PATENT CLAIM ANALYSIS

Application Number: 16061365
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2018-12
Patent Classification: ["514", "230800"]

Abstract:
The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments, in particular for treating cardiovascular disorders.

Claim (Index 1):
A compound of Formula (I): or a stereoisomer, an enantiomer, a diastereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein:\n alk is C 1-6  alkyl substituted with 1-5 R 7 ; \n ring A is 5- to 6-membered heteroaryl; \n ring B is independently selected from C 3-6  cycloalkyl, C 3-6  cycloalkenyl, aryl, bicyclic carbocyclyl, and 6-membered heteroaryl; \n R 1  is independently selected from H, halogen, NO 2 , \u2014(CH 2 ) n OR b , (CH 2 ) n S(O) p R c , \u2014(CH 2 ) n C(\u2550O)R b , \u2014(CH 2 ) n NR a R a , \u2014(CH 2 ) n CN, \u2014(CH 2 ) n C(\u2550O)NR a R a , \u2014(CH 2 ) n NR a C(\u2550O)R b , \u2014(CH 2 ) n NR a C(\u2550O)NR a R a , \u2014(CH 2 ) n NR a C(\u2550O)OR b , \u2014(CH 2 ) n OC(\u2550O)NR a R a , \u2014(CH 2 ) n C(\u2550O)OR b , \u2014(CH 2 ) n S(O) p NR a R a , \u2014(CH 2 ) n NR a S(O) p NR a R a , \u2014(CH 2 ) n NR a S(O) p R c , C 1-4  alkyl substituted with 0-3 R e , \u2014(CH 2 ) n \u2014C 3-6  carbocyclyl substituted with 0-3 R e , and \u2014(CH 2 ) n -heterocyclyl substituted with 0-3 R e ; \n R 2  is independently selected from C 1-5  alkyl substituted with 0-3 R e ; C 2-5  alkenyl substituted with 0-3 R e , aryl substituted with 0-3 R e , heterocyclyl substituted with 0-3 R e , and C 3-6  cycloalkyl substituted with 0-3 R e ; provided when R 2  is C 1-5  alkyl, the carbon atom and the groups attached thereto except the one attached to the pyrimidine ring may be replaced by O, N, and S; \n R 3  is independently selected from\n (1) \u2014(CR 4 R 4 ) r C(\u2550O)OC 1-4  alkyl substituted with 0-5 R e , \n (2) \u2014(CR 4 R 4 ) r NR 8 R 8 , \n (3) \u2014(CR 4 R 4 ) r C(\u2550O)NR 8 R 8 , \n (4) \u2014(CR 4 R 4 ) r NR a C(\u2550O)C 1-4 alkyl substituted with 0-5 R e , \n (5) \u2014(CR 4 R 4 ) r NR a C(\u2550O)(CR 4 R 4 ) n OC 1-4 alkyl substituted with 0-5 R e , \n (6) \u2014(CR 4 R 4 ) r \u2014R 5 , \n (7) \u2014(CR 4 R 4 ) r \u2014OR 5 , and \n (8) \u2014(CR 4 R 4 ) r NR a C(\u2550O)(CR 4 R 4 ) n R 5 ; \n \n R 4  is independently selected from H, halogen, NR a R a , OC 1-4  alkyl, and C 1-4  alkyl; or R 4  and R 4  together with the carbon atom to which they are both attached form C 3-6  cycloalkyl substituted with 0-5 R e ; \n R 5  is independently selected from \u2014(CH 2 ) n \u2014C 3-10  carbocycle and \u2014(CH 2 ) n -heterocycle comprising carbon atoms and 1-3 heteroatoms selected from N, NR 6 , O, and S, each substituted with 0-5 R 6 ; \n R 6  is independently selected from H, halogen, \u2550O, \u2014(CH 2 ) n OR b , (CH 2 ) n S(O) p , \u2014(CH 2 ) n C(\u2550O)R b , \u2014(CH 2 ) n NR a R a , \u2014(CH 2 ) n CN, \u2014(CH 2 ) n C(\u2550O)NR a R a , \u2014(CH 2 ) n NR a C(\u2550O)R b , \u2014(CH 2 ) n NR a C(\u2550O)NR a R a , \u2014(CH 2 ) n NR a C(\u2550O)OR b , \u2014(CH 2 ) n OC(\u2550O)NR a R a , \u2014(CH 2 ) n C(\u2550O)OR b , \u2014(CH 2 ) n S(O) p NR a R a , \u2014(CH 2 ) n NR a S(O) p NR a R a , \u2014(CH 2 ) n NR a S(O) p R c , C 1-5  alkyl substituted with 0-3 R e , (CH 2 ) n \u2014C 3-6  carbocyclyl substituted with 0-3 R e , and \u2014(CH 2 ) n -heterocyclyl substituted with 0-3 R e ; \n R 6a  is independently selected from H, \u2014S(O) p R c , \u2014C(\u2550O)R b , \u2014C(\u2550O)NR a R a , \u2014C(\u2550O)OR b , \u2014S(O) p NR a R a , C 1-5  alkyl substituted with 0-3 R e , (CH 2 ) n \u2014C 3-6  carbocyclyl substituted with 0-3 R e , and \u2014(CH 2 ) n -heterocyclyl substituted with 0-3 R e ; \n R 7  is independently selected from H, C 1-5  alkyl substituted with 0-3 R e , (CH 2 ) n \u2014C 3-6  carbocyclyl substituted with 0-3 R e , and \u2014(CH 2 ) n -heterocyclyl substituted with 0-3 R e ; \n R 8  and R 8  together with the nitrogen atom to which they are both attached form a heterocyclic ring comprising carbon atoms and 0-3 additional heteroatoms selected from N, NR 6 , O, and S, and substituted with 0-5 R 6 ; \n R a , at each occurrence, is independently selected from H, C 1-6  alkyl substituted with 0-5 R e , C 2-6  alkenyl substituted with 0-5 R e , C 2-6  alkynyl substituted with 0-5 R e , \u2014(CH 2 ) n \u2014C 3-10 carbocyclyl substituted with 0-5 R e , and \u2014(CH 2 ) n -heterocyclyl substituted with 0-5 R e ; or R a  and R a  together with the nitrogen atom to which they are both attached form a heterocyclic ring substituted with 0-5 R e ; \n R b , at each occurrence, is independently selected from H, C 1-6  alkyl substituted with 0-5 R e , C 2-6  alkenyl substituted with 0-5 R e , C 2-6  alkynyl substituted with 0-5 R e , \u2014(CH 2 ) n \u2014C 3-10 carbocyclyl substituted with 0-5 R e , and \u2014(CH 2 ) n -heterocyclyl substituted with 0-5 R e ; \n R c , at each occurrence, is independently selected from C 1-6  alkyl substituted with 0-5 R e , C 2-6 alkenyl substituted with 0-5 R e , C 2-6 alkynyl substituted with 0-5 R e , C 3-6 carbocyclyl, and heterocyclyl; \n R d , at each occurrence, is independently selected from H and C 1-4 alkyl substituted with 0-5 R e ; \n R e , at each occurrence, is independently selected from C 1-6  alkyl (optionally substituted with halogen, OH, and CN), C 2-6  alkenyl, C 2-6  alkynyl, \u2014(CH 2 ) n \u2014C 3-6  cycloalkyl, \u2014(CH 2 ) n \u2014C 4-6  heterocyclyl, \u2014(CH 2 ) n -aryl, \u2014(CH 2 ) n -heteroaryl, F, Cl, Br, CN, NO 2 , \u2550O, CO 2 H, \u2014(CH 2 ) n OR f , S(O) p R f , C(\u2550O)NR f R f , NR f C(\u2550O)R f , S(O) p NR f R f , NR f S(O) p R f , NR f C(\u2550O)OR f , OC(\u2550O)NR f R f  and \u2014(CH 2 ) n NR f R f ; \n R f , at each occurrence, is independently selected from H, C 1-5 alkyl (optionally substituted with halogen and OH), C 3-6  cycloalkyl, and phenyl, or R f  and R f  together with the nitrogen atom to which they are both attached form a heterocyclic ring optionally substituted with C 1-4 alkyl; \n n is independently selected from zero, 1, 2, and 3; \n r is independently selected from 1 and 2; and \n p, at each occurrence, is independently selected from zero, 1, and 2.

Metadata:
- Claim Count in Document: 4.0
- Percentile: 94.0
- Lexical Diversity: 1.19512
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['16309161', '15171276', '15468230', '15767364', '16340172']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7747337548274812
- 35 USC 102 Novelty (BERT): 0.561839040970575
- Combined Prediction Score: 0.7534442834417906
- Mean Citation Score: 396.694724
- Max Citation Score: 423.19574000000006
- Similarity Product: 386.9153641361368

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