PATENT CLAIM ANALYSIS

Application Number: 15982038
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-09
Patent Classification: ["514", "249000"]

Abstract:
The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.

Claim (Index 9):
A compound according to Formula (IX): or a stereoisomer, tautomer, pharmaceutically acceptable salt thereof, wherein:\n ring A is C 3-10  carbocycle; \n L is selected from the group consisting of: a bond, \u2014CHR 10 CHR 10 \u2014, \u2014CR 10 \u2550CR 10 \u2014, and \u2014C\u2261C\u2014; \n R 1 , at each occurrence, is selected from the group consisting of: H, halo, C 1-2  alkyl, \u2014O(C 1-4  alkyl), CN, \u2014CH 2 NH 2 , and \u2014C(\u2550NH)NH 2 ; \n R 2  is independently selected from the group consisting of: H, halo, CN, OH C 1-6  alkyl, C 1-4  alkoxy, C 1-6 haloalkyl, C 1-6 haloalkoxy, CO(C 1-4  alkyl), CONH 2 , CO 2 H and a 5- to 7-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NH, N(C 1-4  alkyl), O, and S(O) p , wherein said heterocycle is substituted with 1-2 R 2a ; \n R 2a , at each occurrence, is selected from the group consisting of: H, halo, C 1-4  alkyl, CO 2 H, \u2014CO 2 (C 1-4  alkyl), \u2014CONH 2 , \u2014CH 2 OH, \u2014CH 2 OC 1-4 alkyl, and \u2014CH 2 NH 2 ; \n R 3  is selected from the group consisting of: C 1-6  alkyl substituted with 1-3 R 3a , C 3-10  carbocycle substituted with 1-3 R 3a , and 5-10 membered heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of N, NR 7 , O, and S(O) p ; wherein said heterocycle is substituted with 1-3 R 3a ; \n R 3a , at each occurrence, is selected from the group consisting of: H, halo, C 1-4  alkyl, \u2014OH, C 1-4  alkoxy, \u2014CN, \u2014NH 2 , \u2014NH(C 1-4  alkyl), \u2014N(C 1-4  alkyl) 2 , \u2014CO 2 H, \u2014CH 2 CO 2 H, \u2014CO 2 (C 1-4  alkyl), \u2014CO 2 \u2014C 1-4  alkylene-O(C 1-4  alkyl), \u2014CO 2 \u2014C 1-4  alkylene-N(C 1-4  alkyl) 2 , \u2014CO 2 \u2014C 1-4  alkylene-O\u2014C 1-4  alkylene-N(C 1-4  alkyl) 2 , \u2014CO 2 \u2014C 1-4  alkylene-O\u2014C 1-4  alkylene-O(C 1-4  alkyl), \u2014CONH 2 , \u2014CONH(C 1-6  alkyl), \u2014CON(C 1-4  alkyl) 2 , \u2014CONH\u2014C 1-4  alkylene-CO 2 (C 1-4  alkyl), \u2014CONHCO 2 C 1-4  alkyl, \u2014CONH\u2014C 1-4  alkylene-NHCO(C 1-4  alkyl), \u2014CONH\u2014C 1-4  alkylene-CONH 2 , \u2014NHCOC 1-4  alkyl, \u2014NHCO 2 (C 1-4  alkyl), R c , \u2014CONHR c , and \u2014CO 2 R c ; \n R 4 , at each occurrence, is selected from the group consisting of: H, halo, and C 1-4  alkyl; \n R 5  is selected from the group consisting of: H, halo, C 1-4  alkyl substituted with 0-2 R b , C 2-4  alkenyl substituted with 0-2 R b , \u2014OH, \u2014CN, \u2014NH 2 , \u2014N(C 1-4  alkyl) 2 , \u2014OCO(C 1-4  alkyl), \u2014O\u2014C 1-4  alkylene-O(C 1-4  alkyl), \u2014O\u2014C 1-4  alkylene-N(C 1-4  alkyl) 2 , \u2014CO 2 H, \u2014CO 2 (C 1-4  alkyl), \u2014CONH 2 , \u2014(CH 2 ) 2 CONH 2 , \u2014CONR 9 (C 1-4  alkyl), \u2014CON(C 1-4  alkyl) 2 , \u2014CONR 9 \u2014C 1-4  alkylene-O(C 1-4  alkyl), \u2014CONR 9 \u2014C 1-4  alkylene-N(C 1-4  alkyl) 2 , \u2014CONR 9 \u2014C 1-4  alkylene-CO 2 (C 1-4  alkyl), \u2014NR 9 COC 1-4  alkyl, \u2014NR 9 CO 2 C 1-4  alkyl, \u2014NR 9 CONH(C 1-4  alkyl), \u2014NR 9 CONR 9 \u2014C 1-4  alkylene-CO 2 C 1-4  alkyl, \u2014NR 9 \u2014C 1-4  alkylene-N(C 1-4  alkyl) 2 , \u2014NR 9 SO 2 (C 1-4  alkyl), \u2014S(C 1-4  alkyl), \u2014SO 2 (C 1-4  alkyl), \u2014SO 2 NH 2 , R 8 , C 2-4  alkenylene-R 8 , \u2014OR 8 , \u2014COR 8 , C 2-4  alkenylene-COR 8 , \u2014CONR 9 R 8 , \u2014NR 9 COR 8 , \u2014NR 9 CO 2 R 8 , and \u2014NR 9 CONR 9 R 8 ; \n R 7 , at each occurrence, is selected from the group consisting of: H, C 1-4  alkyl, COC 1-4  alkyl, CO 2 (C 1-4  alkyl), CO 2 Bn, \u2014CONH\u2014C 1-4  alkylene-CO 2 C 1-4  alkyl, phenyl, benzyl, and \u2014CO 2 \u2014C 1-4  alkylene-aryl; \n R 8 , at each occurrence, is selected from the group consisting of: \u2014(CH 2 ) n \u2014C 3-10  carbocycle and \u2014(CH 2 ) n -5- to 10-membered heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NR a , O, and S(O) p ; wherein said carbocycle or heterocycle is substituted with 0-3 R b ; \n R 9 , at each occurrence, is selected from the group consisting of: H and C 1-4 alkyl; \n R 10 , at each occurrence, is selected from the group consisting of: H, halo, OH, and C 1-4  alkyl; \n R a  is selected from the group consisting of: H, C 1-4  alkyl, \u2014(CH 2 ) n OH, CO(C 1-4  alkyl), COCF 3 , CO 2 (C 1-4  alkyl), \u2014CONH 2 , \u2014CONH\u2014C 1-4  alkylene-CO 2 (C 1-4  alkyl), C 1-4  alkylene-CO 2 (C 1-4  alkyl), R c , CO 2 R c , and CONHR c ; \n R b  is selected from the group consisting of: \u2550O, halo, C 1-4  alkyl, C 1-4  alkoxy, OCF 3 , NH 2 , NO 2 , N(C 1-4  alkyl) 2 , CO(C 1-4  alkyl), CO(C 1-4  haloalkyl), CO 2 (C 1-4  alkyl), CONH 2 , \u2014CONH(C 1-4  alkyl), \u2014CON(C 1-4  alkyl) 2 , \u2014CONH\u2014C 1-4  alkylene-O(C 1-4  alkyl), \u2014CONH\u2014C 1-4  alkylene-N(C 1-4  alkyl) 2 , \u2014CONH\u2014C 1-4  alkylene-N + (C 1-4  alkyl) 2 -C 1-4  alkylene-O\u2014P(O)(OH) 2 , \u2014NHCO 2 (C 1-4  alkyl), \u2014R c , COR c , CO 2 R c , and CONHR c ; \n R c  is, independently at each occurrence, selected from the group consisting of: \u2014(CH 2 ) n \u2014C 3-6  cycloalkyl, \u2014(CH 2 ) n -phenyl, and \u2014(CH 2 ) n -5- to 6-membered heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4  alkyl), O, and S(O) p ; wherein each ring moiety is substituted with 0-2 R d ; \n R d  is selected from the group consisting of: \u2550O, halo, \u2014OH, C 1-4  alkyl, NH 2 , NH(C 1-4  alkyl), N(C 1-4  alkyl) 2 , C 1-4  alkoxy, and \u2014NHCO(C 1-4  alkyl), and heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4  alkyl), O, and S(O) p ; \n n, at each occurrence, is selected from 0, 1, 2, 3, and 4; \n p, at each occurrence, is selected from 0, 1, and 2;

Metadata:
- Claim Count in Document: 23.0
- Percentile: 93.0
- Lexical Diversity: 1.17949
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15643891', '15183051', '14799681', '14350411', '14350417']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7912983902153643
- 35 USC 102 Novelty (BERT): 0.5077444282846812
- Combined Prediction Score: 0.762942994022296
- Mean Citation Score: 315.033496
- Max Citation Score: 316.3271200000001
- Similarity Product: 310.860917462721

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