PATENT CLAIM ANALYSIS

Application Number: 16223925
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-06
Patent Classification: ["546", "119000"]

Abstract:
The invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.

Claim (Index 12):
The compound according to  claim 1 , selected from the group consisting of\n 1 2,2-difluoro-N-[rac-(2R,3S)-2-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 2 2,2-difluoro-N-[(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 3 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 4 2,2-difluoro-N-[(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(2-methoxy-4-pyridyl)-5-oxo-pyrrolidin-3-yl]propanamide 5 2,2-difluoro-N-[rac-(2R,3S)-2-(2,4-difluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 6 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(3,4-difluorophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 7 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(3-methoxyphenyl)-5-oxo-pyrrolidin-3-yl]propanamide 8 N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]cyclopropane-carboxamide 9 N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]cyclopropane-sulfonamide 10 N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(3-methoxyphenyl)-5-oxo-pyrrolidin-3-yl]cyclopropanesulfonamide 11 2,2-difluoro-N-[rac-(2R,3S)-2-(4-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 12 N-[(2R,3S)-2-(3-chlorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]-2,2-difluoro-propanamide 13 1-methyl-N-[rac-(2R,3S)-2-(4-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 14 1-fluoro-N-[rac-(2R,3S)-2-(3-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 15 N-[rac-(2R,3S)-2-(3-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]-1-(trifluoromethyl)cyclopropanecarboxamide 16 N-[rac-(2R,3S)-2-(3-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]methanesulfonamide 17 N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(3-methoxyphenyl)-5-oxo-pyrrolidin-3-yl-]1-(trifluoromethyl)cyclopropanecarboxamide 18 1-methyl-N-[rac-(2R,3S)-2-(3-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 19 N-[rac-(2R,3S)-2-(3-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclobutanecarboxamide 20 2,2-difluoro-N-[(2S,3R)-2-(4-fluoro-3-methoxy-phenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 21 2,2-difluoro-N-[(2R,3S)-2-(4-fluoro-3-methoxy-phenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 22 1-methyl-N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(3-methoxyphenyl)-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 23 1-fluoro-N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(3-methoxyphenyl)-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 24 2,2-difluoro-N-[(2S,3R)-2-(2-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 25 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(3-fluorophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 26 2,2-difluoro-N-[rac-(2R,3S)-2-(3,5-difluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 27 2,2-difluoro-N-[rac-(2R,3S)-5-oxo-2-phenyl-1-(1-phenylindazol-5-yl)pyrrolidin-3-yl]propanamide 28 N-[(2R,3S)-2-(2-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclo-propanecarboxamide 29 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(4-cyanophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 30 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(3-cyanophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 31 2,2-difluoro-N-[rac-(2R,3S)-2-(3-chlorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 32 N-[rac-(2R,3S)-2-(3-chlorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclobutanecarboxamide 33 2,2-difluoro-N-[(2R,3S)-2-(2-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 34 N-[(2R,3S)-2-(4-fluoro-3-methoxy-phenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 36 2,2-difluoro-N-[rac-(2S,3S)-2-cyclopropyl-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 37 1-cyclopropyl-N-[rac-(2R,3S)-2-(3-chlorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]methanesulfonamide 38 2,2-difluoro-N-[(2S,3R)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(o-tolyl)-5-oxo-pyrrolidin-3-yl]propanamide 39 N-[(2S,3R)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]cyclopropanecarboxamide 42 2,2-difluoro-N-[(2S,3R)-2-(2-fluoro-5-methoxy-phenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 43 N-[(2S,3R)-2-(2-fluoro-5-methoxy-phenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 45 1:1 mixture of (1 S,2S)-2-fluoro-N-[(2R,3S)-2-(4-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide and (1 S,2S)-2-fluoro-N-[(2S,3R)-2-(4-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 46 rac-(1 S,2R)-2-fluoro-N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(3-methoxyphenyl)-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 48 2,2-difluoro-N-[rac-(2S,3R)-2-cyclopropyl-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 49 N-[(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(2-methoxy-4-pyridyl)-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 51 N-[rac-(2R,3S)-2-(4-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanesulfonamide 52 2-methyl-N-[rac-(2R,3S)-2-(3-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 53 N-[(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(o-tolyl)-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 54 N-[rac-(2R,3S)-2-(4-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 55 N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(3-methoxyphenyl)-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 56 1:1 mixture of (1R,2R)-2-fluoro-N-[(2R,3S)-2-(4-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide and (1R,2R)-2-fluoro-N-[(2S,3R)-2-(4-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 61 N-[rac-(2R,3S)-2-(3-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 62 N-[(2R,3S)-2-(2-fluoro-5-methoxy-phenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 63 1:1 mixture of (1R,2R)-2-fluoro-N-[(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(3-methoxyphenyl)-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide and (1R,2R)-2-fluoro-N-[(2S,3R)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(3-methoxyphenyl)-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 65 N-[(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]cyclopropanecarboxamide 66 N-[rac-(2R,3S)-2-(3-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]acetamide 67 N-[rac-(2R,3S)-2-(3-chlorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 68 2,2-difluoro-N-[rac-(2R,3S)-2-(3-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 69 2,2-difluoro-N-[(2R,3S)-2-(2-fluoro-5-methoxy-phenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 70 1-fluoro-N-[rac-(2R,3S)-2-(4-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]cyclopropanecarboxamide 71 N-[rac-(2R,3S)-2-(4-fluorophenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-pyrrolidin-3-yl]-1-(trifluoromethyl)cyclopropanecarboxamide 72 2,2-difluoro-N-[(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-2-(o-tolyl)-5-oxo-pyrrolidin-3-yl]propanamide 73 1-fluoro-N-[(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]cyclopropanecarboxamide 74 N-[(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]-1-methyl-cyclopropanecarboxamide 75 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(4,4-difluorocyclohexyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 76 2,2-difluoro-N-[rac-(2R,3S)-1-(1-cyclohexylindazol-5-yl)-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 77 2,2-difluoro-N-[rac-(2R,3S)-2-(2-fluoro-5-methoxy-phenyl)-1-(1-methylindazol-5-yl)-5-oxo-pyrrolidin-3-yl]propanamide 78 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(2,2-difluoroethyl)indazol-5-yl]-2-(2-fluoro-5-methoxy-phenyl)-5-oxo-pyrrolidin-3-yl]propanamide 79 2,2-difluoro-N-[rac-(2R,3S)-1-[1-[(2-fluorophenyl)methyl]indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 80 2,2-difluoro-N-[rac-(2R,3S)-1-[1-[(3-fluorophenyl)methyl]indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 81 2,2-difluoro-N-[rac-(2R,3S)-1-[1-[(4-fluorophenyl)methyl]indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 82 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(cyclopropylmethyl)indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 84 2,2-difluoro-N-[rac-(2R,3S)-1-[1-[(4,4-difluorocyclohexyl)methyl]indazol-5-yl]-5-oxo-2-phenyl-pyrrolidin-3-yl]propanamide 85 2,2-difluoro-N-[rac-(2R,3S)-2-(4-fluorophenyl)-1-[1-[(2-fluorophenyl)methyl]indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 86 2,2-difluoro-N-[rac-(2R,3S)-2-(4-fluorophenyl)-1-[1-[(4-fluorophenyl)methyl]indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 87 2,2-difluoro-N-[rac-(2R,3S)-2-(4-fluorophenyl)-1-[1-[(3-fluorophenyl)methyl]indazol-5-yl]-5-oxo-pyrrolidin-3-yl]propanamide 88 N-[(2R,3S)-2-benzyl-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-5-oxopyrrolidin-3-yl]-2,2-difluoropropanamide 89 2,2-difluoro-N-[rac-(2R,3S)-2-ethyl-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxopyrrolidin-3-yl]propanamide 90 2,2-difluoro-N-[rac-(2R,3R)-2-(cyclopropylmethyl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxopyrrolidin-3-yl]propanamide 91 2-cyclopropyl-N-[(2S,3R)-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-5-oxo-2-phenylpyrrolidin-3-yl]acetamide 92 N-[(2R,3S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-5-oxo-2-phenylpyrrolidin-3-yl]-1-methyl-1H-pyrazole-3-carboxamide 93 N-[(2R,3S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-5-oxo-2-phenylpyrrolidin-3-yl]-1H-imidazole-2-carboxamide 94 N-[(2R,3S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-5-oxo-2-phenylpyrrolidin-3-yl]-2-methyloxazole-5-carboxamide 95 N-[(2R,3S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-5-oxo-2-phenylpyrrolidin-3-yl]-5-methylthiazole-4-carboxamide 96 N-[(2R,3S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-5-oxo-2-phenylpyrrolidin-3-yl]pyrimidine-2-carboxamide 97 N-[(2R,3S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-5-oxo-2-phenylpyrrolidin-3-yl]nicotinamide 98 N-[(2R,3S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-5-oxo-2-phenylpyrrolidin-3-yl]oxetane-3-carboxamide 99 N-[(2R,3S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-5-oxo-2-phenylpyrrolidin-3-yl]thiazole-5-sulfonamide 100 N-[rac-(2R,3R)-2-(5-chlorothiophen-2-yl)-1-[1-(4-fluorophenyl)indazol-5-yl]-5-oxopyrrolidin-3-yl]cyclopropanesulfonamide 101 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)pyrazolo[3,4-b]pyridin-5-yl]-5-oxo-2-phenylpyrrolidin-3-yl]propanamide 102 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)pyrazolo[3,4-c]pyridin-5-yl]-5-oxo-2-phenylpyrrolidin-3-yl]propanamide 103 2,2-difluoro-N-[rac-(2R,3S)-1-[1-(4-fluorophenyl)pyrazolo[4,3-b]pyridin-5-yl]-5-oxo-2-phenylpyrrolidin-3-yl]propanamide in each case in the form of the free compound or a physiologically acceptable salt thereof.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 98.0
- Lexical Diversity: 1.19444
- Patent Class: 546.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['16223845', '14409133', '13522823', '13272079', '12307526']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8062793705062651
- 35 USC 102 Novelty (BERT): 0.5694667968748739
- Combined Prediction Score: 0.7825981131431259
- Mean Citation Score: 346.2803560000001
- Max Citation Score: 450.94534
- Similarity Product: 404.74418312697526

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