JP2006525296A5 - - Google Patents
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- Publication number
- JP2006525296A5 JP2006525296A5 JP2006506187A JP2006506187A JP2006525296A5 JP 2006525296 A5 JP2006525296 A5 JP 2006525296A5 JP 2006506187 A JP2006506187 A JP 2006506187A JP 2006506187 A JP2006506187 A JP 2006506187A JP 2006525296 A5 JP2006525296 A5 JP 2006525296A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- formula
- alkoxy
- group
- amino
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 181
- 125000003545 alkoxy group Chemical group 0.000 claims 35
- 229910052757 nitrogen Inorganic materials 0.000 claims 34
- -1 hydroxy, cyano, amino, carboxy, carbamoyl Chemical group 0.000 claims 31
- 125000000623 heterocyclic group Chemical group 0.000 claims 29
- 150000003246 quinazolines Chemical class 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 20
- 125000001424 substituent group Chemical group 0.000 claims 18
- 125000005236 alkanoylamino group Chemical group 0.000 claims 14
- 125000005843 halogen group Chemical group 0.000 claims 12
- 125000003282 alkyl amino group Chemical group 0.000 claims 11
- 125000000304 alkynyl group Chemical group 0.000 claims 11
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 11
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 10
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 9
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 9
- 125000001589 carboacyl group Chemical group 0.000 claims 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000005153 alkyl sulfamoyl group Chemical group 0.000 claims 8
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 8
- 125000004414 alkyl thio group Chemical group 0.000 claims 8
- 125000004423 acyloxy group Chemical group 0.000 claims 7
- 125000003302 alkenyloxy group Chemical group 0.000 claims 7
- 125000005133 alkynyloxy group Chemical group 0.000 claims 7
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 7
- 125000000524 functional group Chemical group 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 6
- 125000001153 fluoro group Chemical group F* 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 229910002091 carbon monoxide Inorganic materials 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 125000001246 bromo group Chemical group Br* 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
- 239000011593 sulfur Chemical group 0.000 claims 3
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 3
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims 2
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 claims 2
- 102000001301 EGF receptor Human genes 0.000 claims 2
- 108060006698 EGF receptor Proteins 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000006533 methyl amino methyl group Chemical group [H]N(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 claims 2
- UCQKNONQJLXCJZ-QGZVFWFLSA-N 1-[(2r)-2-[[4-(3-chloro-4-fluoroanilino)-7-(2-ethoxyethoxy)quinazolin-5-yl]oxymethyl]pyrrolidin-1-yl]-2-hydroxyethanone Chemical compound C=12C(NC=3C=C(Cl)C(F)=CC=3)=NC=NC2=CC(OCCOCC)=CC=1OC[C@H]1CCCN1C(=O)CO UCQKNONQJLXCJZ-QGZVFWFLSA-N 0.000 claims 1
- UHNQJZOECUKVME-OAHLLOKOSA-N 1-[(2r)-2-[[4-(3-chloro-4-fluoroanilino)-7-(2-hydroxyethoxy)quinazolin-5-yl]oxymethyl]pyrrolidin-1-yl]-2-hydroxyethanone Chemical compound C=12C(NC=3C=C(Cl)C(F)=CC=3)=NC=NC2=CC(OCCO)=CC=1OC[C@H]1CCCN1C(=O)CO UHNQJZOECUKVME-OAHLLOKOSA-N 0.000 claims 1
- AKBQOXHXZCHAPE-OAHLLOKOSA-N 1-[(2r)-2-[[4-(3-chloro-4-fluoroanilino)-7-ethoxyquinazolin-5-yl]oxymethyl]pyrrolidin-1-yl]-2-hydroxyethanone Chemical compound C=12C(NC=3C=C(Cl)C(F)=CC=3)=NC=NC2=CC(OCC)=CC=1OC[C@H]1CCCN1C(=O)CO AKBQOXHXZCHAPE-OAHLLOKOSA-N 0.000 claims 1
- NTABFMLTRPTDHH-MRXNPFEDSA-N 1-[(2r)-2-[[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-5-yl]oxymethyl]pyrrolidin-1-yl]-2-(dimethylamino)ethanone Chemical compound C=12C(NC=3C=C(Cl)C(F)=CC=3)=NC=NC2=CC(OC)=CC=1OC[C@H]1CCCN1C(=O)CN(C)C NTABFMLTRPTDHH-MRXNPFEDSA-N 0.000 claims 1
- OGHGSTSLGKIJSN-CQSZACIVSA-N 1-[(2r)-2-[[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-5-yl]oxymethyl]pyrrolidin-1-yl]-2-hydroxyethanone Chemical compound C=12C(NC=3C=C(Cl)C(F)=CC=3)=NC=NC2=CC(OC)=CC=1OC[C@H]1CCCN1C(=O)CO OGHGSTSLGKIJSN-CQSZACIVSA-N 0.000 claims 1
- CJBFTSCWGFCSSK-OAHLLOKOSA-N 1-[(2r)-2-[[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-5-yl]oxymethyl]pyrrolidin-1-yl]-2-methoxyethanone Chemical compound COCC(=O)N1CCC[C@@H]1COC1=CC(OC)=CC2=NC=NC(NC=3C=C(Cl)C(F)=CC=3)=C12 CJBFTSCWGFCSSK-OAHLLOKOSA-N 0.000 claims 1
- PMCYYFHUNBMWPQ-HZPDHXFCSA-N 1-[(2r,4r)-2-[[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-5-yl]oxymethyl]-4-hydroxypyrrolidin-1-yl]-2-(dimethylamino)ethanone Chemical compound C=12C(NC=3C=C(Cl)C(F)=CC=3)=NC=NC2=CC(OC)=CC=1OC[C@H]1C[C@@H](O)CN1C(=O)CN(C)C PMCYYFHUNBMWPQ-HZPDHXFCSA-N 0.000 claims 1
- ZTOORYPSOVNYFG-KGLIPLIRSA-N 1-[(2r,4s)-2-[[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-5-yl]oxymethyl]-4-hydroxypyrrolidin-1-yl]-2-hydroxyethanone Chemical compound C=12C(NC=3C=C(Cl)C(F)=CC=3)=NC=NC2=CC(OC)=CC=1OC[C@H]1C[C@H](O)CN1C(=O)CO ZTOORYPSOVNYFG-KGLIPLIRSA-N 0.000 claims 1
- PIVVDSXLUSYOIB-CABCVRRESA-N 1-[(2r,4s)-2-[[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-5-yl]oxymethyl]-4-hydroxypyrrolidin-1-yl]ethanone Chemical compound C=12C(NC=3C=C(Cl)C(F)=CC=3)=NC=NC2=CC(OC)=CC=1OC[C@H]1C[C@H](O)CN1C(C)=O PIVVDSXLUSYOIB-CABCVRRESA-N 0.000 claims 1
- CELREYOLUBVIRX-SFHVURJKSA-N 1-[(2s)-2-[[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-5-yl]oxymethyl]pyrrolidin-1-yl]-2-pyrrolidin-1-ylethanone Chemical compound C([C@H]1COC=2C=C(C=C3N=CN=C(NC=4C=C(Cl)C(F)=CC=4)C3=2)OC)CCN1C(=O)CN1CCCC1 CELREYOLUBVIRX-SFHVURJKSA-N 0.000 claims 1
- PMCYYFHUNBMWPQ-HOTGVXAUSA-N 1-[(2s,4s)-2-[[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-5-yl]oxymethyl]-4-hydroxypyrrolidin-1-yl]-2-(dimethylamino)ethanone Chemical compound C=12C(NC=3C=C(Cl)C(F)=CC=3)=NC=NC2=CC(OC)=CC=1OC[C@@H]1C[C@H](O)CN1C(=O)CN(C)C PMCYYFHUNBMWPQ-HOTGVXAUSA-N 0.000 claims 1
- 125000000530 1-propynyl group Chemical group [H]C([H])([H])C#C* 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- FPZWZCWUIYYYBU-UHFFFAOYSA-N 2-(2-ethoxyethoxy)ethyl acetate Chemical group CCOCCOCCOC(C)=O FPZWZCWUIYYYBU-UHFFFAOYSA-N 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000005530 alkylenedioxy group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 238000003776 cleavage reaction Methods 0.000 claims 1
- 238000007796 conventional method Methods 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 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 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 230000007017 scission Effects 0.000 claims 1
- 230000019491 signal transduction Effects 0.000 claims 1
- 230000004565 tumor cell growth Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0309850.6A GB0309850D0 (en) | 2003-04-30 | 2003-04-30 | Quinazoline derivatives |
| PCT/GB2004/001799 WO2004096226A1 (en) | 2003-04-30 | 2004-04-27 | Quinazoline derivatives and their use in the treatment of cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006525296A JP2006525296A (ja) | 2006-11-09 |
| JP2006525296A5 true JP2006525296A5 (enExample) | 2007-05-31 |
| JP4673839B2 JP4673839B2 (ja) | 2011-04-20 |
Family
ID=9957316
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006506187A Expired - Fee Related JP4673839B2 (ja) | 2003-04-30 | 2004-04-27 | ガンの処置で使用するためのキナゾリン誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7659279B2 (enExample) |
| EP (1) | EP1622620B1 (enExample) |
| JP (1) | JP4673839B2 (enExample) |
| AT (1) | ATE386530T1 (enExample) |
| DE (1) | DE602004011924T2 (enExample) |
| ES (1) | ES2300767T3 (enExample) |
| GB (1) | GB0309850D0 (enExample) |
| WO (1) | WO2004096226A1 (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005515176A (ja) * | 2001-11-03 | 2005-05-26 | アストラゼネカ アクチボラグ | 抗腫瘍剤としてのキナゾリン誘導体 |
| GB0126433D0 (en) * | 2001-11-03 | 2002-01-02 | Astrazeneca Ab | Compounds |
| GB0309009D0 (en) * | 2003-04-22 | 2003-05-28 | Astrazeneca Ab | Quinazoline derivatives |
| EP1664030A1 (en) * | 2003-09-16 | 2006-06-07 | AstraZeneca AB | Quinazoline derivatives |
| US7569577B2 (en) * | 2003-09-16 | 2009-08-04 | Astrazeneca Ab | Quinazoline derivatives as tyrosine kinase inhibitors |
| GB0321648D0 (en) * | 2003-09-16 | 2003-10-15 | Astrazeneca Ab | Quinazoline derivatives |
| AU2004272350A1 (en) * | 2003-09-16 | 2005-03-24 | Astrazeneca Ab | Quinazoline derivatives as tyrosine kinase inhibitors |
| BRPI0414488A (pt) * | 2003-09-16 | 2006-11-14 | Astrazeneca Ab | derivado de quinazolina, composição farmacêutica, uso de um derivado de quinazolina, métodos para produzir um efeito anti - proliferativo em um animal de sangue quente, para prevenção ou tratamento de tumores em um aminal de sangue quente, para fornecer um efeito inibidor da tirosina quinase de egfr seletivo em um animal de sangue quente e para tratar um cáncer em um animal de sangue quente e, processo para a preparação de um derivado de quinazolina |
| GB0322409D0 (en) * | 2003-09-25 | 2003-10-29 | Astrazeneca Ab | Quinazoline derivatives |
| GB0326459D0 (en) * | 2003-11-13 | 2003-12-17 | Astrazeneca Ab | Quinazoline derivatives |
| ATE413389T1 (de) * | 2004-02-03 | 2008-11-15 | Astrazeneca Ab | Chinazolinderivate |
| CA2567832A1 (en) * | 2004-06-04 | 2005-12-15 | Astrazeneca Ab | Quinazoline derivatives as erbb receptor tyrosine kinases |
| CN101124228B (zh) * | 2004-12-14 | 2011-06-15 | 阿斯利康(瑞典)有限公司 | 用作抗肿瘤药物的吡唑并嘧啶化合物 |
| GB0427697D0 (en) | 2004-12-17 | 2005-01-19 | Astrazeneca Ab | Chemical process |
| GB0504474D0 (en) * | 2005-03-04 | 2005-04-13 | Astrazeneca Ab | Chemical compounds |
| GB0504475D0 (en) * | 2005-03-04 | 2005-04-13 | Astrazeneca Ab | Chemical compounds |
| GB0508715D0 (en) * | 2005-04-29 | 2005-06-08 | Astrazeneca Ab | Chemical compounds |
| GB0508717D0 (en) * | 2005-04-29 | 2005-06-08 | Astrazeneca Ab | Chemical compounds |
| US7820683B2 (en) * | 2005-09-20 | 2010-10-26 | Astrazeneca Ab | 4-(1H-indazol-5-yl-amino)-quinazoline compounds as erbB receptor tyrosine kinase inhibitors for the treatment of cancer |
| US20090239861A1 (en) * | 2005-09-20 | 2009-09-24 | Robert Hugh Bradbury | Quinazoline derivatives as anticancer agents |
| ATE443053T1 (de) * | 2005-12-02 | 2009-10-15 | Astrazeneca Ab | Als inhibitoren von erbb-tyrosinkinase verwendete chinazoleinderivate |
| WO2007063291A1 (en) * | 2005-12-02 | 2007-06-07 | Astrazeneca Ab | 4-anilino-substituted quinazoline derivatives as tyrosine kinase inhibitors |
| BRPI0912170A2 (pt) | 2008-05-13 | 2015-10-13 | Astrazeneca Ab | composto, forma a, processo para a preparação da mesma, composição farmacêutica, uso de um composto, e, método para tratar um câncer em um animal de sangue quente |
| AU2018367909B2 (en) | 2017-11-17 | 2022-03-10 | Cellix Bio Private Limited | Compositions and methods for the treatment of eye disorders |
Family Cites Families (90)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5538325A (en) | 1978-09-11 | 1980-03-17 | Sankyo Co Ltd | 4-anilinoquinazoline derivative and its preparation |
| US4335127A (en) | 1979-01-08 | 1982-06-15 | Janssen Pharmaceutica, N.V. | Piperidinylalkyl quinazoline compounds, composition and method of use |
| GB2160201B (en) | 1984-06-14 | 1988-05-11 | Wyeth John & Brother Ltd | Quinazoline and cinnoline derivatives |
| KR910006138B1 (ko) | 1986-09-30 | 1991-08-16 | 에자이 가부시끼가이샤 | 환상아민 유도체 |
| IL89029A (en) | 1988-01-29 | 1993-01-31 | Lilly Co Eli | Fungicidal quinoline and cinnoline derivatives, compositions containing them, and fungicidal methods of using them |
| US4921863A (en) | 1988-02-17 | 1990-05-01 | Eisai Co., Ltd. | Cyclic amine derivatives |
| CA1340821C (en) | 1988-10-06 | 1999-11-16 | Nobuyuki Fukazawa | Heterocyclic compounds and anticancer-drug reinforcing agents containing them as effective components |
| 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 |
| US5710158A (en) | 1991-05-10 | 1998-01-20 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| US5721237A (en) | 1991-05-10 | 1998-02-24 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties |
| NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
| PT100905A (pt) | 1991-09-30 | 1994-02-28 | Eisai Co Ltd | Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem |
| US5187168A (en) | 1991-10-24 | 1993-02-16 | American Home Products Corporation | Substituted quinazolines as angiotensin II antagonists |
| GB9300059D0 (en) | 1992-01-20 | 1993-03-03 | Zeneca Ltd | Quinazoline derivatives |
| WO1993017682A1 (en) | 1992-03-04 | 1993-09-16 | Abbott Laboratories | Angiotensin ii receptor antagonists |
| GB9323290D0 (en) | 1992-12-10 | 1994-01-05 | Zeneca Ltd | Quinazoline derivatives |
| JPH083144A (ja) | 1994-06-21 | 1996-01-09 | Chugai Pharmaceut Co Ltd | キナゾリン及びキノリン誘導体 |
| GB9510757D0 (en) * | 1994-09-19 | 1995-07-19 | Wellcome Found | Therapeuticaly active compounds |
| TW321649B (enExample) * | 1994-11-12 | 1997-12-01 | Zeneca Ltd | |
| GB2295387A (en) | 1994-11-23 | 1996-05-29 | Glaxo Inc | Quinazoline antagonists of alpha 1c adrenergic receptors |
| GB9424233D0 (en) | 1994-11-30 | 1995-01-18 | Zeneca Ltd | Quinazoline derivatives |
| DE69536015D1 (de) | 1995-03-30 | 2009-12-10 | Pfizer Prod Inc | Chinazolinone Derivate |
| WO1996033977A1 (en) | 1995-04-27 | 1996-10-31 | Zeneca Limited | Quinazoline derivatives |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| GB9508537D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| GB9508535D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivative |
| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| US6046206A (en) | 1995-06-07 | 2000-04-04 | Cell Pathways, Inc. | Method of treating a patient having a precancerous lesions with amide quinazoline derivatives |
| GB9514265D0 (en) | 1995-07-13 | 1995-09-13 | Wellcome Found | Hetrocyclic compounds |
| DE69634900T2 (de) | 1995-09-11 | 2006-05-18 | Osteoarthritis Sciences, Inc., Cambridge | Proteintyrosine-kinaseinhibitoren zur behandlung der osteoarthritis |
| GB9624482D0 (en) | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| CA2216169C (en) | 1996-01-31 | 2007-01-23 | Gist-Brocades B.V. | Use of compositions comprising stabilized biologically effective compounds |
| US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
| WO1997030035A1 (en) | 1996-02-13 | 1997-08-21 | Zeneca Limited | Quinazoline derivatives as vegf inhibitors |
| GB9603097D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline compounds |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| SK284073B6 (sk) | 1996-04-12 | 2004-09-08 | Warner-Lambert Company | Polycyklické zlúčeniny, ich použitie a farmaceutické kompozície na ich báze |
| EP0912559B1 (en) | 1996-07-13 | 2002-11-06 | Glaxo Group Limited | Fused heterocyclic compounds as protein tyrosine kinase inhibitors |
| US6004967A (en) | 1996-09-13 | 1999-12-21 | Sugen, Inc. | Psoriasis treatment with quinazoline compounds |
| GB9718972D0 (en) | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
| EP0837063A1 (en) | 1996-10-17 | 1998-04-22 | Pfizer Inc. | 4-Aminoquinazoline derivatives |
| NZ510991A (en) | 1997-03-05 | 2002-11-26 | Sugen Inc | Use of formulations for hydrophobic pharmaceutical agents in treatment or prevention of cell proliferative disorders |
| AR012634A1 (es) | 1997-05-02 | 2000-11-08 | Sugen Inc | Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion |
| US5929080A (en) | 1997-05-06 | 1999-07-27 | American Cyanamid Company | Method of treating polycystic kidney disease |
| DK0980244T3 (da) | 1997-05-06 | 2003-09-29 | Wyeth Corp | Anvendelse af quinazoline forbindelser til behandling af polycystisk nyresygdom |
| ZA986732B (en) | 1997-07-29 | 1999-02-02 | Warner Lambert Co | Irreversible inhibitiors of tyrosine kinases |
| TW436485B (en) | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
| CA2306155A1 (en) | 1997-11-06 | 1999-05-20 | Philip Frost | Use of quinazoline derivatives as tyrosine kinase inhibitors for treating colonic polyps |
| JP4245682B2 (ja) | 1997-12-25 | 2009-03-25 | 協和発酵キリン株式会社 | キノリン誘導体、イソキノリン誘導体、およびシンノリン誘導体、並びに抗炎症剤および抗アレルギー剤 |
| GB9800575D0 (en) | 1998-01-12 | 1998-03-11 | Glaxo Group Ltd | Heterocyclic compounds |
| HUP0102793A3 (en) | 1998-05-28 | 2002-07-29 | Parker Hughes Inst St Paul | Quinazolines for treating brain tumor and medicaments containing them |
| AU4851599A (en) | 1998-06-30 | 2000-01-17 | Parker Hughes Institute | Method for inhibiting c-jun expression using jak-3 inhibitors |
| US6384223B1 (en) | 1998-07-30 | 2002-05-07 | American Home Products Corporation | Substituted quinazoline derivatives |
| AR020114A1 (es) | 1998-07-30 | 2002-04-10 | America Home Products Corp | Proceso para la preparacion de derivados de quinazolina sustituida y compuestos para su exclusivo uso en dicho proceso |
| WO2000009481A1 (en) | 1998-08-11 | 2000-02-24 | Takeda Chemical Industries, Ltd. | Cyclic amide compounds, process for producing the same, intermediates thereof and herbicides |
| KR20010089171A (ko) | 1998-08-21 | 2001-09-29 | 추후제출 | 퀴나졸린 유도체 |
| US6297258B1 (en) | 1998-09-29 | 2001-10-02 | American Cyanamid Company | Substituted 3-cyanoquinolines |
| HU230728B1 (hu) | 1998-09-29 | 2017-12-28 | Wyeth Holdings Llc | Szubsztituált 3-cianokinolinok mint protein tirozin kinázok inhibitorai |
| BR9914162A (pt) | 1998-10-01 | 2001-06-26 | Astrazeneca Ab | Derivado de amida, processo para preparar um derivado de amida, ou um sal farmaceuticamente aceitável ou éster clivável in vivo do mesmo, composição farmacêutica e uso de um derivado de amida, ou um sal farmaceuticamente aceitável ou éster clivável in vivo do mesmo |
| TW575567B (en) | 1998-10-23 | 2004-02-11 | Akzo Nobel Nv | Serine protease inhibitor |
| UA71945C2 (en) | 1999-01-27 | 2005-01-17 | Pfizer Prod Inc | Substituted bicyclic derivatives being used as anticancer agents |
| BRPI0017548B8 (pt) | 1999-02-10 | 2023-05-02 | Astrazeneca Ab | Composto |
| AU3281600A (en) | 1999-02-27 | 2000-09-21 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transsduction mediated by tyrosine kinases |
| DE19908567A1 (de) | 1999-02-27 | 2000-08-31 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| US6080747A (en) | 1999-03-05 | 2000-06-27 | Hughes Institute | JAK-3 inhibitors for treating allergic disorders |
| DE19911509A1 (de) | 1999-03-15 | 2000-09-21 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| UA73993C2 (uk) * | 2000-06-06 | 2005-10-17 | Астразенека Аб | Хіназолінові похідні для лікування пухлин та фармацевтична композиція |
| DE10040527A1 (de) | 2000-08-18 | 2002-02-28 | Boehringer Ingelheim Pharma | Chinazoline und Verfahren zu ihrer Herstellung |
| US6617329B2 (en) | 2000-08-26 | 2003-09-09 | Boehringer Ingelheim Pharma Kg | Aminoquinazolines and their use as medicaments |
| US20020082270A1 (en) | 2000-08-26 | 2002-06-27 | Frank Himmelsbach | Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases |
| NZ516873A (en) | 2001-02-12 | 2003-11-28 | Warner Lambert Co | Compositions containing retinoids and erb inhibitors and their use in inhibiting retinoid skin damage |
| TWI309647B (enExample) | 2001-02-21 | 2009-05-11 | Mitsubishi Tanabe Pharma Corp | |
| US6562319B2 (en) | 2001-03-12 | 2003-05-13 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Radiolabeled irreversible inhibitors of epidermal growth factor receptor tyrosine kinase and their use in radioimaging and radiotherapy |
| WO2002094790A1 (en) | 2001-05-23 | 2002-11-28 | Mitsubishi Pharma Corporation | Fused heterocyclic compound and medicinal use thereof |
| JP2005515176A (ja) | 2001-11-03 | 2005-05-26 | アストラゼネカ アクチボラグ | 抗腫瘍剤としてのキナゾリン誘導体 |
| GB0126433D0 (en) | 2001-11-03 | 2002-01-02 | Astrazeneca Ab | Compounds |
| TWI324597B (en) | 2002-03-28 | 2010-05-11 | Astrazeneca Ab | Quinazoline derivatives |
| GB0309009D0 (en) | 2003-04-22 | 2003-05-28 | Astrazeneca Ab | Quinazoline derivatives |
| GB0317665D0 (en) | 2003-07-29 | 2003-09-03 | Astrazeneca Ab | Qinazoline derivatives |
| BRPI0413066A (pt) | 2003-07-29 | 2006-10-17 | Astrazeneca Ab | derivado de quinazolina, ou um sal farmaceuticamente aceitável, ou um éster farmaceuticamente aceitável do mesmo, da fórmula i, uso e processo para a preparação do mesmo, composto, composição farmacêutica, e, métodos para a produção de um efeito antiproliferativo em um animal de sangue quente, para a prevenção ou tratamento de um tumor, para prover um efeito inibitório de tirosina quinase de egfr seletivo, e para tratar um cáncer em um animal de sangue quente |
| US7569577B2 (en) | 2003-09-16 | 2009-08-04 | Astrazeneca Ab | Quinazoline derivatives as tyrosine kinase inhibitors |
| BRPI0414488A (pt) | 2003-09-16 | 2006-11-14 | Astrazeneca Ab | derivado de quinazolina, composição farmacêutica, uso de um derivado de quinazolina, métodos para produzir um efeito anti - proliferativo em um animal de sangue quente, para prevenção ou tratamento de tumores em um aminal de sangue quente, para fornecer um efeito inibidor da tirosina quinase de egfr seletivo em um animal de sangue quente e para tratar um cáncer em um animal de sangue quente e, processo para a preparação de um derivado de quinazolina |
| GB0321648D0 (en) * | 2003-09-16 | 2003-10-15 | Astrazeneca Ab | Quinazoline derivatives |
| AU2004272350A1 (en) * | 2003-09-16 | 2005-03-24 | Astrazeneca Ab | Quinazoline derivatives as tyrosine kinase inhibitors |
| DE602004004811T2 (de) | 2003-09-19 | 2007-11-22 | Astrazeneca Ab | Chinazolinderivate |
| US20070043010A1 (en) | 2003-09-25 | 2007-02-22 | Astrazeneca Uk Limited | Quinazoline derivatives |
| GB0322409D0 (en) | 2003-09-25 | 2003-10-29 | Astrazeneca Ab | Quinazoline derivatives |
| GB0326459D0 (en) | 2003-11-13 | 2003-12-17 | Astrazeneca Ab | Quinazoline derivatives |
| ATE413389T1 (de) | 2004-02-03 | 2008-11-15 | Astrazeneca Ab | Chinazolinderivate |
| CA2567832A1 (en) | 2004-06-04 | 2005-12-15 | Astrazeneca Ab | Quinazoline derivatives as erbb receptor tyrosine kinases |
-
2003
- 2003-04-30 GB GBGB0309850.6A patent/GB0309850D0/en not_active Ceased
-
2004
- 2004-04-27 AT AT04729678T patent/ATE386530T1/de not_active IP Right Cessation
- 2004-04-27 US US10/555,085 patent/US7659279B2/en not_active Expired - Fee Related
- 2004-04-27 JP JP2006506187A patent/JP4673839B2/ja not_active Expired - Fee Related
- 2004-04-27 ES ES04729678T patent/ES2300767T3/es not_active Expired - Lifetime
- 2004-04-27 DE DE602004011924T patent/DE602004011924T2/de not_active Expired - Lifetime
- 2004-04-27 WO PCT/GB2004/001799 patent/WO2004096226A1/en not_active Ceased
- 2004-04-27 EP EP04729678A patent/EP1622620B1/en not_active Expired - Lifetime
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