PATENT CLAIM ANALYSIS

Application Number: 16223845
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-06
Patent Classification: ["514", "338000"]

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 1):
A compound according to general formula (I), wherein R 1  represents \u2014C 1-10 -alkyl; \u2014C 3-10 -cycloalkyl; \u2014C 1-6 -alkylene-C 3-10 -cycloalkyl; 3 to 7 membered heterocycloalkyl; \u2014C 1-6 -alkylene-(3 to 7 membered heterocycloalkyl); aryl; \u2014C 1-6 -alkylene-aryl; 5 or 6-membered heteroaryl; or \u2014C 1-6 -alkylene-(5 or 6-membered heteroaryl); R 2  represents \u2014C(\u2550O)\u2014C 1-10 -alkyl; \u2014C(\u2550O)\u2014C 3-10 -cycloalkyl; \u2014C(\u2550O)\u2014C 1-6 -alkylene-C 3-10 -cycloalkyl; \u2014C(\u2550O)-(3 to 7 membered heterocycloalkyl); \u2014C(\u2550O)\u2014C 1-6 -alkylene-(3 to 7 membered heterocycloalkyl); \u2014C(\u2550O)-aryl; \u2014C(\u2550O)\u2014C 1-6 -alkylene-aryl; \u2014C(\u2550O)-(5 or 6-membered heteroaryl); \u2014C(\u2550O)\u2014C 1-6 -alkylene-(5 or 6-membered heteroaryl); \u2014S(\u2550O)-2-C 1-10 -alkyl; \u2014S(\u2550O) 1-2 \u2014C 3-10 -cycloalkyl; \u2014S(\u2550O) 1-2 \u2014C 1-6 -alkylene-C 3-10 -cycloalkyl; \u2014S(\u2550O) 1-2 -(3 to 7 membered heterocycloalkyl); \u2014S(\u2550O) 1-2 \u2014C 1-6 -alkylene-(3 to 7 membered heterocycloalkyl); \u2014S(\u2550O) 1-2 -aryl; \u2014S(\u2550O) 1-2 \u2014C 1-6 -alkylene-aryl; \u2014S(\u2550O) 12 -(5 or 6-membered heteroaryl); or \u2014S(\u2550O) 1-2 \u2014C 1-6 -alkylene-(5 or 6-membered heteroaryl); R 3  represents 3 to 7 membered heterocycloalkyl; \u2014C 1-6 -alkylene-(3 to 7 membered heterocycloalkyl); 5 or 6-membered heteroaryl; \u2014C 1-6 -alkylene-(5 or 6-membered heteroaryl); \u2014C(\u2550O)-(3 to 7 membered heterocycloalkyl); \u2014C(\u2550O)\u2014C 1-6 -alkylene-(3 to 7 membered heterocycloalkyl); \u2014C(\u2550O)-(5 or 6-membered heteroaryl); \u2014C(\u2550O)\u2014C 1-6 -alkylene-(5 or 6-membered heteroaryl); \u2014S(\u2550O) 1-2 -(3 to 7 membered heterocycloalkyl); \u2014S(\u2550O) 1-2 \u2014C 1-6 -alkylene-(3 to 7 membered heterocycloalkyl); \u2014S(\u2550O) 1-2 -(5 or 6-membered heteroaryl); or \u2014S(\u2550O) 1-2 \u2014C 1-6 -alkylene-(5 or 6-membered heteroaryl); R 4  represents \u2014H; \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014CN; \u2014CH 3 ; \u2014CF 3 ; \u2014CF 2 H; \u2014CFH 2  or cyclopropyl; X represents N or CR 5 ; wherein R 5  represents \u2014H; \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014CN; \u2014C 1-10 -alkyl or \u2014C 3-10 -cycloalkyl; Y represents N or CR 6 ; wherein R 6  represents \u2014H; \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014CN; \u2014C 1-10 -alkyl or \u2014C 3-10 -cycloalkyl; Z represents N or CR 7 ; wherein R 7  represents \u2014H; \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014CN; \u2014C 1-10 -alkyl or \u2014C 3-10 -cycloalkyl; wherein \u2014C 1-10 -alkyl, \u2014C 1-4 -alkyl and \u2014C 1-6 -alkylene- in each case independently from one another is linear or branched, saturated or unsaturated; wherein \u2014C 1-10 -alkyl, \u2014C 1-4 -alkyl, \u2014C 1-6 -alkylene-, \u2014C 3-10 -cycloalkyl and 3 to 7 membered heterocycloalkyl in each case independently from one another are unsubstituted or mono- or polysubstituted with one or more substituents selected from \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014CN; \u2014C 1-6 -alkyl; \u2014CF 3 ; \u2014CF 2 H; \u2014CFH 2 ; \u2014CF 2 Cl; \u2014CFCl 2 ; \u2014C(\u2550O)\u2014C 1-6 -alkyl; \u2014C(\u2550O)\u2014OH; \u2014C(\u2550O)\u2014OC 1-6 -alkyl; \u2014C(\u2550O)\u2014NH 2 ; \u2014C(\u2550O)\u2014NH(C 1-6 -alkyl); \u2014C(\u2550O)\u2014N(C 1-6 -alkyl) 2 ; \u2014OH; \u2550O; \u2014OCF 3 ; \u2014OCF 2 H; \u2014OCFH 2 ; \u2014OCF 2 Cl; \u2014OCFCl 2 ; \u2014O\u2014C 1-6 -alkyl; \u2014O\u2014C(\u2550O)\u2014C 1-6 -alkyl; \u2014O\u2014C(\u2550O)\u2014O\u2014C 1-6 -alkyl; \u2014O\u2014(CO)\u2014NH(C 1-6 -alkyl); \u2014O\u2014C(\u2550O)\u2014N(C 1-6 -alkyl) 2 ; \u2014O\u2014S(\u2550O) 2 \u2014NH 2 ; \u2014O\u2014S(\u2550O) 2 \u2014NH(C 1-6 -alkyl); \u2014O\u2014S(\u2550O) 2 \u2014N(C 1-6 -alkyl) 2 ; \u2014NH 2 ; \u2014NH(C 1-6 -alkyl); \u2014N(C 1-6 -alkyl) 2 ; \u2014NH\u2014C(\u2550O)\u2014C 1-6 -alkyl; \u2014NH\u2014C(\u2550O)\u2014O\u2014C 1-6 -alkyl; \u2014NH\u2014C(\u2550O)\u2014NH 2 ; \u2014NH\u2014C(\u2550O)\u2014NH(C 1-6 -alkyl); \u2014NH\u2014C(\u2550O)\u2014N(C 1-6 -alkyl) 2 ; \u2014N(C 1-6 -alkyl)-C(\u2550O)\u2014C 1-6 -alkyl; \u2014N(C 1-6 -alkyl)-C(\u2550O)\u2014O\u2014C 1-6 -alkyl; \u2014N(C 1-6 -alkyl)-C(\u2550O)\u2014NH 2 ; \u2014N(C 1-6 -alkyl)-C(\u2550O)\u2014NH(C 1-6 -alkyl); \u2014N(C 1-6 -alkyl)-C(\u2550O)\u2014N(C 1-6 -alkyl) 2 ; \u2014NH\u2014S(\u2550O) 2 OH; NH\u2014S(\u2550O) 2 \u2014C 1-6 -alkyl; \u2014NH\u2014S(\u2550O) 2 \u2014O\u2014C 1-6 -alkyl; \u2014NH\u2014S(\u2550O) 2 \u2014NH 2 ; \u2014NH\u2014S(\u2550O) 2 \u2014NH(C 1-6 -alkyl); \u2014NH\u2014S(\u2550O) 2 N(C 1-6 -alkyl) 2 ; \u2014N(C 1-6 -alkyl)-S(\u2550O) 2 \u2014OH; \u2014N(C 1-6 -alkyl)-S(\u2550O) 2 \u2014C 1-6 -alkyl; \u2014N(C 1-6 -alkyl)-S(\u2550O) 2 \u2014O\u2014C 1-6 -alkyl; \u2014N(C 1-6 -alkyl)-S(\u2550O) 2 \u2014NH 2 ; \u2014N(C 1-6 -alkyl)-S(\u2550O) 2 \u2014NH(C 1-6 -alkyl); \u2014N(C 1-6 -alkyl)-S(\u2550O) 2 \u2014N(C 1-6 -alkyl) 2 ; \u2014SCF 3 ; \u2014SCF 2 H; \u2014SCFH 2 ; \u2014S\u2014C 1-6 -alkyl; \u2014S(\u2550O)\u2014C 1-6 -alkyl; \u2014S(\u2550O) 2 \u2014C 1-6 -alkyl; \u2014S(\u2550O) 2 \u2014OH; \u2014S(\u2550O) 2 \u2014O\u2014C 1-6 -alkyl; \u2014S(\u2550O) 2 \u2014NH 2 ; \u2014S(\u2550O) 2 \u2014NH(C 1-6 -alkyl); \u2014S(\u2550O) 2 \u2014N(C 1-6 -alkyl) 2 ; \u2014C 3-6 -cycloalkyl; 3 to 6-membered heterocycloalkyl; phenyl; 5 or 6-membered heteroaryl; \u2014O\u2014C 3-6 -cycloalkyl; \u2014O-(3 to 6-membered heterocycloalkyl); \u2014O-phenyl; \u2014O-(5 or 6-membered heteroaryl); \u2014C(\u2550O)\u2014C 3-6 -cycloalkyl; \u2014C(\u2550O)-(3 to 6-membered heterocycloalkyl); \u2014C(\u2550O)-phenyl; \u2014C(\u2550O)-(5 or 6-membered heteroaryl); \u2014S(\u2550O) 2 \u2014(C 3-6 -cycloalkyl); \u2014S(\u2550O) 2 -(3 to 6-membered heterocycloalkyl); \u2014S(\u2550O) 2 -phenyl or \u2014S(\u2550O) 2 -(5 or 6-membered heteroaryl); wherein aryl and 5 or 6-membered heteroaryl in each case independently from one another are unsubstituted or mono- or polysubstituted with one or more substituents selected from \u2014F; \u2014Cl; \u2014Br; \u2014I; \u2014CN; \u2014C 1-6 -alkyl; \u2014CF 3 ; \u2014CF 2 H; \u2014CFH 2 ; \u2014CF 2 Cl; \u2014CFCl 2 ; \u2014C 1-4 -alkylene-CF 3 ; \u2014C 1-4 -alkylene-CF 2 H; \u2014C 1-4 -alkylene-CFH 2 ; \u2014C(\u2550O)\u2014C 1-6 -alkyl; \u2014C(\u2550O)\u2014OH; \u2014C(\u2550O)\u2014OC 1-6 -alkyl; \u2014C(\u2550O)\u2014NH(OH); \u2014C(\u2550O)\u2014NH 2 ; \u2014C(\u2550O)\u2014NH(C 1-6 -alkyl); \u2014C(\u2550O)\u2014N(C 1-6 -alkyl) 2 ; \u2014OH; \u2550O; \u2014OCF 3 ; \u2014OCF 2 H; \u2014OCFH 2 ; \u2014OCF 2 Cl; \u2014OCFCl 2 ; \u2014O\u2014C 1-6 -alkyl; \u2014O\u2014C 3-6 -cycloalkyl; \u2014O-(3 to 6-membered heterocycloalkyl); \u2014NH 2 ; \u2014NH(C 1-6 -alkyl); \u2014N(C 1-6 -alkyl) 2 ; \u2014NH\u2014C(\u2550O)\u2014C 1-6 -alkyl; \u2014N(C 1-6 -alkyl)-C(\u2550O)\u2014C 1-6 -alkyl; \u2014NH\u2014C(\u2550O)\u2014NH 2 ; \u2014NH\u2014C(\u2550O)\u2014NH(C 1-6 -alkyl); \u2014NH\u2014C(\u2550O)\u2014N(C 1-6 -alkyl) 2 ; \u2014N(C 1-6 -alkyl)-C(\u2550O)\u2014NH(C 1-6 -alkyl); \u2014N(C 1-6 -alkyl)-C(\u2550O)\u2014N(C 1-6 -alkyl) 2 ; \u2014NH\u2014S(\u2550O) 2 \u2014C 1-6 -alkyl; \u2014SCF 3 ; \u2014S\u2014C 1-6 -alkyl; \u2014S(\u2550O)\u2014C 1-6 -alkyl; \u2014S(\u2550O) 2 \u2014C 1-6 -alkyl; \u2014S(\u2550O) 2 \u2014NH 2 ; \u2014S(\u2550O) 2 \u2014NH(C 1-6 -alkyl); \u2014S(\u2550O) 2 \u2014N(C 1-6 -alkyl) 2 ; \u2014C 3-6 -cycloalkyl; \u2014C 1-4 -alkylene-C 3-6 -cycloalkyl; 3 to 6-membered heterocycloalkyl; \u2014C 1-4 -alkylene-(3 to 6-membered heterocycloalkyl); phenyl or 5 or 6-membered heteroaryl; in the form of the free compound or a physiologically acceptable salt thereof.

Metadata:
- Claim Count in Document: 26.0
- Percentile: 98.0
- Lexical Diversity: 1.19444
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['14409133', '14383096', '14112581', '13272079', '12558426']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7748578443253461
- 35 USC 102 Novelty (BERT): 0.5312393477872935
- Combined Prediction Score: 0.7504959946715408
- Mean Citation Score: 311.029172
- Max Citation Score: 328.6948
- Similarity Product: 230.4220996750832

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