http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-053090-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/A61K31-53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 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/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-06 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/A61P9-00 |
| filingDate | 2005-07-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2007-04-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-053090-A1 |
| titleOfInvention | IMIDAZOTRIAZINS AS PROTEIN KINASE INHIBITORS AND THEIR USE FOR THE PREPARATION OF MEDICINES |
| abstract | Compound of formula 1 and salts acceptable for pharmaceutical use thereof. These compounds inhibit the IGF-1R enzyme and are useful for the treatment and / or prevention of various diseases and conditions, which respond to the treatment by tyrosine kinase inhibition, such as cancer. Claim 1: A compound represented by formula 1 or a salt acceptable for pharmaceutical use thereof, wherein Q1 is aryl 1, heteroaryl1, C3-10 cyclolalkyl, heterocyclyl, C3-10 cycloalkenyl or heterocycloalkenyl, any of which is optionally substituted by one to five independent substituents G10, R1 is C0- alkyl 10, C3-10 cycloalkyl, C5-10 bicyclo-alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, heterocycle or heterobicyclo-C5-10 alkyl, any of which is optionally substituted with one or more independent G11 substituents; G10 and G11 are each independently halo, oxo, -CF3, -OCF3, -OR2, -NR2R3 (R2a) j1, -C (O) R2, -CO2R2, -CONR2R3, -NO2, -S (O) j1R2, -SO2NR2R3, -NR2C (= O) R3, -NR2C (= O) NR3R2a, -NR2S (O) j1R3, -C (= S) OR2, -C (= O) SR2, -NR2C (= NR3) NR2aR3a, -NR2C (= NR3) OR2a,, NR2C (= NR3) SR2a, -OC (= O) OR2, -OC (= O) NR2R3, -OC (= O) OR2, -CO (= O) NR2R3, C0 alkyl -10, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy-C1-10 alkyl, C1-10 alkoxy-C2-10 alkenyl, C1-10 alkoxy-C2-10 alkynyl, C1-10 alkyl-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-C1-alkyl -10, C3-8 cycloalkyl-C2-10 alkenyl. C3-8 cycloalkenyl C2-10 alkenyl, C3-8 cycloalkyl C2-10 alkynyl, C3-10 cycloalkenyl C2-10 alkynyl, C0-10 heterocyclyl 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 (R222a) j1a, -C (O) R222, -CO2R222, - CONR222R333, -NO2, - CN, S- (O) j1aR222, -SO2NR222R333, -NR222C (= O) R333, -NR222C (= O) OR333, -R222C (= O) NR333R222a, -NR222S (O) j1aR333, -C (= S) OR222 , -C (= O) SR222, -NR222C (= NR333) NR222R333a, -NR222C (= NR333) OR222a, -NR222C (= NR333) SR222a, -OC (= O) OR222, - OC (=) NR222R333, -OC (= O) OR222, -OC (= O) NR222R333, -OC (= O) SR222, -SC (= O) OR222 or -SC (= O) NR222R333; or G10 is optionally - (X1) n- (Y1) m-R4; Or G41 is optionally - (X1) n- (Y1) m-C0-10 alkyl; or G10 and G41 are each optionally independently C0-10 arylalkyl, C2-10 arylalkyl, C2-10 arylalkyl, C0-10 hexylalkyl, C2-10 heteroylalkyl or C2-10 heteroylalkyl, any of which is optionally substituted with one or more independent halo substituents, -CF3, -OCF3, - OR222, -NR222R333 (R222a) j1a, -C (O) R222, -CO2R222, -CONR222R333, -NO2, -CN, S- (O) j1aR222, -SO2NR222R333 , -NR222C (= O) R333, -NR222C (= O) OR333, -R222C (= O) NR333R222a, -NR222S (O) j1aR333, -C (= S) OR222, -C (= O) SR222, -NR222C (= NR333) NR222R333a, - NR222C (= NR333) OR222a, -NR222C (= NR333) SR222a, -OC (= O) OR222, -OC (=) NR222R333, -OC (= O) OR222, -OC (= O ) NR222R333, -OC (= O) SR222, -SC (= O) OR222 or -SC (= O) NR222R333; G11 is halo, oxo, -CF3, -OCF3, -OR21, -NR21R31 (R21a) j3, -C (O) R21, -CO2R21, .CONR21R31, -NO2, - CN, -S (O) j3R21, -SO2NR21R31 , -NR21C (= O) R31, -NR21C (= O) OR31, -NR21C (= O) NR31R21a, -NR21S (O) j3R31, -C (= S) OR21, -C (= S) OR21, -C (= O) SR21, -NR21C (= NR31) NR21aR31a, -NR21C (= NR31) OR21a, -NR21C (= NR31) SR21a, OC (= O) OR21, -OC (= O) NR21R31, -OC (= O ) SR21, - SC (= O) OR21, -SC (= O) NR21R31, -P (O) OR21OR31, C0-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy-C1-10 alkyl , C1-10 alkoxy-C2-10 alkenyl, C1-10 alkoxy, C1-10 alkylthio-C1-10 alkyl, C1-10 alkylthio-C2-10 alkynyl, C1-10 alkylthio-C2-10 alkynyl, C3-8 cycloalkyl , C 3-8 cycloalkenyl, C 3-8 cycloalkyl-C 1-10 alkyl, C 3-8 cycloalkenyl, C 3-8 cycloalkyl-C 3-8 alkenyl-C 2-10 alkenyl, C 3-8 cycloalkenyl , C3-8 cycloalkyl C2-10 alkynyl, C3-8 cycloalkenyl C2-10 alkynyl, heterocyclylC0-10 alkyl, heterocyclylC2-10 alkynyl or C2-10 heterocyclyl-alkynyl, any of which is optionally substituted with n one or more independent substituents halo, oxo, -CF3, -OCF3, - OR2221, -NR2221R3331 (R2221a) j3a, -C (O) R2221, -CO2R2221, -CONR2221R3331, NO2, -CN, -S (O) j3aR2221 , SO2NR2221R3331, -NR2221C (= O) R3331, -NR2221C (= O) OR3331, -NR2221C (= O) NR3331R2221a, -NR2221S (O) j3aR3331, -C (= S) OR2221, -C (= O) SR2221, - NR2221C (= NR3331) NR2221aR3331a, -NR2221C (= NR3331) OR2221a, -NR2221C (= NR3331) SR2221a, -OC (= O) OR2221, -OC (= O) NR2221R3331, -OC (= O) SR2221, -SC (= O) OR2221, -P (O) OR2221OR3331 or -SC (= O) NR2221R3331; or G11 is C0-10 arylalkyl, C2-10 arylalkyl, or G11 is C0-10 arylalkyl, C2-10 arylalkyl, C2-10 arylalkyl, C0-10 heteroaryl, C2-10 heteroaryl or C2-10 heteroaryl, any of which is optionally substituted with one or more C2-10 hetarylalkyl, any of which is optionally substituted with one or more independent substituents halo, -CF3, -OCF3, -OR2221, -NR2221R3331 (R2221a) j3a, -C (O) R2221, -CO2R2221, -CONR2221R3331, -NO2, -CN, -S (O) j3aR2221, -SO2NR2221R3331, -NR2221C (= O) R3331, -NR2221C (= O) OR3331, - NR2221C (= O) NR3331R2221a, -NR ) j3aR3331, -C (= S) OR2221, -C (= O) SR2221, -NR2221C (= NR3331) NR2221aR3331a, -NR2221C (= NR3331) OR2221a, -NR2221C (= NR3331) SR2221a, -OC (= O) OR2221 , -OC (= O) NR2221R3331, -OC (= O) SR2221, -SC (= O) OR2221, -P (O) OR2221OR3331 or - SC (= O) NR2221R3331; or G11 is C, taken together with the carbon to which it is attached forms a double bond C = C that is substituted with R5 and G12, R2, R2a, R3, R3a, R222, Rrrr1, R333, R333a, R21, R21a, R31, R31a, R2221, R2221a, R3331 and R3331a are each independently C0-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy-C1-10 alkyl, C1-10 alkyl-C2-10 alkenyl, C1-10 alkoxy-C2-10 alkynyl, C1-10 alkylthio-C1-10 alkyl, C1-10 alkylthio-C2-10 alkynyl, C1-10 alkylthio-C2-10 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, C3-8 cycloalkyl C1-10 alkyl, C3-8 cycloalkenyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-8 cycloalkenyl-C2-10 alkenyl, C3-8 cycloalkyl, C3-8 cycloalkenyl-C2-10 alkynyl, heterocyclyl-C0-10 alkyl, heterocyclyl-C2-10 alkenyl, heterocyclyl-C2-10 alkynyl, C0-10 arylalkyl, C2-10 arylalkyl, C2-10 arylalkyl, C2-10 heteroaryl alkenyl or C2-10 heteroyalkynyl, any of which is optionally substituted with one or more s independent users G13 or in the case of -NR2R3 (R2a) j1 or -NR21R31 (R21a) j3 or -NR222R333 (R222a) j1a or -NR222R333 (R222a) j2a or -NR2221R3331 (R2221a) j3a, R2 and R3 or R31 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R3 or R222 and R333 or R2221 and R3331, respectively, are optionally taken together with the nitrogen atom to which they are attached to form a saturated or unsaturated 3-10 membered ring, where said ring is optionally substituted with one or more substituents independent G14 and wherein said ring optionally includes one or more independent heteroatoms other than nitrogen to which R2 and R3 or R222 and R333 or R2221 and R3331 are attached; X1 and Y1 are each independently -O-, -NR7-, - S (O) j4-, -CR5R6-, -N (C (O) OR7), -N (C (O) R7) -, -N (SO2R7) -, -CH2O-, -CH2S-, -CH2H (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-, -C ::: C-, -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 (R8) -, -NR7C (O) -O-, -S (O) N (R7) -, -S (O) 2N (R7) -, - N (C (O) R7S (O) -, -N (C (O) R7) S (O) 2-, -N (R7) S (O) N (R8) -, -N (R7) S ( O) 2N (R8) -, -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) 2-O -, -N (R7) S (O) C (O) -, -N (R7) S (O) 2C (O) -, -SON (C (O) R7) -, -SO2N (C (O) R7) -, -N (R7) SON (R8) -, - (R7) SO2N (R8) -, -N (R7) SO2N (R8) -, -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) OR8) -, -CH (R7) N (C (O) R8) -, -CH (R7) N (SO 2R8) -, -CH (R7) -O-. --CH (R7) S-, CH (R7) N (R8) -, - CH (R7) N (C (O) R8) -, -CH (R7) N (C (O) OR8) -, - CH (R7) N (SO2R8) -, -CH (R7) C (= NOR8) -, -CH (R7) C (O) -, -CH (R7) CH (OR8) -, -CH (R7) C (O) N (R8) -, -CH (R7) N (R8) C (O) -, -CH (R7) N (R8) S (O) -, -CH (R7) N (R8) S ( O) 2-, -CH (R7) OC (O) N (R8) -, -CH (R7) N (R8) C (O) N (R7a) -, -CH (R7) NR8C (O) -O -, - CH (R7) S (O) N (R8) -, -CH (R7) S (O) 2N (R8) -, -CH (R7) N (C (O) R8) S (O) - , -CH (R7) N (C (O) R8) S (O) -, -CH (R7) N (R8) S (O) N (R7a) -, -CH (R7) N (R8) S ( O) 2N (R7a) -, -CH (R7) C (O) N (R8) C (O) -, -CH (R7) S (O) N (R8) C (O) -, -CH (R7 ) S (O) 2N (R8) C (O) -, -CH (R7) OS (O) N (R8) -, -CH (R7) OS (O) 2N (R8) -, - CH (R7) N (R8) S (O) -O-, -CH (R7) N (R8) S (O) 2-O-, -CH) R7) N (R8) S (O) C (O) -, - CH (R7) N (R8) S (O) 2C (O) -, -CH (R7) SON (C (O) R8) -, -CH (R7) SO2N (C (O) R8) -, -CH (R7) N (R8) SON (R7a) -, -CH (R7) N (R8) SO2N (R7Aa) -, -CH (R7) C (O) -O-, -CH (R7) N (R8) P (OR7a) -O-, -CH (R7) N (R8) P (OR7a) -, - CH (R7) N (R8) P (O) (OR7a) -O-, -CH (R7) N ( R8) P (O) (OR7a) -, -CH (R7) N (C (O) R8) P (OR7a) -O-, -CH (R7) N (O) R8) P (OR7a) -, - CH (R7) N (C (O) R8) P (O) OR7a) -O- or -CH (R7) N (C (O) R8) P (OR7a) -; or X1 and Y1 are each independently represented by one of the following structural formulas: 1, 2, 3, 4, 5 or 6, R10 taken together with phosphinamide or phosphonamide, form an aryl, heteroaryl or heterocyclyl ring system of 5, 6 or 7 members; R5, R6, G12, G13, G14 and G15 are each independently C0-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy-C1-10 alkyl, C1-10 alkoxy-C2-10 alkenyl, C1-10 alkoxy-C2-10 alkynyl, C1-10 alkylthio-C1-10 alkyl, C1-10 alkylthio-C2-10 alkynyl, C1-10 alkylthio-C2-10 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, C3-8 cycloalkyl C1-10 alkyl, C3-8 cycloalkenyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-8 cycloalkenyl-C2-10 alkenyl, C3-8 cycloalkyl-C2-10 alkynyl, C3-8 cycloalkenyl-C2-10 alkynyl, C0-10 heterocyclyl-alkyl, C2-10 heterocyclyl-alkenyl, C2-10 heterocyclyl-alkynyl, C0-10 aralkyl, C2-10 arylalkyl, C0-10 arylalkyl, , C2-10 hexylalkyl or C2-10 hexylalkyl or C2-10 hexylalkyl, any of |
| priorityDate | 2004-07-20-04:00^^<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: 37.