http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2625256-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-13 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-551 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D217-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-113 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-107 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-541 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D217-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-08 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/A61K31-4725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
| filingDate | 2012-10-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2017-07-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2f14706fa730a7d207793842f3906bdf 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_887a5326cdd9c4ebc8512f8fd497a4c3 |
| publicationDate | 2017-07-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2625256-T3 |
| titleOfInvention | Tetrahydroisoquinoline compounds substituted as XIA factor inhibitors |
| abstract | A compound according to formula (I): ** Formula ** or a stereoisomer, a tautomer, a pharmaceutically acceptable salt or a solvate thereof, wherein: ring A is a C3-6 carbocycle; Ring B is a 4- to 7-membered heterocycle containing additional carbon atoms and 0-3 heteroatoms selected from the group consisting of N, NR6, O and S (O) p; optionally, ring B forms a condensed ring or a spiro ring with a 4- to 7-membered heterocycle containing carbon atoms and 1-3 heteroatoms selected from the group consisting of NR6, O and S (O) p; Ring B, including the condensed ring or the spiro ring, is substituted with 1-3 R5; L is selected from the group consisting of: -CHR10CHR10-, -CR10> = CR10-, -CºC-, -CHR10NH-, -NHCHR10-, - SCH2-, -CH2S-, -SO2CH2-, -CH2SO2-, - NHCH2- and -CH2NH-; R1, at each occurrence, is selected from the group consisting of: H, halo, C1-6 alkyl, C1-4 alkoxy, C1-4 alkylthio, OH, SH, CHF2, CF3, OCF3, CN, NH2, CO- C1-4 alkyl, CO2 (C1-4 alkyl), -CH2CO2H, -CH2CO2 (C1-4 alkyl), - CH2NH2, -CONH2, -CONH (C1-4 alkyl), -NHCO (C1-4 alkyl), - NHCO2 (C1-4 alkyl), -NHSO2 (C1-4 alkyl) and - SO2NH2 and -C (> = NH) NH2; R2 is 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, CH2NH2 and a 5- to 7-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NRc, O and S (O) p, wherein said heterocycle is substituted with 0-2 R2a; R2a, at each occurrence, is selected from the group consisting of: H, halo, C1-4 alkyl, C1-4 alkoxy, OH, CF3, OCF3, CN, NH2, CO2H, CO2 (C1-4 alkyl), CO (C1-4 alkyl), -CONH2, -CH2OH, -CH2O-C1-4 alkyl, -CH2NH2-, CONH (C1-4 alkyl), -CON (C1-4 alkyl) 2, -SO2 (C1-4 alkyl ), -SO2NH2, -SO2NH (C1-4 alkyl) and -SO2N (C1-4 alkyl) 2; R3 is selected from the group consisting of: C1-6 alkyl substituted with 1-3 R3a, - (CH2) n-carbocycle C3-10 substituted with 0-3 R3a or - (CH2) 5-10 membered n-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 0-3 R3a; R3a, at each occurrence, is selected from the group consisting of:> = O, halo, C1-4 alkyl, OH, C1-4 alkoxy, CN, NH2, CO2H, CO2 (C1-4 alkyl), CONH2, CONH (C1-6 alkyl), CON (C1-4 alkyl) 2, -CONH-C1-4 alkylene-C1 (C1-4 alkyl), -CONHCO2-C1-4 alkyl, -CONH-C1-4 alkylene-NHCO ( C1-4alkyl), -CONH-C1-4alkyl-CONH2, -NHCO C1-4alkyl, -NHCO2 (C1-4alkyl), -C1-4alkyl-NHCO2-C1-4alkyl, Rf, CONHRf and - CO2Rf; R4, at each occurrence, is selected from the group consisting of: H, halo and C1-4 alkyl; R5, at each occurrence, is selected from the group consisting of: H,> = O, halo, C1-4 alkyl, OH, CN, NH2, - N (C1-4 alkyl) 2, NO2, C1-4 alkoxy , -OCO (C1-4 alkyl), -O-C1-4 alkylene-O (C1-4 alkyl), -O-C1-4 alkylene (C1-4 alkyl) 2, -CO2H, -CO2 (alkyl C1-4), -CONH2, - (CH2) 2CONH2, -CONR9 (C1-4 alkyl), -CONR9-C1-4 alkylene (C1-4 alkyl), -CON (C1-4 alkyl) 2, - CONR9-C1-4 alkylene (C1-4 alkyl) 2, -CON (C1-4 alkyl) -C 1-4 alkyl (C1-4 alkyl), - CONR9-C1-4 alkylene-C1 (C1 alkyl) -4), -NR9CO-C1-4 alkyl, -NR9CO2-C1-4 alkyl, -NR9CONH (C1-4 alkyl), - NR9CONR9-C1-4 alkylene-CO2-C1-4 alkyl, -NR9-C1-alkylene 4-N (C1-4 alkyl) 2, R8, -OR8, -O-C1-4-R8 alkylene, - COR8, -CO2R8, -CONR9R8, -NR9COR8, -NR9CO2R8 and -NR9CON R9R8; R6 is selected from the group consisting of: H, C1-4 alkyl, -CO2 (C1-4 alkyl), -CO (C1-4 alkyl), -CONH2, - CO-C1-4-N alkylene (C1 alkyl -4) 2, - (CH2) 2N (C1-4 alkyl) 2, -CONR9 (C1-4 alkyl), -CONR9-C1-4 alkylene (C1-4 alkyl), -CONR9-C1-4 alkylene -N (C1-4 alkyl) 2, -CONR9-C1-4 alkylene-CO2 (C1-4 alkyl), -CON (C1-4 alkyl) 2, R8, -COR8, - CO2R8 and -CONR9R8; R7, at each occurrence, is selected from the group consisting of: H, C1-4 alkyl, CO-C1-4 alkyl, CO2 (C1-4 alkyl), CO2Bn, -CONH-C1-4 alkylene-CO2-alkyl C1-4, phenyl, benzyl and -CO2-C1-4 alkylene-aryl; R8, at each occurrence, is selected from the group consisting of: - (CH2) C3-10 n-carbocycle substituted with 0-3 Re and - (CH2) 5-10 membered n-heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of N, NRd, O and S (O) p; wherein said carbocycle and heterocycle are optionally substituted with> = O; R9, at each occurrence, is selected from the group consisting of: H and C1-4 alkyl; R10, at each occurrence, is selected from the group consisting of: H, halo, OH and C1-4 alkyl; Rc is selected, independently at each occurrence, from the group consisting of: H, C1-4 alkyl, CO C1-4 alkyl, CO2-C1-4 alkyl and CO2Bn; Rd is selected, independently at each occurrence, from the group consisting of: H, C1-4 alkyl, CO (C1-4 alkyl), COCF3, CO2 (C1-4 alkyl), -CONH-C1-4 alkylene -C1-4 alkyl, CO2Bn, Rf and CONHRf; Re is selected, independently at each occurrence, from the group consisting of:> = O, halo, C1-4 alkyl, C1-4 alkoxy, OCF3, NH2, NO2, N (C1-4 alkyl) 2, CO (alkyl C1-4), CO (C1-4 haloalkyl), CO2 (C1-4 alkyl), CONH2, - CONH (C1-4 alkyl), -CONHPh, -CON (C1-4 alkyl) 2, -CONH-C1 alkylene -4-O (C1-4 alkyl), -CONH-C1-4 alkylene-N (C1-4 alkyl) 2, -CONH-C1-4 alkylene-C1-4 alkyl, -NHCO2 (C1- alkyl 4), Rf, CORf, CO2Rf and CONHRf; Rf is independently selected at each occurrence from the group consisting of: - (CH2) C3-6 n-cycloalkyl, - (CH2) n-phenyl and - (CH2) 5 to 6 membered n-heterocycle containing atoms carbon and 1-4 heteroatoms selected from the group consisting of N, NRc, O and S (O) p; wherein each rest of the ring is substituted with 0-2 Rg; Rg is independently selected at each occurrence, from the group consisting of:> = O, halo, C1-4 alkyl, OH, C1-4 alkoxy and NHCO (C1-4 alkyl); n, at each occurrence, is selected from 0, 1, 2, 3 and 4; and p, at each occurrence, is selected between 0, 1 and 2. |
| priorityDate | 2011-10-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 58.