PATENT CLAIM ANALYSIS

Application Number: 16042206
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2018-11
Patent Classification: ["514", "210000"]

Abstract:
The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Claim (Index 56):
A method of sensitizing a cell to an agent that induces a DNA lesion comprising contacting the cell with a compound having the formula: wherein\n Q is N or CH; \n R 1  is hydrogen, CH 3 , CH 2 CH 3 , or R 1  and the carbon to which it is bound form a C\u2550CH 2  group; \n Ring A is a ring system selected from \n R A1  is hydrogen, halogen, C 1-4 alkyl, C 0-4 alkyl-C 3-6 cycloalkyl, C 0-4 alkyl-OR A1a , C 0-4 alkyl-SR A1a , C 0-4 alkyl-C(O)N(R A1a ) 2 , C 0-4 alkyl-CN, C 0-4 alkyl-S(O)\u2014C 1-4 alkyl, C 0-4 alkyl-S(O) 2 \u2014C 1-4 alkyl, C 0-4 alkyl-C(O)OR A1b , C 0-4 alkyl-C(O)C 1-4 alkyl, C 0-4 alkyl-N(R A1b )C(O)R A1a , C 0-4 alkyl-N(R A1b )S(O) 2 R A1a , C 0-4 alkyl-N(R A1a ) 2 , C 0-4 alkyl-N(R A1b )(3-6 membered-cycloalkyl), C 0-4 alkyl-N(R A1b )(4-6 membered-heterocyclyl), N(R A1b )C 2-4 alkyl-N(R A1a ) 2 , N(R A1b )C 2-4 alkyl-OR A1a N(R A1b )C 1-4 alkyl-(5-10 membered heteroaryl), N(R A1b )C 1-4 alkyl-(4-6 membered heterocyclyl), N(R A1b )C 2-4 alkyl-N(R A1b )C(O)R A1a , C 0-4 alkyl-N(R A1b )C(O)C 1-4 alkyl, C 0-4 alkyl-N(R A1b )C(O)OC 1-4 alkyl, C 0-4 alkyl-(phenyl), C 0-4 alkyl-(3-10 membered-heterocyclyl), C 0-4 alkyl-C(O)-(4-6 membered-heterocyclyl), C 0-4 alkyl-O\u2014C 0-4 alkyl-(4-6 membered-heterocyclyl), C 0-4 alkyl-(5-6 membered-heteroaryl), C 0-4 alkyl-C(O)-(5-6 membered-heteroaryl), C 0-4 alkyl-O\u2014C 0-4 alkyl-(5-6 membered-heteroaryl), C 0-4 alkyl-N(R A1a )(4-6 membered-heterocyclyl), or C 0-4 alkyl-N(R A1b )(5-6 membered-heteroaryl), wherein each of said R A1  heterocyclyl is a ring system selected from aziridinyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, dioxanyl, dioxolanyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidinedionyl, morpholinyl, piperidinyl, piperazinyl, piperazinonyl, tetrahydrothiophenedioxidyl, 1,1-dioxothietanyl, 2-oxa-6-azaspiro[3.4]octanyl, or isoindolinonyl wherein each of said R A1  heteroaryl is a ring system selected from furanyl, thiophenyl, imidazolyl, benzoimidazolyl, oxazolyl, oxadiazolyl, thiazolyl, pyrazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, triazolyl, or tetrazolyl, and wherein each of said R A1  alkyl, cycloalkyl, phenyl, heterocyclyl, or heteroaryl groups is optionally substituted with up to three F atoms, up to two C 1-2 alkyl groups, a C 3-6 cycloalkyl group, a phenyl group, a benzyl group, an alkenyl-C 0-2 alkyl group, an alkynyl-C 0-2 alkyl group, up to two C 0-2 alkyl-OR A1b  groups, a C 0-2 alkyl-N(R A1b ) 2  group, a SC 1-4 alkyl group, a S(O) 2 C 1-4 alkyl group, a C(O)R A1b  group, a C(O)OR A1b  group, a C(O)N(R A1b ) 2  group, a \u2014CN group, or a C 4-6 heterocyclic ring system selected from oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, piperidinyl, or morpholinyl; each R A1a  is, independently, hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl, C 4-6 heterocyclyl selected from oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, pyrrolidinyl, or piperidinyl, C 5-6 heteroaryl selected from imidazolyl, triazolyl, tetrazolyl, pyrazolyl, thiophenyl, thiazolyl, pyridinyl, pyrimidinyl, or pyrazinyl, or two R A1a  and an intervening nitrogen atom form a 3-6 membered heterocyclic ring selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, piperidinyl, piperidinonyl, tetrahydropyridinyl, piperazinyl, or morpholinyl, wherein each of said R A1a  alkyl, cycloalkyl, heterocyclyl, or heteroaryl groups is optionally substituted with up to three F atoms, up to two C 1-2 alkyl groups, a C 3-6 cycloalkyl group, up to two C 0-2 alkyl-OR A1b  groups, a C 0-2 alkyl-N(R A1b ) 2  group, a SC 1-4 alkyl group, a C(O)R A1b  group, a C(O)OR A1b  group, a C(O)N(R A1b ) 2  group, or a \u2014CN group; each R A1b  is, independently, hydrogen, C 1-2 alkyl, or C 3-4 cycloalkyl; R A2  is hydrogen, C 1-4 alkyl, C 0-4 alkyl-C 3-6 cycloalkyl, C 0-2 alkyl-(4-6 membered)heterocyclyl, C 2-4 alkyl-OR A2a , C 0-2 alkyl-C(O)N(R A2a ) 2 , C 0-2 alkyl-S(O) 2 \u2014C 1-4 alkyl, C 0-2 alkyl-C(O)OC 1-4 alkyl, C 0-2 alkyl-C(O)-(4-6 membered)heterocyclyl, wherein each of said heterocyclyl is selected from oxetanyl, tetrahydropyranyl, tetrahydrofuranyl, dioxanyl, dioxolanyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidinedionyl, morpholinyl, piperidinyl, piperazinyl, piperazinonyl, or 1,1-dioxothietanyl, and each of said R A2  groups except hydrogen is optionally substituted with up to three F atoms, up to two C 1-2 alkyl groups, a C 3-6 cycloalkyl group, an alkenyl-C 0-2 alkyl group, an alkynyl-C 0-2 alkyl group, up to two OR A2b  groups, a C 0-2 alkyl-N(R A2b ) 2  group, a SC 1-4 alkyl group, a S(O) 2 C 1-4 alkyl group, a C(O)R A2b  group, a C(O)OR A2b  group, a C(O)N(R A2b ) 2  group, or a \u2014CN group; each R A2a  is, independently, hydrogen, C 1-4 alkyl, a C 5-6 heteroaryl selected from imidazolyl, triazolyl, tetrazolyl, pyrazolyl, thiophenyl, thiazolyl, pyridinyl, pyrimidinyl, or pyrazinyl, or two R A2a  and an intervening nitrogen atom form a 3-6 membered heterocyclic ring selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, piperidinyl, piperidinonyl, tetrahydropyridinyl, piperazinyl, or morpholinyl; each R A2b  is, independently, hydrogen, C 1-4 alkyl, or C 3-4 cycloalkyl; R A3  is hydrogen or C 1-2 alkyl; each R A4  is, independently, deuterium, halogen, CN, C 1-4 alkyl, or OC 1-4 alkyl, wherein each R A4  alkyl is optionally substituted with up to 3 F atoms, two non-geminal OH groups, or one OC 1-2 alkyl, or two R A4  together with an intervening saturated carbon atom form a spiral cyclopropyl or cyclobutyl ring; n is 0-3; Ring B is a ring system selected from R B1  is hydrogen, C 1-4 alkyl, (CH 2 ) 0-1 C 3-6 cycloalkyl, C(O)C 1-2 alkyl, (CH 2 ) 0-1 -(4-6 membered)heterocyclyl ring wherein said heterocyclic ring is selected from selected from oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, dioxanyl, dioxolanyl, or pyrrolidinonyl, phenyl, benzyl, or (CH 2 ) 1-2 (5-6 membered)heteroaryl ring wherein said heteroaryl ring is selected from pyridinyl, imidazolyl, or pyrazolyl, and wherein each of said R B1  alkyl, cycloalkyl, phenyl, benzyl, heterocyclyl or heteroaryl groups is optionally substituted with up to 3 F atoms, up to two C 1-2 alkyl groups, two non-geminal OH groups, or one OC 1-2 alkyl; R B2  is hydrogen, C 1-4 alkyl, OC 1-4 alkyl; each R B3  is, independently, hydrogen, halogen, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, CN, C(O)H, C(O)C 1-4 alkyl, C(O)OC 1-4 alkyl, C(O)C 1-4 alkyl, C(O)NH 2 , C(O)NHC 1-4 alkyl, C(O)NH(CH 2 ) 0-1 C 3-6 cycloalkyl, C(O)NHCH 2 oxetanyl, C(O)NHCH 2 tetrahydrofuranyl, C(O)NHCH 2 tetrahydropyranyl, C(O)NHphenyl, C(O)NHbenzyl, C(O)NHOH, C(O)NHOC 1-4  alkyl, C(O)NHO(CH 2 ) 0-1 C 3-6 cycloalkyl, C(O)NHO(CH 2 ) 0-1 oxetanyl, C(O)NHO(CH 2 ) 0-1 tetrahydrofuranyl, C(O)NHO(CH 2 ) 0-1 tetrahydropyranyl, C(O)NHOphenyl, C(O)NHObenzyl, NH 2 , NHC(O)C 1-4 alkyl, OC 1-4 alkyl, SC 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 R B3  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 OC 1-2 alkyl, one NH 2 , one NHC 1-2  alkyl, one NHC(O)C 1-2 alkyl, or one N(C 1-2 alkyl) 2 ; each R B4  is, independently, hydrogen, halogen, C 1-4 alkyl, OC 1-4 alkyl, SC 1-4 alkyl, NH 2 , NH(C 1-4 alkyl), N(C 1-4 alkyl) 2 , NHC(O)C 1-4 alkyl, C(O)OH, C(O)OC 1-4 alkyl, C(O)NH 2 , C(O)NHC 1-4 alkyl, C(O)N(C 1-4 alkyl) 2 , CN, a morpholinyl ring, or an imidazolyl ring, wherein each R B4  alkyl is optionally substituted with up to 3 F atoms, two non-geminal OH groups, or one OC 1-2 alkyl, R B5  is hydrogen, C 1-4 alkyl, C(O)C 1-4 alkyl, C(O)OC 1-4 alkyl, C(O)NH 2 , C(O)NHC 1-4 alkyl, or C(O)N(C 1-4 alkyl) 2 , wherein said R B5  alkyl is optionally substituted with up to 3 F atoms, two non-geminal OH groups, or one OC 1-2 alkyl and R B6  is F or C 1-2 alkyl, or two R B6  and an intervening carbon atom from a spirocyclopropyl or spirocyclobutyl ring.

Metadata:
- Claim Count in Document: 26.0
- Percentile: 95.0
- Lexical Diversity: 1.29032
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14515793', '15912074', '15426150', '14205508', '14205657']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8265307759859577
- 35 USC 102 Novelty (BERT): 0.5777298921073217
- Combined Prediction Score: 0.8016506875980941
- Mean Citation Score: 415.617586
- Max Citation Score: 484.16336
- Similarity Product: 378.629515509224

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test