http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2349428-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/C07D207-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4725 |
| filingDate | 2006-01-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2011-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9d4e7e68dc92da3faf7b87fb8a39756f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6c039ad579599d4f1444b59e3959c7a6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ac5ded4dc66b0fd134fa9af3dd6f3e12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c9daf09cc228455de70057063a1a7421 |
| publicationDate | 2011-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2349428-T3 |
| titleOfInvention | USEFUL PHENYLGLYCINAMIDE DERIVATIVES AS ANTICOAGULANTS. |
| abstract | A compound of Formula (Ia): ** Formula ** or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate thereof, wherein: R1 is H, F, Cl, Br, C1-3 alkyl substituted with 0-1 OH, C1-3 haloalkyl, C2-3 alkenyl, C2-3 alkynyl, -O-C1-3 alkyl or C3-6 cycloalkyl; R2 and R3 are, independently each time they are present, H, F, Cl, Br, I, ORa, 10 SRa, OCF3, CN, NO2, -NRbRc, -C (O) Ra, -CO2Ra, -NRdC (O ) Ra, -C (O) NRcRd, NRcC (O) ORa, -NRcC (O) NRcRd, -SO2NRcRd, -NRcSO2NRcRd, -NRcSO2Ri, -NRcSO2CF3, SO2CF3, -S (O) pRi, - (CF2) rC, - (CF2) rC, - (CF2) rC C1-6 alkyl substituted with 0-2 Re, C2-6 alkenyl substituted with 0-2 Re, C2-6 alkynyl substituted with 0-2 Re, C3-10 carbocycle substituted with 0-3 Rf or a 5-10 heterocycle members comprising: carbon atoms and 1-4 heteroatoms selected from N, NRc, O and S (O) p, said heterocycle being substituted with 0-3 Rf; R4 is, independently each time it is present, H, F, Cl, Br, I, ORa, SRa, OCF3, CN, NO2, -NRbRc, -C (O) Ra, -CO2Ra, -NRdC (O) Ra, -C (O) NRcRd, -NRcC (O) ORa, - NRcC (O) NRcRd, -SO2NRcRd, -NRcSO2NRcRd, -NRcSO2Ri, -NRcSO2CF3, -SO2CF3, 20 S (O) pRi, - (CF2) rCF C1-6 substituted with 0-2 Re, C2-6 alkenyl substituted with 0-2 Re, C2-6 alkynyl substituted with 0-2 Re, C3-10 carbocycle substituted with 0-3 Rf or a 5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRc, O and S (O) p, said heterocycle being substituted with 0-3 Rf; alternatively, R2 and R3 can be combined to form a 5-7 membered carbocycle or heterocycle comprising: carbon atoms and 0-4 heteroatoms selected from N, NRc, O and S (O) p, said carbocycle and heterocycle being substituted with 0-3 Rf as an alternative, R3 and R4 can be combined to form a 5- to 7-membered carbocycle or heterocycle comprising: carbon atoms and 0-4 heteroatoms selected from N, NRc, O and S (O) p, being said carbocycle and heterocycle substituted with 0-3 Rf Z is substituted with 0-2 R6 and is selected from: ** Formula ** W is NH or O; R6 is, independently each time it is present, F, Cl, CH3, OH or CF3; X1 and X2 are, independently each time they are present, H or NH2; R7 is, independently each time it is present, ORa, F, Cl, Br, I, CN, NO2, 10 OCF3, -NRbRc, -C (O) Ra, -CO2Ra, -NRdC (O) Ra, -C ( O) NRcRd, -SO2NRcRd, -NRcSO2Ri, - SO2NHC (O) Ra, -C (O) NHSO2Ra, -NRcSO2CF3, -SO2CF3, -S (O) pRi, - (CF2) rCF3, tetrazole, (CH2) r- phenyl substituted with 0-3 Rf or a - (CH2) 5- to 6-membered r-heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRc, O and S (O) p, said heterocycle being substituted with 0-3 Rf; R9 is selected from: ** Formula ** R10a and R10b are, independently each time they are present, H, F, Cl, Br, I, (CH2) r-ORa, SRa, OCF3, SCF3, CN, NO2, - B (OH) 2, - (CH2) r-NRbRc, -C (O) Ra, - (CH2) rCO2Ra, - (CH2) r-NRcCO2Ra. -NRdC (O) Ra, - (CH2) rC (O) NRcRd, -NRcC (O) NRcRd, 20 SO2NRcRd, -OSO2NRcRd, -NRcSO2NRcRd, -NRcSO2Ri, -NRcSO2CF3, -SO2CF3, -S (O) 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) C3-10 r-carbocycle substituted with 0 -3 Rf or (CH2) 5-10 membered r-heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRc, O and S (O) p, said heterocycle being substituted with 0-3 Rf; Ra is, independently each time it is present, H, C1-6 alkyl substituted with 04 Rh, - (CH2) r-carbocycle C3-7 substituted with 0-4 Rf or - (CH2) r-heterocycle of 5 to 10 members comprising: carbon atoms and 1-4 heteroatoms selected from N, NRg, O and S (O) p, said heteroaryl being substituted with 0-4 Rf; Rb is, independently whenever present, H, C1-6 alkyl, - (CH2) n-phenyl, (C1-6 alkyl) C (O) -, (C3-6 cycloalkyl) -C0-4-C alkyl (O) -, (C6-10 aryl) - (C0-4 alkyl) -C (O) -, (5-10 membered heteroaryl) -C0-4-C alkyl (O) -, (C1-6 alkyl ) -NHC (O) -, (C1-6 alkyl) 2NHC (O) -, (C6-10 aryl) -C0-4-NHC (O) -, (5-10 membered heteroaryl) -C0 alkyl 4 NHC (O) -, (C1-6 alkyl) -SO2-, (C6-10 aryl) -C0-4-SO2- alkyl or (5-10 membered heteroaryl) -C0-4-SO2- alkyl, being said phenyl, aryl and heteroaryl substituted with 0-2 Rf; Rc is, independently whenever present, H, C1-6 alkyl substituted with 03 Rh, - (CH2) n-C3-7 cycloalkyl substituted with 0-3 Rh or - (CH2) n-phenyl substituted with 0-3 Rh; alternatively, Rb and Rc, when attached to the same nitrogen atom, can be taken together with the nitrogen atom to form a 4-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRg, O, and S (O) p, the heterocycle being substituted with 0-3 Rf; Rd is, independently each time it is present, H, C1-6 alkyl, - (CH2) C3-10 carboxy substituted with 0-3 Rf or a 5- (CH2) r-heterocycle of 5 to 12 members comprising: atoms of carbon and 1-4 heteroatoms selected from N, NRg, O and S (O) p, said heterocycle being substituted with 0-3 Rf; alternatively, Rc and Rd, when attached to the same nitrogen atom, can be taken together with the nitrogen atom to form a 4-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRg, O and S (O) p, the heterocycle being substituted with 0-3 Rf; Re is, independently each time it is present, = O, ORa, F, Cl, Br, I, CN, NO2, -SRa, -OCF3, -NRbRc, -C (O) Ra, -CO2Ra, -NRdC (O ) Ra, -C (O) NRcRd, -OC (O) Ra, NRdC (O) ORa, -NRdC (O) NRcRd, -OC (O) NRcRd, -SO2NRcRd, -NC (O) ORa, -NRcSO2NRcRd, -NRcSO2Ri, -NRcSO2CF3, -SO2CF3, -S (O) pRi, - (CF2) rCF3, C3-10 carbocycle substituted with 0-3 Rf or a 5- to 12-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRg, O and S (O) p, said heterocycle being substituted with 0-3 Rf; Rf is, independently each time it is present, = O, ORg, F, Cl, Br, I, CN, NO2, -SRg, -OCF3, -NRcRc, -C (O) Rg, -CO2Rg, -NRcC (O ) Rg, -C (O) NRcRc, -OC (O) Rg, NRcC (O) ORg, -NRcC (O) NRcRc, -OC (O) NRcRc, -SO2NRcRc, -NRcSO2NRcRc, -NRcSO2Ri, NRcSO2CF3, -SO2CF3, -SO2CF3, -SO2CF3 , -S (O) pRi, - (CF2) rCF3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocycle substituted with 0-3 Rh or a 5- to 12-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRg, O and S (O) p, and substituted with 0-3 Rh; Rg is, independently each time it is present, H, C1-6 alkyl or - (CH2) n-phenyl; Rh is, independently each time it is present, = O, - (CH2) rORg, F, Cl, Br, I, CN, NO2, -OCF3, -NRgRg, -C (O) Rg, -CO2Rg, -NRgC ( O) Rg, -C (O) NRgRg, -SO2NRgRg, NRgSO2NRgRg, -NRgSO2-C1-4alkyl, -NRgSO2CF3, -NRgSO2-phenyl, -SO2CF3, -S (O) C1-4 -alkyl, -S (O) p-phenyl, - (CF2) rCF3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, (C16 alkyl) C (O) -, (C3-6 cycloalkyl) -C0-4-C alkyl (O ) -, (C6-10 aryl) - (C0-4 alkyl) -C (O) -, (510-member heteroaryl) -C0-4-C alkyl (O) -, (C1-6 alkyl) -NHC ( O) -, (C1-6 alkyl) 2-NHC (O) -, (C6-10 aryl) C0-4-NHC alkyl (O) -, (5-10 membered heteroaryl) -C0-4-NHC alkyl (O) -, (C1-6 alkyl) -SO2, (C6-10 aryl) -C0-4-SO2- alkyl, (5-10 membered heteroaryl) -C0-4-SO2- alkyl, - (CH2) C3-10carbocycle or a - (CH2) 5 to 12 membered r-heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRg, O and S (O) p; Ri is, independently whenever present, H, C1-6 alkyl substituted with 03 Rh, C3-6 cycloalkyl substituted with 0-3 Rh, - (CH2) n-phenyl substituted with 0-3 Rh, - (CH2) 5 to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRg, O and S (O) p, said heterocycle being substituted with 0-3 Rh; n, in each case, is selected from 0, 1, 2, 3 and 4; p, in each case, is selected between 0, 1 and 2; r, in each case, is selected from 0, 1, 2, 3 and 4; and t is selected from 0, 1, 2 and 3. |
| priorityDate | 2005-01-10-04:00^^<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: 1246.