PATENT CLAIM ANALYSIS

Application Number: 15915415
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-07
Patent Classification: ["548", "400000"]

Abstract:
The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein A, R 4 , and R 5  are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.

Claim (Index 83):
The method of  claim 55 , wherein said compound having Formula I is a compound selected from the group consisting of:\n N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-2,3-dihydro-1H-benzo[c][1,2]azaborole-6-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-3-methyl-1H-benzo[c][1,5,2]oxazaborinine-6-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-1H-benzo[c][1,5,2]oxazaborinine-6-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-2-phenyl-3-thioxo-1,2,3,4-tetrahydrobenzo[c][1,5,2]diazaborinine-6-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-3-oxo-2-(p-tolyl)-1,2,3,4-tetrahydrobenzo[c][1,5,2]diazaborinine-6-carbohydrazide; N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-3-(trifluoromethyl)-1H-benzo[c][1,5,2]oxazaborinine-6-carbohydrazide; (4-(2-(tert-butyl)-2-(3,5-dimethylbenzoyl)hydrazine-1-carbonyl)-2-(phenylsulfonamido)phenyl)boronic acid; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-1,3-dihydrobenzo[c][1,2]oxaborole-6-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methyl benzoyl)-2,3-dihydro-1H-benzo[c][1,2]azaborole-6-carbohydrazide; (5-(2-(tert-butyl)-2-(3,5-dimethylbenzoyl)hydrazine-1-carbonyl)-2-((methylamino)methyl)phenyl)boronic acid; (5-(2-(tert-butyl)-2-(3,5-dimethylbenzoyl)hydrazine-1-carbonyl)-2-((dimethylamino)methyl)phenyl)boronic acid; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-3-methyl-1H-benzo[c][1,5,2]oxazaborinine-6-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-1H-benzo[c][1,5,2]oxazaborinine-6-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-2-phenyl-3-thioxo-1,2,3,4-tetrahydrobenzo[c][1,5,2]diazaborinine-6-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-3-oxo-2-phenyl-1,2,3,4-tetrahydrobenzo[c][1,5,2]diazaborinine-6-carbohydrazide; (4-(1-(tert-butyl)-2-(3-methoxy-2-methylbenzoyl)hydrazine-1-carbonyl)-2-(phenylsulfonamido)phenyl)boronic acid; (4-(2-(tert-butyl)-2-(3,5-dimethylbenzoyl)hydrazine-1-carbonyl)-2-((cyanomethyl)amino)phenyl)boronic acid; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-1,2,3,4-tetrahydrobenzo[c][1,2]azaborinine-7-carbohydrazide; (5-(2-(tert-butyl)-2-(3,5-dimethylbenzoyl)hydrazine-1-carbonyl)-2-(cyanomethyl)phenyl)boronic acid; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-1H-benzo[d][1,2,6]oxazaborinine-7-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; (5-(2-(tert-butyl)-2-(3,5-dimethylbenzoyl)hydrazine-1-carbonyl)-2-formylphenyl)boronic acid; N-(tert-butyl)-1-hydroxy-2-isopropyl-3-(isopropylamino)-N\u2032-(3-methoxy-2-methylbenzoyl)-1,2-dihydrobenzo[c][1,5,2]diazaborinine-6-carbohydrazide; N\u2032-(3-amino-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoyl)-N\u2032-(tert-butyl)-3-methoxy-2-methylbenzohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-2-isopropyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-2-methyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; 1,1\u2032-oxybis(N\u2032-(tert-butyl)-N\u2032-(3,5-dimethyl benzoyl)-2-(pyridin-2-yl)-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide); N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-2-phenyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; (R)\u2014N\u2032-(3,5-dimethylbenzoyl)-N\u2032-(2,2-dimethylpentan-3-yl)-1-hydroxy-3-oxo-2-phenyl-1,2,3,4-tetrahydrobenzo[c][1,5,2]diazaborinine-6-carbohydrazide; (R)\u2014N\u2032-(3,5-dimethylbenzoyl)-N\u2032-(2,2-dimethyl pentan-3-yl)-5-hydroxy-3-oxo-4-phenyl-1,3,4,5-tetrahydrobenzo[c][1,2,6,5]oxadiazaborepine-8-carbohydrazide; (4-(2-(tert-butyl)-2-(3,5-dimethylbenzoyl)hydrazine-1-carbonyl)-2-formylphenyl)boronic acid; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-1H-benzo[d][1,2,6]oxazaborinine-6-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1H-hydroxy-1,2-dihydrobenzo[d][1,2,3]diazaborinine-6-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-2-methyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; N-(tert-butyl)-1-hydroxy-2-isopropyl-N\u2032-(3-methoxy-2-methylbenzoyl)-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; (5-(1-(tert-butyl)-2-(3-methoxy-2-methylbenzoyl)hydrazine-1-carbonyl)-2-formylphenyl)boronic acid; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-2-methyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-6-carbohydrazide; (4-(1-(tert-butyl)-2-(3-methoxy-2-methylbenzoyl)hydrazine-1-carbonyl)-2-formylphenyl)boronic acid; N\u2032-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-1H-benzo[d][1,2,6]oxazaborinine-6-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-1,2-dihydrobenzo[d][1,2,3]diazaborinine-6-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-2-methyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-6-carbohydrazide; N\u2032-(tert-butyl)-3-cyano-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborole-6-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-2-(methylsulfonyl)-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-2-tosyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-2-(methylsulfonyl)-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-2-tosyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-2-phenyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; N-(tert-butyl)-3-cyano-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-1,3-dihydrobenzo[c][1,2]oxaborole-6-carbohydrazide; (R)\u2014N\u2032-(3,5-dimethylbenzoyl)-N\u2032-(2,2-dimethylpentan-3-yl)-1-hydroxy-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; (R)\u2014N\u2032-(3,5-dimethylbenzoyl)-N\u2032-(2,2-dimethylpentan-3-yl)-1-hydroxy-2-methyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; (R)\u2014N\u2032-(3,5-dimethylbenzoyl)-N\u2032-(2,2-dimethylpentan-3-yl)-1-hydroxy-2-(methylsulfonyl)-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; (R)\u2014N\u2032-(3,5-dimethylbenzoyl)-N\u2032-(2,2-dimethylpentan-3-yl)-1-hydroxy-2-tosyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; (R)-(5-(2-(3,5-dimethylbenzoyl)-2-(2,2-dimethylpentan-3-yl)hydrazine-1-carbonyl)-2-formylphenyl)boronic acid; (R)\u2014N-(2,2-di methylpentan-3-yl)-1-hydroxy-N\u2032-(3-methoxy-2-methyl benzoyl)-1H-benzo[d][1,2,6]oxazaborinine-7-carbohydrazide; (R)\u2014N-(2,2-dimethylpentan-3-yl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; (R)\u2014N-(2,2-dimethylpentan-3-yl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-2-methyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; (R)-(5-(1-(2,2-dimethylpentan-3-yl)-2-(3-methoxy-2-methylbenzoyl)hydrazine-1-carbonyl)-2-formylphenyl)boronic acid; 2-acetyl-N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-1,2-dihydrobenzo[d][1,2,3]diazaborinine-6-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-2-phenyl-1,2-dihydrobenzo[d][1,2,3]diazaborinine-6-carbohydrazide; N\u2032-(tert-butyl)-N\u2032-(3,5-dimethylbenzoyl)-1-hydroxy-2-(methylsulfonyl)-1,2-dihydrobenzo[d][1,2,3]diazaborinine-6-carbohydrazide; (R)\u2014N\u2032-(3,5-dimethyl benzoyl)-N\u2032-(2,2-dimethylpentan-3-yl)-1-hydroxy-1,3,4,5-tetrahydrobenzo[c][1,5,2]oxazaborepine-7-carbohydrazide; (R)\u2014N\u2032-(3,5-dimethylbenzoyl)-N\u2032-(2,2-dimethylpentan-3-yl)-1-hydroxy-2-phenyl-3-thioxo-1,2,3,4-tetrahydrobenzo[c][1,5,2]diazaborinine-6-carbohydrazide; (R)\u2014N-(2,2-dimethylpentan-3-yl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-2-(methylsulfonyl)-1,2-dihydrobenzo[d][1,2,3]diazaborinine-7-carbohydrazide; (R)\u2014N-(2,2-dimethylpentan-3-yl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-1H-benzo[d][1,2,6]oxazaborinine-7-carbohydrazide; (4-(1-(tert-butyl)-2-(5-methoxy-4-methylnicotinoyl)hydrazine-1H-carbonyl)-3-fluorophenyl)boronic acid; (R)-(4-(2-(3,5-dimethylbenzoyl)-2-(2,2-dimethylpentan-3-yl)hydrazine-1-carbonyl)-2-formylphenyl)boronic acid; (R)\u2014N\u2032-(3,5-dimethylbenzoyl)-N\u2032-(2,2-dimethylpentan-3-yl)-1-hydroxy-1H-benzo[d][1,2,6]oxazaborinine-6-carbohydrazide; (R)\u2014N\u2032-(3,5-dimethylbenzoyl)-N\u2032-(2,2-dimethylpentan-3-yl)-1-hydroxy-1,2-dihydrobenzo[d][1,2,3]diazaborinine-6-carbohydrazide; (R)\u2014N\u2032-(3,5-dimethylbenzoyl)-N\u2032-(2,2-dimethylpentan-3-yl)-1-hydroxy-1H-benzo[d][1,2,6]oxazaborinine-7-carbohydrazide; N-(tert-butyl)-1-hydroxy-N\u2032-(3-methoxy-2-methylbenzoyl)-1H-benzo[d][1,2,6]oxazaborinine-7-carbohydrazide; and R)\u2014N\u2032-(3,5-dimethylbenzoyl)-3-hydroxy-N\u2032-(2,2,3-trimethylpentan-3-yl)-1,3-dihydrobenzo[c][1,2,5]oxazaborole-6-carbohydrazide, or a pharmaceutically acceptable salt, solvate, or boronic anhydride thereof.

Metadata:
- Claim Count in Document: 65.0
- Percentile: 90.0
- Lexical Diversity: 1.57971
- Patent Class: 548.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14855646', '14805837', '15354239', '14212526', '10775883']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8056092761232427
- 35 USC 102 Novelty (BERT): 0.6855282754407248
- Combined Prediction Score: 0.7936011760549909
- Mean Citation Score: 527.6125400000002
- Max Citation Score: 798.55835
- Similarity Product: 663.7169614943683

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