http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2380648-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/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 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/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-501 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 |
| filingDate | 2009-03-12^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2012-05-17^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_209fb42f75d42308965b47d7983b89fc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2ba0a646a2372edfbd7edce4e34a8d1e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fe2bdffced54682eba189c82dfabd74c |
| publicationDate | 2012-05-17^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2380648-T3 |
| titleOfInvention | Pyridazine derivatives as XIA factor inhibitors |
| abstract | A compound of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein: A is phenyl additionally substituted with 0-3 R1, or pyridyl additionally substituted with 0-3 R1; L1 is -CH (R5) CH2-, -CH (NR7R8) CH2-, -C (5 R5) = CH-, -C≡C-, -OCH2-, -CR5R6NH-, -CH2O-, -SCH2-, -S (O) CH2-, - SO2CH2-, -CH2NR10- or -NHNH-; L2 is -CONH- or -NHCO-; with the proviso that when L1 is -NHNH-, -OCH2-, or -SCH2-, then L2 is -CONH-; M is selected from the group consisting of: and R1 is, independently each time it appears, F, Cl, Br, I, OCF3, CHF2, CF3, - (CH2) rORa, - (CH2) rSRa, CN, NO2, - (CH2) rNR7R8, - (CH2) tC (O) ORa, - (CH2) rOC (O) Ra, -C (= NR8) NR8R9, - (CH2) rC (O) NR8R9, - (CH2) rNR8C ( O) Rc, - (CH2) rNR8C (O) ORc, -NR8C (O) NR8Rc, -S (O) pNR8R9, -S (O) Rc, -S (O) 2Rc or C1-6 alkyl substituted with 0- 1 R13; R2 is H, - (CH2) rC (O) Ra, - (CH2) rORa, - (CH2) rNR7R8, C1-6 alkyl substituted with 0-1 R2a, - (CH2) 3 to 7 membered r-carbocyl substituted with 0-2 R2b, or - (CH2) 5 to 7 membered r-heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, O, and S (O) p, wherein said heterocycle is substituted with 0-2 R2b; R2a is F, OCF3, CF3, ORa, SRa, CN, -NR7R8, -C (O) NR8R9, -NR8C (O) Rc, -NR8C (O) ORc, -NR8C (O) NR8Rc, - S (O) pNR8R9, -NR8SO2Rc or - (CF2) rCF3; R2b is, independently each time it appears, = O, F, Br, Cl, OCF3, CF3, - (CH2) rORa, - (CH2) rSRa, - (CH2) rCN, - (CH2) rNR7R8, - (CH2) rC (O) ORa, - (CH2) rOC (O) Ra, - (CH2) rC (O) NR8R9, - (CH2) rNR8C (O) Rc, - (CH2) rNR8C (O) ORc, - (CH2) rS (O) pNR8R9, - (CH2) rNR8SO2Rc C1-4 alkyl or - (CF2) rCF3; R3 is, independently each time it appears, - (CH2) C3-10 carboxy substituted with 0-3 R3a and 0-1 R3d, or - (CH2) 5 to 12 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p, wherein said heterocycle is substituted with 0-3 R3a and 0-1 R3d; R3a is, independently each time it appears, F, Cl, Br, I, OCF3, CF3, - (CH2) rCN, NO2, - (CH2) rORa, - (CH2) rSRa, - (CH2) rNR7R8, -NHC ( O) NR8R9, - (CH2) rC (O) ORa, -C (O) C1-4 alkyl, - (CH2) rNR8C (O) Ra, - (CH2) rNR8CO2Rc, - (CH2) rS (O) pNR8R9, - (CH2) rNR8S (O) pRc, -NHSO2CF3, -S (O) Rc, -S (O) 2Rc, - (CH2) rOC (O) Rc, - (CH2) rC (O) NR8R9, - (CH2 ) rOC (O) NR8R9, C1-4 haloalkyl, C1-4 haloalkyloxy, C1-6 alkyl, C3-6 cycloalkyl substituted with 0-1 R3d, - (CH2) C6-10 carboxy substituted with 0-3 R3d or - (CH2) 5 to 10 membered r-heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p, wherein said heterocycle is substituted with 0-3 R3d; R3d is, independently each time it appears, H, = O, F, Cl, Br, CN, NO2, - (CH2) rNR1R8, - (CH2) rORa, -C (O) Ra, - C (O) ORa, -OC (O) Ra, -NR8C (O) Rc, -C (O) NR8R9, -S (O) 2NR8R9, -NR7R8, -NR8S (O) 2NR8R9, -NR8S (O) 2Rc, -S (O) pRc, - (CF2) rCF3, C1-6 alkyl substituted with 0-2 Re, C2-6 alkenyl substituted with 0-2 Re, C2-6 alkynyl substituted with 0-2 Re, - (CH2) r-carbocycle C3- 10 substituted with 0-3 Rd, or - (CH2) 5 to 10 membered r-heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p, wherein said heterocycle is substituted with 0-3 Rd; R4 is, independently each time it appears, H, F, Cl, Br, I, OCF3, CF3, CN, NO2, - (CH2) rORa, - (CH2) rSR8, - (CH2) rC (O) Ra, - (CH2) rC (O) ORa, -OC (O) Ra, - (CH2) rNR7R8, -NR8 (CH2) rC (O) ORa, - (CH2) rC (O) NR8R9, - (CH2) rNR8C (O ) Rc, - (CH2) rNR8C (O) 2Rb, - (CH2) rNR8C (O) NR8R9, -S (O) pNR8R9, -NR8S (O) pRc, - (CH2) rS (O) 2Rc, - (CH2 ) rOP (O) (ORa) 2, C1-4 alkyl substituted with 0-2 R4a, or C2-4 alkenyl substituted with 0-2 R4a; R4a is, independently each time it appears, H, F 5, = O, C1-6 alkyl, ORa, SRa, CF3, CN, NO2, -C (O) Ra, - C (O) ORa, -NR7R8, - C (O) NR8R9, -NR8C (O) Rc, -S (O) pNR8R9, -NR8S (O) pRc, -S (O) Rc, or -S (O) 2Rc; R5 is, independently each time it appears, H, F, CF3, - (CH2) rORa, = O, - (CH2) rNR7R8, -S (O) pNR8R9, - (CH2) rCO2Ra, - (CH2) rCONR8R9 or alkyl C1-4; R6 is, independently each time it appears, H, F or C1-4 alkyl; R7 is, independently each time it appears, H, C1-6 alkyl, - (CH2) n-C3-10 carbocycle, - (CH2) n- (5-membered heteroaryl), -C (O) Rc, - CHO, -C (O) 2Rc, -S (O) 2Rc, -CONR8Rc, -OCONHRc, -C (O) O- (C1-4 alkyl) OC (O) - (C1-4 alkyl), or -C (O) O- (C1-4 alkyl) OC (O) - (C6-10 aryl); wherein said alkyl, carbocycle, heteroaryl and aryl are substituted with 0-2 Rf; wherein said heteroaryl comprises: carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p; R8 is, independently each time it appears, H, C1-6 alkyl, - (CH2) n-phenyl, or - (CH2) 5 to 10-membered n-heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p; wherein said alkyl, phenyl and heterocycle are optionally substituted with 0-2 Rf; alternatively, R7 and R8, when bound to the same nitrogen, combine to form a 5-10 membered heterocycle comprising: carbon atoms and 0-3 heteroatoms more selected from N, O and S (O) p, in which said heterocycle is substituted with 0-2 Rf; R9 is, independently each time it appears, H, C1-6 alkyl, or - (CH2) n-phenyl; wherein said alkyl and phenyl are optionally substituted with 0-2 Rf; alternatively, R8 and R9, when bound to the same nitrogen, combine to form a 5-12 membered heterocycle comprising: carbon atoms and 0-2 heteroatoms more selected from N, O and S (O) p, in which said heterocycle is substituted with 0-2 Rd; R10 is, independently each time it appears, H or C1-6 alkyl substituted with 0-3 R10a; R10a is, independently each time it appears, H, = O, C1-4 alkyl, ORa, SRa, F, CF3, CN, NO2, -C (O) Ra, - C (O) ORa, -C (O) NR8R9, -NR8C (O) Rc, -S (O) pNR8R9, -NR8S (O) pRc, or -S (O) pRc; R11 is C1-4 haloalkyl, C1-6 alkyl substituted with 0-3 R11a, C2-6 alkenyl substituted with 0-3 R11a, C2-6 alkynyl substituted with 0-3 R11a, - (CH2) s-C3-10 carbocycle substituted with 0-3 R11b, or - (CH2) 4-membered s-heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p, wherein said heterocycle is substituted with 0-3 R11b; R11a is, independently each time H appears, = O, ORa, SRa, F, CF3, CN, NO2, -C (O) Ra, -C (O) ORa, -NR7R8, - C (O) NR8R9, - NR8C (O) Rc, -NR8C (O) ORc, -NR8CHO, -S (O) pNR8R9, -NR8S (O) pRc, -S (O) pRc, C1-4 alkyl, C3-6 cycloalkyl, C1- haloalkyl 4, C1-4 haloalkyloxy, - (CH2) C3-10 r-carbocycle substituted with 0-3 Rd, or - (CH2) 5 to 10 membered r-heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p, and is substituted with 0-3 Rd; R11 is, independently each time it appears, H, = O, = NR8, ORa, -CH2ORa, F, Cl, Br, CN, NO2, CF3, OCF3, OCHF2, -C (CH3) 2ORa, -C (O) Ra, -C (O) ORa, -NR7R8, -C (O) NR8R9, -NR7C (O) Rb, -NR8C (O) 2Rc, -NR8C (O) NR8R9, - S (O) pNR8R9, -NR8S ( O) pRc, -S (O) pRc, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C1-4 haloalkyl, C1-4 haloalkyloxy, - (CH2) C3-carbocycle -10 substituted with 0-3 Rd, or - (CH2) 5 to 10 membered r-heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p, and is substituted with 0- 3 Rd; R12 is, independently each time it appears, H, C1-6 alkyl substituted with 0-2 Rf, or - (CH2) n-phenyl; R13 is F, OCF3, CF3, ORa, SRa, CN, -NR7R8, -C (O) NR8R9, -NR8C (O) Rc, -S (O) pNR8R9, -NR8SO2Rc or - (CF2) rCF3; Ra is, independently each time it appears, H, CF3, C1-6 alkyl, - (CH2) r3-7 cycloalkyl, - (CH2) C6-10 r-aryl, or - (CH2) r-heterocycle of 5 to 10 members comprising carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p; wherein said s, alkyl, cycloalkyl, aryl or heterocycle groups are substituted with 0-2 Rf; Rb is, independently each time it appears, CF3, OH, C1-4 alkoxy, C1-6 alkyl substituted with 0-2 Rd, - (CH2) C3-10 carbocycle substituted with 0-2 Rd, or - (CH2) r - 5 to 10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p and is substituted with 0-3 Rd; Rc is, independently each time it appears, CF3, C1-6 alkyl substituted with 0-2 Rf, C3-6 cycloalkyl substituted with 0-2 Rf, C6-10 aryl, 5-10 membered heteroaryl, (C6-10 aryl ) -C 1-4 alkyl, or (5-10 membered heteroaryl) -C 1-4 alkyl, wherein said aryl is substituted with 0-3 Rf and said heteroaryl comprises: carbon atoms and 1-4 heteroatoms selected from N , O and S (O) py is substituted with 0-3 Rf; Rd is, independently each time it appears, H, = O, = NR8, ORa, F, Cl, Br, I, CN, NO2, -NR7R8, -C (O) Ra, -C (O) ORa, -OC (O) Ra, -NR8C (O) Rc, -C (O) NR8R9, -SO2NR8R9, -NR8SO2NR8R9, -NR 5 8SO2-C1-4 alkyl, -NR8SO2CF3, - NR8SO2-phenyl, -S (O) 2CF3, -S (O) p-C1-4 alkyl, -S (O) p-phenyl, - (CF2) rCF3, C1-6 alkyl substituted with 0-2 Re, C2-6 alkenyl substituted with 0-2 Re, or C2-6 alkynyl substituted with 0-2 Re; Re is, independently each time it appears, = O, ORa, F, Cl, Br, I, CN, NO2, -NR7R8, -C (O) Ra, -C (O) ORa, - NR8C (O) Rc, -C (O) NR8R9, -SO2NR8R9, -NR8SO2NR8R9, -NR8SO2-C1-4 alkyl, -NR8SO2CF3, -NR8SO2-phenyl, - S (O) 2CF3, -S (O) p-C1-4 alkyl, -S (O) p-phenyl, or - (CF2) rCF3; Rf is, independently each time it appears, H, = O, - (CH2) rORg, F, Cl, Br, I, CN, NO2, -NRgRg, -C (O) Rg, - C (O) ORg, - OC (O) Rg, -NRgC (O) Rg, -C (O) NRgRg, -SO2NRgRg, -NRgSO2NRgRg, -NRgSO2-C1-4 alkyl, -NRgSO2CF3, - NRgSO2-phenyl, -S (O) 2CF3, - S (O) p-C1-4 alkyl, -S (O) p-phenyl, - (CF2) rCF3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, - (CH2) n-phenyl, or - (CH2) 5 to 10 membered n-heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, O and S (O) p; Rg is, independently each time it appears, H, C1-6 alkyl, or - (CH2) n-phenyl; n, each time it appears, is selected from 0, 1, 2, 3 and 4; p, each time it appears, is selected between 0, 1 and 2; and r, each time it appears, is selected between 0, 1, 2, 3 and 4. s, each time it appears, is selected between 1, 2, 3 and 4. |
| priorityDate | 2008-03-13^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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