PATENT CLAIM ANALYSIS

Application Number: 15986059
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-10
Patent Classification: ["514", "114000"]

Abstract:
β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

Claim (Index 21):
A compound of Formula (1): or a pharmaceutically acceptable salt thereof, wherein,\n R 1  comprises a first chemotherapeutic moiety; \n R 4  is selected from hydrogen and a second chemotherapeutic moiety; \n each of R 2 , R 3 , and R 5  is hydrogen; \n R 6  is selected from \u2014COOH, substituted C 1-4  heteroalkyl, substituted C 1-4  alkyl, and \u2014PH(\u2550O)(\u2014OH), wherein each substituent group is independently selected from C 1-3  alkyl; \u2550O, and C 1-3  alkoxy; \n each R 7  is independently selected from hydrogen and hydroxyl; \n R 8  is selected from hydrogen and \u2014CH 3 ; and \n L is selected from a bond, \u2014CH 2 \u2014, \u2014CH 2 \u2014O\u2014, \u2014CH 2 \u2014CH 2 \u2014, \u2014CH(\u2014OH)\u2014, \u2014C(\u2550O)\u2014NH\u2014, \u2014C(\u2550O)\u2014N(\u2014CH 3 )\u2014, and \u2014CH 2 \u2014C(\u2550O)\u2014, \n wherein each of the first chemotherapeutic moiety and the second chemotherapeutic moiety is independently selected from \u2014N(\u2014CH 2 \u2014CH 2 \u2014Cl) 2 , \u2014N(\u2014CD 2 -CD 2 -Cl) 2 , \u2014N(\u2014CH 2 \u2014CH 2 \u2014Br) 2 , \u2014N(\u2014CH 2 \u2014CH 2 \u2014OH) 2 , \u2014CH 2 \u2014N(\u2014CH 2 \u2014CH 2 \u2014Cl) 2 , \u2014CH 2 \u2014C(\u2550O)\u2014N(\u2014CH 2 \u2014CH 2 \u2014Cl) 2 , \u2014O\u2014C(\u2550O)\u2014N(\u2014CH 2 \u2014CH 2 \u2014Cl) 2 , \u2014NH\u2014C(\u2550O)\u2014CH 2 \u2014Br, \u2014CH 2 \u2014O\u2014C(\u2550O)\u2014N(\u2014CH 2 \u2014CH 2 \u2014Cl) 2 , \u2014N(\u2014CH 2 \u2014CH 2 \u2014Cl)(\u2014CH 2 \u2014CH 2 \u2014OH), \u2014N(\u2014O\u2014CH 2 \u2014CH 2 \u2014Cl)(\u2014CH 2 \u2014CH 2 \u2014Cl), \u2014NH\u2014CH 2 \u2014CH 2 \u2014Cl, \u2014NH\u2014CH 2 \u2014CH 2 \u2014OH, \u2014N + (\u2014O \u2212 )(\u2014CH 2 \u2014CH 2 \u2014Cl) 2 , \u2014N(\u2014CH 2 \u2014CH 2 \u2014O\u2014S(\u2550O) 2 \u2014CH 3 ) 2 , \u2014N(\u2014CH 2 \u2014CH 2 \u2014Cl)(\u2014CH 2 \u2014CH 2 \u2014O\u2014S(\u2550O) 2 \u2014CH 3 ), \u2014N(\u2014CH 2 \u2014CH 2 \u2014Br)(\u2014CH 2 \u2014CH 2 \u2014O\u2014S(\u2550O) 2 \u2014CH 3 ), \u2014N(\u2014CH 2 \u2014CH 2 \u2014Cl)(\u2014CH 2 \u2014CH 2 \u2014Br), and

Metadata:
- Claim Count in Document: 62.0
- Percentile: 93.0
- Lexical Diversity: 2.43103
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15227237', '15693905', '15182851', '15181020', '15594904']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8142001478708555
- 35 USC 102 Novelty (BERT): 0.7460616184644526
- Combined Prediction Score: 0.8073862949302153
- Mean Citation Score: 614.676122
- Max Citation Score: 852.2758
- Similarity Product: 820.6949101645947

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