PATENT CLAIM ANALYSIS

Application Number: 15890181
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-06
Patent Classification: ["536", "017900"]

Abstract:
The invention comprises a new process for the preparation of GalNAc derivatives of the formula I wherein n is an integer between 0 and 10 and its salts, corresponding enantiomers and/or optical isomers thereof. The GalNAc acid derivative of formula I can be used for the preparation of therapeutically valuable GalNAc oligonucleotide conjugates.

Claim (Index 1):
Process for the preparation of GalNAc acid derivatives of the formula I wherein n is an integer between 0 and 10 and its salts, corresponding enantiomers and/or optical isomers thereof, comprising a) the coupling of a triamine salt of formula II wherein R 1  is an ester protecting group and X is an anion of an acid with a tetrahydropyran acid of formula III wherein R 2  is a hydroxy protecting group and n is as above in the presence of a peptide coupling agent, an amine base and an organic solvent to form the GalNAc ester of formula IV wherein R 1  and R 2  and n are as above; b) the removal of the ester protecting group R 1  and of the hydroxy protecting groups R 2  in the presence of a mineral base to form the GalNAc acid salt of formula V wherein n is as above and M is a metal kation; and c) optionally to transform GalNAc acid salt of formula V into the GalNAc acid derivative of formula I.

Metadata:
- Claim Count in Document: 13.0
- Percentile: 88.0
- Lexical Diversity: 1.33333
- Patent Class: 536.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['10542176', '15534676', '13810062', '14354478', '12341281']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.6018437461177611
- 35 USC 102 Novelty (BERT): 0.507297657032825
- Combined Prediction Score: 0.5923891372092676
- Mean Citation Score: 249.75634800000003
- Max Citation Score: 267.39838
- Similarity Product: 166.8399849734056

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