PATENT CLAIM ANALYSIS

Application Number: 16163829
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-04
Patent Classification: ["514", "210180"]

Abstract:
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present invention can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

Claim (Index 1):
A compound of the formula: wherein:\n each   is independently a single bond or a double bond; \n X 1  is CR 5 , CR 5 R 6 , N, NR 5 , O, S, C\u2550O, C\u2550S, or a carbon atom connected to Q 1 ; \n X 2  is CR 7 , CR 7 R 8 , N, NR 7 , O, S, C\u2550O, C\u2550S, or a carbon atom connected to Q 1 ; \n X 3  is CR 9 , CR 9 R 10 , N, NR 9 , O, S, C\u2550O, C\u2550S, or a carbon atom connected to Q 1 ; \n X 4  is CR 11 , CR 11 R 12 , N, NR 11 , O, S, C\u2550O, C\u2550S, or a carbon atom connected to Q 1 ; \n X 5  is CR 13 , N, or NR 13 ; \n wherein at least one of X 1 , X 2 , X 3 , and X 4  is a carbon atom connected to Q 1 ;\n Q 1  is C\u2550O, C\u2550S, C\u2550CR 14 R 15 , C\u2550NR 14 , alkylene, alkenylene, or alkynylene, each of which is independently substituted or unsubstituted, or a bond; \n m is 1, 2, 3, or 4; \n Y is N, O, or absent; \n R 1  is \u2014C(O)R 16 , \u2014C(O)OR 16 , \u2014C(O)NR 16 R 17 , \u2014OR 16 , \u2014SR 16 , \u2014NR 16 R 17 , \u2014NR 16 C(O)R 16 , \u2014OC(O)R 16 , C\u2550O, C\u2550S, \u2014CN, \u2014SiR 16 R 17 R 18 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, or heterocyclyl, each of which is independently substituted or unsubstituted, or hydrogen; \n each R 3  and R 4  is independently, \u2014C(O)R 19 , \u2014C(O)OR 19 , \u2014C(O)NR 19 R 20 , \u2014SOR 19 , \u2014SO 2 R 19 , alkyl, alkylene, alkenyl, alkenylene, alkynyl, aryl, heteroaryl, or heterocyclyl, each of which is independently substituted or unsubstituted, or hydrogen, or R 3  and R 4  together with the nitrogen atom to which R 3  and R 4  are bound form a ring, wherein the ring is substituted or unsubstituted, or R 3  is absent; \n each R 2 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 , R 15 , R 16 , R 17 , and R 18  is independently \u2014C(O)R 21 , \u2014C(O)OR 21 , \u2014C(O)NR 21 R 22 , \u2014OR 21 , \u2014SR 21 , \u2014NR 21 R 22 , \u2014NR 21 C(O)R 22 , \u2014OC(O)R 21 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, or heterocyclyl, each of which is independently substituted or unsubstituted, or hydrogen or halogen; \n each R 19  and R 20  is C(O)R 23 , \u2014C(O)OR 23 , \u2014C(O)NR 23 R 24 , \u2014OR 23 , \u2014SR 23 , \u2014NR 23 R 24 , \u2014NR 23 C(O)R 24 , \u2014OC(O)R 23 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, or heterocyclyl, each of which is independently substituted or unsubstituted, or hydrogen or halogen; \n each R 21  and R 22  is independently alkyl, alkenyl, alkynyl, aryl, heteroaryl, or heterocyclyl, each of which is independently substituted or unsubstituted, or hydrogen; and \n each R 23  and R 24  is independently alkyl, alkenyl, alkynyl, aryl, heteroaryl, or heterocyclyl, each of which is independently substituted or unsubstituted, or hydrogen, \n or a pharmaceutically-acceptable salt thereof.

Metadata:
- Claim Count in Document: 44.0
- Percentile: 97.0
- Lexical Diversity: 1.71739
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15436333', '14275667', '12538751', '14742481', '15346677']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8021164019238953
- 35 USC 102 Novelty (BERT): 0.5767324722846158
- Combined Prediction Score: 0.7795780089599674
- Mean Citation Score: 345.85709400000013
- Max Citation Score: 544.2079
- Similarity Product: 348.53691197600364

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