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 31
- 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
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000000304 alkynyl group Chemical group 0.000 claims 7
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 7
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 6
- 125000005842 heteroatom 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 atom Chemical group C* 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- -1 G Lifluoromethyl Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- QPJDMGCKMHUXFD-UHFFFAOYSA-N cyanogen chloride Chemical compound ClC#N QPJDMGCKMHUXFD-UHFFFAOYSA-N 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- OUYYNZDOJHSQBW-UHFFFAOYSA-N cyanomethanimidamide Chemical group NC(=N)C#N OUYYNZDOJHSQBW-UHFFFAOYSA-N 0.000 claims 1
- QGBSISYHAICWAH-UHFFFAOYSA-N dicyandiamide Chemical compound NC(N)=NC#N QGBSISYHAICWAH-UHFFFAOYSA-N 0.000 claims 1
- PQIOSYKVBBWRRI-UHFFFAOYSA-N methylphosphonyl difluoride Chemical group CP(F)(F)=O PQIOSYKVBBWRRI-UHFFFAOYSA-N 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 150000003839 salts Chemical class 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 (enExample) | 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)
| Country | Link |
|---|---|
| EP (1) | EP1567506A4 (enExample) |
| JP (1) | JP4611745B2 (enExample) |
| AU (1) | AU2003291394B2 (enExample) |
| CA (1) | CA2506503A1 (enExample) |
| NZ (1) | NZ540092A (enExample) |
| WO (1) | WO2004046101A2 (enExample) |
Families Citing this family (21)
| 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 |
| CA2536140A1 (en) * | 2003-08-18 | 2005-02-24 | Pfizer Products Inc. | Dosing schedule for erbb2 anticancer agents |
| AU2004270016A1 (en) * | 2003-09-11 | 2005-03-17 | Hadasit Medical Research Services And Development Ltd. | Radiolabeled anilinoquinazolines and their use in radioimaging and radiotherapy |
| GB0326459D0 (en) | 2003-11-13 | 2003-12-17 | Astrazeneca Ab | Quinazoline derivatives |
| CN101056639A (zh) | 2004-09-15 | 2007-10-17 | 詹森药业有限公司 | 噻唑并吡啶激酶抑制剂 |
| 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 |
| CL2007003158A1 (es) * | 2006-11-02 | 2008-05-16 | Astrazeneca Ab | Procedimiento de preparacion de compuestos derivados de quinazolina o sus sales farmaceuticamente aceptables; compuestos intermediarios; procedimiento de preparacion. |
| KR20100087185A (ko) | 2007-10-29 | 2010-08-03 | 낫코 파마 리미티드 | 항암제로서의 신규한 4-(테트라졸-5-일)-퀴나졸린 유도체 |
| WO2011002523A1 (en) | 2009-07-02 | 2011-01-06 | Kanionusa Inc. | Phosphorus containing quinazoline compounds and methods of use |
| HK1217092A1 (zh) | 2013-02-15 | 2016-12-23 | Kala Pharmaceuticals, Inc. | 治疗性化合物及其用途 |
| 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 |
| BR112015020139A2 (pt) | 2013-02-20 | 2017-07-18 | Kala Pharmaceuticals Inc | compostos terapêuticos e usos dos mesmos |
| KR20160099084A (ko) | 2013-11-01 | 2016-08-19 | 칼라 파마슈티컬스, 인크. | 치료 화합물의 결정질 형태 및 그의 용도 |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| EP3402536A4 (en) | 2016-01-13 | 2019-07-03 | Hadasit Medical Research Services And Development Limited | RADIOACTIVELY MARKED ERLOTINIB ANALOGUES AND USES THEREOF |
| EP3509423A4 (en) | 2016-09-08 | 2020-05-13 | Kala Pharmaceuticals, Inc. | CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF |
| CA3036336A1 (en) | 2016-09-08 | 2018-03-15 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| CA3036065A1 (en) | 2016-09-08 | 2018-03-15 | 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 |
| IL292837B2 (en) * | 2019-12-02 | 2025-12-01 | Academia Sinica | Pdia4 inhibitors and use thereof for inhibiting ?-cell pathogenesis and treating diabetes |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69522717T2 (de) | 1995-03-30 | 2002-02-14 | Pfizer Inc., New York | Chinazolinderivate |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| JP4471404B2 (ja) * | 1996-02-13 | 2010-06-02 | アストラゼネカ ユーケイ リミテッド | Ｖｅｇｆインヒビターとしてのキナゾリン誘導体 |
| HRP970371A2 (en) | 1996-07-13 | 1998-08-31 | Kathryn Jane Smith | Heterocyclic compounds |
| ES2356886T3 (es) * | 1998-03-31 | 2011-04-14 | Kyowa Hakko Kirin Co., Ltd. | Compuestos heterocíclicos nitrogenados. |
| 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 AU AU2003291394A patent/AU2003291394B2/en not_active Expired - Fee Related
- 2003-11-10 JP JP2004553551A patent/JP4611745B2/ja not_active Expired - Fee Related
- 2003-11-10 WO PCT/US2003/035670 patent/WO2004046101A2/en not_active Ceased