http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-047521-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0a910d33c239980f3a705e312c5bad6a |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-98 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-86 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-98 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4412 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-86 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 |
| filingDate | 2005-01-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2006-01-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-047521-A1 |
| titleOfInvention | PIRIDIN-2-ONA COMPOUNDS USEFUL AS THROMBIN INHIBITORS |
| abstract | The compounds referred to herein are useful in the treatment of conditions in which thrombin inhibition is beneficial (eg conditions, such as thrombus embolisms, where thrombin inhibition is required or desired, and / or conditions in which anticoagulant treatment is indicated Claim 1: A compound of formula (1) in which the dotted line is absent or represents a bond; A represents C (O), S (O) 2, C (O ) O (in whose last group the remainder O is attached to R1), C (O) NH, S (O) 2NH (in whose last two groups the remainder NH is bound to R1) or C1-6 alkylene; R1 represents ( a) C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl (whose last three groups are optionally substituted with one or more substituents selected from halo, CN, C3-10 cycloalkyl (optionally substituted with one or more substituents selected from halo, OH, = O, C1-6 alkyl, C1-6 alkoxy and aryl), OR4a, S (O) nR4b, S (O) 2N (R4c) (R4d), N (R4e) S (O ) 2R4f, N (R4g) ( R4h), B1-C (O) -B2-R4i, aryl and Het1), (b) C3-10 cycloalkyl or C4-10 cycloalkenyl (whose last two groups are optionally substituted with one or more halo substituents selected, = O, CN, C1-10 alkyl, C3-10 cycloalkyl (optionally substituted with one or more substituents selected from halo, OH, = O, C1-6 alkyl, C1-6 alkoxy and aryl), OR4a, S ( O) nR4b, S (O) 2N (R4c) (R4d), N (R4e) S (O) 2R4f, N (R4g) (R4h), B3-C (O) -B4-R4i, aryl and Het2, ( c) aryl, or (d) Het3; R4a to R4i independently represent, at each occurrence, (a) H, (b) C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl (whose last three groups are optionally substituted with one or more substituents selected from halo, OH, C1-6 alkoxy, aryl and Het4), (c) C3-10 cycloalkyl, C4-10 cycloalkenyl (whose last two groups are optionally substituted with one or more substituents selected from halo, OH, = O, C1-6 alkyl, C1-6 alkoxy, aryl and Het5), (d) aryl or (e) Het6, provided that R4b does not represent H when n is 1 or 2; the group -DE- (a) when the dotted line represents a link, represent ta -C (R5a) = C (R5b) -, or (b) when the dotted line is absent, represents -C (R6a) ( R6b) -C (R7a) (R7b) -; R5a represents H, halo, OH, C1-4 alkyl, (whose last group is optionally substituted with C1-3 alkoxy) or C1-4 alkoxy; R5b, R6a, R6b, R7a and R7b independently represent H, F or methyl; R2 represents (a) H, (b) halo; (c) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy (whose last four groups are optionally substituted with one or more substituents selected from halo, OH, C1-4 alkoxy, C ( O) OH, C (O) O-C1-4 alkyl and OC (O) -C 1-4 alkyl) or (d) together with R3a, R2 represents n-C2-3 alkylene, or (n-C1-2 alkylene ), whose last two groups are substituted with halo and where the O atom of the last group is attached to the C atom to which the R2 group is attached; R3a and R3b independently represent H, F or methyl, together with R2, represents C2-3 n-alkylene, or (C1-2 n-alkylene) whose last two groups are optionally substituted with halo and where the atom Or from the last group is attached to the C atom to which the R2 group is attached; (b) together with R2, R3a and R3b represent T2- (H) =], in which T2 is attached to G represents (a) -C (O) N (R8a) - [CH (C (O) R9) 0-1-C0-3- (Q1) alkylene a-, (b) -C (O) N (R8b) -C2-3alkenylene- (Q1) a-, (c) as shown in formula (2) , or (d) as shown in formula (3), R9 represents H or a 5 to 10 membered aromatic heterocyclic group comprising one or two rings and containing, as heteroatom (s), an S or O atom and / or one or more N atoms, whose heterocyclic is optionally substituted with one or more substituents selected from halo and C1-6 alkyl; Q1 represents O, NR10a, [N (H)] 0-1C (O) - C0-2 alkylene, C (O) NHNHC (O), or -N = C (R10b) -; a represents 0 or 1; Q2a represents, any of the groups of formulas (4); Q2b represents any of the groups of formulas (5); L represents (a) C0-6-Ra alkylene, (b) C0-2-CH alkylene = CH0-2-Ra alkylene; (c) C0-2-C alkylene ::: C- C0-2-Ra alkylene, (d) represents the group e formula (6), (e) represents the group of formula (7) in which the dotted line represents an optional double bond, or (f) represents a group of formula (8); Ar represents phenyl or naphthyl; Het represents a 5 to 10 membered heterocyclic group comprising one or two rings and containing, as heteroatom (s), an S or O atom and / or one or more N atoms; R11a represents H or one or more substituents selected from halo, OH, CN, C1-6 alkyl, C1-6 alkoxy (these last two groups are optionally substituted with one or more substituents selected from halo, OH, C1-4 alkoxy , C (O) OR12a and C (O) N (R12b) R12c); R11b and R11c independently represent H or one or more substituents selected from halo, OH, CN, C1-6 alkyl, C1-6 alkoxy (whose last two groups are optionally substituted with one or more halo substituents selected, OH, C1-4 alkoxy, C (O) OR12a and C (O) N (R12b) R12c), = O, = NH, = NOH and = N-CN; R12a to R12c independently represent H, C1-6 alkyl or C3-7 cycloalkyl (whose last two groups are optionally substituted with one or more halo atoms); Ra a Rd independently represent (a) a (h) any of formulas (9 to 16) or Rb a Rd can also represent H; Q3 represents O, N (R10c), S (O) 2, S (O) 2NH, C (O) or -CH = N-; Q4 represents O, S or CH2; a represents 0 or 1; R13a to R13c independently represent (a) H, (b) CN, (c) NH2, (d) OR15 or (e) C (O) OR16; R15 represents (a) H, (b) C1-10 alkyl, C3-10 alkenyl, C3-10 alkynyl, (c) C3-10 cycloalkyl, C4-10 cycloalkenyl, the last two groups of which are optionally substituted with one or more substituents selected from halo and C1-6 alkyl, or (d) C1-3 alkyl, whose last group is optionally interrupted by O and is substituted by aryl or -O-aryl; R16 represents (a) C1-10 alkyl, C3-10 alkenyl, C3-10 alkynyl, whose last three groups are optionally interrupted with one or more O atoms, or (b) C3-10 cycloalkyl, C4-10 cycloalkenyl , whose last two groups are optionally substituted with one or more substituents selected from halo and C1-6 alkyl, or (c) C1-3 alkyl, whose last group is optionally interrupted by O and substituted with aryl or -O -aryl; R8a to R8c, R10a to R10c and R14a to R14g independently represent (a) H or (b) C1-4 alkyl (whose last group is optionally substituted with one or more substituents selected from halo and OH); or R14c represents (a) C1-4 alkyl substituted by C3-7 cycloalkyl or aryl; (b) C3-7 cycloalkyl, (c) C (O) O-C1-6 alkyl (whose alkyl part of the last group is optionally substituted with aryl and / or one or more halo atoms), (d) C ( O) C1-6 alkyl, (e) C (O) N (H) -C1-6 alkyl (whose alkyl part of the last group is optionally substituted with aryl and / or one or more halo atoms) or (f) S (O) 2-C1-6 alkyl (whose alkyl part of the last group is optionally substituted with aryl and / or one or more halo atoms), or R14c and R14d together represent optionally interrupted C3-6 n-alkylene by O, S. N (H) or N (C1-4 alkyl) and / or substituted with one or more C1-4 alkyl groups; each aryl independently represents a C6-10 carbocyclic aromatic group, which may comprise both one and two rings and may be substituted with one or more substituents selected from (a) halo, (b) CN, (c) C1- alkyl 10, C2-10 alkenyl, C2-10 alkynyl (whose last three groups are optionally substituted with one or more substituents selected from halo, OH, C1-6 alkoxy, C (O) OH, C (O) O-alkyl C1-6, phenyl (this last group is optionally substituted with halo) and Het7), (d) C3-10 cycloalkyl, C4-10 cycloalkenyl (whose last two groups are optionally substituted with one or more substituents selected from halo, OH, = O, C1-6 alkyl, C1-6 alkoxy, phenyl (this last group is optionally substituted with halo) and Het8), (e) OR17a, (f) S (O) pR17b, (g ) S (O) 2N (R17c) (R17d), (h) N (R17e) S (O) 2R17f, (i) N (R17g) (R17h), (j) B5-C (O) -B6-R17i , (k) phenyl (whose last group is optionally substituted with halo), (l) Het9 and (m) Si (R1 8a) (R18b) (R18c); R17a to R17i independently represent, at each occurrence, (a) H, (b) C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl (whose last three groups are optionally substituted with one or more substituents selected from halo, OH, C1-6 alkoxy, phenyl (whose last group is optionally substituted with halo) and Het10), (c) C3-10 cycloalkyl, C4-10 cycloalkenyl (whose last groups are optionally substituted with one or more substituents selected from halo, OH, = O, C1-6 alkyl, C1-6 alkoxy, phenyl (whose last group is optionally substituted with halo) and Het11), (d) phenyl (whose last group is substituted in form optional with halo) or (e) Het12, provided that R17b does not represent H when p is 1 or 2; Het 1 to Het12 independently represent 4 to 14 membered heterocyclic groups containing one or more heteroatoms selected from O, N and / or S, whose heterocyclic groups may comprise 1, 2 or 3 rings and may be substituted with one or more more substituents selected from (a) halo, (b) CN, (c) C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl (whose last four groups are optionally substituted with one or more halo substituents selected, OH, C1-6 alkoxy, C (O) OH, C (O) O-C1-6 alkyl, phenyl (whose last group is optionally substituted with halo) and Het a), (d) C3-10 cycloalkyl, C4-10 cycloalkenyl (whose last two groups are optionally substituted with one or more substituents selected from halo, OH, = O, C1-6 alkyl, C1-6 alkoxy, phenyl (whose last group is optionally substituted with halo ) and Het b), (e) = O, (f) OR19a, (g) S (O) qR19b, (h) S (O) 2N (R19c) (R19d), (i) N (R19e) S ( O) 2R19f, (j) N (R19g) (R19h), |
| priorityDate | 2004-02-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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