PATENT CLAIM ANALYSIS

Application Number: 16130842
Application Type: Utility
Filing Date: 2018-09
Publication Date: 2019-08
Patent Classification: ["514", "310000"]

Abstract:
Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention 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, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Claim (Index 2):
A method of treating cancer in a patient, wherein the cancer is selected from: breast cancers, colorectal cancers, tumors of the hematopoietic and lymphoid tissues, liver cancers, lung cancers, ovarian cancers, pancreatic cancers, and prostate cancers, the method comprising administering to the patient a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof: wherein: R 1 , R 2 , R 4 , and R 5  are independently selected from the group consisting of H, halide, amino, unsubstituted \u2014(C 1-3  haloalkyl), and unsubstituted \u2014(C 1-3  alkyl); R 3  is selected from the group consisting of: wherein each of R 7 -R 35  is, independently, a substituent as defined anywhere herein or a single bond connecting R 3  to the isoquinoline ring; wherein only one of R 7 -R 1  (when present) is a bond, only one of R 11 -R 14  (when present) is a bond, only one of R 15 -R 17  (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, only one of R 24 -R 26  (when present) is a bond, only one of R 27 -R 29  (when present) is a bond, only one of R 30 -R 31  (when present) is a bond, only one of R 32 -R 33  (when present) is a bond, and only one of R 34 -R 35  (when present) is a bond; wherein any one of the nitrogen atoms attached to R 7 , R 11 , R 15 , R 18 , or R 21  can serve as the point of attachment of R 3  to the isoquinoline ring; wherein 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 22 , R 23 , R 24 , R 25 , R 26 , R 27 , R 28 , R 29 , R 30 , R 31 , R 32 , R 33 , R 34 , or R 35  can serve as the point of attachment of R 3  to the isoquinoline ring; as 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 nitrogen 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; when the carbon atom to which R 26  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 26  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 27  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 27  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 28  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 28  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 29  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 29  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 30  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 30  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 31  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 31  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 32  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 32  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 33  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 33  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 34  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 34  is a single bond connecting R 3  to the isoquinoline ring; when the carbon atom to which R 35  is attached serves as the point of attachment of R 3  to the isoquinoline ring, then R 35  is a single bond connecting R 3  to the isoquinoline ring; R 6  is selected from the group consisting of -phenyl substituted with 1-5 R 36 , \u2014(C 1-3  alkylene) p pyridinyl optionally substituted with 1-6 R 37 , and a 6-10 membered heteroaryl optionally substituted with 1-6 R 37 ; wherein the carbonyl of Formula I is attached to an aromatic ring of the heteroaryl; wherein \u2014(C 1-3  alkylene) is optionally substituted with one or more substituents as defined anywhere herein; R 7  is selected from the group consisting of a single bond, 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)N(R 48 ) 2 , \u2014(C 1-4  alkylene)OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein \u2014(C 1-4  alkylene) is optionally substituted with one or more substituents as defined anywhere herein; R 8 , R 9 , and R 10  are independently selected from the group consisting of a single bond, 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), \u2014(C 1-4  alkylene) p N(R 48 ) 2 , \u2014(C 1-4  alkylene) p OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; alternatively, one of R 7  and R 8 , R 8  and R 9 , or R 9  and R 10  are taken together to form a ring which is selected from the group consisting of -heterocyclyl optionally substituted with 1-10 R 40  and -carbocyclyl optionally substituted with 1-12 R 41 ; R 11  is selected from the group consisting of a single bond, 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)N(R 48 ) 2 , \u2014(C 1-4  alkylene)OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein \u2014(C 1-4  alkylene) is optionally substituted with one or more substituents as defined anywhere herein; R 12 , R 13 , and R 14  are independently selected from the group consisting of a single bond, 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), \u2014(C 1-4  alkylene) p N(R 48 ) 2 , \u2014(C 1-4  alkylene) p OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; alternatively, one of R 11  and R 12 , R 12  and R 13 , or R 14  and R 11  are taken together to form a ring which is selected from the group consisting of -heterocyclyl optionally substituted with 1-10 R 40  and -carbocyclyl optionally substituted with 1-12 R 41 ; R 15  is selected from the group consisting of a single bond, 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)N(R 48 ) 2 , \u2014(C 1-4  alkylene)OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein \u2014(C 1-4  alkylene) is optionally substituted with one or more substituents as defined anywhere herein; R 16  and R 17  are independently selected from the group consisting of a single bond, 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), \u2014(C 1-4  alkylene) p N(R 48 ) 2 , \u2014(C 1-4  alkylene) p OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; alternatively, one of R 15  and R 16  or R 16  and R 17  are taken together to form a ring which is selected from the group consisting of -heterocyclyl optionally substituted with 1-10 R 40  and -carbocyclyl optionally substituted with 1-12 R 41 ; R 18  is selected from the group consisting of a single bond, 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)N(R 48 ) 2 , \u2014(C 1-4  alkylene)OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein \u2014(C 1-4  alkylene) is optionally substituted with one or more substituents as defined anywhere herein; R 19  and R 20  are independently selected from the group consisting of a single bond, 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), \u2014(C 1-4  alkylene) p N(R 48 ) 2 , \u2014(C 1-4  alkylene) p OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; alternatively, one of R 18  and R 19  or R 18  and R 20  are taken together to form a heterocyclyl optionally substituted with 1-10 R 40 ; R 21  is selected from the group consisting of a single bond, 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)N(R 48 ) 2 , \u2014(C 1-4  alkylene)OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein \u2014(C 1-4  alkylene) is optionally substituted with one or more substituents as defined anywhere herein; R 22  and R 23  are independently selected from the group consisting of a single bond, 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), \u2014(C 1-4  alkylene) p N(R 48 ) 2 , \u2014(C 1-4  alkylene) p OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; alternatively, R 22  and R 23  are taken together to form a ring which is selected from the group consisting of -heterocyclyl optionally substituted with 1-10 R 40  and -carbocyclyl optionally substituted with 1-12 R 41 ; R 24 , R 25 , and R 26  are independently selected from the group consisting of a single bond, 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), \u2014(C 1-4  alkylene) p N(R 48 ) 2 , \u2014(C 1-4  alkylene) p OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; alternatively, one of R 24  and R 25  or R 25  and R 26  are taken together to form a ring which is selected from the group consisting of -heterocyclyl optionally substituted with 1-10 R 40  and -carbocyclyl optionally substituted with 1-12 R 41 ; R 27 , R 28 , and R 29  are independently selected from the group consisting of a single bond, 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), \u2014(C 1-4  alkylene) p N(R 48 ) 2 , \u2014(C 1-4  alkylene) p OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; alternatively, R 27  and R 28  are taken together to form a ring which is selected from the group consisting of -heterocyclyl optionally substituted with 1-10 R 40  and -carbocyclyl optionally substituted with 1-12 R 41 ; R 30  and R 31  are independently selected from the group consisting of a single bond, 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), \u2014(C 1-4  alkylene) p N(R 48 ) 2 , \u2014(C 1-4  alkylene) p OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; alternatively, R 30  and R 31  are taken together to form a ring which is selected from the group consisting of -heterocyclyl optionally substituted with 1-10 R 40  and -carbocyclyl optionally substituted with 1-12 R 41 ; R 32  and R 33  are independently selected from the group consisting of a single bond, 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), \u2014(C 1-4  alkylene) p N(R 48 ) 2 , \u2014(C 1-4  alkylene) p OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; R 34  and R 35  are independently selected from the group consisting of a single bond, 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), \u2014(C 1-4  alkylene) p N(R 48 ) 2 , \u2014(C 1-4  alkylene) p OR 49 , \u2014C(\u2550O)N(R 48 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 38 , and -carbocyclyl optionally substituted with 1-12 R 39 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; alternatively, R 34  and R 35  are taken together to form a ring which is selected from the group consisting of -heterocyclyl optionally substituted with 1-10 R 40  and -carbocyclyl optionally substituted with 1-12 R 41 ; each R 36  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), \u2014XR 42 , \u2014C(\u2550O)N(R 47 ) 2 , \u2014(C 1-4  alkylene) p N(R 50 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 43 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 44 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; each R 37  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), \u2014XR 42 , \u2014C(\u2550O)N(R 47 ) 2 , \u2014(C 1-4  alkylene) p N(R 50 ) 2 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-10 R 43 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 44 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; each R 38  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 44 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; 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 44 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; 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), \u2014CN, and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 44 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; each R 41  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 42  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 48 ) 2 , \u2014(C 1-4  alkylene) p aryl optionally substituted with 1-10 R 46 , \u2014(C 1-4  alkylene) p heterocyclyl optionally substituted with 1-12 R 43 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 44 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; each R 43  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 51 , \u2014N(R 50 ) 2 , and \u2014(C 1-4  alkylene) p carbocyclyl optionally substituted with 1-12 R 44 ; wherein each \u2014(C 1-4  alkylene) is, independently, optionally substituted with one or more substituents as defined anywhere herein; each R 44  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), and \u2014CN; each R 46  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 47  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 48  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 49  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 50  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 48 ) 2 ; wherein \u2014(C 1-4  alkylene) is optionally substituted with one or more substituents as defined anywhere herein; each R 51  is a heteroaryl optionally substituted with 1-6 R 52 ; each R 52  is a -heterocyclyl optionally substituted with 1-10 R 46 ; each X is selected from the group consisting of O, S, and NR 48 ; each Y is selected from the group consisting of O and S; and each p is independently 0 or 1.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 97.0
- Lexical Diversity: 1.62319
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15499013', '15498990', '15833917', '15884112', '15925157']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8211268362136653
- 35 USC 102 Novelty (BERT): 0.5989481320391083
- Combined Prediction Score: 0.7989089657962097
- Mean Citation Score: 545.201964
- Max Citation Score: 618.7224
- Similarity Product: 418.93336151447295

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