JP2006508979A5 - - Google Patents
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- Publication number
- JP2006508979A5 JP2006508979A5 JP2004553551A JP2004553551A JP2006508979A5 JP 2006508979 A5 JP2006508979 A5 JP 2006508979A5 JP 2004553551 A JP2004553551 A JP 2004553551A JP 2004553551 A JP2004553551 A JP 2004553551A JP 2006508979 A5 JP2006508979 A5 JP 2006508979A5
- Authority
- JP
- Japan
- Prior art keywords
- heteroaryl
- aryl
- heterocyclyl
- arylalkyl
- alkyl
- 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
Links
- 125000000623 heterocyclic group Chemical group 0.000 claims 33
- 125000001072 heteroaryl group Chemical group 0.000 claims 32
- 125000003118 aryl group Chemical group 0.000 claims 30
- 125000003710 aryl alkyl group Chemical group 0.000 claims 24
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 22
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 22
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims 15
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 12
- BPXYEYJNCXITEY-UHFFFAOYSA-N diazonio(trifluoromethoxy)azanide Chemical compound FC(F)(F)ON=[N+]=[N-] BPXYEYJNCXITEY-UHFFFAOYSA-N 0.000 claims 11
- 125000004043 oxo group Chemical group O=* 0.000 claims 10
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 9
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 8
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000000304 alkynyl group Chemical group 0.000 claims 7
- 125000004435 hydrogen atoms Chemical class [H]* 0.000 claims 7
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 6
- 125000005842 heteroatoms Chemical group 0.000 claims 5
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004432 carbon atoms Chemical group C* 0.000 claims 3
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 3
- QPJDMGCKMHUXFD-UHFFFAOYSA-N Cyanogen chloride Chemical compound ClC#N QPJDMGCKMHUXFD-UHFFFAOYSA-N 0.000 claims 2
- -1 G Lifluoromethyl Chemical group 0.000 claims 2
- 125000004429 atoms Chemical group 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- YCKRFDGAMUMZLT-UHFFFAOYSA-N fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 claims 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 2
- PQIOSYKVBBWRRI-UHFFFAOYSA-N Methylphosphonyl difluoride Chemical group CP(F)(F)=O PQIOSYKVBBWRRI-UHFFFAOYSA-N 0.000 claims 1
- 125000005418 aryl aryl group Chemical group 0.000 claims 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- QGBSISYHAICWAH-UHFFFAOYSA-N cyanoguanidine Chemical compound NC(N)=NC#N QGBSISYHAICWAH-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrugs Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42754402P | 2002-11-20 | 2002-11-20 | |
| PCT/US2003/035670 WO2004046101A2 (en) | 2002-11-20 | 2003-11-10 | Cyanoguanidines and cyanoamidines as erbb2 and egfr inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006508979A JP2006508979A (ja) | 2006-03-16 |
| JP2006508979A5 true JP2006508979A5 (US07846941-20101207-C00217.png) | 2006-08-03 |
| JP4611745B2 JP4611745B2 (ja) | 2011-01-12 |
Family
ID=32326558
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004553551A Expired - Fee Related JP4611745B2 (ja) | 2002-11-20 | 2003-11-10 | ＥｒｂＢ２及びＥＧＦＲ阻害剤としてのシアノグアニジン及びシアノアミジン |
Country Status (6)
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN1838959A (zh) * | 2003-08-18 | 2006-09-27 | 辉瑞产品公司 | Erbb2抗癌剂的给药方案 |
| WO2005023315A2 (en) * | 2003-09-11 | 2005-03-17 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Radiolabeled anilinoquinazolines and their use in radioimaging and radiotherapy |
| JP2008513463A (ja) | 2004-09-15 | 2008-05-01 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | チアゾロピリジンキナーゼ阻害剤 |
| US7579356B2 (en) | 2005-05-04 | 2009-08-25 | Janssen Pharmaceutica Nv | Thia-tetraazaacenaphthylene kinase inhibitors |
| DE102006012251A1 (de) * | 2006-03-15 | 2007-11-08 | Grünenthal GmbH | Substituierte 4-Amino-chinazolin-Derivate und ihre Verwendung zur Herstellung von Arzneimitteln |
| US7851623B2 (en) * | 2006-11-02 | 2010-12-14 | Astrazeneca Ab | Chemical process |
| AU2008320342B2 (en) | 2007-10-29 | 2012-07-26 | Natco Pharma Limited | Novel 4-(tetrazol-5-yl)-quinazoline derivatives as anti cancer agents |
| CA2804190A1 (en) | 2009-07-02 | 2011-01-06 | Newgen Therapeutics, Inc. | Phosphorus containing quinazoline compounds and methods of use |
| AU2014216178B2 (en) | 2013-02-15 | 2018-06-28 | KALA BIO, Inc. | Therapeutic compounds and uses thereof |
| US9688688B2 (en) | 2013-02-20 | 2017-06-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof |
| ES2831625T3 (es) | 2013-02-20 | 2021-06-09 | Kala Pharmaceuticals Inc | Compuestos terapéuticos y sus usos |
| JP6426194B2 (ja) | 2013-11-01 | 2018-11-21 | カラ ファーマシューティカルズ インコーポレイテッド | 治療用化合物の結晶形態及びその使用 |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| WO2017122205A1 (en) | 2016-01-13 | 2017-07-20 | Hadasit Medical Research Services And Development Ltd. | Radiolabeled erlotinib analogs and uses thereof |
| US10392399B2 (en) | 2016-09-08 | 2019-08-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| BR112019004463A2 (pt) | 2016-09-08 | 2019-05-28 | Kala Pharmaceuticals Inc | formas cristalinas de compostos terapêuticos, seus processos de obtenção e seus métodos de uso |
| EP3509422A4 (en) | 2016-09-08 | 2020-05-20 | Kala Pharmaceuticals, Inc. | CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF |
| CN108285421A (zh) * | 2018-01-26 | 2018-07-17 | 黑龙江鑫创生物科技开发有限公司 | 一种微通道反应器合成拉帕替尼中间体的方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2216796C (en) * | 1995-03-30 | 2003-09-02 | Pfizer Inc. | Quinazoline derivatives |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| EP0880508B1 (en) * | 1996-02-13 | 2003-04-16 | AstraZeneca AB | Quinazoline derivatives as vegf inhibitors |
| HRP970371A2 (en) | 1996-07-13 | 1998-08-31 | Kathryn Jane Smith | Heterocyclic compounds |
| ATE496035T1 (de) | 1998-03-31 | 2011-02-15 | Kyowa Hakko Kirin Co Ltd | Stickstoffenthaltende heterocyclische verbindungen |
| GB2345486A (en) | 1999-01-11 | 2000-07-12 | Glaxo Group Ltd | Heteroaromatic protein tyrosine kinase inhibitors |
| UA71945C2 (en) | 1999-01-27 | 2005-01-17 | Pfizer Prod Inc | Substituted bicyclic derivatives being used as anticancer agents |
| MXPA02012870A (es) | 2000-06-22 | 2003-05-14 | Pfizer Prod Inc | Derivados biciclicos sustituidos para el tratamiento del crecimiento celular anormal. |
-
2003
- 2003-11-10 EP EP03768789A patent/EP1567506A4/en not_active Withdrawn
- 2003-11-10 CA CA002506503A patent/CA2506503A1/en not_active Abandoned
- 2003-11-10 NZ NZ540092A patent/NZ540092A/en not_active IP Right Cessation
- 2003-11-10 JP JP2004553551A patent/JP4611745B2/ja not_active Expired - Fee Related
- 2003-11-10 WO PCT/US2003/035670 patent/WO2004046101A2/en active Application Filing
- 2003-11-10 AU AU2003291394A patent/AU2003291394B2/en not_active Expired - Fee Related
