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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- 150000003930 2-aminopyridines Chemical class 0.000 abstract 2
- 101100005789 Caenorhabditis elegans cdk-4 gene Proteins 0.000 abstract 2
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- 239000003112 inhibitor Substances 0.000 abstract 2
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Classifications
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35087702P | 2002-01-22 | 2002-01-22 | |
| PCT/IB2003/000059 WO2003062236A1 (en) | 2002-01-22 | 2003-01-10 | 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d]PYRIMIDIN-7-ONES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MEP46108A MEP46108A (en) | 2011-02-10 |
| ME00230B true ME00230B (me) | 2011-02-10 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2008-461A ME00230B (me) | 2002-01-22 | 2003-01-10 | 2-(piridin -2-ilamino)-pirido(2,3-d) pirimidin-7-oni |
Country Status (52)
Families Citing this family (323)
| 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 |
| AU2001278908A1 (en) * | 2000-08-04 | 2002-02-18 | Warner Lambert Company | Process for preparing 2-(4-pyridyl)amino-6-dialkyloxyphenyl-pyrido(2,3-d)pyrimidin 7-ones |
| JP2005507392A (ja) * | 2000-08-04 | 2005-03-17 | 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 | 2−(4−ピリジル)アミノ−6−ジアルキルオキシフェニルピリド〔2,3−d〕ピリミジン−7−オン類の製造方法 |
| AU2002256615B2 (en) * | 2001-02-12 | 2007-09-13 | F. Hoffmann-La Roche Ag | 6-substituted pyrido-pyrimidines |
| CN1503797A (zh) | 2001-02-26 | 2004-06-09 | 田边制药株式会社 | 吡啶并嘧啶或二氮杂萘衍生物 |
| EP1408985A4 (en) * | 2001-06-21 | 2006-03-22 | Ariad Pharma Inc | NEW PYRIDOPYRIMIDONE AND ITS USES |
| US20050154046A1 (en) * | 2004-01-12 | 2005-07-14 | Longgui Wang | Methods of treating an inflammatory-related disease |
| JP4291696B2 (ja) | 2002-01-22 | 2009-07-08 | 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−2−イルアミノ)−ピリド[2,3−d]ピリミジン−7−オン |
| CN100432073C (zh) * | 2002-08-06 | 2008-11-12 | 霍夫曼-拉罗奇有限公司 | 作为p-38map激酶抑制剂的6-烷氧基-吡啶并-嘧啶 |
| US7129351B2 (en) | 2002-11-04 | 2006-10-31 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| AU2003288994A1 (en) | 2002-12-10 | 2004-06-30 | Ono Pharmaceutical Co., Ltd. | Nitrogen-containing heterocyclic compounds and medicinal use thereof |
| WO2004089955A1 (en) | 2003-04-10 | 2004-10-21 | F.Hoffmann-La Roche Ag | Pyrimido compounds |
| 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 |
| CA2532965C (en) | 2003-07-22 | 2013-05-14 | Astex Therapeutics Limited | 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators |
| KR20060036105A (ko) * | 2003-07-29 | 2006-04-27 | 제논 파마슈티칼스 인크. | 피리딜 유도체 및 그의 치료제로서의 용도 |
| DE602004005238T2 (de) * | 2003-11-13 | 2007-11-08 | F. Hoffmann-La Roche Ag | Hydroxyalkylsubstituierte pyrido-7-pyrimidin-7-one |
| US20050171182A1 (en) * | 2003-12-11 | 2005-08-04 | Roger Briesewitz | Methods and compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases |
| PL1713806T3 (pl) * | 2004-02-14 | 2013-09-30 | Irm Llc | Związki i kompozycje jako inhibitory kinaz białkowych |
| CA2555724A1 (en) * | 2004-02-18 | 2005-09-09 | Warner-Lambert Company Llc | 2-(pyridin-3-ylamino)-pyrido[2,3-d]pyrimidin-7-ones |
| JP2007530654A (ja) * | 2004-03-30 | 2007-11-01 | ファイザー・プロダクツ・インク | シグナル伝達阻害剤の組合せ |
| US7378423B2 (en) | 2004-06-11 | 2008-05-27 | Japan Tobacco Inc. | Pyrimidine compound and medical use thereof |
| PT1761528E (pt) * | 2004-06-11 | 2008-04-15 | Japan Tobacco Inc | Derivados de 5-amino-2,4,7-trioxo-3,4,7,8-tetra-hidro-2hpirido[ 2,3-d]pirimidina e compostos relacionados para o tratamento do cancro |
| EP1811991B1 (en) | 2004-11-10 | 2018-11-07 | Genzyme Corporation | Treatment of type 2 diabetes using inhibitors of glycosphingolipid synthesis |
| US20060142312A1 (en) * | 2004-12-23 | 2006-06-29 | Pfizer Inc | C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones |
| 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. |
| KR101345002B1 (ko) * | 2005-01-21 | 2013-12-31 | 아스텍스 테라퓨틱스 리미티드 | 제약 화합물 |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| US20080161355A1 (en) * | 2005-01-21 | 2008-07-03 | Astex Therapeutics Limited | Combinations of Pyrazole Kinase Inhibitors and Further Antitumor Agents |
| KR101346886B1 (ko) * | 2005-01-21 | 2014-01-02 | 아스텍스 테라퓨틱스 리미티드 | 제약 화합물 |
| JP5272408B2 (ja) * | 2005-02-25 | 2013-08-28 | 小野薬品工業株式会社 | 含窒素複素環化合物およびその医薬用途 |
| PE20100741A1 (es) * | 2005-03-25 | 2010-11-25 | Glaxo Group Ltd | COMPUESTOS DERIVADOS DE 3,4-DIHIDROPIRIMIDO[4,5-d]PIRIMIDIN-2(1H)-ONA COMO INHIBIDORES DE QUINASA p38 |
| PE20100737A1 (es) * | 2005-03-25 | 2010-11-27 | Glaxo Group Ltd | Nuevos compuestos |
| AU2006244068B9 (en) | 2005-05-10 | 2012-10-25 | Incyte Holdings Corporation | Modulators of indoleamine 2,3-dioxygenase and methods of using the same |
| KR100734837B1 (ko) * | 2005-09-16 | 2007-07-03 | 한국전자통신연구원 | 다중 생체 인식 시스템 및 그 방법 |
| EP1931667A1 (en) * | 2005-09-28 | 2008-06-18 | Ranbaxy Laboratories Limited | Pyrido-pyridimidine derivatives useful as antiinflammatory agents |
| EP1940839B1 (en) * | 2005-10-07 | 2013-07-31 | Exelixis, Inc. | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kalpha |
| JP5480503B2 (ja) * | 2005-10-07 | 2014-04-23 | エクセリクシス, インク. | PI3Kαのピリドピリミジノン型阻害剤 |
| WO2007129062A1 (en) * | 2006-05-08 | 2007-11-15 | 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 |
| AU2007297286A1 (en) * | 2006-09-08 | 2008-03-20 | Pfizer Products Inc. | Synthesis of 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones |
| HRP20110621T2 (hr) | 2006-09-15 | 2013-12-06 | Pfizer Products Inc. | SPOJEVI PIRIDO[2,3-d]PIRIMIDINONA I NJIHOVA UPOTREBA KAO INHIBITORI PI3 |
| 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 |
| EP2084159A1 (en) * | 2006-10-16 | 2009-08-05 | GPC Biotech Inc. | Pyrido ý2, 3-d¨pyrimidines and their use as kinase inhibitors |
| EP1914234A1 (en) | 2006-10-16 | 2008-04-23 | GPC Biotech Inc. | Pyrido[2,3-d]pyrimidines and their use as kinase inhibitors |
| CN101535308A (zh) * | 2006-11-09 | 2009-09-16 | 霍夫曼-拉罗奇有限公司 | 作为激酶抑制剂的取代的6-苯基-吡啶并[2,3-d]嘧啶-7-酮衍生物及其使用方法 |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| WO2009045503A1 (en) | 2007-10-05 | 2009-04-09 | Genzyme Corporation | Method of treating polycystic kidney diseases with ceramide derivatives |
| US8841312B2 (en) | 2007-12-19 | 2014-09-23 | Amgen Inc. | Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors |
| JP5530422B2 (ja) | 2008-04-07 | 2014-06-25 | アムジエン・インコーポレーテツド | 細胞周期阻害薬としてのgem−二置換およびスピロ環式アミノピリジン/ピリミジン |
| EP2112150B1 (en) | 2008-04-22 | 2013-10-16 | Forma Therapeutics, Inc. | Improved raf inhibitors |
| SG192485A1 (en) | 2008-07-08 | 2013-08-30 | Incyte Corp | 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase |
| US8389517B2 (en) | 2008-07-28 | 2013-03-05 | Genzyme Corporation | Glucosylceramide synthase inhibition for the treatment of collapsing glomerulopathy and other glomerular disease |
| ES2522346T3 (es) * | 2008-08-22 | 2014-11-14 | Novartis Ag | Compuestos de pirrolopirimidina como inhibidores de CDK |
| CA2738925A1 (en) * | 2008-10-01 | 2010-04-08 | The University Of North Carolina At Chapel Hill | Hematopoietic protection against chemotherapeutic compounds using selective cyclin-dependent kinase 4/6 inhibitors |
| JP2012504645A (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 | 健康な細胞に対する電離放射線の影響を低下させる又は防止するための医薬組成物 |
| CN107935983A (zh) * | 2008-10-03 | 2018-04-20 | 简詹姆公司 | 2‑酰胺基丙醇型葡糖神经酰胺合酶抑制剂 |
| PA8852901A1 (es) | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| MX2011008303A (es) | 2009-04-03 | 2011-11-29 | Plexxikon Inc | Composiciones del acido propano-1-sulfonico {3-[5-(4-cloro-fenil)- 1h-pirrolo [2,3-b]-piridina-3-carbonil]-2,4-difluoro-fenil}-amida y el uso de las mismas. |
| EP3718560A3 (en) | 2009-05-13 | 2020-12-09 | The University of North Carolina at Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
| JPWO2011025006A1 (ja) * | 2009-08-31 | 2013-01-31 | 日本ケミファ株式会社 | Gpr119作動薬 |
| 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 |
| BR112012012156A2 (pt) | 2009-11-06 | 2015-09-08 | Plexxikon Inc | compostos e métodos para modulação de cinase, e indicações para esta |
| WO2011075616A1 (en) * | 2009-12-18 | 2011-06-23 | Temple University - Of The Commonwealth System Of Higher Education | 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 |
| US20130035336A1 (en) | 2010-04-13 | 2013-02-07 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) 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 |
| WO2011156786A2 (en) * | 2010-06-10 | 2011-12-15 | Afraxis, Inc. | 6-(ethynyl)pyrido[2,3-d]pyrimidin-7(8h)-ones for the treatment of cns disorders |
| EP3399026B1 (en) | 2010-06-14 | 2024-06-26 | The Scripps Research Institute | Reprogramming of cells to a new fate |
| BR112013002375B1 (pt) | 2010-08-05 | 2020-05-12 | Temple University - Of The Commonwealth System Of Higher Education | Composto, processo de preparação do mesmo, composição farmacêutica, e, usos de um composto |
| US8691830B2 (en) | 2010-10-25 | 2014-04-08 | G1 Therapeutics, Inc. | CDK inhibitors |
| HRP20161092T1 (hr) | 2010-10-25 | 2016-10-21 | G1 Therapeutics, Inc. | Cdk inhibitori |
| US9808461B2 (en) | 2010-11-17 | 2017-11-07 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from ischemia through inhibition of the proliferative kinases CDK4 and CDK6 |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | 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 |
| AU2012214762B2 (en) | 2011-02-07 | 2015-08-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| MY161199A (en) * | 2011-03-23 | 2017-04-14 | Amgen Inc | Fused tricyclic dual inhibitors of cdk 4/6 and flt3 |
| KR20140048891A (ko) | 2011-05-27 | 2014-04-24 | 템플 유니버시티-오브 더 커먼웰쓰 시스템 오브 하이어 에듀케이션 | 치환된 2-벤질리덴-2H-벤조[b][1,4]티아진-3(4H)-온, 이의 유도체, 및 이의 치료적 용도 |
| EP2834237B1 (en) * | 2012-03-14 | 2018-06-06 | Lupin Limited | Heterocyclyl compounds as mek inhibitors |
| CA2868966C (en) | 2012-03-29 | 2021-01-26 | Francis Xavier Tavares | Lactam kinase inhibitors |
| US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| PE20190736A1 (es) | 2012-06-13 | 2019-05-23 | Incyte Holdings Corp | Compuestos triciclicos sustituidos como inhibidores del receptor del factor de crecimiento de fibroblastos (fgfr) |
| US8802697B2 (en) | 2012-07-11 | 2014-08-12 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| WO2014022830A2 (en) | 2012-08-03 | 2014-02-06 | Foundation Medicine, Inc. | Human papilloma virus as predictor of cancer prognosis |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| ES2717279T3 (es) | 2012-08-17 | 2019-06-20 | Concert Pharmaceuticals Inc | Baricitinib deuterada |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| WO2014109858A1 (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 |
| CA2900322C (en) * | 2013-02-21 | 2019-03-26 | Pfizer Inc. | Solid forms of the selective cdk4/6 inhibitor compound acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8h-pyrido[2,3-d]pyrimidin-7-one |
| JP2016512831A (ja) * | 2013-03-15 | 2016-05-09 | コンサート ファーマシューティカルズ インコーポレイテッド | 重水素化されたパルボシクリブ |
| WO2014144326A1 (en) | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | Transient protection of normal cells during chemotherapy |
| CN105407723A (zh) | 2013-03-15 | 2016-03-16 | G1治疗公司 | 高效的抗赘生剂和抗增生剂 |
| KR102269032B1 (ko) | 2013-04-19 | 2021-06-24 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| CN104470921B (zh) * | 2013-05-17 | 2017-05-03 | 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 |
| AU2014339972B9 (en) | 2013-10-25 | 2019-05-30 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| AU2014368927B2 (en) * | 2013-12-20 | 2018-10-25 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of CDK and ERK inhibitors |
| US9949976B2 (en) | 2013-12-31 | 2018-04-24 | Xuanzhu Pharma Co., Ltd. | Kinase inhibitor and use thereof |
| HUE039504T2 (hu) | 2013-12-31 | 2019-01-28 | Xuanzhu Pharma Co Ltd | Kináz inhibitor és alkalmazása |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| US20150297606A1 (en) | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic Lactams for Use in the Protection of Hematopoietic Stem and Progenitor Cells Against Ionizing Radiation |
| 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 |
| WO2016014904A1 (en) | 2014-07-24 | 2016-01-28 | Beta Pharma, Inc. | 2-h-indazole derivatives as cyclin-dependent kinase (cdk) inhibitors and therapeutic uses thereof |
| AU2015296322B2 (en) * | 2014-07-26 | 2019-09-19 | Sunshine Lake Pharma Co., Ltd. | 2-amino-pyrido[2,3-d]pyrimidin-7(8h)-one derivatives as CDK inhibitors and uses thereof |
| WO2016016769A1 (en) * | 2014-07-31 | 2016-02-04 | Sun Pharmaceutical Industries Limited | A process for the preparation of palbociclib |
| TW201618773A (zh) * | 2014-08-11 | 2016-06-01 | 艾森塔製藥公司 | Btk抑制劑、pi3k抑制劑、jak-2抑制劑、及/或cdk4/6抑制劑的治療組合物 |
| US20170240543A1 (en) * | 2014-08-14 | 2017-08-24 | 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 |
| WO2016066420A1 (en) * | 2014-10-29 | 2016-05-06 | Sandoz Ag | Crystalline forms of palbociclib monohydrochloride |
| 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 |
| 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 |
| IL278574B2 (en) | 2014-11-12 | 2024-11-01 | Seagen Inc | Glycan-interacting compounds and methods of use |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2016107605A1 (zh) | 2014-12-31 | 2016-07-07 | 昆明积大制药股份有限公司 | 药物组合物及其制备方法 |
| 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 |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| ES2895769T3 (es) | 2015-02-20 | 2022-02-22 | Incyte Corp | Heterociclos bicíclicos como inhibidores de FGFR |
| 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 |
| KR102601320B1 (ko) | 2015-05-29 | 2023-11-10 | 데이진 화-마 가부시키가이샤 | 피리도[3,4-d]피리미딘 유도체 및 그 약학적으로 허용되는 염 |
| 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 |
| WO2017021111A1 (en) * | 2015-08-05 | 2017-02-09 | Ratiopharm Gmbh | New 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 |
| WO2017083582A1 (en) | 2015-11-12 | 2017-05-18 | Siamab Therapeutics, Inc. | Glycan-interacting compounds and methods of use |
| 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 |
| EP3386981B1 (en) * | 2015-12-13 | 2021-10-13 | Hangzhou Innogate Pharma Co., Ltd. | Heterocycles useful as anti-cancer agents |
| 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 |
| US11077110B2 (en) | 2016-03-18 | 2021-08-03 | 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 |
| US10865204B2 (en) | 2016-04-22 | 2020-12-15 | 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 |
| WO2018005863A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based compounds for the treatment of cancer |
| KR20190025943A (ko) | 2016-07-01 | 2019-03-12 | 쥐원 쎄라퓨틱스, 인크. | 피리미딘-기재 항증식제 |
| WO2018005533A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Antiproliferative pyrimidine-based compounds |
| WO2018007927A1 (en) | 2016-07-04 | 2018-01-11 | Dr. Reddy's Laboratories Limited | Process for preparation of palbociclib |
| US10597393B2 (en) | 2016-07-07 | 2020-03-24 | Plantex Ltd. | Solid state forms of Palbociclib dimesylate |
| CN114394966B (zh) * | 2016-08-15 | 2024-10-11 | 辉瑞公司 | 吡啶并嘧啶酮cdk2/4/6抑制剂 |
| IL264950B2 (en) | 2016-08-23 | 2024-01-01 | Eisai R&D Man Co Ltd | Combined treatments for the treatment of malignant liver cell carcinoma |
| CN110022900A (zh) | 2016-09-08 | 2019-07-16 | 蓝图药品公司 | 成纤维细胞生长因子受体4抑制剂与细胞周期蛋白依赖性激酶抑制剂的组合 |
| WO2018065999A1 (en) | 2016-10-07 | 2018-04-12 | Mylan Laboratories Limited | Novel polymorph of an intermediate for palbociclib synthesis |
| BR112019005526A2 (pt) | 2016-10-20 | 2019-06-18 | Pfizer | agentes antiproliferativos para tratamento de pah |
| WO2018073574A1 (en) | 2016-10-20 | 2018-04-26 | Cipla Limited | Polymorphic forms of palbociclib |
| 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 |
| AU2017359333B2 (en) | 2016-11-08 | 2024-03-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods of modulating anti-tumor immunity |
| CA3043681A1 (en) | 2016-11-16 | 2018-05-24 | 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 |
| ES2852123T3 (es) | 2016-11-28 | 2021-09-13 | Teijin Pharma Ltd | Derivados de ((piridin-2-il)-amino)pirido[3,4-d]pirimidina y ((piridazin-3-il)-amino)pirido[3,4-d]pirimidina como inhibidores de CDK4/6 para tratar p. ej. artritis reumatoide, arteriosclerosis, fibrosis pulmonar, infarto cerebral o cáncer |
| RS63004B1 (sr) | 2016-11-28 | 2022-03-31 | Teijin Pharma Ltd | Kristal pirido[3, 4-d]pirimidin derivata ili njegov solvat |
| JP7044801B2 (ja) | 2016-12-16 | 2022-03-30 | シーストーン・ファーマスーティカルズ・(スージョウ)・カンパニー・リミテッド | Cdk4/6阻害剤 |
| EP3565558B1 (en) | 2017-01-06 | 2023-12-06 | G1 Therapeutics, Inc. | Combination therapy with a serd compound and a cdk4/6 inhibitor for the treatment of cancer |
| 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 |
| KR20240044544A (ko) | 2017-03-03 | 2024-04-04 | 씨젠 인크. | 글리칸-상호작용 화합물 및 사용 방법 |
| AU2018229148B2 (en) * | 2017-03-03 | 2022-08-04 | Auckland Uniservices Limited | FGFR kinase inhibitors and pharmaceutical uses |
| CN110636862A (zh) | 2017-03-16 | 2019-12-31 | 卫材 R&D 管理有限公司 | 用于治疗乳腺癌的组合疗法 |
| 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 |
| TW201904577A (zh) | 2017-06-16 | 2019-02-01 | 美商貝達醫藥公司 | N-(2-(2-二甲胺基)乙氧基)-4-甲氧基-5-((4-(1-甲基-1h-吲哚-3-基)嘧啶-2-基)胺基)苯基)丙烯醯胺及其鹽之醫藥調配物 |
| WO2019006393A1 (en) | 2017-06-29 | 2019-01-03 | 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 |
| WO2019020715A1 (en) | 2017-07-28 | 2019-01-31 | Synthon B.V. | PHARMACEUTICAL COMPOSITION COMPRISING PALBOCICLIB |
| 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 |
| CN119162314A (zh) | 2017-08-31 | 2024-12-20 | 诺华股份有限公司 | 选择针对癌症患者的治疗的方法 |
| 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 |
| WO2019070755A1 (en) | 2017-10-02 | 2019-04-11 | The Broad Institute, Inc. | METHODS AND COMPOSITIONS FOR DETECTING AND MODULATING A GENETIC SIGNATURE OF IMMUNOTHERAPY RESISTANCE IN CANCER |
| US11667651B2 (en) | 2017-12-22 | 2023-06-06 | Hibercell, Inc. | Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors |
| 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 |
| CA3088381A1 (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 |
| CN112041307B (zh) | 2018-02-06 | 2024-02-09 | 伊利诺伊大学评议会 | 作为选择性雌激素受体降解剂的取代的苯并噻吩类似物 |
| EP3758753A1 (en) | 2018-02-27 | 2021-01-06 | Pfizer Inc | Combination of a cyclin dependent kinase inhibitor and a bet-bromodomain inhibitor |
| MA52422A (fr) | 2018-02-27 | 2021-01-06 | Incyte Corp | Imidazopyrimidines et triazolopyrimidines en tant qu'inhibiteurs a2a/a2b |
| SI3788047T1 (sl) | 2018-05-04 | 2024-11-29 | Incyte Corporation | Trdne oblike inhibitorja fgfr in postopki priprave le-teh |
| SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
| CA3100144C (en) | 2018-05-14 | 2023-10-03 | Pfizer Inc. | Oral solution formulation of palbociclib in malic or lactic acid buffer |
| MX2020012376A (es) | 2018-05-18 | 2021-03-09 | Incyte Corp | Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b. |
| US11858928B2 (en) | 2018-05-24 | 2024-01-02 | Synthon B.V. | Process for making palbociclib |
| MA53097A (fr) | 2018-07-05 | 2021-05-12 | Incyte Corp | Dérivés de pyrazine fusionnés en tant qu'inhibiteurs d'a2a/a2b |
| KR20210035211A (ko) | 2018-07-23 | 2021-03-31 | 에프. 호프만-라 로슈 아게 | Pi3k 저해제인 gdc-0077로 암을 치료하는 방법 |
| SG11202100429TA (en) | 2018-07-27 | 2021-02-25 | California Inst Of Techn | Cdk inhibitors and uses thereof |
| KR20210049847A (ko) | 2018-08-24 | 2021-05-06 | 쥐원 쎄라퓨틱스, 인크. | 1,4-디아자스피로[5.5]운데칸-3-온의 개선된 합성 |
| 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 |
| EP3863618A1 (en) | 2018-10-08 | 2021-08-18 | F. Hoffmann-La Roche AG | Methods of treating cancer with pi3k alpha inhibitors and metformin |
| 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 |
| BR112021011894A2 (pt) | 2018-12-21 | 2021-09-08 | Daiichi Sankyo Company, Limited | Composição farmacêutica |
| EP3902805A4 (en) | 2018-12-28 | 2023-03-01 | SPV Therapeutics Inc. | CYCLINE-DEPENDENT KINASE INHIBITORS |
| AU2019413683B2 (en) * | 2018-12-28 | 2025-05-22 | 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 |
| US20220125777A1 (en) | 2019-02-01 | 2022-04-28 | Pfizer Inc. | Combination of a cdk inhibitor and a pim inhibitor |
| CA3130210A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Cyclin-dependent kinase 2 biomarkers and uses thereof |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| WO2020180959A1 (en) | 2019-03-05 | 2020-09-10 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2020186101A1 (en) | 2019-03-12 | 2020-09-17 | 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 |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| WO2020223469A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer |
| CA3141531A1 (en) | 2019-05-24 | 2020-12-03 | Pfizer Inc. | Combination therapies using cdk inhibitors |
| CA3141452A1 (en) | 2019-05-24 | 2020-12-03 | Pfizer Inc. | Combination therapies using cdk inhibitors |
| 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 |
| MX2022000279A (es) | 2019-07-07 | 2022-02-03 | Olema Pharmaceuticals Inc | Regimenes de antagonistas del receptor de estrogeno. |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US20210030869A1 (en) | 2019-08-01 | 2021-02-04 | Incyte Corporation | Dosing regimen for an ido inhibitor |
| PH12022550361A1 (en) | 2019-08-14 | 2023-02-27 | Incyte Corp | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| EP4021450B1 (en) | 2019-08-26 | 2025-11-05 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| PE20221905A1 (es) | 2019-10-11 | 2022-12-23 | Incyte Corp | Aminas biciclicas como inhibidoras de la cdk2 |
| US11607416B2 (en) | 2019-10-14 | 2023-03-21 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | 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 |
| WO2021113219A1 (en) | 2019-12-03 | 2021-06-10 | Genentech, Inc. | Combination therapies for treatment of breast cancer |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CA3164619A1 (en) * | 2019-12-16 | 2021-06-24 | Lunella Biotech, Inc. | Selective cdk4/6 inhibitor cancer therapeutics |
| IL293940A (en) | 2019-12-16 | 2022-08-01 | Lunella Biotech Inc | Selective cancer drugs cdk4/6 inhibitors |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TW202146017A (zh) | 2020-03-05 | 2021-12-16 | 美商輝瑞股份有限公司 | 間變性淋巴瘤激酶抑制劑及周期蛋白依賴型激酶抑制劑之組合 |
| AU2021230385A1 (en) | 2020-03-06 | 2022-09-22 | Incyte Corporation | Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors |
| EP4118082A4 (en) * | 2020-03-13 | 2024-05-01 | Prosenestar LLC | PYRIDO[2,3-D]PYRIMIDINE-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 |
| EP4135844A1 (en) | 2020-04-16 | 2023-02-22 | Incyte Corporation | Fused tricyclic kras inhibitors |
| US11739102B2 (en) | 2020-05-13 | 2023-08-29 | Incyte Corporation | Fused pyrimidine compounds as KRAS inhibitors |
| AU2021273744A1 (en) | 2020-05-19 | 2022-12-08 | Pharmacosmos Holding A/S | Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders |
| US20230132667A1 (en) * | 2020-05-28 | 2023-05-04 | 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 |
| BR112023000687A2 (pt) | 2020-07-15 | 2023-02-07 | Pfizer | Métodos e combinações de inibidores de kat6 para o tratamento de câncer |
| US20230321042A1 (en) | 2020-07-20 | 2023-10-12 | Pfizer Inc. | Combination therapy |
| US11999752B2 (en) | 2020-08-28 | 2024-06-04 | Incyte Corporation | Vinyl imidazole compounds as inhibitors of KRAS |
| WO2022063119A1 (zh) * | 2020-09-24 | 2022-03-31 | 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 |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US20240287065A1 (en) * | 2021-06-09 | 2024-08-29 | Tyk Medicines (Zhengzhou) , Inc. | Compound as cdk kinase inhibitor and use thereof |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US12441727B2 (en) | 2021-07-07 | 2025-10-14 | Incyte Corporation | Tricyclic compounds as inhibitors of KRAS |
| JP2024529347A (ja) | 2021-07-14 | 2024-08-06 | インサイト・コーポレイション | Krasの阻害剤としての三環式化合物 |
| TW202320795A (zh) | 2021-07-26 | 2023-06-01 | 美商凱爾科迪股份有限公司 | 使用1-(4-{[4-(二甲胺基)哌啶-1-基]羰基}苯基)-3-[4-(4,6-二嗎啉-4-基-1,3,5-三-2-基)苯基]脲治療癌症之方法 |
| JP2024534187A (ja) | 2021-08-31 | 2024-09-18 | インサイト・コーポレイション | Krasの阻害剤としてのナフチリジン化合物 |
| 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 |
| WO2023040914A1 (zh) * | 2021-09-14 | 2023-03-23 | 甘李药业股份有限公司 | 一种cdk4/6抑制剂的医药用途 |
| WO2023049697A1 (en) | 2021-09-21 | 2023-03-30 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of kras |
| JP2024537824A (ja) | 2021-10-01 | 2024-10-16 | インサイト・コーポレイション | ピラゾロキノリンkras阻害剤 |
| PE20242113A1 (es) | 2021-10-14 | 2024-10-28 | Incyte Corp | Compuestos de quinolina como inhibidores de kras |
| EP4436578A1 (en) | 2021-11-22 | 2024-10-02 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a kras inhibitor |
| US20230203010A1 (en) | 2021-12-03 | 2023-06-29 | Incyte Corporation | Bicyclic amine cdk12 inhibitors |
| 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 |
| CA3240454A1 (en) | 2021-12-10 | 2023-06-15 | Lacey Morgan LITCHFIELD | 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 inhibito |
| WO2023111810A1 (en) | 2021-12-14 | 2023-06-22 | 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 |
| EP4452982A1 (en) | 2021-12-22 | 2024-10-30 | Incyte Corporation | Salts and solid forms of an fgfr inhibitor and processes of preparing thereof |
| TW202341982A (zh) | 2021-12-24 | 2023-11-01 | 大陸商上海齊魯銳格醫藥研發有限公司 | Cdk2抑制劑及其用途 |
| 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 |
| PE20250667A1 (es) | 2022-03-07 | 2025-03-04 | Incyte Corp | Formas solidas, sales y procesos de preparacion de un inhibidor de cdk2 |
| HU231594B1 (hu) * | 2022-05-10 | 2025-03-28 | Egis Gyógyszergyár Zrt. | Palbociclibet és letrozolt tartalmazó gyógyszerkészítmény |
| US20250353842A1 (en) | 2022-06-22 | 2025-11-20 | 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 |
| WO2024023703A1 (en) | 2022-07-29 | 2024-02-01 | Pfizer Inc. | Dosing regimens comprising a kat6 inhibitor for the treatment of cancer |
| TWI866427B (zh) | 2022-08-31 | 2024-12-11 | 美商亞文納營運公司 | 雌激素受體降解劑之給藥方案 |
| KR20250105413A (ko) | 2022-11-02 | 2025-07-08 | 페트라 파마 코포레이션 | 질환의 치료를 위한 포스포이노시티드 3-키나제 (pi3k)의 알로스테릭 크로메논 억제제 |
| EP4615431A1 (en) | 2022-11-11 | 2025-09-17 | Astrazeneca AB | Combination therapies for the treatment of cancer |
| WO2024125581A2 (zh) * | 2022-12-16 | 2024-06-20 | 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 |
| KR20250164842A (ko) | 2023-03-30 | 2025-11-25 | 화이자 인코포레이티드 | Kat6a 억제제에 의한 치료를 위한 예측 바이오마커로서의 kat6a 및 이의 치료 방법 |
| 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 |
| TW202446371A (zh) | 2023-04-18 | 2024-12-01 | 美商英塞特公司 | 2-氮雜雙環[2.2.1]庚烷kras抑制劑 |
| US20240390340A1 (en) | 2023-04-18 | 2024-11-28 | Incyte Corporation | Pyrrolidine kras inhibitors |
| TW202508598A (zh) | 2023-05-05 | 2025-03-01 | 瑞典商阿斯特捷利康公司 | 癌症療法 |
| 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 |
| WO2025122470A1 (en) | 2023-12-04 | 2025-06-12 | Genentech, Inc. | Combination therapies for treatment of breast cancer |
| WO2025129002A1 (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 |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK157451C (da) | 1979-06-14 | 1990-05-21 | Wellcome Found | Analogifremgangsmaade til fremstilling af 2,4-diamino-6-alkoxybenzyl-5-methylpyridooe2,3-daapyrimidiner eller farmaceutisk acceptable syreadditionssalte deraf |
| US4959474A (en) | 1979-06-14 | 1990-09-25 | Burroughs Wellcome Co. | Dialkoxy pyridopyrimidine compounds |
| JPS5618982A (en) | 1979-06-14 | 1981-02-23 | Wellcome Found | Pyrimidine derivatives and medicinal drug containing them |
| AU598093B2 (en) | 1987-02-07 | 1990-06-14 | Wellcome Foundation Limited, The | 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 |
| ATE190978T1 (de) | 1994-11-14 | 2000-04-15 | Warner Lambert Co | 6-aryl-pyrido(2,3-d)pyrimidine und -naphthyridine zur hemmung der durch protein-tyrosin-kinase hervorgerufenen zellvermehrung |
| 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 |
| US5948786A (en) | 1996-04-12 | 1999-09-07 | Sumitomo Pharmaceuticals Company, Limited | Piperidinylpyrimidine derivatives |
| AU2521597A (en) | 1996-04-12 | 1997-11-07 | Sumitomo Pharmaceuticals Company, Limited | Piperidinylpyramidine derivatives |
| US6498163B1 (en) * | 1997-02-05 | 2002-12-24 | Warner-Lambert Company | Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation |
| ES2301194T3 (es) * | 1997-02-05 | 2008-06-16 | Warner-Lambert Company Llc | Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular. |
| CA2306082A1 (en) | 1997-10-27 | 1999-05-06 | Agouron Pharmaceuticals, Inc. | Substituted 4-amino-thiazol-2-y compounds as cdks inhibitors |
| ES2310039T3 (es) * | 1998-05-26 | 2008-12-16 | Warner-Lambert Company Llc | Pirimidinas biciclicas y 3,4-dihidropirimidinas biciclicas como inhibidores de la proliferacion celular. |
| AU5438299A (en) | 1998-08-29 | 2000-03-21 | Astrazeneca Ab | Pyrimidine compounds |
| DE60024631T2 (de) | 1999-07-26 | 2006-06-14 | Banyu Pharma Co Ltd | Biaryl-harnstoff-derivate |
| MXPA02001108A (es) | 1999-09-15 | 2002-08-20 | Warner Lambert Co | Pieridinonas como inhibidores de la cinasa. |
| PL357634A1 (en) * | 2000-01-27 | 2004-07-26 | Warner-Lambert Company | Pyridopyrimidinone derivatives for treatment of neurodegenerative disease |
| SK12472002A3 (sk) * | 2000-03-06 | 2003-04-01 | Warner-Lambert Company | 5-Alkylpyrido[2,3-d]pyrimidínové inhibítory tyrosínových kináz |
| ATE408613T1 (de) | 2000-08-04 | 2008-10-15 | Warner Lambert Co | 2-(4-pyridyl)amino-6-dialkoxyphenyl-pyrido(2,3- d)pyrimidin-7-one |
| ATE281455T1 (de) | 2000-09-01 | 2004-11-15 | Glaxo Group Ltd | Oxindolderivate |
| GB0101686D0 (en) | 2001-01-23 | 2001-03-07 | Cancer Res Campaign Tech | Cyclin dependent kinase inhibitors |
| AU2002256615B2 (en) * | 2001-02-12 | 2007-09-13 | F. Hoffmann-La Roche Ag | 6-substituted pyrido-pyrimidines |
| ES2262899T3 (es) | 2001-12-17 | 2006-12-01 | Smithkline Beecham Corporation | Derivados de pirazolopiridazina. |
| JP4291696B2 (ja) | 2002-01-22 | 2009-07-08 | 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−2−イルアミノ)−ピリド[2,3−d]ピリミジン−7−オン |
| US7189712B2 (en) | 2002-10-10 | 2007-03-13 | Smithkline Beecham Corporation | 1,3-Oxazole compounds for the treatment of cancer |
| WO2004047760A2 (en) | 2002-11-22 | 2004-06-10 | Smithkline Beecham Corporation | Novel chemical compounds |
| WO2004063195A1 (en) * | 2003-01-03 | 2004-07-29 | Sloan-Kettering Institute For Cancer Research | Pyridopyrimidine kinase inhibitors |
| WO2004065378A1 (en) | 2003-01-17 | 2004-08-05 | Warner-Lambert Company Llc | 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation |
| EP1597234B1 (en) | 2003-02-27 | 2008-10-08 | Smithkline Beecham Corporation | Novel compounds |
| 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 |
| AU2007297286A1 (en) | 2006-09-08 | 2008-03-20 | Pfizer Products Inc. | Synthesis of 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones |
-
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