PATENT CLAIM ANALYSIS

Application Number: 15753790
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-09
Patent Classification: ["514", "255030"]

Abstract:
This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.

Claim (Index 1):
A compound of a phenylalanine scaffold of Formula I: wherein i) R 1  and R 2  are independently selected from the group consisting of, H, lower alkyl, halogen, \u2014OH, oxo, amino; ii) R 3  is selected from the group consisting of H, lower alkyl, halogen haloalkyl, hydroxylalkyl, alkoxyl, nitrile; iii) R 4  is selected from the group consisting of H and \u2014OH; iv) R 5  is selected from the group consisting of alkyl, lower alkyl, branched alkyl, aryl substituted alkyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, and an amino acid, wherein the amino acid is an L- or D-isomer of the formula \u2014CHR 6 \u2014CON\u2014R 7  wherein i) R 6  is selected from the group consisting of natural or unnatural peptide side chains; ii) R 7  is selected from the group consisting of alkyl, lower alkyl, branched alkyl, cycloalkyl, and heterocycle; v) X 1  through X 5  are selected independently from the group of C and N; vi) W is C, CH, or N, wherein when W is C then a saturated 5 member ring may optionally be constructed from Y as CH 2 ; or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

Metadata:
- Claim Count in Document: 7.0
- Percentile: 88.0
- Lexical Diversity: 1.75309
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15505017', '14825700', '14767126', '15558491', '14421778']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8191585591330401
- 35 USC 102 Novelty (BERT): 0.5736525976064795
- Combined Prediction Score: 0.7946079629803842
- Mean Citation Score: 357.37668
- Max Citation Score: 545.69147
- Similarity Product: 349.9601810585582

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