DK3141548T3 - Fremgangsmåder og mellemprodukter til fremstilling af azaindoler - Google Patents

Fremgangsmåder og mellemprodukter til fremstilling af azaindoler Download PDF

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Publication number
DK3141548T3
DK3141548T3 DK16190960.1T DK16190960T DK3141548T3 DK 3141548 T3 DK3141548 T3 DK 3141548T3 DK 16190960 T DK16190960 T DK 16190960T DK 3141548 T3 DK3141548 T3 DK 3141548T3
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DK
Denmark
Prior art keywords
azaindoles
intermediates
preparation
methods
Prior art date
Application number
DK16190960.1T
Other languages
English (en)
Inventor
Gerald J Tanoury
Young Chun Jung
Derek Magdziak
Adam Looker
Billie J Kline
Olmo Beatriz Dominguez
Václav Jurcík
Original Assignee
Vertex Pharma
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Publication of DK3141548T3 publication Critical patent/DK3141548T3/da

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/04Esters of boric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Steroid Compounds (AREA)
DK16190960.1T 2011-07-05 2012-07-03 Fremgangsmåder og mellemprodukter til fremstilling af azaindoler DK3141548T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161504351P 2011-07-05 2011-07-05
US201261636296P 2012-04-20 2012-04-20
EP12735411.6A EP2729465A2 (en) 2011-07-05 2012-07-03 Processes and intermediates for producing azaindoles

Publications (1)

Publication Number Publication Date
DK3141548T3 true DK3141548T3 (da) 2020-07-06

Family

ID=46513874

Family Applications (1)

Application Number Title Priority Date Filing Date
DK16190960.1T DK3141548T3 (da) 2011-07-05 2012-07-03 Fremgangsmåder og mellemprodukter til fremstilling af azaindoler

Country Status (19)

Country Link
US (5) US8513414B2 (da)
EP (2) EP2729465A2 (da)
JP (3) JP2014520815A (da)
KR (1) KR20140058547A (da)
CN (2) CN106432311A (da)
AR (1) AR087069A1 (da)
AU (1) AU2012279046B2 (da)
BR (1) BR112014000115A2 (da)
CA (1) CA2839937C (da)
DK (1) DK3141548T3 (da)
ES (1) ES2804528T3 (da)
MX (1) MX2013015147A (da)
NZ (2) NZ619699A (da)
PL (1) PL3141548T3 (da)
PT (1) PT3141548T (da)
RU (1) RU2014103806A (da)
TW (1) TW201321378A (da)
WO (1) WO2013006634A2 (da)
ZA (1) ZA201400049B (da)

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EP2311837B1 (en) * 2004-03-30 2014-05-21 Vertex Pharmaceuticals Inc. Azaindoles useful as inhibitors of jak and other protein kinases
NZ597059A (en) 2009-06-17 2014-01-31 Vertex Pharma Inhibitors of influenza viruses replication
CA2839937C (en) 2011-07-05 2020-11-03 Vertex Pharmaceuticals Incorporated Processes and intermediates for producing azaindoles
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
WO2014201332A1 (en) 2013-06-14 2014-12-18 Vertex Pharmaceuticals Incorporated Pharmaceutical combinations useful for treating rheumatoid arthritis
EP3036225A1 (en) 2013-08-22 2016-06-29 Vertex Pharmaceuticals Incorporated Isotopically enriched azaindoles
US9296727B2 (en) 2013-10-07 2016-03-29 Vertex Pharmaceuticals Incorporated Methods of regioselective synthesis of 2,4-disubstituted pyrimidines
HUE052178T2 (hu) * 2013-11-13 2021-04-28 Vertex Pharma Eljárások influenzavírus-replikáció inhibitorainak elõállítására
SG10201804026WA (en) 2013-11-13 2018-06-28 Vertex Pharma Inhibitors of influenza viruses replication
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
MA42422A (fr) 2015-05-13 2018-05-23 Vertex Pharma Inhibiteurs de la réplication des virus de la grippe
RU2737190C2 (ru) * 2015-12-09 2020-11-25 Саншайн Лейк Фарма Ко., Лтд. Ингибиторы репликации вируса гриппа, способы их применения и использование
CN105523986A (zh) * 2015-12-30 2016-04-27 江汉大学 一种外排泵抑制剂n-氢-2-芳基吲哚及其衍生物的合成方法
SI3510031T1 (sl) * 2016-09-09 2021-03-31 F. Hoffmann-La Roche Ag Postopek za pripravo 2-(6-nitropiridin-3-il)-9H-dipirido(2,3-b;3',4'-d)pirola
EP4183786A1 (en) 2016-12-23 2023-05-24 Felicitex Therapeutics, Inc. Derivatives of quinolines as inhibitors of dyrk1a and/or dyrk1b kinases
JP2022515272A (ja) * 2018-12-24 2022-02-17 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド ピロロピリミジン化合物の治療的使用およびその固形医薬組成物
CN113121452A (zh) * 2021-05-10 2021-07-16 甘肃堡昌化工有限公司 一种硫酸法尿嘧啶的精制工艺
CN113851244A (zh) * 2021-09-18 2021-12-28 浙江爱索拓科技有限公司 一种含放射性同位素碳-14废水的处理方法
CN113896716A (zh) * 2021-10-27 2022-01-07 浙江爱索拓科技有限公司 一种放射性同位素碳-14双标记甲磺酸伏美替尼合成方法

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GB9721437D0 (en) 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
AU3704101A (en) 2000-02-17 2001-08-27 Amgen Inc Kinase inhibitors
UY26942A1 (es) * 2000-09-20 2002-04-26 Abbott Lab N-acilsulfonamidas promotoras de la apoptosis
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
EP1506189A1 (en) 2002-04-26 2005-02-16 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
CN1656079A (zh) 2002-05-31 2005-08-17 卫材株式会社 吡唑化合物和含有该化合物的药物组合物
EP1675830A4 (en) * 2003-09-30 2008-08-20 Scios Inc HETEROCYCLIC AMIDES AND SULFONAMIDES
JP4605606B2 (ja) 2004-01-30 2011-01-05 長瀬産業株式会社 軸不斉を有する光学活性な4級アンモニウム塩およびそれを用いたα−アミノ酸およびその誘導体の製造方法
EP2311837B1 (en) 2004-03-30 2014-05-21 Vertex Pharmaceuticals Inc. Azaindoles useful as inhibitors of jak and other protein kinases
UA87494C2 (en) * 2004-03-30 2009-07-27 Вертекс Фармасьютикалс Инкорпорейтед Azaindoles useful as inhibitors of jak and other protein kinases
WO2006038001A1 (en) * 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
RU2435769C2 (ru) 2005-05-20 2011-12-10 Вертекс Фармасьютикалз Инкорпорейтед Пирролопиридины, полезные в качестве ингибиторов протеинкиназы
JP5591471B2 (ja) 2006-01-17 2014-09-17 バーテックス ファーマシューティカルズ インコーポレイテッド ヤヌスキナーゼ阻害剤として有用なアザインドール
CN101374839A (zh) * 2006-01-17 2009-02-25 沃泰克斯药物股份有限公司 适用作詹纳斯激酶抑制剂的吖吲哚类
ES2431466T3 (es) * 2006-06-30 2013-11-26 Sunesis Pharmaceuticals, Inc. Inhibidores de piridinonil pdk1
JP4450857B2 (ja) * 2006-08-08 2010-04-14 中外製薬株式会社 Pi3k阻害剤としてのピリミジン誘導体およびその用途
MX2009006345A (es) 2006-12-14 2009-06-23 Vertex Pharma Compuestos utiles como inhibidores de proteina cinasa.
CA2704633C (en) * 2007-11-05 2015-10-20 Novartis Ag 4-benzylamino-1-carboxyacyl-piperidine derivatives as cetp inhibitors useful for the treatment of diseases such as hyperlipidemia or arteriosclerosis
ATE522535T1 (de) * 2008-02-25 2011-09-15 Hoffmann La Roche Pyrrolotriazin-kinasehemmer
NZ597059A (en) 2009-06-17 2014-01-31 Vertex Pharma Inhibitors of influenza viruses replication
CA2839937C (en) 2011-07-05 2020-11-03 Vertex Pharmaceuticals Incorporated Processes and intermediates for producing azaindoles
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
EP2776036A1 (en) 2011-11-07 2014-09-17 Vertex Pharmaceuticals Incorporated Methods for treating inflammatory diseases and pharmaceutical combinations useful therefor
EP3036225A1 (en) 2013-08-22 2016-06-29 Vertex Pharmaceuticals Incorporated Isotopically enriched azaindoles

Also Published As

Publication number Publication date
US20150099884A1 (en) 2015-04-09
ES2804528T3 (es) 2021-02-08
RU2014103806A (ru) 2015-08-10
NZ714502A (en) 2017-04-28
US9090614B2 (en) 2015-07-28
EP3141548B9 (en) 2020-08-12
AU2012279046A1 (en) 2014-01-23
CN103702998A (zh) 2014-04-02
JP2014520815A (ja) 2014-08-25
US20150284388A1 (en) 2015-10-08
US20140309421A1 (en) 2014-10-16
WO2013006634A2 (en) 2013-01-10
US8796453B2 (en) 2014-08-05
JP2018162314A (ja) 2018-10-18
JP6761448B2 (ja) 2020-09-23
BR112014000115A2 (pt) 2016-10-04
US20130102782A1 (en) 2013-04-25
AU2012279046B2 (en) 2017-08-31
MX2013015147A (es) 2014-03-27
CN106432311A (zh) 2017-02-22
EP2729465A2 (en) 2014-05-14
US20130303764A1 (en) 2013-11-14
CA2839937C (en) 2020-11-03
US8513414B2 (en) 2013-08-20
US8946425B2 (en) 2015-02-03
PT3141548T (pt) 2020-07-10
CA2839937A1 (en) 2013-01-10
ZA201400049B (en) 2015-04-29
EP3141548A1 (en) 2017-03-15
JP2017002067A (ja) 2017-01-05
WO2013006634A3 (en) 2013-05-10
EP3141548B1 (en) 2020-04-08
NZ619699A (en) 2016-03-31
PL3141548T3 (pl) 2020-09-07
WO2013006634A9 (en) 2013-03-21
KR20140058547A (ko) 2014-05-14
TW201321378A (zh) 2013-06-01
AR087069A1 (es) 2014-02-12

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