PATENT CLAIM ANALYSIS

Application Number: 16172553
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-05
Patent Classification: ["546", "143000"]

Abstract:
Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an isoquinoline 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 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 a 6-10-membered heteroaryl optionally substituted with 1-4 R; R 6  is selected from the group consisting of \u2014(C 1-4  alkylene) p heteroaryl optionally substituted with 1-6 R 9 , \u2014(C 1-4  alkylene) p aryl optionally substituted with 1-6 R 25 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 10 , \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 11 , \u2014(C 1-4  alkylene)N(R 12 )(R 13 ), \u2014N(R 14 )(R 15 ), \u2014CF(C 1-9  alkyl) 2 , \u2014(C 1-4  alkylene) p O(C 1-9 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 halides or one or more unsubstituted \u2014(C 1-3  alkyl); R 7  is selected from the group consisting of halide and \u2014N(R 16 ) 2 ; R 8  is 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, \u2014N(R 17 )(R 18 ), \u2014(C 1-4  alkylene) p X 1 R 19 , \u2014C(\u2550O)N(R 20 ) 2 , and \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 21 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); 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 1-9  haloalkyl), \u2014X 2 R 22 , \u2014C(\u2550O)N(R 23 ) 2 , \u2014(C 1-4  alkylene) p N(R 24 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 25 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 26 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); 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), \u2014(C 1-4  alkylene) p OR 27 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 28 , \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 29 , \u2014C(\u2550O)(R 30 ), \u2014(C 1-4  alkylene) p C(\u2550O)OR 30 , \u2014N(R 20 ) 2 , \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 31 ); wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); alternatively, if two R 10  are attached to the same carbon atom can together represent \u2550O to form a carbonyl group; 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 27 , \u2014N(R 20 ) 2 , \u2014C(\u2550O)(R 30 ), \u2014C(\u2550O)OR 30 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 28 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 29 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); R 12  is attached to the nitrogen and 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 32 , and -carbocyclyl optionally substituted with 1-12 R 33 ; wherein \u2014(C 1-4  alkylene) is, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); R 13  is attached to the nitrogen and 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 32 , and -carbocyclyl optionally substituted with 1-12 R 33 ; wherein \u2014(C 1-4  alkylene) is, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); R 14  is attached to the nitrogen and 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 15  is attached to the nitrogen and is selected from the group consisting of \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 32 , and -\u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 33 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); R 16  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 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 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 halides or one or more unsubstituted \u2014(C 1-3  alkyl); alternatively, two adjacent R 16  are taken together to form a -heterocyclyl ring optionally substituted with 1-10 R 32 ; R 17  is attached to the nitrogen and 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 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 34 , 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 halides or one or more unsubstituted \u2014(C 1-3  alkyl); 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), 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 halides or one or more unsubstituted \u2014(C 1-3  alkyl); each R 20  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); 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 \u2014N(R 20 ) 2 , \u2014CN, and \u2014OH; each R 22  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 34 ) 2 , \u2014(C 1-4  alkylene) p aryl optionally substituted with 1-10 R 35 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-12 R 36 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 29 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); 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), and unsubstituted \u2014(C 1-5  haloalkyl); 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), and \u2014(C 1-4  alkylene)N(R 34 ) 2 ; wherein \u2014(C 1-4  alkylene) is optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); each R 25  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, \u2014C(\u2550O)R 37 , \u2014N(R 38 ) 2 , \u2014(C 1-4  alkylene) p OR 27 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 32 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 26 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; each R 26  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 27  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), and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 29 , 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 halides or one or more unsubstituted \u2014(C 1-3  alkyl); each R 28  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, and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 29 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); each R 29  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; R 30  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 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 halides or one or more unsubstituted \u2014(C 1-3  alkyl); R 31  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 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 \u2014(C 1-4  alkylene) is, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); each R 32  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), and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 29 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); each R 33  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), and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 29 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); R 34  is attached to the nitrogen and 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); each R 35  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 36  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 37 , \u2014N(R 38 ) 2 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 29 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); each R 37  is a heteroaryl optionally substituted with 1-6 R 39 ; each R 38  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), and \u2014(C 1-4  alkylene)N(R 34 ) 2 ; wherein \u2014(C 1-4  alkylene) is optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); each R 39  is a -heterocyclyl optionally substituted with 1-10 R 29 ; each X 1  is selected from the group consisting of O and S; each X 2  is selected from the group consisting of O, S, and NR 34 ; each p is independently 0 or 1; and with the proviso that Formula I is not a structure selected from the group consisting of:

Metadata:
- Claim Count in Document: 2.0
- Percentile: 97.0
- Lexical Diversity: 1.45902
- Patent Class: 546.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['16172589', '15943864', '15498990', '16164447', '16130842']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8711175814178954
- 35 USC 102 Novelty (BERT): 0.5922577048960774
- Combined Prediction Score: 0.8432315937657137
- Mean Citation Score: 488.735218
- Max Citation Score: 516.59186
- Similarity Product: 479.972197750684

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

Dataset: test