http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2863903-T3

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filingDate 2017-06-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2021-10-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2584a92d398cd910920e8a4b13662caa
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publicationDate 2021-10-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2863903-T3
titleOfInvention 6-hydroxy-5- (phenyl / heteroarylsulfonyl) pyrimidin-4 (1H) -one as APJ agonists
abstract A compound of Formula (I): ** (See formula) ** or a stereoisomer, an enantiomer, a diastereoisomer, a tautomer or a pharmaceutically acceptable salt thereof, wherein ring A is independently selected from C3-6 cycloalkyl, 5- or 6-membered aryl and heterocyclyl- (CH2) 0-1 comprising carbon atoms and 1-4 heteroatoms selected from N, NR3a, O and S, each substituted with 1-3 R3 and 1-2 R5; provided that R3 and R5 are neither H; Ring B is independently selected from C 3-6 cycloalkyl, C 3-6 cycloalkenyl, aryl, bicyclic carbocyclyl, 6-membered heteroaryl, 6-membered heterocyclyl, and bicyclic heterocyclyl, each substituted with 1-3 R1; R1 is independently selected from H, F, Cl, Br, NO2, - (CH2) nORb, (CH2) n, S (O) pRc, - (CH2) nC (= O) Rb, - (CH2) nNRaRa, - (CH2) nCN, - (CH2) nC (= O) NRaRa, - (CH2) nNRaC (= O) Rb, - (CH2) nNRaC (= O) NRaRa, - (CH2) nNRaC (= O) ORb, - (CH2) nOC (= O) NRaRa, - (CH2) nC (= O) ORb, - (CH2) nS (O) pNRaRa, - (CH2) nNRaS (O) pNRaRa, - (CH2) nNRaS (O) pRc , C 1-4 alkyl substituted with 0-3 Re, - (CH2) n-C3-6 carbocyclyl substituted with 0-3 Re and - (CH2) n-heterocyclyl substituted with 0-3 Re; R2 is independently selected from C1-5 alkyl substituted with 0-3 Re; C2-5 alkenyl substituted with 0-3 Re, aryl substituted with 0-3 Re, heterocyclyl substituted with 0-3 Re and C3-6 cycloalkyl substituted with 0-3 Re; provided that when R2 is C1-5 alkyl, the carbon atom except that attached to the pyrimidine ring can be replaced by O, N and S; R3 is independently selected from H, F, Cl, Br, C1-5 alkyl substituted with 0-3 Re, - (CH2) nORb, - (CH2) nNRaRa, - (CH2) nCN, - (CH2) nC (= O ) Rb, - (CH2) nC (= O) ORb, - (CH2) nC (= O) NRaRa, - (CH2) nNHC (= O) Rb, - (CH2) nNHC (= O) NRaRa, - (CH2 ) nNHC (= O) ORb, - (CH2) nNHS (O) pNRaRa, - (CH2) nNHS (O) pRc- (CH2) nS (O) pRc, - (CH2) nS (O) pNRaRa and - (CH2 ) nOC (= O) NRaRa; R3a is independently selected from H, C1-5 alkyl substituted with 0-3 Re, -S (O) pRc, -C (= O) Rb, -C (= O) NRaRa, -C (= O) ORb, S (O) pNRaRa, R6, -S (O) pR6, -C (= O) R6, -C (= O) NRaR6, -C (= O) OR6 and -S (O) pNRaR6; R4 is independently selected from H, C1-5 alkyl substituted with 0-3 Re, C2-5 alkenyl substituted with 0-3 Re, (CH2) n-C3-6 carbocyclyl substituted with 0-3 Re and - (CH2) n -heterocyclyl substituted with 0-3 Re; R5 is independently selected from H, R6, -OR6, -S (O) pR6, -C (= O) R6, -C (= O) OR6, -NRaR6, -C (= O) NRaR6, -NRaC (= O) R6, -NRaC (= O) OR6, -OC (= O) NRaR6, -S (O) pNRaR6, -NRaS (O) pNRaR6 and -NRaS (O) pR6; R6 is independently selected from - (CR7R7) n-aryl, - (CR7R7) n-C3-6 cycloalkyl, and - (CR7R7) n-heteroaryl, each substituted with 1-6 R8; R7 is independently selected from H, C1-4 alkyl and (CH2) n-C3-12 carbocyclyl substituted with 0-3 Re; R8 is independently selected from H, F, Cl, Br, - (CH2) nCN, - (CH2) nORb, - (CH2) nC (= O) Rb, - (CH2) nC (= O) ORb, - (CH2 ) nC (= O) NRaRa, - (CH2) nNRaRa, - (CH2) nNRaC (= O) Rb, - (CH2) nNRaC (= O) ORb, - (CH2) nNRaC (= O) NRaRa, - (CH2 ) nOC (= O) NRaRa, - (CH2) nS (O) pRc, - (CH2) nS (O) pNRaRa, - (CH2) nNRaS (O) pNRaRa, - (CH2) nNRaS (O) pRc, C1 alkyl -4 substituted with 0-3 Re, (CH2) n-C3-6 carbocyclyl substituted with 0-3 Re and - (CH2) n-heterocyclyl substituted with 0-3 Re; Ra is independently selected from H, C1-6 alkyl substituted with 0-5 Re, C2-6 alkenyl substituted with 0-5 Re, C2-6 alkynyl substituted with 0-5 Re, - (CH2) n-C3-10 carbocyclyl substituted with 0-5 Re and - (CH2) n-heterocyclyl substituted with 0-5 Re; or Ra and Ra together with the nitrogen atom to which they are both attached form a heterocyclic ring substituted with 0-5 Re; Rb is independently selected from H, C1-6 alkyl substituted with 0-5 Re, C2-6 alkenyl substituted with 0-5 Re, C2-6 alkynyl substituted with 0-5 Re, - (CH2) n-C3-10 carbocyclyl substituted with 0-5 Re and - (CH2) n-heterocyclyl substituted with 0-5 Re; Rc is independently selected from C1-6 alkyl substituted with 0-5 Re, C2-6 alkenyl substituted with 0-5 Re, C2-6 alkynyl substituted with 0-5 Re, C3-6 carbocyclyl and heterocyclyl; Re is independently selected from C1-6 alkyl substituted with 0-5 Rf, C2-6 alkenyl, C2-6 alkynyl, - (CH2) n-C3-6 cycloalkyl, - (CH2) C4-6 nheterocyclyl, - (CH2 ) n-aryl, - (CH2) n-heteroaryl, F, Cl, Br, CN, NO2, = O, CO2H, - (CH2) nORf, S (O) pRf, C (= O) NRfRf, NRfC (= O) Rf, S (O) pNRfRf, NRfS (O) pRf, NRfC (= O) ORf, OC (= O) NRfRf and - (CH2) nNRfRf; Rf is independently selected from H, F, Cl, Br, CN, OH, C1-5 alkyl (optimally substituted with F, Cl, Br and OH), C3-6 cycloalkyl and phenyl, or Rf and Rf together with the atom nitrogen to which they are both attached, form a heterocyclic ring optionally substituted with C1-4 alkyl; n is independently selected from zero, 1, 2, 3, and 4; and p is independently selected from zero, 1, and 2.
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Total number of triples: 1343.