JP2013529619A5 - - Google Patents
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- Publication number
- JP2013529619A5 JP2013529619A5 JP2013515902A JP2013515902A JP2013529619A5 JP 2013529619 A5 JP2013529619 A5 JP 2013529619A5 JP 2013515902 A JP2013515902 A JP 2013515902A JP 2013515902 A JP2013515902 A JP 2013515902A JP 2013529619 A5 JP2013529619 A5 JP 2013529619A5
- Authority
- JP
- Japan
- Prior art keywords
- chloropyrimidin
- thiazol
- tert
- butyl
- preparation
- 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.)
- Pending
Links
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
- XHYXSIFQGLTLTM-UHFFFAOYSA-N 3-[2-tert-butyl-5-(2-chloropyrimidin-4-yl)-1,3-thiazol-4-yl]-2-fluoroaniline Chemical compound S1C(C(C)(C)C)=NC(C=2C(=C(N)C=CC=2)F)=C1C1=CC=NC(Cl)=N1 XHYXSIFQGLTLTM-UHFFFAOYSA-N 0.000 description 1
- NDJDJAPJBPWWIV-UHFFFAOYSA-N N-[3-[2-tert-butyl-5-(2-chloropyrimidin-4-yl)-1,3-thiazol-4-yl]-2-fluorophenyl]methanesulfonamide Chemical compound S1C(C(C)(C)C)=NC(C=2C(=C(NS(C)(=O)=O)C=CC=2)F)=C1C1=CC=NC(Cl)=N1 NDJDJAPJBPWWIV-UHFFFAOYSA-N 0.000 description 1
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 238000005694 sulfonylation reaction Methods 0.000 description 1
Description
工程３. Ｎ−(３−(２−ｔｅｒｔ−ブチル−５−(２−クロロピリミジン−４−イル)チアゾール−４−イル)−２−フルオロフェニル)メタンスルホンアミドの製造：
表題中間体を、３−(２−ｔｅｒｔ−ブチル−５−(２−クロロピリミジン−４−イル)チアゾール−４−イル)−２−フルオロアニリンから、出発物質IV、工程３の製造に使用したスルホニル化法に従い、溶媒としてピリジンを使用して製造した：LCMS(m/z): 441.1(MH+), tR = 1.04 min。
表題中間体を、３−(２−ｔｅｒｔ−ブチル−５−(２−クロロピリミジン−４−イル)チアゾール−４−イル)−２−フルオロアニリンから、出発物質IV、工程３の製造に使用したスルホニル化法に従い、溶媒としてピリジンを使用して製造した：LCMS(m/z): 441.1(MH+), tR = 1.04 min。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35860310P | 2010-06-25 | 2010-06-25 | |
| US61/358,603 | 2010-06-25 | ||
| US36853410P | 2010-07-28 | 2010-07-28 | |
| US61/368,534 | 2010-07-28 | ||
| PCT/EP2011/060561 WO2011161216A1 (en) | 2010-06-25 | 2011-06-23 | Heteroaryl compounds and compositions as protein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013529619A JP2013529619A (ja) | 2013-07-22 |
| JP2013529619A5 true JP2013529619A5 (ja) | 2014-07-24 |
Family
ID=44280749
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013515902A Pending JP2013529619A (ja) | 2010-06-25 | 2011-06-23 | タンパク質キナーゼ阻害剤としてのヘテロアリール化合物および組成物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20130096149A1 (ja) |
| EP (1) | EP2585454A1 (ja) |
| JP (1) | JP2013529619A (ja) |
| KR (2) | KR20140117684A (ja) |
| CN (1) | CN103080107A (ja) |
| AU (1) | AU2011268906A1 (ja) |
| BR (1) | BR112012032884A2 (ja) |
| CA (1) | CA2803055A1 (ja) |
| EA (1) | EA201201676A1 (ja) |
| MX (1) | MX2012015100A (ja) |
| WO (1) | WO2011161216A1 (ja) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9199979B2 (en) * | 2011-02-24 | 2015-12-01 | Nerviano Medical Sciences S.R.L. | Thiazolylphenyl-benzenesulfonamido derivatives as kinase inhibitors |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| WO2014172639A1 (en) * | 2013-04-19 | 2014-10-23 | Ruga Corporation | Raf kinase inhibitors |
| UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
| CN109715163B (zh) | 2016-09-19 | 2022-11-22 | 诺华股份有限公司 | 包含raf抑制剂和erk抑制剂的治疗组合 |
| US20190263796A1 (en) | 2016-09-23 | 2019-08-29 | Cellipse | Lim kinase inhibitors, pharmaceutical composition and method of use in limk-mediated diseases |
| WO2020124397A1 (en) * | 2018-12-19 | 2020-06-25 | Inventisbio Shanghai Ltd. | C-terminal src kinase inhibitors |
| CN114746419B (zh) * | 2019-12-05 | 2023-10-24 | 国家医疗保健研究所 | N-(3-(5-(嘧啶-4-基)噻唑-4-基)苯基)磺酰胺化合物及其用作braf抑制剂的用途 |
| CN111320548B (zh) * | 2020-04-24 | 2022-10-18 | 浦拉司科技（上海）有限责任公司 | 抗癌药物中间体2-氟-3-氨基苯甲酸甲酯的合成方法 |
| US20240101516A1 (en) * | 2021-01-20 | 2024-03-28 | Basf Se | Synthesis of polyfluorinated aryl and heteroaryl carboxamides |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6391636B1 (en) | 1994-05-31 | 2002-05-21 | Isis Pharmaceuticals, Inc. | Antisense oligonucleotide modulation of raf gene expression |
| US6358932B1 (en) | 1994-05-31 | 2002-03-19 | Isis Pharmaceticals, Inc. | Antisense oligonucleotide inhibition of raf gene expression |
| US6037136A (en) | 1994-10-24 | 2000-03-14 | Cold Spring Harbor Laboratory | Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto |
| US5717100A (en) | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
| EP0910401A1 (en) | 1996-05-23 | 1999-04-28 | Applied Research Systems ARS Holdings N.V. | Compounds that inhibit the binding of raf-1 or 14-3-3 proteins to the beta chain of il-2 receptor, and pharmaceutical compositions containing same |
| 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 |
| US6187799B1 (en) | 1997-05-23 | 2001-02-13 | Onyx Pharmaceuticals | Inhibition of raf kinase activity using aryl ureas |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| US6022884A (en) | 1997-11-07 | 2000-02-08 | Amgen Inc. | Substituted pyridine compounds and methods of use |
| US6204467B1 (en) | 1998-03-24 | 2001-03-20 | Ford Global Technologies, Inc. | Method and apparatus for resistive welding |
| ME00275B (me) | 1999-01-13 | 2011-02-10 | Bayer Corp | ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE |
| WO2002018654A1 (en) | 2000-08-30 | 2002-03-07 | The Board Of Trustees Of The University Of Arkansas | Induction of ldl receptor expression by extracellular-signal regulated kinase, erk-1/2 |
| JP2003063993A (ja) * | 2001-06-11 | 2003-03-05 | Takeda Chem Ind Ltd | 医薬組成物 |
| ES2549159T3 (es) | 2002-03-13 | 2015-10-23 | Array Biopharma, Inc. | Derivados de bencimidazol N3-alquilados como inhibidores de MEK |
| US7666901B2 (en) | 2004-10-13 | 2010-02-23 | Wyeth | Analogs of 17-hydroxywortmannin as PI3K inhibitors |
| CA2599320A1 (en) | 2005-02-25 | 2006-08-31 | Kudos Pharmaceuticals Limited | Hydrazinomethyl, hydr zonomethyl and 5-membered heterocylic compounds which act as mtor inhibitors and their use as anti cancer agents |
| CA2599212A1 (en) | 2005-02-25 | 2006-08-31 | Kudos Pharmaceuticals Limited | 2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors |
| JP5161102B2 (ja) | 2005-11-22 | 2013-03-13 | クドス ファーマシューティカルズ リミテッド | ｍＴＯＲ阻害剤としてのピリドピリミジン、ピラゾピリミジンおよびピリミドピリミジン誘導体 |
| WO2007080382A1 (en) | 2006-01-11 | 2007-07-19 | Astrazeneca Ab | Morpholino pyrimidine derivatives and their use in therapy |
| SI2057156T1 (sl) | 2006-08-23 | 2017-06-30 | Kudos Pharmaceuticals Limited | Derivati 2-metilmorfolin pirido-, pirazo- in pirimido-pirimidina kot inhibitorji mTOR |
| BRPI0814423B1 (pt) * | 2007-07-17 | 2022-04-19 | Plexxikon, Inc | Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos |
| WO2009076140A1 (en) * | 2007-12-13 | 2009-06-18 | Smithkline Beecham Corporation | Thiazole and oxazole kinase inhibitors |
| UA103319C2 (en) * | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| CN102105459B (zh) * | 2008-07-24 | 2014-09-10 | 内尔维阿诺医学科学有限公司 | 作为蛋白激酶抑制剂的3,4-二芳基吡唑类 |
| EP2498608A4 (en) * | 2009-11-10 | 2013-04-24 | Glaxosmithkline Llc | BENZOLSULFONAMIDE THIAZOL AND OXAZOLE COMPOUNDS |
-
2011
- 2011-06-23 EA EA201201676A patent/EA201201676A1/ru unknown
- 2011-06-23 BR BR112012032884A patent/BR112012032884A2/pt not_active IP Right Cessation
- 2011-06-23 CA CA2803055A patent/CA2803055A1/en not_active Abandoned
- 2011-06-23 KR KR1020147024689A patent/KR20140117684A/ko not_active Application Discontinuation
- 2011-06-23 AU AU2011268906A patent/AU2011268906A1/en not_active Abandoned
- 2011-06-23 EP EP11728247.5A patent/EP2585454A1/en not_active Withdrawn
- 2011-06-23 US US13/805,793 patent/US20130096149A1/en not_active Abandoned
- 2011-06-23 MX MX2012015100A patent/MX2012015100A/es not_active Application Discontinuation
- 2011-06-23 KR KR1020137001935A patent/KR20130048293A/ko active IP Right Grant
- 2011-06-23 WO PCT/EP2011/060561 patent/WO2011161216A1/en active Application Filing
- 2011-06-23 CN CN201180040746XA patent/CN103080107A/zh active Pending
- 2011-06-23 JP JP2013515902A patent/JP2013529619A/ja active Pending
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