PATENT CLAIM ANALYSIS

Application Number: 15910677
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-09
Patent Classification: ["514", "064000"]

Abstract:
A method is disclosed for altering the redox equilibrium of a transmembrane receptor-like protein tyrosine phosphatase (RPTP), particularly a type IIa RPTP, by chemically modulating the activity through contact of such an enzyme with a diaryl boron compound that preferentially reacts with an RPTP in an oxidized state (CyS-OH). This redox modulation is most readily observed and put to use by assaying the inhibition of the phosphatase activity of the RPTP. Such an assay can be carried out on an enzyme in vitro or by contacting the enzyme in a living organism (in vivo). A useful diaryl boron compound corresponds in structure to Formula I in which Ar-1, Ar-2, R 1 , R 2 , R 3  and R 4  are defined within. A pharmaceutical composition containing a useful diaryl boron compound is also disclosed, as are particularly preferred diaryl boron compounds.

Claim (Index 1):
A method of inhibiting the phosphatase activity of a transmembrane receptor-like protein tyrosine phosphatase (RPTP) that comprises the steps of contacting said RPTP with an effective amount of a boron-containing compound of Formula I, and maintaining said contact for as long a time period as desired to inhibit said phosphatase activity, wherein in Formula I, wherein:\n the circled substituents Ar-1 and Ar-2 bonded to the boron atom, B, are the same or different aromatic substituent that is carbocyclic or heterocyclic, contains one ring, or two or three fused rings, and when heterocyclic, contains up to four nitrogen atoms in the ring or fused rings, or one oxygen and up to three nitrogens in the ring or fused rings, \n R 1  and R 2  are the same or different substituents the sum of whose Hammett sigma functions for para and/or meta substituents, as appropriate, is greater than about zero, \n R 3  and R 4  are both fluoride, the depicted boron atom has a negative charge (B \u2212 ) and a charge-balancing pharmaceutically acceptable cation (M + ) is present, or R 3  is OH and R 4  is absent.

Metadata:
- Claim Count in Document: 116.0
- Percentile: 90.0
- Lexical Diversity: 1.73626
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['11280724', '10777186', '11219402', '12043872', '11508605']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7166224921055054
- 35 USC 102 Novelty (BERT): 0.5107969076142627
- Combined Prediction Score: 0.6960399336563812
- Mean Citation Score: 225.159968
- Max Citation Score: 234.57724
- Similarity Product: 154.71771428987262

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