PATENT CLAIM ANALYSIS

Application Number: 16122975
Application Type: Utility
Filing Date: 2018-09
Publication Date: 2019-01
Patent Classification: ["514", "269000"]

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.

Claim (Index 1):
A compound of Formula (I): or a stereoisomer, an enantiomer, a diastereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein: alk is C 1-6  alkylene substituted with 0-5 R e ; ring B is independently selected from C 3-6  cycloalkyl, C 3-6  cycloalkenyl, aryl, bicyclic carbocyclyl, and 6-membered heteroaryl; R 1 , at each occurrence, 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 ; R 2  is independently selected from C 1-10  alkyl substituted with 0-3 R e ; C 2-5  alkenyl substituted with 0-3 R e , aryl substituted with 0-3 R e , heteroaryl substituted with 0-3 R e , and C 3-6  cycloalkyl substituted with 0-3 R e ; provided when R 2  is C 1-10  alkyl, the carbon atoms and the groups attached thereto except the carbon atom attached to the pyrimidine ring may be replaced by O, N, and S; R 3  is independently selected from H and C 1-5  alkyl: R 4  is independently selected from \u2014(CR 7 R 7 ) n \u2014R 6 , \u2014(CR 7 R 7 ) n OR 6 , \u2014(CR 7 R 7 ) n S(O) p R 6 , \u2014(CR 7 R 7 ) n C(\u2550O)R 6 , \u2014(CR 7 R 7 ) n NR a R 6 , \u2014(CR 7 R 7 ) n NR a C(\u2550O)R 6 , \u2014(CR 7 R 7 ) n S(O) p NR a R 6 , and \u2014(CR 7 R 7 ) n NR a S(O) p R 6 ; alternatively, R 3  and R 4  together with the nitrogen atom to which they are both attached form a heterocyclic ring or a spiro heterocyclic ring comprising carbon atoms and additional 1 to 4 heteroatoms selected from NR 5 a, 0, and S and substituted with 0-5 R 5 ; R 5 , at each occurrence, is independently selected from OH, halogen, \u2014(CR 7 R 7 ) n \u2014R 6 , \u2014OR 6 , \u2014S(O) p R 6 , \u2014C(\u2550O)R 6 , \u2014NR a R 6 , \u2014C(\u2550O)NR a R 6 , \u2014NR a C(\u2550O)R 6 , \u2014NR a C(\u2550O)OR 6 , \u2014OC(\u2550O)NR a R 6 , \u2014C(\u2550O)OR 6 , \u2014S(O) p NR a R 6 , \u2014NR a S(O) p NR a R 6 ,  an d \u2014NR a S(O) p R 6 ; R 5a , at each occurrence, is independently selected from \u2014C(\u2550O)OR 6 , C(\u2550O)NR a R 6 , \u2014(CR 7 R 7 ) n \u2014R 6 , \u2014C(\u2550O)\u2014R 6 , and \u2014S(O) p R 6 ; R 6 , at each occurrence, is independently selected from \u2014(CR 7 R 7 ) n \u2014C 3-10  carbocyclyl and \u2014(CR 7 R 7 ) n -heteroaryl, each substituted with 0-3 R 8 ; R 7 , at each occurrence, is independently selected from H, C 1-4  alkyl, and \u2014(CH 2 ) n \u2014C 3-12  carbocyclyl substituted with 0-3 R e ; R 8 , at each occurrence, is independently selected from H, halogen, \u2014(CH 2 ) n OR b ,\u2550O, (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 e , C 1-5  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 ; 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 ; 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 ; 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; R e , at each occurrence, is independently selected from F, Cl, Br, CN, NO 2 , \u2550O, CO 2 H, C 1-6  alkyl substituted with 0-5 R f , 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, \u2014(CH 2 ) n OR f , \u2014S(O) p R f , \u2014C(\u2550O)NR f R f , \u2014NR f C(\u2550O)R f , \u2014S(O) p NR f R f , \u2014NR f S(O) p Rf, \u2014NRfC(\u2550O)OR f , \u2014OC(\u2550O)NR f R f  and \u2014(CH 2 ) n NR f R f ; R f , at each occurrence, is independently selected from H, F, Cl, Br, CN, OH, 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, at each occurrence, is independently selected from zero, 1, 2, 3, and 4; and p, at each occurrence, is independently selected from zero, 1, and 2.

Metadata:
- Claim Count in Document: 27.0
- Percentile: 97.0
- Lexical Diversity: 1.16667
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15468230', '15767364', '16309161', '16061365', '15171276']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7956783766873504
- 35 USC 102 Novelty (BERT): 0.5519261106061977
- Combined Prediction Score: 0.7713031500792352
- Mean Citation Score: 382.398828
- Max Citation Score: 411.5391
- Similarity Product: 401.0285654640378

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