PATENT CLAIM ANALYSIS

Application Number: 16164447
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-04
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 2):
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 and halide; R 3  is selected from the group consisting of: wherein each of R 7 -R 25  is, independently, a substituent or a single bond connecting R 3  to the isoquinoline ring; wherein only one of R 7 -R 10  (when present) is a bond, only one of R 11 -R 14  (when present) is a bond, only one of R 15 -R 7  (when present) is a bond, only one of R 18 -R 20  (when present) is a bond, only one of R 21 -R 23  (when present) is a bond, and only one of R 24 -R 25  (when present) is a bond; for purposes of clarification, any one of the nitrogen atoms attached to R 7 , R 11 , R 15 , or R 18  can serve as the point of attachment of R 3  to the isoquinoline ring; likewise, any one of the carbon atoms attached to R 8 , R 9 , R 10 , R 12 , R 13 , R 14 , R 16 , R 17 , R 19 , R 20 , R 21 , R 22 , R 23 , R 24 , and R 25 , can serve as the point of attachment of R 3  to the isoquinoline ring; so that: when the nitrogen atom to which R 7  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 7  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 8  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 8  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 9  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 9  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 10  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 10  is a single bond connecting R 3  to the isoquinoline ring; when the nitrogen atom to which R 11  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 11  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 12  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 12  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 13  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 13  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 14  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 14  is a single bond connecting R 3  to the isoquinoline ring; when the nitrogen atom to which R 15  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 15  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 16  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 16  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 17  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 17  is a single bond connecting R 3  to the isoquinoline ring; when the nitrogen atom to which R 18  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 18  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 19  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 19  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 20  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 20  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 21  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 21  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 22  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 22  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 23  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 23  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 24  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 24  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 25  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 25  is a single bond connecting R 3  to the isoquinoline ring; R 6  is selected from the group consisting of \u2014CH 2 phenyl substituted with 1-5 R 41 , \u2014CH\u2550CHphenyl optionally substituted with halide, \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-5 R 27 , -carbocyclyl substituted with 1-5 R 28 , and wherein \u2014(C 1-4  alkylene) is, optionally substituted with one or more halides or one or more unsubstituted \u2014(C 1-3  alkyl); wherein n is 1-4, m is 0-2 and each Z is independently selected from the group consisting of CR 32  and N;\n R 7  is selected from the group consisting of a single bond, H, and unsubstituted \u2014(C 1-5  alkyl); \n R 8 , R 9 , and R 10  are independently selected from the group consisting of a single bond, H, and unsubstituted \u2014(C 1-5  alkyl); \n R 11  is selected from the group consisting of a single bond, H, and unsubstituted \u2014(C 1-5  alkyl); \n R 12 , R 13 , and R 14  are independently selected from the group consisting of a single bond, H, and unsubstituted \u2014(C 1-5  alkyl); \n R 15  is selected from the group consisting of a single bond, H, and unsubstituted \u2014(C 1-5  alkyl); \n R 16  and R 17  are independently selected from the group consisting of a single bond, H, and unsubstituted \u2014(C 1-5  alkyl); \n R 18  is selected from the group consisting of a single bond, H, and unsubstituted \u2014(C 1-5  alkyl); \n R 19  and R 20  are independently selected from the group consisting of a single bond, H, and unsubstituted \u2014(C 1-5  alkyl); \n R 21 , R 22 , and R 23  are independently selected from the group consisting of a single bond, H, and unsubstituted \u2014(C 1-5  alkyl); \n R 24  and R 25  are independently selected from the group consisting of a single bond, H, and unsubstituted \u2014(C 1-5  alkyl); \n each R 27  is independently selected from the group consisting of halide, and \u2014N(R 43 )(R 44 ), with the proviso that if one or more R 27  is halide, at least one R 27  is \u2014N(R 43 )(R 44 ); \n each R 28  is independently \u2014N(R 33 )(R 34 ); \n 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), and unsubstituted \u2014(C 1-5  haloalkyl); \n R 33  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); \n R 34  is attached to the nitrogen and is selected from the group consisting of unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 39 , \u2014(C 1-4  alkylene)OR 35 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more halides or unsubstituted \u2014(C 1-3  alkyl); \n each R 35  is independently selected from the group consisting of H and unsubstituted \u2014(C 1-5  alkyl); \n each R 38  is independently selected from the group consisting of halide and unsubstituted \u2014(C 1-5  alkyl); \n each R 39  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 40 ; 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); \n each R 40  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; \n each R 41  is independently selected from the group consisting of halide and \u2014OMe; \n each R 43  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); \n each R 44  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), unsubstituted \u2014(C 1-5  haloalkyl), \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 39 , and \u2014(C 1-4  alkylene)OR 35 ; 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); \n each X is O or S; \n each p is independently 0 or 1; and \n wherein one or more H are optionally replaced by D.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 97.0
- Lexical Diversity: 1.45902
- Patent Class: 546.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['16130842', '15499013', '15498990', '15925157', '15833917']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8651652826046379
- 35 USC 102 Novelty (BERT): 0.5734254001896475
- Combined Prediction Score: 0.8359912943631389
- Mean Citation Score: 459.46616000000006
- Max Citation Score: 491.91196
- Similarity Product: 417.8281930410743

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