PATENT CLAIM ANALYSIS

Application Number: 16086408
Application Type: Utility
Filing Date: 2018-09
Publication Date: 2019-04
Patent Classification: ["514", "256000"]

Abstract:
A series of substituted fused pentacyclic benzimidazole derivatives, and analogues thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Claim (Index 1):
A compound of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt thereof: wherein\n A represents N or C\u2014R 6 ; \n B represents N or C\u2014R 7 ; \n D represents N or C\u2014R 8 ; \n E represents a fused heteroaromatic ring system selected from the groups of formula (Ea), (Eb) and (EC): \n wherein the asterisks (*) represent the site of attachment of E to the remainder of the molecule;\n R 1  represents hydrogen, halogen, cyano, trifluoromethyl, trifluoromethoxy, \u2014OR a , \u2014SR a , \u2014SOR a , \u2014SO 2 R a , \u2014NR b R c , \u2014NR c COR d , \u2014NR c CO 2 R d , \u2014NHCONR b R c , \u2014NR c SO 2 R e , \u2014COR d , \u2014CO 2 R d , \u2014CONR b R c , \u2014SO 2 NR b R c , or \u2014S(O)(N\u2014R b )R e ; or R 1  represents C 1-6  alkyl, C 3-7  cycloalkyl, C 4-7  cycloalkenyl, aryl, aryl(C 1-6 )alkyl, C 3-7  heterocycloalkyl, C 3-7  heterocycloalkenyl, heteroaryl, heteroaryl(C 1-6 )alkyl, (C 3-7 )heterocycloalkyl(C 1-6 )alkyl-aryl-, (C 3-7 )heterocycloalkenyl-aryl-, (C 3-7 )cycloalkyl-heteroaryl-, (C 3-7 )cycloalkyl-(C 1-6 )alkyl-heteroaryl-, (C 4-7 )cycloalkenyl-heteroaryl-, (C 4-9 )bicycloalkyl-heteroaryl-, (C 3-7 )heterocycloalkyl-heteroaryl-, (C 3-7 )heterocycloalkyl(C 1-6 )alkyl-heteroaryl-, (C 3-7 )heterocycloalkenyl-heteroaryl-, (C 4-9 )heterobicycloalkyl-heteroaryl- or (C 4-9 )spiroheterocycloalkyl-heteroaryl-, any of which groups may be optionally substituted by one or more substituents; \n R 2  represents hydrogen, halogen, cyano, nitro, hydroxy, trifluoromethyl, trifluoromethoxy or \u2014OR a ; or R 2  represents C 1-6  alkyl or heteroaryl, either of which groups may be optionally substituted by one or more substituents; \n R 3  and R 4  independently represent hydrogen, halogen or trifluoromethyl: or C 1-6  alkyl, which group may be optionally substituted by one or more substituents; \n R 5  represents hydrogen, halogen, hydroxy, cyano, trifluoromethyl, difluoro-methoxy, trifluoromethoxy, \u2014OR a  or C 1-6  alkylsulphonyl; or R 5  represents C 1-6 alkyl, which group may be optionally substituted by one or more substituents; \n R 6 , R 7  and R 8  independently represent hydrogen, halogen, trifluoromethyl, C 1-6  alkyl or C 1-6  alkoxy; \n R 12  represents hydrogen or C 1-6  alkyl; \n R a  represents C 1-6  alkyl, C 3-7  cycloalkyl, aryl, aryl(C 1-6 )alkyl, C 3-7  hetero-cycloalkyl, heteroaryl or heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents; \n R b  and R c  independently represent hydrogen or trifluoromethyl; or C 1-6  alkyl, C 3-7  cycloalkyl, C 3-7  cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, C 3-7  heterocycloalkyl, C 3-7  heterocycloalkyl(C 1-6 )alkyl, heteroaryl or heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents; or \n R b  and R c , when taken together with the nitrogen atom to which they are both attached, represent a heterocyclic moiety selected from azetidin-1-yl, pyrrolidin-1-yl, oxazolidin-3-yl, isoxazolidin-2-yl, thiazolidin-3-yl, isothiazolidin-2-yl, piperidin-1-yl, morpholin-4-yl, thiomorpholin-4-yl, piperazin-1-yl, homopiperidin-1-yl, homomorpholin-4-yl, homopiperazin-1-yl, (imino)(oxo)thiazinan-4-yl, (oxo)thiazinan-4-yl and (dioxo)-thiazinan-4-yl, any of which groups may be optionally substituted by one or more substituents; \n R d  represents hydrogen; or R d  represents C 1-6  alkyl, C 3-7  cycloalkyl, aryl, C 3-7  heterocycloalkyl or heteroaryl, any of which groups may be optionally substituted by one or more substituents; \n R c  represents C 1-6  alkyl, aryl or heteroaryl, any of which groups may be optionally substituted by one or more substituents; and \n R f  and R g  independently represent hydrogen or C 1-6  alkyl.

Metadata:
- Claim Count in Document: 14.0
- Percentile: 97.0
- Lexical Diversity: 1.52381
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15513357', '15101767', '15101798', '15580137', '15102003']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8003373647108842
- 35 USC 102 Novelty (BERT): 0.5534663388877278
- Combined Prediction Score: 0.7756502621285687
- Mean Citation Score: 402.34228999999993
- Max Citation Score: 409.78156
- Similarity Product: 307.27701293017867

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