RU2004127869A - Новые лекарственные композиции на основе антихолинергических средств и ингибиторов egfr-киназы - Google Patents
Новые лекарственные композиции на основе антихолинергических средств и ингибиторов egfr-киназы Download PDFInfo
- Publication number
- RU2004127869A RU2004127869A RU2004127869/15A RU2004127869A RU2004127869A RU 2004127869 A RU2004127869 A RU 2004127869A RU 2004127869/15 A RU2004127869/15 A RU 2004127869/15A RU 2004127869 A RU2004127869 A RU 2004127869A RU 2004127869 A RU2004127869 A RU 2004127869A
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- RU
- Russia
- Prior art keywords
- amino
- chloro
- fluorophenyl
- buten
- oxo
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims 10
- 239000000812 cholinergic antagonist Substances 0.000 title claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 title claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 title claims 2
- 229940043355 kinase inhibitor Drugs 0.000 title claims 2
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 title claims 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 title claims 2
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 title 1
- 239000003814 drug Substances 0.000 claims 15
- 229940079593 drug Drugs 0.000 claims 14
- 239000013543 active substance Substances 0.000 claims 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- -1 3-chloro-4-fluorophenyl Chemical group 0.000 claims 5
- MPIZUARKKMOKKZ-INIZCTEOSA-N n-[4-(3-chloro-4-fluoroanilino)-7-[4-[(2s)-2-methyl-6-oxomorpholin-4-yl]butoxy]quinazolin-6-yl]prop-2-enamide Chemical compound C1C(=O)O[C@@H](C)CN1CCCCOC1=CC2=NC=NC(NC=3C=C(Cl)C(F)=CC=3)=C2C=C1NC(=O)C=C MPIZUARKKMOKKZ-INIZCTEOSA-N 0.000 claims 4
- 239000003380 propellant Substances 0.000 claims 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- ODRFRBOBDWUQES-UHFFFAOYSA-N ethyl 3-[[4-[[4-(3-chloro-4-fluoroanilino)-7-(cyclopropylmethoxy)quinazolin-6-yl]amino]-4-oxobut-2-enyl]-(2-ethoxy-2-oxoethyl)amino]propanoate Chemical compound N1=CN=C2C=C(OCC3CC3)C(NC(=O)C=CCN(CCC(=O)OCC)CC(=O)OCC)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ODRFRBOBDWUQES-UHFFFAOYSA-N 0.000 claims 3
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 3
- ZIISKCSUEHVFLY-AWEZNQCLSA-N n-[4-(3-chloro-4-fluoroanilino)-7-[2-[(2s)-2-methyl-6-oxomorpholin-4-yl]ethoxy]quinazolin-6-yl]prop-2-enamide Chemical compound C1C(=O)O[C@@H](C)CN1CCOC1=CC2=NC=NC(NC=3C=C(Cl)C(F)=CC=3)=C2C=C1NC(=O)C=C ZIISKCSUEHVFLY-AWEZNQCLSA-N 0.000 claims 3
- QLVAINZHTQIWQM-QHCPKHFHSA-N n-[4-(3-chloro-4-fluoroanilino)-7-[2-[4-[(2s)-5-oxooxolane-2-carbonyl]piperazin-1-yl]ethoxy]quinazolin-6-yl]prop-2-enamide Chemical compound C1=C(Cl)C(F)=CC=C1NC1=NC=NC2=CC(OCCN3CCN(CC3)C(=O)[C@H]3OC(=O)CC3)=C(NC(=O)C=C)C=C12 QLVAINZHTQIWQM-QHCPKHFHSA-N 0.000 claims 3
- SBXDXDHBBHYRGU-HXUWFJFHSA-N n-[7-(cyclopropylmethoxy)-4-[[(1r)-1-phenylethyl]amino]quinazolin-6-yl]-4-morpholin-4-ylbut-2-enamide Chemical compound N([C@H](C)C=1C=CC=CC=1)C(C1=CC=2NC(=O)C=CCN3CCOCC3)=NC=NC1=CC=2OCC1CC1 SBXDXDHBBHYRGU-HXUWFJFHSA-N 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- YTKFKKLZSIVJMX-ZDUSSCGKSA-N (6s)-4-[2-[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-yl]oxyethyl]-6-methylmorpholin-2-one Chemical compound C=12C=C(OCCN3CC(=O)O[C@@H](C)C3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 YTKFKKLZSIVJMX-ZDUSSCGKSA-N 0.000 claims 2
- 125000004343 1-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- AZHVHFBKXHCSIL-JOCHJYFZSA-N 4-[bis(2-methoxyethyl)amino]-n-[7-(cyclopropylmethoxy)-4-[[(1r)-1-phenylethyl]amino]quinazolin-6-yl]but-2-enamide Chemical compound C1([C@@H](C)NC2=C3C=C(C(=CC3=NC=N2)OCC2CC2)NC(=O)C=CCN(CCOC)CCOC)=CC=CC=C1 AZHVHFBKXHCSIL-JOCHJYFZSA-N 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims 2
- 239000000443 aerosol Substances 0.000 claims 2
- 150000002016 disaccharides Chemical class 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 150000004676 glycans Chemical class 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 229940041682 inhalant solution Drugs 0.000 claims 2
- 150000002772 monosaccharides Chemical class 0.000 claims 2
- ARFWPHOPKFABNZ-UHFFFAOYSA-N n-[4-(3-chloro-4-fluoroanilino)-7-(cyclopropylmethoxy)quinazolin-6-yl]-4-(diethylamino)but-2-enamide Chemical compound N1=CN=C2C=C(OCC3CC3)C(NC(=O)C=CCN(CC)CC)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ARFWPHOPKFABNZ-UHFFFAOYSA-N 0.000 claims 2
- BHEXDWNZKZGCJR-UHFFFAOYSA-N n-[4-(3-chloro-4-fluoroanilino)-7-(cyclopropylmethoxy)quinazolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound N1=CN=C2C=C(OCC3CC3)C(NC(=O)C=CCN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 BHEXDWNZKZGCJR-UHFFFAOYSA-N 0.000 claims 2
- RZWHMWFZGYRQSS-LJQANCHMSA-N n-[4-(3-chloro-4-fluoroanilino)-7-(cyclopropylmethoxy)quinazolin-6-yl]-4-[(2r)-2-(methoxymethyl)-6-oxomorpholin-4-yl]but-2-enamide Chemical compound C1C(=O)O[C@@H](COC)CN1CC=CC(=O)NC(C(=CC1=NC=N2)OCC3CC3)=CC1=C2NC1=CC=C(F)C(Cl)=C1 RZWHMWFZGYRQSS-LJQANCHMSA-N 0.000 claims 2
- CCOKBACMAWRBJZ-MRXNPFEDSA-N n-[4-(3-chloro-4-fluoroanilino)-7-(cyclopropylmethoxy)quinazolin-6-yl]-4-[(2r)-2-methyl-6-oxomorpholin-4-yl]but-2-enamide Chemical compound C1C(=O)O[C@H](C)CN1CC=CC(=O)NC(C(=CC1=NC=N2)OCC3CC3)=CC1=C2NC1=CC=C(F)C(Cl)=C1 CCOKBACMAWRBJZ-MRXNPFEDSA-N 0.000 claims 2
- KMAPIHHPUBUULD-UHFFFAOYSA-N n-[4-(3-chloro-4-fluoroanilino)-7-(cyclopropylmethoxy)quinazolin-6-yl]-4-[2-methoxyethyl(methyl)amino]but-2-enamide Chemical compound N1=CN=C2C=C(OCC3CC3)C(NC(=O)C=CCN(C)CCOC)=CC2=C1NC1=CC=C(F)C(Cl)=C1 KMAPIHHPUBUULD-UHFFFAOYSA-N 0.000 claims 2
- PQTDSJWQNYBZMA-UHFFFAOYSA-N n-[4-(3-chloro-4-fluoroanilino)-7-(cyclopropylmethoxy)quinazolin-6-yl]-4-morpholin-4-ylbut-2-enamide Chemical compound C1=C(Cl)C(F)=CC=C1NC(C1=C2)=NC=NC1=CC(OCC1CC1)=C2NC(=O)C=CCN1CCOCC1 PQTDSJWQNYBZMA-UHFFFAOYSA-N 0.000 claims 2
- ULXXDDBFHOBEHA-MRXNPFEDSA-N n-[4-(3-chloro-4-fluoroanilino)-7-[(3r)-oxolan-3-yl]oxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound N1=CN=C2C=C(O[C@H]3COCC3)C(NC(=O)C=CCN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-MRXNPFEDSA-N 0.000 claims 2
- YHDXPFVJAIHRAS-AEFFLSMTSA-N n-[4-(3-chloro-4-fluoroanilino)-7-[(3s)-oxolan-3-yl]oxyquinazolin-6-yl]-4-[(2r)-2-methyl-6-oxomorpholin-4-yl]but-2-enamide Chemical compound C1C(=O)O[C@H](C)CN1CC=CC(=O)NC(C(=CC1=NC=N2)O[C@@H]3COCC3)=CC1=C2NC1=CC=C(F)C(Cl)=C1 YHDXPFVJAIHRAS-AEFFLSMTSA-N 0.000 claims 2
- MPIZUARKKMOKKZ-MRXNPFEDSA-N n-[4-(3-chloro-4-fluoroanilino)-7-[4-[(2r)-2-methyl-6-oxomorpholin-4-yl]butoxy]quinazolin-6-yl]prop-2-enamide Chemical compound C1C(=O)O[C@H](C)CN1CCCCOC1=CC2=NC=NC(NC=3C=C(Cl)C(F)=CC=3)=C2C=C1NC(=O)C=C MPIZUARKKMOKKZ-MRXNPFEDSA-N 0.000 claims 2
- UIJGHCUIUFFXJL-QGZVFWFLSA-N n-[4-(3-chloro-4-fluoroanilino)-7-[[(2r)-oxolan-2-yl]methoxy]quinazolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound N1=CN=C2C=C(OC[C@@H]3OCCC3)C(NC(=O)C=CCN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 UIJGHCUIUFFXJL-QGZVFWFLSA-N 0.000 claims 2
- GWFMAFOGZMQEDM-UHFFFAOYSA-N n-[4-(3-chloro-4-fluoroanilino)-7-cyclopentyloxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound N1=CN=C2C=C(OC3CCCC3)C(NC(=O)C=CCN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 GWFMAFOGZMQEDM-UHFFFAOYSA-N 0.000 claims 2
- UBUIJVSWEKUFRP-UHFFFAOYSA-N n-[4-(3-chloro-4-fluoroanilino)-7-cyclopentyloxyquinazolin-6-yl]-4-[cyclopropyl(methyl)amino]but-2-enamide Chemical compound C1CC1N(C)CC=CC(=O)NC(C(=CC1=NC=N2)OC3CCCC3)=CC1=C2NC1=CC=C(F)C(Cl)=C1 UBUIJVSWEKUFRP-UHFFFAOYSA-N 0.000 claims 2
- BTSVDJBLKHJYMN-OAQYLSRUSA-N n-[7-(cyclopropylmethoxy)-4-[[(1r)-1-phenylethyl]amino]quinazolin-6-yl]-4-[methyl(oxan-4-yl)amino]but-2-enamide Chemical compound N([C@H](C)C=1C=CC=CC=1)C(C1=CC=2NC(=O)C=CCN(C)C3CCOCC3)=NC=NC1=CC=2OCC1CC1 BTSVDJBLKHJYMN-OAQYLSRUSA-N 0.000 claims 2
- ADOYXBQVLRRQGX-OAQYLSRUSA-N n-[7-cyclopentyloxy-4-[[(1r)-1-phenylethyl]amino]quinazolin-6-yl]-4-morpholin-4-ylbut-2-enamide Chemical compound N([C@H](C)C=1C=CC=CC=1)C(C1=CC=2NC(=O)C=CCN3CCOCC3)=NC=NC1=CC=2OC1CCCC1 ADOYXBQVLRRQGX-OAQYLSRUSA-N 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 150000002482 oligosaccharides Polymers 0.000 claims 2
- 229920001282 polysaccharide Polymers 0.000 claims 2
- 239000005017 polysaccharide Substances 0.000 claims 2
- 239000000843 powder Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 150000005846 sugar alcohols Polymers 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- LERNTVKEWCAPOY-DZZGSBJMSA-N tiotropium Chemical class O([C@H]1C[C@@H]2[N+]([C@H](C1)[C@@H]1[C@H]2O1)(C)C)C(=O)C(O)(C=1SC=CC=1)C1=CC=CS1 LERNTVKEWCAPOY-DZZGSBJMSA-N 0.000 claims 2
- 229940110309 tiotropium Drugs 0.000 claims 2
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- XRYJULCDUUATMC-CYBMUJFWSA-N 4-[4-[[(1r)-1-phenylethyl]amino]-7h-pyrrolo[2,3-d]pyrimidin-6-yl]phenol Chemical compound N([C@H](C)C=1C=CC=CC=1)C(C=1C=2)=NC=NC=1NC=2C1=CC=C(O)C=C1 XRYJULCDUUATMC-CYBMUJFWSA-N 0.000 claims 1
- KULGXJSSBLEZRX-UHFFFAOYSA-N 4-[bis(2-methoxyethyl)amino]-n-[4-(3-chloro-4-fluoroanilino)-7-(cyclopropylmethoxy)quinazolin-6-yl]but-2-enamide Chemical compound N1=CN=C2C=C(OCC3CC3)C(NC(=O)C=CCN(CCOC)CCOC)=CC2=C1NC1=CC=C(F)C(Cl)=C1 KULGXJSSBLEZRX-UHFFFAOYSA-N 0.000 claims 1
- XJURCGMPAMROEA-UHFFFAOYSA-N 4-n-(3-chloro-4-fluorophenyl)-6-n-[4-(dimethylamino)cyclohexyl]pyrimido[5,4-d]pyrimidine-4,6-diamine Chemical compound C1CC(N(C)C)CCC1NC1=NC=C(N=CN=C2NC=3C=C(Cl)C(F)=CC=3)C2=N1 XJURCGMPAMROEA-UHFFFAOYSA-N 0.000 claims 1
- GZELITDCOZGUPD-UHFFFAOYSA-N 6,7-dimethoxy-n-(3-methyl-2h-indazol-6-yl)quinazolin-4-amine Chemical compound C1=C2C(C)=NNC2=CC(NC=2N=CN=C3C=C(C(=CC3=2)OC)OC)=C1 GZELITDCOZGUPD-UHFFFAOYSA-N 0.000 claims 1
- NVOYVOBDTVTBDX-AGUVMIOSSA-N 8g15t83e6i Chemical class C1([C@@H](CO)C(=O)OC2C[C@@H]3[N+]([C@H](C2)[C@@H]2[C@H]3O2)(C)CC)=CC=CC=C1 NVOYVOBDTVTBDX-AGUVMIOSSA-N 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- ULXXDDBFHOBEHA-INIZCTEOSA-N N-[4-(3-chloro-4-fluoroanilino)-7-[[(3S)-3-oxolanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)C=CCN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-INIZCTEOSA-N 0.000 claims 1
- 229940065524 anticholinergics inhalants for obstructive airway diseases Drugs 0.000 claims 1
- OMZCMEYTWSXEPZ-UHFFFAOYSA-N canertinib Chemical compound C1=C(Cl)C(F)=CC=C1NC1=NC=NC2=CC(OCCCN3CCOCC3)=C(NC(=O)C=C)C=C12 OMZCMEYTWSXEPZ-UHFFFAOYSA-N 0.000 claims 1
- 229960005395 cetuximab Drugs 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 claims 1
- OEXHQOGQTVQTAT-JRNQLAHRSA-N ipratropium Chemical class O([C@H]1C[C@H]2CC[C@@H](C1)[N@@+]2(C)C(C)C)C(=O)C(CO)C1=CC=CC=C1 OEXHQOGQTVQTAT-JRNQLAHRSA-N 0.000 claims 1
- 229960001888 ipratropium 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
- JZMJDSHXVKJFKW-UHFFFAOYSA-M methyl sulfate(1-) Chemical compound COS([O-])(=O)=O JZMJDSHXVKJFKW-UHFFFAOYSA-M 0.000 claims 1
- RZWHMWFZGYRQSS-IBGZPJMESA-N n-[4-(3-chloro-4-fluoroanilino)-7-(cyclopropylmethoxy)quinazolin-6-yl]-4-[(2s)-2-(methoxymethyl)-6-oxomorpholin-4-yl]but-2-enamide Chemical compound C1C(=O)O[C@H](COC)CN1CC=CC(=O)NC(C(=CC1=NC=N2)OCC3CC3)=CC1=C2NC1=CC=C(F)C(Cl)=C1 RZWHMWFZGYRQSS-IBGZPJMESA-N 0.000 claims 1
- VIBUZWQYVPGBOP-UHFFFAOYSA-N n-[4-(3-chloro-4-fluoroanilino)-7-[4-(2,2-dimethyl-6-oxomorpholin-4-yl)butoxy]quinazolin-6-yl]prop-2-enamide Chemical compound C1C(=O)OC(C)(C)CN1CCCCOC1=CC2=NC=NC(NC=3C=C(Cl)C(F)=CC=3)=C2C=C1NC(=O)C=C VIBUZWQYVPGBOP-UHFFFAOYSA-N 0.000 claims 1
- UIJGHCUIUFFXJL-KRWDZBQOSA-N n-[4-(3-chloro-4-fluoroanilino)-7-[[(2s)-oxolan-2-yl]methoxy]quinazolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound N1=CN=C2C=C(OC[C@H]3OCCC3)C(NC(=O)C=CCN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 UIJGHCUIUFFXJL-KRWDZBQOSA-N 0.000 claims 1
- IMBFFWDWIAWOLR-UHFFFAOYSA-N n-[4-(3-chloro-4-fluoroanilino)-7-cyclopentyloxyquinazolin-6-yl]-4-[2-methoxyethyl(methyl)amino]but-2-enamide Chemical compound N1=CN=C2C=C(OC3CCCC3)C(NC(=O)C=CCN(C)CCOC)=CC2=C1NC1=CC=C(F)C(Cl)=C1 IMBFFWDWIAWOLR-UHFFFAOYSA-N 0.000 claims 1
- FATKBDRSEQUQER-HXUWFJFHSA-N n-[7-(cyclopropylmethoxy)-4-[[(1r)-1-phenylethyl]amino]quinazolin-6-yl]-4-[2-methoxyethyl(methyl)amino]but-2-enamide Chemical compound C1([C@@H](C)NC2=C3C=C(C(=CC3=NC=N2)OCC2CC2)NC(=O)C=CCN(C)CCOC)=CC=CC=C1 FATKBDRSEQUQER-HXUWFJFHSA-N 0.000 claims 1
- RHTFXIJREGOKBI-OAQYLSRUSA-N n-[7-(cyclopropylmethoxy)-4-[[(1r)-1-phenylethyl]amino]quinazolin-6-yl]-4-[ethyl(2-methoxyethyl)amino]but-2-enamide Chemical compound C1([C@@H](C)NC2=C3C=C(C(=CC3=NC=N2)OCC2CC2)NC(=O)C=CCN(CCOC)CC)=CC=CC=C1 RHTFXIJREGOKBI-OAQYLSRUSA-N 0.000 claims 1
- WVUNYSQLFKLYNI-AATRIKPKSA-N pelitinib Chemical compound C=12C=C(NC(=O)\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC1=CC=C(F)C(Cl)=C1 WVUNYSQLFKLYNI-AATRIKPKSA-N 0.000 claims 1
- 210000002345 respiratory system Anatomy 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 claims 1
- 229960000575 trastuzumab Drugs 0.000 claims 1
Classifications
-
- 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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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- A—HUMAN NECESSITIES
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- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
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- A—HUMAN NECESSITIES
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- A61P11/16—Central respiratory analeptics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
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- 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
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- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10206505.5 | 2002-02-16 | ||
| DE10206505A DE10206505A1 (de) | 2002-02-16 | 2002-02-16 | Neue Arzneimittelkompositionen auf der Basis von Anticholinergika und EGFR-Kinase-Hemmern |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2004127869A true RU2004127869A (ru) | 2005-08-27 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2004127869/15A RU2004127869A (ru) | 2002-02-16 | 2003-02-12 | Новые лекарственные композиции на основе антихолинергических средств и ингибиторов egfr-киназы |
Country Status (21)
| Country | Link |
|---|---|
| EP (1) | EP1478398B1 (enExample) |
| JP (1) | JP2005517039A (enExample) |
| KR (1) | KR20040083519A (enExample) |
| CN (1) | CN1633305A (enExample) |
| AR (1) | AR038494A1 (enExample) |
| AT (1) | ATE430581T1 (enExample) |
| AU (1) | AU2003206881B2 (enExample) |
| BR (1) | BR0307703A (enExample) |
| CA (1) | CA2476127C (enExample) |
| CO (1) | CO5611134A2 (enExample) |
| DE (2) | DE10206505A1 (enExample) |
| ES (1) | ES2326968T3 (enExample) |
| MX (1) | MXPA04007813A (enExample) |
| NZ (1) | NZ535166A (enExample) |
| PE (1) | PE20030859A1 (enExample) |
| PL (1) | PL369736A1 (enExample) |
| RU (1) | RU2004127869A (enExample) |
| TW (1) | TW200400036A (enExample) |
| UY (1) | UY27670A1 (enExample) |
| WO (1) | WO2003068264A1 (enExample) |
| ZA (1) | ZA200404787B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10230751A1 (de) * | 2002-07-09 | 2004-01-22 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittelkompositionen auf der Basis neuer Anticholinergika und EGFR-Kinase-Hemmern |
| US7569577B2 (en) | 2003-09-16 | 2009-08-04 | Astrazeneca Ab | Quinazoline derivatives as tyrosine kinase inhibitors |
| DE102004001607A1 (de) * | 2004-01-09 | 2005-08-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittelkombinationen auf der Basis von Scopin- oder Tropensäureestern mit EGFR-Kinase-Hemmern |
| US20060035893A1 (en) * | 2004-08-07 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
| WO2007029251A2 (en) * | 2005-09-06 | 2007-03-15 | T.K. Signal Ltd. | Polyalkylene glycol derivatives of 4- (phenylamino)quinazolines useful as irreversible inhibitors of epidermal gr0wth fact0r receptor tyrosine kinase |
| KR100832593B1 (ko) * | 2005-11-08 | 2008-05-27 | 한미약품 주식회사 | 신호전달 저해제로서의 퀴나졸린 유도체 및 이의 제조방법 |
| US8507502B2 (en) | 2008-11-10 | 2013-08-13 | National Health Research Institutes | Fused bicyclic and tricyclic pyrimidine compounds as tyrosine kinase inhibitors |
| US20120220557A1 (en) * | 2011-02-17 | 2012-08-30 | Chiesi Farmaceutici S.P.A. | Liquid propellant-free formulation comprising an antimuscarinic drug |
| US10710968B2 (en) | 2016-01-13 | 2020-07-14 | Hadasit Medical Research Services And Development Ltd. | Radiolabeled erlotinib analogs and uses thereof |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9508538D0 (en) * | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| GB9622363D0 (en) * | 1996-10-28 | 1997-01-08 | Celltech Therapeutics Ltd | Chemical compounds |
| DE19921693A1 (de) * | 1999-05-12 | 2000-11-16 | Boehringer Ingelheim Pharma | Neuartige Arzneimittelkompositionen auf der Basis von anticholinergisch wirksamen Verbindungen und ß-Mimetika |
| DE19911509A1 (de) * | 1999-03-15 | 2000-09-21 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| DE10042062A1 (de) * | 2000-08-26 | 2002-03-07 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Hertellung |
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2002
- 2002-02-16 DE DE10206505A patent/DE10206505A1/de not_active Withdrawn
-
2003
- 2003-02-12 DE DE50311496T patent/DE50311496D1/de not_active Expired - Lifetime
- 2003-02-12 KR KR10-2004-7012713A patent/KR20040083519A/ko not_active Ceased
- 2003-02-12 CN CNA038039427A patent/CN1633305A/zh active Pending
- 2003-02-12 PL PL03369736A patent/PL369736A1/xx not_active Application Discontinuation
- 2003-02-12 MX MXPA04007813A patent/MXPA04007813A/es not_active Application Discontinuation
- 2003-02-12 ES ES03704593T patent/ES2326968T3/es not_active Expired - Lifetime
- 2003-02-12 BR BR0307703-9A patent/BR0307703A/pt not_active IP Right Cessation
- 2003-02-12 AU AU2003206881A patent/AU2003206881B2/en not_active Ceased
- 2003-02-12 RU RU2004127869/15A patent/RU2004127869A/ru unknown
- 2003-02-12 NZ NZ535166A patent/NZ535166A/en unknown
- 2003-02-12 JP JP2003567444A patent/JP2005517039A/ja active Pending
- 2003-02-12 CA CA2476127A patent/CA2476127C/en not_active Expired - Fee Related
- 2003-02-12 WO PCT/EP2003/001357 patent/WO2003068264A1/de not_active Ceased
- 2003-02-12 AR ARP030100439A patent/AR038494A1/es not_active Application Discontinuation
- 2003-02-12 AT AT03704593T patent/ATE430581T1/de active
- 2003-02-12 EP EP03704593A patent/EP1478398B1/de not_active Expired - Lifetime
- 2003-02-14 TW TW092103090A patent/TW200400036A/zh unknown
- 2003-02-14 UY UY27670A patent/UY27670A1/es not_active Application Discontinuation
- 2003-02-14 PE PE2003000163A patent/PE20030859A1/es not_active Application Discontinuation
-
2004
- 2004-06-17 ZA ZA200404787A patent/ZA200404787B/en unknown
- 2004-09-13 CO CO04090723A patent/CO5611134A2/es active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| DE10206505A1 (de) | 2003-08-28 |
| UY27670A1 (es) | 2003-09-30 |
| JP2005517039A (ja) | 2005-06-09 |
| AU2003206881B2 (en) | 2009-02-26 |
| ZA200404787B (en) | 2005-08-11 |
| CA2476127C (en) | 2011-06-14 |
| EP1478398B1 (de) | 2009-05-06 |
| KR20040083519A (ko) | 2004-10-02 |
| AU2003206881A1 (en) | 2003-09-04 |
| ES2326968T3 (es) | 2009-10-22 |
| CA2476127A1 (en) | 2003-08-21 |
| BR0307703A (pt) | 2005-01-04 |
| PL369736A1 (en) | 2005-05-02 |
| AR038494A1 (es) | 2005-01-19 |
| DE50311496D1 (de) | 2009-06-18 |
| TW200400036A (en) | 2004-01-01 |
| CO5611134A2 (es) | 2006-02-28 |
| EP1478398A1 (de) | 2004-11-24 |
| CN1633305A (zh) | 2005-06-29 |
| PE20030859A1 (es) | 2003-11-18 |
| WO2003068264A1 (de) | 2003-08-21 |
| NZ535166A (en) | 2007-01-26 |
| ATE430581T1 (de) | 2009-05-15 |
| MXPA04007813A (es) | 2004-10-15 |
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