http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2587514-T3
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Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dcce39a20bef16c3f04497659caba40f |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-14 |
filingDate | 2012-02-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2016-10-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8352ecbd99fa453761cb93c2e0eb4dc4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b8fff1b68aba0b91bced1777bc1b1b20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d53d92135e9f3e2d41d8cbe3c127606c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3f63a674fb9cff31fdc283afa2e16e3f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dbe156d08120d27a19fbc741a9f5e8d4 |
publicationDate | 2016-10-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | ES-2587514-T3 |
titleOfInvention | Tricyclic Kinase Inhibitors |
abstract | A compound of the formula (I): ** Formula ** wherein X is N or CR1; Y is N or CR2; Z is O, S, or NH; R1 is H or C1-6-alkyl; R2 is H or C1-6-alkyl; R3 is C1-8-alkyl, C2-8-alkenyl, C3-8-cycloalkyl, aryl, or heteroaryl, wherein (a) C1-8-alkyl or C2-8-alkenyl is optionally substituted with one or more substituents selected from the group consisting of halogen, cyano, nitro, -ORa, -C (O) Ra, -C (O) ORa, -OC (O) R a, -NRbRc, -NRbC (O) Ra, -NHC (O ) NHRb, -C (O) NRbRc, -NHSO2Ra, and -SO2NRbNRc; and (b) C3-8-cycloalkyl, aryl, and heteroaryl are optionally substituted with one or more substituents selected from the group consisting of C1-6-alkyl, C1-6-haloalkyl, C2-6-alkenyl, heterocycloalkyl, aryl, heteroaryl, halogen, oxo, cyano, nitro, -ORd, -C (O) Rd, -C (O) ORd, -OC (O) Rd, -SRd, - S (O) Rd, -SO2Rd, -NReRf, -NHC (O) Re, -NHC (O) NHRe, -NHC (O) ORe, -NHSO2Rd, -C (O) NHRe, and -SO2NHNRe; R4 is (a) phenyl, naphthyl, tetrahydronaphthyl, indenyl, or indanyl, wherein phenyl, naphthyl, tetrahydronaphthyl, indenyl, or indanyl are optionally substituted with one or more R5; or (b) 5-16 membered monocyclic, bicyclic, or tricyclic heterocyclyl, wherein the heterocyclyl is optionally substituted with one or more R6; R5, at each occurrence, is independently CN, NO2, halo, C1-6-alkyl, ORg, SRg, C (O) Rg, C (O) NRhRi, C (O) ORg, NRhRi, NRhC (O) Rg, S (O) 2Rg, NRhS (O) 2Rg, S (O) 2NRhRi, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, or heterocycloalkenyl, wherein C1-6-alkyl is optionally substituted with one or more substituents selected from the group consisting of CN, halo, hydroxy, S (O) 2NH (C1-6-alkyl), C1-6-alkoxy, heterocycloalkyl, cycloalkyl, heteroaryl, aryl, -NH2, -NHCl-6-alkyl, and -N (C1-6 -alkyl) 2; wherein aryl, cycloalkyl, heteroaryl, or heterocycloalkyl, alone or as part of another moiety, is optionally substituted with one or more R7; R6, at each occurrence, is independently CN, NO2, halo, C3-8 cycloalkyl, ORj, SRj, C (O) Rj, C (O) NRkR1, C (O) ORj, NRkRl, NRkC (O) Rj, S (O) 2Rj, NRkS (O) 2Rj, or S (O) 2NRkRl, wherein the C1-6-alkyl is optionally substituted with one or more substituents selected from the group consisting of CN, halo, hydroxy, C1-6-alkoxy , heterocycloalkyl, cycloalkyl, heteroaryl, aryl, -NH2, -NHCl-6-alkyl, and -N (C1-6-alkyl) 2; wherein the heterocycloalkyl, cycloalkyl, heteroaryl, aryl, alone or as part of another moiety, are optionally substituted with one, two or three substituents independently selected from CN, halo, heteroaryl, benzyl, and C1-6-alkyl; R7, at each occurrence, is independently CN, NO2, halo, oxo, C1-6-alkyl, aryl, C3-8 cycloalkyl, heteroaryl, heterocycloalkyl, ORm, SRm, C (O) Rm, C (O) NRnRo, C (O) ORm, OC (O) Rm, OC (O) NRnRo, NRnRo, NRnC (O) Rm, S (O) Rm, S (O) NRnRo, S (O) 2Rm, NRnS (O) 2Rm, or S (O) 2NRnRo, wherein the C1-6-alkyl is optionally substituted with one or more substituents selected from the group consisting of CN, halo, hydroxy, C1-6-alkoxy, heterocycloalkyl, cycloalkyl, aryl, heteroaryl, -NH2, -NHCl-6-alkyl, and -N (C1-6-alkyl) 2, wherein the aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl, alone or as part of another moiety, are optionally substituted with one, two or three substituents independently selected from CN, halo, and C1-6-alkyl; Ra, at each occurrence, is independently selected from the group consisting of H, C1-6-alkyl, C1-6-haloalkyl, aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl; Rb and Rc, at each occurrence, are independently selected from the group consisting of H, C1-6-alkyl, C1-6-haloalkyl, aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl; Rd, at each occurrence, is independently selected from the group consisting of H, C1-6-alkyl, C1-6-haloalkyl, aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl; Re and Rf, at each occurrence, are independently selected from the group consisting of H, C1-6-alkyl, C1-6-haloalkyl, aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl; Rg, at each occurrence, is independently selected from the group consisting of H, C1-6-alkyl, aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl; wherein C1-6-alkyl is optionally substituted with one or more substituents selected from the group consisting of CN, halo, hydroxy, C1-6-alkoxy, heterocycloalkyl, -NH2, -NHCl-6-alkyl, and -N (C1 -6-alkyl) 2, and wherein the aryl, C3-8 cycloalkyl, heteroaryl, or heterocycloalkyl, alone or as part of another moiety, is optionally substituted with one or more substituents selected from the group consisting of halo, C1-6- alkyl, C1-6-haloalkyl, C1-6-hydroxyalkyl, hydroxy, oxo, C1-6-alkoxy, C1-6-haloalkoxy, -C (O) C1-6-alkyl, -S (O) 2C1-6- alkyl, -NH2, -NH (C1-6-alkyl), -N (C1-6-alkyl) 2, and -N (C1-6-alkyl) (C3-8-cycloalkyl); Rh and Ri, at each occurrence, are independently selected from the group consisting of H, C1-6-alkyl, aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl; wherein C1-6-alkyl is optionally substituted with one or more substituents selected from the group consisting of CN, halo, hydroxy, C1-6-alkoxy, heterocycloalkyl, -NH2, -NHCl-6-alkyl, and -N (C1 -6-alkyl) 2, and wherein the aryl, C3-8 cycloalkyl, heteroaryl, or heterocycloalkyl, alone or as part of another moiety, is optionally substituted with one or more substituents selected from the group consisting of halo, C1-6- alkyl, C1-6-haloalkyl, C1-6-hydroxyalkyl, hydroxy, oxo, C1-6-alkoxy, C1-6-haloalkoxy, -C (O) C1-6-alkyl, -S (O) 2C1-6- alkyl, -NH2, -NH (C1-6-alkyl), N (C1-6-alkyl) 2, and -N (C1-6-alkyl) (C3-8-cycloalkyl); Rj, at each occurrence, is independently selected from the group consisting of H, C1-6-alkyl, aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl; wherein C1-6-alkyl is optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, C1-6-alkoxy, -NH2, -NHCl-6-alkyl, and - N (C1-6-alkyl ) 2, and wherein the aryl, C3-8 cycloalkyl, heteroaryl, or heterocycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halo, C1-6-alkyl, C1-6-haloalkyl, C1-6-hydroxyalkyl , hydroxy, oxo, C1-6-alkoxy, C1-6-haloalkoxy, -NH2, -NH (C1-6-alkyl), and N (C1-6-alkyl) 2; Rk and Rl, at each occurrence, are independently selected from the group consisting of H, C1-6-alkyl, aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl; wherein C1-6-alkyl is optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, C1-6-alkoxy, -NH2, -NHCl-6- alkyl, and -N (C1-6-alkyl ) 2, and wherein the aryl, C3-8 cycloalkyl, heteroaryl, or heterocycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halo, C1-6-alkyl, C1-6-haloalkyl, C1-6-hydroxyalkyl , hydroxy, oxo, C1-6-alkoxy, C1-6-haloalkoxy, -NH2, -NH (C1-6-alkyl), and N (C1-6-alkyl) 2; Rm, at each occurrence, is independently selected from the group consisting of H, C1-6-alkyl, aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl; wherein C1-6-alkyl is optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, C1-6-alkoxy, -NH2, -NHCl-6-alkyl, and - N (C1-6-alkyl ) 2, and wherein the aryl, C3-8 cycloalkyl, heteroaryl, or heterocycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halo, C1-6-alkyl, C1-6-haloalkyl, C1-6-hydroxyalkyl , hydroxy, oxo, C1-6-alkoxy, C1-6-haloalkoxy, -NH2, -NH (C1-6-alkyl), and N (C1-6-alkyl) 2; Rn and Ro, at each occurrence, are independently selected from the group consisting of H, C1-6-alkyl, aryl, C3-8 cycloalkyl, heteroaryl, and heterocycloalkyl; wherein C1-6-alkyl is optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, C1-6-alkoxy, -NH2, -NHCl-6- alkyl, and -N (C1-6-alkyl ) 2, and wherein the aryl, C3-8 cycloalkyl, heteroaryl, or heterocycloalkyl is optionally substituted with one or more substituents selected from the group consisting of halo, C1-6-alkyl, C1-6-haloalkyl, C1-6-hydroxyalkyl , hydroxy, oxo, C1-6-alkoxy, C1-6-haloalkoxy, -NH2, -NH (C1-6-alkyl), and N (C1-6-alkyl) 2; or an acceptable pharmaceutical salt or solvate thereof; with the proviso that said compound is not 6- (2,6-dimethylphenyl) -2 - ((4- (4-methyl-1- piperazinyl) phenyl) amino) imidazo [1,2-a] imido [5, 4-e] pyrimidin-5 (6H) -one. |
priorityDate | 2011-02-28-04:00^^<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: 1086.