PATENT CLAIM ANALYSIS

Application Number: 16097440
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-05
Patent Classification: ["514", "340000"]

Abstract:
Compounds of the formula I in which X, Y, R 1  and R 2  have the meanings indicated in claim  1 , are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.

Claim (Index 8):
Compounds according to  claim 1 , selected from the group No. Name \u201cA1\u201d 1-((R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-propionyl)-piperidine-4- carboxylic acid methyl-p-tolyl-amide \u201cA2\u201d 1-((R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-propionyl)-piperidine-4- carboxylic acid (2-fluoro-4-methyl-phenyl)-methyl-amide \u201cA3\u201d 1-((R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-propionyl)-piperidine-4- carboxylic acid (2-chloro-4-trifluoromethyl-phenyl)-methyl-amide \u201cA4\u201d 1-((R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-propionyl)-piperidine-4- carboxylic acid (4-cyano-phenyl)-methyl-amide \u201cA5\u201d 1-((R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-propionyl)-piperidine-4- carboxylic acid (4-chloro-phenyl)-methyl-amide \u201cA6\u201d N,3-Dimethyl-N-(4-methylphenyl)-1-[(2R)-3,3,3-trifluoro-2-hydroxy- 2-methylpropanoyl]piperidine-4-carboxamide \u201cA7\u201d (3S,4S)-N,3-Dimethyl-N-(4-methylphenyl)-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidine-4-carboxamide \u201cA8\u201d (3R,4R)-N,3-Dimethyl-N-(4-methylphenyl)-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidine-4-carboxamide \u201cA9\u201d N-(4-chlorophenyl)-N,3-dimethyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy- 2-methylpropanoyl]piperidine-4-carboxamide \u201cA10\u201d (3S,4S)-N-(4-chlorophenyl)-N,3-dimethyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidine-4-carboxamide \u201cA11\u201d (3R,4R)-N-(4-chlorophenyl)-N,3-dimethyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidine-4-carboxamide \u201cA12\u201d N-(2-fluoro-4-methylphenyl)-N,3-dimethyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidine-4-carboxamide \u201cA13\u201d (3S,4S)-N-(2-fluoro-4-methylphenyl)-N,3-dimethyl-1-[(2R)-3,3,3- trifluoro-2-hydroxy-2-methylpropanoyl]piperidine-4-carboxamide \u201cA14\u201d (3R,4R)-N-(2-fluoro-4-methylphenyl)-N,3-dimethyl-1-[(2R)-3,3,3- trifluoro-2-hydroxy-2-methylpropanoyl]piperidine-4-carboxamide \u201cA15\u201d N-[2-chloro-4-(trifluoromethyl)phenyl]-N,3-dimethyl-1-[(2R)-3,3,3- trifluoro-2-hydroxy-2-methylpropanoyl]piperidine-4-carboxamide \u201cA16\u201d 4-Chloro-N-methyl-N-{1-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl- propanoyl]piperidin-4-yl}benzamide \u201cA17\u201d N,4-Dimethyl-N-{1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl}benzamide \u201cA18\u201d 2-Fluoro-4,N-dimethyl-N-{1-[(R)-3,3,3-trifluoro-2-hydroxy-2- methyl-propionyl]-piperidin-4-yl}-benzamide \u201cA19\u201d 2-Chloro-N-methyl-N-{1-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl- propanoyl]piperidin-4-yl}-4-(trifluoromethyl)benzamide \u201cA20\u201d 4-Chloro-N-methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy- 2-methylpropanoyl]piperidin-4-yl}benzamide \u201cA21\u201d 4-Chloro-N-methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA22\u201d 4-Chloro-N-methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA23\u201d N,4-Dimethyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl}benzamide, mixture of diastereomers \u201cA24\u201d N,4-Dimethyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA25\u201d N,4-Dimethyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA26\u201d 2-Fluoro-N,4-dimethyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl}benzamide \u201cA27\u201d 2-Fluoro-N,4-dimethyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro- 2-hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA28\u201d 4-Fluoro-N-methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl}benzamide \u201cA29\u201d 4-Fluoro-N-methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA30\u201d 4-Fluoro-N-methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA31\u201d N-Methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl- propanoyl]piperidin-4-yl}benzamide \u201cA32\u201d N-Methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl]benzamide \u201cA33\u201d N-Methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl]benzamide \u201cA34\u201d 4-Methoxy-N-methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl}benzamide \u201cA35\u201d 4-Methoxy-N-methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA36\u201d 4-Methoxy-N-methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA37\u201d 2,4-Difluoro-N-methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl}benzamide \u201cA38\u201d 2,4-Difluoro-N-methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro- 2-hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA39\u201d 2,4-Difluoro-N-methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro- 2-hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA40\u201d 3,5-Difluoro-N-methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl}pyridine-2-carboxamide \u201cA41\u201d 3,5-Difluoro-N-methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro- 2-hydroxy-2-methylpropanoyl]piperidin-4-yl]pyridine-2-carboxamide \u201cA42\u201d 3,5-Difluoro-N-methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro- 2-hydroxy-2-methylpropanoyl]piperidin-4-yl]pyridine-2-carboxamide \u201cA43\u201d 4-Cyano-N-methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl}benzamide \u201cA44\u201d 4-Cyano-N-methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA45\u201d 4-Cyano-N-methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA46\u201d 2-Fluoro-N-methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl}-4-(trifluoromethyl)benzamide \u201cA47\u201d 2-Fluoro-N-methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]-4- (trifluoromethyl)benzamide \u201cA48\u201d 2-Fluoro-N-methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]-4- (trifluoromethyl)benzamide \u201cA49\u201d 2-Chloro-4-fluoro-N-methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl}benzamide \u201cA50\u201d 2-Chloro-4-fluoro-N-methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3- trifluoro-2-hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA51\u201d 2-Chloro-4-fluoro-N-methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3- trifluoro-2-hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA52\u201d 5-Fluoro-N-methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl}pyridine-2-carboxamide \u201cA53\u201d 5-Fluoro-N-methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]pyridine-2-carboxamide \u201cA54\u201d 5-Fluoro-N-methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]pyridine-2-carboxamide \u201cA55\u201d N,1-Dimethyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl}-1H-pyrazole-4-carboxamide \u201cA56\u201d N,1-Dimethyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]-1H-pyrazole-4- carboxamide \u201cA57\u201d N,1-Dimethyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl]-1H-pyrazole-4- carboxamide \u201cA58\u201d 4-Chloro-2-fluoro-N-methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2- hydroxy-2-methylpropanoyl]piperidin-4-yl}benzamide \u201cA59\u201d 4-Chloro-2-fluoro-N-methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3- trifluoro-2-hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA60\u201d 4-Chloro-2-fluoro-N-methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3- trifluoro-2-hydroxy-2-methylpropanoyl]piperidin-4-yl]benzamide \u201cA61\u201d N-Methyl-N-{3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl- propanoyl]piperidin-4-yl}-4-(trifluoromethyl)benzamide \u201cA62\u201d N-Methyl-N-[(3R,4S)-3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl]-4-(trifluoromethyl)benzamide \u201cA63\u201d N-Methyl-N-[(3S,4R)-3-methyl-1-[(2R)-3,3,3-trifluoro-2-hydroxy-2- methylpropanoyl]piperidin-4-yl]-4-(trifluoromethyl)benzamide \u201cA64\u201d N-Ethyl-2-fluoro-4-methyl-N-[1-((R)-3,3,3-trifluoro-2-hydroxy-2- methyl-propionyl)-piperidin-4-yl]-benzamide \u201cA65\u201d 2-Fluoro-N-isopropyl-4-methyl-N-[1-((R)-3,3,3-trifluoro-2-hydroxy- 2-methyl-propionyl)-piperidin-4-yl]-benzamide \u201cA66\u201d 4-Cyano-N-ethyl-N-[1-((R)-3,3,3-trifluoro-2-hydroxy-2-methyl- propionyl)-piperidin-4-yl]-benzamide \u201cA67\u201d 4-Cyano-N-isopropyl-N-[1-((R)-3,3,3-trifluoro-2-hydroxy-2-methyl- propionyl)-piperidin-4-yl]-benzamide and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.

Metadata:
- Claim Count in Document: 32.0
- Percentile: 97.0
- Lexical Diversity: 1.34211
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15105154', '15748786', '14420003', '16069326', '15039226']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7795769314090255
- 35 USC 102 Novelty (BERT): 0.568372242296281
- Combined Prediction Score: 0.7584564624977511
- Mean Citation Score: 359.29564
- Max Citation Score: 434.02216
- Similarity Product: 386.4494216638279

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