HRP20230376T1 - Sastav koji sadrži inhibitore fosfoinozitid 3-kinaze i drugo antiproliferativno sredstvo - Google Patents
Sastav koji sadrži inhibitore fosfoinozitid 3-kinaze i drugo antiproliferativno sredstvo Download PDFInfo
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- HRP20230376T1 HRP20230376T1 HRP20230376TT HRP20230376T HRP20230376T1 HR P20230376 T1 HRP20230376 T1 HR P20230376T1 HR P20230376T T HRP20230376T T HR P20230376TT HR P20230376 T HRP20230376 T HR P20230376T HR P20230376 T1 HRP20230376 T1 HR P20230376T1
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- 239000000203 mixture Substances 0.000 title claims 15
- 239000003795 chemical substances by application Substances 0.000 title claims 13
- 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 10
- 206010028980 Neoplasm Diseases 0.000 claims 9
- 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
- 229940079156 Proteasome inhibitor Drugs 0.000 claims 5
- 239000003207 proteasome inhibitor Substances 0.000 claims 5
- 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
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- 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 4
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- 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 3
- 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 3
- 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
- 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 3
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- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 3
- IIQUYGWWHIHOCF-UHFFFAOYSA-N n-(2-hydroxyethyl)-3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide Chemical compound OCCNC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 IIQUYGWWHIHOCF-UHFFFAOYSA-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
- 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
- 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
- KQJSQWZMSAGSHN-UHFFFAOYSA-N (9beta,13alpha,14beta,20alpha)-3-hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid Natural products CC12CCC3(C)C4CC(C)(C(O)=O)CCC4(C)CCC3(C)C2=CC=C2C1=CC(=O)C(O)=C2C KQJSQWZMSAGSHN-UHFFFAOYSA-N 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
- PZIRTMUUDNWDHP-BGPOSVGRSA-N (e)-2-cyano-n-[2-[[(e)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enoyl]amino]ethyl]-3-(3,4-dihydroxyphenyl)prop-2-enamide Chemical compound C1=C(O)C(O)=CC=C1\C=C(/C#N)C(=O)NCCNC(=O)C(\C#N)=C\C1=CC=C(O)C(O)=C1 PZIRTMUUDNWDHP-BGPOSVGRSA-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
- 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
- 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
- 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
- PFMPOBVAYMTUOX-GOSISDBHSA-N 2-amino-1-ethyl-7-[(3r)-3-hydroxy-4-methoxy-3-methylbut-1-ynyl]-n-methyl-4-oxo-1,8-naphthyridine-3-carboxamide Chemical compound C1=C(C#C[C@@](C)(O)COC)N=C2N(CC)C(N)=C(C(=O)NC)C(=O)C2=C1 PFMPOBVAYMTUOX-GOSISDBHSA-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
- 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
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- 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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- WRLVHADVOGFZOZ-UHFFFAOYSA-N 4-[(2-ethoxyphenyl)diazenyl]-5-methyl-2-(4-phenyl-1,3-thiazol-2-yl)-1H-pyrazol-3-one Chemical compound CCOC1=CC=CC=C1N=NC2=C(NN(C2=O)C3=NC(=CS3)C4=CC=CC=C4)C WRLVHADVOGFZOZ-UHFFFAOYSA-N 0.000 claims 2
- XXJWYDDUDKYVKI-UHFFFAOYSA-N 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]quinazoline Chemical compound COC1=CC2=C(OC=3C(=C4C=C(C)NC4=CC=3)F)N=CN=C2C=C1OCCCN1CCCC1 XXJWYDDUDKYVKI-UHFFFAOYSA-N 0.000 claims 2
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- UQRCJCNVNUFYDX-UHFFFAOYSA-N Golvatinib Chemical compound C1CN(C)CCN1C1CCN(C(=O)NC=2N=CC=C(OC=3C=C(F)C(NC(=O)C4(CC4)C(=O)NC=4C=CC(F)=CC=4)=CC=3)C=2)CC1 UQRCJCNVNUFYDX-UHFFFAOYSA-N 0.000 claims 1
- 239000003798 L01XE11 - Pazopanib Substances 0.000 claims 1
- 239000002118 L01XE12 - Vandetanib Substances 0.000 claims 1
- 239000012820 MEK1 Inhibitor Substances 0.000 claims 1
- YHUIUSRCUKUUQA-UHFFFAOYSA-N N-(4-chloro-2-fluorophenyl)-6,7-dimethoxy-4-quinazolinamine Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC1=CC=C(Cl)C=C1F YHUIUSRCUKUUQA-UHFFFAOYSA-N 0.000 claims 1
- VIUAUNHCRHHYNE-JTQLQIEISA-N N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)-4-pyridinecarboxamide Chemical compound OC[C@@H](O)CNC(=O)C1=CC=NC=C1NC1=CC=C(I)C=C1F VIUAUNHCRHHYNE-JTQLQIEISA-N 0.000 claims 1
- CXQHYVUVSFXTMY-UHFFFAOYSA-N N1'-[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide Chemical compound C1=CN=C2C=C(OCCCN3CCOCC3)C(OC)=CC2=C1OC(C(=C1)F)=CC=C1NC(=O)C1(C(=O)NC=2C=CC(F)=CC=2)CC1 CXQHYVUVSFXTMY-UHFFFAOYSA-N 0.000 claims 1
- 241000364051 Pima Species 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 229960003982 apatinib Drugs 0.000 claims 1
- 229950008692 foretinib Drugs 0.000 claims 1
- 229950010662 golvatinib Drugs 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 229960003784 lenvatinib Drugs 0.000 claims 1
- WOSKHXYHFSIKNG-UHFFFAOYSA-N lenvatinib Chemical compound C=12C=C(C(N)=O)C(OC)=CC2=NC=CC=1OC(C=C1Cl)=CC=C1NC(=O)NC1CC1 WOSKHXYHFSIKNG-UHFFFAOYSA-N 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- WPEWQEMJFLWMLV-UHFFFAOYSA-N n-[4-(1-cyanocyclopentyl)phenyl]-2-(pyridin-4-ylmethylamino)pyridine-3-carboxamide Chemical compound C=1C=CN=C(NCC=2C=CN=CC=2)C=1C(=O)NC(C=C1)=CC=C1C1(C#N)CCCC1 WPEWQEMJFLWMLV-UHFFFAOYSA-N 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
- 229960000639 pazopanib Drugs 0.000 claims 1
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- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
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- CRDZYJSQHCXHEG-SFVBTVKNSA-N protectin D1 Chemical compound CC\C=C/C[C@H](O)\C=C/C=C/C=C/[C@H](O)C\C=C/C\C=C/CCC(O)=O CRDZYJSQHCXHEG-SFVBTVKNSA-N 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229960000940 tivozanib 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
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
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- 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
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- 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
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- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| 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 |
| EP16756763.5A EP3337477B1 (en) | 2015-08-19 | 2016-08-19 | Compositions comprising phosphoinositide 3-kinase inhibitors and a second antiproliferative agent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20230376T1 true HRP20230376T1 (hr) | 2023-06-23 |
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Family Applications (1)
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|---|---|---|---|
| HRP20230376TT HRP20230376T1 (hr) | 2015-08-19 | 2016-08-19 | Sastav koji sadrži inhibitore fosfoinozitid 3-kinaze i drugo antiproliferativno sredstvo |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US10668077B2 (enExample) |
| EP (1) | EP3337477B1 (enExample) |
| JP (1) | JP2018523689A (enExample) |
| KR (1) | KR20180064387A (enExample) |
| CN (2) | CN108348505B (enExample) |
| AU (1) | AU2016307885B2 (enExample) |
| CA (1) | CA2995898A1 (enExample) |
| DK (1) | DK3337477T3 (enExample) |
| ES (1) | ES2939815T3 (enExample) |
| FI (1) | FI3337477T3 (enExample) |
| GB (1) | GB201514760D0 (enExample) |
| HR (1) | HRP20230376T1 (enExample) |
| HU (1) | HUE061615T2 (enExample) |
| IL (1) | IL257499A (enExample) |
| LT (1) | LT3337477T (enExample) |
| MX (1) | MX2018001926A (enExample) |
| PL (1) | PL3337477T3 (enExample) |
| PT (1) | PT3337477T (enExample) |
| RS (1) | RS64095B1 (enExample) |
| SI (1) | SI3337477T1 (enExample) |
| SM (1) | SMT202300063T1 (enExample) |
| WO (1) | WO2017029517A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2010286168B2 (en) | 2009-08-20 | 2014-05-15 | Karus Therapeutics Limited | Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors |
| 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 |
| 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 |
| GB201514758D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Formulation |
| JP7467423B2 (ja) * | 2018-09-11 | 2024-04-15 | キュリス，インコーポレイテッド | 亜鉛結合部分を有するホスホイノシチド３－キナーゼ阻害剤との併用療法 |
| AU2019341976A1 (en) * | 2018-09-18 | 2021-04-15 | General Incorporated Association Pharma Valley Project Supporting Organization | Cancer combination therapy using quinoline carboxamide derivative |
| PT3930715T (pt) * | 2019-02-27 | 2024-08-02 | Astrazeneca Ab | Saracatinib para uso no tratamento de fibrose pulmonar idiopática |
| 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 |
| WO2022105836A1 (en) * | 2020-11-19 | 2022-05-27 | Guangzhou Healthquest Pharma Co., Ltd. | Combination therapies for treating cancer |
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| DE1445742A1 (de) | 1963-11-06 | 1968-12-19 | Bayer Ag | Verfahren zur Herstellung von 2-Stellung substituierten Benzoxazinonen |
| US4017500A (en) | 1973-07-16 | 1977-04-12 | Schering Corporation | Certain 8-amino-1,7-naphthyridines |
| BE786081A (fr) * | 1971-07-13 | 1973-01-10 | Uniroyal Sa | Appareil et procede pour maintenir les tringles des bourrelets de pneu |
| US5703075A (en) | 1988-12-21 | 1997-12-30 | Pharmacia & Upjohn Company | Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones |
| CN1250294A (zh) * | 1999-07-27 | 2000-04-12 | 邮电部武汉邮电科学研究院 | 以太网与同步数字体系或同步光网络融合的适配方法 |
| NZ516616A (en) | 1999-08-03 | 2003-07-25 | Lilly Icos Llc | Beta-carboline pharmaceutical compositions |
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| US6905669B2 (en) | 2001-04-24 | 2005-06-14 | Supergen, Inc. | Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase |
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| KR20080016659A (ko) | 2005-05-20 | 2008-02-21 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제의 억제제로서 유용한 피롤로피리딘 |
| JP2009523812A (ja) | 2006-01-19 | 2009-06-25 | オーエスアイ・ファーマスーティカルズ・インコーポレーテッド | 融合へテロ二環式キナーゼ阻害剤 |
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| EP2035436B1 (en) | 2006-06-26 | 2011-05-25 | UCB Pharma S.A. | Fused thiazole derivatives as kinase inhibitors |
| CN101501035B (zh) * | 2006-08-08 | 2013-01-23 | 中外制药株式会社 | 作为pi3k抑制剂的嘧啶衍生物及其用途 |
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| EP2154965A4 (en) | 2007-05-29 | 2011-08-17 | Glaxosmithkline Llc | NAPHTHYRIDINE DERIVATIVES AS P13 KINASE INHIBITORS |
| GB0710528D0 (en) | 2007-06-01 | 2007-07-11 | Glaxo Group Ltd | Novel compounds |
| AU2008298948B2 (en) * | 2007-09-12 | 2014-09-04 | F. Hoffmann-La Roche Ag | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| WO2010015520A1 (de) | 2008-08-05 | 2010-02-11 | Boehringer Ingelheim International Gmbh | Substituierte naphthyridine und ihre verwendung als arzneimittel |
| CA2742550A1 (en) | 2008-10-03 | 2010-04-08 | Merck Serono S.A. | 4-morpholino-pyrido[3,2-d]pyrimidines |
| GB2465405A (en) | 2008-11-10 | 2010-05-19 | Univ Basel | Triazine, pyrimidine and pyridine analogues and their use in therapy |
| US8981087B2 (en) | 2009-07-29 | 2015-03-17 | Karus Therapeutics Limited | Benzo [E] [1,3] oxazin-4-one derivatives as phosphoinositide 3-kinase inhibitors |
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| US20110207736A1 (en) | 2009-12-23 | 2011-08-25 | Gatekeeper Pharmaceuticals, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| GB201007347D0 (en) | 2010-04-30 | 2010-06-16 | Karus Therapeutics Ltd | Compounds |
| CN101849934B (zh) * | 2010-05-25 | 2011-11-09 | 苏州大学 | 一种磷脂酰肌醇-3-激酶抑制剂及其应用 |
| EP2518070A1 (en) | 2011-04-29 | 2012-10-31 | Almirall, S.A. | Pyrrolotriazinone derivatives as PI3K inhibitors |
| MY161925A (en) | 2011-07-27 | 2017-05-15 | Astrazeneca Ab | 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer |
| WO2013017480A1 (en) | 2011-07-29 | 2013-02-07 | Cellzome Limited | Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors |
| GB201204125D0 (en) | 2012-03-08 | 2012-04-25 | Karus Therapeutics Ltd | Compounds |
| EP3181564B1 (en) | 2012-11-20 | 2019-09-18 | H. Hoffnabb-La Roche Ag | Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants |
| ES2688815T3 (es) | 2013-05-10 | 2018-11-07 | Karus Therapeutics Limited | Inhibidores de histona desacetilasa novedosos |
| ES2834638T3 (es) * | 2013-05-30 | 2021-06-18 | Infinity Pharmaceuticals Inc | Tratamiento de cánceres usando moduladores de isoforma de PI3 cinasa |
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| 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 |
| GB201321728D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201321738D0 (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 |
| GB201514754D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds |
| GB201514751D0 (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 |
| GB201514756D0 (en) * | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compound and method of use |
| GB201909468D0 (en) | 2019-07-01 | 2019-08-14 | Karus Therapeutics Ltd | Compounds for treating cancer |
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2015
- 2015-08-19 GB GBGB1514760.6A patent/GB201514760D0/en not_active Ceased
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2016
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- 2016-08-19 KR KR1020187007564A patent/KR20180064387A/ko not_active Withdrawn
- 2016-08-19 PL PL16756763.5T patent/PL3337477T3/pl unknown
- 2016-08-19 DK DK16756763.5T patent/DK3337477T3/da active
- 2016-08-19 CN CN201680057437.6A patent/CN108348505B/zh active Active
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- 2016-08-19 MX MX2018001926A patent/MX2018001926A/es unknown
- 2016-08-19 SI SI201631666T patent/SI3337477T1/sl unknown
- 2016-08-19 CN CN202111104917.2A patent/CN113786409B/zh active Active
- 2016-08-19 LT LTEPPCT/GB2016/052575T patent/LT3337477T/lt unknown
- 2016-08-19 CA CA2995898A patent/CA2995898A1/en not_active Abandoned
- 2016-08-19 AU AU2016307885A patent/AU2016307885B2/en not_active Ceased
- 2016-08-19 PT PT167567635T patent/PT3337477T/pt unknown
- 2016-08-19 EP EP16756763.5A patent/EP3337477B1/en active Active
- 2016-08-19 ES ES16756763T patent/ES2939815T3/es active Active
- 2016-08-19 SM SM20230063T patent/SMT202300063T1/it unknown
- 2016-08-19 WO PCT/GB2016/052575 patent/WO2017029517A1/en not_active Ceased
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- 2016-08-19 HU HUE16756763A patent/HUE061615T2/hu unknown
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2018
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2020
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2022
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Also Published As
| Publication number | Publication date |
|---|---|
| EP3337477A1 (en) | 2018-06-27 |
| ES2939815T3 (es) | 2023-04-27 |
| US20180243313A1 (en) | 2018-08-30 |
| JP2018523689A (ja) | 2018-08-23 |
| SI3337477T1 (sl) | 2023-04-28 |
| RS64095B1 (sr) | 2023-04-28 |
| IL257499A (en) | 2018-07-31 |
| KR20180064387A (ko) | 2018-06-14 |
| US11291669B2 (en) | 2022-04-05 |
| DK3337477T3 (en) | 2023-02-20 |
| HUE061615T2 (hu) | 2023-07-28 |
| MX2018001926A (es) | 2018-06-19 |
| CA2995898A1 (en) | 2017-02-23 |
| AU2016307885B2 (en) | 2019-07-25 |
| PL3337477T3 (pl) | 2023-07-03 |
| US20230066999A1 (en) | 2023-03-02 |
| CN108348505B (zh) | 2021-10-12 |
| EP3337477B1 (en) | 2023-02-01 |
| SMT202300063T1 (it) | 2023-03-17 |
| LT3337477T (lt) | 2023-03-10 |
| PT3337477T (pt) | 2023-03-20 |
| AU2016307885A1 (en) | 2018-03-08 |
| CN108348505A (zh) | 2018-07-31 |
| US12257254B2 (en) | 2025-03-25 |
| US20210069200A1 (en) | 2021-03-11 |
| CN113786409B (zh) | 2024-04-02 |
| US10668077B2 (en) | 2020-06-02 |
| GB201514760D0 (en) | 2015-09-30 |
| FI3337477T3 (fi) | 2023-04-27 |
| HK1251467A1 (en) | 2019-02-01 |
| CN113786409A (zh) | 2021-12-14 |
| WO2017029517A1 (en) | 2017-02-23 |
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