CH (NHSO2R7) -, -CH (NHC (O) OR7) -, -CH (OC (O ) R7) -, -CH (OC (O) NHR7) -, -CH = CH-, -CsC-, -C (= NOR7) -, - C (O) -, -CH (OR7) -, -C (O) N (R7) -, -N (R7) C (O) -, -N (R7) S (O) -, -N (R7) S (O) 2-, -OC (O) N ( R7) -, -N (R7) C (O) N (R7) -, -NR7C (O) O-, -S (O) N (R7) -, -S (O) 2N (R7) -, - N (C (O) R7) S (O) -, -N (C (O) R7) S (O) 2-, -N (R7) S (O) N (R7) -, -N (R7) S (O) 2N (R7) -, -C (O) N (R7) C (O) -, -S (O) N (R7) C (O) -, - S (O) 2N (R7) C (O) -, -OS (O) N (R7) -, -OS (O) 2N (R7) -, -N (R7) S (O) O-, -N (R7) S (O) 2O- , -N (R7) S (O) C (O), -N (R7) S (O) 2C (O) -, -SON (C (O) R7) -, -SO2N (C (O) R7) -, -N (R7) SON (R7) -, -N (R7) SO2N (R7) -, -C (O) O-, -N (R7) P (OR8) O-, -N (R7) P (OR8) -, -N (R7) P (O) (OR8) O-, -N (R7) P (O) (OR8) -, -N (C (O) R7) P (OR8) O-, -N (C (O) R7) P (OR8) -, -N (C (O) R7) P (O) (OR8) O-, -N (C (O) R7) P (OR8) -, - CH (R7) S (O) -, - CH (R7) S (O) 2-, -CH (R7) N (C (O) OR7) -, -CH (R7) N (C (O) R7) -, -CH (R7) N (SO2R7), -CH (R7) O-, -CH (R7) S-, -CH (R7) N (R7) -, -CH (R7) N (C (O) R7) -, -CH (R7) N (C (O) OR7) -, - CH ( R7) N (SO2R7) -, -CH (R7) C (= NOR7) -, -CH (R7) C (O) -, -CH (R7) CH (OR7) -, -CH (R7) C (O ) N (R7) -, -CH (R7) N (R7) C (O) -, -CH (R7) N (R7) S (O) -, -CH (R7) N (R7) S (O) 2-, -CH (R7) OC (O) N (R7) -, -CH (R7) N (R7) C (O) N (R7) -, -CH (R7) NR7C (O) O-, - CH (R7) S (O) N (R7) -, -CH (R7) S (O) 2N (R7) -, - CH (R7) N (C (O) R7) S (O) -, -CH (R7) N (C (O) R7) S (O) -, -CH (R7) N (R7) S (O) N (R7) -, -CH (R7) N (R7) S (O) 2N (R7) -, -CH (R7) C (O) N (R7) C (O) -, -CH (R7) S (O) N (R7) C (O) -, -CH (R7) S ( O) 2N (R7) C (O) -, -CH (R7) OS (O) N (R7) -, -CH (R7) OS (O) 2N (R7) -, -CH (R7) N (R7 ) S (O) O-, -CH (R7) N (R7) S (O) 2O-, - CH (R7) N (R7) S (O) C (O) -, -CH (R7) N ( R7) S (O) 2C (O) -, -CH (R7) SON (C (O) R7) -, -CH (R7) SO2N (C (O) R7) -, -CH (R7) N (R7 ) SON (R7) -, -CH (R7) N (R7) SO2N (R7) -, -CH (R7) C (O) O-, -CH (R7) N (R7) P (OR8) O-, -CH (R7) N (R7) P (OR8) -, -CH (R7) N (R7) P (O) (OR8) O-, -CH (R7) N (R7) P (O) (OR8) -, - CH (R7) N (C (O) R7) P (OR8) O-, -CH (R7) N (C (O) R7) P (OR8) -, -CH (R7) N (C ( O) R7) P (O) (OR8) O-, or -CH (R7) N (C (O) R7) P (OR8) -; or X1 and Y1 are each represented by one of the structural formulas (2), (3), (4), (5), (6) or (7); R10, taken together with phosphinamide or phosphonamide, is a 5-, 6-, or 7-membered aryl, heteroaryl or heterocyclyl ring system; R5, R6 and G111 are each independently C0-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxyC1-10 alkyl, C1-10 alkoxyC2-10 alkenyl, C1-10 alkoxyC2-10 alkynyl, alkylthio C1-10 C1-10 alkyl, C1-10 alkylthio C2-10 alkynyl, C1-10 alkylthio C2-10 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, cycloalkyl |
| priorityDate | 2003-10-15-04:00^^<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: 53.