BR112012002971A2 - preparação regioseletiva de derivados 2-amino-5-trifluorometil-pirmidinas - Google Patents

preparação regioseletiva de derivados 2-amino-5-trifluorometil-pirmidinas

Info

Publication number
BR112012002971A2
BR112012002971A2 BR112012002971A BR112012002971A BR112012002971A2 BR 112012002971 A2 BR112012002971 A2 BR 112012002971A2 BR 112012002971 A BR112012002971 A BR 112012002971A BR 112012002971 A BR112012002971 A BR 112012002971A BR 112012002971 A2 BR112012002971 A2 BR 112012002971A2
Authority
BR
Brazil
Prior art keywords
pyrmidines
trifluoromethyl
derivatives
amino
regioselective preparation
Prior art date
Application number
BR112012002971A
Other languages
English (en)
Portuguese (pt)
Inventor
Gerd Kraemer
Guenter Linz
Juergen Schnaubelt
Sabrina Kusserow
Original Assignee
Boehringer Ingelheim Int
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42712695&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112012002971(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of BR112012002971A2 publication Critical patent/BR112012002971A2/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
BR112012002971A 2009-08-14 2010-08-13 preparação regioseletiva de derivados 2-amino-5-trifluorometil-pirmidinas BR112012002971A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09167934 2009-08-14
PCT/EP2010/061840 WO2011018518A1 (en) 2009-08-14 2010-08-13 Regioselective preparation of 2 -amino-5-trifluoromethylpyrimidine derivatives

Publications (1)

Publication Number Publication Date
BR112012002971A2 true BR112012002971A2 (pt) 2015-10-13

Family

ID=42712695

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012002971A BR112012002971A2 (pt) 2009-08-14 2010-08-13 preparação regioseletiva de derivados 2-amino-5-trifluorometil-pirmidinas

Country Status (17)

Country Link
US (1) US8933227B2 (https=)
EP (1) EP2464634B1 (https=)
JP (1) JP5539519B2 (https=)
KR (1) KR20120046248A (https=)
CN (1) CN102471287A (https=)
AR (1) AR077925A1 (https=)
AU (1) AU2010283713A1 (https=)
BR (1) BR112012002971A2 (https=)
CA (1) CA2767965A1 (https=)
CL (1) CL2012000278A1 (https=)
EA (1) EA201200282A1 (https=)
IL (1) IL217112A0 (https=)
IN (1) IN2012DN01342A (https=)
MX (1) MX2012001469A (https=)
NZ (1) NZ597538A (https=)
TW (1) TW201124385A (https=)
WO (1) WO2011018518A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8372974B2 (en) * 2008-03-20 2013-02-12 Boehringer Ingelheim International Gmbh Regioselective preparation of substituted pyrimidines
UY31714A (es) * 2008-03-20 2009-11-10 Boehringer Ingelheim Int Preparación selectiva de pirimidinas sustituidas
WO2011018517A1 (en) 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
CN102887860B (zh) * 2012-09-29 2015-07-01 上海泰坦科技有限公司 4-氯-6-三氟甲基嘧啶类化合物的制备方法
JP6391985B2 (ja) * 2014-05-16 2018-09-19 東ソー・ファインケム株式会社 2−置換−4−(2,2,2−トリフルオロエトキシ)−5−(トリフルオロメチル)ピリミジン誘導体及びその製造方法
JP6391988B2 (ja) * 2014-05-21 2018-09-19 東ソー・ファインケム株式会社 5−(トリフルオロメチル)ピリミジン誘導体の製造方法及び新規5−(トリフルオロメチル)ピリミジン誘導体
JP6262079B2 (ja) * 2014-06-02 2018-01-17 東ソー・ファインケム株式会社 4−(2,2,2−トリフルオロエトキシ)−5−(トリフルオロメチル)ピリミジン誘導体及びその製造方法
JP6431294B2 (ja) * 2014-06-16 2018-11-28 東ソー・ファインケム株式会社 5−(トリフルオロメチル)ピリミジン誘導体及びその製造法
JP6479486B2 (ja) * 2015-01-16 2019-03-06 東ソー・ファインケム株式会社 4−アルコキシ−5−(トリフルオロメチル)ピリミジン誘導体及びその製造方法

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6262A (ja) 1986-03-05 1987-01-06 Ishihara Sangyo Kaisha Ltd ベンゾイルウレア系化合物の製造方法
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
ATE407678T1 (de) 2001-10-17 2008-09-15 Boehringer Ingelheim Pharma Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
DE10161763A1 (de) 2001-12-15 2003-07-17 Bayer Cropsience Ltd Neues herbizides Verfahren
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
WO2003095448A1 (en) 2002-05-06 2003-11-20 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
JP2006508997A (ja) 2002-11-28 2006-03-16 シエーリング アクチエンゲゼルシャフト Chk−、Pdk−およびAkt−阻害性ピリミジン、それらの製造および薬剤としての使用
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
CA2529611C (en) 2002-12-20 2009-12-15 Pfizer Products Inc. Pyrimidine derivatives for the treatment of abnormal cell growth
WO2005023780A1 (en) * 2003-09-05 2005-03-17 Pfizer Products Inc. Selective synthesis of cf3-substituted pyrimidines
US20070105839A1 (en) 2003-09-18 2007-05-10 Patricia Imbach 2, 4-Di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
BRPI0511138A (pt) 2004-05-14 2007-11-27 Pfizer Prod Inc derivados de pirimidina para o tratamento de desenvolvimento celular anormal
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
JP2008505910A (ja) 2004-07-08 2008-02-28 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド Pkc−シータのインヒビターとして有用なピリミジン誘導体
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
US7776869B2 (en) 2004-10-18 2010-08-17 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
ATE519759T1 (de) 2004-12-30 2011-08-15 Exelixis Inc Pyrimidinderivate als kinasemodulatoren und anwendungsverfahren
US7323447B2 (en) 2005-02-08 2008-01-29 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
EP1705177A1 (en) 2005-03-23 2006-09-27 Schering Aktiengesellschaft N-aryl-sulfoximine-substituted pyrimidines as CDK- and/or VEGF inhibitors, their production and use as pharmaceutical agents
CN101218229A (zh) 2005-05-05 2008-07-09 阿斯利康(瑞典)有限公司 吡唑基-氨基取代的嘧啶及其在癌症治疗中的应用
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20070032514A1 (en) 2005-07-01 2007-02-08 Zahn Stephan K 2,4-diamino-pyrimidines as aurora inhibitors
JP2009513615A (ja) 2005-10-28 2009-04-02 アストラゼネカ アクチボラグ 癌の治療においてチロシンキナーゼ阻害剤として使用するための4−(3−アミノピラゾール)ピリミジン誘導体
WO2007063384A2 (en) 2005-12-01 2007-06-07 Pfizer Products Inc. Pyrimidine derivatives for the treatment of abnormal cell growth
CA2634646C (en) 2005-12-21 2012-04-10 Pfizer Products Inc. Pyrimidine derivatives for the treatment of abnormal cell growth
TW200804364A (en) 2006-02-22 2008-01-16 Boehringer Ingelheim Int New compounds
CA2648170A1 (en) 2006-04-10 2007-10-18 Boehringer Ingelheim International Gmbh 2, 4-diaminopyrimidine derivatives and their use for the treatment of cancer
PE20120006A1 (es) 2006-05-15 2012-02-02 Boehringer Ingelheim Int Compuestos derivados de pirimidina como inhibidores de la quinasa aurora
JP5301431B2 (ja) 2006-05-18 2013-09-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング キラルな環状β−アミノカルボキサミドの製造方法
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
CA2654670A1 (en) 2006-07-06 2008-01-10 Boehringer Ingelheim International Gmbh New compounds
DE102006041382A1 (de) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren
WO2008040951A1 (en) 2006-10-03 2008-04-10 Astrazeneca Ab Compounds
WO2008045978A1 (en) 2006-10-10 2008-04-17 Rigel Pharmaceuticals, Inc. Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors
WO2008046216A1 (en) 2006-10-18 2008-04-24 Methylgene, Inc. Kinase inhibitors and uses thereof
RU2009112496A (ru) 2006-10-19 2010-11-27 Ф. Хоффманн-Ля Рош Аг (Ch) Аминометил-4-имидазолы
ES2555803T3 (es) 2006-10-23 2016-01-08 Cephalon, Inc. Fusión de derivados bicíclicos 2,4-diaminopirimidina como utilizar inhibidores ALK y c-Met
MX2009005881A (es) 2006-12-13 2009-06-12 Hoffmann La Roche Derivados de 2-(piperidin-4-il)-4-fenoxi o fenilamino-pirimidina como inhibidores de la transcriptasa inversa no nucleosida.
CN101563327A (zh) 2006-12-19 2009-10-21 健泰科生物技术公司 嘧啶类激酶抑制剂
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
CN101678022A (zh) 2006-12-21 2010-03-24 弗特克斯药品有限公司 可用作蛋白激酶抑制剂的5-氰基-4-(吡咯并[2,3b]吡啶-3-基)嘧啶衍生物
WO2008077885A2 (en) 2006-12-22 2008-07-03 Boehringer Ingelheim International Gmbh 2- [(phenylamino) -pyrimidin-4ylamin0] -cyclopentane carboxamide derivatives and related compounds as inhibitors of kinases of the cell cycle for the treatment of cancer
PE20081636A1 (es) 2007-01-26 2009-01-10 Smithkline Beecham Corp Inhibidores de antranilamida para aurora quinasa
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CN101678215B (zh) 2007-04-18 2014-10-01 辉瑞产品公司 用于治疗异常细胞生长的磺酰胺衍生物
CN101903357A (zh) 2007-07-17 2010-12-01 里格尔药品股份有限公司 作为pkc抑制剂的环状胺取代的嘧啶二胺
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
EA017252B1 (ru) 2007-08-28 2012-11-30 Айрм Ллк Производные 2-бифениламино-4-аминопиримидина в качестве ингибиторов киназ
WO2009063240A1 (en) 2007-11-16 2009-05-22 Arrow Therapeutics Limited 2,4-diaminopyrimidine derivatives useful as inhibitors of aurora kinase
US8461147B2 (en) 2007-12-03 2013-06-11 Boehringer Ingelheim International Gmbh Diaminopyridines for the treatment of diseases which are characterised by excessive or anomal cell proliferation
ES2389752T3 (es) 2007-12-14 2012-10-31 Ardea Biosciences, Inc. Inhibidores de la transcriptasa inversa
UY31714A (es) 2008-03-20 2009-11-10 Boehringer Ingelheim Int Preparación selectiva de pirimidinas sustituidas
US8372974B2 (en) 2008-03-20 2013-02-12 Boehringer Ingelheim International Gmbh Regioselective preparation of substituted pyrimidines
AU2009262198B2 (en) 2008-06-25 2012-09-27 Irm Llc Pyrimidine derivatives as kinase inhibitors
PE20100087A1 (es) 2008-06-25 2010-02-08 Irm Llc Compuestos y composiciones como inhibidores de cinasa
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
EP2179991A1 (de) 2008-10-21 2010-04-28 Bayer Schering Pharma Aktiengesellschaft Sulfoximinsubstituierte Anilino-Pyrimidinderivate als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
EP2179992A1 (de) 2008-10-21 2010-04-28 Bayer Schering Pharma Aktiengesellschaft Sulfonsubstituierte Anlinopyrimidinderivative als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
UY32240A (es) 2008-11-14 2010-06-30 Boeringer Ingelheim Kg Nuevas 2,4-diaminopirimidinas, sus sales farmacéuticamente aceptables, composiciones conteniéndolas y aplicaciones.
TW201024281A (en) 2008-11-24 2010-07-01 Boehringer Ingelheim Int New compounds
AR074210A1 (es) 2008-11-24 2010-12-29 Boehringer Ingelheim Int Derivados de pirimidina como inhibidores de ptk2-quinasa
WO2011018517A1 (en) 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines

Also Published As

Publication number Publication date
CL2012000278A1 (es) 2012-10-12
AU2010283713A1 (en) 2012-02-02
US8933227B2 (en) 2015-01-13
KR20120046248A (ko) 2012-05-09
TW201124385A (en) 2011-07-16
CN102471287A (zh) 2012-05-23
IL217112A0 (en) 2012-02-29
MX2012001469A (es) 2012-02-22
CA2767965A1 (en) 2011-02-17
NZ597538A (en) 2014-05-30
EP2464634A1 (en) 2012-06-20
JP5539519B2 (ja) 2014-07-02
EA201200282A1 (ru) 2012-09-28
IN2012DN01342A (https=) 2015-06-05
US20110190499A1 (en) 2011-08-04
AR077925A1 (es) 2011-10-05
WO2011018518A1 (en) 2011-02-17
JP2013501759A (ja) 2013-01-17
EP2464634B1 (en) 2016-11-30

Similar Documents

Publication Publication Date Title
EP2418213A4 (en) NEURO MEDIN-U DERIVATIVE
BRPI1013246A2 (pt) derivados de benzofuralina
BR112012002828A2 (pt) derivados de 5-fluorpirimidinona
EP2350110A4 (en) NEW STEVIOLGLYKOSIDE
BR112012000769A2 (pt) lupeol -tipo de derivados triterpenos como antivirais
BR112012002971A2 (pt) preparação regioseletiva de derivados 2-amino-5-trifluorometil-pirmidinas
EP2433940A4 (en) SPIROIMIDAZOLONDERIVAT
BRPI1013844A2 (pt) derivados de piridina-isoxazol
DK2397480T3 (da) Diazepindionderivat
EP2442821A4 (en) SAFE ADMINISTRATION OF DESMOPRESSIN
PL2493466T3 (pl) Nowe przeciwguzowe zastosowanie kabazytakselu
BRPI1014454A2 (pt) derivados de isoxazol-pirazol
SMT201600076B (it) Derivati di 2-osso-1-pirrolidinil imidazotiadiazolo
PT2492266E (pt) Derivado de 5-hidroxipirimidino-4-carboxamida
BR112012002810A2 (pt) derivados de n1-acil-5-fluoropirimidinona
BRPI1014688A2 (pt) aplicações terapêuticas de derivados de quinazolinadiona
DK2387580T3 (da) Deoxyactagardinderivater
IT1398296B1 (it) Disposizione di sensori
EP2401281A4 (en) PYRIMIDINPYRIMIDOINDAZOLDERIVAT
DK2453858T3 (da) Fremgangsmåde
BRPI1011416A2 (pt) derivados de antraquinova novos
DK2571843T3 (da) Forbedret fremstilling af chalcon-derivater
CU23884B1 (es) Derivados de dibenzotiazepina
EP2623503A4 (en) CHROME DERIVATIVES
PT2467136E (pt) Formulações de 4-metilpirazol

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2344 DE 08-12-2015 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.