PATENT CLAIM ANALYSIS

Application Number: 16095822
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-06
Patent Classification: ["514", "210210"]

Abstract:
The present invention relates to a substituted purine derivative of formula (1) wherein R 1  is alkoxy or the like, R 2  is alkyl or the like, Ring Q 1  is aryl or the like, W 1  is alkylene or the like, Ring Q 2  is aromatic carbocyclyl or the like, n is 1-4, R 3  is hydrogen atom or the like, X 1  is single bond or the like, W 2  is alkylene or the like, and R 4  is hydrogen atom or the like, or a pharmaceutically acceptable salt thereof, which has a potent inhibitory effect against TLR7, and thereby is useful for treating autoimmune disease.

Claim (Index 28):
The compound of  claim 1  which is selected from the following compounds, or a pharmaceutically acceptable salt thereof:\n 1-(3-fluoro-4-{[8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purin-9-yl]methyl}phenyl)-N,N-dimethylmethanamine, \n 9-[4-(azetidin-1-ylmethyl)-2-fluorobenzyl]-8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purine, \n 9-(2-fluoro-4-{[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]methyl}benzyl)-8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purine, \n 9-[2-fluoro-4-(1-methylpiperidin-4-yl)benzyl]-8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purine, \n 9-[4-(1-ethylpiperidin-4-yl)-2-fluorobenzyl]-8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purine, \n 9-(2-fluoro-4-{[(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]oxy}benzyl)-8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purine, \n 9-(2-fluoro-4-{[(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]oxy}benzyl)-2-methoxy-6-methyl-8-(pyrimidin-5-yl)-9H-purine, \n 5-[9-(2-fluoro-4-{[(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]oxy}benzyl)-2-methoxy-6-methyl-9H-purin-8-yl]pyridine-3-carbonitrile, \n 5-[9-(4-{[(3-endo)-8-ethyl-8-azabicyclo[3.2.1]oct-3-yl]oxy}-2-fluorobenzyl)-2-methoxy-6-methyl-9H-purin-8-yl]pyridine-3-carbonitrile, \n 9-[4-(1-azabicyclo[2.2.2]oct-3-yl)-2-fluorobenzyl]-2-methoxy-6-methyl-8-(pyridin-3-yl)-9H-purine, \n 9-[4-(1-azabicyclo[2.2.2]oct-3-yl)-2-fluorobenzyl]-2-methoxy-6-methyl-8-(4-methylpyridin-3-yl)-9H-purine, \n 9-[4-(1-azabicyclo[2.2.2]oct-3-yl)-2-fluorobenzyl]-2-methoxy-6-methyl-8-(5-methylpyridin-3-yl)-9H-purine, \n 5-[9-(2-fluoro-4-{[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]methyl}benzyl)-2-methoxy-6-methyl-9H-purin-8-yl]pyridine-3-carbonitrile, \n 5-[9-(4-{[(1S,4S)-5-ethyl-2,5-diazabicyclo[2.2.1]hept-2-yl]methyl}-2-fluorobenzyl)-2-methoxy-6-methyl-9H-purin-8-yl]pyridine-3-carbonitrile, \n 9-(2-fluoro-4-{[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]methyl}benzyl)-2-methoxy-6-methyl-8-(pyridin-3-yl)-9H-purine, \n 5-[2-ethoxy-9-(2-fluoro-4-{[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]methyl}benzyl)-6-methyl-9H-purin-8-yl]pyridine-3-carbonitrile, \n 2-ethoxy-9-(2-fluoro-4-{[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]methyl}benzyl)-6-methyl-8-(pyrimidin-5-yl)-9H-purine, \n 2-ethoxy-9-(2-fluoro-4-{[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]methyl}benzyl)-8-(5-fluoropyridin-3-yl)-6-methyl-9H-purine, \n 5-(9-{4-[(3S)-1-azabicyclo[2.2.2]oct-3-yloxy]-2-fluorobenzyl}-2-methoxy-6-methyl-9H-purin-8-yl)pyridine-3-carbonitrile, \n 9-{[6-(1-azabicyclo[2.2.2]oct-3-yl)pyridin-3-yl]methyl}-2-ethoxy-8-(5-fluoropyridin-3-yl)-6-methyl-9H-purine, \n 9-[4-(1-azabicyclo[2.2.2]oct-3-yl)-2-fluorobenzyl]-8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purine, \n 5-{9-[4-(1-azabicyclo[2.2.2]oct-3-yl)-2-fluorobenzyl]-2-methoxy-6-methyl-9H-purin-8-yl}pyridine-3-carbonitrile, \n Example 412: 9-{4-[(3S)-1-azabicyclo[2.2.2]oct-3-yloxy]-2-fluorobenzyl}-8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purine, \n 9-{4-[(3R)-1-azabicyclo[2.2.2]oct-3-yloxy]-2-fluorobenzyl}-8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purine, \n 9-(2-fluoro-4-{[(3-exo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]oxy}benzyl)-8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purine, and \n 9-[5-(1-azabicyclo[2.2.2]oct-3-yl)-2-fluorobenzyl]-8-(5-fluoropyridin-3-yl)-2-methoxy-6-methyl-9H-purine.

Metadata:
- Claim Count in Document: 10.0
- Percentile: 97.0
- Lexical Diversity: 2.08475
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['13508905', '13819881', '13395429', '13380376', '11547036']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7900898133216743
- 35 USC 102 Novelty (BERT): 0.5437826765395146
- Combined Prediction Score: 0.7654590996434584
- Mean Citation Score: 368.977162
- Max Citation Score: 377.30194
- Similarity Product: 307.16532020520805

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

Dataset: test