http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2754599-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D237-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-86 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4192 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4178 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D237-14 |
| filingDate | 2016-08-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2020-04-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_896e2c8810106a19419155cd1a6c7ad0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_21fd7fbb79f28d9512cc7fed659169f6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a28e4230fa1667a4b6c44fb85af3f8aa http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2f14706fa730a7d207793842f3906bdf |
| publicationDate | 2020-04-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2754599-T3 |
| titleOfInvention | Novel substituted glycine-derived FXIa inhibitors |
| abstract | A compound of Formula (I): ** Formula ** or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof, wherein: A is independently selected from ** Formula ** and Hal is halogen; R1 and R2 are independently selected from H, halogen, CN, NRaRa, C1-6 alkyl substituted with 1-5 R10, - ORb, -C (= O) Rb, -C (= O) ORb, - (CH2) n -aryl substituted with 1-5 R10, - (CH2) n-C3-6 cycloalkyl substituted with 1-5 R10 and - (CH2) n-4-6 membered heterocyclyl substituted with 1-5 R10; R3 is independently selected from C1-4 alkyl substituted with 1-5 R5, - (CH2) n-C3-10 carbocyclyl substituted with 1-5 R5 and - (CH2) n-heterocyclyl 4 to 10 membered substituted with 1-5 R5 ; R4 is independently selected from H and C1-4 alkyl substituted with 1-5 R6; alternatively, R3 and R4 together with the nitrogen atom to which they are both attached form a heterocyclic ring substituted with 1-5 R5; R5, at each occurrence, is independently selected from H, halogen, C1-6 alkyl substituted with 0-5 Re, = O, - (CH2) nCN, - (CH2) n-ORb, - (CH2) n-NRaRa, - (CH2) nC (= O) Rb, - (CH2) nC (= O) ORb, - (CH2) nC (= O) NRaRa, - (CH2) n- C (= NH) NHRa, - (CH2) n-NRaC (= O) ORb, - (CH2) n-NRaC (= O) Rb, - (CH2) n-NRaC (N-CN) NHRa, - (CH2) n-NRaC (NH) NHRa, - ( CH2) nN = CRbNRaRa, - (CH2) n-NRaC (= O) NRaRa, - (CH2) nC (= O) NRaRa, - (CH2) n-NRaC (= S) NRaC (= O) Rb, - ( CH2) n- S (= O) pRc, - (CH2) nS (= O) pNRaRa, - (CH2) n-NRaS (= O) pNRaRa, - (CH2) n-NRaS (= O) pRc, - ( CH2) n-C3-10 carbocyclyl substituted with 1-5 R6, - (CH2) n-heterocyclyl substituted with 1-5 R6 and 4-10 membered -O-heterocyclyl substituted with 1-5 R6; R6, at each occurrence, is independently selected from H, - (CH2) n-ORb, = O, - (CH2) nNH2, - (CH2) nCN, halogen, C1-6 alkyl substituted with 0-5 Re, - ( CH2) nC (= O) ORb, - (CH2) n-ORb, - (CH2) n-C3-10 carbocyclyl and - (CH2) n-heterocyclyl 4 to 10 membered substituted with 0-5 Re; R7 is independently selected from H, hydroxyl, ORb, halogen, NRaRa, and C1-3 alkyl; R8 is independently selected from - (CH2) nC (O) NRaRa, C1-6 alkyl substituted with 1-5 R9, C2-6 alkenyl substituted with 1-5 R9, C2-6 alkynyl substituted with 1-5 R9, - ( CRdRd) n-C3-10 carbocyclyl substituted with 1-5 R9 and - (CRdRd) n-heterocyclyl from 5 to 10 membered comprising carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p and substituted with 1-5 R9; R9, in each case, is independently selected from H, = O, C1-4 alkyl substituted with 1-3 R10, halogen, ORb, CF3, CN, NO2, -NRaRa, -C (O) NRaRa, -NRaC (O ) Rb, -S (O) pNRaRa, -NRaS (O) pRc, -C (O) Rb, -C (O) ORb, -S (O) pRc '- (CH2) n-C3-10 carbocycle substituted with 1-3 R10 and - (CH2) n-5 to 10 membered heterocyclyl comprising carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p and substituted with 1-3 R10; R10, at each occurrence, is independently selected from H, C1-6 alkyl substituted with 1-5 R11, C2-6 alkenyl substituted with 1-5 R11, C2-6 alkynyl substituted with 1-5 R11, aryl substituted with 1- 5 R11, - (CH2) n-C3-6 cycloalkyl substituted with 1-5 R11, - (CH2) nO-4- to 10-membered heterocyclyl substituted with 1-5 R11, halogen, CN, NO2, = O, C ( = O) NRaRa, C (= O) ORb, Si (C1-4 alkyl) 3, - (CH2) n-ORb, - (CH2) n-NRaRa and C (= NOH) NH2; R11, at each occurrence, is independently selected from H, halogen, - (CH2) n-OH, C3-6 cycloalkyl, phenyl, and heterocyclyl; Ra, at each occurrence, is independently selected from H, CN, 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 ) C3-10 n-carbocyclyl substituted with 0-5 Re and - (CH2) nheterocyclyl 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, at each occurrence, 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) nheterocyclyl substituted with 0-5 Re; Rc, at each occurrence, 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; Rd, at each occurrence, is independently selected from H and C1-4 alkyl substituted with 0-5 Re; Re, in each case, is independently selected from F, Cl, Br, CN, NO2, = O, C1-6 alkyl substituted with 0-5 Rf, C2-6 alkenyl, C2-6 alkynyl, - (CH2) n- C 3-6 cycloalkyl, - (CH2) n-aryl, - (CH2) n-heterocyclyl, CO2H, - (CH2) nORf, SRf and - (CH2) nNRfRf; Rf, in each case, is independently selected from H, C1-5 alkyl optionally substituted with F, Cl, Br, C3-6 cycloalkyl and phenyl, or Rf and Rf together with the nitrogen atom to which they are both attached form a ring heterocyclic optionally substituted with C1-4 alkyl; n, in each case, is an integer independently selected from 0, 1, 2, 3, and 4; p, in each case, is an integer independently selected from 0, 1, and 2. |
| priorityDate | 2015-08-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 1120.