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 (https=) | 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 (https=) |
| EP (1) | EP1622620B1 (https=) |
| JP (1) | JP4673839B2 (https=) |
| AT (1) | ATE386530T1 (https=) |
| DE (1) | DE602004011924T2 (https=) |
| ES (1) | ES2300767T3 (https=) |
| GB (1) | GB0309850D0 (https=) |
| WO (1) | WO2004096226A1 (https=) |
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 |
| AU2004272346A1 (en) * | 2003-09-16 | 2005-03-24 | Astrazeneca Ab | Quinazoline derivatives |
| ES2305844T3 (es) * | 2003-09-16 | 2008-11-01 | Astrazeneca Ab | Derivados de quinazolina como inhibidores de tirosina cinasa. |
| AU2004272345A1 (en) * | 2003-09-16 | 2005-03-24 | Astrazeneca Ab | Quinazoline derivatives |
| GB0321648D0 (en) * | 2003-09-16 | 2003-10-15 | Astrazeneca Ab | Quinazoline derivatives |
| US20070032508A1 (en) * | 2003-09-16 | 2007-02-08 | Bradbury Robert H | Quinazoline derivatives as tyrosine kinase inhibitors |
| GB0322409D0 (en) * | 2003-09-25 | 2003-10-29 | Astrazeneca Ab | Quinazoline derivatives |
| GB0326459D0 (en) | 2003-11-13 | 2003-12-17 | Astrazeneca Ab | Quinazoline derivatives |
| JP5032851B2 (ja) | 2004-02-03 | 2012-09-26 | アストラゼネカ アクチボラグ | キナゾリン誘導体 |
| AU2005250224A1 (en) * | 2004-06-04 | 2005-12-15 | Astrazeneca Ab | Quinazoline derivatives as ERBB receptor tyrosine kinases |
| EP1838712B8 (en) * | 2004-12-14 | 2011-10-12 | AstraZeneca AB | Pyrazolopyrimidine compounds as antitumor agents |
| GB0427697D0 (en) * | 2004-12-17 | 2005-01-19 | Astrazeneca Ab | Chemical process |
| GB0504475D0 (en) * | 2005-03-04 | 2005-04-13 | Astrazeneca Ab | Chemical compounds |
| GB0504474D0 (en) * | 2005-03-04 | 2005-04-13 | Astrazeneca Ab | Chemical compounds |
| GB0508717D0 (en) * | 2005-04-29 | 2005-06-08 | Astrazeneca Ab | Chemical compounds |
| GB0508715D0 (en) * | 2005-04-29 | 2005-06-08 | Astrazeneca Ab | Chemical compounds |
| JP2009508917A (ja) * | 2005-09-20 | 2009-03-05 | アストラゼネカ アクチボラグ | 抗癌剤としてのキナゾリン誘導体 |
| WO2007034144A1 (en) * | 2005-09-20 | 2007-03-29 | Astrazeneca Ab | 4- (ih-indazol-s-yl-amino)-quinazoline compounds as erbb receptor tyrosine kinase inhibitors for the treatment of cancer |
| JP2009517450A (ja) * | 2005-12-02 | 2009-04-30 | アストラゼネカ アクチボラグ | チロシンキナーゼ阻害薬としての４−アニリノ置換キナゾリン誘導体 |
| JP2009517451A (ja) * | 2005-12-02 | 2009-04-30 | アストラゼネカ アクチボラグ | Ｅｒｂｂチロシンキナーゼの阻害剤として使用されるキナゾリン誘導体 |
| EP2303276B1 (en) | 2008-05-13 | 2013-11-13 | AstraZeneca AB | Fumarate salt of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(n-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline |
| CA3081553C (en) | 2017-11-17 | 2022-11-15 | Cellix Bio Private Limited | Compositions and methods for the treatment of eye disorders |
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| 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 |
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| GB9514265D0 (en) | 1995-07-13 | 1995-09-13 | Wellcome Found | Hetrocyclic compounds |
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-
2003
- 2003-04-30 GB GBGB0309850.6A patent/GB0309850D0/en not_active Ceased
-
2004
- 2004-04-27 EP EP04729678A patent/EP1622620B1/en not_active Expired - Lifetime
- 2004-04-27 JP JP2006506187A patent/JP4673839B2/ja not_active Expired - Fee Related
- 2004-04-27 AT AT04729678T patent/ATE386530T1/de not_active IP Right Cessation
- 2004-04-27 DE DE602004011924T patent/DE602004011924T2/de not_active Expired - Lifetime
- 2004-04-27 ES ES04729678T patent/ES2300767T3/es not_active Expired - Lifetime
- 2004-04-27 US US10/555,085 patent/US7659279B2/en not_active Expired - Fee Related
- 2004-04-27 WO PCT/GB2004/001799 patent/WO2004096226A1/en not_active Ceased
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