JP2007501212A5 - - Google Patents
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- Publication number
- JP2007501212A5 JP2007501212A5 JP2006522409A JP2006522409A JP2007501212A5 JP 2007501212 A5 JP2007501212 A5 JP 2007501212A5 JP 2006522409 A JP2006522409 A JP 2006522409A JP 2006522409 A JP2006522409 A JP 2006522409A JP 2007501212 A5 JP2007501212 A5 JP 2007501212A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkanoyl
- alkoxy
- carbamoyl
- 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 344
- 125000001589 carboacyl group Chemical group 0.000 claims 109
- 125000003545 alkoxy group Chemical group 0.000 claims 96
- 125000003282 alkyl amino group Chemical group 0.000 claims 89
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 84
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 84
- 125000000623 heterocyclic group Chemical group 0.000 claims 66
- 125000001424 substituent group Chemical group 0.000 claims 66
- -1 C 1-6 fluoroalkanoyl Chemical group 0.000 claims 43
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 40
- 125000003342 alkenyl group Chemical group 0.000 claims 39
- 125000000304 alkynyl group Chemical group 0.000 claims 38
- 229910052757 nitrogen Inorganic materials 0.000 claims 32
- 229920006395 saturated elastomer Polymers 0.000 claims 31
- 125000005842 heteroatom Chemical group 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 25
- 229910052717 sulfur Inorganic materials 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 22
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 20
- 125000005843 halogen group Chemical group 0.000 claims 19
- 150000002431 hydrogen Chemical class 0.000 claims 19
- 125000004043 oxo group Chemical group O=* 0.000 claims 17
- 229910052760 oxygen Inorganic materials 0.000 claims 17
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 16
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 15
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 13
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 13
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 13
- 125000004103 aminoalkyl group Chemical group 0.000 claims 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 125000004966 cyanoalkyl group Chemical group 0.000 claims 13
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 10
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 8
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 8
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 8
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 4
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- JGLLVNSIUQPNQA-MRXNPFEDSA-N 1-[(3r)-3-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]-2-(dimethylamino)ethanone Chemical compound N1=CN=C2C=C(OC[C@H]3CN(CCC3)C(=O)CN(C)C)C(OC)=CC2=C1NC1=CC=C(Cl)C=C1F JGLLVNSIUQPNQA-MRXNPFEDSA-N 0.000 claims 1
- JGLLVNSIUQPNQA-INIZCTEOSA-N 1-[(3s)-3-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]-2-(dimethylamino)ethanone Chemical compound N1=CN=C2C=C(OC[C@@H]3CN(CCC3)C(=O)CN(C)C)C(OC)=CC2=C1NC1=CC=C(Cl)C=C1F JGLLVNSIUQPNQA-INIZCTEOSA-N 0.000 claims 1
- IWASYXNYJUYQBV-UHFFFAOYSA-N 1-[4-[2-[4-(4-bromo-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxyethyl]piperidin-1-yl]-2-(dimethylamino)ethanone Chemical compound N1=CN=C2C=C(OCCC3CCN(CC3)C(=O)CN(C)C)C(OC)=CC2=C1NC1=CC=C(Br)C=C1F IWASYXNYJUYQBV-UHFFFAOYSA-N 0.000 claims 1
- VYRBUOLLDDZYRU-UHFFFAOYSA-N 1-[4-[2-[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxyethyl]piperidin-1-yl]-2-(dimethylamino)ethanone Chemical compound N1=CN=C2C=C(OCCC3CCN(CC3)C(=O)CN(C)C)C(OC)=CC2=C1NC1=CC=C(Cl)C=C1F VYRBUOLLDDZYRU-UHFFFAOYSA-N 0.000 claims 1
- VTPJWYMUVTZUAY-UHFFFAOYSA-N 1-[4-[[4-(4-bromo-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]-2-(dimethylamino)ethanone Chemical compound N1=CN=C2C=C(OCC3CCN(CC3)C(=O)CN(C)C)C(OC)=CC2=C1NC1=CC=C(Br)C=C1F VTPJWYMUVTZUAY-UHFFFAOYSA-N 0.000 claims 1
- WLAGZIBGTRJBLJ-UHFFFAOYSA-N 1-[4-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]-2-(2-methoxyethylamino)ethanone Chemical compound C1CN(C(=O)CNCCOC)CCC1COC1=CC2=NC=NC(NC=3C(=CC(Cl)=CC=3)F)=C2C=C1OC WLAGZIBGTRJBLJ-UHFFFAOYSA-N 0.000 claims 1
- HFWPMRCXAOALMT-UHFFFAOYSA-N 1-[4-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]-2-(3,3-difluoropyrrolidin-1-yl)ethanone Chemical compound N1=CN=C2C=C(OCC3CCN(CC3)C(=O)CN3CC(F)(F)CC3)C(OC)=CC2=C1NC1=CC=C(Cl)C=C1F HFWPMRCXAOALMT-UHFFFAOYSA-N 0.000 claims 1
- ILOFHIKOHSYOMT-UHFFFAOYSA-N 1-[4-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]-2-(dimethylamino)ethanone Chemical compound N1=CN=C2C=C(OCC3CCN(CC3)C(=O)CN(C)C)C(OC)=CC2=C1NC1=CC=C(Cl)C=C1F ILOFHIKOHSYOMT-UHFFFAOYSA-N 0.000 claims 1
- FAANUEQUJPCZNF-UHFFFAOYSA-N 1-[4-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]-2-(methylamino)ethanone Chemical compound C1CN(C(=O)CNC)CCC1COC1=CC2=NC=NC(NC=3C(=CC(Cl)=CC=3)F)=C2C=C1OC FAANUEQUJPCZNF-UHFFFAOYSA-N 0.000 claims 1
- HCYPMPNKQOOPLW-IBGZPJMESA-N 1-[4-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]-2-[(3s)-3-hydroxypyrrolidin-1-yl]ethanone Chemical compound N1=CN=C2C=C(OCC3CCN(CC3)C(=O)CN3C[C@@H](O)CC3)C(OC)=CC2=C1NC1=CC=C(Cl)C=C1F HCYPMPNKQOOPLW-IBGZPJMESA-N 0.000 claims 1
- OCYPSDDYPPRKEV-UHFFFAOYSA-N 1-[4-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]-2-piperidin-1-ylethanone Chemical compound N1=CN=C2C=C(OCC3CCN(CC3)C(=O)CN3CCCCC3)C(OC)=CC2=C1NC1=CC=C(Cl)C=C1F OCYPSDDYPPRKEV-UHFFFAOYSA-N 0.000 claims 1
- PZGRIHOWUZQLNY-UHFFFAOYSA-N 1-[4-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]-2-pyrrolidin-1-ylethanone Chemical compound N1=CN=C2C=C(OCC3CCN(CC3)C(=O)CN3CCCC3)C(OC)=CC2=C1NC1=CC=C(Cl)C=C1F PZGRIHOWUZQLNY-UHFFFAOYSA-N 0.000 claims 1
- ZLGXMJUMDIQCQX-UHFFFAOYSA-N 2-(4-acetylpiperazin-1-yl)-1-[4-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]ethanone Chemical compound N1=CN=C2C=C(OCC3CCN(CC3)C(=O)CN3CCN(CC3)C(C)=O)C(OC)=CC2=C1NC1=CC=C(Cl)C=C1F ZLGXMJUMDIQCQX-UHFFFAOYSA-N 0.000 claims 1
- IKUGFRROILOMDR-WMPKNSHKSA-N 2-[(3ar,6as)-3a,4,6,6a-tetrahydro-[1,3]dioxolo[4,5-c]pyrrol-5-yl]-1-[4-[[4-(4-chloro-2-fluoroanilino)-6-methoxyquinazolin-7-yl]oxymethyl]piperidin-1-yl]ethanone Chemical compound N1=CN=C2C=C(OCC3CCN(CC3)C(=O)CN3C[C@@H]4OCO[C@@H]4C3)C(OC)=CC2=C1NC1=CC=C(Cl)C=C1F IKUGFRROILOMDR-WMPKNSHKSA-N 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 241000790917 Dioxys <bee> Species 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 230000001772 anti-angiogenic effect Effects 0.000 claims 1
- 230000002137 anti-vascular effect Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 0 Cc1cc2ncnc(*c3ccc(*)cc3F)c2cc1* Chemical compound Cc1cc2ncnc(*c3ccc(*)cc3F)c2cc1* 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0318423.1A GB0318423D0 (en) | 2003-08-06 | 2003-08-06 | Chemical compounds |
| PCT/GB2004/003393 WO2005013998A1 (en) | 2003-08-06 | 2004-08-05 | Quinazoline derivatives as inhibitors of vegf receptor tyrosine kinases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007501212A JP2007501212A (ja) | 2007-01-25 |
| JP2007501212A5 true JP2007501212A5 (enExample) | 2007-09-06 |
Family
ID=27839733
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006522409A Withdrawn JP2007501212A (ja) | 2003-08-06 | 2004-08-05 | Ｖｅｇｆ受容体型チロシンキナーゼの阻害薬としてのキナゾリン誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20070027145A1 (enExample) |
| EP (1) | EP1653965A1 (enExample) |
| JP (1) | JP2007501212A (enExample) |
| KR (1) | KR20060058781A (enExample) |
| CN (1) | CN1863534A (enExample) |
| AU (1) | AU2004262982A1 (enExample) |
| BR (1) | BRPI0413280A (enExample) |
| CA (1) | CA2534422A1 (enExample) |
| GB (1) | GB0318423D0 (enExample) |
| IL (1) | IL173483A0 (enExample) |
| MX (1) | MXPA06001394A (enExample) |
| NO (1) | NO20060641L (enExample) |
| WO (1) | WO2005013998A1 (enExample) |
| ZA (1) | ZA200601030B (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1625555A (zh) * | 2002-02-01 | 2005-06-08 | 阿斯特拉曾尼卡有限公司 | 喹唑啉化合物 |
| US7569577B2 (en) | 2003-09-16 | 2009-08-04 | Astrazeneca Ab | Quinazoline derivatives as tyrosine kinase inhibitors |
| GB0326459D0 (en) | 2003-11-13 | 2003-12-17 | Astrazeneca Ab | Quinazoline derivatives |
| ATE413389T1 (de) | 2004-02-03 | 2008-11-15 | Astrazeneca Ab | Chinazolinderivate |
| GB0519879D0 (en) | 2005-09-30 | 2005-11-09 | Astrazeneca Ab | Chemical process |
| US7829574B2 (en) | 2008-05-09 | 2010-11-09 | Hutchison Medipharma Enterprises Limited | Substituted quinazoline compounds and their use in treating angiogenesis-related diseases |
| WO2010005527A1 (en) | 2008-06-30 | 2010-01-14 | Angioblast Systems, Inc. | Treatment of eye diseases and excessive neovascularization using a combined therapy |
| KR20120107993A (ko) * | 2009-12-15 | 2012-10-04 | 뉴롭, 인코포레이티드 | 신경계 장애의 치료를 위한 화합물 |
| TWI577671B (zh) * | 2011-11-14 | 2017-04-11 | Sunshine Lake Pharma Co Ltd | Aminoquinazoline derivatives and salts thereof and methods of use thereof |
| CN105330653A (zh) | 2014-08-11 | 2016-02-17 | 石药集团中奇制药技术（石家庄）有限公司 | 喹唑啉衍生物 |
| US9854482B2 (en) * | 2015-04-21 | 2017-12-26 | International Business Machines Corporation | Controlling a delivery of voice communications over a cellular data network or a wireless network based on user's profile |
| CA3012718A1 (en) | 2016-02-08 | 2017-08-17 | Vitrisa Therapeutics, Inc. | Compositions with improved intravitreal half-life and uses thereof |
| CN106565681B (zh) * | 2016-11-10 | 2019-07-09 | 中国医学科学院放射医学研究所 | 含硝基咪唑基团的苯胺喹唑啉类化合物及其制备方法和应用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9624482D0 (en) * | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| WO1997030035A1 (en) * | 1996-02-13 | 1997-08-21 | Zeneca Limited | Quinazoline derivatives as vegf inhibitors |
| PT885198E (pt) * | 1996-03-05 | 2002-06-28 | Astrazeneca Ab | Derivados de 4-anilinoquinazolina |
| GB9718972D0 (en) * | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
| HK1039126B (en) * | 1998-10-08 | 2005-09-30 | 阿斯特拉曾尼卡有限公司 | Quinazoline derivatives |
| BRPI0017548B8 (pt) * | 1999-02-10 | 2023-05-02 | Astrazeneca Ab | Composto |
| EE05330B1 (et) * | 1999-11-05 | 2010-08-16 | Astrazeneca Ab | Kinasoliini derivaadid kui VEGF-i inhibiitorid |
| CN1240688C (zh) * | 2000-04-07 | 2006-02-08 | 阿斯特拉曾尼卡有限公司 | 喹唑啉化合物 |
-
2003
- 2003-08-06 GB GBGB0318423.1A patent/GB0318423D0/en not_active Ceased
-
2004
- 2004-08-05 MX MXPA06001394A patent/MXPA06001394A/es unknown
- 2004-08-05 AU AU2004262982A patent/AU2004262982A1/en not_active Abandoned
- 2004-08-05 BR BRPI0413280-7A patent/BRPI0413280A/pt not_active IP Right Cessation
- 2004-08-05 JP JP2006522409A patent/JP2007501212A/ja not_active Withdrawn
- 2004-08-05 EP EP04801817A patent/EP1653965A1/en not_active Withdrawn
- 2004-08-05 WO PCT/GB2004/003393 patent/WO2005013998A1/en not_active Ceased
- 2004-08-05 KR KR1020067002552A patent/KR20060058781A/ko not_active Withdrawn
- 2004-08-05 CA CA002534422A patent/CA2534422A1/en not_active Abandoned
- 2004-08-05 US US10/566,841 patent/US20070027145A1/en not_active Abandoned
- 2004-08-05 CN CNA2004800288013A patent/CN1863534A/zh active Pending
-
2006
- 2006-01-31 IL IL173483A patent/IL173483A0/en unknown
- 2006-02-03 ZA ZA200601030A patent/ZA200601030B/en unknown
- 2006-02-09 NO NO20060641A patent/NO20060641L/no not_active Application Discontinuation
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