PATENT CLAIM ANALYSIS

Application Number: 15914189
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-09
Patent Classification: ["514", "265100"]

Abstract:
The invention relates to glucuronide prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula I: where A 1  and R 1  are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.

Claim (Index 52):
A compound of formula 2 or formula 5: wherein P 1  is a carboxy-protecting group; each P 2  is independently a hydroxyl-protecting group; L 2  is an acyl leaving group; R 1  is hydrogen or C 1-3  alkyl; A 1  is selected from: (a) a group having formula (i):\n \u2014[CH 2 ] a \u2014N(R 2 )C(O)\u2014\u2003\u2003(i) \n wherein a is 2 or 3; and R 2  is hydrogen or C 1-3  alkyl; (b) a group having formula (ii): wherein b is 0 or 1; c is 0 or 1; R 3  is hydrogen or C 1-3  alkyl; and B 1  is selected from C 6-10  aryl, C 1-9  heteroaryl, C 3-10  cycloalkyl and C 2-9  heterocyclic; wherein the heteroaryl group contains from 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur; the aryl or heteroaryl group is unsubstituted or substituted with 1 to 3 substituents independently selected from C 1-4  alkyl, C 1-3  alkoxy, amino, cyano, halo, hydroxy, nitro and trifluoromethyl; the heterocyclic group contains from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur; and the cycloalkyl or heterocyclic group is unsubstituted or substituted with 1 to 4 substituents independently selected from C 1-4  alkyl, C 1-3  alkoxy, hydroxy, and trifluoromethyl; and (c) a group having formula (iii): wherein d is 2 or 3; e is 0 or 1; R 4  is hydrogen or C 1-3  alkyl; and B 2  is selected from C 6-10  aryl, C 1-9  heteroaryl, C 3-10  cycloalkyl and C 2-9  heterocyclic; wherein the heteroaryl group contains from 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur; the aryl or heteroaryl group is unsubstituted or substituted with 1 to 3 substituents independently selected from C 1-4  alkyl, C 1-3  alkoxy, amino, cyano, halo, hydroxy, nitro and trifluoromethyl; the heterocyclic group contains from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur; and the cycloalkyl or heterocyclic group is unsubstituted or substituted with 1 to 4 substituents independently selected from C 1-4  alkyl, C 1-3  alkoxy, hydroxy, and trifluoromethyl; or a salt thereof.

Metadata:
- Claim Count in Document: 73.0
- Percentile: 90.0
- Lexical Diversity: 1.35556
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15358462', '12503384', '13379301', '15799771', '14082786']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7948452160187068
- 35 USC 102 Novelty (BERT): 0.5455524890728677
- Combined Prediction Score: 0.7699159433241229
- Mean Citation Score: 336.024834
- Max Citation Score: 403.78525
- Similarity Product: 296.32437705774606

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