http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2702707-T3
Outgoing Links
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| filingDate | 2013-04-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2019-03-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a3db7caa923ed1742e6a7d3cfcb67ca4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3a9ab9e012f48cc399e49a5d00198251 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_027e174d784999ae7947417c8e64754c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c57318a7170ff1b5c53448088bada85d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fb37f0f1ff822d522dc0af0ade763ad1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f8db5ccdf7e64dfd47e118a58c1abeb9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a521f68b5425ea0dfcb683d6efc682f0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_761ae74c221b9e3e58e1942fa4b6bc3f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ce3d9a26069b882392a59e3664f23083 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_59cc7806ec2682354b5a846ef65cf9b5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c73bb3f79deccec4e0a68cf3c5da4ac1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_89637bde8cf9d59857a44e3b994d87f2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0d2bf27ade66031d8b04468384c1d127 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4a902284347373674ccb4075fe02bf3b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dd941ebc540a249abd846121dd5d43b9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_064f8ecfaecefb5ca3b21bd398bd8d39 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8ec388b3f7e6dc8b1f29e9edef06c57b |
| publicationDate | 2019-03-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2702707-T3 |
| titleOfInvention | DNA-PK inhibitors |
| abstract | A compound having the formula: ** Formula ** a pharmaceutically acceptable salt thereof, wherein Q is N or CH; R1 is hydrogen, CH3 or CH2CH3, or R1 and the carbon to which it is attached form a group C = CH2; Ring A is a ring system selected from ** Formula ** RA1 is hydrogen, halogen, C1-4 alkyl, C0-4 alkyl-C3-6 cycloalkyl, C0-4 alkyl-ORA1a, C0-4 alkyl-SRA1a, C0-4 alkyl- C (O) N (RA1a) 2, C0-4 alkyl-CN, C0-4 alkyl-S (O) -C1-4 alkyl, C0-4 alkyl-S (O) 2-C1 alkyl -4, C0-4 alkyl-C (O) ORA1b, C0-4 alkyl-C (O) C1-4 alkyl, C0-4 alkyl-N (RA1b) C (O) RA1a, C0-4 alkyl-N ( RA1b) S (O) 2RA1a, C0-4 alkyl N (RA1a) 2, C0-4 alkyl N (RA1b) (3-6 membered cycloalkyl), C0-4 alkyl N (RA1b) (4-heterocyclyl) -6 members), N (RA1b) alkyl C2-4-N (RA1a) 2, N (RA1b) alkyl C2-4-ORA1a, N (RA1b) alkyl C1-4- (heteroaryl 10 of 5-10 members), N (RA 1b) C 1-4 alkyl- (4-6 membered heterocyclyl), N (RA 1b) C 2-4 alkyl-N (RA 1b) C (O) RA 1a, C 0-4 alkyl-N (RA 1b) C (O) C1-4 alkyl, C0-4 alkyl (RA1b) C (O) C1-4 alkyl, C0-4 alkyl (phenyl), C04 alkyl- (3-10 membered heterocyclyl), C0-4 alkyl -C (O) - (4-6 membered heterocyclyl), C0-4 alkyl-O-C0-4 alkyl (4-6 membered heterocyclyl), C0-4 alkyl- (heteroaryl d) e 5-6 members), alkyl C0-4-C (O) - (5-6 membered heteroaryl), C0-4 alkyl-O-C0-4 alkyl- (5-6 membered heteroaryl), C0 alkyl- 4-N (RA1a) (4-6 membered heterocyclyl) or C0-4-N alkyl (RA1b) (5-6 membered heteroaryl), wherein each of said heterocyclyl RA1 is a ring system selected from aziridinyl, oxetanyl , tetrahydrofuranyl, tetrahydropyranyl, dioxanyl, dioxolanyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidinadionyl, morpholinyl, piperidinyl, piperazinyl, piperazinonyl, tetrahydrothiophenodioxidyl, 1,1-dioxothienyl, 2-oxa-6-azaspiro [3.4] octanyl and isoindolinonyl, each of said heteroaryl RA1 is a ring system selected from furanyl, thiophenyl, imidazolyl, benzoimidazolyl, oxazolyl, oxadiazolyl, thiazolyl, pyrazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, triazolyl and tetrazolyl and wherein each of said alkyl, cycloalkyl, phenyl groups , heterocyclyl and heteroaryl RA1 is optionally substituted with up to three F atoms, up to two C1-2 alkyl groups, a C3-6 cycloalkyl group, a phenyl group, a benzyl group, a C2-2 alkenylalkyl group, an alkynyl-C02 alkyl group, up to two alkyl groups C0-2-ORA1b, a C0-2-N-alkyl group (RA1b) 2, a C1-4-C4 group, a S (O) 2 C1-4 alkyl group, a C (O) RA1b group, a C (O) group ORA1b, a C (O) N (RA1b) 2 group, a CN-group or a C4-6 heterocyclic ring system selected from oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, piperidinyl and morpholinyl; each RA1a is, independently, hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl, C 4-6 heterocyclyl selected from oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, pyrrolidinyl and piperidinyl, C 5-6 heteroaryl selected from imidazolyl, triazolyl, tetrazolyl, pyrazolyl, thiophenyl, thiazolyl, pyridinyl, pyrimidinyl and pyrazinyl or two RA1a and an intermediate nitrogen atom form a 3-6 member heterocyclic ring selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, piperidinyl, piperidinonyl, tetrahydropyridinyl, piperazinyl and morpholinyl, wherein each of said alkyl, cycloalkyl, heterocyclyl and heteroaryl groups RA1a is optionally substituted with up to three F atoms, up to two C1-2 alkyl groups, a C3-6 cycloalkyl group, up to two C0-2 alkyl groups-ORA1b, a C0-2 alkyl group- N (RA1b) 2, a C1-4alkyl group, a C (O) RA1b group, a C (O) ORA1b group, a C (O) N (RA1b) 2 group or a -CN group; each RA1b is, independently, hydrogen, C1-2 alkyl or C3-4 cycloalkyl; RA2 is hydrogen, C1-4 alkyl, C0-4 alkyl-C3-6 cycloalkyl, C0-2 alkyl heterocyclyl (4-6 members), C2-4 alkyl-ORA2a, C0-2 alkyl C (O) N ( RA 2a) 2, C 0-2-S (O) 2-C 1-4 alkyl, C 0-2-C (O) C 1-4 alkyl, C 0-2-C (O) -heterocyclyl alkyl (4-6 members) ), wherein each of said heterocyclyl is selected from oxetanyl, tetrahydropyranyl, tetrahydrofuranyl, dioxanyl, dioxolanyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidinadionyl, morpholinyl, piperidinyl, piperazinyl, piperazinonyl and 1,1-dioxothietanyl and each of said groups RA2, except hydrogen, is optionally substituted with up to three F atoms, up to two C1-2 alkyl groups, a C3-6 cycloalkyl group, an alkenyl-C0-2 alkyl group, an alkynyl-C0-2 alkyl group, up to two ORA2b groups, a C 0-2-N (RA 2b) 2 alkyl group, a C 1-4 Salicyl group, a S (O) 2 C 1-4 alkyl group, a C (O) RA 2b group, a C (O) ORA 2b group, a C group (O) N (RA2b) 2 or a -CN group; each RA2a is, independently, hydrogen, C1-4alkyl, a C5-6 heteroaryl selected from imidazolyl, triazolyl, tetrazolyl, pyrazolyl, thiophenyl, thiazolyl, pyridinyl, pyrimidinyl and pyrazinyl or two RA2a and an intermediate nitrogen atom form a heterocyclic ring 3-6 members selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, piperidinyl, piperidinonyl, tetrahydropyridinyl, piperazinyl and morpholinyl; each RA2b is, independently, hydrogen, C1-4 alkyl or C3-4 cycloalkyl; RA3 is hydrogen or C1-2 alkyl; each RA4 is, independently, deuterium, halogen, CN, C1-4alkyl or C1-4alkyl, where each RA4 alkyl is optionally substituted with up to 3 F atoms, two non-geminal OH groups or a C1-2 O-alkyl, or two RA4 together with an intermediate saturated carbon atom form a cyclobutyl or spiro-linked cyclopropyl ring; n is 0-3; ring B is a ring system selected from ** Formula ** RB1 is hydrogen, C1-4 alkyl, (CH2) 0-1 C3-6 cycloalkyl, C (O) C1-5 alkyl 2, (CH2) 0-1 - heterocyclyl ring (4-6 members) wherein said heterocyclic ring is selected from oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, dioxanyl, dioxolanyl and pyrrolidinonyl, phenyl, benzyl or (CH 2) 1-2 heteroaryl heteroaryl (5-6 members) wherein said heteroaryl ring is selected from pyridinyl, imidazolyl and pyrazolyl and wherein each of said alkyl, cycloalkyl, phenyl, benzyl, heterocyclyl and heteroaryl RB1 groups is optionally substituted with up to 3 F atoms, up to two C1-2 alkyl groups, two non-geminal OH groups or a C1-2alkyl; RB2 is hydrogen, C1-4alkyl or C1-4alkyl; each RB3 is, independently, hydrogen, halogen, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, CN, C (O) H, C (O) C1-4 alkyl, C (O) C1-4alkyl , C (O) C 1-4 alkyl, C (O) NH 2, C (O) C 1-4 NH 4 alkyl, C (O) NH (CH 2) 0-1 C 3-6 cycloalkyl, C (O) NHCH 2 oxetanyl, C (O) NHCH2tetrahydrofuranyl, C (O) NHCH2tetrahydropyranyl, C (O) NHphenyl, C (O) NHbenzyl, C (O) NHOH, C (O) NHO C1-4alkyl, C (O) NHO (CH2) 0-1C3-6cycloalkyl, C (O) NHO (CH2) 0-1-oxetanyl, C (O) NHO (CH2) 0-1-tetrahydrofuranyl, C (O) NHO (CH2) 0-1-tetrahydropyranyl, C (O) NHOphenyl, C (O) NHObenzyl, NH2, NHC (O) C 1-4 alkyl, C 1-4 alkyl, C 1-4 alkyl, S (O) C 1-4 alkyl or a 5-membered heteroaryl ring system selected from furanyl, thiophenyl, imidazolyl, pyrrole, pyrazolyl and oxadiazolyl, wherein each RB3 group, except hydrogen or halogen, is optionally substituted with Cl, up to three F atoms, up to two non-geminal OH groups, up to two C1-C2alkyl, an NH2, a C1-2 NHalkyl, an NHC (O) alkyl C1-2 or an N (C1-2 alkyl) 2; each RB4 is, independently, hydrogen, halogen, C1-4alkyl, C1-4alkyl, C1-4alkyl, NH2, NH (C1-4alkyl), N (C1-4alkyl) 2 NHC (O) C1- alkyl 4, C (O) OH, C (O) C1-4alkyl, C (O) NH2, C (O) NH4alkyl C1-4, C (O) N (C1-4alkyl) 2, CN, a morpholinyl ring or an imidazolyl ring, wherein each RB4 alkyl is optionally substituted with up to 3 F atoms, two non-geminal OH groups or a C1-2 O-alkyl; RB5 is hydrogen, C1-4alkyl, C (O) C1-4alkyl, C (O) C1-4alkyl, C (O) NH2, C (O) NH4alkyl C1-4 or C (O) N (C1alkyl) - 4) 2, wherein said alkyl RB5 is optionally substituted with up to 3 F atoms, two non-geminal OH groups or a C1-2 O-alkyl and RB6 is F or C1-2 alkyl or two RB6 and an intermediate carbon atom forms a ring Spirocyclopropyl or Spirocyclobutyl; wherein the expression "alkyl" or "alkyl group" means a straight chain (ie, unbranched) or branched, substituted or unsubstituted hydrocarbon, which is completely saturated; and the terms "alkoxy" and "thioalkyl" refer to an alkyl group attached to the main carbon chain through an oxygen or a sulfur, respectively; and the term "heterocycle", "heterocyclyl", "heterocycloalkyl", or "heterocyclic", as used herein, refers to a monocyclic, bicyclic or tricyclic ring system where at least one ring in the system contains one or more heteroatoms, which is the same or different and which is completely saturated or which contains one or more units of unsaturation, but which is not aromatic and which has a single point of attachment to the rest of the molecule. |
| priorityDate | 2012-04-24-04:00^^<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: 558.