PATENT CLAIM ANALYSIS

Application Number: 16177149
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-05
Patent Classification: ["514", "300000"]

Abstract:
Diazanaphthalene compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a diazanaphthalene compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.

Claim (Index 1):
A compound, or a pharmaceutically acceptable salt thereof, of Formula I: wherein: R 1 , R 2 , R 4 , and R 5  are independently absent or selected from the group consisting of H, halide, unsubstituted \u2014(C 1-3  haloalkyl), and unsubstituted \u2014(C 1-3  alkyl); R 3  is selected from the group consisting of -aryl optionally substituted with 1-5 R 7  and -heteroaryl optionally substituted with 1-4 R 8 ; R 6  is selected from the group consisting of \u2014(C 1-4  alkylene) p aryl substituted with 1-5 R 9 , \u2014(C 2-4  alkenylene) p aryl substituted with 1-5 R 9 , \u2014(C 1-4  alkylene) p heteroaryl optionally substituted with 1-6 R 10 ; \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 11 , \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 12 , \u2014(C 1-4  alkylene)N(R 13 )(R 14 ), \u2014N(R 15 )(R 16 ), \u2014CF(C 1-9  alkyl) 2 , \u2014(C 1-4  alkylene) p O(C 3-9  alkyl), and \u2014(C 2-9  alkynyl) optionally substituted with one or more halides; wherein each alkyl of \u2014CF(C 1-9  alkyl) 2  is, independently, optionally substituted with one or more halides; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; wherein \u2014(C 1-4  alkenylene) is, optionally substituted with one or more substituents; R 7  is selected from the group consisting of halide and \u2014N(R 17 ) 2 ; each R 8  is independently selected from the group consisting of H, halide, unsubstituted \u2014(C 1-9  alkyl), unsubstituted \u2014(C 2-9  alkenyl), unsubstituted \u2014(C 2-9  alkynyl), unsubstituted \u2014(C 1-9  haloalkyl), \u2014CN, \u2014N(R 15 )(R 18 ), \u2014(C 1-4  alkylene) p XR 19 , \u2014C(\u2550O)N(R 15 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 20 , and -carbocyclyl optionally substituted with 1-12 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; alternatively, two adjacent R 8  are taken together to form a ring which is selected from the group consisting of -heterocyclyl optionally substituted with 1-10 R 22  and -carbocyclyl optionally substituted with 1-12 R 21 ; each R 9  is independently selected from the group consisting of halide, unsubstituted \u2014(C 1-9  alkyl), unsubstituted \u2014(C 2-9  alkenyl), unsubstituted \u2014(C 2-9  alkynyl), unsubstituted \u2014(C 9  haloalkyl), \u2014XR 23 , \u2014C(\u2550O)N(R 15 ) 2 , \u2014(C 1-4  alkylene) p N(R 24 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 22 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; with the proviso that when Y 2  is N then R 9  is not \u2014OMe or each R 10  is independently selected from the group consisting of halide, unsubstituted \u2014(C 1-9  alkyl), unsubstituted \u2014(C 2-9  alkenyl), unsubstituted \u2014(C 2-9  alkynyl), unsubstituted \u2014(C 1-9  haloalkyl), \u2014CN, \u2014XR 23 , \u2014C(\u2550O)N(R 15 ) 2 , \u2014(C 1-4  alkylene) p N(R 24 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 22 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; each R 11  is independently selected from the group consisting of halide, unsubstituted \u2014(C 1-9  alkyl), unsubstituted \u2014(C 2-9  alkenyl), unsubstituted \u2014(C 2-9  alkynyl), unsubstituted \u2014(C 1-9  haloalkyl), \u2014(C 1-4  alkylene) p OR 19 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 22 , \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 , \u2014N(R 15 )(R 25 ), \u2014C(\u2550O)(R 26 ), \u2014(C 1-4  alkylene)C(\u2550O)OR 27 , \u2014(C 1-4  alkylene)aryl optionally substituted with one or more halides, \u2014(C 1-4  alkylene) p heteroaryl optionally substituted with one or more halides, and \u2014SO 2 (R 28 ); wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; alternatively, two R 11  attached to the same carbon atom can together represent \u2550O to form a carbonyl group; each R 12  is independently selected from the group consisting of halide, unsubstituted \u2014(C 1-9  alkyl), unsubstituted \u2014(C 2-9  alkenyl), unsubstituted \u2014(C 2-9  alkynyl), unsubstituted \u2014(C 1-9  haloalkyl), \u2014(C 1-4  alkylene) p OR 19 , \u2014N(R 15 )(R 29 ), \u2014C(\u2550O)(R 26 ), \u2014C(\u2550O)OR 27 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 22 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; R 13  is selected from the group consisting of H, unsubstituted \u2014(C 1-9  alkyl), unsubstituted \u2014(C 2-9  alkenyl), unsubstituted \u2014(C 2-9  alkynyl), unsubstituted \u2014(C 1-9  haloalkyl), \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 20 , and -carbocyclyl optionally substituted with 1-12 R 21 ; wherein \u2014(C 1-4  alkylene) is, optionally substituted with one or more substituents; R 14  is selected from the group consisting of unsubstituted \u2014(C 1-9  alkyl), unsubstituted \u2014(C 2-9  alkenyl), unsubstituted \u2014(C 2-9  alkynyl), unsubstituted \u2014(C 1-9  haloalkyl), \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 20 , and -carbocyclyl optionally substituted with 1-12 R 21 ; wherein \u2014(C 1-4  alkylene) is, optionally substituted with one or more substituents; each R 15  is selected from the group consisting of H, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), and unsubstituted \u2014(C 1-5  haloalkyl); R 16  is selected from the group consisting of \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 20 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; R 17  is independently selected from the group consisting of H, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), and unsubstituted \u2014(C 1-5  haloalkyl); alternatively, two adjacent R 17  are taken together to form a -heterocyclyl ring optionally substituted with 1-10 R 22 ; R 18  is independently selected from the group consisting of H, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C\u2550O)R 15 , and \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl); wherein \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; each R 19  is independently selected from the group consisting of H, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl), and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; each R 20  independently is selected from the group consisting of halide, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014CN, \u2014OH, \u2014N(R 15 ) 2 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; each R 21  is independently selected from the group consisting of halide, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), and \u2014CN; each R 22  is independently selected from the group consisting of halide, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014CN, \u2014OH, \u2014N(R 15 ) 2 , \u2014C(\u2550O)R 34 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; each R 23  is independently selected from the group consisting of H, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C 1-4  alkylene)N(R 15 ) 2 , \u2014(C 1-4  alkylene) p aryl optionally substituted with 1-10 R 30 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-12 R 31 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; each R 24  is independently selected from the group consisting of H, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl), and \u2014(C 1-4  alkylene)N(R 15 ) 2 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; each R 25  is selected from the group consisting of H, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 32 , \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 , \u2014(C 1-4  alkylene)OR 33 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; R 26  is selected from the group consisting of H, unsubstituted \u2014(C 3-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C 1-4  alkylene) p aryl optionally substituted with one or more halides or unsubstituted \u2014(C 1-5  alkyl), \u2014(C 1-4  alkylene) p heteroaryl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl), and \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl); wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; R 27  is selected from the group consisting of H, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C 1-4  alkylene) p aryl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl), \u2014(C 1-4  alkylene) p heteroaryl optionally substituted with one or more halides or unsubstituted \u2014(C 1-5  alkyl), and \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl); wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; R 28  is selected from the group consisting of unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C 1-4  alkylene) p aryl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl), \u2014(C 1-4  alkylene) p heteroaryl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl), and \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl); wherein \u2014(C 1-4  alkylene) is, optionally substituted with one or more substituents; each R 29  is selected from the group consisting of H, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 32 , \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 , \u2014(C 1-4  alkylene)OR 33 , and \u2014C(\u2550O)O(C 1-5  alkyl); wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; each R 30  is independently selected from the group consisting of halide, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), and \u2014CN; each R 31  is independently selected from the group consisting of halide, unsubstituted \u2014(C 1-5  alkyl), unsubstituted \u2014(C 2-5  alkenyl), unsubstituted \u2014(C 2-5  alkynyl), unsubstituted \u2014(C 1-5  haloalkyl), \u2014CN, \u2014OH, \u2014C(\u2550O)R 34 , \u2014N(R 24 ) 2 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents; each R 32  is independently selected from the group consisting of halide and unsubstituted \u2014(C 1-5  alkyl); each R 33  is independently selected from the group consisting of H and unsubstituted \u2014(C 1-5  alkyl); each R 34  is independently selected from the group consisting of \u2014O(C 1-5  alkyl) and a heteroaryl optionally substituted with 1-6 R 35 ; each R 35  is a -heterocyclyl optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-5  alkyl); each X is selected from the group consisting of O and S; Y 3  is CH or nitrogen; Y 1 , Y 2 , Y 4 , and Y 5  are independently selected from the group consisting of carbon and nitrogen; wherein if Y 1  is nitrogen then Y 2 , Y 4 , and Y 5  are carbon, Y 3  is CH, and R 4  is absent; if Y 2  is nitrogen then Y 1 , Y 4 , and Y 5  are carbon, Y 3  is CH, and R 5  is absent; if Y 3  is nitrogen then Y 1 , Y 2 , Y 4 , and Y 5  are carbon; if Y 4  is nitrogen then Y 1 , Y 2 , and Y 5  are carbon, Y 3  is CH, and R 1  is absent; if Y 5  is nitrogen then Y 1 , Y 2 , and Y 4  are carbon, Y 3  is CH, and R 2  is absent; and each p is independently 0 or 1.

Metadata:
- Claim Count in Document: 20.0
- Percentile: 97.0
- Lexical Diversity: 1.45902
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15498990', '15749587', '15749923', '15749910', '15749922']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8254798570429529
- 35 USC 102 Novelty (BERT): 0.591886592638085
- Combined Prediction Score: 0.8021205306024661
- Mean Citation Score: 444.7209820000001
- Max Citation Score: 527.2941
- Similarity Product: 444.8366355682611

Labels:
- Claim Label 101: 1
- Claim Label 102: 0
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 0
- Label 101 Adjusted: 1

Dataset: test