PATENT CLAIM ANALYSIS

Application Number: 15766799
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-08
Patent Classification: ["514", "211100"]

Abstract:
Inhibitors of Wnt signaling pathway with structures of Formula I are disclosed, together with their pharmaceutical salts. Applications of compounds of Formula I in inhibiting or modulating the Wnt signaling pathway are also disclosed. Compounds of Formula I can treat disorders caused by aberrant activation of the Wnt signaling pathway.

Claim (Index 1):
A compound of Formula I: or a pharmaceutically acceptable salt, solvate, stereoisomer or a tautomer thereof, wherein\n A is A1, A2, A3 or A4; \n U is U1, U2, U3 or U4; \n L is L1, L2, or L3; \n Q is Q1, Q2, Q3 or Q4; \n Z is Z1, Z2, Z3 or Z4; \n A1 is \n wherein X 1  to X 7  are independently selected from N and C\u2014R 13 ;\n A2 is \n A3 is A4 is wherein X 13  and X 15  are independently O, N, S or C\u2014R 4c , and X 14  is N or C;\n U1 is \n wherein X 8  to X 10  are independently selected from N and C\u2014R 14 ;\n G 1  and G 2  are independently selected from N and C; \n V 1  and V 2  are independently selected from N, O, S and C\u2014R 15 ; \n W is V 3 , V 4 \u2014V 5  or V 4 \u2550V 5 , wherein V 3  to V 5  are independently selected from N, O, S and C\u2014R 16 , wherein V 4  connects with V 1 ; and \n V 5  connects with V 2 ; \n U2 is C 6 -C 10  aryl, 5-12 membered heteroaryl, 11-13 membered heterocyclophenyl or 10-13 membered heterocycloheteroaryl, wherein heterocycle and heteroaryl comprises 1 to 4 heteroatoms independently selected from N, O and S; and \n C 6 -C 10  aryl, 5-12 membered heteroaryl, 11-13 membered heterocyclophenyl and 10-13 membered heterocycloheteroaryl are unsubstituted or substituted with 1 to 4 R 6a  groups; \n U3 is \u2014OR 14b , \u2014NR 14b R 15b , C 6 -C 12  aryl unsubstituted or substituted with 1-6 R 13b  group, 5-14 membered heteroaryl unsubstituted or substituted with 1-6 R 13b  group, 11-13 membered heterocyclophenyl unsubstituted or substituted with 1-6 R 13b  group, 10-13 membered heterocycloheteroaryl unsubstituted or substituted with 1-6 R 13b  group, C 2 -C 8  alkenyl substituted with 5-6 membered aryl or heteroaryl, C 2 -C 8  alkynyl substituted with 5-6 membered aryl or heteroaryl, or \n unsubstituted or substituted with 1 to 2 R 13b  groups, wherein heterocycle and heteroaryl comprises 1 to 4 heteroatoms independently selected from N, O and S; and\n X 11  is N or C\u2014R 13b ; \n U4 is \n wherein X 8  to X 10  are independently selected from N and C\u2014R 15c ;\n G 1  and G 2  are independently selected from N and C; \n V 1  and V 2  are independently selected from N, O, S and C\u2014R 16c ; \n W is V 3 , V 4 \u2014V 5  or V 4 \u2550V 5 , wherein V 3  to V 5  are independently selected from N, O, S and C\u2014R 17c , wherein V 4  connects with V 1 ; and \n V 5  connects with V 2 ; \n L1 is L2 is wherein Y 2  is blank, \u2014O\u2014, \u2014S\u2014, \u2014N(R 18b )\u2014 or \u2014C(R 18 )(R 19b )\u2014;\n L3 is \u2014C(R 2c )(R 3c )\u2014 or \u2014NHCH 2 CH 2 \u2014; \n Q1 is C 6 -C 10  arylene or 5-12 membered heteroarylene, wherein 5-12 membered heteroarylene comprises 1 to 4 heteroatoms independently selected from N, O and S; and\n C 6 -C 10  aryl and 5-12 membered heteroarylene are unsubstituted or substituted with 1 to 4 R 17  groups; \n \n Q2 is C 6 -C 10  arylene or 5-10 membered heteroarylene, wherein 5-10 membered heteroarylene comprises 1 to 4 heteroatoms independently selected from N, O and S; and\n C 6 -C 10  arylene and 5-10 membered heteroarylene are unsubstituted or substituted with 1 to 4 R 4a  groups; \n \n Q3 is C 6 -C 12  arylene unsubstituted or substituted with 1-6 R 6b  group, 5-14 membered heteroarylene unsubstituted or substituted with 1-6 R 6b  group, C 3 -C 6  cycloalkylene unsubstituted or substituted with 1-6 R 6b  group, C 3 -C 6  heterocylene unsubstituted or substituted with 1-6 R 6b  group, or \n unsubstituted or substituted with 1 to 2 R 6b  groups, wherein heterocyclene and heteroarylene comprises 1 to 4 heteroatoms independently selected from N, O and S; and\n X 12  is N or C\u2014R 6b ; \n Q4 is C 6 -C 10  arylene or 5-12 membered heteroarylene, wherein 5-12 membered heteroarylene comprises 1 to 4 heteroatoms independently selected from N, O and S; and \n C 6 -C 10  arylene and 5-12 membered heteroarylene are unsubstituted or substituted with 1 to 4 R 5c  groups; \n Z1 is \u2014CN, C 6  aryl, 5-6 membered heteroaryl, or \n wherein 5-6 membered heteroaryl comprises 1 to 3 heteroatoms independently selected from N, O and S;\n C 6  aryl and 5-6 membered heteroaryl are unsubstituted or substituted with 1 to 3 R 18  groups; \n Y 1  is O or NR 20 ; and \n q is 0, 1, 2, or 3; \n Z2 is H, \u2014CN, halide, \u2014OH, C 1 -C 8  alkyl, C 3 -C 8  cycloalkyl, C 2 -C 8  alkenyl, C 2 -C 8  alkynyl, C 1 -C 8  alkylsulfonyl, C 1 -C 8  acyl, aminoacyl, C 1 -C 8  acylamino, C 1 -C 8  alkylcarbamoylamino, C 1 -C 8  alkoxycarbamoyl, C 1 -C 8  alkylsulfonamido, C 1 -C 8  alkylaminosulphonyl, C 1 -C 8  alkoxy, C 2 -C 8  alkoxyacyl, phenyl, 5-6 membered heteroaryl, or 5-7 membered heterocycle, wherein 5-6 membered heteroaryl and 5-7 membered heterocycle comprise one or more hetero atoms independently selected from N, O and S; and\n phenyl, 5-6 membered heteroaryl and 5-7 membered heterocycle are unsubstituted or substituted with 1 to 3 R 5a  groups; \n \n Z3 is H, \u2014CN, halide, \u2014OH, C 1 -C 8  alkyl unsubstituted or substituted with 1 to 3 R 12b  groups, C 3 -C 8  cycloalkyl, C 2 -C 8  alkenyl, C 2 -C 8  alkynyl, C 1 -C 8  alkylsulfonyl, C 1 -C 8  acyl, aminoacyl, C 1 -C 8  acylamino, C 1 -C 8  alkylcarbamoylamino, C 1 -C 8  alkoxycarbamoyl, C 1 -C 8  alkylsulfonamido, C 1 -C 8  alkylaminosulphonyl, C 1 -C 8  alkoxy, C 2 -C 8  alkoxyacyl, \u2014N(R 7b )(R 8b ) unsubstituted or substituted with 1 to 3 R 12b  groups, phenyl unsubstituted or substituted with 1 to 3 R 9b  groups, 5-6 membered heteroaryl unsubstituted or substituted with 1 to 3 R 10b  groups, or 5-7 membered heterocycle unsubstituted or substituted with 1 to 3 R 11b  groups, wherein 5-6 membered heteroaryl and 5-7 membered heterocycle comprises 1-3 hetero atoms independently selected from N, O and S; \n Z4 is \u2014CN, C 6  aryl, 5-6 membered heteroaryl, or \n wherein 5-6 membered heteroaryl comprises 1 to 3 heteroatoms independently selected from N, O and S;\n C 6  aryl and 5-6 membered heteroaryl are unsubstituted or substituted with 1 to 3 R 6c  groups;\n Y 3  is O or NR 8c ; and \n q is 0, 1, 2, or 3; \n \n R 1  to R 3  are independently selected from H and C 1 -C 6  alkyl, wherein C 1 -C 6  alkyl is unsubstituted or substituted with 1 to 3 halide, \u2014CN, \u2014OH, C 1 -C 3  alkyl, C 3 -C 5  cycloalkyl, or C 1 -C 3  alkoxy groups; \n R 4  is H, halide, \u2014CN, \u2014OH, \u2014NO 2 , C 1 -C 6  alkyl, C 3 -C 8  cycloalkyl, or C 1 -C 6  alkoxy, wherein C 1 -C 6  alkyl, C 3 -C 8  cycloalkyl and C 1 -C 6  alkoxy are unsubstituted or substituted with 1 to 3 halide; \n R 5  and R 6  are independently selected from H, halide, \u2014CN, \u2014OH, amino, C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl and C 1 -C 6  alkoxy, wherein C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl and C 1 -C 6  alkoxy are unsubstituted or substituted with 1 to 3 halide; \n R 7  and R 8  are independently selected from H and C 1 -C 6  alkyl, or R 7  and R 8  together are oxo (\u2550O); \n R 9  to R 12  are independently selected from H, C 1 -C 6  alkyl; \n R 13  is H, halide, \u2014CN, \u2014OH, amino, \u2014NO 2 , C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl, C 1 -C 6  alkoxy, C 1 -C 6  alkylthio or 1-pyrrolidino, wherein amino, C 1 -C 6  alkyl and C 1 -C 6  alkoxy are unsubstituted or substituted with 1 to 3 halide, C 1 -C 3  alkyl or C 3 -C 6  cycloalkyl groups; \n R 14  to R 17  are independently selected from H, halide, \u2014CN, \u2014OH, amino, C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl, C 1 -C 6  alkoxy and C 1 -C 6  alkylthio, wherein amino, C 1 -C 6  alkyl and C 1 -C 6  alkoxy are unsubstituted or substituted with 1 to 3 halide, C 1 -C 3  alkyl or C 3 -C 6  cycloalkyl groups; \n R 18  is H, halide, \u2014CN, \u2014OH, amino, C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl or C 1 -C 6  alkoxy, wherein amino, C 1 -C 6  alkyl and C 1 -C 6  alkoxy are unsubstituted or substituted with 1 to 3 halide, C 1 -C 3  alkyl or C 3 -C 6  cycloalkyl groups; \n R 19  and R 20  are independently selected from H and C 1 -C 3  alkyl, or R 19  and R 20  together, with adjacent atoms they attached to, form a cyclic structure; \n R 4a , R 5a  and R 6a  are independently selected from halide, \u2014CN, and \u2014OH, or R 4a , R 5a  and R 6a  are independently selected from C 1 -C 8  alkyl, C 3 -C 8  cycloalkyl, C 1 -C 8  alkoxy, C 2 -C 8  alkenyl, C 2 -C 8  alkynyl, C 1 -C 8  alkylsulfonyl, C 1 -C 8  acyl, aminoacyl, C 1 -C 8  acylamino, C 1 -C 8  alkylcarbamoylamino, C 1 -C 8  alkoxycarbamoyl, C 1 -C 8  alkylsulfonamido, C 1 -C 8  alkylaminosulphonyl, C 2 -C 8  alkoxyacyl, and 3-8 membered heterocycle, all of which are unsubstituted or substituted with 1-3 halide, \u2014OH, \u2014CN, C 1 -C 3  alkyl, C 1 -C 3  alkoxyl or C 3 -C 8  cycloalkyl groups, wherein 3-8 membered heterocycle comprises one or more hetero atoms from N, O or S; \n R 2m  is H, deuterium, tritium, halide, \u2014OH, \u2014CN, C 1 -C 8  alkyl, C 3 -C 8  cycloalkyl or C 1 -C 8  alkoxy; \n R 2b  and R 3b  are independently selected from H, C 1 -C 6  alkyl unsubstituted or substituted with 1-3 groups selected from halide, \u2014CN, \u2014OH, C 1 -C 6  alkyl, C 3 -C 5  cycloalkyl and C 1 -C 3  alkoxy; \n R 4b  and R 5b  are independently selected from H, halide, \u2014CN, amino, C 1 -C 8  alkyl, C 3 -C 8  cycloalkyl, C 1 -C 8  alkoxy, and C 1 -C 3  alkylamino; \n R 6b  is H, halide, \u2014CN or \u2014OH, or R 6b  is selected from amino, C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl, C 1 -C 6  alkoxy, and C 1 -C 3  alkylamino, all of which are unsubstituted or substituted with 1-3 halide, C 1 -C 3  alkyl, or C 3 -C 6  cycloalkyl groups; \n R 7b  and R 8b  are independently selected from H, C 1 -C 8  alkyl and C 3 -C 8  cycloalkyl, the latter two of which are unsubstituted or substituted with 1-3 R 12b , or R 7  and R 8  together, with adjacent atoms they attached to, form a cyclic structure; \n R 9b  and R 10b  are independently selected from H, halide, \u2014CN and \u2014OH, or R 9b  and \n R 10b  are independently selected from amino, C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl, and C 1 -C 6  alkoxy, all of which are unsubstituted or substituted with 1-3 halide, C 1 -C 3  alkyl, or C 3 -C 6  cycloalkyl groups; \n R 11b  is H, halide, \u2014CN, \u2014OH, amino, C 1 -C 6  alkyl unsubstituted or substituted with halide, C 3 -C 6  cycloalkyl, oxo, or C 1 -C 6  alkoxy; \n R 12b  is H, \u2014CN, \u2014OH, amino, C 1 -C 6  alkyl unsubstituted or substituted with halide, C 3 -C 6  cycloalkyl, oxo, or C 1 -C 6  alkoxy; \n R 13b  is H, halide, \u2014CN, \u2014OH, amino, C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl, C 1 -C 6  alkoxy, C 2 -C 6  alkylcarbamoylamino, C 2 -C 6  alkoxycarbamoyl, C 1 -C 3  alkylsulphonyl, \u2014N(R 16b )S(O) 2 \u2014C 1 -C 3  alkyl, or \u2014N(R 16b )C(O)\u2014C 1 -C 3  alkyl; \n R 14b  and R 15b  are independently selected from H, C 3 -C 6  cycloalkyl unsubstituted or substituted with 1 to 3 R 20b  groups, C 1 -C 6  alkyl unsubstituted or substituted with 1 to 3 R 20b  groups, 5-6 membered aryl unsubstituted or substituted with 1 to 3 R 20b  groups, 5-6 membered heteroaryl unsubstituted or substituted with 1 to 3 R 20b  groups, and 5-6 membered heterocycle unsubstituted or substituted with 1 to 3 R 20b  groups, wherein 5-6 membered heteroaryl and 5-7 membered heterocycle comprise 1 to 3 hetero atoms independently selected from N, O and S, or R 14b  and R 15b  together, with adjacent atoms they attached to, form a cyclic structure; \n R 16b  to R 19b  are independently selected from H and C 1 -C 6  alkyl unsubstituted or substituted with halide; \n R 20b  is H, \u2014CN, \u2014OH, amino, C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl, C 1 -C 6  alkoxy, 5-6 membered aryl, or 5-6 membered heteroaryl, wherein 5-6 membered heteroaryl comprises 1 to 3 hetero atoms independently selected from N, O and S; \n R 21b  is H or C 1 -C 6  alkyl; \n R 2c  and R 3c  are independently selected from H and C 1 -C 6  alkyl unsubstituted or substituted with 1-3 halide; \n R 4c  is H, halide, C 1 -C 3  alkyl, C 3 -C 5  cycloalkyl, or C 1 -C 3  alkoxy; \n R 5c  and R 6c  are independently selected from H, halide, \u2014CN, \u2014OH, amino, C 1 -C 6  alkyl unsubstituted or substituted with 1-3 halide, C 3 -C 5  cycloalkyl, and C 1 -C 6  alkoxy; \n R 7c  and R 8c  are independently selected from H and C 1 -C 6  alkyl, or R 7c  and R 8c  together, with adjacent atoms they attached to, form a cyclic structure; \n R 9c  to R 14c  are independently selected from H, C 1 -C 6  alkyl and \u2014CF 3 ; \n R 15c  to R 17c  are independently selected from H, halide, \u2014CN, \u2014OH, amino, C 1 -C 6  alkyl unsubstituted or substituted with 1-3 halide, C 3 -C 5  cycloalkyl, and C 1 -C 6  alkoxy.

Metadata:
- Claim Count in Document: 38.0
- Percentile: 91.0
- Lexical Diversity: 1.63636
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15620761', '15923668', '15501233', '15326262', '14342656']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7857134857370551
- 35 USC 102 Novelty (BERT): 0.5441525905044828
- Combined Prediction Score: 0.7615573962137979
- Mean Citation Score: 372.209424
- Max Citation Score: 379.16312
- Similarity Product: 264.9304515825892

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

Dataset: test