http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2822130-T3
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D225-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4188 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-08 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-08 |
filingDate | 2011-02-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2021-04-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8b66b1296652e8182127477ff5f73312 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2ba0a646a2372edfbd7edce4e34a8d1e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3eb950f5b4529a233c95b938d25e6bb4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fe2bdffced54682eba189c82dfabd74c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fe428762740712f4e272f8d147c35a48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_82c2f3eec01bc83064be2217cb0163ce http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_12bf52cf056e724b2d03027040b490eb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_970ae3d168fac5265e0224f9006c0e09 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8908bf7f93ce19df37996522c5cfa521 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_209fb42f75d42308965b47d7983b89fc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bc87520a6c99439fcc22b85dedf752cd |
publicationDate | 2021-04-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | ES-2822130-T3 |
titleOfInvention | Macrocycles as factor XIa inhibitors |
abstract | A compound of formula (I): ** (See formula) ** or a stereoisomer, a tautomer, an N-oxide, a pharmaceutically acceptable salt or a solvate thereof, wherein: ring A is independently selected from the group consisting of: benzene, cyclohexane, indane, tetrahydronaphthalene, naphthalene, isoxazoline, isoxazole, pyrazole, imidazole, triazole, piperidine, pyridine, indazole, indole, benzoimidazole, quinoline, isoquinoline, tetrahydroquinoline, and tetrahydroisoquinoline; ** (See formula) ** is independently selected from the group consisting of: ** (See formula) ** and ** (See formula) ** is independently selected from the group consisting of: ** (See formula) * * L1 is independently selected from the group consisting of: a bond, -CH2CH2-, -CH = CH-, and -C (Me) = CH. L is independently selected from the group consisting of: C3-7 alkylene and C3-7 alkenylene; wherein said alkylene and alkenylene are substituted with 0-2 R7 and, optionally, one or two of the carbon atoms of said alkylene and alkenylene can be replaced by O, NH, N (C1-4 alkyl), CONH, NHCO or CON (C1-4 alkyl); Y is independently selected from the group consisting of: -CH2-, O, NH, N (C1-4 alkyl), -NHCO-, - CONH-, -CONHCH2-, -CON (C1-4 alkyl) CH2-, -OCONH-, -NHCONH- and -SO2NH-; alternatively, L-Y is -C 3-6 alkylene-CH = N-; R1 is selected, independently at each occurrence, from the group consisting of: halogen, C1-6 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 haloalkyl, OH, OCH2F, OCHF2, OCF3, CN, NH2, NH (C1-4 alkyl), N (C1-4 alkyl) 2, CO2 (C1-4 alkyl), CO (C1-4 alkyl), -CH2NH2, -CONH2, -CONH (C1-4 alkyl), -OCH2CO2H , -NHCO (C1-4 alkyl), -NHCO2 (C1-4 alkyl), -NHSO2 (C1-4 alkyl), -SO2NH2, -C (= NH) NH2 and phenyl substituted with 0-2 Ra; R2 is independently selected from the group consisting of: triazolyl and tetrazolyl; R3 is independently selected from the group consisting of: H, halogen, and C1-4 alkyl; R4 is independently selected from the group consisting of: H, and C1-4 alkyl; R6 is selected, independently at each occurrence, from the group consisting of: halogen, NH2, CO2H, CO2 (C1-4 alkyl), CONH2, CONH (C1-4 alkyl), CON (C1-4 alkyl) 2, - NHCO2 (C1-4 alkyl), -CH2NHCO2 (C1-4 alkyl), -NHCO2CH2CO2H, -NHCO2 (CH2) 2OH, -NHCO2 (CH2) 2O (C1-4 alkyl), -NHCO2CH2CH (C1-4 alkyl) O ( C1-4 alkyl), ** (See formula) ** R7 is selected, independently at each occurrence, from the group consisting of: halogen, OH, NH2, CH2NH2, C1-4 haloalkyl, OCH2F, OCHF2, OCF3, - NH (C1-4 alkyl), -N (C1-4 alkyl) 2, C1-4 alkoxy, CH2OH, CH2O (C1-4 alkyl), CH2O (CH2) 1-4O (C1-4 alkyl), CO2H, CO2 (C1-4 alkyl), CO2 (CH2) 2O (C1-4 alkyl), CO2 (C1-4 haloalkyl), CO2 (CH2) 2SO2 (C1-4 alkyl), CH2CO2H, CH2CO2 (C1-4 alkyl), CONH2 , CONH (C1-4 alkyl), CON (C1-4 alkyl) 2, -OCO (C1-4 alkyl), -CH2NH (CH2) 2O (C1-4 alkyl), -CONH (C1-4 alkoxy), - CO2 (CH2) 2O (C1-4 alkyl), -CO2 (CH2) 2N (C1-4 alkyl) 2, -CONH (CH2) 2O (C1-4 alkyl), -CONH (CH2) 2N (C1-4 alkyl ) 2, -CON (C1-4 alkyl) (CH2) 2O (alkyl C1-4), -CON (C1-4 alkyl) (CH2) 2N (C1-4 alkyl) 2, C1-4 alkyl, -CONHBn, -CONH (OBn), - (CO) 0-1 (CH2) 0 -3-C3-6 carbocycle and - (CH2) 0-1- (CO) 0-1- (W) 0-1- (CH2) 0-2- (4- to 6-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NH, N (C1-4 alkyl), O and S (O) p); wherein said carbocycle and heterocycle are substituted with 0-2 R8; R8 is selected, independently at each occurrence, from the group consisting of: halogen, OH, CHF2, CF3, C1-4 alkoxy, CH2OH, CO2H, CO2 (C1-4 alkyl), CONH2, and C1-4 alkyl; Ra is selected, independently at each occurrence, from the group consisting of: halogen, OH, CF3, C1-4 alkoxy, and C1-4 alkyl; W is independently selected from the group consisting of: O, NH, and N (C1-4 alkyl) and p is selected, independently at each occurrence, from the group consisting of: 0, 1, and 2. |
priorityDate | 2010-02-11-04:00^^<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: 1514.