FI3337477T3 - Koostumukset, jotka käsittävät fosfoinositidi-3-kinaasin estäjiä ja toista antiproliferatiivista ainetta - Google Patents
Koostumukset, jotka käsittävät fosfoinositidi-3-kinaasin estäjiä ja toista antiproliferatiivista ainetta Download PDFInfo
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- FI3337477T3 FI3337477T3 FIEP16756763.5T FI16756763T FI3337477T3 FI 3337477 T3 FI3337477 T3 FI 3337477T3 FI 16756763 T FI16756763 T FI 16756763T FI 3337477 T3 FI3337477 T3 FI 3337477T3
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- 239000000203 mixture Substances 0.000 title claims 15
- 239000003795 chemical substances by application Substances 0.000 title claims 4
- 230000001028 anti-proliverative effect Effects 0.000 title 1
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 title 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title 1
- -1 CG11746 Chemical compound 0.000 claims 35
- 239000003112 inhibitor Substances 0.000 claims 16
- 206010028980 Neoplasm Diseases 0.000 claims 10
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 claims 8
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 claims 8
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims 8
- 239000002176 L01XE26 - Cabozantinib Substances 0.000 claims 6
- 229960001292 cabozantinib Drugs 0.000 claims 6
- ONIQOQHATWINJY-UHFFFAOYSA-N cabozantinib Chemical compound C=12C=C(OC)C(OC)=CC2=NC=CC=1OC(C=C1)=CC=C1NC(=O)C1(C(=O)NC=2C=CC(F)=CC=2)CC1 ONIQOQHATWINJY-UHFFFAOYSA-N 0.000 claims 6
- 229940079156 Proteasome inhibitor Drugs 0.000 claims 5
- 239000003207 proteasome inhibitor Substances 0.000 claims 5
- WCWUXEGQKLTGDX-LLVKDONJSA-N (2R)-1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methyl-6-pyrrolo[2,1-f][1,2,4]triazinyl]oxy]-2-propanol Chemical compound C1=C2NC(C)=CC2=C(F)C(OC2=NC=NN3C=C(C(=C32)C)OC[C@H](O)C)=C1 WCWUXEGQKLTGDX-LLVKDONJSA-N 0.000 claims 4
- YABJJWZLRMPFSI-UHFFFAOYSA-N 1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-2-benzimidazolamine Chemical compound N=1C2=CC(OC=3C=C(N=CC=3)C=3NC(=CN=3)C(F)(F)F)=CC=C2N(C)C=1NC1=CC=C(C(F)(F)F)C=C1 YABJJWZLRMPFSI-UHFFFAOYSA-N 0.000 claims 4
- GKJCVYLDJWTWQU-CXLRFSCWSA-N 2-[4-[(e)-2-[5-[(1r)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1h-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol Chemical compound O([C@H](C)C=1C(=CN=CC=1Cl)Cl)C(C=C12)=CC=C1NN=C2\C=C\C=1C=NN(CCO)C=1 GKJCVYLDJWTWQU-CXLRFSCWSA-N 0.000 claims 4
- NHFDRBXTEDBWCZ-ZROIWOOFSA-N 3-[2,4-dimethyl-5-[(z)-(2-oxo-1h-indol-3-ylidene)methyl]-1h-pyrrol-3-yl]propanoic acid Chemical compound OC(=O)CCC1=C(C)NC(\C=C/2C3=CC=CC=C3NC\2=O)=C1C NHFDRBXTEDBWCZ-ZROIWOOFSA-N 0.000 claims 4
- ZCCPLJOKGAACRT-UHFFFAOYSA-N 4-methyl-3-[[1-methyl-6-(3-pyridinyl)-4-pyrazolo[3,4-d]pyrimidinyl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide Chemical compound CC1=CC=C(C(=O)NC=2C=C(C=CC=2)C(F)(F)F)C=C1NC(C=1C=NN(C)C=1N=1)=NC=1C1=CC=CN=C1 ZCCPLJOKGAACRT-UHFFFAOYSA-N 0.000 claims 4
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims 4
- 101001056180 Homo sapiens Induced myeloid leukemia cell differentiation protein Mcl-1 Proteins 0.000 claims 4
- 102100026539 Induced myeloid leukemia cell differentiation protein Mcl-1 Human genes 0.000 claims 4
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims 4
- 239000002137 L01XE24 - Ponatinib Substances 0.000 claims 4
- YJDAOHJWLUNFLX-UHFFFAOYSA-N NU 1025 Chemical compound C1=CC=C2C(=O)NC(C)=NC2=C1O YJDAOHJWLUNFLX-UHFFFAOYSA-N 0.000 claims 4
- DXCUKNQANPLTEJ-UHFFFAOYSA-N PD173074 Chemical compound CC(C)(C)NC(=O)NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C1=CC(OC)=CC(OC)=C1 DXCUKNQANPLTEJ-UHFFFAOYSA-N 0.000 claims 4
- 108010090931 Proto-Oncogene Proteins c-bcl-2 Proteins 0.000 claims 4
- 102000013535 Proto-Oncogene Proteins c-bcl-2 Human genes 0.000 claims 4
- OVDSPTSBIQCAIN-UHFFFAOYSA-N ap26113 Chemical compound COC1=CC(N2CCC(CC2)N(C)C)=CC=C1NC(N=1)=NC=C(Cl)C=1NC1=CC=CC=C1P(C)(C)=O OVDSPTSBIQCAIN-UHFFFAOYSA-N 0.000 claims 4
- 239000003886 aromatase inhibitor Substances 0.000 claims 4
- 229940046844 aromatase inhibitors Drugs 0.000 claims 4
- 229950004272 brigatinib Drugs 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 239000002955 immunomodulating agent Substances 0.000 claims 4
- 229960003648 ixazomib Drugs 0.000 claims 4
- MXAYKZJJDUDWDS-LBPRGKRZSA-N ixazomib Chemical compound CC(C)C[C@@H](B(O)O)NC(=O)CNC(=O)C1=CC(Cl)=CC=C1Cl MXAYKZJJDUDWDS-LBPRGKRZSA-N 0.000 claims 4
- 229960001131 ponatinib Drugs 0.000 claims 4
- PHXJVRSECIGDHY-UHFFFAOYSA-N ponatinib Chemical compound C1CN(C)CCN1CC(C(=C1)C(F)(F)F)=CC=C1NC(=O)C1=CC=C(C)C(C#CC=2N3N=CC=CC3=NC=2)=C1 PHXJVRSECIGDHY-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 230000019491 signal transduction Effects 0.000 claims 4
- 229960003787 sorafenib Drugs 0.000 claims 4
- FYXRSVDHGLUMHB-UHFFFAOYSA-N 4-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-methylimidazol-2-yl]piperidin-1-yl]-1h-pyrazolo[3,4-d]pyrimidine Chemical compound N1=C(C2CCN(CC2)C=2C=3C=NNC=3N=CN=2)N(C)C=C1C1=CC=C(F)C(C(F)(F)F)=C1 FYXRSVDHGLUMHB-UHFFFAOYSA-N 0.000 claims 3
- 239000002177 L01XE27 - Ibrutinib Substances 0.000 claims 3
- XKFTZKGMDDZMJI-HSZRJFAPSA-N N-[5-[(2R)-2-methoxy-1-oxo-2-phenylethyl]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-3-yl]-4-(4-methyl-1-piperazinyl)benzamide Chemical compound O=C([C@H](OC)C=1C=CC=CC=1)N(CC=12)CC=1NN=C2NC(=O)C(C=C1)=CC=C1N1CCN(C)CC1 XKFTZKGMDDZMJI-HSZRJFAPSA-N 0.000 claims 3
- 229960001467 bortezomib Drugs 0.000 claims 3
- GXJABQQUPOEUTA-RDJZCZTQSA-N bortezomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)B(O)O)NC(=O)C=1N=CC=NC=1)C1=CC=CC=C1 GXJABQQUPOEUTA-RDJZCZTQSA-N 0.000 claims 3
- 229950002966 danusertib Drugs 0.000 claims 3
- 229960001507 ibrutinib Drugs 0.000 claims 3
- XYFPWWZEPKGCCK-GOSISDBHSA-N ibrutinib Chemical compound C1=2C(N)=NC=NC=2N([C@H]2CN(CCC2)C(=O)C=C)N=C1C(C=C1)=CC=C1OC1=CC=CC=C1 XYFPWWZEPKGCCK-GOSISDBHSA-N 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229950010746 selumetinib Drugs 0.000 claims 3
- CYOHGALHFOKKQC-UHFFFAOYSA-N selumetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1Cl CYOHGALHFOKKQC-UHFFFAOYSA-N 0.000 claims 3
- 239000000126 substance Substances 0.000 claims 3
- 238000002560 therapeutic procedure Methods 0.000 claims 3
- ZADWXFSZEAPBJS-SNVBAGLBSA-N (2r)-2-amino-3-(1-methylindol-3-yl)propanoic acid Chemical compound C1=CC=C2N(C)C=C(C[C@@H](N)C(O)=O)C2=C1 ZADWXFSZEAPBJS-SNVBAGLBSA-N 0.000 claims 2
- KGWWHPZQLVVAPT-STTJLUEPSA-N (2r,3r)-2,3-dihydroxybutanedioic acid;6-(4-methylpiperazin-1-yl)-n-(5-methyl-1h-pyrazol-3-yl)-2-[(e)-2-phenylethenyl]pyrimidin-4-amine Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.C1CN(C)CCN1C1=CC(NC2=NNC(C)=C2)=NC(\C=C\C=2C=CC=CC=2)=N1 KGWWHPZQLVVAPT-STTJLUEPSA-N 0.000 claims 2
- WQAVPPWWLLVGFK-VTNASVEKSA-N (2s)-3-(4-methoxyphenyl)-n-[(2s)-1-[(2r)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]-2-[[(2s)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide Chemical compound C1=CC(OC)=CC=C1C[C@@H](C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)[C@]1(C)OC1)NC(=O)[C@H](C)NC(=O)CN1CCOCC1 WQAVPPWWLLVGFK-VTNASVEKSA-N 0.000 claims 2
- CVCLJVVBHYOXDC-IAZSKANUSA-N (2z)-2-[(5z)-5-[(3,5-dimethyl-1h-pyrrol-2-yl)methylidene]-4-methoxypyrrol-2-ylidene]indole Chemical compound COC1=C\C(=C/2N=C3C=CC=CC3=C\2)N\C1=C/C=1NC(C)=CC=1C CVCLJVVBHYOXDC-IAZSKANUSA-N 0.000 claims 2
- KCOYQXZDFIIGCY-CZIZESTLSA-N (3e)-4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1,3-dihydrobenzimidazol-2-ylidene]quinolin-2-one Chemical compound C1CN(C)CCN1C1=CC=C(N\C(N2)=C/3C(=C4C(F)=CC=CC4=NC\3=O)N)C2=C1 KCOYQXZDFIIGCY-CZIZESTLSA-N 0.000 claims 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 2
- 125000006832 (C1-C10) alkylene group Chemical group 0.000 claims 2
- MLSAQOINCGAULQ-QFMPWRQOSA-N (E)-SB-590885 Chemical compound C1=CC(OCCN(C)C)=CC=C1C1=NC(C=2C=CN=CC=2)=C(C=2C=C3CCC(/C3=CC=2)=N\O)N1 MLSAQOINCGAULQ-QFMPWRQOSA-N 0.000 claims 2
- LIDOPKHSVQTSJY-VMEIHUARSA-N (e)-3-(6-bromopyridin-2-yl)-2-cyano-n-[(1s)-1-phenylbutyl]prop-2-enamide Chemical compound N([C@@H](CCC)C=1C=CC=CC=1)C(=O)C(\C#N)=C\C1=CC=CC(Br)=N1 LIDOPKHSVQTSJY-VMEIHUARSA-N 0.000 claims 2
- LFKQSJNCVRGFCC-UHFFFAOYSA-N 1-(2,4-difluorophenyl)-3-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]urea Chemical compound C=12C=C(OC)C(OC)=CC2=NC=CC=1OC(C=C1F)=CC=C1NC(=O)NC1=CC=C(F)C=C1F LFKQSJNCVRGFCC-UHFFFAOYSA-N 0.000 claims 2
- RZUOCXOYPYGSKL-GOSISDBHSA-N 1-[(1s)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]pyridin-2-one Chemical compound CN1N=CC=C1NC1=NC=CC(C2=CC(=O)N([C@H](CO)C=3C=C(F)C(Cl)=CC=3)C=C2)=N1 RZUOCXOYPYGSKL-GOSISDBHSA-N 0.000 claims 2
- VPBYZLCHOKSGRX-UHFFFAOYSA-N 1-[2-chloro-4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-propylurea Chemical compound C1=C(Cl)C(NC(=O)NCCC)=CC=C1OC1=NC=NC2=CC(OC)=C(OC)C=C12 VPBYZLCHOKSGRX-UHFFFAOYSA-N 0.000 claims 2
- DKNUPRMJNUQNHR-UHFFFAOYSA-N 1-[3-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]urea Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1OC(C=1)=CC=CC=1NC(=O)NC=1C=C(C(C)(C)C(F)(F)F)ON=1 DKNUPRMJNUQNHR-UHFFFAOYSA-N 0.000 claims 2
- RGJOJUGRHPQXGF-INIZCTEOSA-N 1-ethyl-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-7-(oxetan-3-yl)-6,8-dihydro-5h-pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea Chemical compound C1=CC(NC(=O)NCC)=CC=C1C(N=C1N2[C@H](COCC2)C)=NC2=C1CCN(C1COC1)C2 RGJOJUGRHPQXGF-INIZCTEOSA-N 0.000 claims 2
- RAYNZUHYMMLQQA-ZEQRLZLVSA-N 2,3,5-trihydroxy-7-methyl-n-[(2r)-2-phenylpropyl]-6-[1,6,7-trihydroxy-3-methyl-5-[[(2r)-2-phenylpropyl]carbamoyl]naphthalen-2-yl]naphthalene-1-carboxamide Chemical compound C1([C@@H](C)CNC(=O)C=2C3=CC(C)=C(C(=C3C=C(O)C=2O)O)C=2C(O)=C3C=C(O)C(O)=C(C3=CC=2C)C(=O)NC[C@H](C)C=2C=CC=CC=2)=CC=CC=C1 RAYNZUHYMMLQQA-ZEQRLZLVSA-N 0.000 claims 2
- UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 claims 2
- QFWCYNPOPKQOKV-UHFFFAOYSA-N 2-(2-amino-3-methoxyphenyl)chromen-4-one Chemical compound COC1=CC=CC(C=2OC3=CC=CC=C3C(=O)C=2)=C1N QFWCYNPOPKQOKV-UHFFFAOYSA-N 0.000 claims 2
- GFMMXOIFOQCCGU-UHFFFAOYSA-N 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide Chemical compound C=1C=C(I)C=C(Cl)C=1NC1=C(F)C(F)=CC=C1C(=O)NOCC1CC1 GFMMXOIFOQCCGU-UHFFFAOYSA-N 0.000 claims 2
- RWEVIPRMPFNTLO-UHFFFAOYSA-N 2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-3-pyridinecarboxamide Chemical compound CN1C(=O)C(C)=CC(C(=O)NOCCO)=C1NC1=CC=C(I)C=C1F RWEVIPRMPFNTLO-UHFFFAOYSA-N 0.000 claims 2
- RQVGFDBMONQTBC-UHFFFAOYSA-N 2-(6,7-dimethoxyquinazolin-4-yl)sulfanyl-5-methyl-1,3,4-thiadiazole Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1SC1=NN=C(C)S1 RQVGFDBMONQTBC-UHFFFAOYSA-N 0.000 claims 2
- AHIVQGOUBLVTCB-AWEZNQCLSA-N 2-[2-fluoro-4-[(2s)-pyrrolidin-2-yl]phenyl]-1h-benzimidazole-4-carboxamide Chemical compound N=1C=2C(C(=O)N)=CC=CC=2NC=1C(C(=C1)F)=CC=C1[C@@H]1CCCN1 AHIVQGOUBLVTCB-AWEZNQCLSA-N 0.000 claims 2
- DDTPGANIPBKTNU-UHFFFAOYSA-N 2-[2-methoxy-4-(4-methyl-1-piperazinyl)anilino]-5,11-dimethyl-6-pyrimido[4,5-b][1,4]benzodiazepinone Chemical compound C=1C=C(NC=2N=C3N(C)C4=CC=CC=C4C(=O)N(C)C3=CN=2)C(OC)=CC=1N1CCN(C)CC1 DDTPGANIPBKTNU-UHFFFAOYSA-N 0.000 claims 2
- TWYCZJMOEMMCGC-UHFFFAOYSA-N 2-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-n-(1-propan-2-ylpyrazol-4-yl)acetamide Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1OC(C=C1)=CC=C1CC(=O)NC=1C=NN(C(C)C)C=1 TWYCZJMOEMMCGC-UHFFFAOYSA-N 0.000 claims 2
- WUGANDSUVKXMEC-UHFFFAOYSA-N 2-[4-[(4-bromophenyl)sulfonylamino]-1-hydroxynaphthalen-2-yl]sulfanylacetic acid Chemical compound C=12C=CC=CC2=C(O)C(SCC(=O)O)=CC=1NS(=O)(=O)C1=CC=C(Br)C=C1 WUGANDSUVKXMEC-UHFFFAOYSA-N 0.000 claims 2
- RMNLLPXCNDZJMJ-IDVLALEDSA-N 2-[[(1r,2s)-2-aminocyclohexyl]amino]-4-[3-(triazol-2-yl)anilino]pyrimidine-5-carboxamide;hydrochloride Chemical compound Cl.N[C@H]1CCCC[C@H]1NC1=NC=C(C(N)=O)C(NC=2C=C(C=CC=2)N2N=CC=N2)=N1 RMNLLPXCNDZJMJ-IDVLALEDSA-N 0.000 claims 2
- HZTYDQRUAWIZRE-UHFFFAOYSA-N 2-[[2-[[1-[2-(dimethylamino)-1-oxoethyl]-5-methoxy-2,3-dihydroindol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide Chemical compound CNC(=O)C1=C(F)C=CC=C1NC1=C2C=CN=C2NC(NC=2C(=CC=3CCN(C=3C=2)C(=O)CN(C)C)OC)=N1 HZTYDQRUAWIZRE-UHFFFAOYSA-N 0.000 claims 2
- CBIAKDAYHRWZCU-UHFFFAOYSA-N 2-bromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC1=CC=C(O)C(Br)=C1 CBIAKDAYHRWZCU-UHFFFAOYSA-N 0.000 claims 2
- QIHBWVVVRYYYRO-ZDUSSCGKSA-N 3-(4-oxo-1h-quinazolin-2-yl)-n-[(1s)-1-phenylethyl]propanamide Chemical compound C1([C@@H](NC(=O)CCC=2NC(=O)C3=CC=CC=C3N=2)C)=CC=CC=C1 QIHBWVVVRYYYRO-ZDUSSCGKSA-N 0.000 claims 2
- FGTCROZDHDSNIO-UHFFFAOYSA-N 3-(4-quinolinylmethylamino)-N-[4-(trifluoromethoxy)phenyl]-2-thiophenecarboxamide Chemical compound C1=CC(OC(F)(F)F)=CC=C1NC(=O)C1=C(NCC=2C3=CC=CC=C3N=CC=2)C=CS1 FGTCROZDHDSNIO-UHFFFAOYSA-N 0.000 claims 2
- PYEFPDQFAZNXLI-UHFFFAOYSA-N 3-(dimethylamino)-N-[3-[[(4-hydroxyphenyl)-oxomethyl]amino]-4-methylphenyl]benzamide Chemical compound CN(C)C1=CC=CC(C(=O)NC=2C=C(NC(=O)C=3C=CC(O)=CC=3)C(C)=CC=2)=C1 PYEFPDQFAZNXLI-UHFFFAOYSA-N 0.000 claims 2
- RCLQNICOARASSR-SECBINFHSA-N 3-[(2r)-2,3-dihydroxypropyl]-6-fluoro-5-(2-fluoro-4-iodoanilino)-8-methylpyrido[2,3-d]pyrimidine-4,7-dione Chemical compound FC=1C(=O)N(C)C=2N=CN(C[C@@H](O)CO)C(=O)C=2C=1NC1=CC=C(I)C=C1F RCLQNICOARASSR-SECBINFHSA-N 0.000 claims 2
- UFKSWYKDQZBJTH-UHFFFAOYSA-N 3-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-5-iodo-1,2-dihydroindol-2-ol Chemical compound OC1NC2=CC=C(I)C=C2C1=CC1=CC(Br)=C(O)C(Br)=C1 UFKSWYKDQZBJTH-UHFFFAOYSA-N 0.000 claims 2
- JUSFANSTBFGBAF-IRXDYDNUSA-N 3-[2,4-bis[(3s)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl]-n-methylbenzamide Chemical compound CNC(=O)C1=CC=CC(C=2N=C3N=C(N=C(C3=CC=2)N2[C@H](COCC2)C)N2[C@H](COCC2)C)=C1 JUSFANSTBFGBAF-IRXDYDNUSA-N 0.000 claims 2
- OCUQMWSIGPQEMX-UHFFFAOYSA-N 3-[3-[N-[4-[(dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-1H-indol-6-yl]-N-ethylprop-2-ynamide Chemical compound CCNC(=O)C#CC1=CC2=C(C=C1)C(=C(N2)O)C(=NC3=CC=C(C=C3)CN(C)C)C4=CC=CC=C4 OCUQMWSIGPQEMX-UHFFFAOYSA-N 0.000 claims 2
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical compound NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 claims 2
- ZGXOBLVQIVXKEB-UHFFFAOYSA-N 3-[N-[3-[(dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-N,N-dimethyl-1H-indole-6-carboxamide Chemical compound CN(C)CC1=CC(=CC=C1)N=C(C2=CC=CC=C2)C3=C(NC4=C3C=CC(=C4)C(=O)N(C)C)O ZGXOBLVQIVXKEB-UHFFFAOYSA-N 0.000 claims 2
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- 229960004891 lapatinib Drugs 0.000 claims 1
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- PDYXPCKITKHFOZ-UHFFFAOYSA-N n-[4-(2-amino-3-chloropyridin-4-yl)oxy-3-fluorophenyl]-5-(4-fluorophenyl)-4-oxo-1h-pyridine-3-carboxamide Chemical compound NC1=NC=CC(OC=2C(=CC(NC(=O)C=3C(C(C=4C=CC(F)=CC=4)=CNC=3)=O)=CC=2)F)=C1Cl PDYXPCKITKHFOZ-UHFFFAOYSA-N 0.000 claims 1
- YRCHYHRCBXNYNU-UHFFFAOYSA-N n-[[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-(4-fluorophenyl)acetamide Chemical compound N1=CC(CNCCOC)=CC=C1C1=CC2=NC=CC(OC=3C(=CC(NC(=S)NC(=O)CC=4C=CC(F)=CC=4)=CC=3)F)=C2S1 YRCHYHRCBXNYNU-UHFFFAOYSA-N 0.000 claims 1
- 229960003301 nivolumab Drugs 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229960000940 tivozanib Drugs 0.000 claims 1
- 235000013976 turmeric Nutrition 0.000 claims 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 1
- 229960000241 vandetanib Drugs 0.000 claims 1
- UHTHHESEBZOYNR-UHFFFAOYSA-N vandetanib Chemical compound COC1=CC(C(/N=CN2)=N/C=3C(=CC(Br)=CC=3)F)=C2C=C1OCC1CCN(C)CC1 UHTHHESEBZOYNR-UHFFFAOYSA-N 0.000 claims 1
- 229950001576 voxtalisib Drugs 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/69—Boron compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1514760.6A GB201514760D0 (en) | 2015-08-19 | 2015-08-19 | Compounds and method of use |
| PCT/GB2016/052575 WO2017029517A1 (en) | 2015-08-19 | 2016-08-19 | Compositions comprising phosphoinositide 3-kinase inhibitors and a second antiproliferative agent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| FI3337477T3 true FI3337477T3 (fi) | 2023-04-27 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| FIEP16756763.5T FI3337477T3 (fi) | 2015-08-19 | 2016-08-19 | Koostumukset, jotka käsittävät fosfoinositidi-3-kinaasin estäjiä ja toista antiproliferatiivista ainetta |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US10668077B2 (https=) |
| EP (1) | EP3337477B1 (https=) |
| JP (1) | JP2018523689A (https=) |
| KR (1) | KR20180064387A (https=) |
| CN (2) | CN113786409B (https=) |
| AU (1) | AU2016307885B2 (https=) |
| CA (1) | CA2995898A1 (https=) |
| DK (1) | DK3337477T3 (https=) |
| ES (1) | ES2939815T3 (https=) |
| FI (1) | FI3337477T3 (https=) |
| GB (1) | GB201514760D0 (https=) |
| HR (1) | HRP20230376T1 (https=) |
| HU (1) | HUE061615T2 (https=) |
| IL (1) | IL257499A (https=) |
| LT (1) | LT3337477T (https=) |
| MX (1) | MX2018001926A (https=) |
| PL (1) | PL3337477T3 (https=) |
| PT (1) | PT3337477T (https=) |
| RS (1) | RS64095B1 (https=) |
| SI (1) | SI3337477T1 (https=) |
| SM (1) | SMT202300063T1 (https=) |
| WO (1) | WO2017029517A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2012002059A (es) | 2009-08-20 | 2012-04-19 | Karus Therapeutics Ltd | Compestos heterociclicos triciclicos como inhibidores de fosfoionositida 3-quinasa. |
| GB201204125D0 (en) | 2012-03-08 | 2012-04-25 | Karus Therapeutics Ltd | Compounds |
| GB201402431D0 (en) | 2014-02-12 | 2014-03-26 | Karus Therapeutics Ltd | Compounds |
| US10722527B2 (en) | 2015-04-10 | 2020-07-28 | Capsugel Belgium Nv | Abiraterone acetate lipid formulations |
| GB201514754D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds |
| GB201514758D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Formulation |
| GB201514760D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds and method of use |
| GB201514751D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds |
| CN113164466B (zh) * | 2018-09-11 | 2025-07-08 | 柯瑞斯公司 | 使用具有锌结合部分的磷酸肌醇3-激酶抑制剂的联合治疗 |
| WO2020059705A1 (ja) * | 2018-09-18 | 2020-03-26 | 株式会社ヤクルト本社 | キノリンカルボキサミド誘導体を用いるがん併用療法 |
| EP3930715B1 (en) * | 2019-02-27 | 2024-05-08 | Astrazeneca AB | Saracatinib for use in the treatment of idiopathic pulmonary fibrosis |
| CN111904958B (zh) * | 2019-05-09 | 2022-09-13 | 浙江大学 | Umi-77作为线粒体自噬诱导剂在制备治疗炎症及神经退行性疾病药物中的应用 |
| GB201909468D0 (en) * | 2019-07-01 | 2019-08-14 | Karus Therapeutics Ltd | Compounds for treating cancer |
| CN114533879B (zh) * | 2020-11-19 | 2023-09-29 | 广州顺健生物医药科技有限公司 | 治疗癌症的联合疗法 |
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| BE786081A (fr) * | 1971-07-13 | 1973-01-10 | Uniroyal Sa | Appareil et procede pour maintenir les tringles des bourrelets de pneu |
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| GB201321738D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic Agents |
| GB201321728D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201321729D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201321730D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201402431D0 (en) * | 2014-02-12 | 2014-03-26 | Karus Therapeutics Ltd | Compounds |
| MA40933A (fr) | 2014-11-11 | 2017-09-19 | Piqur Therapeutics Ag | Difluorométhyl-aminopyridines et difluorométhyl-aminopyrimidines |
| GB201514756D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compound and method of use |
| GB201514758D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Formulation |
| GB201514751D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds |
| GB201514754D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds |
| GB201514760D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds and method of use |
| GB201909468D0 (en) | 2019-07-01 | 2019-08-14 | Karus Therapeutics Ltd | Compounds for treating cancer |
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2015
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2016
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- 2016-08-19 HR HRP20230376TT patent/HRP20230376T1/hr unknown
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- 2016-08-19 LT LTEPPCT/GB2016/052575T patent/LT3337477T/lt unknown
- 2016-08-19 US US15/753,353 patent/US10668077B2/en active Active
- 2016-08-19 FI FIEP16756763.5T patent/FI3337477T3/fi active
- 2016-08-19 JP JP2018508757A patent/JP2018523689A/ja not_active Withdrawn
- 2016-08-19 KR KR1020187007564A patent/KR20180064387A/ko not_active Withdrawn
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2022
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| DK3337477T3 (en) | 2023-02-20 |
| US20180243313A1 (en) | 2018-08-30 |
| EP3337477A1 (en) | 2018-06-27 |
| ES2939815T3 (es) | 2023-04-27 |
| US10668077B2 (en) | 2020-06-02 |
| GB201514760D0 (en) | 2015-09-30 |
| CN108348505A (zh) | 2018-07-31 |
| LT3337477T (lt) | 2023-03-10 |
| AU2016307885A1 (en) | 2018-03-08 |
| PT3337477T (pt) | 2023-03-20 |
| PL3337477T3 (pl) | 2023-07-03 |
| HK1251467A1 (en) | 2019-02-01 |
| JP2018523689A (ja) | 2018-08-23 |
| CA2995898A1 (en) | 2017-02-23 |
| AU2016307885B2 (en) | 2019-07-25 |
| US12257254B2 (en) | 2025-03-25 |
| CN108348505B (zh) | 2021-10-12 |
| IL257499A (en) | 2018-07-31 |
| RS64095B1 (sr) | 2023-04-28 |
| EP3337477B1 (en) | 2023-02-01 |
| HRP20230376T1 (hr) | 2023-06-23 |
| HUE061615T2 (hu) | 2023-07-28 |
| MX2018001926A (es) | 2018-06-19 |
| CN113786409A (zh) | 2021-12-14 |
| CN113786409B (zh) | 2024-04-02 |
| US20230066999A1 (en) | 2023-03-02 |
| WO2017029517A1 (en) | 2017-02-23 |
| US20210069200A1 (en) | 2021-03-11 |
| KR20180064387A (ko) | 2018-06-14 |
| US11291669B2 (en) | 2022-04-05 |
| SI3337477T1 (sl) | 2023-04-28 |
| SMT202300063T1 (it) | 2023-03-17 |
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