PATENT CLAIM ANALYSIS

Application Number: 15756367
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2019-01
Patent Classification: ["514", "300000"]

Abstract:
The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.

Claim (Index 1):
The compound of the formula (I) or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof, wherein:\n ring A is a 5-membered heteroaryl comprising carbon atoms and 1-4 heteroatoms selected from N, NR 1 , O, and S; wherein said heteroaryl is substituted with 0-1 R 2  and 0-2 R 3 ; \n R 1  is independently selected from: H, C 1-4  alkyl substituted with 0-1 C 1-4  alkoxy, C 1-4  haloalkyl, SO 2 (C 1-4  alkyl), \u2014X 2 \u2014C 3-12  carbocycle and \u2014X 2 -(5- to 10-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 13 , O, and S); wherein said carbocycle and heterocycle are substituted with 0-1 R 6  and 0-2 R 7 ; \n R 2  is independently selected from: C 1-4  alkyl substituted with 0-1 OH, CN, CO 2 (C 1-4  alkyl), SO 2 (C 1-4  alkyl), and \u2014(CH 2 ) n R 4 ; \n R 3  is, independently at each occurrence, selected from: OH, halogen, C 1-4  alkyl, and C 1-4  haloalkyl; \n alternatively, when R 2  and one of the R 3 s are attached to two adjacent carbon atoms of ring A, they can be combined with the two attached carbon atoms to form a 5- to 6-membered carbocycle or heterocycle comprising carbon atoms and 0-3 additional heteroatoms selected from N, NR b , O, and S(O) p , wherein said carbocycle or heterocycle is substituted with 0-2 R a ; \n R 4  is, independently at each occurrence, selected from: C 3-6  cycloalkyl substituted with 0-3 R c , phenyl substituted with 0-4 R c , and 5- to 10-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR b , O, and S; wherein said heterocycle is substituted with 0-3 R c ; \n X 1  is independently selected from: a bond, CH 2 , C 1-4  alkylene, and CH 2 CO; \n X 2  is independently selected from: X 1  and CH(C 1-4  alkyl substituted 0-1 R 5 ); \n R 5  is independently selected from: OH and OSi(C 1-4  alkyl) 3 ; \n R 6  is independently selected from: \u2550O, halogen, C 1-4  alkyl substituted with 0-1 OH, C 1-4  haloalkyl, C 1-4  alkoxy, C 1-4  haloalkoxy, \u2014O(CH 2 ) 1-3 N(C 1-4  alkyl) 2 , CN, CO 2 H, NH 2 , \u2014CH 2 NH 2 , \u2014CH 2 N(C 1-4  alkyl) 2 , \u2014CH 2 NHCOCH 2 N(C 1-4  alkyl) 2 , CONR 8 R 9 , SO 2 (C 1-4  alkyl), \u2014(CH 2 ) n \u2014(O) n (CH 2 ) t \u2014R 10 , \u2014CO\u2014R 10 , and \u2014SO 2 \u2014R 10 ; \n R 7  is independently at each occurrence, selected from: halogen, CN, C 1-4  alkyl substituted with 0-1 OH, C 1-4  haloalkyl, C 1-4  alkoxy, and C 1-4  haloalkoxy; \n R 8  is independently selected from: H, C 1-4  alkyl substituted with 0-1 R d , \u2014X 3 \u2014R 10 ; \n X 3  is independently selected from: a bond, CH 2 , CH 2 CH 2 , CH 2 CH 2 CH 2 , and CH(C 1-4  alkyl); \n R 9  is independently selected from: H and C 1-4  alkyl; \n R 10  is, independently at each occurrence, selected from: C 3-10  carbocycle and 5- to 10-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR b , O, and S; wherein each ring moiety is substituted with 0-1 R 11  and 0-2 R a ; \n R a  is, independently at each occurrence, selected from: \u2550O, OH, CN, NH 2 , halogen, C 1-4  alkyl substituted with 0-1 OH, benzyl, C 1-4  alkoxy, C 1-4  haloalkyl, and C 1-4  haloalkoxy; \n R 11  is, independently at each occurrence, selected from: halogen, \u2550O, OH, CN, NH 2 , C 1-4  alkyl substituted with 0-1 R d , C 1-4  haloalkyl, C 1-4  alkoxy, C 1-4  haloalkoxy, \u2014CH 2 OBn, CO 2 (C 1-4  alkyl), CON(C 1-4  alkyl) 2 , \u2014CH 2 NHCH 2 CO 2 (C 1-4  alkyl), \u2014(CH 2 ) 0-1 -(phenyl substituted with 0-2 R 14 ), and \u2014(CH 2 ) 0-1 -(a 5- to 6-membered heteroaryl comprising carbon atoms and 1-2 heteroatoms selected from N, NR 1 , O, and S; wherein said heteroaryl is substituted with 0-2 R 14 ), \n R 12  is, independently at each occurrence, selected from: \u2014CO 2 CH 2 OCOCH 2 O(C 1-4  alkyl), \u2014CO 2 CH(C 1-4  alkyl)OCO(C 1-4  alkyl), and \n R 13  is, independently at each occurrence, selected from: R 12  and R b ; R a  is, independently at each occurrence, selected from: halogen, C 1-4  alkyl, and C 1-4  alkoxy; R b  is, independently at each occurrence, selected from: H, C 1-4  alkyl substituted with 0-1 R e , C 1-4  haloalkyl, CO(C 1-4  alkyl), CO 2 (C 1-4  alkyl), SO 2 (C 1-4  alkyl, CO 2 Bn, \u2014(CH 2 ) t -(phenyl substituted with 0-1 R e ) and \u2014(CO) n \u2014(CH 2 ) n -(5- to 6-membered heterocyclic ring comprised of carbon atoms and 1-2 heteroatoms selected from N, NH, O, and S; wherein said heterocycle is substituted with 0-1 R e ); R c  is, independently at each occurrence, selected from: OH, halogen, C 1-6  alkyl substituted with 0-1 OH, C 1-4  alkoxy, C 1-4  haloalkyl, C 1-4  haloalkoxy, CN, CONH 2 , CONH(C 1-4  alkyl), and CON(C 1-4  alkyl) 2 ; R d  is, independently at each occurrence, selected from: OH, NH 2 , NH(C 1-4  alkyl), N(C 1-4  alkyl) 2 , CONH 2 , CONH(C 1-4  alkyl), and CON(C 1-4  alkyl) 2 ; R e  is independently at each occurrence, selected from: halogen, C 1-4  alkyl substituted with 0-1 OH, C 1-4  haloalkyl, C 1-4  alkoxy, C 1-4  haloalkoxy, CN, and NH 2 ; n is, independently at each occurrence, selected from 0 and 1; p is, independently at each occurrence, selected from 0, 1 and 2; and t is, independently at each occurrence, selected from 0, 1, 2, and 3.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 88.0
- Lexical Diversity: 1.26829
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15756373', '15756378', '16099010', '13944921', '13936311']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7761779917581461
- 35 USC 102 Novelty (BERT): 0.6178843438106977
- Combined Prediction Score: 0.7603486269634012
- Mean Citation Score: 444.768054
- Max Citation Score: 554.2722
- Similarity Product: 510.18683494091033

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