PATENT CLAIM ANALYSIS

Application Number: 16088852
Application Type: Utility
Filing Date: 2018-09
Publication Date: 2019-04
Patent Classification: ["546", "270700"]

Abstract:
The invention relates to novel compounds of the Formula (I), to a process for their preparation and to their use as medicaments, in particular as antiviral medicaments.

Claim (Index 1):
A compound represented by Formula (I) or an enantiomer, diastereomer, tautomer, N-oxide, solvate, formulation and pharmaceutically acceptable salt thereof, wherein: X is selected from R 1  is selected from H, halogen, C 1-6 -alkyl, C 3-6 -cycloalkyl, halo-C 3-6 -cycloalkyl, \u2014O-halo-C 1-6 -alkyl and \u2014NH\u2014C 1-6 -alkyl, with the proviso that in the case that X is one of then R 1  is not hydrogen (H);\n R 2  is selected from H, \u2014ON, \u2014NO 2 , C 1-10 -alkyl, C 2-10 -alkenyl, C 2-10 -alkynyl, C 0-10 -alkylene-C 3-10 -cycloalkyl, C 0-10 -alkylene-C 3-10 -heterocycloalkyl, C 0-10 -alkylene-(5- to 10-membered heteroaryl), C 0-10 -alkylene-(6- to 10-membered aryl), C 0-10 -alkylene-(6- to 10-membered heteroaryl), C 0-10 -alkylene-OR 11 , C 0-10 -alkylene-CO 2 R 11 , C 0-10 -alkylene-C(\u2550O)NR 11 R 12 , C 0-10 -alkylene-C(\u2550S)NR 11 R 12 , C 0-10 -alkylene-C(\u2550O)NR 11 SO 2 R 13 , C 0-10 -alkylene-C(\u2550S)NR 11 SO 2 R 11 , C 0,10 -alkylene-C(\u2550O)R 11 , C 0-10 -alkylene-C(\u2550S)R 11 , C 0-10 -alkylene-SR 11 , C 0-10 -alkylene-SO x R 13 , C 0-10 -alkylene-SO 3 R 11 , C 0-10 -alkylene-SO 2 NR 11 R 12 , C 0-10 -alkylene-NR 11 C(\u2550O)R 11 , C 0-10 -alkylene-NR 11 C(\u2550S)R 11 , C 0-10 -alkylene-NR 11 SO 2 R 13 , C 0-10 -alkylene-NR 11 C(\u2550O)NR 11 R 12 , C 0-10 -alkylene-NR 11 C(\u2550S)NR 11 R 12 , C 0-10 -alkylene-NR 11 SO 2 NR 11 R 12 , C 0-10 -alkylene-NR 11 R 12 , wherein alkyl, alkenyl, alkynyl, alkylene, cycloalkyl, heterocycloalkyl, aryl and heteroaryl is unsubstituted or substituted with 1 to 7 substituents independently selected from the group consisting of oxo, CN, \u2014NO 2 , OR 11 , O\u2014C 2-6 -alkylene-OR 11 , halo-C 1-6 -alkyl, halogen, CO 2 R 11 , C(\u2550O)NR 11 R 12 , C(\u2550O)NR 11 SO 2 R 11 , C(\u2550O)R 11 , SR 11 , SO x R 11 , SO 3 R 11 , P(\u2550O)(OR 11 ) 2 , SO 2 NR 11 R 12 , NR 11 C(\u2550O)R 11 , NR 11 SO 2 R 13 , NR 11 C(\u2550O)NR 11 R 12 , NR 11 SO 2 NR 11 R 12 , C 3-10 -cycloalkyl, O\u2014C 3-10 -cycloalkyl, C 3-10 -heterocycloalkyl, O\u2014C 3-10 -heterocycloalkyl and NR 11 R 12 ; \n R 3  is selected from H, C 1-6  alkyl, halo-C 1-6 -alkyl, \u2014O\u2014C 1-6 -alkyl, \u2014O-halo-C 1-6 -alkyl, C 3-6 -cycloalkyl and C 3-6 -heterocycloalkyl, wherein alkyl, cycloalkyl and heterocycloalkyl are optionally substituted with 1 to 5 substituents independently selected from halogen, \u2014CN, OH, oxo, C 1-3 -alkyl, halo-C 1-3 -alkyl, O\u2014C 1-3 -alkyl, O-halo-C 1-3 -alkyl, SO 2 \u2014C 1-3 -alkyl, CO 2 H; \n or R 2  and R 3  when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 4 substituents independently selected from the group consisting of halogen, \u2014CN, \u2014NO 2 , OH, oxo, alkyl, O-halo-C 1-3 -alkyl, SO 2 \u2014C 1-3 -alkyl, CO 2 H; \n R 4  is selected from H, C 1-6 -alkyl, C 1-6 -acyl, C 2-6 -alkenyl, C 3-8 -cycloalkyl and C 3-8 -heterocycloalkyl, wherein alkyl, acyl, alkenyl, cycloalkyl and heterocycloalkyl are optionally substituted with 1 to 5 substituents independently selected from halogen, \u2014CN, OH, oxo, C 1-3 -alkyl, halo-C 1-3 -alkyl, O\u2014C 1-3 -alkyl, O-halo-C 1-3 -alkyl; \n R 5  and R 6  and R 5\u2032  and R 6\u2032  are independently selected from H, halogen, C 1-6 -alkyl, NH 2 , NHC 1-6 -alkyl, N(C 1-6 -alkyl) 2 , C 0-6 -alkylene-C(\u2550O)NH 2 ; \n or R 5  and R 6  and R 5\u2032  and R 6\u2032  independently when taken together with the carbon to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 4 substituents independently selected from the group consisting of halogen, \u2014CN, \u2014NO 2 , OH, oxo, C 1-3 -alkyl, halo-C 1-3 -alkyl, O\u2014C 1-3 -alkyl, O-halo-C 1-3 -alkyl, SO 2 \u2014C 1-3 -alkyl, CO 2 H; \n or R 5  and R 5\u2032  and R 6  and R 6\u2032  independently when taken together with the two adjacent carbon to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 4 substituents independently selected from the group consisting of halogen, \u2014CN, \u2014NO 2 , OH, oxo, C 1-3 -alkyl, halo-C 1-3 -alkyl, O\u2014C 1-3 -alkyl, O-halo-C 1-3 -alkyl, SO 2 \u2014C 1-3 -alkyl, CO 2 H; \n R 7  is selected from a 6-membered aryl and 5- or 6-membered heteroaryl, wherein aryl and heteroaryl are optionally substituted with 1 to 4 substituents independently selected from halogen, \u2014CN, \u2014NO 2 , OH, C 1-6 -alkyl, O\u2014C 1-6 -alkyl, C 3-6 -cycloalkyl, O\u2014C 3-6 -cycloalkyl, C 3-6 -heterocycloalkyl, O\u2014C 3-6 -heterocycloalkyl, SO y \u2014C 1-6 -alkyl, CO 2 H, C(\u2550O)O\u2014C 1-6 -alkyl, 6- to 10-membered aryl, 5- or 10-membered heteroaryl, O-(6- to 10-membered aryl) and O-(5- or 10-membered heteroaryl), wherein alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl are optionally substituted with 1 to 5 substituents independently selected from halogen, \u2014CN, \u2014NO 2 , OH, R 13 , OR 13 , CO 2 R 11 , NR 11 R 12 , C(\u2550O)R 11 , C(\u2550S)R 11 , C(\u2550O)NR 11 R 12 , NR 11 C(\u2550O)NR 11 R 12 , NR 11 C(\u2550O)OR 13 , OC(\u2550O)NR 11 R 12 , C(\u2550S)NR 11 R 12 , NR 11 C(\u2550S)NR 11 R 12 , NR 11 C(\u2550S)OR 13 , OC(\u2550S)NR 11 R 12 ; SO y \u2014C 1-6 -alkyl, SO y -halo-C 1-6 -alkyl, SR 11 , SO x R 13 , SO 3 R 11 , SO 2 NR 11 R 12 , NR 11 SO 2 R 13 , NR 11 SO 2 NR 11 R 12 ; \n R 8  is selected from H, \u2014CN, \u2014NO 2 , C 1-10 -alkyl, C 2-10 -alkenyl, C 2-10 -alkynyl, C 0-10 -alkylene-C 3-10 -cycloalkyl, C 0-10 -alkylene-C 3-10 -heterocycloalkyl, C 0-10 -alkylene-(5 to 10-membered heteroaryl), C 0-10 -alkylene-(6 to 10-membered aryl), C 0-10 -alkylene-(6 to 10-membered heteroaryl), C 0-10 -alkylene-OR 11 , C 0-10 -alkylene-CO 2 R 11 , C 0-10 -alkylene-C(\u2550O)NR 11 R 12 , C 0-10 -alkylene-C(\u2550S)NR 11 R 12 , C 0-10 -alkylene-C(\u2550O)NR 11 SO 2 R 13 , C 0-10 -alkylene-C(\u2550S)NR 11 SO 2 R 11 , C 0-10 -alkylene-C(\u2550O)R 11 , C 0-10 -alkylene-C(\u2550S)R 11 , C 0-10 -alkylene-SR 11 , C 0-10 -alkylene-SO x \u2014R 13 , C 0-10 -alkylene-SO 3 R 11 , C 0-10 -alkylene-SO 2 NR 11 R 12 , C 0-10 -alkylene-NR 11 C(\u2550O)R 11 , C 0-10 -alkylene-NR 11 C(\u2550S)R 11 , C 0-10 -alkylene-NR 11 SO 2 R 11 , C 0-10 -alkylene-NR 11 C(\u2550O)NR 11 R 12 , C 0-10 -alkylene-NR 11 C(\u2550S)NR 11 R 12 , C 0-10 -alkylene-NR 11 \u2014SO 2 \u2014NR 11 R 12 , C 0-10 -alkylene-NR 11 R 12 , wherein alkyl, alkenyl, alkynyl, alkylene, cycloalkyl, heterocycloalkyl, aryl and heteroaryl is unsubstituted or substituted with 1 to 7 substituents independently selected from the group consisting of oxo, CN, \u2014NO 2 , OR 11 , O\u2014C 2-6 -alkylene-OR 11 , C 1-6 -alkyl, halo-C 1-6 -alkyl, halogen, CO 2 R 11 , CONR 11 R 12 , CONR 11 SO 2 R 11 , COR 11 , SO x R 11 , SO 3 H, PO(OH) 2 , SO 2 NR 11 R 12 , NR 11 COR 11 , NR 11 SO 2 R 11 , NR 11 \u2014CO_NR 11 R 12 , NR 11 \u2014SO 2 \u2014NR 11 R 12 , C 3-10 -cycloalkyl, O\u2014C 3-10 -cycloalkyl, C 1-10 -heterocycloalkyl, O\u2014C 3-10 -heterocycloalkyl and NR 11 R 12 ; \n R 9  is selected from C 1-10 -alkyl, C 2-10 -alkenyl, C 2-10 -alkynyl, C 0-10 -alkylene-C 3-10 -cycloalkyl, C 0-10 -alkylene-C 3-10 -heterocycloalkyl, C 0-10 -alkylene-(5- to 10-membered heteroaryl), C 0-10 -alkylene-(6- to 10-membered aryl), C 0-10 -alkylene-(6- to 10-membered heteroaryl), C 0-10 -alkylene-OR 11 , C 0-10 -alkylene-CO 2 R 11 , C 0-10 -alkylene-C(\u2550O)NR 11 R 12 , C 0-10 -alkylene-C(\u2550S)NR 11 R 12 , C 0-10 -alkylene-C(\u2550O)NR 11 SO 2 R 13 , C 0-10 -alkylene-C(\u2550S)NR 11 SO 2 R 11 , C 0-10 -alkylene-C(\u2550O)R 11 , C 0-10 -alkylene-C(\u2550S)R 11 , C 0-10 -alkylene-SR 11 , C 0-10 -alkylene-SO x R 13 , C 0-10 -alkylene-SO 3 R 11 , C 0-10 -alkylene-SO 2 NR 11 R 12 , C 0-10 -alkylene-NR 11 C(\u2550O)R 11 , C 0-10 -alkylene-NR 11 C(\u2550S)R 11 , C 0-10 -alkylene-NR 11 SO 2 R 13 , C 0-10 -alkylene-NR 11 C(\u2550O)NR 11 R 12 , C 0-10 -alkylene-NR 11 C(\u2550S)NR 11 R 12 , C 0-10 -alkylene-NR 11 SO 2 NR 11 R 12 , C 0-10 -alkylene-NR 11 R 12 , wherein alkyl, alkenyl, alkynyl, alkylene, cycloalkyl, heterocycloalkyl, aryl and heteroaryl is unsubstituted or substituted with 1 to 7 substituents independently selected from the group consisting of oxo, CN, \u2014NO 2 , OR 11 , O\u2014C 2-6 -alkylene-OR 11 , C 1-6 -alkyl, halo-C 1-6 -alkyl, halogen, CO 2 R 11 , C(\u2550O)NR 11 R 12 , C(\u2550O)NR 11 SO 2 R 11 , C(\u2550O)R 11 , SR 11 , SO x R 11 , SO 3 R 11 , P(\u2550O)(OR 11 ) 2 , SO 2 NR 11 R 12 , NR 11 C(\u2550O)R 11 , NR 11 SO 2 R 13 ; NR 11 C(\u2550O)NR 11 R 12 , NR 11 SO 2 NR 11 R 12 , C 3-10 -cycloalkyl, O\u2014C 1-10 -cycloalkyl, C 3-10 -heterocycloalkyl, O\u2014C 3-10 -heterocycloalkyl and NR 11 R 12 ; \n R 10  is selected from \u2014CN, OH, and \u2014NO 2 ; \n R 11  is independently selected from H, C 1-6 -alkyl, C 0-6 -alkylene-C 3-10 -cycloalkyl and C 0-6 -alkylene-C 3-10 -heterocycloalkyl, wherein alkyl, alkylene, cycloalkyl and heterocycloalkyl is unsubstituted or substituted with 1 to 6 substituents independently selected from the group consisting of halogen, \u2014CN, OH, oxo, C 1-3 -alkyl, halo-C 1-3 -alkyl, O\u2014C 1-3 -alkyl, O-halo-C 1-3 -alkyl, NH 2 , NH(C 1-3 -alkyl), N(C 1-3 -alkyl) 2 , C 3-6 -heterocycloalkyl, C 3-6 -cycloalkyl, SO 2 \u2014NHC 1-3 -alkyl, SO 2 \u2014N(C 1-3 -alkyl) 2  and SO 2 \u2014C 1-3 -alkyl, wherein cycloalkyl and heterocycloalkyl is unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of F, OH, oxo, CH 3 , CHF 2  and CF 3 ; \n R 12  is independently selected from H, halo-C 1-6 -alkyl and C 3-6 -cycloalkyl; \n or R 11  and R 12  when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 4 substituents independently selected from the group consisting of halogen, \u2014CN, \u2014NO 2 , OH, oxo, C 1 -3 alkyl, halo C 1-3 -alkyl, O\u2014C 1-3 -alkyl, O-halo-O 1-3 -alkyl, SO 2 \u2014C 1-3 -alkyl, CO 2 H; \n R 13  is independently selected from C 1-6 -alkyl, C 0-6 -alkylene-C 3-10 -cycloalkyl and C 0-6 -alkylene-C 3-10 -heterocycloalkyl, wherein alkyl, alkylene, cycloalkyl and heterocycloalkyl is unsubstituted or substituted with 1 to 6 substituents independently selected from the group consisting of halogen, \u2014CN, OH, oxo, C 1-3 -alkyl, halo-C 1-3 -alkyl, O\u2014C 1-3 -alkyl, O-halo-C 1-3 -alkyl, NH 2 , NH(C 1-3 -alkyl), N(C 1-3 -alkyl) 2 , C 3-6 -heterocycloalkyl, C 3-6 -cycloalkyl, SO 2 \u2014NHC 1-3 -alkyl, SO 2 \u2014N(C 1-3 -alkyl) 2  and SO 2 \u2014C 1-3 -alkyl, wherein cycloalkyl and heterocycloalkyl is unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of F, OH, oxo, CH 3 , CHF 2  and CF 3 ; \n n is selected from 0 and 1; \n x is independently selected from 1 and 2; \n y is independently selected from 0, 1 and 2; \n and wherein optionally R 1  is connected to one residue selected from R 2 , R 3 , R 8 , R 9 , R 10  or R 12  to form a 5 to 8-membered heterocycle, which is optionally substituted with 1 to 4 substituents independently selected from the group consisting of halogen, \u2014ON, \u2014NO 2 , OH, oxo, C 1 -3 alkyl, halo C 1-3 -alkyl, O\u2014C 1-3 -alkyl, O-halo-C 1-3 -alkyl, SO 2 \u2014C 1-3 -alkyl, CO 2 H.

Metadata:
- Claim Count in Document: 50.0
- Percentile: 97.0
- Lexical Diversity: 1.23077
- Patent Class: 546.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14403903', '14419468', '14360905', '14359278', '12394083']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7905145063414242
- 35 USC 102 Novelty (BERT): 0.5077471520453525
- Combined Prediction Score: 0.762237770911817
- Mean Citation Score: 269.8413
- Max Citation Score: 283.72034
- Similarity Product: 221.5831554897476

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