http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2770026-T3
Outgoing Links
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|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c5cf811e10ad9068ddf72c04b69c8ba8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-05 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-497 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5025 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5386 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-541 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-553 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K51-0453 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 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/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B59-002 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4355 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-433 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-435 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4439 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4355 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-433 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5025 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-02 |
| filingDate | 2013-04-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2020-06-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0a23a549c0a04742c141cbca13b8ef1a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0fc532a5ee760863ccda95e3d300e37a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fd987fb1663f2d42d7a7050040e3e658 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1be30a6a83bd0ebd5cf2863976835364 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1a6f6b6c6705b99f2448f457754c8491 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9cb61ef1ae396be99a0b71b98d4a27d2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_412760bddeeb4e0db0d22be8676459bc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_70221e70c0796cadec7b78fdb0123763 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_538e095cd9cc4374565d1e3840e7a081 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_20813a347cdab313db1a0ea49889bc9e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b9623a1695f8ce6ce1b41da6918caea1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_35edfef66633ef99c44f747f0f48e718 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_43a14e7f4cb91837f3a219c0e390e24a |
| publicationDate | 2020-06-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2770026-T3 |
| titleOfInvention | Imidazothiazole and imidazopyrazine derivatives as protease-activated receptor 4 (PAR4) inhibitors to treat platelet aggregation |
| abstract | A compound of formula I: ** (See formula) ** or a pharmaceutically acceptable stereoisomer, tautomer, salt or solvate thereof, wherein: W is O; R0 is R1; Y is S or -CR8 = CR9-; R1 is independently selected from the group consisting of: H, halo C1-C2 alkyl, cyclopropyl C1-C2 alkoxy, C1-C2 alkylthio, halo C1-C2 alkyl, containing 1 to 5 halogens, wherein halo is F or Cl, and C3-C4 halocycloalkyl R8 and R9 are independently selected from the group consisting of: H, fluorine, chlorine, C1-C3 alkyl, C1-C2 alkoxy, and C1-C2 haloalkyl; provided that at least one of R1, R8 and R9 is other than H; R2 is H; X1 is selected from the group consisting of CH or N; X2, X3 and X4 are independently selected from CR3; R3 is selected from the group consisting of H, C1-C3 alkyl, C1-C3 alkoxy, fluorine, chlorine, OCF3, and C1-C2 haloalkyl, containing 1 to 5 halogens; R4 and R5 are independently selected from H and methyl; ** (See formula) ** is a 5-membered heteroaryl ring selected from thiazole, thiadiazole, oxazole, oxadiazole and triazole; R6 is selected from the group consisting of H, halo, OCF3, OCHF2, OH, CN, NO2, NR11R12, C1-C4 alkoxycarbonyl, (C = O) NR11R12, and C1-C5 alkyl substituted with 0 to 7 groups independently selected from halo, CF3, OCF3, OH, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkoxy, C1-C4 dialkylaminophenyl- C1-C4 alkyl, (C1-C4 dialkoxy-C1-C4 alkyl) -C1-C4 alkyl, C1-C4 dialkylamino, C3-C6 cycloalkyl, and C1-C4 alkylthio or R6 is BD-, where D is a linker that is selected from: a single bond, ** (See formula) ** alkylene C1-C4 substituted with 0 to 4 groups independently selected from halo or OH, C1-C4 alkyleneoxy, C2-C6 alkenylene and B is selected from the group consisting of: C6-C10 aryl substituted with 0 to 3 groups independently selected group consisting of halo, C1-C4 alkoxy, halo-C1-C4 alkoxy, C1-C4 alkyl, C1-C4 haloalkyl, C3-C6 cycloalkyl, cyano, nitro, NR11R12, OH, C1-C4 alkylcarbonyloxy-C1-C4 alkyl, C1-C4 hydroxyalkyl, COOR 14, SO2R14, (C = O) NR11R12, SO2NR11R12, N (R13) (C = O) NR11R12, N (R13) (C = O) OR14, N (R13) (C = O) R14, NR13S (O) R14, NR13SO2R14, O (C = O) NR11R12, O (C = O) OR14, O (C = O) R14, (C = O) OR14 and 5-6 membered heteroaryl, 5 to 10 membered heteroaryl substituted with 0 to 3 groups independently selected from the group consisting of halo, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl, C1-C4 haloalkyl, C3-C6 cycloalkyl, cyano, nitro, NR11R12, OH, C1-alkylcarbonyloxy C4-C1-C4 alkyl, C1-C4 hydroxyalkyl, COOR14, SO2R14, (C = O) NR11R12, SO2NR11R12, N (R13) (C = O) NR11R12, N (R13) (C = O) OR14, N (R13 ) (C = O) R14, NR13S (O) R14, NR13SO2R14, O (C = O) NR11R12, O (C = O) OR14, O (C = O) R14, (C = O) OR14, heteroaryl of 5 -6-membered and (CH2) phenyl, 4- to 10-membered heterocyclyl containing carbon atoms and 1 to 2 additional heteroatoms selected from N, O, and S, and substituted with 0 to 3 groups independently selected from the group consisting of halo, oxo, - (CHR13) n1-5- or 6-membered heteroaryl substituted with de 0 to 3 groups independently selected from the group consisting of halo, C1-C4 alkoxy, C1-C4 alkyl, cyclopropyl, CF3, OCF3 and CF2CH3; NR13S (O) R14, NR13SO2R14, - (CHR13) n1-4- to 10-membered heterocyclyl substituted with 0 to 3 groups independently selected from the group consisting of halo, C1-C4 alkoxy, C1-C4 alkyl, cyclopropyl, CF3, OCF3 and CF2CH3; OH, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 dialkylamino-C1-C4 alkyl, NR11R12, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C3-C6 cycloalkyl, C1-C4 alkoxy -C1-C4 alkyl, C3-C6 cycloalkyl-C1-C4 alkylcarbonyl, C6-C10 arylcarbonyl, C1-C4 alkylcarbonyloxy-C1-C4 alkyl, COOR14, SO2R14, (C = O) NR11R12, SO2NR11R12, N (R13) (C = O) NR11R12, N (R13) (C = O) OR14, N (R13) (C = O) R14, O (C = O) NR11R12, O (C = O) OR14, O (C = O) R14 , (C = O) OR14 and C6-C10 aryl substituted with 0 to 3 groups independently selected from the group consisting of halo, C1-C4 alkoxy, C1-C4 alkyl, cyclopropyl, C1-C4 alkoxycarbonyl, (C = O) NR11R12, CF3, OCF3 and CF2CH3; C3-C6 cycloalkyl which may contain unsaturation, substituted with 0 to 3 groups independently selected from the group consisting of halo, CF3, OCF3, 5- or 6-membered heteroaryl, OH, oxo, C1-C4 hydroxyalkyl, C6-C10 aryl, COOH, oxo, C1-C4 alkoxycarbonyl, (C = O) NR11R12 and C1-C4 alkyl and C5-C11 spirocycloalkyl which may contain unsaturation and optionally contains 1 to 3 heteroatoms selected from O, N or S and which is substituted with 0 to 3 groups independently selected from the group consisting of halo, CF3, OCF3, 5- or 6-membered heteroaryl, OH, C1-C4 hydroxyalkyl, C6-C10 aryl, and C1-C4 alkyl; R11 and R12 are each independently selected from the group consisting of: H, C1-C4 alkyl, C1-C4 haloalkyl, C2-C4 alkenyl, - (CR14R14) n1-phenyl substituted with 0 to 3 selected groups independently from the group consisting of halo, C1-C4 alkoxy, C1-C4 alkyl, cyclopropyl, CF3, OCF3, 5- or 6-membered heteroaryl, OH, OCHF2, C1-C4 dialkylamino and cyano, - (CHR13) n1-cycloalkyl C3-C6 substituted with 0 to 3 groups independently selected from the group consisting of halo, CF3, OCF3, 5- or 6-membered heteroaryl, OH, C1-C4 hydroxyalkyl and C1-C4 alkyl, - (CHR13) n1-heterocyclyl of 4 to 10 membered substituted with 0 to 3 groups independently selected from the group consisting of halo, CF3, OCF3, 5- or 6-membered heteroaryl, OH, oxo, C1-C4 hydroxyalkyl and C1-C4 alkyl, - (CHR13) n1 -5 to 10 membered heteroaryl substituted with 0 to 3 groups independently selected from the group consisting of halo, CF3, OCF3, 5- or 6-heteroaryl members, OH, C1-C4 hydroxyalkyl and C1-C4 alkyl, C1-C4 dialkylamino-C1-C4 alkyl, C1-C4 dialkoxy-C1-C4 alkyl, C1-C4 hydroxyalkyl, C1-C4 cyanoalkyl, C1-C4 alkoxy-alkyl C1-C4, C1-C4 alkoxycarbonyl-C1-C4 alkyl, C1-C4 alkoxycarbonyl, C1-C4 alkylcarbonyl, phenylcarbonyl; C1-C4 alkoxycarbonylamino-C1-C4 alkylcarbonyl and C1-C4 dialkylamino-C1-C4 alkylcarbonyl, alternatively, R11 and R12, when attached to the same nitrogen, combine to form a 4- to 8-membered heterocyclic ring containing atoms carbon, substituted with 0 to 3 groups independently selected from the group consisting of halo, CF3, CHF2, OCF3, OCHF2, OCH2F, 5- or 6-membered heteroaryl, OH, oxo, C1-C4 hydroxyalkyl, C1-C4 alkyl, and C1-C4 alkoxy, and 0 to 2 additional heteroatoms selected from N, NR13, O and S (O) p; R13 is selected, at each occurrence, independently from the group consisting of H, C1-C6 alkyl and - (CH2) phenyl; R14 is selected, at each occurrence, independently from the group consisting of H, C1-C6 alkyl, C1-C4 haloalkyl-, C1-C4 alkoxycarbonylamino- and - (CH2) n1-phenyl substituted with 0 to 3 groups independently selected from the group that consists of halo, C1-C4 alkoxy, C1-C4 alkyl, cyclopropyl, CF3, OCF3, 5- or 6-membered heteroaryl, OH, OCHF2, C1-C4 dialkylamino, and cyano; R7 is selected from the group consisting of H, halo, hydroxyl, oxo, C1-C3 alkyl, C1-C3 hydroxyalkyl, and C1-C2 haloalkyl, containing 1 to 5 halogens; n1, in each case, is selected from 0, 1, 2, or 3 and p, in each case, is independently 0, 1, and 2. |
| priorityDate | 2012-04-26-04:00^^<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: 1180.