http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-059098-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/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 |
| filingDate | 2007-01-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2008-03-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-059098-A1 |
| titleOfInvention | FUSIONED HETEROBICICLIC QUINASE INHIBITORS |
| abstract | They are useful for the treatment and / or prevention of hyperproliferative diseases such as cancer. The compounds are also useful in the treatment of: inflammation, allergy, asthma, diseases and disorders of the immune system, diseases and disorders of the nervous system, cardiovascular diseases, diseases and disorders of the eye, dermatological diseases, osteoporosis, diabetes, multiple sclerosis, and infections Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein: X1 or X2 are each independently N or -C (E1) -; X3, X4 and X5 are each independently N, O, S, C (E1a) -, o = C (E1) -; as long as X3 is O or S when X4 and X5 combine to match- C (E1a) = C (E1) -; X5 is NH, O, or S when X3 and X4 combine to equal -C (E1a) = C (E1) -; X5 is NH when X3 and X4 combine to equal -N = C (E1) -; X5 is NH when X3 and X4 combine to equal -C (E1) = N-; Q1 is 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- alkylthio 10- C1-10 alkyl, C1-10 alkylthio-C2-10 alkenyl, C1-10 alkylthio-C2-10 alkynyl, cyanoC3-8 alkyl, C3-8 cycloalkenyl, C3-8 alkylC1-10 alkyl, C3- cycloalkenyl 8-C 1-10 alkyl, C 3-8 cycloalkyl-C 2-10 alkenyl, C 3-8 cycloalkenyl, C 2-10 cycloalkenyl, C 3-10 cycloalkyl, C 3-8 cycloalkenyl, C 0-10 alkynyl, C 0- heterocyclyl alkyl 10, C2-10 heterocyclylalkenyl, C2-10 heterocyclylalkyl, C0-10 arylalkyl, C2-10 arylalkyl, C2-10 arylalkyl, C0-10 heteroylalkyl, C2-10 heteroaryl alkenyl, C5-10 heterocycloalkyl, or 5-5 spirocycloalkyl heteroespiroalkyl; or - (Z1) n- (Y1) m-R1; any of which is optionally substituted with one or more independent substituents G1; E1, E1a, and G1 are, in each case, each independently equal to halo, -CF3, -OCF3, -OR2, - NR2R3 (R4) j1, -C (= O) R2, -CO2R2, -CONR2R3, - NO2, -CN, -S (O) j1R2, -SO2NR2R3, -NR2C (= O) R3, -NR2C (= O) OR3, -NR2C (= O) NR3R4, -NR2S (O) j1R3, -C (= S) 0R2, -C (= O) SR2, -NR2C (= NR3) NR4R5, -NR2C (= NR3) OR4, -NR2C (= NR3) SR4, -OC (= O) OR2, -OC (= O) NR2R3, -OC (= O) SR2, - SC (= O) OR2, -SC (= O) NR2R3, 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 alkenyl, C1-10 alkylthio-C2-10 alkynyl , C3-8 cycloalkyl, C3-8 cycloalkenyl, C3-8 alkylC1-10 alkyl, C3-8 cycloalkenylC1-10 alkyl, C3-8 cycloalkyl-C2-10 alkenyl, C3-8 cycloalkenyl C2-10 alkenyl , C3-8-C2-10 cycloalkyl, C3-8 cycloalkenyl-C2-10 alkynyl, C0-10 heterocyclylalkyl, C2-10 heterocyclylalkyl, C2-10 heterocyclylalkyl, C2-10 arylalkyl, C2-10 arylalkyl hetari C0-10 alkyl, C2-10 hexylalkyl, or C2-10 hexylalkyl, any of which is optionally substituted with one or more independent substituents halo, oxo, -CF3, -OCF3, -OR22, -NR22R33 (R22a) j1, - C (= O) R22, -CO2R22, -C (= O) NR22R33, -NO2, -CN, -S (= O) j1aR22, -SO2NR22R33, -NR22C (= O) R33, -NR22C (= O) OR33 , - NR22C (= O) NR33R22a, -NR22S (O) j1aR22, -C (= S) OR22, -C (= O) SR22, -NR22C (= NR33) NR22aR33a, -NR22C (= NR33) OR22a, -NR22C (= NR33) SR22a, -OC (= O) OR22, -OC (= O) NR22R33, -OC (= O) SR22, -SC (= O) OR22, or -SC (= O) NR22R33, Z1 is cycloalkyl C3-8, C0-10 heterocyclyl alkyl, C0-10 arylalkyl, C0-10 heteroaryl alkyl, C5-10 heterobicycloalkyl, spiroalkyl, or heteroespiroalkyl, any of which is optionally substituted with one or more G1 substituents; Y1 is -O -, - NR6 -, - S (O) j2-, -CR6aR7a-, -N (C (O) OR6) -, - N (C (O) R6) - -N (SO2R6) -, - (CR6aR7a) O-, - (CR6aR7a) S-, - (CR6aR7a) N (R6) -, -CR6a (NR6) -, - (CR6aR7a) N (C (O) R6) -, - (CR6aR7a) N (C (O) OR6) -, - (CR6aR7a) N (SO2R6) -, - (CR6a) (NHR6) - (CR6a) (NHC (O) R6) -, - (CR6a) (NHSO2R6) -, - ( CR6a) (NHC (O) OR6) -, - (CR6a) (OC (O) R6) -, - (CR6a) (OC (O) NHR6) -, - (CR6a) = (CR6a) -, -C: :: C-, -C (= NOR6) -, -C (O) -, - (CR6a) (OR6) -, -C (O) N (R6) -, -N (R6) C (O) - , -N (R6) S (O) -, -N (R6) S (O) 2-, -OC (O) N (R6) -, -N (R6) C (O) N (R6a) -, -NR6C (O) O-, -S (O) N (R6) -, -S (O) 2N (R6) -, -N (C (O) R6) S (O) -, -N (C ( O) R6) S (O) 2-, N (R6) S (O) N (R7) -, -N (R6) S (O) 2N (R7) -, -C (O) N (R6) C (O) -, -S (O) N (R7) C (O) -, -S (O) 2N (R6) C (O) -, -OS (O) N (R6) -, -OS (O ) 2N (R6) -, -N (R6) S (O) O-, -N (R6) S (O) 2O-, -N (R6) S (O) C (O) -, -N (R6 ) S (O) 2C (O) -, -SON (C (O) R6) -, -SO2N (C (O) R6-, -N (R6) SON (R7) -, -N (R6) SO2N ( R7) -, - C (O) O-, -N (R6) P (OR7) O-, -N (R6) P (OR7) -, -N (R6) P (O) (OR7) O-, -N (R6) P (O) (OR7) -, -N (C (O) R6) P (OR7) O-, -N (C (O) R6) P (OR7) -, -N (C ( O) R6) P (O) (OR7) O-, -N (C (O) R6) P (OR7) -, - (CR6aR7a) S (O) -, - (CR6aR7a) S (O) 2-, - (CR6aR7a) N (C (O) OR7) -, - (CR6 aR7a) N (C (O) R7) -, - (CR6aR7a) N (SO2R7) -, - (CR6aR7a) C (= NOR7) -, - (CR6aR7a) C (O) -, - (CR6aR7a) (CR6aa) (OR7) -, - (CR6aR7a) C (O) N (R7) -, - (CR6aR7a) N (R6) C (O) -, - (CR6aR7a) N (R7) S (O) -, - (CR6aR7a ) N (R7) S (O) 2-, - (CR6aR7a) OC (O) N (R7) -, - (CR6aR7a) N (R7) C (O) N (R8) -, - (CR6aR7a) NR7C ( O) O-, - (CR6aR7a) S (O) N (R7) -, - (CR6aR7a) S (O) 2N (R7) -, - (CR6aR7a) N (C (O) R7) S (O) - , - (CR6aR7a) N (C (O) R7) S (O) -, - (CR6aR7a) N (R7) S (O) N (R8) -, - (CR6aR7a) N (R7) S (O) 2N (R8) -, - (CR6aR7a) C (O) N (R7) C (O) -, - (CR6aR7a) S (O) N (R7) C (O) -, - (CR6aR7a) S (O) 2N (R7) C (O) -, - (CR6aR7a) OS (O) N (R7) -, - (CR6aR7a) OS (O) 2N (R7) -, - (CR6aR7a) N (R7) S (O) O -, - (CR6aR7a) N (R7) S (O) 2s-, - (CR6aR7a) N (R7) S (O) C (O) -, - (CR6aR7a) N (R7) S (O) 2C (O ) -, - (CR6aR7a) SON (C (O) R7) -, - (CR6aR7a) SO2N (C (O) R7) -, - (CR6aR7a) N (R7) SON (R8) -, - (CR6aR7a) N (R7) SO2N (R8) -, - (CR6aR7a) C (O) O-, - (CR6aR7a) N (R7) P (OR8) O-, - (CR6aR7a) N (R7) P (OR8) -, - (CR6aR7a) N (R7) P (O) (OR8) O-, - (CR6aR7a) N (R7) P (O) (OR8) -, - (CR6aR7a) N (C (O) R7) P (OR8) O-, - (CR6aR7a) N (C (O) R7P (OR8) -, - (CR6aR7a) N (C (O) R7P (O) (OR8) O-, or - (CR6aR7a) N (C (O) R7P (OR8) -; R1, R2, R3, R4, R5, R6, R7, R8, R22, R22a, R33, and R33a are, in each case, independently C0-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1 alkoxy -10-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 alkenyl, C1-alkylthio -10-C2-10 alkynyl, C3-8 cyclo or C3-8 alkyl, C3-8 cycloalkenyl, C3-8 alkylC1-10 alkyl, C3-8 cycloalkenyl-C1-10 alkyl, C3-8 cycloalkyl C2-10 alkynyl, C3 cycloalkenyl -8-C2-10 alkenium, C3-8-cycloalkyl C2-10, C3-8 cycloalkenyl-C2-10 alkynyl, C0-10 heterocyclylalkyl, C2-10 heterocyclyl alkenyl, C0-10 heterocyclylalkyl, C2-10 arylalkyl -10, or C2-10 arylalkyl, C0-10 hexylalkyl, C2-10 hexylalkyl, or C2-10 hexylalkyl, any of which is optionally substituted with one or more independent G11 substituents; R6a, R6aa, and R7a are, in each case, each independently fluorine, trifluoromethyl, C0-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy-C1-10 alkyl, C1-10 alkenyl C2-10, C1-10 alkoxy-C2-10 alkynyl, C1-10 alkylthio-C1-10 alkyl, C1-10 alkylthio-C2-10 alkylthio, C1-10 alkylthio-C2-10 alkynyl, cyclo or C3-8 alkyl, cycloalkenyl C3-8, C 3-8 cycloalkyl-C 1-10 alkyl, C 3-8 cycloalkenyl-C 1-10 alkyl, C 3-8 cycloalkyl, C 3-10 cycloalkenyl, C 3-10 cycloalkenyl, C 3-8 cycloalkyl C2-10, C3-8 cycloalkenyl-C2-10 alkynyl, C0-10 heterocyclylalkyl, C2-10 heterocyclylalkyl, C2-10 heterocyclylalkyl, C0-10 arylalkyl, or C2-10 arylalkyl, C0-10 heteroaryl, C2-10 hetarylalkyl, or C2-10 hetarylalkyl, any of which is optionally substituted with one or more independent G11a substituents; or in the case of -NR2R3 (R4) j1, -NR3R4, -NR4R5, -NR2bR3b (R4b) j1b, -NR3bR4b, -NR4bR5b, -NR9R10, -NR10R11, -NR11R12, -NR22R33a, R22a-J22, R33a-R22a, R33a-R22a, R33a-J22, R33a -NR33R22a, -NR6R1, -NR7R1, and -NR8R1 then R2 and R3, or R3 and R4, or R4 and R5, R2b and R3b, or R3b and R4b, or R4b and R5b, or R9 and R10, or R10 and R11 , or R11 and R12, or R22 and R33, or R22a and R33a, or R33 and R22a, or R6 and R1, or R7 and R1, or R8 and R1, respectively, are optionally taken together with the nitrogen atom to which they are attached to form a saturated or unsaturated ring of 3 to 10 members, wherein said ring is optionally substituted with one or more independent substituents G111 and where said ring optionally includes one or more heterogenous other than nitrogen to which R2 and R3, or R3 and R4 , or R4 and R5, R2b and R3b, or R3b and R4b, or R4b and R5b, or R9 and R10, or R10 and R11, or R11 and R12, or R22 and R33, or R22a and R33a, or R33 and R22a, or R6 and R1, or R7 and R1, or R8 and R1 are attached respectively; or in the case of CR6aR7a, R6a and R7a can be taken together with the carbon to which they are attached to form a saturated or unsaturated cycloalkyl or heterocycloalkyl ring of 3 to 10 members, wherein said ring is optionally substituted with one or more independent substituents G111a and wherein said ring optionally includes one or more heteroatoms; G11, G11a, G111, and G111a are, in each case, each independently halo, -CF3, -OCF3, -OR2b, NR2bR3b (R4b) j1b, - C (= O) R2b, -CO2R2b, -CONR2bR3b, -NO2 , -CN, -S (O) j1bR2b, -SO2NR2bR3b, -NR2bC (= O) R3b, -NR2bC (= O) OR3b, -NR2bC (= O) NR3bR4b, -NR2bS (O) j1bR3b, -C (= S ) OR2b, -C (= O) SR2b, -NR2bC (= NR3b) NR4bR5b, -NR2bC (= NR3b) OR4b, -NR2bC (= NR3b) SR4b, -OC (= O) OR2b, -OC (= O) NR2bR3b , - OC (= O) SR2b, -SC (= O) OR2b, -SC (= O) NR2bR3b, 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 alkenyl, C1-10 alkylthio-C2-10 alkynyl, C3-8 cyclo-C3-8 alkyl, C3-8 cycloalkenyl, C3-8 alkylC1-10 alkyl, C3-8 cycloalkenyl-C1-10 alkyl, C3-8 cycloalkyl-C2-10 alkenyl, C3-8-cycloalkenyl C2-10 alkenyl, C3-8-aC2-10 cycloalkyl, C3-8 cycloalkenyl-C2-10 alkynyl, C0-10 heterocyclylalkyl, C2-10 heterocyclylalkyl, C2-10 heterocyclylalkyl, aryl alkyl C0-10, arylalkyl C2-10 enyl, C2-10 arylalkyl, C0-10 hexylalkyl, C2-10 hexylalkyl, or C2-10 hexylalkyl, any of which is optionally substituted with one or more halo independent substituents, -CF3, -OCF3, -OR9, -NR9R10, -C (O) R9, -CO2R9, -CONR9R10, -NO2, -CN, -S (O) j2aR9, -SO2NR9R10, -NR9C (= O) R10, -NR9C (= O) 0R |
| priorityDate | 2006-01-19-04:00^^<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: 28.