PATENT CLAIM ANALYSIS

Application Number: 15934536
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-10
Patent Classification: ["530", "334000"]

Abstract:
This application pertains to orthogonally protected esters of peptide nucleic acid (PNA) monomers, which ester groups can be removed under conditions that permit typical backbone and side chain acid- and base-labile protecting groups to remain substantially intact thereby permitting the high yield of PNA monomer carboxylic acids that are suitable for use in PNA oligomer synthesis. Exemplary ester groups include, but are not limited to, 2,2,2-trichloroethyl (TCE), 2,2,2-tribromoethyl (TBE), 2-bromoethyl (2-BE) and 2-iodoethyl groups (2-IE). This invention also pertains to novel methods for the synthesis of Backbone Ester compounds and related Backbone Ester Acid Salts.

Claim (Index 94):
A method comprising:\n a) providing a Backbone Ester of formula Vb or a Backbone Ester Acid Salt according to formula VIb: b) providing a nucleobase acetic acid of formula IX: c) activating the carboxylic acid group of said nucleobase acetic acid to produce an activated nucleobase acetic acid in the presence of an organic base and a carboxylic acid activation agent; and d) mixing the Backbone Ester of formula Vb or Backbone Ester Acid Salt of formula VIb with said activated nucleobase acetic acid to thereby form a PNA Monomer Ester of formula IIb: wherein, B is a nucleobase, optionally comprising one or more protecting groups; Y \u2212  is an anion; Pg 1  is an amine protecting group; R 2  is H, D or C 1 -C 4  alkyl; each of R 3 , R 4 , R 5 , and R 6  is independently selected from the group consisting of: H, D, F, and a side chain selected from the group consisting of: IIIa, IIIb, IIIc, IIId, IIIe, IIIf, IIIg, IIIh, IIIi, IIIj, IIIk, IIIm, IIIn, IIIo, IIIp, IIIq, IIIr, IIIs, IIIt, IIIu, IIIv, IIIw, IIIx, IIIy, IIIz, IIIaa and IIIab, wherein each of IIIi, IIIj, IIIk, IIIm, IIIn, IIIo, IIIp, IIIq, IIIr, IIIs, IIIt, IIIu, IIIv, IIIw, IIIx, IIIy, and IIIz optionally comprise a protecting group; each of R 9  and R 10  is independently selected from the group consisting of: H, D and F; each R 11  is independently H, D, F, C 1 -C 6  alkyl, C 3 -C 6  cycloalkyl or aryl; each of R 12 , R 13  and R 14  is independently H, D, F, Cl, Br or I, provided however that at least one of R 12 , R 13  and R 14  is selected from Cl, Br and I; R 16  is selected from H, D and C 1 -C 4  alkyl group; and n is a whole number from 0 to 10, inclusive.

Metadata:
- Claim Count in Document: 51.0
- Percentile: 90.0
- Lexical Diversity: 1.48684
- Patent Class: 530.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['13937674', '11182936', '10819769', '12151585', '13411450']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.6591113728090306
- 35 USC 102 Novelty (BERT): 0.5132482745171394
- Combined Prediction Score: 0.6445250629798416
- Mean Citation Score: 226.086488
- Max Citation Score: 299.57407
- Similarity Product: 215.2177085383612

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