PATENT CLAIM ANALYSIS

Application Number: 15765377
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-10
Patent Classification: ["514", "217090"]

Abstract:
The present invention relates to arylcyclohexyl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.

Claim (Index 1):
A compound of Formula (I) wherein: R 1  is \u2014CF 3 , \u2014C 3-7 cycloalkyl, or \u2014C 4-7 heterocycloalkyl, wherein the \u2014C 3-7 cycloalkyl, and \u2014C 4-7 heterocycloalkyl is unsubstituted or substituted by one or two substituents independently selected from \u2014C 1-3 alkyl, phenyl, triazolyl, pyridyl, pyridazinyl, imidazolyl, pyrazolyl, isoxazolyl, halo, \u2014NR 9 \u2014C(O)\u2014R 10  and \u2014C(O)R 10 , and wherein the phenyl, triazolyl, pyridyl, pyridazinyl, imidazolyl, pyrazolyl and isoxazolyl is substituted by one or two substituents independently selected from \u2014C 1-3 alkyl and halo; or R 1  is \u2014C 2-3 alkyl-R 11 ; Each R 2  is independently hydrogen, halo, or \u2014C 1-3 alkyl; G is CH or N; A is R 3  is \u2014(CH 2 ) n \u2014C(O)N(R 5 )(R 6 ), or R 3  is \u2014O\u2014C 1-3 alkyl, \u2014C 4-7 heterocycloalkyl, \u2014O\u2014C 4-7 heterocycloalkyl, \u2014C 3-7 cycloalkyl, \u2014O\u2014C 3-7 cycloalkyl, \u2014C(O)\u2014O\u2014C 1-5  alkyl, \u2014C(O)\u2014C 1-5 alkyl, \u2014C(O)-aryl, \u2014S\u2014C 4-7 heterocycloalkyl, \u2014S\u2014C 3-7 cycloalkyl, \u2014S(O)\u2014C 1-3 alkyl, \u2014S(O)\u2014C 4-7 heterocycloalkyl, \u2014S(O)\u2014C 3-7 cycloalkyl, \u2014S(O) 2 \u2014C 1-3 alkyl, \u2014S(O) 2 \u2014C 4-7 heterocycloalkyl, \u2014S(O) 2 \u2014C 3-7 cycloalkyl, \u2014S(O) 2 -aryl, wherein each of \u2014O\u2014C 1-3 alkyl, \u2014C 1-6 alkyl, \u2014C 4-7 heterocycloalkyl, \u2014O\u2014C 4-7 heterocycloalkyl, \u2014C 3-7 cycloalkyl, \u2014O\u2014C 3-7 cycloalkyl, \u2014C(O)\u2014C 1-5 alkyl, \u2014C(O)-aryl, \u2014S\u2014C 4-7 heterocycloalkyl, \u2014S\u2014C 3-7 cycloalkyl, \u2014S(O)\u2014C 1-3 alkyl, \u2014S(O)\u2014C 4-7 heterocycloalkyl, \u2014S(O)\u2014C 3-7 cycloalkyl, \u2014S(O) 2 \u2014C 1-3 alkyl, \u2014S(O) 2 \u2014C 4-7 heterocycloalkyl, \u2014S(O) 2 \u2014C 3-7 cycloalkyl-S(O) 2 -aryl, is unsubstituted or substituted by one or two substituents independently selected from \u2014C 1-7 alkyl, \u2014C 3-7 cycloalkyl, \u2014OH, \u2550O, \u2014O\u2014C 1-5 alkyl, \u2014C 4-7 heterocycloalkyl, phenyl, pyridyl, pyrazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, and triazolyl, and wherein the \u2014C 1-7 alkyl, \u2014C 3-7 cycloalkyl, \u2014C 4-7 heterocycloalkyl, phenyl, pyridyl, pyrazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, or triazolyl is further unsubstituted or substituted by one or two substituents independently selected from C 1-5  alkyl and halo; Each R 4  is independently hydrogen, halo or \u2014C 1-3 alkyl, R 5  and R 6  are independently H, \u2014C 3-7 cycloalkyl or \u2014C 4-7 heterocycloalkyl, wherein each of \u2014C 1-6 alkyl, \u2014C 3-7 cycloalkyl or \u2014C 4-7 heterocycloalkyl is unsubstituted or substituted by one or two substituents independently selected from F, \u2014CH\u2014F 2 , \u2014CF 3 , \u2014(CH 2 ) n \u2014O\u2014(CH 2 ) m \u2014CH 3 , and \u2014C 3-7 cycloalkyl; or R 5  and R 6  together with the nitrogen atom to which they are attached form a 5-8-membered ring or an 8-10-membered bicyclic ring or a 9-10-membered bridged bicyclic ring, wherein each 5-8-membered ring, 8-11-membered bicyclic ring, or 9-10-membered bridged bicyclic ring optionally includes one or more oxygen ring atoms or another nitrogen ring atom, and wherein each 5-8-membered ring, 8-11-membered bicyclic ring, or 9-10-membered bridged bicyclic ring is unsubstituted or substituted by one or two substituents independently selected from \u2014C 1-5 alkyl, \u2014C 3-7 cycloalkyl, \u2014C 4-7 heterocycloalkyl, F, \u2014CHF 2 , \u2014CF 3 , and \u2014(CH 2 ) n \u2014O\u2014(CH 2 ) m \u2014CH 3 ; R 5  and R 6  together with the nitrogen atom to which they are attached form 4-azaspiro[2.5]octane, 7-azaspiro[4.5]decane, 2-oxa-8-azaspiro[5.5]undecane, 6-oxa-9-azaspiro[4.5]decane, 2-oxa-8-azaspiro[5.5]undecane, or 1-azaspiro[4.5]decane; R 7  and R 8  are independently H, \u2014C 1-6 alkyl, \u2014C 3-7 cycloalkyl or \u2014C 4-7 heterocycloalkyl wherein each of \u2014C 1-6  alkyl, \u2014C 3-7  cycloalkyl or \u2014C 4-7  heterocycloalkyl is unsubstituted or substituted by one or two substituents independently selected from F, CHF 2 , CF 3 , and (CH 2 ) n \u2014O\u2014(CH 2 ) m \u2014CH 3 , or R 7  and R 8  together with the carbon atoms to which they are attached form a 5-8-membered ring, which optionally includes one or more oxygen or nitrogen atoms as ring atoms, and wherein the 5-8-membered ring is unsubstituted or substituted by one or two substituents independently selected from \u2014C 1-5 alkyl, \u2014C 3-7 cycloalkyl, \u2014C 4-7 heterocycloalkyl, F, \u2014CHF 2 , \u2014CF 3 , \u2550O, and \u2014(CH 2 ) n \u2014O\u2014(CH 2 ) m \u2014CH 3 ; R 9  is H or \u2014C 1-3 alkyl; R 10  is \u2014C 1-3  alkyl; R 11  is phenyl, triazolyl, pyridyl, pyridazinyl, imidazolyl, or pyrazolyl, wherein each of phenyl, triazolyl, pyridyl, pyridazinyl, imidazolyl, or pyrazolyl is unsubstituted or substituted by one or two substituents independently selected from C 1-3 alkyl and halo; Each n is independently 0 or 1; Each m is independently 0 or 1; or a pharmaceutically acceptable salt thereof.

Metadata:
- Claim Count in Document: 1.0
- Percentile: 91.0
- Lexical Diversity: 1.07407
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15765354', '15735977', '15736075', '15105306', '12899410']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7803139928735499
- 35 USC 102 Novelty (BERT): 0.606157902115879
- Combined Prediction Score: 0.7628983837977829
- Mean Citation Score: 389.988172
- Max Citation Score: 523.7763
- Similarity Product: 473.4515269741416

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

Dataset: test