PATENT CLAIM ANALYSIS

Application Number: 16181230
Application Type: Utility
Filing Date: 2018-11
Publication Date: 2019-08
Patent Classification: ["536", "017400"]

Abstract:
The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Claim (Index 2):
A method of preparing a compound of Formula (I): or a salt thereof, the method comprising a step of reacting a compound of the formula: or a salt thereof, with a compound of the formula: HNR 3 R 4 , or a salt thereof, wherein:\n X is hydrogen, halogen, trifluoromethyl, lower alkyl, unsubstituted or substituted phenyl, lower alkyl-thio, phenyl-lower alkyl-thio, lower alkyl-sulfonyl, or phenyl-lower alkyl-sulfonyl; \n Y is hydrogen, hydroxyl, mercapto, lower alkoxy, lower alkyl-thio, halogen, lower alkyl, unsubstituted or substituted mononuclear aryl, or \u2014N(R 2 ) 2 ; \n R 1  is hydrogen or lower alkyl; \n each R 2  is independently \u2014R 7 , \u2014(CH 2 ) m \u2014OR 8 , \u2014(CH 2 ) m \u2014NR 7 R 10 , \u2014(CH 2 ) n (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014(CH 2 CH 2 O) m \u2014R 8 , \u2014(CH 2 CH 2 O) m \u2014CH 2 CH 2 NR 7 R 10 , \u2014(CH 2 ) n \u2014C(\u2550O)NR 7 R 10 , \u2014(CH 2 ) n \u2014(Z) g -R 7 , \u2014(CH 2 ) m NR 10 -CH 2 (CHOR 8 )(CHOR 8 ) n CH 2 OR 8 , \u2014(CH 2 ) n CO 2 R 7 , or \n R 3  and R 4  are each independently hydrogen, a group represented by Formula (A), lower alkyl, hydroxyl lower alkyl, phenyl, phenyl-lower alkyl, (halophenyl)-lower alkyl, lower-(alkylphenylalkyl), lower (alkoxyphenyl)-lower alkyl, naphthyl-lower alkyl, or pyridyl-lower alkyl, with the proviso that at least one of R 3  and R 4  is a group represented by Formula (A): and wherein:\n each R L  is independently \u2014R 7 , \u2014(CH 2 ) n \u2014OR 8 , \u2014O\u2014(CH 2 ) m \u2014OR 8 , \u2014(CH 2 ) n \u2014NR 7 R 10 , \u2014O\u2014(CH 2 ) m \u2014NR 7 R 10 , \u2014(CH 2 ) n (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014O\u2014(CH 2 ) m (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014(CH 2 CH 2 O) m \u2014R 8 , \u2014O\u2014(CH 2 CH 2 O) m \u2014R 8 , \u2014(CH 2 CH 2 O) m \u2014CH 2 CH 2 NR 7 R 10 , \u2014O\u2014(CH 2 CH 2 O) m \u2014CH 2 CH 2 NR 7 R 10 , \u2014(CH 2 ) n \u2014C(\u2550O)NR 7 R 10 , \u2014O\u2014(CH 2 ) m \u2014C(\u2550O)NR 7 R 10 , \u2014(CH 2 ) n \u2014(Z) g \u2014R 7 , \u2014O\u2014(CH 2 ) m \u2014(Z) g \u2014R 7 , \u2014(CH 2 ) n \u2014NR 10 -CH 2 (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014O\u2014(CH 2 ) m \u2014NR 10 -CH 2 (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014(CH 2 ) n \u2014CO 2 R 7 , \u2014O\u2014(CH 2 ) m \u2014CO 2 R 7 , \u2014OSO 3 H, \u2014O-glucuronide, \u2014O-glucose, \n each o is independently an integer from 0 to 10; each p is an integer from 0 to 10; with the proviso that the sum of o and p in each contiguous chain is from 1 to 10; each x is independently O, NR 10 , C(\u2550O), CHOH, C(\u2550N\u2014R 10 ), CHNR 7 R 10 , or a single bond; each R 5  is independently \u2014(CH 2 ) m \u2014OR 8 , \u2014O\u2014(CH 2 ) m \u2014OR 8 , \u2014(CH 2 ) n \u2014NR 7 R 10 , \u2014O\u2014(CH 2 ) m \u2014NR 7 R 10 , \u2014(CH 2 ) n (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014O\u2014(CH 2 ) m (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014(CH 2 CH 2 O) m \u2014R 8 , \u2014O\u2014(CH 2 CH 2 O) m \u2014R 8 , \u2014(CH 2 CH 2 O) m \u2014CH 2 CH 2 NR 7 R 10 , \u2014O\u2014(CH 2 CH 2 O) m \u2014CH 2 CH 2 NR 7 R 10 , \u2014(CH 2 ) n \u2014C(\u2550O)NR 7 R 10 , \u2014O\u2014(CH 2 ) m \u2014C(\u2550O)NR 7 R 10 , \u2014(CH 2 ) n \u2014(Z) g -R 7 , \u2014O\u2014(CH 2 ) m \u2014(Z) g -R 7 , \u2014(CH 2 ) n \u2014NR 10 -CH 2 (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014O\u2014(CH 2 ) m \u2014NR 10 -CH 2 (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014(CH 2 ) n \u2014CO 2 R 7 , \u2014O\u2014(CH 2 ) m \u2014CO 2 R 7 , \u2014OSO 3 H, \u2014O-glucuronide, \u2014O-glucose, each R 6  is independently \u2014R 7 , \u2014OR 11 , \u2014N(R 7 ) 2 , \u2014(CH 2 ) m \u2014OR 8 , \u2014O\u2014(CH 2 ) m \u2014OR 8 , \u2014(CH 2 ) n \u2014NR 7 R 10 , \u2014O\u2014(CH 2 ) m \u2014NR 7 R 10 , \u2014(CH 2 ) n (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014O\u2014(CH 2 ) m (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014(CH 2 CH 2 O) m \u2014R 8 , \u2014O\u2014(CH 2 CH 2 O) m -R 8 , \u2014(CH 2 CH 2 O) m \u2014CH 2 CH 2 NR 7 R 10 , \u2014O\u2014(CH 2 CH 20 ) m \u2014CH 2 CH 2 NR 7 R 10 , \u2014(CH 2 ) n \u2014C(\u2550O)NR 7 R 10 , \u2014O\u2014(CH 2 ) m \u2014C(\u2550O)NR 7 R 10 , \u2014(CH 2 ) n \u2014(Z) g -R 7 , \u2014O\u2014(CH 2 ) m \u2014(Z) g -R 7 , \u2014(CH 2 ) n \u2014NR 10 -CH 2 (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014O\u2014(CH 2 ) m \u2014NR 10 -CH 2 (CHOR 8 )(CHOR 8 ) n \u2014CH 2 OR 8 , \u2014(CH 2 ) n \u2014CO 2 R 7 , \u2014O\u2014(CH 2 ) m \u2014CO 2 R 7 , \u2014OSO 3 H, \u2014O-glucuronide, \u2014O-glucose, wherein when two R 6  are \u2014OR 11  and are located adjacent to ech other on a phenyl ring, the alkyl moieties of the two R 6  may be bonded together to form a methylenedioxy group; each R 7  is independently hydrogen or lower alkyl; each R 8  is independently hydrogen, lower alkyl, \u2014C(\u2550O)-R 11 , glucuronide, 2-tetrahydropyranyl, or each R 9  is independently \u2014CO 2 R 7 , \u2014CON(R 7 ) 2 , \u2014SO 2 CH 3 , or C(\u2550O)R 7 ; each R 10  is independently \u2014H, \u2014SO 2 CH 3 , \u2014CO 2 R 7 , \u2014C(\u2550O)NR 7 R 9 , \u2014C(\u2550O)R 7 , or CH 2 \u2014(CHOH) n CH 2 OH; each Z is independently CHOH, C(\u2550O), CHNR 7 R 10 , C\u2550NR 10 , or NR 10 ; each R 11  is independently lower alkyl; each g is independently an integer from 1 to 6; each m is independently an integer from 1 to 7; each n is independently an integer from 0 to 7; and each Q is independently C\u2014R 5  or C\u2014R 6 , wherein one Q is C\u2014R 5 .

Metadata:
- Claim Count in Document: 57.0
- Percentile: 98.0
- Lexical Diversity: 1.42105
- Patent Class: 536.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15336574', '10828352', '10828171', '10828479', '12703441']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7310109530936832
- 35 USC 102 Novelty (BERT): 0.5690638679538779
- Combined Prediction Score: 0.7148162445797028
- Mean Citation Score: 510.86763600000006
- Max Citation Score: 521.1096
- Similarity Product: 384.0685783086777

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