ME00230B - 2-(piridin -2-ilamino)-pirido(2,3-d) pirimidin-7-oni - Google Patents
2-(piridin -2-ilamino)-pirido(2,3-d) pirimidin-7-oniInfo
- Publication number
- ME00230B ME00230B MEP-2008-461A MEP46108A ME00230B ME 00230 B ME00230 B ME 00230B ME P46108 A MEP46108 A ME P46108A ME 00230 B ME00230 B ME 00230B
- Authority
- ME
- Montenegro
- Prior art keywords
- pyrimidin
- pyrido
- pyridin
- cyclopentyl
- ylamino
- Prior art date
Links
- 201000010099 disease Diseases 0.000 claims abstract 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 13
- 150000001875 compounds Chemical class 0.000 claims abstract 12
- -1 trifluoromethylalkyl Chemical group 0.000 claims 13
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- 241000124008 Mammalia Species 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000002837 carbocyclic group Chemical group 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 125000004430 oxygen atom Chemical group O* 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 229920002554 vinyl polymer Polymers 0.000 claims 6
- 229910020008 S(O) Inorganic materials 0.000 claims 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 5
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 5
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 5
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 5
- 125000004103 aminoalkyl group Chemical group 0.000 claims 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000004663 dialkyl amino group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 150000002825 nitriles Chemical class 0.000 claims 5
- 239000001301 oxygen Substances 0.000 claims 5
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 5
- 239000011593 sulfur Substances 0.000 claims 5
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 3
- QZDZRDATWGQUSE-UHFFFAOYSA-N 6-bromo-8-cyclopentyl-5-methyl-2-(pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3N=CC=CC=3)=NC=C2C(C)=C(Br)C(=O)N1C1CCCC1 QZDZRDATWGQUSE-UHFFFAOYSA-N 0.000 claims 3
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 3
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- RNDSKWSXUGROBX-UHFFFAOYSA-N 6-acetyl-2-[[5-[bis(2-methoxyethyl)amino]pyridin-2-yl]amino]-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(N(CCOC)CCOC)=CC=C1NC1=NC=C(C(C)=C(C(C)=O)C(=O)N2C3CCCC3)C2=N1 RNDSKWSXUGROBX-UHFFFAOYSA-N 0.000 claims 2
- JPJBKLUESOYNLD-UHFFFAOYSA-N 6-bromo-8-cyclopentyl-2-(pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(Br)=CC2=CN=C1NC1=CC=CC=N1 JPJBKLUESOYNLD-UHFFFAOYSA-N 0.000 claims 2
- JQDVILMFUIXCRM-UHFFFAOYSA-N 6-bromo-8-cyclopentyl-2-[[5-(2-methoxyethoxy)pyridin-2-yl]amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(OCCOC)=CC=C1NC1=NC=C(C=C(Br)C(=O)N2C3CCCC3)C2=N1 JQDVILMFUIXCRM-UHFFFAOYSA-N 0.000 claims 2
- POJKMTSCTDNKEZ-UHFFFAOYSA-N 6-bromo-8-cyclopentyl-2-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(C)=NC=C2C=C(Br)C(=O)N1C1CCCC1 POJKMTSCTDNKEZ-UHFFFAOYSA-N 0.000 claims 2
- 101100134922 Gallus gallus COR5 gene Proteins 0.000 claims 2
- 108091008648 NR7C Proteins 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- RRUDCFGSUDOHDG-UHFFFAOYSA-N acetohydroxamic acid Chemical compound CC(O)=NO RRUDCFGSUDOHDG-UHFFFAOYSA-N 0.000 claims 2
- 229960001171 acetohydroxamic acid Drugs 0.000 claims 2
- 208000009956 adenocarcinoma Diseases 0.000 claims 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 210000001072 colon Anatomy 0.000 claims 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 210000003800 pharynx Anatomy 0.000 claims 2
- 230000035755 proliferation Effects 0.000 claims 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- KECYKUOBQYTMFK-UHFFFAOYSA-N 2-[(6-acetyl-5-piperazin-1-ylpyridin-2-yl)amino]-8-cyclopentyl-6-ethylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(CC)=CC2=CN=C1NC(N=C1C(C)=O)=CC=C1N1CCNCC1 KECYKUOBQYTMFK-UHFFFAOYSA-N 0.000 claims 1
- GNOBPPBWGCDWJR-UHFFFAOYSA-N 2-[[5-(2-aminoethylamino)pyridin-2-yl]amino]-6-bromo-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3N=CC(NCCN)=CC=3)=NC=C2C(C)=C(Br)C(=O)N1C1CCCC1 GNOBPPBWGCDWJR-UHFFFAOYSA-N 0.000 claims 1
- VZEIYMGFCZFVGP-UHFFFAOYSA-N 2-[[5-(2-aminoethylamino)pyridin-2-yl]amino]-6-bromo-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(NCCN)=CC=C1NC1=NC=C(C=C(Br)C(=O)N2C3CCCC3)C2=N1 VZEIYMGFCZFVGP-UHFFFAOYSA-N 0.000 claims 1
- DGXNULHJVNJWJP-UHFFFAOYSA-N 2-[[5-(3-aminopyrrolidin-1-yl)pyridin-2-yl]amino]-6-bromo-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound C1C(N)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(Br)C(=O)N2C3CCCC3)C2=N1 DGXNULHJVNJWJP-UHFFFAOYSA-N 0.000 claims 1
- WTZZGELFDNPANA-UHFFFAOYSA-N 2-[[5-(3-aminopyrrolidin-1-yl)pyridin-2-yl]amino]-8-cyclopentyl-6-(hydroxymethyl)pyrido[2,3-d]pyrimidin-7-one Chemical compound C1C(N)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(CO)C(=O)N2C3CCCC3)C2=N1 WTZZGELFDNPANA-UHFFFAOYSA-N 0.000 claims 1
- RFJNBZVTUKMOKC-UHFFFAOYSA-N 2-[[5-(3-aminopyrrolidin-1-yl)pyridin-2-yl]amino]-8-cyclopentyl-6-ethylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(CC)=CC2=CN=C1NC(N=C1)=CC=C1N1CCC(N)C1 RFJNBZVTUKMOKC-UHFFFAOYSA-N 0.000 claims 1
- CIEGNEASRBFQLF-UHFFFAOYSA-N 2-[[5-(3-aminopyrrolidin-1-yl)sulfonylpyridin-2-yl]amino]-6-bromo-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3N=CC(=CC=3)S(=O)(=O)N3CC(N)CC3)=NC=C2C(C)=C(Br)C(=O)N1C1CCCC1 CIEGNEASRBFQLF-UHFFFAOYSA-N 0.000 claims 1
- QYBHBZQEIJFIID-UHFFFAOYSA-N 2-[[5-(3-aminopyrrolidin-1-yl)sulfonylpyridin-2-yl]amino]-6-bromo-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound C1C(N)CCN1S(=O)(=O)C(C=N1)=CC=C1NC1=NC=C(C=C(Br)C(=O)N2C3CCCC3)C2=N1 QYBHBZQEIJFIID-UHFFFAOYSA-N 0.000 claims 1
- YXHQPGZZOMKDKV-UHFFFAOYSA-N 2-[[5-(3-aminopyrrolidin-1-yl)sulfonylpyridin-2-yl]amino]-8-cyclopentyl-6-ethylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(CC)=CC2=CN=C1NC(N=C1)=CC=C1S(=O)(=O)N1CCC(N)C1 YXHQPGZZOMKDKV-UHFFFAOYSA-N 0.000 claims 1
- KRWHAQTXQAMXTB-UHFFFAOYSA-N 2-[[5-(azepan-1-yl)pyridin-2-yl]amino]-6-bromo-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(Br)=CC2=CN=C1NC(N=C1)=CC=C1N1CCCCCC1 KRWHAQTXQAMXTB-UHFFFAOYSA-N 0.000 claims 1
- XIWCDJIWKPEYPF-UHFFFAOYSA-N 2-[[5-(azepan-1-yl)pyridin-2-yl]amino]-8-cyclopentyl-6-(hydroxymethyl)pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(CO)=CC2=CN=C1NC(N=C1)=CC=C1N1CCCCCC1 XIWCDJIWKPEYPF-UHFFFAOYSA-N 0.000 claims 1
- ONLZGBFWCPBYLE-UHFFFAOYSA-N 2-[[5-(azetidin-1-yl)pyridin-2-yl]amino]-6-bromo-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(Br)=CC2=CN=C1NC(N=C1)=CC=C1N1CCC1 ONLZGBFWCPBYLE-UHFFFAOYSA-N 0.000 claims 1
- PKSPQJGYKMMCFO-UHFFFAOYSA-N 2-[[5-[3-(2-aminopropan-2-yl)pyrrolidin-1-yl]pyridin-2-yl]amino]-6-bromo-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound C1C(C(C)(N)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(Br)C(=O)N2C3CCCC3)C2=N1 PKSPQJGYKMMCFO-UHFFFAOYSA-N 0.000 claims 1
- GLIAQJVFZZCNRM-UHFFFAOYSA-N 2-[[5-[3-(benzenesulfonyl)propoxy]pyridin-2-yl]amino]-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C=CC2=CN=C1NC(N=C1)=CC=C1OCCCS(=O)(=O)C1=CC=CC=C1 GLIAQJVFZZCNRM-UHFFFAOYSA-N 0.000 claims 1
- GDHUHDALUPEYNQ-UHFFFAOYSA-N 2-[[5-[bis(2-hydroxyethyl)amino]pyridin-2-yl]amino]-6-bromo-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(N(CCO)CCO)=CC=C1NC1=NC=C(C=C(Br)C(=O)N2C3CCCC3)C2=N1 GDHUHDALUPEYNQ-UHFFFAOYSA-N 0.000 claims 1
- RNSUPAGDKUJPOH-UHFFFAOYSA-N 2-[[5-[bis(2-methoxyethyl)amino]pyridin-2-yl]amino]-6-bromo-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(N(CCOC)CCOC)=CC=C1NC1=NC=C(C(C)=C(Br)C(=O)N2C3CCCC3)C2=N1 RNSUPAGDKUJPOH-UHFFFAOYSA-N 0.000 claims 1
- FUPSONGCEPFMNO-UHFFFAOYSA-N 2-[[5-[bis(2-methoxyethyl)amino]pyridin-2-yl]amino]-6-bromo-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(N(CCOC)CCOC)=CC=C1NC1=NC=C(C=C(Br)C(=O)N2C3CCCC3)C2=N1 FUPSONGCEPFMNO-UHFFFAOYSA-N 0.000 claims 1
- YDDZYJNEXVSNOR-UHFFFAOYSA-N 6-acetyl-2-[[5-(2-aminoethylamino)pyridin-2-yl]amino]-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC1=CC=C(NCCN)C=N1 YDDZYJNEXVSNOR-UHFFFAOYSA-N 0.000 claims 1
- QTZVWABNQLQVPQ-UHFFFAOYSA-N 6-acetyl-2-[[5-(3-aminopyrrolidin-1-yl)sulfonylpyridin-2-yl]amino]-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1S(=O)(=O)N1CCC(N)C1 QTZVWABNQLQVPQ-UHFFFAOYSA-N 0.000 claims 1
- IQKCFVDADWUFCR-UHFFFAOYSA-N 6-acetyl-2-[[5-[3-(2-aminopropan-2-yl)pyrrolidin-1-yl]pyridin-2-yl]amino]-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCC(C(C)(C)N)C1 IQKCFVDADWUFCR-UHFFFAOYSA-N 0.000 claims 1
- WNFVIHQULLTZRP-UHFFFAOYSA-N 6-acetyl-2-[[5-[bis(2-methoxyethyl)amino]pyridin-2-yl]amino]-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(N(CCOC)CCOC)=CC=C1NC1=NC=C(C=C(C(C)=O)C(=O)N2C3CCCC3)C2=N1 WNFVIHQULLTZRP-UHFFFAOYSA-N 0.000 claims 1
- PNYDSWBFIYYAOD-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-2-[(5-morpholin-4-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCOCC1 PNYDSWBFIYYAOD-UHFFFAOYSA-N 0.000 claims 1
- NVURUIMJTOVZJR-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-2-[[5-(2,6-dimethylmorpholin-4-yl)pyridin-2-yl]amino]-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C1C(C)OC(C)CN1C(C=N1)=CC=C1NC1=NC=C(C(C)=C(C(C)=O)C(=O)N2C3CCCC3)C2=N1 NVURUIMJTOVZJR-UHFFFAOYSA-N 0.000 claims 1
- JDAYPETZCPTRRN-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-2-[[5-(2-methoxyethoxy)pyridin-2-yl]amino]-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(OCCOC)=CC=C1NC1=NC=C(C(C)=C(C(C)=O)C(=O)N2C3CCCC3)C2=N1 JDAYPETZCPTRRN-UHFFFAOYSA-N 0.000 claims 1
- RSOGDQWTVSCHQY-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-2-[[5-(2-methoxyethoxy)pyridin-2-yl]amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(OCCOC)=CC=C1NC1=NC=C(C=C(C(C)=O)C(=O)N2C3CCCC3)C2=N1 RSOGDQWTVSCHQY-UHFFFAOYSA-N 0.000 claims 1
- YAWYHLNWDSFVDA-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-2-[[5-(2-methoxyethoxymethyl)pyridin-2-yl]amino]-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(COCCOC)=CC=C1NC1=NC=C(C(C)=C(C(C)=O)C(=O)N2C3CCCC3)C2=N1 YAWYHLNWDSFVDA-UHFFFAOYSA-N 0.000 claims 1
- SUMIDHRKHFHCBN-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-2-[[5-(2-methoxyethoxymethyl)pyridin-2-yl]amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(COCCOC)=CC=C1NC1=NC=C(C=C(C(C)=O)C(=O)N2C3CCCC3)C2=N1 SUMIDHRKHFHCBN-UHFFFAOYSA-N 0.000 claims 1
- OTNPSIGYUQFCTR-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-2-[[5-(diethylamino)pyridin-2-yl]amino]-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(N(CC)CC)=CC=C1NC1=NC=C(C(C)=C(C(C)=O)C(=O)N2C3CCCC3)C2=N1 OTNPSIGYUQFCTR-UHFFFAOYSA-N 0.000 claims 1
- GYICIMVQXWJGLP-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-2-[[5-(dimethylamino)pyridin-2-yl]amino]-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(N(C)C)=CC=C1NC1=NC=C(C(C)=C(C(C)=O)C(=O)N2C3CCCC3)C2=N1 GYICIMVQXWJGLP-UHFFFAOYSA-N 0.000 claims 1
- VEQOPAOFGZKFHM-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-2-[[5-[2-(diethylamino)ethoxy]pyridin-2-yl]amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CC(OCCN(CC)CC)=CC=C1NC1=NC=C(C=C(C(C)=O)C(=O)N2C3CCCC3)C2=N1 VEQOPAOFGZKFHM-UHFFFAOYSA-N 0.000 claims 1
- GGNIULHSXFVFEY-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-morpholin-4-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCOCC1 GGNIULHSXFVFEY-UHFFFAOYSA-N 0.000 claims 1
- MJMAOJBJOJYBLM-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-morpholin-4-ylsulfonylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1S(=O)(=O)N1CCOCC1 MJMAOJBJOJYBLM-UHFFFAOYSA-N 0.000 claims 1
- MZBKJNDTXYIZDF-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-pyrrolidin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCCC1 MZBKJNDTXYIZDF-UHFFFAOYSA-N 0.000 claims 1
- CTQWHSWXTOSBOZ-UHFFFAOYSA-N 6-amino-2-[[5-(azepan-1-yl)pyridin-2-yl]amino]-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(N)=CC2=CN=C1NC(N=C1)=CC=C1N1CCCCCC1 CTQWHSWXTOSBOZ-UHFFFAOYSA-N 0.000 claims 1
- WXQRJGNEEAQTOZ-UHFFFAOYSA-N 6-amino-2-[[5-(azetidin-1-yl)pyridin-2-yl]amino]-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(N)=CC2=CN=C1NC(N=C1)=CC=C1N1CCC1 WXQRJGNEEAQTOZ-UHFFFAOYSA-N 0.000 claims 1
- UOMYGSOEHPHNDW-UHFFFAOYSA-N 6-amino-2-[[5-[3-(2-aminopropan-2-yl)pyrrolidin-1-yl]pyridin-2-yl]amino]-8-cyclopentylpyrido[2,3-d]pyrimidin-7-one Chemical compound C1C(C(C)(N)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(N)C(=O)N2C3CCCC3)C2=N1 UOMYGSOEHPHNDW-UHFFFAOYSA-N 0.000 claims 1
- CCWNTMZZYJTKES-UHFFFAOYSA-N 6-amino-8-cyclopentyl-2-[[5-[(4-fluorophenyl)methylamino]pyridin-2-yl]amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(N)=CC2=CN=C1NC(N=C1)=CC=C1NCC1=CC=C(F)C=C1 CCWNTMZZYJTKES-UHFFFAOYSA-N 0.000 claims 1
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- 210000002784 stomach Anatomy 0.000 claims 1
- 210000001550 testis Anatomy 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 210000002105 tongue Anatomy 0.000 claims 1
- 208000010576 undifferentiated carcinoma Diseases 0.000 claims 1
- 241001529453 unidentified herpesvirus Species 0.000 claims 1
- 208000010570 urinary bladder carcinoma Diseases 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 150000003930 2-aminopyridines Chemical class 0.000 abstract 2
- 101100005789 Caenorhabditis elegans cdk-4 gene Proteins 0.000 abstract 2
- 102000013701 Cyclin-Dependent Kinase 4 Human genes 0.000 abstract 2
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 230000003389 potentiating effect Effects 0.000 abstract 2
- 230000002062 proliferating effect Effects 0.000 abstract 2
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Abstract
Ovaj pronalazak daje supstituisane 2-aminopiridine koji su korisni u liječenju proliferativnih oboljenja ćelija. Nova jedinjenja iz ovog pronalaska su potentni inhibitori ciklin-zavisnih kinaza 4 ( cdk4 ). (II). Ovaj pronalazak daje supstituisane 2-aminopiridine koji su korisni u liječenju proliferativnih oboljenja ćelija. Nova jedinjenja iz ovog pronalaska su potentni inhibitori ciklin-zavisnih kinaza 4 ( cdk4 ). (II).
Claims (15)
1. Jedinjenje formule I: I pri čemu: isprekidana linija predstavlja opcionu vezu, X1, X2 i X3 su u svakom slučaju nezavisno izabrani od vodonika, halogena, C1-C6 alkil, C1-C6 haloalkil, C1-C8 alkoksi, C1-C8 alkoksialkil, CN, NO2, OR5, NR5R6, CO2R5, COR5, S(O)nR5, conr5r6, nr5cor6, nr5so2r6, SO2NR5R6 i P(O)(OR5)(OR6) grupe; pod uslovom da najmanje jedan od X1, X2 i X3 mora da bude vodonik; n = 0-2 R1 je, u svakom slučaju, nezavisno, vodonik, halogen, C1-C6 alkil, C1-C6 haloalkil,C1-C6 hidroksialkil ili C3-C7 cikloalkil; R2 i R4 su nezavisno izabrani od vodonika, halogena, C1-C8 alkil, C3-C7 cikloalkil, C1-C8 alkoksi, C1-C8 alkoksialkil, C1-C8 haloalkil, C1-C8 hidroksialkil, C2-C8 alkenil, C2-C8 alkinil, nitril, nitro, OR5, SR5, NR5R6, N(O)NR5R6, P(O)(0R5)(OR6), (CR5R6)mNR7R8, COR5, (CR4R5)mC(0)R7, C02R5, CONR5R6, C(O)NR5SO2R6, NR5SO2R6, C(O)NR5OR6, S(O)nR5, SO2NR5R6, P(O)(OR5)(OR6), (CR5R6)mP(O)(OR7)(OR8), (CR5R6)m-aril, (CR5R6)m-heteroaril, -T(CH2)mQR5, -C(O)T(CH2)mR5, NR5C(O)T(CH2)mR5 i -CR5=CR6C(O)R7 grupe; ili R1 i R2 mogu da formiraju karbocikiičnu grupu koja sadrži prsten sa 3-7 članova, preferirano prsten sa 5-6 članova, od kojih do četiri člana može opciono da bude zamenjeno sa heteroatomom nezavisno izabranim od kiseonika, sumpora i azota, i pri čemu je karbociklična grupa nesupstituisana ili supstituisana sa jednom, dve ili tri grupe nezavisno izabrane od halogena, hidroksi, hidroksialkil, nitril, niže C1-C8 alkil, niže C1-C8 alkoksi, alkoksikarbonil, alkilkarbonil, alkilkarbonilamino, aminoalkil, trifluorometil, N-hidroksiacetamid, trifluorometilalkil, amino i mono ili dialkilamino, (CH2)mC(O)NR5R6 i O(CH2)mC(O)OR5 grupe, pod uslovom, međutim, da je u karbocikličnom prstenu najmanje jedan atom ugljenika i da, u koliko se nalaze dva ili više atoma kiseonika u prstenu, atomi kiseonika u prstenu se ne nalaze jedan pored drugog; T je O, S, NR7, N(O)R7, NR7R8W ili CR7R8 grupa; Q je O, S, NR7, N(O)R7, NR7R8W, CO2, O(CH2)m-heteroaril, O(CH2)mS(O)nR8, (CH2)-heteroaril ili karbociklična grupa koja sadrži 3-7 članova u prstenu, od kojih su do četiri člana prstena opciono heteroatomi nezavisno izabrani od kiseonika, sumpora i azota, pod uslovom, međutim, daje u karbocikličnom prstenu najmanje jedan atom ugljenika i da, u koliko se nalaze dva ili više atoma kiseonika u prstenu, atomi kiseonika u prstenu se ne nalaze jedan pored drugog, pri čemu je karbociklična grupa nesupstituisana ili supstituisana sa jednom, dve ili tri grupe nezavisno izabrane od halogena, hidroksi, hidroksialkil, niže alkil, niže alkoksi, alkoksikarbonil, alkilkarbonil, alkilkarbonilamino, aminoalkil, trifluorometil, N-hidroksiacetamid, trifluorometilalkil, amino i mono ili dialkilamino grupe; W je anjon izabran iz grupe koja sadrži hlorid, bromid, trifluoroacetat i trietilamonijum anjon; m = 0-6; R4 i jedan od X1, X2 i X3 mogu da formiraju aromatični prsten koji sadrži do tri heteroatoma nezavisno izabrana od kiseonika, sumpora i azota i koji je opciono supsituisan sa do 4 grupe nezavisno izabrane od halogena, hidroksi, hidroksialkil, niže alkil, niže alkoksi, alkoksikarbonil, alkilkarbonil, alkilkarbonilamino, aminoalkil, aminoalkilkarbonil, trifluorometil, trifluorometilalkil, trifluorometilaminoalkil, amino, mono- ili dialkilamino, N-hidroksiacetamido, aril, heteroaril, karboksialkil, nitril, NR7SO2R8, C(O)NR7R8, NR7C(O)R8, C(O)OR7, C(O)NR7SO2R8, (CH2)mS(O)nR7, (CH2)m-heteroaril, O(CH2)m-heteroaril, (CH2)mC(O)NR7R8, O(CH2)mC(O)OR7, (CH2)mSO2NR7R8 i C(O)R7 grupe; R3 je vodonik, aril, C1-C8 alkil, C1-C8 alkoksi, C3-C7 cikloalkil ili C3-C7 heterociklil grupa; R3 i R6 su nezavisno vodonik, C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, arilalkil, cikloalkil, heterocikloalkil, aril, heteroaril ili heteroarilalkil grupa; ili R3 i R6, kada su vezani za isti atom azota, uzeti zajedno sa azotom za koji su vezani, grade heterociklični prsten koji sadrži od 3-8 članova u prstenu, od kojih do četiri člana može opciono da se zameni sa heteroatomima nezavisno izabranim od kiseonika, sumpora, S(O), S(O)2 i azota, pod uslovom, međutim, da je u karbocikličnom prstenu najmanje jedan atom ugljenika i da, u koliko se nalazi dva ili više atoma kiseonika u prstenu, atomi kiseonika u prstenu se ne nalaze jedan pored drugog, pri čemu je heterociklična grupa nesupstituisana ili supstituisana sa jednom, dve ili tri grupe nezavisno izabrane od halogena, hidroksi, hidroksialkil, niže alkil, niže alkoksi, alkoksikarbonil, alkilkarbonil, alkilkarbonilamino, aminoalkil, aminoalkilkarbonil, trifluorometil, trifluorometilalkil, trifluorometilalkilaminoalkil, amino, nitril, mono- ili dialkilamino, N-hidroksiacetamido, aril, heteroaril, karboksialkil, NR7SO2R8, C(O)NR7R8, NR7C(O)R8, C(O)0R7, C(O)NR7SO2R8, (CH2)mS(O)nR7, (CH2)m-heteroaril, O(CH2)m-heteroaril, (CH2)mC(O)NR7R8, O(CH2)mC(O)OR7 i (CH2)mSO2NR7R8 grupe; R7 i R8 su nezavisno vodonik, C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, arilalkil, cikloalkil, heterocikloalkil, aril, heteroaril ili heteroarilalkil grupa; ili R7 i R8, kada su vezani za isti atom azota, uzeti zajedno sa azotom za koji su vezani, grade heterociklični prsten koji sadrži od 3-8 članova u prstenu, od kojih su četiri opciono heteroatomi nezavisno izabrani od kiseonika, sumpora, S(O), S(O)2 i azota, pod uslovom, međutim, da je u karbocikličnom prstenu najmanje jedan atom ugljenika i da, u koliko se u prestenu nalazi dva ili više atoma kiseonika, atomi kiseonika u prstenu se ne nalaze jedan pored drugog, pri čemu je heterociklična grupa nesupstituisana ili supstituisana sa jednom, dve ili tri grupe nezavisno izabrane od halogena, hidroksi, hidroksialkil, niže alkil, niže alkoksi, alkoksikarbonil, alkilkarbonil, alkilkarbonilamino, aminoalkil, aminoalkilkarbonil, trifluorometil, trifluorometilalkil, trifluorometilalkilaminoalkil, amino, nitril, mono- ili dialkilamino, N-hidroksiacetamido, aril, heteroaril, karboksialkil grupe i njihove farmaceutski prihvatljive soli, estri, amidi i prolekovi.
2. Jedinjenje u skladu sa patentnim zahtevom 1, naznačeno time što ima sledeću strukturu: pri čemu su R1, R2, R3, R4, X1, X2 i X3 kako je definisano za formulu I.
3. Jedinjenje u skladu sa patentnim zahtevom 1 ili patentnim zahtevom 2, naznačeno time stoje R3 ciklopentil grupa.
4. Jedinjenje u skladu sa patentnim zahtevom 2 ili patentnim zahtevom 3, naznačeno time što je R1 alkil grupa.
5. Jedinjenje u skladu sa patentnim zahtevom 2 ili patentnim zahtevom 3, naznačeno time što je R1 metil grupa.
6. Jedinjenje u skladu sa patentnim zahtevom 2 ili patentnim zahtevom 3, naznačeno time što je R2 (CO)CH3 grupa.
7. Jedinjenje u skladu sa patentnim zahtevom 1 naznačeno time što je izabrano iz grupe koja sadrži: 8-Ciklopenlil-2-(piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 8-Ciklopentil-6-etil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, Etil estar hidrohlorid 8-ciklopentil-7-okso-2-(5-piperazin-l -il-piridin-2-ilamino)-7, 8-dihidro-pirido[2, 3-d]pirimidin-6-karboksilatne kiseline, 6-Amino-8-ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 6-Bromo-8-ciklopentil-2-[5-((R)-1-metil-l-pirolidin-2-il)-piridin-2-ilamino]-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 6-Bromo-8-cikloheksil-2-(piridin-2-il-amino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-il)-piridin-2-ilamino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(3, 3-dimetil-piperazin-l-il)-piridin-2-ilamino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-[5-(4-metil-piperazin-l-il)-piridin-2-ilamino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-[5-(3-amino-pirolidin-l-il)-piridin-2-ilamino]-8-ciklopentil-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-(5-morfolin-4-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 2-{5-[Bis-(2-metoksi-etil)-amino]-piridin-2-ilamino}-6-bromo-8-ciklopentil-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-(5-morfolin-4-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-{5-[bis-(2-metoksi-etil)-amino]-piridin-2-ilamino}-8-ciklopentil-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-[6-(8-ciklopentil-6-jodo-5-metil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-piperazin-l-karboksilatne kiseline, 8-Ciklopentil-6-jodo-5-metil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-[6-(8-ciklopentil-6-(2-etok. si-etoksi)-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-piperazin-l-karboksilatne kiseline, 8-Ciklopentil-6-(2-etoksi-etoksi)-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 2-{5-[Bis-(2-metoksi-etil)-amino]-piridin-2-ilamino}-6-bromo-8-ciklopentil-5-metil-8H-pirido[2, 3-d]pirimidin 7 on, 6-Acetil-2-{5-[bis-(2-metoksi-etil)-amino]-piridin-2-ilamino}-8-ciklopentil-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-[6-(8-izopropil-7-okso-7, 8-dihidro-pirido[2, 3]pirimidin-2-ilamino)-piridin-3-il]-piperazin-l-karboksilatne kiseline, 8-Izopropil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-[6-(8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3]pirimidin-2-ilamino)-piridin-3-il]-piperazin-1 -karboksilatne kiseline, 8-Ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-[6-(8-cikloheksil-7-okso-7, 8-dihidro-pirido[2, 3]pirimidin-2-ilamino)-piridin-3-il]-piperazin-l-karboksilatne kiseline, 8-Cikloheksil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-[6-(8-ciklopropil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piriđin-3-il ]-piperazin-1 -karboksilatne kiseline, 8-Ciklopropil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(piridin-2, 6-ildiamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-(piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-[5-(4-metil-piperazin-l-il)-piridin-2-ilamino]-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-( 1 -etoksi-vinil)-5-metil-2-[5-(4-metil-piperazin-1 -il)-piridin-2-ilamino]-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar (l-{6-[8-ciklopentil-6-(l-etoksi-vinil)-5-metil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino]-piridin-3-il}-pirolidin-3-il)-karbamatne kiseline, 6-Acetil-8-ciklopentil-2-(4-hidroksi-3, 4, 5, 6-tetrahidro-2H-[l, 3']bipiridinil-6'-ilamino)-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-[6-(6-bromo-8-ciklopentil-5-metil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-iilamino)-piridin-3-il]-azepan-1 -karboksilatne kiseline, 6-Bromo-8-ciklopentil-2-(5-[l, 4]diazepan-l-il-piridin-2-ilamino)-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-{6-[8-ciklopentil-6-(l-etoksi-vinil)-5-metoksi-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino]-piridin-3-il}-[l, 4]diazepan-l-karboksilatne kiseline, 6-Acetil-8-ciklopentil-2-(5-[l, 4Jdiazepan-l-il-piridin-2-ilamino)-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-(piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-{6-[8-ciklopentil-5-metil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-piperazin-l-karboksilatne kiseline, 8-Ciklopentil-5-metil-2-(5-piperazin-4-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-[6-(6-bromo-8-ciklopentil-5-metil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-2, 2-dimetil-piperazin-l-karboksilatne kiseline, 6-Bromo-8-ciklopentil-2-[5-(3, 3-dimetil-piperazin-l-il)-piridin-2-iilamino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-{6-[8-ciklopentil-6-(l-etoksi-vinil)-5-metil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino]-piridin-3-il}-2, 2-dimetil-piperazin-l-karboksilatne kiseline, Terc-butil estar 4-[6-(6-bromo-8-ciklopentil-5-metil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-2, 6-dimetil-piperazin-l-karboksilatne kiseline, 6-Bromo-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-il)-piridin-2-iilamino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-{6-[8-ciklopentil-6-(l-etoksi-vinil)-5-metil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino]-piridin-3-il}-2, 6-dimetil-piperazin-l-karboksilatne kiseline, 8-Ciklopentil-6-(l-etoksi-vinil)-5-metil-2-(5-morfolin-4-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-(3, 4, 5, 6-tetrahidro-2H-[l, 3']bipiridinil-6'-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-(l-etoksi-vinil)-5-metil-2-(3, 4, 5, 6-tetrahidro-2H-[1, 3']bipiridinil-6'-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-(3, 4, 5, 6-tetrahidro-2H-[l, 3']bipiridinil-6'-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-{6-[8-ciklopentil-6-(2-etoksi-etil)-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino]-piridin-3-il}-piperazin-l-karboksilatne kiseline, 8-Ciklopentil-6-(2-etoksi-etil)-2-(5-piperazin-l-il-piriđin-3-ilamino-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-{6-[8-ciklopentil-6-(2-metoksi-etoksimetil)-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino]-piridin-3-il}-piperazin-l-karboksilatne kiseline, 8-Ciklopentil-6-(2-metoksi-etoksimetil)-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-[6-(8-ciklopentil-6-etoksimetil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-piperazin-1 -karboksilatne kiseline, 8-Ciklopentil-6-etoksimetil-2-(5-piperazin-1 -il-piridin-2-ilamino)- 8H-pirido[2, 3-d]pirimidin-7-on, Terc-butil estar 4-f6-(8-ciklopentil-6-metoksimelil-7-ukso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-piperazin-l-karboksilatne kiseline, 8-Ciklopentil-6-metoksimetil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopenLil-2-[5-(2, 6-dirnetil-morfolin-4-il)-piridin-2-i1amino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-etoksimetil-2-(3, 4, 5, 6-tetrahidro-2H-[l, 3']bipiridinil-6'-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-etoksimetil-2-(5-morfolin-4-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, Benzil estar [8-ciklopentil-7-okso-2-(3, 4, 5, 6-tetrahidro-2H-[l, 3']bipiridinil-6'-ilamino)-7, 8-dihidro-pirido[2, 3-d]pirimidin-6-ilmetil]-karbamatne kiseline, 8-Ciklopentil-2-[5-(2, 6-dimetil-morfolin-4-il)-piridin-2-ilamino]-6-(l-etoksi-vinil)-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(2, 6-dimetil-morfolin-4-il)-piridin-2-ilamino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-5-metil-2-(5-piperazin-l-il-piridin-2-ilamino)-6-propionil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-fluoro-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 8-Ciklopentil-6-metil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 8-Ciklopentil-6-izobutoksi-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 6-Benzil-8-ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 8-Ciklopentil-6-hidroksimetil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, Etil estar 2-[5-(4-terc-butoksikarbonil-piperazin-1 -il)-piridin-2-ilamino]-8-ciklopentil-5-metil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-6-karboksilatne kiseline, 6-Acetil-8-ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-(5-piperazin-l-il-piridin-2-ilamino-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-(piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-il)-piridin-2-ilamino]-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(3, 3-dimctil-piperazin-l-il)-piridin-2-ilamino]-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(4-melil-piperaziii-l-il)-pindin-2-ilamino]-8H-pirido[2, 3-d]pirimidin-7-on, 2-[5-(3-Amino-pirolidin-l-il)-piridin-2-ilamino]-6-bromo-8-ciklopentil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-eiklopentil-2-[5-(3-etilamino-pirolidin-1-il)-piridin-2-ilamino]-8I I-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(5-pirolidin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 2-{5-[3-(l-Amino-l-metil-etil)-pirolidin-l-il]-piridin-2-ilamino}-6-bromo-8-ciklopentil-8H-pirido[2, 3-d]pirimidin-7-on, l-[6-(6-Bromo-8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-pirolidin-2-karboksilatna kiselina, 6-Bromo-8-ciklopentil-2-[5-(4-dietilamino-butilamino)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(3-etilamino-pirolidin-l-il)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-(5-pirolidin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-{5-[3-(l-amino-l-metil-etil)-pirolidin-l-il]-piridin-2-ilamino}-8-ciklopentil-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 1-[6-(6-Acetil-8-ciklopentil-5-metil-7-okso7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-pirolidin-2-karboksilatna kiselina, 6-Acetil-8-ciklopentil-2-[5-(4-dietilamino-butilamino)-piridin-2-ilamino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-il)-piridin-2-ilamino]-6-etil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-2-[5-(3, 3-dimetil-piperazin-l-il)-piridin-2-ilamino]-6-etil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-[5-(4-metil-piperazin-l-il)-piridin-2-ilamino]-6-etil-8H-pirido[2, 3-d]pirimidin-7-on, 2- [5-(3-Amino-pirolidin-l-il)-piridin-2-ilamino]-8-ciklopentil-6-etil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-[5-(3-etilamino-pirolidinl-l-il)-piridin-2-ilamino]-6-etil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-(5-pirolidin-1 -il-piridin-2-ilamino)-8II-pirido[2, 3-d]pirimidin-7-on, 2- {5-[3-( 1 -Amino-1 -metil-etil)-pirolidin-1 -il-piridin-2-ilamino}-8-ciklopentil-6-etil-8H-pirido[2, 3-d]pirimidin-7-on, l-[6-(8-Ciklopentil-6-etil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-pirolidin-2-karboksilatna kiselina, 8-Ciklopentil-2-[5-(4-dietilamino-butilamino)-piridin-2-ilamino]-6-etil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Benzil-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-il)-piridin-2-ilamino]-8H- piriilo[2, 3-d]pirimidin-7-on, 6-Benzil-8-ciklopentil-2-[5-(3, 3-dimetil-piperazin-l-il)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Benzil-8-ciklopentil-2-[5-(4-metil-piperazin-l-il)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 2-[5-(3-Amino-pirolidin-l-il)-piridin-2-ilamino]-6-benzil-8-ciklopentil-8H- pirido[2, 3-d]pirimidin-7-on, 6-Benzil-8-ciklopentil-2-[5-(3-etilamino-pirolidin-l-il)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Benzil-8-ciklopentil-2-(5-pirolidin-l-il-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 2- {5-[3-( 1 -Amino-1 -metil-etil)-pirolidin-1 -il]-piridin-2-ilamino} -6-benzil-8-ciklopentil-8H-pirido[2, 3-d]pirimidin-7-on, 1-[6-(6-Benzil-8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-pirolidin-2-karboksilatna kiselina, 6-Benzil-8-ciklopentil-2-[5-(4-dietilamino-butilamino)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-il)-piridin-2-ilamino]-6- hidroksimetil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-2-[5-(3, 3-dimetil-piperazin-l-il)-piridin-2-ilamino]-6- hidroksimetil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-hidroksimetil-2-[5-(4-metil-piperazin-l-il)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 2-[5-(3-Amino-pirolidin-l-il)-piridin-2-ilamino]-8-ciklopentil-6-hidroksimetil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-2-[5-(3-etilamino-pirolidin-l-il)-piridin-2-ilamino]-6- hidroksimetil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-hidroksimetil-2-(5-pirolidin-l-il-piridin-2-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 2-{5-[3-(l-Amino-l-metil-etil)-pirolidin-l-il]-piridin-2-ilamino}-8-ciklopentil- 6-hidroksimetil-8H-pirido[2, 3-d]pirimidin-7-on, l-[6-(8-Ciklopentil-6-hidroksimetil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-pirolidin-2-karboksilatna kiselina, 8-Ciklopentil-2-[5-(4-dietilamino-butilamino)-piridin-2-ilamino]-6- hidroksimetil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Amino-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-il)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Amino-8-ciklopentil-2-[5-(3, 3-dimetil-piperazin-l-il)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Amino-8-ciklopentil-2-[5-(4-metil-piperazin-l -il)-piridin-2-ilamino]-8H-pirido[2, 3-d]pirimidin-7-on, 6-Amino-2-[5-(3-aminu-pirulidiii-l-il)-pii'idin-2-ilamino]-8-ciklopenlil-8II- pirido[2, 3-d]pirimidin-7-on, 6-Aminn-8-ciklopentil-2-[5-(3-etilamino-pirolidin-l-il)-piridin-2-ilarnino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Aminu-8-eiklopenLil-2-(5-pirulidiii-l-il-pindin-2-ilamino)-8II-pirido[2, 3- d]pirimidin-7-on, 6-Amino-2-{5-[3-(l-amino-l-metil-etil)-pirolidin-l-il]-piridin-2-ilamino}-8- ciklopentil-8H-pirido[2, 3-d]pirimidin-7-on, 1-[6-(6-Amino-8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-il]-pirolidin-2-karboksilatna kiselina, 6-Amino-8-ciklopentil-2-[5-(4-dietilamino-butilamino)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(3, 4, 5, 6-tetrahidro-2H-[l, 3'[bipiridinil-6'-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(5-morfolin-4-il-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(5-dietilamino-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 2-{5-[Bis-(2-hidroksi-etil)-amino]-piridin-2-ilamino}-6-bromo-8-ciklopentil-8H-pirido[2, 3-d]pirimidin-7-on, 2-{5-[Bis-(2-metoksi-etil)-amino]-piridin-2-ilamino}-6-bromo-8-ciklopentil- 8H-pirido[2, 3-d]pirimidin-7-on, 2-[5-(2-Amino-etilamino)-piridin-2-ilamino]-6-bromo-8-ciklopentil-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(5-dimetilamino-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, N-[6-(6-Bromo-8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2- ilamino)-piridin-3-il]-N-metil-acetamid, 6-Bromo-8-ciklopentil-2-[5-(2-metoksi-etoksi)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(2-metoksi-etoksimetil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(2-dietilamino-etoksi)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(5-pirolidin-l-il-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(6-metil-5-piperazin-l-il-piridin-2-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-(3, 4, 5, 6-tetrahidro-2II-[1, 3']bipiridinil-6'- ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(5-dietilamino-piridin-2-ilamino)-5-metil-8H- pirido[2, 3-d]pirimidin-7-on, 2-{5-[Bis-(2-hidroksi-etil)-amino]-piridin-2-ilamino}-6-bromo-8-ciklopentil-5- metil-8H-pirido[2, 3-d]pirimidin-7-on, 2-[5-(2-Amino-etilamino)-piridin-2-ilamino]-6-bromo-8-ciklopentil-5-metil- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(5-dimetilamino-piridin-2-ilamino)-5-metil-8H- pirido[2, 3-d]pirimidin-7-on, N-[6-(6-Bromo-8-ciklopentil-5-metil-7-okso-7, 8-dihidro-pirido[2, 3- d]pirimidin-2-ilamino)-piridin-3-il]-N-metil-acetamid, 6-Bromo-8-ciklopentil-2-[5-(2-metoksi-etoksi)-piridin-2-ilamino]-5-metil-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(2-metoksi-etoksimetil)-piridin-2-ilamino]-5- metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(2-dietilamino-etoksi)-piridin-2-ilamino]-5-rnetil- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-(5-pirolidin-l-il-piridin-2-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-(6-metil-5-piperazin-l-il-piridin-2-ilamino)- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-(3, 4, 5, 6-tetrahidro-2H-[l, 3']bipiridinil-6'- ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-(5-dietilamino-piridin-2-ilamino)-5-metil-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-{5-[bis-(2-hidroksi-etil)-amino]-piridin-2-ilamino}-8-ciklopentil-5- metil-8H-pirido[2, 3~d]pirimidin-7-on, 6-Acetil-2-[5-(2-amino-etilamino)-piridin-2-ilamino]-8-ciklopentil-5-metil-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-(5-dimetilamino-piridin-2-ilamino)-5-metil-8H- pirido[2, 3-d]pirimidin-7-on, N-[6-(6-Acetil-8-ciklopentil-5-metil-7-okso-7, 8-dihidro-pirido[2, 3- d]pirimidin-2-ilamino)-piridin-3-il]-en-metil-acetamid, 6-Acetil-8-ciklopentil-2-[5-(2-metoksi-etoksi)-piridin-2-ilamino]-5-metil-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(2-metoksi-etoksimetil)-piridin-2-ilamino]-5-metil- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(2-dietilamino-etoksimetil)-piridin-2-ilamino]-5- metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-(5-pirolidin-l-il-piridin-2-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-(6-metil-5-piperazin-l-il-piridin-2-ilamino)- 8II-pirido[2,3-d]pirirnidin-7-on, 6-Acetil-8-ciklopentil-2-(3, 4, 5, 6'tetrahidro-2H-[ 1, 3']bipiridinil-6'-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-(5-morfolin-4-il-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-(5-dietilarnino-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Acetil-2'{5-[bis-(2-hidroksi-etil)-aminoj-piridin-2-ilamino}-8-ciklopenlil- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-{5-[bis-(2-metoksi-etil)-amino]-piridin-2-ilamino}-8-ciklopentil- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-[5-(2-amino-etilamino)-piridin-2-ilamino]-8-ciklopentil-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-(5-dimetilamino-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, N-[6-(6-Acetil-8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2- ilamino)-piridin-3-il]-N-metil-acetamid, 6-Acetil-8-ciklopentil-2-[5-(2-metoksi-etoksi)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(2-metoksi-etoksimetil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(2-dietilamino-etoksi)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-(5-pirolidin-l-piridin-2-ilamino)-8H-pirido[2, 3- dJpirimidin-7-on, 6-Acetil-8-ciklopentil-2-(6-metil-5-piperazin-l-piridin-2-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(2-metoksi-etoksi)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(2-metoksi-etilamino)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 2-(5-Azetidin-l-il-piridin-2-ilamino)-6-bromo-8-ciklopentil-8H-pirido[2, 3- d]pirimidin-7-on, 2-(5-Azepan-l-il-piridin-2-ilamino)-6-bromo-8-ciklopentil-8H-pirido[2, 3- d]pirimidin-7-on, N-[6-(6-Bromo-8-ciklopentil-2-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2- ilamino)-piridin-3-il]-acetamid, 6-Bromo-8-ciklopentil-2-(5-fenilamino-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(4-fluoro-benzilamino)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, N-[6-(6-Bromo-8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2- ilamino)-piridin-3-il]-metansulfonamid, 6-Bromo-8-ciklopentil-2-(5-metansulfonil-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Bromo-8-ciklopentil 2-(5-fenil-piridin-2-ilamino)-8H-pirido[2! 3-d]pirimidin-7-on, 6-Amino-8-ciklopenLil-2-[5-(2-metoksi-etoksi)-piridin-2-ilamino]-8II- pirido[2! 3-d]pirimidin-7-on, 6-Amino-8-ciklopentil-2-[5-(2-metoksi-etilamino)-piridin-2-ilamino]-8li- pirido[2, 3-d]pirimidin-7-on, 6-Amino-2-(5-azetidin-l-il-piridin-2-ilamino)-8-ciklopentil-8H-pirido[2, 3- d]pirimidin-7-on, 6-Amino-2-(5-azepan-l-il-piridin-2-ilamino)-8-ciklopentil-8H-pirido[2, 3- d]pirimidin-7-on, N[6-(6-Amino-8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2- iiamino)-piridin-3-il]-acetamid, 6-Amino-8-ciklopentil-2-(5-fenilamino-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Amino-8-ciklopentil-2-[5-(4-fluoro-benzilamino)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, N[6-(6-Amino-8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2- iiamino)-piridin-3-il]-metansulfonamid, 6-Amino-8-ciklopentil-2-(5-metansulfonil-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Amino-8-ciklopentil-2-(5-fenil-piridin-2-ilamino)-8H~pirido[2, 3- d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(2-metoksi-etoksi)-piridin-2-ilamino]-5-rnetil-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(2-metoksi-etilamino)-piridin-2-ilamino]-5-metil- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-(5-azetidin-l-il-piridin-2-ilamino)-8-ciklopentil-5-metil-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-(5-azepan-l-il-piridin-2-ilamino)-8-ciklopentil-5-metil-8H- pirido[2, 3-d]pirimidin-7-on, N-[6-(6-Acetil-8-ciklopentil-5-metil-7-okso-7, 8-dihidro-pirido[2, 3- d]pirimidin-2-ilamino)-piridin-3-il]-acetamid, 6-Acetil-8-ciklopentil-5-metil-2-(5-fenilamino-piridin-2-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(4-fluoro-benzilamino)-piridin-2-ilamino]-5-metil- 8H-pirido[2, 3-d]pirimidin-7-on, N-[6-(6-Acetil-8-ciklopentil-5-metil-7-okso-7, 8-dihidro-pirido[2, 3- d]pirimidin-2-ilamino)-piridin-3-il]-metansulfonamid, 6-Acetil-8-ciklopentil-2-(5-metansulfonil-piridin-2-ilamino)-5-metil-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-(5-fenil-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Benzil-8-ciklopentil-2-f5-(2-metoksi-etoksi)-piridin-2-ilamino]-8H- pirido[2, 3-dJpirimidin-7-on, 6-Benzil-8-ciklopentil-2-[5-(2-metoksi-etilamino)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidui-7-on, 2-(5-Azetidin-l-il-piridin-2-ilamino)-6-benzil-8-ciklopentil-8H-pirido[2, 3- d]pirimidin-7-on. 2-(5-Azepan-l-il-piridin-2-ilamino)-6-benzil-8-ciklopentil-8H-pirido[2, 3- d]pirimidin-7-on, N-[6-(6-Benzil-8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2- ilamino)-piridin-3-il]-acetamid, 6-Benzil-8-ciklopentil-2-(5-fenilamino-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Benzil-8-ciklopentil-2-[5-(4-fluoro-benzilamino)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, N-[6-(6-Benzil-8-ciklopentil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2- ilamino)-piridin-3-il]-metansulfonamid, 6-Benzil-8-ciklopentil-2-(5-metansulfonil-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Benzil-8-ciklopentil-2-(5-fenil-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin- 7-on, 8-Ciklopentil-6-hidroksimetil-2-[5-(2-metoksi-etoksi)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-hidroksimetil-2-[5-(2-metoksi-etilamino)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 2-(5-Azetidin-l-il-piridin-2-ilamino)-8-ciklopentil-6-hidroksimetil-8H- pirido[2, 3-d]pirimidin-7-on, 2-(5-Azepan-l-il-piridin-2-ilamino)-8-ciklopentil-6-hidroksimetil-8H- pirido[2, 3-d]pirimidin-7-on, N-[6-(8-Ciklopentil-6-hidroksimetil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin- 2-ilamino)-piridin-3-il]-acetamid, 8-Ciklopentil-6-hidroksimetil-2-(5-fenilamino-piridin-2-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-2-[5-(4-fluoro-benzilamino)-piridin-2-ilamino]-6-hidroksimetil- 8H-pirido[2, 3-d]pirimidin-7-on, N-[6-(8-Ciklopentil-6-hidroksimetil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin- 2-ilamino)-piridin-3-il]-metansulfonamid, 8-Ciklopentil-6-hidroksimetil-2-(5-metansulfonil-piridin-2-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-hidroksimetil-2-(5-fenil-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-|5-(2-mctoksi-etoksi)-piridin-2-i]amino]-8H-pirido[2, 3- d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-[5-(2-metoksi-et. i1amino)-piridin-2dlamino]-8H- pirido[2, 3-d]pirimidin-7-on, 2-(5-Azetidin-l -il-piridin-2-ilamino)-8-ciklopentil-6-ctil-8H-pirido[2, 3-d]pirimidin-7-on, 2-(5-Azepan-l-il-piridin-2-ilamino)-8-ciklopentil-6-etil-8H-pirido[2, 3- d]pirimidin-7-on, N-[6-(8-Ciklopentil-6-etil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2- ilamino)-piridin-3-il]-acetamid, 8-Ciklopentil-6-etil-2-(5-fenilamino-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 8-Ciklopentil-2-[5-(4-fluoro-benzilamino)-piridin-2-ilamino]-6-etil-8H- pirido[2, 3-d]pirimidin-7-on, N-[6-(8-Ciklopentil-6-etil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2- ilamino)-piridin-3-il]-metansulfonamid, 8-Ciklopentil-6-etil-2-(5-metansulfonil-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-(5-fenil-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7- on, 6-Bromo8-ciklopentil-2-[5-(piperazin-l-karbonil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-karbonil)-piridin-2- ilamino]-8H-pirido[2, 3-d]pirimidin-7-on, 2-[5-(3-Amino-pirolidin-l-karbonil)-piridin-2-ilamino]-6-bromo-8-ciklopentil- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(morfolin-4-karbonil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-[5-(piperazin-l-karbonil)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-karbonil)-piridin-2- ilamino]-8H-pirido[2, 3-d]pirimidin-7-on, 2-[5-(3-Amino-pirolidin-l-karbonil)-piridin-2-ilamino]-6-bromo-8-ciklopentil- 5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-[5-(morfolin-4-karbonil)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-[5-(piperazin-l-karbonil)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-karbonil)-piridin-2- ilamino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-[5-(3-amino pirolidin-l-karbonil)-piridin-2-ilamino]-8-ciklopentil-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-[5-(morfolin-4-karbonil)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-[5-(piperazin-l-karbonil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-karbonil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 2-[5-(3-Amino-pirolidin-l-karbonil)-piridin-2-ilamino]-8-ciklopentil-6-etil- 8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-[5-(morfolin-4-karbonil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(piperazin-l-sulfonil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(morfolin-4-sulfonil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 2-[5-(3-Amino-pirolidin-l-sulfonil)-piridin-2-ilamino]-6-bromo-8-ciklopentil- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-sulfonil)-piridin-2- ilamino]-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-rnetil-2-[5-(piperazin-l-sulfonil)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-[5-(morfolin-4-sulfonil)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 2-[5-(3-Amino-pirolidin-l-sulfonil)-piridin-2-ilamino]-6-bromo-8-ciklopentil- 5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-sulfonil)-piridin-2- ilamino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-[5-(piperazin-l-sulfonil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-[5-(morfolin-4-sulfonil)-piridin-2-ilamino]-8H- pirido[2, 3-d]pirimidin-7-on, 2-[5-(3-Amino-pirolidin-l-sulfonil)-piridin-2-ilamino]-8-ciklopentil-6-etil-8H- pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-sulfonil)-piridin-2-ilamino]-6-etil- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-[5-(piperazin-l-sulfonil)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-[5-(morfolin-4-sulfonil)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-[5-(3-amino-pirolidin-l-sulfonil)-piridin-2-ilamino]-8-ciklopentil-5- metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-(3, 5-dimetil-piperazin-l-sulfonil)-piridin-2-ilamino]-5-mctil-8H-pirido[2, 3-d]pirimidin-7-on, i 6-Acetil-8-ciklopentil-5-metil-2-([l, 6]naftiridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Acetil-8-ciklopentil-2-[5-( 1, 1 -diokso-116-tiomorfolin-4-il)-piridin-2-ilamino]-5-metil-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-hidroksimetil-5-metil-2-(5-piperazin-l-il-piridin-2-ilamino- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acelil-2-(3-hl()ro-5-piperazin-l-il-piiidin-2-ilamino)-8-ciklopentil-5-metil- 8H-pirido[2, 3-d]pirimidin-7-on, 4-[6-Acetil-5-metil-7-okso-2-(piridin-2-ilamino)-7H-pirido[2, 3-d]pirimidin-8-il]-cikloheksankarboksilatna kiselina, 4-[6-Acetil-2-(5-dimetilamino-piridin-2-ilamino)-5-metil-7-okso-7H-pirido[2, 3-d]pirimidin-8-il]-cikloheksankarboksilatna kiselina, 6-Bromo-8-ciklopentil-5-metil-2-[5-(piperazin-l-sulfonil)-piridin-2-ilamino]- 8H-pirido[2, 3-d]pirimidin-7-on, 6-(8-Ciklopentil-6-etil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-3-piperazin-1 -il-piridin-2-karboksilatna kiselina, 2-(6-Acetil-5-piperazin-l-il-piridin-2-ilamino)-8-ciklopentil-6-etil-8H-pirido[2, 3-d]pirimidin-7-on, 3-{2-[6-(8-Ciklopentil-6-etil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-iloksi]-etoksi}-propionatna kiselina, [6-(8-Ciklopentil-6-etil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-2-ilamino)-piridin-3-iloksi]-acetatna kiselina, 8-Ciklopentil-2-(5-{2-[2-(5-metil-piridin-2-il)-etoksi]-etoksi}-piridin-2- ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 2-[5-(3-Benzensulfonil-propoksi)-piridin-2-ilamino]-8-ciklopentil-8H- pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-etil-2-{5-[2-(2-metoksi-etoksi)-etoksi]-piridin-2-ilamino}-8H- pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-2-(5-{[3-(3, 5-dimetil-piperazin-l-il)-propil]-metil-amino}- piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-2-{5-[(3-imidazol-l-il-propil)-metil-amino]-piridin-2-ilamino}- 8H-pirido[2, 3-d]pirimidin-7-on, 6-Acetil-5-metil-2-(5-metil-2-piridin-2-ilamino)-8-piperidin-4-il-8H- pirido[2, 3-d]pirimidin-7-on, 6-Acetil-2-[5-(3, 4-dihidroksi-pirolidin-l-il)-piridin-2-ilamino]-8-metoksimetil- 5-metil-8H-pirido[2, 3-d]pirimidin-7-on.
8. Jedinjenje u skladu sa patentnim zahtevom 10 naznačeno time što je izabrano iz grupe koja sadrži: 8-Ciklopentil-2-(piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 8-Ciklopentil-6-etil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, Hidrohlorid etil estra 8-ciklopentil-7-okso-2-(5-piperazin-l-il-piridin-2-ilamino)-7, 8-dihidro-pirido[2, 3-d]pirimidin-6-karboksilatne kiseline, 6 Amino-8-ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-dJpirimidin-7-on hidrohlorid, 6-Bromo-8-ciklopentil-2-[5-((R)-1-metil-1-pirolidin-2-il)-piridin-2-ilamino]-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 6-Bromo-8-cikloheksil-2-(piridin-2-il-amino)-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-2-metil-8H-pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 8-Ciklopentil-6-fluoro-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 8-Ciklopentil-6-metil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 8-Ciklopentil-6-izobutoksi-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 6-Benzil-8-ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, 8-Ciklopentil-6-hidroksimetil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on hidrohlorid, Etil estar 2-[5-(4-terc-butoksikarbonil-piperazin-l-il)-piridin-2-ilamino]-8-ciklopentil-5-metil-7-okso-7, 8-dihidro-pirido[2, 3-d]pirimidin-6-karboksilatne kiseline, 6-Acetil-8-ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H-pirido[2, 3- d]pirimidin-7-on, 6-Acetil-8-ciklopentil-5-metil-2-(5-piperazin-l-il-piridin-2-ilamino)-8H- pirido[2, 3-d]pirimidin-7-on, 6-Bromo-8-ciklopentil-5-metil-2-(piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on, i 6-bromo-8-ciklopentil-2-(piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on.
9. 6-Acetil-8-ciklopentil-5-metil-2-(5-piperazin-1 -il-piridin-2-ilamino)-8H-pirido[2, 3-d]pirimidin-7-on.
10. Postupak za lečenje oboljenja ili stanja izazvanih abnormalnom proliferacijom ćelija kod sisara, uključujući ljude, koji uključuje primenu na navedenom sisaru određene količine jedinjenja u skladu sa patentnim zahtevom 1, naznačene time što je efikasna u lečenju takvog stanja ili oboljenja.
11. Postupak u skladu sa patentnim zahtevom 14, naznačen time što je oboljenje ili stanje koje se tretira izabrano iz grupe koja sadrži vaskularnu proliferaciju glatkih mišića povezanu sa aterosklerozom, posthirurške vaskularne stenoze i restenoze i endometrioze.
12. Postupak za lečenje oboljenja ili stanja izazvanih infekcijama koje su izabrane iz grupe koja sadrži virusne infekcije kao što DNA virusi, kao herpesi i RNA virusi kao HIV i gljivične infekcije kod sisara, uključujući i ljude, koji uključuje primenu na navedenom sisaru one količine jedinjenja u skladu sa patentnim zahtevom 1, koja je efikasna u lečenju takvog stanja ili oboljenja.
13. Postupak za lečenje oboljenja izabranih iz grupe koja sadrži autoimune bolesti izabrane iz grupe koja sadrži psorijaze, inflamacije kao reumatoidni artritis, lupus, dijabetes tip 1, dijabetičnu nefropatiju, multiple sklerozu, glomerulonefritis, odbacivanje transplantiranog organa, uključujući bolest domaćina kao reakcija na graft kod sisara, uključujući ljude, koji uključuje primenu na navedenom sisaru one količine jedinjenja u skladu sa patentnim zahtevom 1, koja je efikasna u lečenju takvog stanja ili oboljenja.
14. Postupak za lečenje neurodegenerativnih oboljenja, kao što je Alchajmerova bolest kod sisara, uključujući ljude, koji obuhvata primenu na navedenom sisaru one količine jedinjenja u skladu sa patentnim zahtevom 1 koja je efikasna u lečenju takvog stanja ili oboljenja.
15. Postupak u skladu sa patentnim zahtevom 14, naznačen time je abnormalna proliferacija ćelija kancer izabran iz grupe koja sadrži kancere dojke, ovarijuma, cerviksa, prostate, testisa, ezofagusa, stomaka, kože, pluća, kostiju, kolona, pankreasa, tiroide, bilijarnih pasaža, bukalne duplje i faringsa (oralno), usne, jezika, usta, faringsa, tankog creva, kolon-rektuma, debelog creva, rektuma, mozga i centralnog nervnog sistema, glioblastomu, neuroblastomu, keratokantomu, epidermoidni karcinom, karcinom velike ćelije, adenokarcinom, adenom, adenokarcinom, folikularni karcinom, nediferencirani karcinom, papilarni karcinom, seminom, melanom, sarkom, karcinom bešike, karcinom jetre, karcinom bubrega, mijeloidna oboljenja, limfoidna oboljenja, Hočkins, ćelije folikule dlake i leukemija.
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| PCT/IB2003/000059 WO2003062236A1 (en) | 2002-01-22 | 2003-01-10 | 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d]PYRIMIDIN-7-ONES |
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Families Citing this family (327)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7053070B2 (en) * | 2000-01-25 | 2006-05-30 | Warner-Lambert Company | Pyrido[2,3-d]pyrimidine-2,7-diamine kinase inhibitors |
| EP1417207B1 (en) * | 2000-08-04 | 2005-08-31 | Warner-Lambert Company Llc | Process for preparing 2-(4-pyridyl) amino-6-dialkyloxyphenyl-pyrido(2,3-d)pyrimidin-7-ones |
| US6960662B2 (en) * | 2000-08-04 | 2005-11-01 | Warner-Lambert Company | Process for preparing 2-(4-pyridyl)amino-6-dialkyloxyphenyl-pyrido[2,3-d]pyrimidin-7-ones |
| CZ20032416A3 (cs) * | 2001-02-12 | 2004-07-14 | F. Hoffmann-La Roche Ag | 6-Substituované pyridopyrimidiny |
| JP4166991B2 (ja) * | 2001-02-26 | 2008-10-15 | 田辺三菱製薬株式会社 | ピリドピリミジンまたはナフチリジン誘導体 |
| US20030100572A1 (en) * | 2001-06-21 | 2003-05-29 | Ariad Pharmaceuticals,Inc. | Novel pyridopyrimidones and uses thereof |
| US20050154046A1 (en) * | 2004-01-12 | 2005-07-14 | Longgui Wang | Methods of treating an inflammatory-related disease |
| DE60303009T2 (de) | 2002-01-22 | 2006-07-13 | Warner-Lambert Co. Llc | 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-one |
| RU2324695C2 (ru) | 2002-08-06 | 2008-05-20 | Ф.Хоффманн-Ля Рош Аг | 6-АЛКОКСИПИРИДОПИРИМИДИНЫ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ АКТИВНОСТЬЮ ИНГИБИТОРОВ КИНАЗЫ МАР р38 |
| US7112676B2 (en) | 2002-11-04 | 2006-09-26 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| EP1571146A4 (en) | 2002-12-10 | 2010-09-01 | Ono Pharmaceutical Co | NITROGENIC HETEROCYCLIC COMPOUNDS AND THEIR MEDICAL USE |
| CN100497339C (zh) | 2003-04-10 | 2009-06-10 | 霍夫曼-拉罗奇有限公司 | 嘧啶并化合物 |
| JP4053073B2 (ja) * | 2003-07-11 | 2008-02-27 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | 選択的cdk4阻害剤のイセチオン酸塩 |
| NZ544756A (en) | 2003-07-22 | 2009-09-25 | Astex Therapeutics Ltd | 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators |
| SG145695A1 (en) * | 2003-07-29 | 2008-09-29 | Xenon Pharmaceuticals Inc | Pyridyl derivatives and their use as therapeutic agents |
| WO2005047284A1 (en) * | 2003-11-13 | 2005-05-26 | F. Hoffmann-La Roche Ag | Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones |
| JP2007513967A (ja) * | 2003-12-11 | 2007-05-31 | セラヴァンス, インコーポレーテッド | 変異レセプターチロシンキナーゼが駆動する細胞増殖性疾患の処置において使用するための組成物 |
| CN1918158B (zh) * | 2004-02-14 | 2011-03-02 | Irm责任有限公司 | 作为蛋白激酶抑制剂的化合物和组合物 |
| JP2007523151A (ja) * | 2004-02-18 | 2007-08-16 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | 2−(ピリジン−3−イルアミノ)−ピリド[2,3−d]ピリミジン−7−オン |
| WO2005094830A1 (en) * | 2004-03-30 | 2005-10-13 | Pfizer Products Inc. | Combinations of signal transduction inhibitors |
| JP4163738B2 (ja) * | 2004-06-11 | 2008-10-08 | 日本たばこ産業株式会社 | 癌の治療用の5−アミノ−2,4,7−トリオキソ−3,4,7,8−テトラヒドロ−2H−ピリド’2,3−d!ピリミジン誘導体及び関連化合物 |
| US7378423B2 (en) | 2004-06-11 | 2008-05-27 | Japan Tobacco Inc. | Pyrimidine compound and medical use thereof |
| CA2586761A1 (en) | 2004-11-10 | 2006-05-18 | Genzyme Corporation | Methods of treating diabetes mellitus |
| US20060142312A1 (en) * | 2004-12-23 | 2006-06-29 | Pfizer Inc | C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones |
| EP1845973B1 (en) * | 2005-01-21 | 2015-08-12 | Astex Therapeutics Limited | Pharmaceutical compounds |
| AU2006207321B2 (en) * | 2005-01-21 | 2012-09-06 | Astex Therapeutics Limited | Pharmaceutical compounds |
| EP1845975A1 (en) * | 2005-01-21 | 2007-10-24 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors and further antitumor agents |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| AR054425A1 (es) | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
| US8680092B2 (en) | 2005-02-25 | 2014-03-25 | Ono Pharmaceutical Co., Ltd. | Nitrogenous heterocyclic compound and medicinal use thereof |
| MY145343A (en) * | 2005-03-25 | 2012-01-31 | Glaxo Group Ltd | Novel compounds |
| PE20061193A1 (es) * | 2005-03-25 | 2006-12-02 | Glaxo Group Ltd | DERIVADOS DE 3,4-DIHIDROPIRIMIDO[4,5-d]PIRIMIDIN-2-[1H]-0NA COMO INHIBIDORES DE QUINASA p38 |
| RS52711B (sr) | 2005-05-10 | 2013-08-30 | Incyte Corporation | Modulatori indolamin 2,3-dioksigenaze i postupci upotrebe istih |
| KR100734837B1 (ko) * | 2005-09-16 | 2007-07-03 | 한국전자통신연구원 | 다중 생체 인식 시스템 및 그 방법 |
| WO2007036791A1 (en) * | 2005-09-28 | 2007-04-05 | Ranbaxy Laboratories Limited | Pyrido-pyridimidine derivatives useful as antiinflammatory agents |
| US8044062B2 (en) * | 2005-10-07 | 2011-10-25 | Exelixis, Inc. | Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha |
| US8247408B2 (en) * | 2005-10-07 | 2012-08-21 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer |
| US20090142337A1 (en) * | 2006-05-08 | 2009-06-04 | Astex Therapeutics Limited | Pharmaceutical Combinations of Diazole Derivatives for Cancer Treatment |
| EP2032134B1 (en) | 2006-05-09 | 2015-06-24 | Genzyme Corporation | Methods of treating fatty liver disease comprising inhibiting glucosphingolipid synthesis |
| RU2009108006A (ru) * | 2006-09-08 | 2010-10-20 | Пфайзер Продактс Инк. (Us) | Синтез 2-(пиридин-2-иламино)-пиридо[2, 3-d]пиримидин-7-онов |
| GEP20115306B (me) | 2006-09-15 | 2011-10-10 | Pfizer Prod Inc | |
| WO2008150260A1 (en) * | 2007-06-06 | 2008-12-11 | Gpc Biotech, Inc. | 8-oxy-2-aminopyrido (2, 3-d) pyrimidin-7-one derivatives as kinase inhibitors and anticancer agents |
| BRPI0715566A2 (pt) * | 2006-10-16 | 2013-07-02 | Gpc Biotech Inc | composto, prà-droga, composiÇço farmacÊutica, uso de um composto, mÉtodo para inibir a proliferaÇço de cÉlulas e mÉtodo para sintetizar um composto |
| EP1914234A1 (en) | 2006-10-16 | 2008-04-23 | GPC Biotech Inc. | Pyrido[2,3-d]pyrimidines and their use as kinase inhibitors |
| JP2010509265A (ja) * | 2006-11-09 | 2010-03-25 | エフ.ホフマン−ラ ロシュ アーゲー | キナーゼ阻害剤としての置換6−フェニル−ピリド[2,3−d]ピリミジン−7−オン誘導体及びそれの使用方法 |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| KR20160085917A (ko) | 2007-10-05 | 2016-07-18 | 젠자임 코포레이션 | 세라마이드 유도체로 다낭성 신장질환을 치료하는 방법 |
| WO2009085185A1 (en) | 2007-12-19 | 2009-07-09 | Amgen Inc. | Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors |
| MX2010010975A (es) | 2008-04-07 | 2010-11-01 | Amgen Inc | Amino piridinas/pirimidinas gem-disustituidas y espirociclicas como inhibidores de ciclo celular. |
| EP2112150B1 (en) | 2008-04-22 | 2013-10-16 | Forma Therapeutics, Inc. | Improved raf inhibitors |
| PL2315756T3 (pl) | 2008-07-08 | 2015-02-27 | Incyte Holdings Corp | 1,2,5-oksadiazole jako inhibitory 2,3-dioksygenazy indoloaminy |
| WO2010014554A1 (en) | 2008-07-28 | 2010-02-04 | Genzyme Corporation | Glucosylceramide synthase inhibition for the treatment of collapsing glomerulopathy and other glomerular disease |
| KR101353857B1 (ko) * | 2008-08-22 | 2014-01-21 | 노파르티스 아게 | Cdk 억제제로서 피롤로피리미딘 화합물 |
| JP2012504646A (ja) * | 2008-10-01 | 2012-02-23 | ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | 選択的サイクリン依存性キナーゼ4/6阻害剤を用いた化学療法化合物に対する造血系の防護 |
| CN102231983A (zh) * | 2008-10-01 | 2011-11-02 | 北卡罗来纳大学查珀尔希尔分校 | 使用选择性细胞周期蛋白依赖性激酶4/6抑制剂对抗电离辐射的造血防护 |
| US8309593B2 (en) | 2008-10-03 | 2012-11-13 | Genzyme Corporation | 2-acylaminopropoanol-type glucosylceramide synthase inhibitors |
| PA8852901A1 (es) * | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| EA031116B1 (ru) | 2009-04-03 | 2018-11-30 | Ф. Хоффманн-Ля Рош Аг | КРИСТАЛЛИЧЕСКИЕ ПОЛИМОРФНЫЕ ФОРМЫ {3-[5-(4-ХЛОРФЕНИЛ)-1H-ПИРРОЛО[2,3-b]ПИРИДИН-3-КАРБОНИЛ]-2,4-ДИФТОРФЕНИЛ}АМИДА ПРОПАН-1-СУЛЬФОНОВОЙ КИСЛОТЫ |
| CA2761896A1 (en) * | 2009-05-13 | 2010-11-18 | The University Of North Carolina At Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
| EP2474540A4 (en) * | 2009-08-31 | 2013-03-13 | Nippon Chemiphar Co | GPR119 AGONIST |
| CA2776770A1 (en) * | 2009-10-09 | 2011-04-14 | Afraxis, Inc. | 8-ethyl-6-(aryl)pyrido[2,3-d]pyrimidin-7(8h)-ones for the treatment of cns disorders |
| UA105813C2 (uk) | 2009-11-06 | 2014-06-25 | Плексікон, Інк. | Сполуки-інгібітори кіназ та фармацевтична композиція (варіанти) |
| CA2784749C (en) | 2009-12-18 | 2017-12-12 | E. Premkumar Reddy | Substituted pyrido[2,3-d]pyrimidin-7(8h)-ones and therapeutic uses thereof |
| PH12012501361A1 (en) | 2009-12-31 | 2012-10-22 | Centro Nac De Investigaciones Oncologicas Cnio | Tricyclic compounds for use as kinase inhibitors |
| AU2011240735B2 (en) | 2010-04-13 | 2015-01-29 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (CDK4/6) inhibitor and an mTOR inhibitor for treating cancer |
| TWI619713B (zh) | 2010-04-21 | 2018-04-01 | 普雷辛肯公司 | 用於激酶調節的化合物和方法及其適應症 |
| US8680099B2 (en) * | 2010-06-10 | 2014-03-25 | Afraxis Holdings, Inc. | 6-(ethynyl)pyrido[2,3-D]pyrimidin-7(8H)-ones for the treatment of CNS disorders |
| EP2580320B1 (en) | 2010-06-14 | 2018-08-01 | The Scripps Research Institute | Reprogramming of cells to a new fate |
| DK2600719T3 (da) | 2010-08-05 | 2014-12-15 | Univ Temple | 2-substituerede 8-alkyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-carbonnitriler og anvendelser deraf |
| MX379532B (es) | 2010-10-25 | 2025-03-10 | G1 Therapeutics Inc | Inhibidores de cdk. |
| US8691830B2 (en) | 2010-10-25 | 2014-04-08 | G1 Therapeutics, Inc. | CDK inhibitors |
| WO2012068381A2 (en) | 2010-11-17 | 2012-05-24 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from schema through inhibition of the proliferative kisses cdk4 and cdk6 |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| WO2012098387A1 (en) | 2011-01-18 | 2012-07-26 | Centro Nacional De Investigaciones Oncológicas (Cnio) | 6, 7-ring-fused triazolo [4, 3 - b] pyridazine derivatives as pim inhibitors |
| PL2672967T3 (pl) | 2011-02-07 | 2019-04-30 | Plexxikon Inc | Związki i sposoby modulacji kinaz i wskazania ku temu |
| PT2688887E (pt) | 2011-03-23 | 2015-07-06 | Amgen Inc | Inibidores duais tricíclicos fusionados de cdk 4/6 e flt3 |
| AU2012262489A1 (en) | 2011-05-27 | 2013-04-04 | Icahn School Of Medicine At Mount Sinai | Substituted 2-benzylidene-2H-benzo[b][1,4]thiazin-3(4H)-ones, derivatives thereof, and therapeutic uses thereof |
| UA114906C2 (uk) * | 2012-03-14 | 2017-08-28 | Люпін Лімітед | Гетероциклільні сполуки як інгібітори мек |
| WO2013148748A1 (en) | 2012-03-29 | 2013-10-03 | Francis Xavier Tavares | Lactam kinase inhibitors |
| US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| US9611267B2 (en) | 2012-06-13 | 2017-04-04 | Incyte Holdings Corporation | Substituted tricyclic compounds as FGFR inhibitors |
| DK2872491T3 (da) | 2012-07-11 | 2021-08-09 | Blueprint Medicines Corp | Inhibitorer af fibroblastvækstfaktorreceptoren |
| AU2013296237B2 (en) | 2012-08-03 | 2019-05-16 | Foundation Medicine, Inc. | Human papilloma virus as predictor of cancer prognosis |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| BR112015003153A2 (pt) | 2012-08-17 | 2017-07-04 | Concert Pharmaceuticals Inc | baricitinib deuterado |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| US20140199728A1 (en) | 2013-01-14 | 2014-07-17 | Amgen Inc. | Methods of using cell-cycle inhibitors to modulate one or more properties of a cell culture |
| PL2958916T3 (pl) * | 2013-02-21 | 2019-01-31 | Pfizer Inc. | Stałe postacie selektywnego inhibitora CDK4/6 |
| US20140271460A1 (en) | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | Highly Active Anti-Neoplastic and Anti-Proliferative Agents |
| US9527857B2 (en) | 2013-03-15 | 2016-12-27 | GI Therapeutics, Inc. | HSPC-sparing treatments for RB-positive abnormal cellular proliferation |
| AU2014235462C1 (en) | 2013-03-15 | 2018-11-01 | Concert Pharmaceuticals, Inc. | Deuterated palbociclib |
| TWI649318B (zh) | 2013-04-19 | 2019-02-01 | 英塞特控股公司 | 作為fgfr抑制劑之雙環雜環 |
| WO2014183520A1 (zh) * | 2013-05-17 | 2014-11-20 | 上海恒瑞医药有限公司 | 吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| WO2014203129A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Combinations of benzopyran compounds, compositions and uses thereof |
| BR112016008849B8 (pt) | 2013-10-25 | 2022-09-06 | Blueprint Medicines Corp | Compostos ou sais farmaceuticamente aceitáveis dos mesmos, uso dos referidos compostos e composições farmacêuticas |
| EP4512480A3 (en) * | 2013-12-20 | 2025-05-07 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of cdk and erk inhibitors |
| CN105916848B (zh) | 2013-12-31 | 2018-01-09 | 山东轩竹医药科技有限公司 | 激酶抑制剂及其用途 |
| US9949976B2 (en) | 2013-12-31 | 2018-04-24 | Xuanzhu Pharma Co., Ltd. | Kinase inhibitor and use thereof |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| WO2015161283A1 (en) | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic lactams for use in hspc-sparing treatments for rb-positive abnormal cellular proliferation |
| ES2873959T3 (es) | 2014-05-28 | 2021-11-04 | Piramal Entpr Ltd | Combinación farmacéutica que comprende un inhibidor de CDK y un inhibidor de tiorredoxina reductasa para el tratamiento del cáncer |
| US9878994B2 (en) | 2014-07-24 | 2018-01-30 | Beta Pharma Inc. | 2-H-indazole derivatives as cyclin-dependent kinase (CDK) inhibitors and therapeutic uses thereof |
| WO2016015598A1 (en) | 2014-07-26 | 2016-02-04 | Sunshine Lake Pharma Co., Ltd. | 2-amino-pyrido[2,3-d]pyrimidin-7(8h)-one derivatives as cdk inhibitors and uses thereof |
| EP3174878A4 (en) * | 2014-07-31 | 2017-12-27 | Sun Pharmaceutical Industries Limited | A process for the preparation of palbociclib |
| AR101504A1 (es) * | 2014-08-11 | 2016-12-21 | Acerta Pharma Bv | Combinaciones terapéuticas de un inhibidor de la btk, un inhibidor de la pi3k, un inhibidor de la jak-2, y/o un inhibidor de la cdk4/6 |
| WO2016024249A1 (en) * | 2014-08-14 | 2016-02-18 | Sun Pharmaceutical Industries Limited | Crystalline forms of palbociclib |
| WO2016040858A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| CN105111201B (zh) * | 2014-10-16 | 2017-01-11 | 上海页岩科技有限公司 | 5-甲基-2-(吡啶-2-基氨基)-8H-吡啶并[2,3-d]嘧啶-7-酮化合物 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CN105622638B (zh) * | 2014-10-29 | 2018-10-02 | 广州必贝特医药技术有限公司 | 嘧啶或吡啶并吡啶酮类化合物及其制备方法和应用 |
| WO2016066420A1 (en) * | 2014-10-29 | 2016-05-06 | Sandoz Ag | Crystalline forms of palbociclib monohydrochloride |
| CN105616418A (zh) * | 2014-11-07 | 2016-06-01 | 江苏豪森药业集团有限公司 | 含有细胞周期蛋白抑制剂的药物制剂及其制备方法 |
| EP4183806A3 (en) | 2014-11-12 | 2023-08-02 | Seagen Inc. | Glycan-interacting compounds and methods of use |
| CN104496983B (zh) | 2014-11-26 | 2016-06-08 | 苏州明锐医药科技有限公司 | 一种帕博西尼的制备方法 |
| CN104447743B (zh) | 2014-11-26 | 2016-03-02 | 苏州明锐医药科技有限公司 | 帕博西尼的制备方法 |
| WO2016090257A1 (en) * | 2014-12-05 | 2016-06-09 | Crystal Pharmatech Inc. | Salts and crystalline forms of 6-acetyl-8-cyclopentyl-5-methyl-2((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d] pyrimidin-7(8h)-one (palbociclib) |
| WO2016092442A1 (en) * | 2014-12-08 | 2016-06-16 | Sun Pharmaceutical Industries Limited | Processes for the preparation of crystalline forms of palbociclib acetate |
| EP4205743A1 (en) | 2014-12-31 | 2023-07-05 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical composition and preparation method therefor |
| CN105732615B (zh) * | 2014-12-31 | 2018-05-01 | 山东轩竹医药科技有限公司 | Cdk激酶抑制剂 |
| CN104610254B (zh) * | 2015-01-26 | 2017-02-01 | 新发药业有限公司 | 一种帕博赛布的低成本制备方法 |
| CZ201589A3 (cs) | 2015-02-11 | 2016-08-24 | Zentiva, K.S. | Pevné formy soli Palbociclibu |
| TWI690533B (zh) | 2015-02-12 | 2020-04-11 | 南北兄弟藥業投資有限公司 | Cdk類小分子抑制劑的化合物及其用途 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| AU2016219822B2 (en) | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| AR104068A1 (es) | 2015-03-26 | 2017-06-21 | Hoffmann La Roche | Combinaciones de un compuesto inhibidor de fosfoinosítido 3-cinasa y un compuesto inhibidor de cdk4/6 para el tratamiento del cáncer |
| WO2016156070A1 (en) | 2015-04-02 | 2016-10-06 | Sandoz Ag | Modified particles of palbociclib |
| EP3078663A1 (en) | 2015-04-09 | 2016-10-12 | Sandoz Ag | Modified particles of palbociclib |
| CN106795159B (zh) * | 2015-04-22 | 2018-12-28 | 江苏恒瑞医药股份有限公司 | 一种周期素依赖性蛋白激酶抑制剂的结晶形式及其制备方法 |
| TWI696617B (zh) * | 2015-04-28 | 2020-06-21 | 大陸商上海復尚慧創醫藥研究有限公司 | 特定蛋白質激酶抑制劑 |
| WO2016194831A1 (ja) * | 2015-05-29 | 2016-12-08 | 帝人ファーマ株式会社 | ピリド[3,4-d]ピリミジン誘導体及びその薬学的に許容される塩 |
| HUE047477T2 (hu) | 2015-06-04 | 2020-04-28 | Pfizer | Palbociclib szilárd dózisformái |
| CN104892604B (zh) * | 2015-06-19 | 2016-08-24 | 北京康立生医药技术开发有限公司 | 一种cdk4抑制剂的合成方法 |
| CN106699785A (zh) * | 2015-07-13 | 2017-05-24 | 南开大学 | 作为CDK4/6抑制剂的2-(N-氧化吡啶-2基氨基)-吡啶并[2,3-d]嘧啶-7-酮类化合物 |
| US10526326B2 (en) | 2015-08-05 | 2020-01-07 | Ratiopharm Gmbh | Crystalline form and acetic acid adducts of palbociclib |
| CN105085517B (zh) * | 2015-08-06 | 2016-11-23 | 天津华洛康生物科技有限公司 | 一种结晶型帕博西尼游离碱水合物及其制备方法 |
| CN105130986B (zh) * | 2015-09-30 | 2017-07-18 | 广州科擎新药开发有限公司 | 嘧啶或吡啶并吡啶酮类化合物及其应用 |
| HU230962B1 (hu) | 2015-10-28 | 2019-06-28 | Egis Gyógyszergyár Zrt. | Palbociclib sók |
| CN106632311B (zh) | 2015-11-02 | 2021-05-18 | 上海科胜药物研发有限公司 | 一种帕博西尼晶型a和晶型b的制备方法 |
| CN108463248B (zh) | 2015-11-12 | 2022-10-21 | 西雅图基因公司 | 聚糖相互作用化合物及使用方法 |
| CN105418603A (zh) * | 2015-11-17 | 2016-03-23 | 重庆莱美药业股份有限公司 | 一种高纯度帕布昔利布及其反应中间体的制备方法 |
| CN106810536A (zh) * | 2015-11-30 | 2017-06-09 | 甘李药业股份有限公司 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
| JP6951767B2 (ja) * | 2015-12-13 | 2021-10-20 | ハンジョウ イノゲート ファーマ カンパニー リミテッドHangzhou Innogate Pharma Co.,Ltd. | 抗癌薬として使用される複素環式化合物 |
| EP3398947B1 (en) | 2015-12-31 | 2024-08-28 | Shanghai Pharmaceuticals Holding Co., Ltd. | Nitrogen-containing fused heterocyclic compound, as well as preparation method, intermediate, composition and application thereof |
| CN105418609B (zh) * | 2015-12-31 | 2017-06-23 | 山东大学 | 4‑(1,2,3‑三氮唑取代苯胺基)‑吡啶骈嘧啶酮衍生物及其制备方法与应用 |
| CN106967061A (zh) * | 2016-01-13 | 2017-07-21 | 常州方楠医药技术有限公司 | 帕博西林的盐、晶型及其制备方法 |
| WO2017130219A1 (en) | 2016-01-25 | 2017-08-03 | Mylan Laboratories Limited | Amorphous solid dispersion of palbociclib |
| WO2017145054A1 (en) | 2016-02-24 | 2017-08-31 | Lupin Limited | Modified particles of crystalline palbociclib free base and process for the preparation thereof |
| WO2017161253A1 (en) | 2016-03-18 | 2017-09-21 | Tufts Medical Center | Compositions and methods for treating and preventing metabolic disorders |
| US10449195B2 (en) | 2016-03-29 | 2019-10-22 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical formulation of palbociclib and a preparation method thereof |
| CN107266421B (zh) * | 2016-04-08 | 2020-12-04 | 正大天晴药业集团股份有限公司 | 取代的苯并咪唑类衍生物 |
| CN107286180B (zh) * | 2016-04-11 | 2019-07-02 | 上海勋和医药科技有限公司 | 杂代吡啶并嘧啶酮衍生物作为cdk抑制剂及其应用 |
| CA3018434A1 (en) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
| CN106336411B (zh) * | 2016-04-27 | 2018-03-06 | 上海医药集团股份有限公司 | Cdk4/6抑制剂帕博西尼高纯度原料药的制备工艺及用途 |
| CN105949189B (zh) * | 2016-06-05 | 2017-09-22 | 童明琼 | 一种用于治疗乳腺癌的帕博西尼的制备方法 |
| EA201990187A1 (ru) | 2016-07-01 | 2019-07-31 | Г1 Терапьютикс, Инк. | Антипролиферационные средства на основе пиримидина |
| WO2018005533A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Antiproliferative pyrimidine-based compounds |
| WO2018005863A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based compounds for the treatment of cancer |
| US10807978B2 (en) | 2016-07-04 | 2020-10-20 | Dr. Reddy's Laboratories Limited | Process for preparation of palbociclib |
| EP3481825A1 (en) | 2016-07-07 | 2019-05-15 | Plantex Ltd. | Solid state forms of palbociclib dimesylate |
| JP6563623B1 (ja) | 2016-08-15 | 2019-08-21 | ファイザー・インク | ピリドピリミジノンcdk2/4/6阻害剤 |
| CA3034875C (en) | 2016-08-23 | 2024-05-28 | Eisai R&D Management Co., Ltd. | Combination therapies for the treatment of hepatocellular carcinoma |
| WO2018049233A1 (en) | 2016-09-08 | 2018-03-15 | Nicolas Stransky | Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors |
| WO2018065999A1 (en) | 2016-10-07 | 2018-04-12 | Mylan Laboratories Limited | Novel polymorph of an intermediate for palbociclib synthesis |
| WO2018073574A1 (en) | 2016-10-20 | 2018-04-26 | Cipla Limited | Polymorphic forms of palbociclib |
| EP3804724B1 (en) | 2016-10-20 | 2022-12-07 | Pfizer Inc. | Cdk inhibitors for treating pah |
| CN106565707B (zh) * | 2016-11-03 | 2019-01-04 | 杭州科巢生物科技有限公司 | 帕博西尼新合成方法 |
| EP3538148A1 (en) | 2016-11-08 | 2019-09-18 | Dana-Farber Cancer Institute | Compositions and methods of modulating anti-tumor immunity |
| US20190275049A1 (en) | 2016-11-16 | 2019-09-12 | Pfizer Inc. | Combination of an EGFR T790M Inhibitor and a CDK Inhibitor for the Treatment of Non-Small Cell Lung Cancer |
| WO2018094143A1 (en) | 2016-11-17 | 2018-05-24 | Siamab Therapeutics, Inc. | Glycan-interacting compounds and methods of use |
| MY199852A (en) | 2016-11-28 | 2023-11-25 | Teijin Pharma Ltd | Crystal of pyrido[3,4-d]pyrimidine derivative or solvate thereof |
| SI3546458T1 (sl) | 2016-11-28 | 2021-03-31 | Teijin Pharma Limited | Derivati ((piridin-2-il)-amino)pirido(3,4-d)pirimidina in ((piridazin-3-il)amino)pirido(3,4-d)pirimidina kot zaviralci CDK4/6 za zdravljenje npr. revmatoidnega artritisa, arterioskleroze, pljučne fibroze, možganske kapi ali raka |
| KR102513448B1 (ko) | 2016-12-16 | 2023-03-23 | 씨스톤 파마슈티컬즈 | Cdk4/6 억제제 |
| TWI823845B (zh) | 2017-01-06 | 2023-12-01 | 美商G1治療公司 | 用於治療癌症的組合療法 |
| CN108191857B (zh) * | 2017-01-24 | 2020-10-23 | 晟科药业(江苏)有限公司 | 6-取代的吡啶并[2,3-d]嘧啶类化合物作为蛋白激酶抑制剂 |
| US10729692B2 (en) * | 2017-02-26 | 2020-08-04 | Institute For Cancer Research | Dual inhibition of CDK and HSP90 destabilize HIF1alpha and synergistically induces cancer cell death |
| AU2018229148B2 (en) * | 2017-03-03 | 2022-08-04 | Auckland Uniservices Limited | FGFR kinase inhibitors and pharmaceutical uses |
| WO2018160909A1 (en) | 2017-03-03 | 2018-09-07 | Siamab Therapeutics, Inc. | Glycan-interacting compounds and methods of use |
| MX2019010981A (es) | 2017-03-16 | 2020-09-07 | Eisai R&D Man Co Ltd | Terapias de combinacion para el tratamiento de cancer de mama. |
| CN108658855A (zh) * | 2017-03-28 | 2018-10-16 | 中国海洋大学 | 一种含氮双环化合物及其制备方法和用途 |
| CN108658854A (zh) * | 2017-03-28 | 2018-10-16 | 中国海洋大学 | 一种生物碱化合物及其制备方法和作为海洋防污剂的应用 |
| US11913075B2 (en) | 2017-04-01 | 2024-02-27 | The Broad Institute, Inc. | Methods and compositions for detecting and modulating an immunotherapy resistance gene signature in cancer |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| MX2019015177A (es) | 2017-06-16 | 2020-02-07 | Beta Pharma Inc | Formulaciones farmaceuticas de n-(2-(2-(dimetilamino)etoxi)-4-meto xi-5((4-(1-metil-1h-indol-3-il)pirimidin-2-il)amino)fenil)acrilam ida y las sales de ellas. |
| EP4455146A3 (en) | 2017-06-29 | 2025-01-01 | G1 Therapeutics, Inc. | Morphic forms of git38 and methods of manufacture thereof |
| EA036060B1 (ru) * | 2017-07-17 | 2020-09-21 | Пфайзер Инк. | Пиридопиримидиноновые ингибиторы cdk2/4/6 |
| EA202090402A1 (ru) | 2017-07-28 | 2020-05-19 | Синтон Б.В. | Фармацевтическая композиция, содержащая пальбоциклиб |
| CN109384767B (zh) * | 2017-08-08 | 2020-05-05 | 江苏恒瑞医药股份有限公司 | 一种吡啶并嘧啶类衍生物的制备方法及其中间体 |
| ES3049655T3 (en) | 2017-08-31 | 2025-12-17 | Novartis Ag | Methods of selecting a treatment for breast cancer patients |
| CN107488175A (zh) * | 2017-09-04 | 2017-12-19 | 上海微巨实业有限公司 | 一种帕博西林关键中间体的制备方法 |
| US12043870B2 (en) | 2017-10-02 | 2024-07-23 | The Broad Institute, Inc. | Methods and compositions for detecting and modulating an immunotherapy resistance gene signature in cancer |
| MX2020006587A (es) | 2017-12-22 | 2020-12-10 | Ravenna Pharmaceuticals Inc | Derivados de aminopiridina como inhibidores de fosfatidilinositol fosfato cinasa. |
| CN108586452A (zh) * | 2018-01-12 | 2018-09-28 | 重庆市碚圣医药科技股份有限公司 | 一种帕博西尼中间体的合成方法 |
| WO2019148161A1 (en) | 2018-01-29 | 2019-08-01 | Beta Pharma, Inc. | 2h-indazole derivatives as cdk4 and cdk6 inhibitors and therapeutic uses thereof |
| CN108218861B (zh) * | 2018-02-05 | 2019-07-23 | 黑龙江中医药大学 | 一种预防和治疗糖尿病的药物及其制备方法 |
| WO2019157020A1 (en) | 2018-02-06 | 2019-08-15 | The Board Of Trustees Of The University Of Illinois | Substituted benzothiophene analogs as selective estrogen receptor degraders |
| JP2021514975A (ja) | 2018-02-27 | 2021-06-17 | ファイザー・インク | サイクリン依存性キナーゼ阻害剤およびbet−ブロモドメイン阻害剤の組合せ |
| US20190292188A1 (en) | 2018-02-27 | 2019-09-26 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors |
| TW201946630A (zh) | 2018-05-04 | 2019-12-16 | 美商英塞特公司 | Fgfr抑制劑之鹽 |
| ES2991427T3 (es) | 2018-05-04 | 2024-12-03 | Incyte Corp | Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas |
| EP4309656A3 (en) | 2018-05-14 | 2024-02-28 | Pfizer Inc. | Oral solution formulation |
| MA52940A (fr) | 2018-05-18 | 2021-04-28 | Incyte Corp | Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b |
| SI3802529T1 (sl) | 2018-05-24 | 2024-03-29 | Synthon B.V. | Postopek za izdelavo palbocikliba |
| CN113166153B (zh) | 2018-07-05 | 2024-11-01 | 因赛特公司 | 作为a2a/a2b抑制剂的稠合吡嗪衍生物 |
| CN117281814A (zh) | 2018-07-23 | 2023-12-26 | 豪夫迈·罗氏有限公司 | 用pi3k抑制剂gdc-0077治疗癌症的方法 |
| CA3107750A1 (en) | 2018-07-27 | 2020-01-30 | California Institute Of Technology | Cdk inhibitors and uses thereof |
| CN120817904A (zh) | 2018-08-24 | 2025-10-21 | 法码科思莫斯有限公司 | 1,4-二氮杂螺[5.5]十一烷-3-酮改进的合成 |
| JP6952747B2 (ja) | 2018-09-18 | 2021-10-20 | ファイザー・インク | がん処置のためのTGFβ阻害剤およびCDK阻害剤の組合せ |
| TW202027736A (zh) | 2018-10-08 | 2020-08-01 | 瑞士商赫孚孟拉羅股份公司 | 用PI3Kα抑制劑及二甲雙胍治療癌症之方法 |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| WO2020114519A1 (zh) * | 2018-12-07 | 2020-06-11 | 杭州英创医药科技有限公司 | 作为cdk-hdac双通路抑制剂的杂环化合物 |
| US20220040324A1 (en) | 2018-12-21 | 2022-02-10 | Daiichi Sankyo Company, Limited | Combination of antibody-drug conjugate and kinase inhibitor |
| CA3124569A1 (en) | 2018-12-28 | 2020-07-02 | Spv Therapeutics Inc. | Cyclin-dependent kinase inhibitors |
| WO2020140055A1 (en) * | 2018-12-28 | 2020-07-02 | Spv Therapeutics Inc. | Cyclin-dependent kinase inhibitors |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| WO2020157709A1 (en) | 2019-02-01 | 2020-08-06 | Pfizer Inc. | Combination of a cdk inhibitor and a pim inhibitor |
| US11384083B2 (en) | 2019-02-15 | 2022-07-12 | Incyte Corporation | Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors |
| MA54947A (fr) * | 2019-02-15 | 2021-12-22 | Incyte Corp | Biomarqueurs de kinase 2 dépendant de la cycline et leurs utilisations |
| US11472791B2 (en) | 2019-03-05 | 2022-10-18 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| US20220154282A1 (en) | 2019-03-12 | 2022-05-19 | The Broad Institute, Inc. | Detection means, compositions and methods for modulating synovial sarcoma cells |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| EP3976043A1 (en) | 2019-05-24 | 2022-04-06 | Pfizer Inc. | Combination therapies using cdk inhibitors |
| CN113874036A (zh) | 2019-05-24 | 2021-12-31 | 辉瑞公司 | 使用cdk抑制剂的联合治疗 |
| CN112010844B (zh) * | 2019-05-31 | 2023-07-25 | 中国药科大学 | N-(嘧啶-2-基)香豆素-7-胺衍生物作为蛋白激酶抑制剂的制法和应用 |
| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| CN112094272A (zh) | 2019-06-18 | 2020-12-18 | 北京睿熙生物科技有限公司 | Cdk激酶抑制剂 |
| TW202114685A (zh) * | 2019-06-20 | 2021-04-16 | 大陸商江蘇恒瑞醫藥股份有限公司 | 藥物組合物以及其製備方法 |
| CN110143948B (zh) * | 2019-06-21 | 2021-05-14 | 上海博悦生物科技有限公司 | Cdk4/6抑制剂、其药物组合物、制备方法及应用 |
| JP7616794B2 (ja) | 2019-07-07 | 2025-01-17 | オレマ ファーマシューティカルズ インク. | エストロゲン受容体アンタゴニストのレジメン |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021022172A1 (en) | 2019-08-01 | 2021-02-04 | Incyte Corporation | A dosing regimen for an ido inhibitor |
| MX2022001940A (es) | 2019-08-14 | 2022-05-10 | Incyte Corp | Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2. |
| IL290789B2 (en) | 2019-08-26 | 2025-09-01 | Arvinas Operations Inc | Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CN119930610A (zh) | 2019-10-11 | 2025-05-06 | 因赛特公司 | 作为cdk2抑制剂的双环胺 |
| GEAP202415945A (en) | 2019-10-14 | 2024-04-25 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CN112759589B (zh) * | 2019-11-01 | 2022-04-08 | 暨南大学 | 嘧啶并吡啶酮类化合物及其应用 |
| US11697648B2 (en) | 2019-11-26 | 2023-07-11 | Theravance Biopharma R&D Ip, Llc | Fused pyrimidine pyridinone compounds as JAK inhibitors |
| IL293347A (en) | 2019-12-03 | 2022-07-01 | Genentech Inc | Combined therapies for the treatment of breast cancer |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| IL293940B1 (en) | 2019-12-16 | 2026-01-01 | Lunella Biotech Inc | Selective cancer drugs cdk4/6 inhibitors |
| US12319690B2 (en) * | 2019-12-16 | 2025-06-03 | Lunella Biotech, Inc. | Selective CDK 4/6 inhibitor cancer therapeutics |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021176349A1 (en) | 2020-03-05 | 2021-09-10 | Pfizer Inc. | Combination of an anaplastic lymphoma kinase inhibitor and a cyclin dependent kinase inhibitor |
| EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| WO2021183994A1 (en) * | 2020-03-13 | 2021-09-16 | Prosenestar Llc | Pyrido[2,3-d]pyrimidin-7(8h)-ones as cdk inhibitors |
| CN114245753A (zh) * | 2020-03-27 | 2022-03-25 | 江苏康宁杰瑞生物制药有限公司 | 用于肿瘤治疗的抗her2抗体与cdk抑制剂的组合 |
| JP2021167301A (ja) | 2020-04-08 | 2021-10-21 | ファイザー・インク | Cdk2阻害剤に対する腫瘍適応を抑制するためのcdk4/6およびcdk2阻害剤による同時処置 |
| IL297165A (en) | 2020-04-16 | 2022-12-01 | Incyte Corp | Soysag tricyclic CRS inhibitors |
| US11739102B2 (en) | 2020-05-13 | 2023-08-29 | Incyte Corporation | Fused pyrimidine compounds as KRAS inhibitors |
| EP4652997A3 (en) | 2020-05-19 | 2026-03-04 | Pharmacosmos Holding A/s | Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders |
| EP4157847A4 (en) * | 2020-05-28 | 2024-06-19 | University of Washington | Drug-like molecules and methods for the therapeutic targeting of viral rna structures |
| US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
| CN113880809B (zh) | 2020-07-03 | 2022-10-18 | 盛世泰科生物医药技术(苏州)有限公司 | 一种嘧啶类衍生物及其制备方法和应用 |
| EP4667055A3 (en) | 2020-07-15 | 2026-02-25 | Pfizer Inc. | Kat6 inhibitor methods and combinations for cancer treatment |
| US20230321042A1 (en) | 2020-07-20 | 2023-10-12 | Pfizer Inc. | Combination therapy |
| WO2022047093A1 (en) | 2020-08-28 | 2022-03-03 | Incyte Corporation | Vinyl imidazole compounds as inhibitors of kras |
| CN114246841B (zh) * | 2020-09-24 | 2024-02-02 | 南京济群医药科技股份有限公司 | 一种羟乙磺酸哌柏西利的组合物及药物 |
| CN114306245A (zh) | 2020-09-29 | 2022-04-12 | 深圳市药欣生物科技有限公司 | 无定形固体分散体的药物组合物及其制备方法 |
| US11767320B2 (en) | 2020-10-02 | 2023-09-26 | Incyte Corporation | Bicyclic dione compounds as inhibitors of KRAS |
| WO2022091001A1 (en) | 2020-10-29 | 2022-05-05 | Pfizer Ireland Pharmaceuticals | Process for preparation of palbociclib |
| WO2022123419A1 (en) | 2020-12-08 | 2022-06-16 | Pfizer Inc. | Treatment of luminal subtypes of hr-positive, her2-negative early breast cancer with palbociclib |
| CN112569361B (zh) * | 2020-12-30 | 2023-01-10 | 扬子江药业集团上海海尼药业有限公司 | 一种哌柏西利干混悬组合物及其制备方法 |
| WO2022155941A1 (en) | 2021-01-25 | 2022-07-28 | Qilu Regor Therapeutics Inc. | Cdk2 inhibitors |
| WO2022162122A1 (en) | 2021-01-29 | 2022-08-04 | Biotx.Ai Gmbh | Genetically verified netosis inhibitor for use in the treatment of a sars-cov2 infection |
| WO2022206888A1 (en) | 2021-03-31 | 2022-10-06 | Qilu Regor Therapeutics Inc. | Cdk2 inhibitors and use thereof |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| AR126101A1 (es) | 2021-06-09 | 2023-09-13 | Incyte Corp | Heterociclos tricíclicos como inhibidores de fgfr |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022258023A1 (zh) * | 2021-06-09 | 2022-12-15 | 郑州同源康医药有限公司 | 用作cdk激酶抑制剂的化合物及其应用 |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| CA3224674A1 (en) | 2021-07-07 | 2023-01-12 | Pei Gan | Tricyclic compounds as inhibitors of kras |
| EP4370515A1 (en) | 2021-07-14 | 2024-05-22 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| EP4370126A4 (en) | 2021-07-16 | 2025-05-28 | Dana-Farber Cancer Institute, Inc. | Small molecule cyclin dependent kinase 4/6 (cdk4/6) and ikzf2 (helios) degraders and methods of use thereof |
| JP2024529430A (ja) | 2021-07-26 | 2024-08-06 | セルキュイティー インコーポレイテッド | がんの処置における使用のための1-(4-{[4-(ジメチルアミノ)ピペリジン-1-イル]カルボニル}フェニル)-3-[4-(4,6-ジモルホリン-4-イル-1,3,5-トリアジン-2-イル)フェニル]尿素(ゲダトリシブ)およびその組合せ |
| CA3229855A1 (en) | 2021-08-31 | 2023-03-09 | Incyte Corporation | Naphthyridine compounds as inhibitors of kras |
| CN113683612B (zh) * | 2021-09-07 | 2022-06-17 | 山东铂源药业股份有限公司 | 一种帕布昔利布的制备方法 |
| CN118119393A (zh) * | 2021-09-14 | 2024-05-31 | 甘李药业股份有限公司 | 一种cdk4/6抑制剂的医药用途 |
| US12030883B2 (en) | 2021-09-21 | 2024-07-09 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of KRAS |
| WO2023056421A1 (en) | 2021-10-01 | 2023-04-06 | Incyte Corporation | Pyrazoloquinoline kras inhibitors |
| IL312114A (en) | 2021-10-14 | 2024-06-01 | Incyte Corp | Quinoline compounds as Kras inhibitors |
| JP2024542248A (ja) | 2021-11-22 | 2024-11-13 | インサイト・コーポレイション | Fgfr阻害剤とkras阻害剤を含む併用療法 |
| US20230203010A1 (en) | 2021-12-03 | 2023-06-29 | Incyte Corporation | Bicyclic amine cdk12 inhibitors |
| AU2022408062B2 (en) | 2021-12-10 | 2025-08-14 | Eli Lilly And Company | Cdk4 and 6 inhibitor in combination with fulvestrant for the treatment of hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced or metastatic breast cancer in patients previously treated with a cdk4 and 6 inhibitor |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
| US20250049802A1 (en) | 2021-12-14 | 2025-02-13 | Pfizer Inc. | Combination therapies and uses for treating cancer |
| WO2023114264A1 (en) | 2021-12-15 | 2023-06-22 | Eli Lilly And Company | Combination for treatment of high-risk metastatic hormone-sensitive prostate cancer |
| TW202340215A (zh) | 2021-12-22 | 2023-10-16 | 美商英塞特公司 | Fgfr抑制劑之鹽及固體形式以及其製備方法 |
| WO2023116884A1 (en) | 2021-12-24 | 2023-06-29 | Qilu Regor Therapeutics Inc. | Cdk2 inhibitors and use thereof |
| WO2023168686A1 (en) | 2022-03-11 | 2023-09-14 | Qilu Regor Therapeutics Inc. | Substituted cyclopentanes as cdk2 inhibitors |
| CN114456180B (zh) * | 2022-02-18 | 2023-07-25 | 贵州大学 | 用于治疗和/或预防恶性肿瘤的化合物及药物制剂和应用 |
| CR20240408A (es) | 2022-03-07 | 2024-11-22 | Incyte Corp | Formas sólidas, sales y procesos de preparación de un inhibidor de cdk2. |
| HU231594B1 (hu) * | 2022-05-10 | 2025-03-28 | Egis Gyógyszergyár Zrt. | Palbociclibet és letrozolt tartalmazó gyógyszerkészítmény |
| WO2023250430A1 (en) | 2022-06-22 | 2023-12-28 | Incyte Corporation | Bicyclic amine cdk12 inhibitors |
| EP4302755B1 (en) | 2022-07-07 | 2025-08-20 | Lotus Pharmaceutical Co., Ltd. | Palbociclib formulation containing an amino acid |
| EP4302832A1 (en) | 2022-07-07 | 2024-01-10 | Lotus Pharmaceutical Co., Ltd. | Palbociclib formulation containing glucono delta lactone |
| WO2024015731A1 (en) | 2022-07-11 | 2024-01-18 | Incyte Corporation | Fused tricyclic compounds as inhibitors of kras g12v mutants |
| CN117430597A (zh) * | 2022-07-14 | 2024-01-23 | 浙江同源康医药股份有限公司 | 用作cdk4激酶抑制剂的化合物及其应用 |
| CN119604288A (zh) | 2022-07-29 | 2025-03-11 | 辉瑞大药厂 | 用于治疗癌症的包含kat6抑制剂的给药方案 |
| IL319242A (en) | 2022-08-31 | 2025-04-01 | Arvinas Operations Inc | Estrogen Receptor Blocker Dosage Regimen |
| CN120456897A (zh) | 2022-11-02 | 2025-08-08 | 佩特拉制药公司 | 用于治疗疾病的磷酸肌醇3-激酶(pi3k)变构色原酮抑制剂 |
| CN120187416A (zh) | 2022-11-11 | 2025-06-20 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症的组合疗法 |
| CN120344527A (zh) * | 2022-12-16 | 2025-07-18 | 上海岸阔医药科技有限公司 | 化合物及其用途 |
| WO2024132652A1 (en) | 2022-12-22 | 2024-06-27 | Synthon B.V. | Pharmaceutical composition comprising palbociclib |
| WO2024133726A1 (en) | 2022-12-22 | 2024-06-27 | Synthon B.V. | Pharmaceutical composition comprising palbociclib |
| CN120981721A (zh) | 2023-03-30 | 2025-11-18 | 辉瑞大药厂 | Kat6a作为用kat6a抑制剂治疗的预测性生物标志物和相关治疗方法 |
| WO2024201340A1 (en) | 2023-03-30 | 2024-10-03 | Pfizer Inc. | Kat6a as a predictive biomarker for treatment of breast cancer with a cdk4 inhibitor and an antiestrogen and methods of treatment thereof |
| WO2024220532A1 (en) | 2023-04-18 | 2024-10-24 | Incyte Corporation | Pyrrolidine kras inhibitors |
| EP4698542A1 (en) | 2023-04-18 | 2026-02-25 | Incyte Corporation | 2-azabicyclo[2.2.1]heptane kras inhibitors |
| WO2024231275A1 (en) | 2023-05-05 | 2024-11-14 | Astrazeneca Ab | Combination of capivasertib, a cdk4/6 inhibitor and fulvestrant for use in the treatment of breast cancer |
| WO2024235844A1 (en) | 2023-05-12 | 2024-11-21 | Institut National de la Santé et de la Recherche Médicale | Methods of preventing on-target genotoxicity induced by nucleases |
| WO2024254245A1 (en) | 2023-06-09 | 2024-12-12 | Incyte Corporation | Bicyclic amines as cdk2 inhibitors |
| WO2025051337A1 (en) | 2023-09-06 | 2025-03-13 | Afyx Development A/S | Compositions and methods for treating and preventing oral cancer |
| WO2025096738A1 (en) | 2023-11-01 | 2025-05-08 | Incyte Corporation | Kras inhibitors |
| US20250177414A1 (en) | 2023-12-04 | 2025-06-05 | Genentech, Inc. | Combination therapies for treatment of breast cancer |
| US20250195536A1 (en) | 2023-12-13 | 2025-06-19 | Incyte Corporation | Bicyclooctane kras inhibitors |
| WO2025202854A1 (en) | 2024-03-27 | 2025-10-02 | Pfizer Inc. | Cdk4 inhibitors and combinations with cdk2 inhibitors or further agents for use in the treatment of cancer |
| WO2026024674A1 (en) | 2024-07-22 | 2026-01-29 | Genesis Therapeutics, Inc. | Methods of treating skp2-associated cancers |
| WO2026025013A2 (en) | 2024-07-26 | 2026-01-29 | Pfizer Inc. | Combination therapy using cdk4 inhibitors for cancer treatments |
| US20260053814A1 (en) | 2024-08-21 | 2026-02-26 | Celcuity Inc. | Treatment regimens for gedatolisib in hormonally-driven disorders |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ194045A (en) | 1979-06-14 | 1984-09-28 | Wellcome Found | 6-(2,5-or 3,4-dialkoxybenzyl)-2,4-diamino-5-methylpyrido(2,3-d)pyrimidines |
| US4959474A (en) | 1979-06-14 | 1990-09-25 | Burroughs Wellcome Co. | Dialkoxy pyridopyrimidine compounds |
| ZA803539B (en) | 1979-06-14 | 1982-01-27 | Wellcome Found | Alkoxybenzylrimidines method for their preparation formulation thereof and their use in medicine |
| EP0278686A1 (en) | 1987-02-07 | 1988-08-17 | The Wellcome Foundation Limited | Pyridopyrimidines methods for their preparation and pharmaceutical formulations thereof |
| AU658646B2 (en) | 1991-05-10 | 1995-04-27 | Rhone-Poulenc Rorer International (Holdings) Inc. | Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| US5426110A (en) | 1993-10-06 | 1995-06-20 | Eli Lilly And Company | Pyrimidinyl-glutamic acid derivatives |
| GB9325217D0 (en) | 1993-12-09 | 1994-02-09 | Zeneca Ltd | Pyrimidine derivatives |
| RU2191188C2 (ru) | 1994-11-14 | 2002-10-20 | Варнер-Ламберт Компани | Производные 6-арилпиридо[2,3-d]-пиримидины и -нафтиридины, фармацевтическая композиция, обладающая ингибирующим действием клеточной пролиферации, вызываемой протеиновой тирозинкиназой, и способ ингибирования клеточной пролиферации |
| US5801183A (en) | 1995-01-27 | 1998-09-01 | State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University And The University Of Oregon | Aza and aza (N-oxy) analogs of glycine/NMDA receptor antagonists |
| US5620981A (en) | 1995-05-03 | 1997-04-15 | Warner-Lambert Company | Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation |
| IL117923A (en) | 1995-05-03 | 2000-06-01 | Warner Lambert Co | Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds |
| JP2001511764A (ja) | 1996-04-12 | 2001-08-14 | 住友製薬株式会社 | ピペリジニルピリミジン誘導体 |
| US5948786A (en) | 1996-04-12 | 1999-09-07 | Sumitomo Pharmaceuticals Company, Limited | Piperidinylpyrimidine derivatives |
| DE69839338T2 (de) * | 1997-02-05 | 2008-07-10 | Warner-Lambert Company Llc | Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation |
| US6498163B1 (en) * | 1997-02-05 | 2002-12-24 | Warner-Lambert Company | Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation |
| US6569878B1 (en) | 1997-10-27 | 2003-05-27 | Agouron Pharmaceuticals Inc. | Substituted 4-amino-thiazol-2-yl compounds as cyclin-dependent kinase inhibitors |
| EE200000706A (et) * | 1998-05-26 | 2002-06-17 | Warner-Lambert Company | Bitsüklilised pürimidiinid ja bitsüklilised 3,4-dihüdropürimidiinid kui rakkude proliferatsiooni inhibiitorid |
| DE69933680T2 (de) | 1998-08-29 | 2007-08-23 | Astrazeneca Ab | Pyrimidine verbindungen |
| US6958333B1 (en) | 1999-07-26 | 2005-10-25 | Banyu Pharmaceutical Co., Ltd. | Biarylurea derivatives |
| EA005287B1 (ru) | 1999-09-15 | 2004-12-30 | Уорнер-Ламберт Компани | Птеридиноны в качестве ингибиторов киназ |
| CN1433417A (zh) * | 2000-01-27 | 2003-07-30 | 沃尼尔·朗伯公司 | 用于治疗神经变性疾病的吡啶并嘧啶酮衍生物 |
| YU66502A (sh) * | 2000-03-06 | 2005-09-19 | Warner-Lambert Company | 5-alkilpirido(2,3-d)pirimidini, inhibitori tirozinkinaza |
| ES2311532T3 (es) | 2000-08-04 | 2009-02-16 | Warner-Lambert Company Llc | 2-(4-pirdil)amino-6-dialcoxifenil-pirido(2.3-d)pirimidin-7-onas. |
| ES2230337T3 (es) | 2000-09-01 | 2005-05-01 | Glaxo Group Limited | Derivados de oxindol. |
| GB0101686D0 (en) | 2001-01-23 | 2001-03-07 | Cancer Res Campaign Tech | Cyclin dependent kinase inhibitors |
| CZ20032416A3 (cs) * | 2001-02-12 | 2004-07-14 | F. Hoffmann-La Roche Ag | 6-Substituované pyridopyrimidiny |
| DE60210819T2 (de) | 2001-12-17 | 2007-04-19 | Smithkline Beecham Corp. | Pyrazolopyridazinderivate |
| DE60303009T2 (de) | 2002-01-22 | 2006-07-13 | Warner-Lambert Co. Llc | 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-one |
| US7189712B2 (en) | 2002-10-10 | 2007-03-13 | Smithkline Beecham Corporation | 1,3-Oxazole compounds for the treatment of cancer |
| EP1567112B1 (en) | 2002-11-22 | 2008-10-15 | Smithkline Beecham Corporation | THIAZOLIDIN-4-ONES FOR INHIBITING hYAK3 PROTEINS |
| WO2004063195A1 (en) * | 2003-01-03 | 2004-07-29 | Sloan-Kettering Institute For Cancer Research | Pyridopyrimidine kinase inhibitors |
| JP2006516561A (ja) | 2003-01-17 | 2006-07-06 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | 細胞増殖の阻害剤としての2−アミノピリジン置換ヘテロ環類 |
| DE602004016964D1 (de) | 2003-02-27 | 2008-11-20 | Smithkline Beecham Corp | Neue verbindungen |
| JP4053073B2 (ja) | 2003-07-11 | 2008-02-27 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | 選択的cdk4阻害剤のイセチオン酸塩 |
| RU2009108006A (ru) | 2006-09-08 | 2010-10-20 | Пфайзер Продактс Инк. (Us) | Синтез 2-(пиридин-2-иламино)-пиридо[2, 3-d]пиримидин-7-онов |
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