PATENT CLAIM ANALYSIS

Application Number: 15782002
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2019-01
Patent Classification: ["549", "029000"]

Abstract:
The invention provides compounds that are inhibitors of bacterial RNA polymerase. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.

Claim (Index 1):
A compound selected from compounds of structural formulae (I)-(VI): and tautomers and salts thereof, wherein:\n R 2 , R 6 , and R 7  each independently is H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 1 -C 6 )alkoxy, which (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 1 -C 6 )alkoxy optionally is substituted with halo; \n R 1  is fluoromethyl, difluoromethyl, fluoroethyl, difluoroethyl, trifluoroethyl, fluoropropyl, difluoropropyl, trifluoropropyl, fluoromethoxy difluoromethoxy fluoroethoxy, difluoroethoxy, trifluoroethoxy, fluoropropoxy, difluoropropoxy, trifluoropropoxy, alkaryl, alkheteroaryl, aryloxy, heteroaryloxy, or benzyloxy, which alkaryl, alkheteroaryl, aryloxy, heteroarlyoxy, or benzyloxy is substituted by one or more of halo, fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, aryl, heteroaryl, aryloxy, and heteroaryloxy; and R 3 , R 4 , and R 5  each independently is H, halo, (C 1 -C 8 )alkyl, or (C 2 -C 8 )alkenyl, which (C 1 -C 8 )alkyl, or (C 2 -C 8 )alkenyl optionally is substituted with one or more of halo, oxo, hydroxy, carboxy, cyano, \u2014NR a R b , fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, (C 1 -C 7 )C(\u2550O)NH\u2014, aryl, heteroaryl, aryloxy, and heteroaryloxy; R a  and R b  each independently is H or (C 1 -C 6 )alkyl, or R a  and R b , together with the nitrogen to which they are attached, form a morpholino, piperazine, pyrrolidino, or piperidino; and at least one of R 3 , R 4 , and R 5  is other than H; or \n R 1  is (C 2 -C 8 )alkenyl, alkaryl, alkheteroaryl, aryloxy, heteroaryloxy, or benzyloxy, which (C 2 -C 8 )alkenyl, alkaryl, alkheteroaryl, aryloxy, heteroarlyoxy, or benzyloxy optionally is substituted by one or more of halo, fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, aryl, heteroaryl, aryloxy, or heteroaryloxy; and R 3 , R 4 , and R 5  each is H; \n X and Y are individually carbon, sulfur, oxygen, or nitrogen, wherein at least one of X and Y is other than carbon; \n R 2\u2032 , R 6\u2032 , and R 7\u2032  each independently is H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 1 -C 6 )alkoxy, which (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 1 -C 6 )alkoxy optionally is substituted with halo; \n R 1\u2032  is halo, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, aryl, heteroaryl, alkaryl, alkheteroaryl, aryloxy, heteroaryloxy, or benzyloxy, which (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, aryl, heteroaryl, alkaryl, alkheteroaryl, aryloxy, heteroaryloxy, or benzyloxy optionally is substituted with one or more of halo, fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, heteroaryl, aryloxy, and heteroaryloxy; \n R 3\u2032 , R 4\u2032 , and R 5\u2032  each independently is H, halo, (C 1 -C 8 )alkyl, or (C 2 -C 8 )alkenyl, which (C 1 -C 8 )alkyl, or (C 2 -C 8 )alkenyl optionally is substituted with one or more of halo, oxo, hydroxy, carboxy, cyano, \u2014NR a\u2032 R b\u2032 , fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, (C 1 -C 7 )C(\u2550O)NH\u2014, aryl, heteroaryl, aryloxy, and heteroaryloxy; and R a\u2032  and R b\u2032  each independently is H or (C 1 -C 6 )alkyl, or R a\u2032  and R b\u2032 , together with the nitrogen to which they are attached, form a morpholino, piperazino, pyrrolidino, or piperidino; \n R 2\u2033 , R 6\u2033 , and R 7\u2033  each independently is H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 1 -C 6 )alkoxy, which (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 1 -C 6 )alkoxy optionally is substituted with halo; \n R 1\u2033  is fluoro, bromo, iodo, (C 2 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkoxy, aryl, heteroaryl, alkaryl, alkheteroaryl, aryloxy, heteroaryloxy, or benzyloxy, which (C 2 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkoxy, aryl, heteroaryl, alkaryl, alkheteroaryl, aryloxy, heteroaryloxy, or benzyloxy optionally is substituted with one or more of halo, fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, aryl, heteroaryl, aryloxy, and heteroaryloxy; and R 3\u2033 , R 4\u2033 , and R 5\u2033  each independently is H, halo, (C 1 -C 8 )alkyl, or (C 2 -C 8 )alkenyl, which (C 1 -C 8 )alkyl, or (C 2 -C 8 )alkenyl optionally is substituted with one or more of halo, oxo, hydroxy, carboxy, cyano, \u2014NR a\u2033 R b\u2033 , fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, (C 1 -C 7 )C(\u2550O)NH\u2014, aryl, heteroaryl, aryloxy, and heteroaryloxy; R a\u2033  and R b\u2033  each independently is H or (C 1 -C 6 )alkyl, or R a\u2033  and R b\u2033 , together with the nitrogen to which they are attached, form a morpholino, piperazino, pyrrolidino, or piperidino; and at least one of R 3\u2033 , R 4\u2033 , and R 5\u2033  is other than H; or \n R 1\u2033  is fluoromethyl, difluoromethyl, trifluoromethyl, fluoroethyl, difluoroethyl, trifluoroethyl, fluoropropyl, difluoropropyl, trifluoropropyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, fluoroethoxy, difluoroethoxy, trifluoroethoxy, fluoropropoxy, difluoropropoxy, trifluoropropoxy, aryloxy, heteroaryloxy, alkaryl, or alkheteroaryl, which aryloxy, heteroarlyoxy, alkaryl, alkheteroaryl optionally is substituted by one or more of halo, fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, aryl, heteroaryl, aryloxy, and heteroaryloxy; and R 3\u2033 , R 4\u2033 , and R 5\u2033  each is H; \n X\u2032 and Y\u2032 are individually carbon, sulfur, oxygen, or nitrogen, wherein at least one of X and Y is other than carbon; \n R 2\u2032\u2033 , R 6\u2032\u2033 , and R 7\u2032\u2033  each independently is H, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 1 -C 6 )alkoxy, which (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, or (C 1 -C 6 )alkoxy optionally is substituted with halo; \n R 1\u2032\u2033  is halo, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, aryl, heteroaryl, alkaryl, alkheteroaryl, aryloxy, heteroaryloxy, or benzyloxy, which (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, aryl, heteroaryl, alkaryl, alkheteroaryl, aryloxy, heteroaryloxy, or benzyloxy optionally is substituted with one or more of halo, fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, aryl, heteroaryl, aryloxy, and heteroaryloxy; and \n R 3\u2032\u2033 , R 4\u2032\u2033 , and R 5\u2032\u2033  each independently is H, halo, (C 1 -C 8 )alkyl, or (C 2 -C 8 )alkenyl, which (C 1 -C 8 )alkyl, or (C 2 -C 8 )alkenyl optionally is substituted with one or more of halo, oxo, hydroxy, carboxy, cyano, \u2014NR a\u2032\u2033 R b\u2032\u2033 , fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, (C 1 -C 8 )alkyl, (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkoxy, (C 1 -C 7 )C(\u2550O)NH\u2014, aryl, heteroaryl, aryloxy, or heteroaryloxy; and R a\u2032\u2033  and R b\u2032\u2033  each independently is H or (C 1 -C 6 )alkyl, or R a\u2032\u2033  and R b\u2032\u2033 , together with the nitrogen to which they are attached, form a morpholino, piperazino, pyrrolidino, or piperidino.

Metadata:
- Claim Count in Document: 1.0
- Percentile: 94.0
- Lexical Diversity: 1.78125
- Patent Class: 549.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['14409407', '15064452', '13538698', '14679866', '14099276']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7608184701292847
- 35 USC 102 Novelty (BERT): 0.5086993045263708
- Combined Prediction Score: 0.7356065535689934
- Mean Citation Score: 288.092476
- Max Citation Score: 289.92883
- Similarity Product: 226.7700378221517

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