JP2003504360A5 - - Google Patents
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- Publication number
- JP2003504360A5 JP2003504360A5 JP2001509712A JP2001509712A JP2003504360A5 JP 2003504360 A5 JP2003504360 A5 JP 2003504360A5 JP 2001509712 A JP2001509712 A JP 2001509712A JP 2001509712 A JP2001509712 A JP 2001509712A JP 2003504360 A5 JP2003504360 A5 JP 2003504360A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- ylmethoxy
- propoxy
- methoxy
- 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.)
- Withdrawn
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- 125000000217 alkyl group Chemical group 0.000 description 88
- -1 cyano, isocyano, nitro, hydroxy, mercapto, amino, formyl Chemical group 0.000 description 45
- 229910052757 nitrogen Inorganic materials 0.000 description 23
- 125000001424 substituent group Chemical group 0.000 description 19
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 18
- 239000001257 hydrogen Substances 0.000 description 18
- 229910052739 hydrogen Inorganic materials 0.000 description 18
- 125000003118 aryl group Chemical group 0.000 description 13
- 229910052760 oxygen Inorganic materials 0.000 description 13
- 125000001072 heteroaryl group Chemical group 0.000 description 11
- 125000000623 heterocyclic group Chemical group 0.000 description 11
- 125000005236 alkanoylamino group Chemical group 0.000 description 10
- 229910052717 sulfur Inorganic materials 0.000 description 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 7
- 125000003545 alkoxy group Chemical group 0.000 description 6
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 6
- 125000005115 alkyl carbamoyl group Chemical group 0.000 description 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 6
- 125000000753 cycloalkyl group Chemical group 0.000 description 6
- 125000005843 halogen group Chemical group 0.000 description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 6
- 150000003246 quinazolines Chemical class 0.000 description 6
- 150000003839 salts Chemical class 0.000 description 6
- 125000004423 acyloxy group Chemical group 0.000 description 5
- 125000003282 alkyl amino group Chemical group 0.000 description 5
- 125000005153 alkyl sulfamoyl group Chemical group 0.000 description 5
- 125000004644 alkyl sulfinyl group Chemical group 0.000 description 5
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 5
- 125000004414 alkyl thio group Chemical group 0.000 description 5
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 description 5
- 125000001589 carboacyl group Chemical group 0.000 description 5
- 239000002253 acid Substances 0.000 description 4
- 125000003342 alkenyl group Chemical group 0.000 description 4
- 125000003302 alkenyloxy group Chemical group 0.000 description 4
- 125000000304 alkynyl group Chemical group 0.000 description 4
- 125000005133 alkynyloxy group Chemical group 0.000 description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 4
- 125000001246 bromo group Chemical group Br* 0.000 description 3
- 229910052799 carbon Inorganic materials 0.000 description 3
- 125000001309 chloro group Chemical group Cl* 0.000 description 3
- 125000001153 fluoro group Chemical group F* 0.000 description 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- PDKQWNNPSOCARZ-UHFFFAOYSA-N 1-(6,7-dimethoxyquinazolin-4-yl)-3-phenylurea Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC(=O)NC1=CC=CC=C1 PDKQWNNPSOCARZ-UHFFFAOYSA-N 0.000 description 2
- 125000005530 alkylenedioxy group Chemical group 0.000 description 2
- 125000000392 cycloalkenyl group Chemical group 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 2
- SQQWBSBBCSFQGC-JLHYYAGUSA-N ubiquinone-2 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CCC=C(C)C)=C(C)C1=O SQQWBSBBCSFQGC-JLHYYAGUSA-N 0.000 description 2
- LFKKTLUGAAHREA-UHFFFAOYSA-N 1-(2,6-dichlorophenyl)-3-[6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-yl]urea Chemical compound N1=CN=C2C=C(OCC3CCN(C)CC3)C(OC)=CC2=C1NC(=O)NC1=C(Cl)C=CC=C1Cl LFKKTLUGAAHREA-UHFFFAOYSA-N 0.000 description 1
- XFMBZTKSOUNGDD-UHFFFAOYSA-N 1-(2,6-dichlorophenyl)-3-[7-(3-morpholin-4-ylpropoxy)quinazolin-4-yl]urea Chemical compound ClC1=CC=CC(Cl)=C1NC(=O)NC1=NC=NC2=CC(OCCCN3CCOCC3)=CC=C12 XFMBZTKSOUNGDD-UHFFFAOYSA-N 0.000 description 1
- VJPCAEOLFMRBIO-UHFFFAOYSA-N 1-(2,6-dichlorophenyl)-3-[7-[3-(1,1-dioxo-1,4-thiazinan-4-yl)propoxy]quinazolin-4-yl]urea Chemical compound ClC1=CC=CC(Cl)=C1NC(=O)NC1=NC=NC2=CC(OCCCN3CCS(=O)(=O)CC3)=CC=C12 VJPCAEOLFMRBIO-UHFFFAOYSA-N 0.000 description 1
- KSNTYYGPIMDEGF-UHFFFAOYSA-N 1-(2,6-difluorophenyl)-3-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinazolin-4-yl]urea Chemical compound N1=CN=C2C=C(OCCCN3CCOCC3)C(OC)=CC2=C1NC(=O)NC1=C(F)C=CC=C1F KSNTYYGPIMDEGF-UHFFFAOYSA-N 0.000 description 1
- BVQIOKJOQYMERO-UHFFFAOYSA-N 1-(2,6-difluorophenyl)-3-[6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-yl]urea Chemical compound N1=CN=C2C=C(OCC3CCN(C)CC3)C(OC)=CC2=C1NC(=O)NC1=C(F)C=CC=C1F BVQIOKJOQYMERO-UHFFFAOYSA-N 0.000 description 1
- VQANQTNLUVCABE-UHFFFAOYSA-N 1-(2,6-difluorophenyl)-3-[6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-yl]urea Chemical compound N1=CN=C2C=C(OCCCN3CCN(C)CC3)C(OC)=CC2=C1NC(=O)NC1=C(F)C=CC=C1F VQANQTNLUVCABE-UHFFFAOYSA-N 0.000 description 1
- WEHHOPRHJGOSQH-UHFFFAOYSA-N 1-(2,6-dimethylphenyl)-3-[6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl]urea Chemical compound N1=CN=C2C=C(OCCCN3CCCCC3)C(OC)=CC2=C1NC(=O)NC1=C(C)C=CC=C1C WEHHOPRHJGOSQH-UHFFFAOYSA-N 0.000 description 1
- MYGNHGMKCUOIOX-UHFFFAOYSA-N 1-(2,6-dimethylphenyl)-3-[6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-yl]thiourea Chemical compound N1=CN=C2C=C(OCC3CCN(C)CC3)C(OC)=CC2=C1NC(=S)NC1=C(C)C=CC=C1C MYGNHGMKCUOIOX-UHFFFAOYSA-N 0.000 description 1
- QGOLHIOJZCVCEQ-UHFFFAOYSA-N 1-(2,6-dimethylphenyl)-3-[6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-yl]urea Chemical compound N1=CN=C2C=C(OCC3CCN(C)CC3)C(OC)=CC2=C1NC(=O)NC1=C(C)C=CC=C1C QGOLHIOJZCVCEQ-UHFFFAOYSA-N 0.000 description 1
- HJRYVXJYTOOIHN-UHFFFAOYSA-N 1-(2,6-dimethylphenyl)-3-[6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-yl]urea Chemical compound N1=CN=C2C=C(OCCCN3CCN(C)CC3)C(OC)=CC2=C1NC(=O)NC1=C(C)C=CC=C1C HJRYVXJYTOOIHN-UHFFFAOYSA-N 0.000 description 1
- METZVMMERANODX-UHFFFAOYSA-N 1-(2-chloro-6-methylphenyl)-3-[6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-yl]urea Chemical compound N1=CN=C2C=C(OCC3CCN(C)CC3)C(OC)=CC2=C1NC(=O)NC1=C(C)C=CC=C1Cl METZVMMERANODX-UHFFFAOYSA-N 0.000 description 1
- NXIYIURBAQLTKU-UHFFFAOYSA-N 1-(3-bromophenyl)-3-[5-(4-methoxyphenoxy)quinazolin-4-yl]urea Chemical compound C1=CC(OC)=CC=C1OC1=CC=CC2=NC=NC(NC(=O)NC=3C=C(Br)C=CC=3)=C12 NXIYIURBAQLTKU-UHFFFAOYSA-N 0.000 description 1
- KZNSMKOBZHUBQO-UHFFFAOYSA-N 1-[5-(4-methoxyphenoxy)quinazolin-4-yl]-3-(3-methoxyphenyl)urea Chemical compound C1=CC(OC)=CC=C1OC1=CC=CC2=NC=NC(NC(=O)NC=3C=C(OC)C=CC=3)=C12 KZNSMKOBZHUBQO-UHFFFAOYSA-N 0.000 description 1
- NIHRUDAZAJTAHA-UHFFFAOYSA-N 1-[5-(4-methoxyphenoxy)quinazolin-4-yl]-3-phenylurea Chemical compound C1=CC(OC)=CC=C1OC1=CC=CC2=NC=NC(NC(=O)NC=3C=CC=CC=3)=C12 NIHRUDAZAJTAHA-UHFFFAOYSA-N 0.000 description 1
- ARDYBEPURLDBAR-UHFFFAOYSA-N 1-[6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-yl]-3-(1-phenylethyl)urea Chemical compound N1=CN=C2C=C(OCC3CCN(C)CC3)C(OC)=CC2=C1NC(=O)NC(C)C1=CC=CC=C1 ARDYBEPURLDBAR-UHFFFAOYSA-N 0.000 description 1
- PWLOZSWLRKABAU-UHFFFAOYSA-N 1-benzyl-3-[6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-yl]urea Chemical compound N1=CN=C2C=C(OCC3CCN(C)CC3)C(OC)=CC2=C1NC(=O)NCC1=CC=CC=C1 PWLOZSWLRKABAU-UHFFFAOYSA-N 0.000 description 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 125000002947 alkylene group Chemical group 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 1
- 239000001301 oxygen Chemical group 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 description 1
- 239000011593 sulfur Chemical group 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP99401692.1 | 1999-07-07 | ||
| EP99401692 | 1999-07-07 | ||
| EP00401221 | 2000-05-04 | ||
| EP00401221.7 | 2000-05-04 | ||
| PCT/GB2000/002566 WO2001004102A1 (en) | 1999-07-07 | 2000-07-04 | Quinazoline derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003504360A JP2003504360A (ja) | 2003-02-04 |
| JP2003504360A5 true JP2003504360A5 (https=) | 2007-08-02 |
Family
ID=26073473
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001509712A Withdrawn JP2003504360A (ja) | 1999-07-07 | 2000-07-04 | キナゾリン誘導体 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US6806274B1 (https=) |
| EP (1) | EP1218353B1 (https=) |
| JP (1) | JP2003504360A (https=) |
| KR (1) | KR20020029419A (https=) |
| CN (1) | CN1360582A (https=) |
| AT (1) | ATE375984T1 (https=) |
| AU (1) | AU6578900A (https=) |
| BR (1) | BR0012157A (https=) |
| CA (1) | CA2378291A1 (https=) |
| DE (1) | DE60036812T2 (https=) |
| ES (1) | ES2292461T3 (https=) |
| IL (1) | IL147280A0 (https=) |
| MX (1) | MXPA01012887A (https=) |
| NO (1) | NO20020042L (https=) |
| WO (1) | WO2001004102A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2001235804A1 (en) | 2000-03-06 | 2001-09-17 | Astrazeneca Ab | Therapy |
| WO2002000644A1 (en) * | 2000-06-24 | 2002-01-03 | Astrazeneca Ab | Guanidine derivatives of quinazoline and quinoline for use in the treatment of autoimmune diseases |
| US6503914B1 (en) * | 2000-10-23 | 2003-01-07 | Board Of Regents, The University Of Texas System | Thienopyrimidine-based inhibitors of the Src family |
| JP4564713B2 (ja) | 2000-11-01 | 2010-10-20 | ミレニアム・ファーマシューティカルズ・インコーポレイテッド | 窒素性複素環式化合物、ならびに窒素性複素環式化合物およびその中間体を作製するための方法 |
| GB0128108D0 (en) | 2001-11-23 | 2002-01-16 | Astrazeneca Ab | Therapeutic use |
| SI1474420T1 (sl) | 2002-02-01 | 2012-06-29 | Astrazeneca Ab | Spojine kinazolina |
| US6924285B2 (en) | 2002-03-30 | 2005-08-02 | Boehringer Ingelheim Pharma Gmbh & Co. | Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them |
| GB0208224D0 (en) * | 2002-04-10 | 2002-05-22 | Celltech R&D Ltd | Chemical compounds |
| GB0221245D0 (en) * | 2002-09-13 | 2002-10-23 | Astrazeneca Ab | Chemical process |
| GB0317665D0 (en) | 2003-07-29 | 2003-09-03 | Astrazeneca Ab | Qinazoline derivatives |
| DE602005010824D1 (de) | 2004-02-03 | 2008-12-18 | Astrazeneca Ab | Chinazolinderivate |
| AR056200A1 (es) * | 2005-09-27 | 2007-09-26 | Wyeth Corp | Tieno [2,3-b]piridin-5-carbonitrilos como inhibidores de proteina quinasa |
| EP1921070A1 (de) | 2006-11-10 | 2008-05-14 | Boehringer Ingelheim Pharma GmbH & Co. KG | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstelllung |
| AU2008212999A1 (en) | 2007-02-06 | 2008-08-14 | Boehringer Ingelheim International Gmbh | Bicyclic heterocycles, drugs containing said compounds, use thereof, and method for production thereof |
| US7951832B2 (en) | 2007-10-31 | 2011-05-31 | Burnham Institute For Medical Research | Pyrazole derivatives as kinase inhibitors |
| US8497369B2 (en) | 2008-02-07 | 2013-07-30 | Boehringer Ingelheim International Gmbh | Spirocyclic heterocycles medicaments containing said compounds, use thereof and method for their production |
| JP5739802B2 (ja) | 2008-05-13 | 2015-06-24 | アストラゼネカ アクチボラグ | ４−（３−クロロ−２−フルオロアニリノ）−７−メトキシ−６−｛［１−（ｎ−メチルカルバモイルメチル）ピペリジン−４−イル］オキシ｝キナゾリンのフマル酸塩 |
| EP2313397B1 (de) | 2008-08-08 | 2016-04-20 | Boehringer Ingelheim International GmbH | Cyclohexyloxy-substituierte heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung |
| CN102068434B (zh) * | 2011-01-25 | 2012-08-22 | 林治华 | 4-(环己基)-胺基喹唑啉类化合物的应用 |
| DK3126330T3 (en) * | 2014-04-04 | 2019-04-23 | Pfizer | BICYCLE-FUSED HETEROARYL OR ARYL COMPOUNDS AND USE THEREOF AS IRAC4 INHIBITORS |
| US10711036B2 (en) | 2015-08-28 | 2020-07-14 | Cornell University | MALT1 inhibitors and uses thereof |
| WO2018036414A1 (zh) * | 2016-08-23 | 2018-03-01 | 北京诺诚健华医药科技有限公司 | 稠杂环类衍生物、其制备方法及其在医学上的应用 |
| US10689366B2 (en) * | 2016-11-01 | 2020-06-23 | Cornell University | Compounds for MALT1 degredation |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4659736A (en) * | 1984-01-21 | 1987-04-21 | Bayer Aktiengesellschaft | Benzoyl urea compounds as agents for repelling snails and slugs |
| JPH0720943B2 (ja) * | 1988-08-19 | 1995-03-08 | 宇部興産株式会社 | アミノピリミジン誘導体、その製法及び殺虫・殺菌剤 |
| JPH11503110A (ja) * | 1995-02-17 | 1999-03-23 | スミスクライン・ビーチャム・コーポレイション | Ｉｌ−８受容体拮抗剤 |
| US5773459A (en) | 1995-06-07 | 1998-06-30 | Sugen, Inc. | Urea- and thiourea-type compounds |
| GB9514265D0 (en) * | 1995-07-13 | 1995-09-13 | Wellcome Found | Hetrocyclic compounds |
| AU743024B2 (en) | 1997-03-05 | 2002-01-17 | Sugen, Inc. | Formulations for hydrophobic pharmaceutical agents |
| 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 |
| US6211165B1 (en) | 1997-05-09 | 2001-04-03 | The Trustees Of The University Of Pennsylvania | Methods and compositions for reducing ischemic injury of the heart by administering adenosine receptor agonists and antagonists |
| DE69826695T2 (de) | 1997-05-23 | 2006-02-02 | Bayer Pharmaceuticals Corp., West Haven | Arylharnstoffderivate zur behandlung von inflammatorischen oder immunomodulatorischen erkrankungen |
| AR016817A1 (es) * | 1997-08-14 | 2001-08-01 | Smithkline Beecham Plc | Derivados de fenilurea o feniltiourea, procedimiento para su preparacion, coleccion de compuestos, compuestos intermediarios, composicion farmaceutica,metodo de tratamiento y uso de dichos compuestos para la manufactura de un medicamento |
| EP1232150B1 (en) * | 1999-11-16 | 2007-10-10 | Boehringer Ingelheim Pharmaceuticals Inc. | Urea derivatives as anti-inflammatory agents |
| WO2002000644A1 (en) | 2000-06-24 | 2002-01-03 | Astrazeneca Ab | Guanidine derivatives of quinazoline and quinoline for use in the treatment of autoimmune diseases |
| US7074805B2 (en) * | 2002-02-20 | 2006-07-11 | Abbott Laboratories | Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor |
-
2000
- 2000-07-04 CN CN00810040A patent/CN1360582A/zh active Pending
- 2000-07-04 JP JP2001509712A patent/JP2003504360A/ja not_active Withdrawn
- 2000-07-04 EP EP00953271A patent/EP1218353B1/en not_active Expired - Lifetime
- 2000-07-04 KR KR1020027000188A patent/KR20020029419A/ko not_active Withdrawn
- 2000-07-04 DE DE60036812T patent/DE60036812T2/de not_active Expired - Fee Related
- 2000-07-04 AT AT00953271T patent/ATE375984T1/de not_active IP Right Cessation
- 2000-07-04 ES ES00953271T patent/ES2292461T3/es not_active Expired - Lifetime
- 2000-07-04 AU AU65789/00A patent/AU6578900A/en not_active Abandoned
- 2000-07-04 MX MXPA01012887A patent/MXPA01012887A/es unknown
- 2000-07-04 CA CA002378291A patent/CA2378291A1/en not_active Abandoned
- 2000-07-04 BR BR0012157-6A patent/BR0012157A/pt not_active Application Discontinuation
- 2000-07-04 WO PCT/GB2000/002566 patent/WO2001004102A1/en not_active Ceased
- 2000-07-04 US US10/019,945 patent/US6806274B1/en not_active Expired - Fee Related
- 2000-07-04 IL IL14728000A patent/IL147280A0/xx unknown
-
2002
- 2002-01-04 NO NO20020042A patent/NO20020042L/no unknown
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