PATENT CLAIM ANALYSIS

Application Number: 15748786
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2019-01
Patent Classification: ["544", "350000"]

Abstract:
Compounds of the formula Ia or of the formula Ib 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 5):
Compounds according to  claim 1 , selected from the group No. Name \u201cA1\u201d (2R)-1-[1-(4-chlorophenyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5- yl]-3,3,3-trifluoro-2-hydroxy-2-methyl-propan-1-one \u201cA2\u201d (2R)-1-[2-(4-chlorophenyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin- 5-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl-propan-1-one \u201cA3\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-(1-phenyl-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl)-propan-1-one \u201cA4\u201d (R)-3,3,3-Trifluoro-1-[1-(4-fluoro-phenyl)-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl-propan-1-one \u201cA5\u201d (R)-1-[1-(2,4-Difluoro-phenyl)-1,4,6,7-tetrahydro-pyrazolo[4,3- c]pyridin-5-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl-propan-1-one \u201cA6\u201d (R)-1-[2-(2,4-Difluoro-phenyl)-2,4,6,7-tetrahydro-pyrazolo[4,3- c]pyridin-5-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl-propan-1-one \u201cA7\u201d (R)-1-(1-tert-Butyl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl)- 3,3,3-trifluoro-2-hydroxy-2-methyl-propan-1-one \u201cA8\u201d (R)-1-(2-tert-Butyl-2,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl)- 3,3,3-trifluoro-2-hydroxy-2-methyl-propan-1-one \u201cA9\u201d (2R)-1-[1-(4-chlorophenyl)-7-methyl-6,7-dihydro-4H-pyrazolo[4,3- c]pyridin-5-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl-propan-1-one \u201cA10\u201d (R)-1-[(R)-1-(4-Chloro-phenyl)-7-methyl-1,4,6,7-tetrahydro- pyrazolo[4,3-c]pyridin-5-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl- propan-1-one \u201cA11\u201d (R)-1-[(S)-1-(4-Chloro-phenyl)-7-methyl-1,4,6,7-tetrahydro- pyrazolo[4,3-c]pyridin-5-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl- propan-1-one \u201cA12\u201d (2R)-3,3,3-trifluoro-1-[1-(4-fluorophenyl)-7-methyl-6,7-dihydro-4H- pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl-propan-1-one \u201cA13\u201d (2R)-3,3,3-trifluoro-1-[2-(4-fluorophenyl)-7-methyl-6,7-dihydro-4H- pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl-propan-1-one \u201cA14\u201d (R)-3,3,3-Trifluoro-1-[(R)-1-(4-fluoro-phenyl)-7-methyl-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl-propan- 1-one \u201cA15\u201d (R)-3,3,3-Trifluoro-1-[(S)-1-(4-fluoro-phenyl)-7-methyl-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl-propan- 1-one \u201cA16\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-(7-methyl-1-phenyl- 1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl)-propan-1-one \u201cA17\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-(7-methyl-2-phenyl- 2,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl)-propan-1-one \u201cA18\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-((R)-7-methyl-1-phenyl- 1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl)-propan-1-one \u201cA19\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-((S)-7-methyl-1-phenyl- 1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl)-propan-1-one \u201cA20\u201d (R)-1-[(R)-1-(2,4-Difluoro-phenyl)-7-methyl-1,4,6,7-tetrahydro- pyrazolo[4,3-c]pyridin-5-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl- propan-1-one \u201cA21\u201d (R)-1-[(S)-1-(2,4-Difluoro-phenyl)-7-methyl-1,4,6,7-tetrahydro- pyrazolo[4,3-c]pyridin-5-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl- propan-1-one \u201cA22\u201d (R)-1-((R)-1-tert-Butyl-7-methyl-1,4,6,7-tetrahydro-pyrazolo[4,3- c]pyridin-5-yl)-3,3,3-trifluoro-2-hydroxy-2-methyl-propan-1-one \u201cA23\u201d (R)-1-((S)-1-tert-Butyl-7-methyl-1,4,6,7-tetrahydro-pyrazolo[4,3- c]pyridin-5-yl)-3,3,3-trifluoro-2-hydroxy-2-methyl-propan-1-one \u201cA24\u201d (R)-3,3,3-Trifluoro-1-[(R)-1-(2-fluoro-phenyl)-7-methyl-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl-propan- 1-one \u201cA25\u201d (R)-3,3,3-Trifluoro-1-[(S)-1-(2-fluoro-phenyl)-7-methyl-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl-propan- 1-one \u201cA26\u201d 2-[(R)-7-Methyl-5-((R)-3,3,3-trifluoro-2-hydroxy-2-methyl- propionyl)-4,5,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-1-yl]- benzonitrile \u201cA27\u201d 2-[(S)-7-Methyl-5-((R)-3,3,3-trifluoro-2-hydroxy-2-methyl- propionyl)-4,5,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-1-yl]- benzonitrile \u201cA28\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-((R)-7-methyl-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl)-propan-1-one \u201cA29\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-((S)-7-methyl-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl)-propan-1-one \u201cA30\u201d (R)-3,3,3-Trifluoro-2-hydroxy-1-[(R)-1-(6-methoxy-pyridin-3-yl)-7- methyl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-methyl- propan-1-one \u201cA31\u201d (R)-3,3,3-Trifluoro-2-hydroxy-1-[(S)-1-(6-methoxy-pyridin-3-yl)-7- methyl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-methyl- propan-1-one \u201cA32\u201d (R)-3,3,3-Trifluoro-1-[(R)-1-(3-fluoro-pyridin-2-yl)-7-methyl- 1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl- propan-1-one \u201cA33\u201d (R)-3,3,3-Trifluoro-1-[(S)-1-(3-fluoro-pyridin-2-yl)-7-methyl- 1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl- propan-1-one \u201cA34\u201d (R)-1-[(R)-1-(3,5-Difluoro-pyridin-2-yl)-7-methyl-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl- propan-1-one \u201cA35\u201d (R)-1-[(S)-1-(3,5-Difluoro-pyridin-2-yl)-7-methyl-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-3,3,3-trifluoro-2-hydroxy-2- methyl-propan-1-one \u201cA36\u201d (R)-3,3,3-Trifluoro-1-[(R)-1-(5-fluoro-2-methoxy-pyrimidin-4-yl)-7- methyl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2- methyl-propan-1-one \u201cA37\u201d (R)-3,3,3-Trifluoro-1-[(S)-1-(5-fluoro-2-methoxy-pyrimidin-4-yl)-7- methyl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2- methyl-propan-1-one \u201cA38\u201d (R)-3,3,3-Trifluoro-2-hydroxy-1-[(R)-1-(4-hydroxy-cyclohexyl)-7- methyl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-methyl- propan-1-one \u201cA39\u201d (R)-3,3,3-Trifluoro-2-hydroxy-1-[(S)-1-(4-hydroxy-cyclohexyl)-7- methyl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-methyl- propan-1-one \u201cA40\u201d (R)-3,3,3-Trifluoro-1-[(R)-1-(5-fluoro-pyridin-2-yl)-7-methyl-1,4,6,7- tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl- propan-1-one \u201cA41\u201d (R)-3,3,3-Trifluoro-1-[(S)-1-(5-fluoro-pyridin-2-yl)-7- methyl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxy-2-methyl- propan-1-one \u201cA43\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-(3-phenyl-3,4,6,7- tetrahydro-imidazo[4,5-c]pyridin-5-yl)-propan-1-one \u201cA44\u201d (R)-3,3,3-Trifluoro-1-[1-(4-fluoro-phenyl)-1,4,6,7-tetrahydro- imidazo[4,5-c]pyridin-5-yl]-2-hydroxy-2-methyl-propan-1-one \u201cA45\u201d (R)-1-[1-(4-Chloro-phenyl)-1,4,6,7-tetrahydro-imidazo[4,5- c]pyridin-5-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl-propan-1-one \u201cA46\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-(1-phenyl-1,4,6,7- tetrahydro-[1,2,3]triazolo[4,5-c]pyridin-5-yl)-propan-1-one \u201cA47\u201d (R)-3,3,3-Trifluoro-1-[1-(4-fluoro-phenyl)-1,4,6,7-tetrahydro- [1,2,3]triazolo[4,5-c]pyridin-5-yl]-2-hydroxy-2-methyl-propan-1-one \u201cA48\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-(3-phenyl-5,6-dihydro- 8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl)-propan-1-one \u201cA49\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-(3-phenyl-5,6-dihydro- 8H-imidazo[1,2-a]pyrazin-7-yl)-propan-1-one \u201cA50\u201d (R)-3,3,3-Trifluoro-2-hydroxy-2-methyl-1-(3-phenyl-5,6-dihydro- 8H-imidazo[1,5-a]pyrazin-7-yl)-propan-1-one \u201cA51\u201d (R)-3,3,3-Trifluoro-1-[3-(4-fluoro-phenyl)-5,6-dihydro-8H- imidazo[1,5-a]pyrazin-7-yl]-2-hydroxy-2-methyl-propan-1-one \u201cA52\u201d (R)-3,3,3-Trifluoro-1-[(R)-3-(4-fluoro-phenyl)-5-methyl-5,6- dihydro-8H-imidazo[1,5-a]pyrazin-7-yl]-2-hydroxy-2-methyl- propan-1-one \u201cA53\u201d (R)-3,3,3-Trifluoro-1-[(S)-3-(4-fluoro-phenyl)-5-methyl-5,6- dihydro-8H-imidazo[1,5-a]pyrazin-7-yl]-2-hydroxy-2-methyl- propan-1-one \u201cA54\u201d (R)-1-[(R)-3-(2,4-Difluoro-phenyl)-5-methyl-5,6-dihydro-8H- imidazo[1,5-a]pyrazin-7-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl- propan-1-one \u201cA55\u201d (R)-1-[(S)-3-(2,4-Difluoro-phenyl)-5-methyl-5,6-dihydro-8H- imidazo[1,5-a]pyrazin-7-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl- propan-1-one \u201cA56\u201d (R)-1-[(S)-3-(3,5-Difluoro-pyridin-2-yl)-5-methyl-5,6-dihydro-8H- imidazo[1,5-a]pyrazin-7-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl- propan-1-one \u201cA57\u201d (R)-1-[(R)-3-(3,5-Difluoro-pyridin-2-yl)-5-methyl-5,6-dihydro-8H- imidazo[1,5-a]pyrazin-7-yl]-3,3,3-trifluoro-2-hydroxy-2-methyl- propan-1-one and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.

Metadata:
- Claim Count in Document: 18.0
- Percentile: 86.0
- Lexical Diversity: 1.4
- Patent Class: 544.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15105154', '09927324', '12298369', '14342749', '14420003']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7923522635771248
- 35 USC 102 Novelty (BERT): 0.5456670926457083
- Combined Prediction Score: 0.7676837464839832
- Mean Citation Score: 375.832478
- Max Citation Score: 391.2317
- Similarity Product: 336.1248932077825

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