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 1):
A compound of formula (I) wherein R 1  is selected from the group consisting of \u2014C 1-4 alkyl, hydroxy substituted C 1-4 alkyl, \u2014CH 2 \u2014R 10 , C 3-6 cycloalkyl, hydroxy substituted C 3-6 cycloalkyl, \u2014C(O)OH and \u2014C(O)O\u2014(C 1-4 alkyl); wherein R 10  is selected from the group consisting of fluoro, C 1-2 alkoxy, cyano and NR A R B ; wherein R A  and R B  are each independently selected from the group consisting of hydrogen and C 1-2 alkyl; R 2  is selected from the group consisting of hydrogen, halogen, hydroxy, C 1-4 alkyl, \u2014(C 1-4 alkyl)-OH, C 1-4 alkoxy, cyano substituted C 1-4 alkoxy, C 2-4 alkenyl, C 2-4 alkenyl-oxy, benzyloxy and carboxy; R 3  is selected from the group consisting of hydrogen, halogen, C 1-4 alkyl and C 2-4 alkenyl; R 4  is selected from the group consisting of hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, fluorinated C 1-2 alkyl, C 1-4 alkoxy, fluorinated C 1-2 alkoxy, cyano substituted C 1-4 alkoxy, and C 3-6 cycloalkyl; alternatively, R 2  and R 3  or R 3  and R 4  are taken together with the carbon atoms to which they are bound to form a ring structure selected from the group consisting of 2,3-dihydro-furanyl and 3,4-dihydro-2H-pyranyl; wherein the 2,3-dihyfro-furanyl or 3,4-dihydro-2H-pyranyl is optionally substituted with one or more substituents independently selected from the group consisting of hydroxy, methyl, ethyl, hydroxy-methyl- and hydroxyethyl-; R 5  and R 6  are the same and are hydrogen;  is selected from the group consisting of C 5-12 cycloalkyl, C 5-12 cycloalkenyl, phenyl, heteroaryl and heterocyclyl; wherein the phenyl, heteroaryl or heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, hydroxy, oxo (i.e. \u2550O), C 1-4 alkyl, C 1-4 alkoxy, fluorinated C 1-2 alkyl, fluorinated C 1-2 alkoxy, cyano, 2,5-dimethyl-thien-3-yl, 5-methyl-thiazol-2-yl and \u2014C(O)\u2014R 11 ; wherein R 11  is selected from the group consisting of C 1-4 alkyl, C 1-4 alkoxy, C 3-6 cycloalkyl, azetidin-1-yl, pyrrolidin-1-yl, piperidin-1-yl, piperazin-1-yl, morpholin-4-yl, thiomorpholin-4-yl and thiazol-2-yl; provided that when   is bicyclo[4.2.0]octa-1 (6),2,4-trien-3-yl or bicyclo[4.2.0]octan-3-yl, then R 2  and R 3  or R 3  and R 4  are taken together with the carbon atoms to which they are bound to form a ring structure selected from the group consisting of 4,5-dihydro-furanyl and tetrahydropyranyl; wherein 4,5-dihyfro-furanyl or tetrahydropyranyl is optionally substituted with one or more substituents independently selected from the group consisting of hydroxy, methyl, ethyl, hydroxy-methyl- and hydroxyethyl-; provided further that when   is phenyl, wherein the phenyl is optionally substituted, then R 2  and R 3  or R 3  and R 4  are taken together with the carbon atoms to which they are bound to form a ring structure selected from the group consisting of 2,3-dihydro-furanyl and 3,4-dihydro-2H-pyranyl provided further that when   is thienyl or pyridyl, then R 2  and R 3  or R 3  and R 4  are taken together with the carbon atoms to which they are bound to form a ring structure selected from the group consisting of 2,3-dihydro-furanyl and 3,4-dihydro-2H-pyranyl; provided further that when R 1  is \u2014CH 2 OH, R 2  is H, R 3  is H, R 4  is H or Cl, R 5  is H and R 6  is H, then   is other than benzothien-2-yl; or an isotopologue or pharmaceutically acceptable salt thereof.

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

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8365186248688304
- 35 USC 102 Novelty (BERT): 0.5294301590732059
- Combined Prediction Score: 0.8058097782892679
- Mean Citation Score: 351.143048
- Max Citation Score: 357.37866
- Similarity Product: 230.632564152124

Labels:
- Claim Label 101: 1
- Claim Label 102: 0
- Claim Label 103: 0
- Claim Label 112: 1
- Combined Label: 0
- Label 101 Adjusted: 1

Dataset: test