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 3):
A compound of  claim 1  selected from:\n 5-Cyclopropyl-1-{3-[3-(dimethylcarbamoyl)cyclohexyl]phenyl}-1H-pyrazole-4-carboxylic acid (cis-racemate); \n 5-Cyclopropyl-1-{3-[3-(4,5,6,7-tetrahydro-1H-indazol-1-yl)cyclohexyl]phenyl}-1H-pyrazole-4-carboxylic acid; \n 5-Cyclopropyl-1-{3-[3-(piperidine-1-carbonyl)cyclohexyl]phenyl}-1H-pyrazole-4-carboxylic acid (cis-racemate); \n 1-[3-(3-{7-Azaspiro[4. 5]decane-7-carbonyl}cyclohexyl)phenyl]-5-cyclopropyl-1H-pyrazole-4-carboxylic acid (cis-racemate); \n 5-Cyclopropyl-1-{3-[3-(2-propylpiperidine-1-carbonyl)cyclohexyl]phenyl}-1H-pyrazole-4-carboxylic acid; \n 5-cyclopropyl-1-{3-[3-(2,2-dimethylpyrrolidine-1-carbonyl)cyclohexyl]phenyl}-1H-pyrazole-4-carboxylic acid; \n 1-[3-(3-{1-Azaspiro [4.5]decane-1-carbonyl}cyclohexyl)phenyl]-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 1-{3-[3-(2-butylpyrrolidine-1-carbonyl)cyclohexyl]phenyl}-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 1-[3-(3-{1H,4H,5H,6H,7H,8H-cyclohepta[c]pyrazol-1-yl}cyclohexyl)phenyl]-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 1-[3-(3-{1H,4H,5H,6H-cyclopenta[c]pyrazol-1-yl}cyclopentyl)phenyl]-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 5-Cyclopropyl-1-(3-{3-[2-(3-methylbutyl)pyrrolidine-1-carbonyl]cyclohexyl}phenyl)-1H-pyrazole-4-carboxylic acid; \n 5-Cyclopropyl-1-{3-[3-(2-cyclopropylpyrrolidine-1-carbonyl)cyclohexyl]phenyl}-1H-pyrazole-4-carboxylic acid; \n 1-{3-[3-(2-cyclobutylpyrrolidine-1-carbonyl)cyclohexyl]phenyl}-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 5-Cyclopropyl-1-{3-[(cis)-3-(6-methyl-5,6-dihydro-4H-cyclopentapyrazol-1-yl)-cyclohexyl]-phenyl}-1H-pyrazole-4-carboxylic acid (cis racemic); \n 5-Cyclopropyl-1-{3-[3-(4-oxo-4,5,6,7-tetrahydro-indazol-1-yl)-cyclopentyl]-phenyl}-1H-pyrazole-4-carboxylic acid; \n 5-Cyclopropyl-1-[3-(3-{6-propyl-1H,4H,5H,6H-cyclopenta[c]pyrazol-1-yl}cyclohexyl)phenyl]-1H-pyrazole-4-carboxylic acid (cis racemic); \n 1-{3-3-[2-butylpyrrolidine-1-carbonyl]cyclohexyl]phenyl}-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 5-Cyclopropyl-1-(3-{3-[(2S)-2-(ethoxymethyl)pyrrolidine-1-carbonyl]cyclohexyl}phenyl)-1H-pyrazole-4-carboxylic acid (resolved cis diastereoisomers); \n 5-Cyclopropyl-1-(3-{3-[(2S)-2-(ethoxymethyl)pyrrolidine-1-carbonyl]cyclohexyl}phenyl)-1H-pyrazole-4-carboxylic acid (resolved cis diastereoisomers); \n 1-(5\u2032-(Azepane-1-carbonyl)-2\u2032,3\u2032,4\u2032,5\u2032-tetrahydro-[1,1\u2032-biphenyl]-3-yl)-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 1-(3-(3-(Azepane-1-carbonyl)cyclohexyl)phenyl)-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 1-(3-(3-(Cyclohexyl(methyl)carbamoyl)cyclohexyl)phenyl)-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 5-Cyclopropyl-1-(3-(3-(methyl(2-propylcyclohexyl)carbamoyl)cyclohexyl)phenyl)-1H-pyrazole-4-carboxylic acid; \n 5-Cyclopropyl-1-(3-(t-3-(6,6-dimethyl-5,6-dihydrocyclopenta[c]pyrazol-1(4H)-yl)cyclohexyl)phenyl)-1H-pyrazole-4-carboxylic acid (trans racemic); \n 5-Cyclopropyl-1-(3-(-3-(6,6-dimethyl-5,6-dihydrocyclopenta[c]pyrazol-1(4H)-yl)cyclohexyl)phenyl)-1H-pyrazole-4-carboxylic acid (cis racemate); \n 5-Cyclopropyl-1-{3-[3-(3-methyl-pyrrolidine-1-carbonyl)-cyclohexyl]-phenyl}-1H-pyrazole-4-carboxylic acid; \n 1-(3-(1-(tert-butoxycarbonyl)piperidin-3-yl)phenyl)-5-((1R,2R)-2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1H-pyrazole-4-carboxylic acid; \n 1-(3-(1-(tert-Butoxycarbonyl)piperidin-3-yl)phenyl)-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 1-(3-(1-(cyclohexylmethyl)piperidin-3-yl)phenyl)-5-cyclopropyl-1H-pyrazole-4-carboxylic acid, Hydrochloride; \n 5-((1R,2R)-2-(1-Methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1-(3-(1-phenethylpiperidin-3-yl)phenyl)-1H-pyrazole-4-carboxylic acid, Hydrochloride; \n 5-((1R,2R)-2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1-(3-(1-(phenylsulfonyl)piperidin-3-yl)phenyl)-1H-pyrazole-4-carboxylic acid; \n 1-(3-(1-(2-cyclohexylacetyl)piperidin-3-yl)phenyl)-5-((1R,2R)-2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1H-pyrazole-4-carboxylic acid; \n 5-((1R,2R)-2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1-(3-(1-pivaloylpiperidin-3-yl)phenyl)-1H-pyrazole-4-carboxylic acid; \n 1-(3-(1-benzoylpiperidin-3-yl)phenyl)-5-((1R,2R)-2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1H-pyrazole-4-carboxylic acid; \n 5-((1R,2R)-2-(1-Methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1-(3-(1-((R)-2-propylpiperidine-1-carbonyl)piperidin-3-yl)phenyl)-1H-pyrazole-4-carboxylic acid; \n 1-(3-(3-(2-cyclohexylethyl)piperidin-1-yl)phenyl)-5-((1R,2R)-2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1H-pyrazole-4-carboxylic acid; \n 1-(3-((S)-3-(2-Cyclohexylethyl)piperidin-1-yl)phenyl)-5-((1R,2R)-2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1H-pyrazole-4-carboxylic acid; \n 1-(3-((R)-3-(2-cyclohexylethyl)piperidin-1-yl)phenyl)-5-((1R,2R)-2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1H-pyrazole-4-carboxylic acid; \n 1-(3-((1R,3S)-3-(6-Butyl-5,6-dihydrocyclopenta[c]pyrazol-1(4H)-yl)cyclohexyl)phenyl)-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 1-(3-((1,3-trans)-3-(6-Butyl-5,6-dihydrocyclopenta[c]pyrazol-1(4H)-yl)cyclohexyl)phenyl)-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 1-(3-((1,3-cis)-3-(6,6-Dimethyl-5,6-dihydrocyclopenta[c]pyrazol-1(4H)-yl)cyclohexyl)phenyl)-5-(2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1H-pyrazole-4-carboxylic acid; \n 1-(3-((1,3-trans)-3-(6,6-Dimethyl-5,6-dihydrocyclopenta[c]pyrazol-1(4H)-yl)cyclohexyl)phenyl)-5-(2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1H-pyrazole-4-carboxylic acid; \n 1-(3-(3-((2-Butylcyclopentyl)(methyl)carbamoyl)cyclohexyl)phenyl)-5-cyclopropyl-1H-pyrazole-4-carboxylic acid; \n 1-(3-(3-(2-Butylpyrrolidine-1-carbonyl)cyclohexyl)phenyl)-5-(2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1H-pyrazole-4-carboxylic acid; and \n 1-(3-((R)-3-(Cyclohexylmethoxy)piperidin-1-yl)phenyl)-5-((1R,2R)-2-(1-methyl-1H-1,2,3-triazol-4-yl)cyclopropyl)-1H-pyrazole-4-carboxylic acid.

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): 0.780738561683465
- 35 USC 102 Novelty (BERT): 0.6047061404799683
- Combined Prediction Score: 0.7631353195631153
- Mean Citation Score: 389.988172
- Max Citation Score: 523.7763
- Similarity Product: 466.7067412506223

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