AR087069A1 - Procesos e intermediarios para producir azaindoles - Google Patents

Procesos e intermediarios para producir azaindoles

Info

Publication number
AR087069A1
AR087069A1 ARP120102438A ARP120102438A AR087069A1 AR 087069 A1 AR087069 A1 AR 087069A1 AR P120102438 A ARP120102438 A AR P120102438A AR P120102438 A ARP120102438 A AR P120102438A AR 087069 A1 AR087069 A1 AR 087069A1
Authority
AR
Argentina
Prior art keywords
compound
formula
occurrences
optionally substituted
unsubstituted
Prior art date
Application number
ARP120102438A
Other languages
English (en)
Inventor
J Tanoury Gerard
Chun Jung Young
Magdziak Derek
Looker Adam
Original Assignee
Vertex Pharma
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
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR087069A1 publication Critical patent/AR087069A1/es

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    • 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
    • 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
    • C07F5/04Esters 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

Landscapes

  • 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)

Abstract

La presente se refiere a procesos e intermediarios para la preparación de los compuestos útiles como inhibidores de las quinasas Janus (JAK). Estos compuestos son útiles en el tratamiento de dolencias tales como las enfermedades autoinmunes (alergia, asma), rechazo de transplantes, leucemia, linfomas, policitemia, trombocitemia esencial, mielofibrosis. Reivindicación 1: Un proceso para preparar un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, caracterizada porque: R¹ es -H, -Cl o -F; R² es -H o -F; R³ es -alifático C₁₋₄ opcionalmente sustituido con 1 - 5 ocurrencias de R⁵; R⁴ es -alquil C₁₋₂ opcionalmente sustituido con 1 - 3 ocurrencias de R⁵; o R³ y R⁴ se toman juntos para formar un anillo saturado carbocíclico o heterocíclico de 3 - 7 miembros opcionalmente sustituido con 1 - 5 ocurrencias de R⁵; cada R⁵ se selecciona independientemente entre halógeno, -OCH₃, -OH, -NO₂, -NH₂, -SH, -SCH₃, -NHCH₃, -CN, o alifático C₁₋₂ insustituido, o dos grupos R⁵, junto con el carbono al que están ligados, forman un anillo ciclopropilo; R⁶ es -H o alquilo C₁₋₂ insustituido; y R⁷ es un -CH₂CR₃ o -(CH₂)₂CR₃ donde cada R es independientemente -H o -F; que comprende los pasos de: i) hacer reaccionar un compuesto de la fórmula (2) con una sal de clorhidrato de un compuesto de la fórmula (3) en presencia de agua, un solvente orgánico, una base y un catalizador de metal de transición para generar un compuesto de la fórmula (1).
ARP120102438A 2011-07-05 2012-07-05 Procesos e intermediarios para producir azaindoles AR087069A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161504351P 2011-07-05 2011-07-05
US201261636296P 2012-04-20 2012-04-20

Publications (1)

Publication Number Publication Date
AR087069A1 true AR087069A1 (es) 2014-02-12

Family

ID=46513874

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120102438A AR087069A1 (es) 2011-07-05 2012-07-05 Procesos e intermediarios para producir azaindoles

Country Status (19)

Country Link
US (5) US8513414B2 (es)
EP (2) EP3141548B9 (es)
JP (3) JP2014520815A (es)
KR (1) KR20140058547A (es)
CN (2) CN103702998A (es)
AR (1) AR087069A1 (es)
AU (1) AU2012279046B2 (es)
BR (1) BR112014000115A2 (es)
CA (1) CA2839937C (es)
DK (1) DK3141548T3 (es)
ES (1) ES2804528T3 (es)
MX (1) MX2013015147A (es)
NZ (2) NZ714502A (es)
PL (1) PL3141548T3 (es)
PT (1) PT3141548T (es)
RU (1) RU2014103806A (es)
TW (1) TW201321378A (es)
WO (1) WO2013006634A2 (es)
ZA (1) ZA201400049B (es)

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PT1730146E (pt) * 2004-03-30 2011-07-11 Vertex Pharma Azaindoles úteis como inibidores de jak e outras proteínas quinases
WO2010148197A1 (en) 2009-06-17 2010-12-23 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
WO2013006634A2 (en) * 2011-07-05 2013-01-10 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
SG10201804021TA (en) * 2013-11-13 2018-07-30 Vertex Pharma Methods of preparing inhibitors of influenza viruses replication
JP6615755B2 (ja) 2013-11-13 2019-12-04 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 インフルエンザウイルスの複製の阻害剤
MA42422A (fr) 2015-05-13 2018-05-23 Vertex Pharma Inhibiteurs de la réplication des virus de la grippe
WO2016183116A1 (en) * 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
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
WO2018046428A1 (en) * 2016-09-09 2018-03-15 F. Hoffmann-La Roche Ag Process for preparation of 2-(6-nitropyridin-3-yl)-9h-dipyrido[2,3-b;3',4'-d]pyrrole
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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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UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
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EP3036225A1 (en) 2013-08-22 2016-06-29 Vertex Pharmaceuticals Incorporated Isotopically enriched azaindoles

Also Published As

Publication number Publication date
EP3141548B9 (en) 2020-08-12
MX2013015147A (es) 2014-03-27
WO2013006634A3 (en) 2013-05-10
BR112014000115A2 (pt) 2016-10-04
EP3141548B1 (en) 2020-04-08
JP6761448B2 (ja) 2020-09-23
US8796453B2 (en) 2014-08-05
US20150284388A1 (en) 2015-10-08
EP2729465A2 (en) 2014-05-14
CN106432311A (zh) 2017-02-22
AU2012279046A1 (en) 2014-01-23
US20150099884A1 (en) 2015-04-09
PT3141548T (pt) 2020-07-10
PL3141548T3 (pl) 2020-09-07
DK3141548T3 (da) 2020-07-06
US9090614B2 (en) 2015-07-28
JP2014520815A (ja) 2014-08-25
JP2017002067A (ja) 2017-01-05
CN103702998A (zh) 2014-04-02
JP2018162314A (ja) 2018-10-18
CA2839937C (en) 2020-11-03
RU2014103806A (ru) 2015-08-10
ZA201400049B (en) 2015-04-29
WO2013006634A2 (en) 2013-01-10
KR20140058547A (ko) 2014-05-14
NZ714502A (en) 2017-04-28
WO2013006634A9 (en) 2013-03-21
US8513414B2 (en) 2013-08-20
US20130303764A1 (en) 2013-11-14
US20140309421A1 (en) 2014-10-16
CA2839937A1 (en) 2013-01-10
AU2012279046B2 (en) 2017-08-31
EP3141548A1 (en) 2017-03-15
ES2804528T3 (es) 2021-02-08
TW201321378A (zh) 2013-06-01
NZ619699A (en) 2016-03-31
US20130102782A1 (en) 2013-04-25
US8946425B2 (en) 2015-02-03

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