http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2359857-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-74 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-56 |
| filingDate | 2006-01-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2011-05-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_97fcb7d06eb87afbd2b2df3682d5c45c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb78c39887128023a882182ed0b8e856 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_66fcc6337d407c3e09475eb9676da499 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a4ad75e5525414a5d62f3c3835491040 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5752d023961cb420d32c7bdc816c2cde http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_45538783968e97ac8c9abbd7ee28e10d |
| publicationDate | 2011-05-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2359857-T3 |
| titleOfInvention | DERIVATIVES OF 2-FENOXI-N- (1,3,4-TIADIZOL-2-IL) PIRIDIN-3-AMINA AND RELATED COMPOUNDS AS INHIBITORS OF THE P2Y1 RECEPTOR FOR THE TREATMENT OF THROMBOEMBOLIC DISORDERS. |
| abstract | A compound of Formula (II): ** Formula ** or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate thereof, in which: ring A is selected from: alternatively, ring A is substituted with 0-3 R1 and is selected from: R1, R1a R1b, R1c, R1d, and R1e are, independently each time they are present, H, C1-6 alkyl substituted with 10 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra , C2-6 alkynyl substituted with 0-2 Ra, Br, CN, CF3, -CF2CF3, C (NH2) = N (OH), C (O) Rc, -CH (= NOH), -C (O) ORc , NR12R13, -C (O) NR12R13, -CON (Me) (CH2) 2OH, -CO-morpholin-4yl, -SO2-morpholin-4-yl, -S (O) pNR12R13, - (CH2) r-cycloalkyl C3-6 substituted with 0-2 Rb, - (CH2) r-adamantyl substituted with 0-2 Rb, - (CH2) r-phenyl substituted with 0-4 Rb, - (CH2) rnaphthyl substituted with 0-4 Rb, - (CH2) 3 to 10-membered r-heterocycle substituted with 0-4 Rb, wherein said heterocycle is selected from: aziridinyl, azetidinyl, pyrrolidinyl, furanyl, imidazolyl, oxadiazolyl, thienyl, pyrrolyl, iso xazolyl, triazolyl, tetrazolyl, pyridinyl, pyrazinyl, pyrimidinyl, piperdinyl, morpholinyl, piperazinyl, 1,3-benzodioxolyl, benzothienyl, isoindolinyl, 1,4-diazacycloheptanyl, tetrahydroisoquinolyl and alternatively, R1a and R1b or R1b with R1b or R1b atoms carbon to which they are attached, form a 5 or 6-membered carbocycle or heterocycle comprising: additional carbon atoms and 0-3 heteroatoms selected from N, NR11, O and S (O) p, 0-2 carbonyl and 0- 1 additional double bond, wherein said carbocycle and heterocycle is substituted with 0-3 Rb; alternatively, two R1 combine with the carbon atoms to which they are attached, form a 5- or 6-membered carbocycle or heterocycle comprising: additional carbon atoms and 0-3 heteroatoms selected from N, NR11, O and S ( O) p, 0-2 carbonyl and 0-1 additional double bond, wherein said carbocycle and heterocycle is substituted with 0-3 Rb; R5 is phenyl substituted with 1-4 R5a; R5a is, independently each time it is present, F, Cl, Br, I, - (CRiRi) r-ORc, SRc, CN, CF3, -CF2CF3, OCF3, -OCF2CF2H, -OCF2CF3, -NR12R13, -C (O ) Rc, -C (O) ORc, -C (O) NR12R13, NR14C (O) Rd, -S (O) pNR12R13, S (O) Rd, -S (O) 2Rd, -Si (Me) 3, Si (C1-4 alkyl) 3, C1-4 haloalkyl, C1-4 haloalkyloxy, C1-4 alkyloxy, C1-4 alkylthio, C1-4-C alkyl (O) -, C1-4-OC alkyl ( O) -, C1-4-C alkyl (O) NH-, C1-8 alkyl substituted with 0-2 Ra, C2-8 alkenyl substituted with 0-2 Ra, C2-8 alkynyl substituted with 0-2 Ra, - (CRfRf) C3-10 r-carbocycle substituted with 0-3 Re or - (CRfRf) 5 to 10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from, N, NR11, O and S (O) p, wherein said heterocycle is substituted with 0-3 Re; alternatively, two R5a groups attached to two adjacent carbon atoms, together with the carbon atoms to which they are attached, form a 5- to 7-membered carbocyclic or heterocyclic ring comprising: carbon atoms and 0-2 heteroatoms selected from N, NR11, O and S (O) p, 0-1 carbonyl and 0-3 double bonds, wherein said carbocyclic or heterocyclic ring is substituted with 0-3 Re; R7 is H, Br, CN, NH2, NMe2 or -NH (4-OMe-Ph); R8 is H, Br, CN, NMe2 or -N (Me) (4-OMe-Ph); R11 is, independently each time it is present, H, -COPh, -COBn, -SO2Me, -SO2Ph, -SO2Bn, C1-6 alkyl substituted with 1-5 fluorine, - (CRfRf) rC (O) NR12R13, C1 alkyl -4 substituted with 0-2 Ra, - (CH2) r-C3-6 cycloalkyl substituted with 0-2 Rb, - (CH2) r-phenyl substituted with 0-3 Rb, -CHMe-phenyl substituted with 0-3 Rb or - (CH2) 5 to 10 membered heterocycle substituted with 0-3 Rb; wherein said heterocycle is selected from: furanyl, thienyl, thiazolyl, pyridyl and indolyl; R12 is, independently each time it is present, H, C1-6 alkyl substituted with 1-5 fluorine, (CRfRf) rC (O) NRfRf, C1-6 alkyl, - (CH2) r-C3-6 cycloalkyl, - ( CH2) n-phenyl, - (CH2) 5-6 membered r-heterocycle selected from pyrrolidinyl, furanyl, thienyl, pyrrolyl, isoxazolyl, triazolyl, tetrazolyl, pyridinyl, pyrazinyl, pyrimidinyl, piperdinyl, morpholinyl and piperazinyl; wherein said alkyl and phenyl are substituted with 0-2 Rg; said 5-10 membered heterocycle is substituted with 0-2 Rg; R13 is, independently each time it is present, H, C1-6 alkyl or - (CH2) n-phenyl; alternatively, R12 and R13, when bound to the same nitrogen, combine to form a 5-10 membered heterocyclic ring comprising: additional carbon atoms and 1-2 heteroatoms selected from N, NRf, O and S (O) p; R14 is, independently whenever present, H, C1-6 alkyl, C2-6 alkenyl, - (CH2) r-phenyl carbocycle substituted with 0-3 Rg, or - (CH2) 5 to 10 membered r-heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRf, O and S (O) p, wherein said heterocycle is substituted with 0-3 Rg; Ra is, independently each time it is present, H, F, OCF3, CF3; - (CRfRf) rORc, - (CRfRf) rSRc, CN, (CRfRf) rNR12R13, - (CRfRf) rC (O) Rc, - (CRfRf) rC (O) ORc, - (CRfRf) rC (O) NR12R13, - (CRfRf) rNR14C (O) Rd, (CRfRf) rS (O) pNR12R13, - (CRfRf) rS (O) Rd, - (CRfRf) rS (O) 2Rd, C1-4 alkyl substituted with 1-5 fluorine, - (CH2) C3-10 r-carbocycle substituted with 0-3 Re, or - (CH2) 5 to 10 membered r-heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRf, O and S ( O) p, wherein said heterocycle is substituted with 0-3 Re; Rb is, independently whenever present, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, F, Cl, Br, CF3 , -OCF3, - (CH2) r-ORc, - (CH2) rC (O) ORc, (CRfRf) rNR12R13, - (CH2) rC (O) NR12R13, CN, -OCH2C (Me) 2CH2NMe2, NO2, -SO2Me , OBn, - (CH2) r3-6 cycloalkyl, - (CH2) r-phenyl substituted with 0-2 Re, - (CH2) r-naphthyl substituted with 0-3 Re, - (CH2) r-heterocycle of 5 to 10 members substituted with 0-4 Re; wherein said heterocycle is selected from: thienyl, thiazolyl, imidazolyl, tetrazolyl, pyrrolidinyl, morpholinyl, piperidinyl, azepanyl, morpholinyl, piperazinyl, pyridinyl, tetrahydropyranyl or tetrahydroisoquinolinyl; Rc is, independently each time it is present, H, C1-6 alkyl substituted with 0-2 Re or - (CH2) r-phenyl substituted with 0-2 Re; Rd is, independently whenever present, CF3, OH, C1-4 alkoxy, C1-6 alkyl, - (CH2) r-carbocycle C310 substituted with 0-2 Re or - (CH2) r-heterocycle from 5 to 10 members comprising: carbon atoms and 1-4 heteroatoms selected from N, NRf, O and S (O) p, wherein said heterocycle is substituted with 0-2 Re; Re is, independently each time it is present, H, = O, - (CH2) r-ORf F, Cl, Br, I, CN, NO2, (CH2) rNR12R13, -C (O) Rf, - (CH2) rC (O) ORf, -NR14C (O) Rf, - (CH2) rC (O) NR12R13, -SO2NR12R13, -NR14SO2NR12R13, NR14SO2- C1-4 alkyl, -NR14SO2CF3, -NR14SO2-phenyl, -S (O) 2CF3 , -S (O) p-C1-4 alkyl, -S (O) p-phenyl, - (CF2) rCF3, Si (C1-4 alkyl) 3, C1-8 alkyl substituted with 0-2 Rg, C2 alkenyl -8 substituted with 0-2 Rg, C2-8 alkynyl substituted with 0-2 Rg, - (CH2) C3-8 r-cycloalkyl substituted with 0-2 Rg, - (CH2) C6-10 r-aryl substituted with 0 -2 Rg or - (CH2) 5 to 10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRf, O and S (O) p, wherein said heterocycle is substituted with 0-2 Rg; alternatively, two Re groups, together with the carbon atoms to which they are attached, form a 5- to 7-membered carbocyclic ring comprising: carbon atoms and 0-2 heteroatoms selected from N, NRf, O and S (O ) p, 0-1 carbonyl and 0-3 double bonds, wherein said carbocyclic or heterocyclic ring is substituted with 0-2 Rg; Rf is, independently each time it is present, H, F, C1-6 alkyl or - (CH2) n-phenyl; Rg is, independently each time it is present, H, = O, ORf, F, Cl, Br, I, CN, NO2, -NRfRf, -C (O) Rf, C (O) ORf, -NRfC (O) Rf, -C (O) NRfRf, -SO2NRfRf, -NRfSO2NRfRf, -NRfSO2-S (O) p-C1-4 alkyl, -S (O) p-phenyl, (CF2) rCF3, C1-6 alkyl, C2 alkenyl -6 or C2-6 alkynyl; Ri is, independently each time it is present, H or C1-6 alkyl; n, each time it is present, is selected from 0, 1, 2, 3 and 4; p, each time it is present, is selected between 0, 1 and 2; and r, each time it is present, is selected from 0, 1, 2, 3 and 4. |
| priorityDate | 2005-01-19-04:00^^<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: 1310.