JP2012508252A5 - - Google Patents
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- Publication number
- JP2012508252A5 JP2012508252A5 JP2011535715A JP2011535715A JP2012508252A5 JP 2012508252 A5 JP2012508252 A5 JP 2012508252A5 JP 2011535715 A JP2011535715 A JP 2011535715A JP 2011535715 A JP2011535715 A JP 2011535715A JP 2012508252 A5 JP2012508252 A5 JP 2012508252A5
- Authority
- JP
- Japan
- Prior art keywords
- heteroaryl
- aryl
- alkyl
- heterocycloalkenyl
- cycloalkyl
- 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
- 125000001072 heteroaryl group Chemical group 0.000 claims 43
- 125000003118 aryl group Chemical group 0.000 claims 34
- 150000001875 compounds Chemical class 0.000 claims 29
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 28
- 125000000217 alkyl group Chemical group 0.000 claims 27
- 125000000753 cycloalkyl group Chemical group 0.000 claims 26
- 125000003342 alkenyl group Chemical group 0.000 claims 22
- 125000000304 alkynyl group Chemical group 0.000 claims 22
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 22
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 22
- 229910052757 nitrogen Inorganic materials 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 229910052721 tungsten Inorganic materials 0.000 claims 4
- -1 or NH Inorganic materials 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 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
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 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
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11286508P | 2008-11-10 | 2008-11-10 | |
| US61/112,865 | 2008-11-10 | ||
| PCT/US2009/063684 WO2010054285A2 (en) | 2008-11-10 | 2009-11-09 | Fused bicyclic and tricyclic pyrimidine compounds as tyrosine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012508252A JP2012508252A (ja) | 2012-04-05 |
| JP2012508252A5 true JP2012508252A5 (enExample) | 2014-09-04 |
| JP5781934B2 JP5781934B2 (ja) | 2015-09-24 |
Family
ID=42153606
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011535715A Active JP5781934B2 (ja) | 2008-11-10 | 2009-11-09 | チロシンキナーゼ阻害剤としての融合２環および３環ピリミジン化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8507502B2 (enExample) |
| JP (1) | JP5781934B2 (enExample) |
| KR (1) | KR101703941B1 (enExample) |
| CN (1) | CN102264745B (enExample) |
| TW (1) | TWI385174B (enExample) |
| WO (1) | WO2010054285A2 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2014202057B2 (en) * | 2010-06-23 | 2016-05-05 | Hanmi Science Co., Ltd. | Novel Fused Pyrimidine Derivatives for Inhibition of Tyrosine Kinase Activity |
| MX342164B (es) * | 2010-06-23 | 2016-09-19 | Hanmi Science Co Ltd | Derivados de pirimidina fusionados novedosos para la inhibicion de la actividad de tirosina cinasa. |
| EP2595993B1 (en) | 2010-07-23 | 2018-04-18 | President and Fellows of Harvard College | Tricyclic proteasome activity enhancing compounds |
| TW201217387A (en) | 2010-09-15 | 2012-05-01 | Hoffmann La Roche | Azabenzothiazole compounds, compositions and methods of use |
| CN103087077B (zh) * | 2011-11-03 | 2016-05-18 | 上海希迈医药科技有限公司 | 噻吩并嘧啶和呋喃并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| EP2806875B1 (en) | 2012-01-25 | 2017-07-19 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating compounds |
| AU2013202373B2 (en) * | 2012-01-25 | 2016-04-14 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| CN103360407B (zh) * | 2012-04-10 | 2016-06-22 | 上海希迈医药科技有限公司 | 一种噻吩并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| CN104140395B (zh) * | 2013-05-08 | 2018-07-24 | 中国医学科学院药物研究所 | 丁炔酰胺衍生物及其制法和药物组合物与用途 |
| CN104016983B (zh) * | 2013-10-08 | 2018-11-02 | 上海创诺制药有限公司 | 吡咯并三嗪类衍生物及其制法和用途 |
| FR3015483B1 (fr) | 2013-12-23 | 2016-01-01 | Servier Lab | Nouveaux derives de thienopyrimidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| CN104974104B (zh) * | 2014-04-03 | 2019-10-01 | 中国医学科学院药物研究所 | 含噁唑的丙炔酰胺类衍生物及其制法和药物组合物与用途 |
| CN104974109B (zh) * | 2014-04-03 | 2019-10-01 | 中国医学科学院药物研究所 | 含噻唑的丙炔酰胺类衍生物及其制法和药物组合物与用途 |
| CN105085406B (zh) * | 2014-05-16 | 2020-11-03 | 中国医学科学院药物研究所 | 含苯并咪唑环丙炔酰胺类衍生物及其制法和药物组合物与用途 |
| CN106458969A (zh) * | 2014-08-25 | 2017-02-22 | 四川海思科制药有限公司 | 一种(取代的苯基)(取代的嘧啶)胺基衍生物及其制备方法和药物用途 |
| FR3037959B1 (fr) * | 2015-06-23 | 2017-08-04 | Servier Lab | Nouveaux derives bicycliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| EP3111960B1 (en) * | 2015-07-03 | 2019-12-11 | Kyoto University | Nuclear medicine diagnostic imaging agent |
| CN105061462B (zh) * | 2015-08-18 | 2017-05-24 | 沈阳药科大学 | 含有酰胺的四氢苯并[4,5]噻吩并[2,3‑d]嘧啶类化合物及其应用 |
| CN105061460B (zh) * | 2015-08-18 | 2017-06-30 | 沈阳药科大学 | 含有硫醚结构的四氢苯并[4,5]噻吩并[2,3‑d]嘧啶类化合物及其应用 |
| CN105061461B (zh) * | 2015-08-18 | 2017-06-30 | 沈阳药科大学 | 含有苄胺结构的四氢苯并[4,5]噻吩并[2,3‑d]嘧啶类化合物及其应用 |
| CN105037385B (zh) * | 2015-08-18 | 2017-04-26 | 沈阳药科大学 | 含有哌嗪结构的四氢苯并[4,5]噻吩并[2,3‑d]嘧啶类化合物及其应用 |
| FR3046792B1 (fr) * | 2016-01-19 | 2018-02-02 | Les Laboratoires Servier | Nouveaux derives d'ammonium, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| CN106946896B (zh) * | 2017-03-30 | 2019-05-21 | 成都知普莱生物医药科技有限公司 | 呋喃并[2,3-d]嘧啶-4-胺衍生物 |
| WO2020132384A1 (en) | 2018-12-21 | 2020-06-25 | Celgene Corporation | Thienopyridine inhibitors of ripk2 |
| MX2021010319A (es) * | 2019-03-01 | 2021-12-10 | Revolution Medicines Inc | Compuestos biciclicos de heteroarilo y usos de estos. |
| WO2021041539A2 (en) * | 2019-08-28 | 2021-03-04 | Ferro Therapeutics, Inc. | Compounds and methods of use |
| TWI809967B (zh) | 2021-07-06 | 2023-07-21 | 石 全 | (s, e)-4-(二甲胺基)-n-(3-(4-(2-羥基-1-苯乙胺基)-6-苯基呋喃并[2,3-d]嘧啶-5-基)苯基)丁-2-烯醯胺游離鹼之晶型 |
| TWI906763B (zh) * | 2024-02-05 | 2025-12-01 | 財團法人國家衛生研究院 | 表皮生長因子受體抑制劑 |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL112249A (en) * | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
| GB9424233D0 (en) * | 1994-11-30 | 1995-01-18 | Zeneca Ltd | Quinazoline derivatives |
| SI9620103A (sl) * | 1995-07-06 | 1998-10-31 | Novartis Ag | Pirolopirimidini in postopki za njihovo pripravo |
| EA001595B1 (ru) | 1996-04-12 | 2001-06-25 | Варнер-Ламберт Компани | Необратимые ингибиторы тирозинкиназ |
| GB9613021D0 (en) | 1996-06-21 | 1996-08-28 | Pharmacia Spa | Bicyclic 4-aralkylaminopyrimidine derivatives as tyrosine kinase inhibitors |
| EA199900021A1 (ru) * | 1996-07-13 | 1999-08-26 | Глаксо, Груп Лимитед | Бициклические гетероароматические соединения в качестве ингибиторов протеинтирозинкиназы |
| US6002008A (en) * | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| CA2361174C (en) | 1999-02-27 | 2009-10-27 | Boehringer Ingelheim Pharma Kg | 4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transduction mediated by tyrosine kinases |
| HK1044769B (zh) | 1999-06-21 | 2005-02-25 | 贝林格尔英格海姆法玛两合公司 | 雙環雜環化合物，含有該化合物的藥物組合物，該化合物的用途及其製備方法 |
| IL150594A0 (en) | 2000-01-07 | 2003-02-12 | Ustav Ex Botan Adademie Ved Ce | Purine derivatives, process for their preparation and use |
| WO2001077104A1 (de) | 2000-04-08 | 2001-10-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Bicyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung |
| DE10042060A1 (de) | 2000-08-26 | 2002-03-07 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| DE10042062A1 (de) | 2000-08-26 | 2002-03-07 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Hertellung |
| DE10042064A1 (de) | 2000-08-26 | 2002-03-07 | Boehringer Ingelheim Pharma | Chinazoline, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| DE10042061A1 (de) | 2000-08-26 | 2002-03-07 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| DE10206505A1 (de) | 2002-02-16 | 2003-08-28 | Boehringer Ingelheim Pharma | Neue Arzneimittelkompositionen auf der Basis von Anticholinergika und EGFR-Kinase-Hemmern |
| US7776315B2 (en) * | 2000-10-31 | 2010-08-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmaceutical compositions based on anticholinergics and additional active ingredients |
| DE10063435A1 (de) * | 2000-12-20 | 2002-07-04 | Boehringer Ingelheim Pharma | Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| DE10204462A1 (de) | 2002-02-05 | 2003-08-07 | Boehringer Ingelheim Pharma | Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse |
| DE10221018A1 (de) | 2002-05-11 | 2003-11-27 | Boehringer Ingelheim Pharma | Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie |
| DE10230751A1 (de) | 2002-07-09 | 2004-01-22 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittelkompositionen auf der Basis neuer Anticholinergika und EGFR-Kinase-Hemmern |
| SE0202462D0 (sv) * | 2002-08-14 | 2002-08-14 | Astrazeneca Ab | Novel use |
| DE10334226A1 (de) | 2003-07-28 | 2005-02-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse |
| US7399865B2 (en) * | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| DE102004001607A1 (de) | 2004-01-09 | 2005-08-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittelkombinationen auf der Basis von Scopin- oder Tropensäureestern mit EGFR-Kinase-Hemmern |
| US20050239806A1 (en) * | 2004-01-13 | 2005-10-27 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
| US20050239778A1 (en) * | 2004-04-22 | 2005-10-27 | Boehringer Ingelheim International Gmbh | Novel medicament combinations for the treatment of respiratory diseases |
| US7674907B2 (en) * | 2004-07-23 | 2010-03-09 | Amgen Inc. | Furanopyridine derivatives and methods of use |
| US20060035893A1 (en) | 2004-08-07 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
| ATE476434T1 (de) * | 2004-12-09 | 2010-08-15 | Xention Ltd | Thienopyridinderivate als kaliumkanalinhibitoren |
| EP1845992A1 (de) | 2005-02-04 | 2007-10-24 | Boehringer Ingelheim International GmbH | Verwendung von tyrosinkinase-inhibitoren zur behandlung der chronischen rhinosinusitis |
| DE102005030733A1 (de) * | 2005-07-01 | 2007-01-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittelkombinationen zur Behandlung von Atemwegserkrankungen enthaltend langwirksame Beta-2-Agonisten und wenigstens einen weiteren Wirkstoff |
| WO2007056208A2 (en) | 2005-11-02 | 2007-05-18 | Cytovia, Inc. | N-arylalkyl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof |
| PT1948180E (pt) | 2005-11-11 | 2013-05-10 | Boehringer Ingelheim Int | Tratamento de combinação de cancro compreendendo inibidores de egfr/her2 |
| AR059901A1 (es) | 2006-03-20 | 2008-05-07 | Bayer Pharmaceuticals Corp | Compuestos de tetrahidropiridotienopirimidina utiles para tratar o prevenir trastornos proliferativos celulares. |
| CN101100466B (zh) | 2006-07-05 | 2013-12-25 | 天津和美生物技术有限公司 | 不可逆蛋白质酪氨酸磷酰化酶抑制剂及其制备和应用 |
| CA2699349C (en) | 2007-09-14 | 2016-04-19 | Bayer Schering Pharma Aktiengesellschaft | Substituted tricyclic heterocyclic compounds for use as egfr inhibitors |
-
2009
- 2009-11-09 US US12/614,584 patent/US8507502B2/en active Active
- 2009-11-09 TW TW098137894A patent/TWI385174B/zh active
- 2009-11-09 WO PCT/US2009/063684 patent/WO2010054285A2/en not_active Ceased
- 2009-11-09 KR KR1020117011218A patent/KR101703941B1/ko active Active
- 2009-11-09 CN CN200980144458.1A patent/CN102264745B/zh active Active
- 2009-11-09 JP JP2011535715A patent/JP5781934B2/ja active Active
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