PATENT CLAIM ANALYSIS

Application Number: 16106104
Application Type: Utility
Filing Date: 2018-08
Publication Date: 2019-02
Patent Classification: ["514", "301000"]

Abstract:
The present invention is directed to 5-fluoro-C-(aryl or hetercyclyl)-glycoside derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity.

Claim (Index 23):
A process for the preparation of a compound of formula (V-S) wherein A 1 , A 2  and A 3  are each an independently selected from the group consisting of C 1-8 alkyl, C 3-6 cycloalkyl, bicyclo[2.2.1]heptan-2-yl, phenyl and 3,5-di(trifluoromethyl)phenyl; comprising reacting (2S,3R,4S,5R,6R)-2-(allyloxy)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, with an acylating agent; in the presence of an inorganic or organic base; neat, when in the presence of an organic base or when in the presence of an inorganic base, in an organic solvent; at a temperature in the range of from about \u221250\u00b0 C. to about room temperature; to yield the corresponding compound of formula (A-1), wherein W is the corresponding acyl group, preferably \u2014C(O)-methyl, \u2014C(O)-ethyl, \u2014C(O)-benzyl, more preferably \u2014C(O)-benzyl (benzoyl); reacting the compound of formula (A-1) with a fluorinating agent; in an organic solvent or mixture of organic solvents; at a temperature in the range of from about \u221250\u00b0 C. to about room temperature; to yield the corresponding compound of formula (A-2); de-protecting the compound of formula (A-2) to yield (2S,3R,4R,5S,6R)-2-(allyloxy)-5-fluoro-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4-diol; reacting (2S,3R,4R,5S,6R)-2-(allyloxy)-5-fluoro-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4-diol with a trialkyl silyl reagent; in the presence of an organic base; in an organic solvent or mixture of organic solvents; at a temperature in the range of from about 0\u00b0 C. to about 50\u00b0 C.; to yield the corresponding compound of formula (A-3) wherein A 1 , A 2  and A 3  are the corresponding alkyl groups; reacting the compound of formula (A-3) with allyl isomerization catalyst in an organic solvent or mixture of water and a water miscible organic solvent; at a temperature of in the range of from about 75\u00b0 C. to about 105\u00b0 C.; to yield the corresponding compound of formula (A-4), wherein the compound of formula (A-4) is not isolated; reacting the compound of formula (A-4) with an co-oxidant; in the presence of an oxidizing reagent; in an organic solvent or mixture of water and a water miscible organic solvent; at a temperature in the range of from about 0\u00b0 C. to about 50\u00b0 C.; to yield the corresponding compound o formula (A-5); reacting the compound of formula (A-5) under SWERN oxidation conditions; to yield the corresponding compound of formula (V-S).

Metadata:
- Claim Count in Document: 47.0
- Percentile: 96.0
- Lexical Diversity: 1.08108
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14593071', '16059072', '16059074', '13634597', '14122836']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7969206175595319
- 35 USC 102 Novelty (BERT): 0.5291865358768993
- Combined Prediction Score: 0.7701472093912687
- Mean Citation Score: 351.143048
- Max Citation Score: 357.37866
- Similarity Product: 255.85924898681404

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