http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-080982-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_3b70512b2076a2759fccaecf9fe962d5 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-02 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/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-498 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-113 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-6524 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 |
| filingDate | 2011-04-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2012-05-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-080982-A1 |
| titleOfInvention | QUINOXALINE DERIVATIVES |
| abstract | Pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds in the treatment of diseases, for example, cancer. Claim 1: A compound of the formula (1) including any tautomeric or stereochemically isomeric form thereof, wherein n represents an integer equal to 0, 1, 2, 3 or 4; R 1 represents hydrogen, C 1-6 alkyl, C 2-4 alkenyl, C 1-6 hydroxyalkyl, C 1-6 haloalkyl, C 1-6 hydroxyhaloalkyl, C 1-4 cyanoalkyl, C 1-6 alkoxy-C 1-6 alkyl, wherein each C 1-6 alkyl 6 may be optionally substituted with one or two hydroxyl groups, C1-6 alkyl substituted with -NR4R5, C1-6 alkyl substituted with -C (= O) -NR4R5, -S (= O) 2-C1-6 alkyl, - S (= O) 2-C1-6 haloalkyl, -S (= O) 2-NR14R15, C1-6 alkyl substituted with -S (= O) 2-C1-6 alkyl, C1-6 alkyl substituted with -S ( = O) 2-halo C1-6 alkyl, C1-6 alkyl substituted with -S (= O) 2-NR14R15, C1-6 alkyl substituted with -NH-S (= O) 2-C1-6 alkyl, C1- alkyl 6 substituted with -NH-S (= O) 2-C1-6 haloalkyl, C1-6 alkyl substituted with -NR12-S (= O) 2-NR14R15, R6, C1-6 alkyl substituted with R6, C1-6 alkyl substituted with -C (= O) -R6, C1-6 hydroxyalkyl substituted with R6, C1-6 alkyl substituted with -Si (CH3) 3, C1-6 alkyl substituted with -P (= O) (OH) 2 or alkyl C1-6 substituted with -P (= O) (C1-6 alkyl) 2; each R1a is independently selected from hydrogen, C1-4 alkyl, C1-4 hydroxyalkyl, C1-4 alkyl substituted with amino or mono- or di (C1-4 alkyl) amino or -NH (C3-8 cycloalkyl) , C1-4 cyanoalkyl, C1-4 alkoxy-C1-4 alkyl and C1-4 alkyl substituted with one or more fluorine atoms; each R2 is independently selected from hydroxyl, halogen, cyano, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 alkoxy, C1-4 hydroxyalkyl, C1-4 hydroxyalkoxy, C1-4 haloalkyl , C1-4 haloalkoxy, C1-4 hydroxyhaloalkyl, C1-4 hydroxyhaloalkoxy, C1-4 alkoxy-C1-4 alkyl, C1-4 haloalkoxy-C1-4 alkyl, C1-4 alkoxy-C1-4 alkyl, wherein each alkyl C1-4 may be optionally substituted with one or two hydroxyl groups, hydroxyhaloalkoxy C1-4-C1-4 alkyl, R13, C1-4 alkyl substituted with R13, C1-4 alkyl substituted with -C (= O) -R13, alkoxy C1-4 substituted with R13, C1-4 alkoxy substituted with -C (= O) -R13, -C (= O) -R13, C1-4 alkyl substituted with -NR7R8, C1-4 alkyl substituted with -C (= O) -NR7R8, C1-4 alkoxy substituted with -NR7R8, C1-4 alkoxy substituted with -C (= O) -NR7R8, -NR7R8 and -C (= O) -NR7R8, or when two R2 groups are attached to atoms adjacent carbon, can be taken together to form a radical of the formula -O- (C (R17) 2) pO-; -X-CH = CH-; or -X-CH = N-; wherein R17 represents hydrogen or fluorine, p represents 1 or 2 and X represents O or S; R3 represents hydroxyl, C1-6 alkoxy, C1-6 hydroxyalkoxy, C1-6 alkoxy substituted with -NR10R11, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl optionally substituted with -OC (= O ) -C 1-6 alkyl, C 1-6 hydroxyalkyl optionally substituted with -OC (= O) -C 1-6 alkyl, C 2-6 hydroxyalkenyl, C 2-6 hydroxyalkynyl, C 1-6 hydroxyhaloalkyl, C 1-6 cyanoalkyl, C 1-6 alkyl carboxyl substituted, C1-6 alkyl substituted with -C (= O) -C1-6 alkyl, C1-6 alkyl substituted with -C (= O) -O-C1-6 alkyl, C1-6 alkyl substituted with C1 alkoxy -6-C1-6-OC alkyl (= O) -, C1-6 alkyl substituted with C1-6 alkoxy-C1-6-C alkyl (= O) -, C1-6 alkyl substituted with -OC (= O) -C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, wherein each C1-6 alkyl can be optionally substituted with one or two hydroxyl groups or with -OC (= O) -C1-6 alkyl, C2 alkenyl 6 substituted with C1-6 alkoxy, C2-6 alkynyl substituted with C1-6 alkoxy, C1-6 alkyl substituted with R9 and optionally substituted with -OC (= O) -C alkyl 1-6, C1-6 alkyl substituted with -C (= O) -R9, C1-6 alkyl substituted with hydroxyl and R9, C2-6 alkenyl substituted with R9, C2-6 alkynyl substituted with R9, C1-6 alkyl substituted with -NR10R11, C2-6 alkenyl substituted with -NR10R11, C2-6 alkynyl substituted with -NR10R11, C1-6 alkyl substituted with hydroxyl and -NR10R11, C1-6 alkyl substituted with one or two halogens and -NR10R11, -C1 alkyl -6-C (R12) = NO-R12, C1-6 alkyl substituted with -C (= O) -NR10R11, C1-6 alkyl substituted with -OC (= O) -NR10R11, -S (= O) 2- C1-6 alkyl, -S (= O) 2-C1-6 haloalkyl, -S (= O) 2-NR14R15, C1-6 alkyl substituted with -S (= O) 2-C1-6 alkyl, C1- alkyl 6 substituted with -S (= O) 2-halo C1-6 alkyl, C1-6 alkyl substituted with -S (= O) 2-NR14R15, C1-6 alkyl substituted with -NR12-S (= O) 2-C1 alkyl -6, C1-6 alkyl substituted with -NH-S (= O) 2-haloalkyl C1-6, C1-6 alkyl substituted with -NR12-S (= O) 2-NR14R15, R13, C1-6 alkyl substituted with -P (= O) (OH) 2 or C1-6 alkyl substituted with -P (= O) (C1-6 alkyl) 2; R4 and R5 each independently represent hydrogen, C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 haloalkyl, C1-6 hydroxyhaloalkyl, C1-6 alkoxy where each C1-6 alkyl can be optionally substituted with one or two hydroxyl groups, -S (= O) 2-C1-6 alkyl, -S (= O) 2-C1-6 haloalkyl, -S (= O) 2-NR14R15, C1-6 alkyl substituted with - S (= O) 2-C1-6 alkyl, C1-6 alkyl substituted with -S (= O) 2-C1-6 haloalkyl, C1-6 alkyl substituted with -S (= O) 2-NR14R15, C1- alkyl 6 substituted with -NH-S (= O) 2-C1-6 alkyl, C1-6 alkyl substituted with -NH-S (= O) 2-C1-6 haloalkyl, C1-6 alkyl substituted with -NH-S ( = O) 2-NR14R15, R13 or C1-6 alkyl substituted with R13; R 6 represents C 3-8 cycloalkyl, C 3-8 cycloalkenyl, phenyl, 4- to 7-membered monocyclic heterocyclyl containing at least one heteroatom selected from N, O or S; said C3-8 cycloalkyl, C3-8 cycloalkenyl, phenyl, 4- to 7-membered monocyclic heterocyclyl, optionally and, independently, each substituted with 1, 2, 3, 4 or 5 substituents, each substituent being independently selected cyano, C1-6 alkyl, C1-6 cyanoalkyl, hydroxyl, carboxyl, C1-6 hydroxyalkyl, halogen, C1-6 haloalkyl, hydroxyhaloalkyl C1-6, C1-6 alkoxy, C1-6 alkoxy-C1-6 alkyl, alkyl C16-OC (= O) -, -NR14R15, -C (= O) -NR14R15, C1-6 alkyl substituted with -NR14R15, C1-6 alkyl substituted with -C (= O) -NR14R15, -S (= O ) 2-C1-6 alkyl, -S (= O) 2- C1-6 haloalkyl, -S (= O) 2-NR14R15, C1-6 alkyl substituted with -S (= O) 2-C1-6 alkyl, C1-6 alkyl substituted with -S (= O) 2-haloalkyl C1-6, C 1-6 alkyl substituted with -S (= O) 2-NR4R15, C1-6 alkyl substituted with -NH-S (= O) 2- C1-6 alkyl, C1-6 alkyl substituted with -NH-S (= O) 2-C1-6 haloalkyl or C1-6 alkyl substituted with -NH-S (= O) 2-NR14R15; R 7 and R 8 each independently represent hydrogen, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 haloalkyl, C 1-6 hydroxyhaloalkyl or C 1-6 alkoxy-C 1-6 alkyl; R9 represents C3-8 cycloalkyl, C3-8 cycloalkenyl, phenyl, naphthyl or 3- or 12-membered monocyclic or bicyclic heterocyclyl containing at least one heteroatom selected from N, O or S, said C3-8 cycloalkyl being, C3-8 cycloalkenyl , phenyl, naphthyl or monocyclic or bicyclic heterocyclyl of 3 to 12 members optionally and independently substituted with 1, 2, 3, 4 or 5 substituents, each substituent being independently selected from = O, C 1-4 alkyl, hydroxyl, carboxyl, C1-4 hydroxyalkyl, cyano, C1-4 cyanoalkyl, C1-4-OC alkyl (= O) -, C1-4 alkyl substituted with C1-4-alkyl (= O) -, C1-4-C alkyl (= O) -, C1-4 alkoxy-C1-4 alkyl, wherein each C1-4 alkyl may be optionally substituted with one or two hydroxyl, halogen, C1-4 haloalkyl, C1-4 hydroxyhaloalkyl groups, -NR14R15, -C ( = O) -NR14R15, C1-4 alkyl substituted with -NR14R15, C1-4 alkyl substituted with -C (= O) -NR14R15, C1-4 alkoxy, -S (= O) 2-C1-4 alkyl, -S (= O) 2-C1-4 haloalkyl, -S (= O) 2-NR14 R15, C1-4 alkyl substituted with -S (= O) 2-NR14R15, C1-4 alkyl substituted with -NH-S (= O) 2-C1-4 alkyl, C1-4 alkyl substituted with - NH-S ( = O) 2-haloC 1-4 alkyl, C1-4 alkyl substituted with -NH-S (= O) 2-NR14R15, R13, -C (= O) -R13, C1-4 alkyl substituted with R13, optionally substituted phenyl with R16, C1-6 phenylalkyl, wherein the phenyl is optionally substituted with R16, a 5 or 6 membered monocyclic aromatic heterocyclyl containing at least one heteroatom selected from N, O or S wherein said heterocyclyl is optionally substituted with R16; or when two of the R9 substituents are attached to the same atom, they can be taken together to form a 4- to 7-membered saturated monocyclic heterocyclyl containing at least one heteroatom selected from N, O or S; R10 and R11 each independently represent hydrogen, carboxyl, C1-6 alkyl, C1-6 cyanoalkyl, C1-6 alkyl substituted with -NR14R15, C1-6 alkyl substituted with -C (= O) -NR14R15, haloalkyl C 1-6, C 1-6 hydroxyalkyl, C 1-6 hydroxyhaloalkyl, C 1-6 alkoxy, C 1-6 alkoxy-C 1-6 alkyl, wherein each C 1-6 alkyl can be optionally substituted with one or two hydroxyl groups, R 6, alkyl C1-6 substituted with R6, -C (= O) -R6, -C (= O) -C1-6 alkyl, -C (= O) -hydroxyalkyl C1-6, -C (= O) -haloalkyl C1- 6, -C (= O) - C1-6 hydroxyhaloalkyl, C1-6 alkyl substituted with -Si (CH3) 3, -S (= O) 2-C1-6 alkyl, -S (= O) 2-haloalkyl C1 -6, -S (= O) 2-NR14R15, C1-6 alkyl substituted with -S (= O) 2-C1-6 alkyl, C1-6 alkyl substituted with -S (= O) 2-C1-6 haloalkyl , C1-6 alkyl substituted with -S (= O) 2-NR14R15, C1-6 alkyl substituted with -NH-S (= O) 2-C1-6 alkyl, C1-6 alkyl substituted with -NH-S (= O) 2-haloC 1-6 alkyl or C 1-6 alkyl substituted with -NH-S (= O) 2-NR14R15; R12 represents hydrogen or C1-4 alkyl optionally substituted with C1-4 alkoxy; R13 represents C3-8 cycloalkyl or a 4 to 6 membered saturated monocyclic heterocyclyl containing at least one heteroatom selected from N, O or S, wherein said C3-8 cycloalkyl or monocyclic heterocyclyl is optionally substituted with 1, 2 or 3 substituents each independently selected from halogen, hydroxyl, C1-6 alkyl, -C (= O) -C 1-6 alkyl, C1-6 alkoxy or -NR14R15; R14 and R15 each independently represent hydrogen or C1-4 haloalkyl or C1-4 alkyl optionally substituted with a substitute |
| priorityDate | 2010-04-30-04:00^^<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: 60.