http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-104963-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cef4f341fe4f2caf061611a818576e40 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-437 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P5-00 |
| filingDate | 2016-06-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7f00186df1d24eef942b38ca01ee07f6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_72f1bb0649fd2e8a478dbf261723af26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dde3d1dbbff6a025f2162d0af558e57c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c6536a3cbf613323afc5eddeae5d3a3d |
| publicationDate | 2017-08-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-104963-A1 |
| titleOfInvention | DERIVATIVES OF 2- (PIRAZOLOPIRIDIN-3-IL) PYRIMIDINE AS JAK INHIBITORS |
| abstract | Derivatives of 2- (pyrazolopyridin-3-yl) pyrimidine are described, as well as a process for their preparation, pharmaceutical compositions comprising them and their use in therapy as Janus kinase inhibitors (JAK). Claim 1: Derivative of 2- (pyrazolopyridin-3-yl) pyrimidine, for use in the treatment of the human or animal body, derivative of 2- (pyrazolopyridin-3-yl) pyrimidine which is a compound of formula (1), or a salt, or solvate, or N-oxide, or stereoisomer or pharmaceutically acceptable deuterated derivative thereof, wherein X represents a group -O- or -NR³-; R¹ and R² are independently selected from the group consisting of a hydrogen atom, a halogen atom, a linear or branched C₁₋₄ alkyl group, a linear or branched C₁₋₄ alkoxy group and a -CN group; R³ is selected from the group consisting of a hydrogen atom, a linear or branched C₁₋₄ alkyl group, a group - (CH₂) ₁₋₃NRR and a group - (CH₂) ₁₋₃-pyrrolidine; G¹ is selected from the group consisting of a group -CN, a group -CO-Rᵃ, a group -O-R⁶, a group - (CHR⁷) ₘ-NRR, a phenyl group, a monocyclic C₅₋₇ cycloalkyl group, a 5 to 6 monocyclic heteroaryl group containing at least one heteroatom selected from O, S and N and a 5 to 6 monocyclic heterocyclyl group containing at least one heteroatom selected from O, S and N, in which the phenyl groups , cycloalkyl, heteroaryl and heterocyclyl are not substituted or substituted with one or more substituents selected from a halogen atom, a hydroxyl group, a linear or branched C₁₋₄ alkyl group, a linear or branched C₁₋₆ hydroxyalkyl group, a group linear or branched C₁₋₄ alkoxy, a group - (CH₂) ₀₋₂NRR, a group - (CH₂) ₀₋₂CN and a group -CO-Rᵃ, in which Rᵃ represents a hydrogen atom, a hydroxyl group, a linear or branched C₁₋₃ alkyl group, a C₁₋₃ alkoxy group linear or branched, or an amino group; Q is selected from the group consisting of the compounds of the group of formulas (2) in which R⁴ is selected from the group consisting of a linear or branched C₁₋₄ alkyl group, a -CO-R group, a -CO ( CH₂) ₁₋₂-OH; a -CO (CH₂) ₁₋₂-CN group, a -CO (CH₂) ₁₋₂-CF₃ group, a cyanothiazole group, a monocyclic 4- to 6-membered heterocyclyl group containing at least one heteroatom selected from O, S and N and a monocyclic 5-6 membered heteroaryl group containing at least one heteroatom selected from O, S and N, in which the heterocyclyl and heteroaryl group are not substituted or substituted with one or more substituents selected from a group - (CH₂) ₘ-CN and a C₁₋₂ hydroxyalkyl group; R⁵ represents a group - (CH₂) ₘ-CN or a group - (CH₂) ₘ-OH; G² represents a phenyl group, a pyrimidino group or a pyridino group in which the phenyl, pyrimidino and pyridino groups are unsubstituted with one or more substituents selected from a halogen atom, a linear or branched C₁₋₄ alkyl group, a group hydroxyl, a group -CN; R⁶ is selected from the group consisting of a hydrogen atom, a group - (CH -) ₁₋₂-CO-OR, a linear or branched (C₁₋₆ alkoxy) - (C alquilo alkyl) group and a C₁ alkyl group ₋₆ linear or branched wherein said linear or branched C₁₋₆ alkyl group is not substituted or is substituted with one or more substituents selected from a halogen atom, a hydroxyl group and a -NRR group; R⁷ represents a hydrogen atom, a hydroxyl group or C₁₋₂ alkyl; R and R independently represent a hydrogen atom, a linear or branched C₁₋₃ alkyl group, a linear or branched C₁₋₃ hydroxyalkyl group, a linear or branched C₁₋₃ alkoxy group; R represents a C₁₋₂ alkyl group or a benzyl group; and m independently has a value from 0 to 3; wherein the derivative of 2- (pyrazolopyridin-3-yl) pyrimidine is not: 3 - {(3R) -3 - [[2- (dimethylamino) ethyl] (5-fluoro-6-morpholin-4-yl- 2-pyrazolo [1,5-a] pyridin-3-ylpyrimidin-4-yl) amino] piperidin-1-yl} -3-oxopropanonitrile, 3 - {(3R) -3 - [(5-fluoro-6- morpholin-4-yl-2-pyrazolo [1,5-a] pyridin-3-ylpyrimidin-4-yl) amino] piperidin-1-yl} -3-oxopropanonitrile, (3 - {(3R) -3- [ (5-fluoro-6-morpholin-4-yl-2-pyrazolo [1,5-a] pyridin-3-ylpyrimidin-4-yl) amino] piperidin-1-yl} oxetan-3-yl) acetonitrile, ( 3R) -3 - [(5-fluoro-6-morpholin-4-yl-2-pyrazolo [1,5-a] pyridin-3-ylpyrimidin-4-yl) amino] piperidine-1-carboxylate ethyl, 2 - {(3R) -3 - [(5-fluoro-6-morpholin-4-yl-2-pyrazolo [1,5-a] pyridin-3-ylpyrimidin-4-yl) amino] piperidin-1-yl} -2-oxoethanol, 3 - [(3R) -3 - ({5-fluoro-6- [4- (hydroxymethyl) piperidin-1-yl] -2-pyrazolo [1,5-a] pyridin-3-ylpyrimidin -4-yl} amino) piperidin-1-yl] -3-oxopropanonitrile, 3 - [(3R) -3 - ({5-fluoro-6- [4- (hydroxymethyl) phenyl] -2-pyrazolo [1, 5-a] pyridin-3-ylpyrimidin-4-yl} amino) piperidin-1-yl] -3-oxopropanonitrile, 3 - ((3R) -3 - {[5-fluoro-6- (4-formylphenyl) -2-pyrazolo [1,5-a] pyridin-3-ylpyrimidin-4-yl] amino} piperidin-1-yl) -3-oxopropanonitrile, 3 - {(3R) -3 - [( 5-fluoro-6- {3-hydroxy-4 - [(methylamino) methyl] phenyl} -2-pyrazolo [1,5-a] pyridin-3-ylpyrimidin-4-yl) amino] piperidin-1-yl} -3-oxopropanonitrile. |
| priorityDate | 2015-06-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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