PATENT CLAIM ANALYSIS

Application Number: 15768960
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-11
Patent Classification: ["514", "220000"]

Abstract:
The present invention relates to a benzodiazepine derivative of Formula I as a short-acting anesthetic, a pharmaceutical composition comprising the same, a kit comprising the same, a preparation method thereof, an method of anesthesia using the same and use thereof in the manufacture of an anesthetic medicament.

Claim (Index 7):
A compound selected from the group consisting of:\n methyl 3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)acrylate (compound 1), methyl 3-(8-bromo-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 2), methyl 3-(8-chloro-6-phenyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 3), methyl 3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 4), methyl 3-(8-bromo-1-cyclopropyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 5), methyl 3-(8-bromo-1-deuteromethyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 6), methyl 3-(8-chloro-6-(2-fluorophenyl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 7), methyl 3-(8-bromo-1-cyclopropyl-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 8), methyl 3-(8-bromo-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 9), methyl 3-(8-bromo-1-(methoxymethyl)-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 10), methyl 3-(8-bromo-1-deuteromethyl-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 11), methyl 3-(8-chloro-1-cyclopropyl-6-(2-fluorophenyl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 12), methyl 3-(8-bromo-1-ethenyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 13), methyl 3-(8-chloro-1-cyclopropyl-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 14), methyl 3-(8-bromo-1-ethyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 15), methyl 3-(8-bromo-1-(methoxymethyl)-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 16), methyl 3-(8-bromo-1-isopropyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 17), methyl 3-(8-chloro-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 18), methyl 3-(8-chloro-1-cyclopropyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 19), methyl 3-(8-bromo-1-cyclobutyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 20), methyl 3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)butyrate (compound 21), methyl 3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)-2-methylpropanoate (compound 22), methyl 3-(8-bromo-1-cyclopropyl-2-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 23), methyl 3-(8-bromo-1-(hydroxymethyl)-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 24), methyl 3-(8-chloro-6-(2-fluorophenyl)-1-(methoxymethyl)-4H-benzo[f][1,2,4]triazolo[4,3a][1,4]diazepin-4-yl)propanoate (compound 25), methyl 3-(8-chloro-6-(2-fluorophenyl)-1-(methoxymethyl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 26), methyl 3-(8-chloro-1-cyclobutyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 27), methyl 3-(8-chloro-1-ethyl-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 28), methyl 3-(8-chloro-1-isopropyl-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 29), ethyl 3-(8-chloro-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 30), methyl 3-(8-chloro-1-cyclopropyl-2-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 31), methyl 3-(8-chloro-1-(methoxymethyl)-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)propanoate (compound 32), methyl 3-(8-chloro-1-(methoxymethyl)-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 33), methyl 3-(8-chloro-6-(2-fluorophenyl)-1-cyclopropyl-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 34), methyl 3-(8-bromo-1-(difluoromethyl)-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 35), methyl 3-(8-bromo-6-(pyridin-2-yl)-1-(trifluoromethyl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 36), methyl 3-(8-bromo-1-((N,N-dimethylamino)methyl)-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 37), methyl 3-(8-bromo-1-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 38), methyl 3-((8-bromo-1-methoxy-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 39), methyl 3-(8-bromo-1-(2-(N,N-dimethylamino)ethyl)-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 40), methyl 3-(8-bromo-2-((N,N-dimethylamino)methyl)-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 41), methyl 3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-4-yl)propanoate (compound 42), methyl 3-(8-bromo-1-(1-methylcyclopropyl)-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 43), methyl 3-(8-bromo-1-(oxetan-3-yl)-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate (compound 44), methyl 3-(8-chloro-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)butyrate (compound 45), methyl 3-(8-bromo-24N,N-diethylamino)methyl)-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propionate (compound 46), and methyl 3-(8-chloro-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)-2-methylpropionate (compound 47), or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorph, solvate, metabolite or prodrug thereof; preferably, the compound is selected from the group consisting of:

Metadata:
- Claim Count in Document: 29.0
- Percentile: 91.0
- Lexical Diversity: 1.57576
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['12598882', '14858159', '14448160', '09927324', '15150038']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8354914338553039
- 35 USC 102 Novelty (BERT): 0.5328590360264769
- Combined Prediction Score: 0.8052281940724213
- Mean Citation Score: 356.00754
- Max Citation Score: 373.12048
- Similarity Product: 304.67882869045263

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

Dataset: test