http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2699226-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/C07D217-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 |
| classificationIPCInventive | 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/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D217-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 |
| filingDate | 2012-10-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2019-02-08-04:00^^<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_45ba971efd38b7c74e7cb5f3494562f1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2f14706fa730a7d207793842f3906bdf |
| publicationDate | 2019-02-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2699226-T3 |
| titleOfInvention | Substituted tetrahydroisoquinoline compounds as inhibitors of factor XIa |
| abstract | A compound according to Formula (IX): ** Formula ** or a pharmaceutically acceptable stereoisomer, tautomer, salt or solvate thereof, wherein: ring A is C3-10 carbocycle; L is selected from the group consisting of: a bond, -CHR10CHR10-, - CR10 = CR10- and -C≡C-; R1, in each case, is selected from the group consisting of: H, halo, C1-2alkyl, -O (C1-4alkyl), CN, -CH2NH2 and -C (= NH) NH2; R2 is independently selected from the group consisting of: H, halo, CN, OH, C1-6 alkyl, C1-4 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, CO (C1-4 alkyl), CONH2, CO2H and a 5-7 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NH, N (C1-4alkyl), O and S (O) p, wherein said heterocycle is substituted with 1-2 R2a; R2a, in each case, is selected from the group consisting of: H, halo, C1-4alkyl, CO2H, -CO2 (C1-4alkyl), -CONH2, -CH2OH, -CH2O C1-4alkyl and -CH2NH2 ; R3 is selected from the group consisting of: C3-10 carbocycle substituted with 1-3 R3a and a 5-10 membered heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of N, NR7, O and S (O) p; wherein said heterocycle is substituted with 1-3 R3a; R3a, in each case, is selected from the group consisting of: H, halo, C1-4alkyl, -OH, C1-4alkoxy, -CN, -NH2, -NH (C1-4alkyl), -N ( C1-4alkyl) 2, -CO2H, -CH2CO2H, -CO2 (C1-4alkyl), -CO2-C1-4alkylene-O (C1-4alkyl), -CO2- C1-4alkylene-N (C1alkyl -4) 2, -CO2-C1-4alkylene-O-C1-4alkylene-N (C1-4alkyl) 2, -CO2-C1-4alkylene-O-C1-4alkylene-O (C1-4alkyl ), -CONH2, -CONH (C1-6alkyl), -CON (C1-4alkyl) 2, -CONH-C1-4alkylene-CO2 (C1-4alkyl), - CONHCO2C1-4alkyl, -CONH-alkylene C1-4-NHCO (C1-4alkyl), -CONH-C1-4alkylene-CONH2, -NHCO C1-4alkyl, -NHCO2 (C1-4alkyl), Rc, -CONHRc and -CO2Rc; R4, in each case, is selected from the group consisting of: H, halo and C1-4alkyl; R5 is selected from the group consisting of: H, halo, C1-4 alkyl substituted with 0-2 Rb, C2-4 alkenyl substituted with 0-2 Rb, -OH, -CN, -NH2, -N (C1 alkyl -4) 2, -OCO (C1-4alkyl), -O-C1-4alkylene-O (C1-4alkyl), -O C1-4alkylene-N (C1-4alkyl) 2, -CO2H, -CO2 (C1-4alkyl), -CONH2, - (CH2) 2CONH2, -CONR9 (C1-4alkyl), - CON (C1-4alkyl) 2, -CONR9-C1-4alkylene-C1 (C1-4alkyl) , -CONR9-C1-4alkylene-N (C1-4alkyl) 2, -CONR9-C1-4alkylene-C1 (C1-4alkyl), -NR9CO1-4-4alkyl, -NR9CO2 C1-4alkyl, -NR9CONH (alkyl C1-4), -NR9CONR9-C1-4alkylene-C1-4alkyl, -NR9-C1-4alkylene -N (C1-4alkyl) 2, -NR9SO2 (C1-4alkyl), -S (C1-alkyl) 4), -SO2 (C1-4alkyl), -SO2NH2, R8, alkenylene C2-4-R8, -OR8, -COR8, alkenylene C2-4-COR8, -CONR9R8, -NR9COR8, -NR9CO2R8 35 and - NR9CONR9R8; R7, in each case, is selected from the group consisting of: H, C1-4alkyl, CO1-4-4alkyl, CO2 (C1-4alkyl), CO2Bn, -CONH-C1-4alkylene-C1-4alkyl, phenyl, benzyl and -CO2-C1-4alkylene-aryl; R8, in each case, is selected from the group consisting of: - (CH2) n-carbocycle C3-10 and - (CH2) n-heterocycle with 5 to 10 members containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NRa, O and S (O) p; wherein said carbocycle or heterocycle are substituted with 0-3 Rb; R9, in each case, is selected from the group consisting of: H and C1-4alkyl; R10, in each case, is selected from the group consisting of: H, halo, OH and C1-4 alkyl; Ra is selected from the group consisting of: H, C1-4 alkyl, - (CH2) nOH, CO (C1-4 alkyl), COCF3, CO2 (C1-4 alkyl), -CONH2, -CONH-C1- alkylene 4-CO2 (C1-4 alkyl), C1-4 alkylene-CO2 (C1-4 alkyl), Rc, CO2Rc and CONHRc; Rb is selected from the group consisting of: = O, halo, C1-4alkyl, C1-4alkoxy, OCF3, NH2, NO2, N (C1-4alkyl) 2, CO (C1-4alkyl), CO ( halo (C1-4alkyl), CO2 (C1-4alkyl), CONH2, -CONH (C1-4alkyl), -CON (C1-4alkyl) 2, - CONH-C1-4alkylene-O (C1-4alkyl) , -CONH-C1-4 alkylene (C1-4alkyl) 2, -CONH-C1-4alkylene-N + (C1-4alkyl) 2- C1-4alkylene-OP (O) (OH) 2, - NHCO2 (C1-4alkyl), -Rc, CORc, CO2Rc and CONHRc; Rc is selected, independently in each occurrence, from the group consisting of: - (CH2) n-C3-6 cycloalkyl, - (CH2) n-phenyl and - (CH2) n-hetero-5- to 6-membered heterocycle carbon and 1-4 heteroatoms selected from the group consisting of: N, NH, N (C1-4alkyl), O and S (O) p; wherein each ring residue is substituted with 0-2 Rd; Rd is selected from the group consisting of: = O, halo, -OH, C1-4alkyl, NH2, NH (C1-4alkyl), N (C1-4alkyl) 2, C1-4alkoxy, and -NHCO ( C1-4alkyl) and carbon-containing heterocycle and 1-4 heteroatoms selected from the group consisting of: N, NH, N (C1-4alkyl), O and S (O) p; n, in each case, is selected from 0, 1, 2, 3 and 4; and p, in each case, is selected from 0, 1 and 2; with the proviso that the compound is not |
| priorityDate | 2011-10-14-04:00^^<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: 958.