PATENT CLAIM ANALYSIS

Application Number: 15747290
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-08
Patent Classification: ["514", "210200"]

Abstract:
The present disclosure features compounds such as those having the Formulae (I) and (II), which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound, such as a compound of Formula (I) or (II).

Claim (Index 1):
A method of treating cystic fibrosis in a patient in need thereof, comprising administering a pharmaceutically effective amount of a compound represented by formula I and II: and pharmaceutically acceptable salts, stereoisomers, and prodrugs thereof, wherein:\n X 1  is CR 33  or N; \n X 3  is selected from the group consisting of O, S, and NR hh ; \n pp is 1, 2, or 3; \n R 11  is independently selected for each occurrence from the group consisting of hydrogen, halogen, and C 1-4  alkyl (optionally substituted by one, two or three halogens); \n R 31  is selected from the group consisting of hydrogen, halogen, and C 1-4  alkyl; \n R 33  is selected from the group consisting of H, halogen, C 1-4  alkyl, and \u2014NR\u2032R\u2033 wherein R\u2032 and R\u2033 are each independently selected for each occurrence from H and C 1-4  alkyl or taken together with the nitrogen to which they are attached form a heterocyclic ring; \n L 1  is selected from the group consisting of C 1-6  alkylene, C 3-6  cycloalkylene, C 3-6  cycloalkylene-C 1-4  alkylene, C 1-3  alkylene-NR hh \u2014S(O) w \u2014, \u2014C 1-3  alkylene-S(O) w \u2014NR hh \u2014, C 3-6  cycloalkylene-C 0-2  alkylene-S(O) w \u2014NR hh , and C 3-6  cycloalkylene-C 0-2  alkylene NR hh \u2014S(O) w \u2014, wherein L 1  may be optionally substituted by one, two or three substituents selected from the group consisting of halogen, hydroxyl, and C 1-3  alkyl (optionally substituted by one, two or three substituents each selected independently from R ff ); \n R 44  is selected from the group consisting of H, halogen, hydroxyl, C 1-3  alkoxy, phenyl, \u2014O-phenyl, \u2014NR\u2032-phenyl, heterocycle, and a 5-6 membered monocyclic or 8-10 membered bicyclic heteroaryl having one, two or three heteroatoms each selected from O, N, and S; wherein phenyl, \u2014O-phenyl, \u2014NR\u2032-phenyl, heterocycle and heteroaryl may be optionally substituted by one or two substituents each selected independently from R gg ; \n R ff  is selected for each occurrence from group consisting of halogen, hydroxyl, C 1-4  alkyl, C 1-4  alkyoxy, C 2-4  alkenyl, C 3-6  cycloalkyl, \u2014NR\u2032R\u2033, \u2014NR\u2032\u2014S(O) w \u2014C 1-3  alkyl, S(O) w \u2014NR\u2032R\u2033, and \u2014S(O) w \u2014C 1-3  alkyl, where w is 0, 1, or 2, wherein C 1-4  alkyl, C 1-4  alkyoxy, C 2-4  alkenyl and C 3-6  cycloalkyl may be optionally substituted by one, two or three substituents each independently selected from the group consisting of halogen, hydroxyl, \u2014NR\u2032R\u2033, \u2014NR\u2032\u2014S(O) w \u2014C 1-3  alkyl, S(O) w \u2014NR\u2032R\u2033, and \u2014S(O) w \u2014C 1-3  alkyl; \n R gg  is selected for each occurrence from the group consisting of halogen, hydroxyl, cyano, \u2014NR\u2032R\u2033, \u2014NR\u2032\u2014S(O) w \u2014C 1-3  alkyl, \u2014S(O) w \u2014NR\u2032R\u2033, and \u2014S(O) w \u2014C 1-3  alkyl, where w is 0, 1, or 2; heterocycle, C 1-6  alkyl, C 3-6  cycloalkyl, and C 1-6  alkenyl, wherein C 1-6  alkyl, C 3-6  cycloalkyl, and C 1-6  alkenyl are optionally substituted by one, two, or three substituents each independently selected from R jj ; and heterocycle is optionally substituted by one, two, or three substituents each independently selected from R ll ; \n R jj  is selected for each occurrence from the group consisting of halogen, hydroxyl, C 1-6  alkoxy (optionally substituted by one, two, or three substituents each independently selected from R kk ); C 3-6  cycloalkyl, C 3-6  cycloalkoxy, heterocycle, C(O)OH, \u2014C(O)OC 1-6  alkyl, \u2014NR\u2032R\u2033, \u2014NR\u2033\u2014S(O) w \u2014C 1-3  alkyl, \u2014S(O) w \u2014NR\u2032R\u2033, and \u2014S(O) w \u2014C 1-3  alkyl, where w is 0, 1, or 2; \n R kk  is selected for each occurrence from the group consisting of halogen, hydroxyl, C 1-6  alkyl (optionally substituted by one, two, or three substituents each independently selected from halogen, hydroxyl, C 3-6  cycloalkyl, and heterocycle (optionally substituted by C 1-6  alkyl)), C 3-6  cycloalkyl (optionally substituted by one, two, or three substituents each independently selected from halogen, hydroxyl, and C 1-6  alkyl), phenyl, heterocycle (optionally substituted by one, two or three substituents independently selected from halogen, hydroxyl, and C 1-6  alkyl), and heteroaryl; \n R ll is selected for each occurrence from the group consisting of halogen, hydroxyl, C 1-6  alkyl (optionally substituted by one, two, or three substituents each independently selected from halogen, hydroxyl, and C 3-6  cycloalkyl) and heterocycle (optionally substituted by one, two or three substituents independently selected from halogen, hydroxyl, and C 1-6  alkyl); \n R\u2032 and R\u2033 are each independently selected for each occurrence from H, C 1-4  alkyl, phenyl and heterocycle; \n w is 0, 1 or 2; \n R hh , is selected for each occurrence from the group consisting of H, C 1-6  alkyl and C 3-6  cycloalkyl; and \n optionally administering to said patient a) CFTR potentiator and/or b) a CFTR corrector.

Metadata:
- Claim Count in Document: 167.0
- Percentile: 86.0
- Lexical Diversity: 1.63158
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15539392', '15320172', '15539405', '15766667', '15539397']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8058075430557424
- 35 USC 102 Novelty (BERT): 0.5583344574327498
- Combined Prediction Score: 0.7810602344934432
- Mean Citation Score: 418.138532
- Max Citation Score: 446.75592
- Similarity Product: 358.1242229252244

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

Dataset: test