PATENT CLAIM ANALYSIS

Application Number: 16038734
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-01
Patent Classification: ["514", "332000"]

Abstract:
The invention relates to oligopyridylamide alpha-helix mimetic compounds and their use to inhibit p53 aggregation and restore its tumor suppressor function for treating diseases, e.g., cancers, associated with p53 mutations, e.g., R248W p53 mutation.

Claim (Index 13):
A method of treating a disease in a subject in need of such treatment, wherein the disease is associated with one or more p53 mutations, comprising administering to said subject an effective amount of a compound of formula (I): wherein R a  is independently selected at each occurrence from hydrogen, C 1 -C 12  hydrocarbons, \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014OH, \u2014OR*; \u2014NO; \u2014NO 2 ; \u2014NO 3 ; \u2014O\u2014NO; \u2014N 3 ; \u2014NH 2 ; \u2014NHR*; and \u2014N(R*) 2 ; X is independently at each occurrence selected from \u2014O\u2014; \u2014S\u2014; \u2014NH\u2014; \u2014NR*\u2014; and \u2014C(R*) 2 ; Y is independently at each occurrence selected from \u2014O\u2014; \u2014S\u2014; \u2014NH\u2014; and \u2014NR*\u2014; R 1  is selected from hydrogen or a straight chained, branched or cyclic aliphatic C 1 -C 20  hydrocarbon; an aromatic C 6 -C 20  hydrocarbon; a heteroaromatic C 1 -C 20  hydrocarbon; an aryl C 6 -C 20  hydrocarbon; a heteroaryl C 1 -C 20  hydrocarbon, a C 1 -C 12  perfluorocarbon, or a combination thereof, each of which optionally contains 1-8 heteroatoms selected from halogen, O, N, and S, and each of which is optionally substituted with one or more of \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014OH, \u2014OR*; \u2014NO; \u2014NO 2 ; \u2014NO 3 ; \u2014O\u2014NO; \u2014N 3 ; \u2014NH 2 ; \u2014NHR*; \u2014N(R*) 2 ; \u2014N(R*) 3 + ; \u2014N(R*)\u2014OH; \u2014O\u2014N(R*) 2 ; \u2014N(R*)\u2014O\u2014R*; \u2014CN; \u2014NC; \u2014(C\u2550O)\u2014R*; \u2014CHO; \u2014CO 2 H; \u2014CO 2 R*; \u2014(C\u2550O)\u2014S\u2014R*; \u2014O\u2014(C\u2550O)\u2014H; \u2014O\u2014(C\u2550O)\u2014R*; \u2014S\u2014(C\u2550O)\u2014R*; \u2014(C\u2550O)\u2014NH 2 ; \u2014(C\u2550O)\u2014N(R*) 2 ; \u2014(C\u2550O)\u2014NHNH 2 ; \u2014O\u2014(C\u2550O)\u2014NHNH 2 ; \u2014(C\u2550S)\u2014NH 2 ; \u2014(C\u2550S)\u2014N(R*) 2 ; \u2014N(R*)\u2014CHO; \u2014N(R*)\u2014(C\u2550O)\u2014R*; \u2014SCN; \u2014NCS; \u2014NSO; \u2014SSR*; \u2014SO 2 R*; \u2014SO 2 \u2014N(R*) 2 ; \u2014S(\u2550O)\u2014OR*; \u2014S(\u2550O)\u2014R*; \u2014Si(R*) 3 ; \u2014CF 3 ; \u2014O\u2014CF 3 ; \u2014P(R*) 2 ; \u2014O\u2014P(\u2550O)(OR*) 2 ; \u2014P(\u2550O)(OR*) 2  and combinations thereof; R 2  is independently at each occurrence selected from hydrogen or a straight chained, branched or cyclic aliphatic C 1 -C 20  hydrocarbon; an aromatic C 6 -C 20  hydrocarbon; a heteroaromatic C 1 -C 20  hydrocarbon; an aryl C 6 -C 20  hydrocarbon; a heteroaryl C 1 -C 20  hydrocarbon, a C 1 -C 12  perfluorocarbon, or a combination thereof, each of which optionally contains 1-8 heteroatoms selected from halogen, O, N, and S, and each of which is optionally substituted with one or more of \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014OH, \u2014OR*; \u2014NO; \u2014NO 2 ; \u2014NO 3 ; \u2014O\u2014NO; \u2014N 3 ; \u2014NH 2 ; \u2014NHR*; \u2014N(R*) 2 ; \u2014N(R*) 3 + ; \u2014N(R*)\u2014OH; \u2014O\u2014N(R*) 2 ; \u2014N(R*)\u2014O\u2014R*; \u2014CN; \u2014NC; \u2014(C\u2550O)\u2014R*; \u2014CHO; \u2014CO 2 H; \u2014CO 2 R*; \u2014(C\u2550O)\u2014S\u2014R*; \u2014O\u2014(C\u2550O)\u2014H; \u2014O\u2014(C\u2550O)\u2014R*; \u2014S\u2014(C\u2550O)\u2014R*; \u2014(C\u2550O)\u2014NH 2 ; \u2014(C\u2550O)\u2014N(R*) 2 ; \u2014(C\u2550O)\u2014NHNH 2 ; \u2014O\u2014(C\u2550O)\u2014NHNH 2 ; \u2014(C\u2550S)\u2014NH 2 ; \u2014(C\u2550S)\u2014N(R*) 2 ; \u2014N(R*)\u2014CHO; \u2014N(R*)\u2014(C\u2550O)\u2014R*; \u2014SCN; \u2014NCS; \u2014NSO; \u2014SSR*; \u2014SO 2 R*; \u2014SO 2 \u2014N(R*) 2 ; \u2014S(\u2550O)\u2014OR*; \u2014S(\u2550O)\u2014R*; \u2014Si(R*) 3 ; \u2014CF 3 ; \u2014O\u2014CF 3 ; \u2014P(R*) 2 ; \u2014O\u2014P(\u2550O)(OR*) 2 ; \u2014P(\u2550O)(OR*) 2  and combinations thereof; R 3  is selected from hydrogen or a straight chained, branched or cyclic aliphatic C 1 -C 20  hydrocarbon; an aromatic C 6 -C 20  hydrocarbon; a heteroaromatic C 1 -C 20  hydrocarbon; an aryl C 6 -C 20  hydrocarbon; a heteroaryl C 1 -C 20  hydrocarbon, a C 1 -C 12  perfluorocarbon, or a combination thereof, each of which optionally contains 1-8 heteroatoms selected from halogen, O, N, and S, and each of which is optionally substituted with one or more of \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014OH, \u2014OR*; \u2014NO; \u2014NO 2 ; \u2014NO 3 ; \u2014O\u2014NO; \u2014N 3 ; \u2014NH 2 ; \u2014NHR*; \u2014N(R*) 2 ; \u2014N(R*) 3 ; \u2014N(R*)\u2014OH; \u2014O\u2014N(R*) 2 ; \u2014N(R*)\u2014O\u2014R*; \u2014CN; \u2014NC; \u2014(C\u2550O)\u2014R*; \u2014CHO; \u2014CO 2 H; \u2014CO 2 R*; \u2014(C\u2550O)\u2014S\u2014R*; \u2014O\u2014(C\u2550O)\u2014H; \u2014O\u2014(C\u2550O)\u2014R*; \u2014S\u2014(C\u2550O)\u2014R*; \u2014(C\u2550O)\u2014NH 2 ; \u2014(C\u2550O)\u2014N(R*) 2 ; \u2014(C\u2550O)\u2014NHNH 2 ; \u2014O\u2014(C\u2550O)\u2014NHNH 2 ; \u2014(C\u2550S)\u2014NH 2 ; \u2014(C\u2550S)\u2014N(R*) 2 ; \u2014N(R*)\u2014CHO; \u2014N(R*)\u2014(C\u2550O)\u2014R*; \u2014SCN; \u2014NCS; \u2014NSO; \u2014SSR*; \u2014SO 2 R*; \u2014SO 2 \u2014N(R*) 2 ; \u2014S(\u2550O)\u2014OR*; \u2014S(\u2550O)\u2014R*; \u2014Si(R*) 3 ; \u2014CF 3 ; \u2014O\u2014CF 3 ; \u2014P(R*) 2 ; \u2014O\u2014P(\u2550O)(OR*) 2 ; \u2014P(\u2550O)(OR*) 2  and combinations thereof; A is selected from hydrogen, \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014OH, \u2014OR*; \u2014NO; \u2014NO 2 ; \u2014NO 3 ; \u2014O\u2014NO; \u2014N 3 ; \u2014NH 2 ; \u2014NHR*; \u2014N(R*) 2 ; \u2014N(R*) 3 + ; \u2014N(R*)\u2014OH; \u2014O\u2014N(R*) 2 ; \u2014N(R*)\u2014O\u2014R*; \u2014CN; \u2014NC; \u2014(C\u2550O)\u2014R*; \u2014CHO; \u2014CO 2 H; \u2014CO 2 R*; \u2014(C\u2550O)\u2014S\u2014R*; \u2014O\u2014(C\u2550O)\u2014H; \u2014O\u2014(C\u2550O)\u2014R*; \u2014S\u2014(C\u2550O)\u2014R*; \u2014(C\u2550O)\u2014NH 2 ; \u2014(C\u2550O)\u2014N(R*) 2 ; \u2014(C\u2550O)\u2014NHNH 2 ; \u2014O\u2014(C\u2550O)\u2014NHNH 2 ; \u2014(C\u2550S)\u2014NH 2 ; \u2014(C\u2550S)\u2014N(R*) 2 ; \u2014N(R*)\u2014CHO; \u2014N(R*)\u2014(C\u2550O)\u2014R*; \u2014SCN; \u2014NCS; \u2014NSO; \u2014SSR*; \u2014SO 2 R*; \u2014SO 2 \u2014N(R*) 2 ; \u2014S(\u2550O)\u2014OR*; \u2014S(\u2550O)\u2014R*; \u2014Si(R*) 3 ; \u2014CF 3 ; \u2014O\u2014CF 3 ; \u2014P(R*) 2 ; \u2014O\u2014P(\u2550O)(OR*) 2 ; \u2014P(\u2550O)(OR*) 2 ; C 1 -C 8  perfluorocarbon; an aliphatic C 1 -C 12  hydrocarbon; an aromatic C 1 -C 12  hydrocarbon; and a C 1 -C 12  heteroaryl; B is selected from hydrogen, \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014OH, \u2014OR*; \u2014NO; \u2014NO 2 ; \u2014NO 3 ; \u2014O\u2014NO; \u2014N 3 ; \u2014NH 2 ; \u2014NHR*; \u2014N(R*) 2 ; \u2014N(R*) 3 + ; \u2014N(R*)\u2014OH; \u2014O\u2014N(R*) 2 ; \u2014N(R*)\u2014O\u2014R*; \u2014CN; \u2014NC; \u2014(C\u2550O)\u2014R*; \u2014CHO; \u2014CO 2 H; \u2014CO 2 R*; \u2014(C\u2550O)\u2014S\u2014R*; \u2014O\u2014(C\u2550O)\u2014H; \u2014O\u2014(C\u2550O)\u2014R*; \u2014S\u2014(C\u2550O)\u2014R*; \u2014(C\u2550O)\u2014NH 2 ; \u2014(C\u2550O)\u2014N(R*) 2 ; \u2014(C\u2550O)\u2014NHNH 2 ; \u2014O\u2014(C\u2550O)\u2014NHNH 2 ; \u2014(C\u2550S)\u2014NH 2 ; \u2014(C\u2550S)\u2014N(R*) 2 ; \u2014N(R*)\u2014CHO; \u2014N(R*)\u2014(C\u2550O)\u2014R*; \u2014SCN; \u2014NCS; \u2014NSO; \u2014SSR*; \u2014SO 2 R*; \u2014SO 2 \u2014N(R*) 2 ; \u2014S(\u2550O)\u2014OR*; \u2014S(\u2550O)\u2014R*; \u2014Si(R*) 3 ; \u2014CF 3 ; \u2014O\u2014CF 3 ; \u2014P(R*) 2 ; \u2014O\u2014P(\u2550O)(OR*) 2 ; \u2014P(\u2550O)(OR*) 2 ; C 1 -C 8  perfluorocarbon; an aliphatic C 1 -C 12  hydrocarbon; an aromatic C 1 -C 12  hydrocarbon; and a C 1 -C 12  heteroaryl; R* is independently selected at each occurrence from hydrogen or C 1 -C 12  hydrocarbons each of which optionally contains 1-8 heteroatoms selected from halogen, O, N, and S and combinations thereof; and n is an integer from 0 to 2; with the proviso that (i) when n is 0, and Y is O, R 1  and R 3  are not both \u2014CH 2 CO 2 H; (ii) when n is 1, Y is O, and R 1  and R 3  are both \u2014CH 2 CO 2 H, R 2  is not \u2014CH 2 CO 2 H or a straight chained, branched or cyclic aliphatic or aryl C 1 -C 12  hydrocarbon, or R 2  does not have the structure \u2014C(CH 2 CO 2 H) 3 ; (iii) when n is 1, and Y is O, R 1  through R 3  are not each an unsubstituted C 1 -C 8  hydrocarbon; and (iv) when n is 2, and Y is O, R 1  through R 3  are not \u2014CH 2 CO 2 H at all occurrences, or a pharmaceutically acceptable salt thereof.

Metadata:
- Claim Count in Document: 29.0
- Percentile: 95.0
- Lexical Diversity: 1.29032
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14521972', '14409607', '13721491', '12344868', '14412185']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7379697100391555
- 35 USC 102 Novelty (BERT): 0.5264168851694095
- Combined Prediction Score: 0.7168144275521808
- Mean Citation Score: 278.346004
- Max Citation Score: 285.72833
- Similarity Product: 164.36528137195168

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