TN2011000615A1 - Improved method for synthesizing pirfenidone - Google Patents

Improved method for synthesizing pirfenidone

Info

Publication number
TN2011000615A1
TN2011000615A1 TNP2011000615A TN2011000615A TN2011000615A1 TN 2011000615 A1 TN2011000615 A1 TN 2011000615A1 TN P2011000615 A TNP2011000615 A TN P2011000615A TN 2011000615 A TN2011000615 A TN 2011000615A TN 2011000615 A1 TN2011000615 A1 TN 2011000615A1
Authority
TN
Tunisia
Prior art keywords
pirfenidone
disclosed
synthesizing
improved method
butanol
Prior art date
Application number
TNP2011000615A
Other languages
English (en)
Inventor
Ramachadran Radhakrishnan
Mike Cyr
Sabine Marie Francoise Boutet
Original Assignee
Intermune Inc
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=43298478&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TN2011000615(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Intermune Inc filed Critical Intermune Inc
Publication of TN2011000615A1 publication Critical patent/TN2011000615A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • C07D213/6432-Phenoxypyridines; Derivatives thereof
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/40Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Agronomy & Crop Science (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Cardiology (AREA)
  • Pyridine Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
TNP2011000615A 2009-06-03 2011-12-01 Improved method for synthesizing pirfenidone TN2011000615A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18358809P 2009-06-03 2009-06-03
PCT/US2010/037090 WO2010141600A2 (en) 2009-06-03 2010-06-02 Improved method for synthesizing pirfenidone

Publications (1)

Publication Number Publication Date
TN2011000615A1 true TN2011000615A1 (en) 2013-05-24

Family

ID=43298478

Family Applications (1)

Application Number Title Priority Date Filing Date
TNP2011000615A TN2011000615A1 (en) 2009-06-03 2011-12-01 Improved method for synthesizing pirfenidone

Country Status (35)

Country Link
US (6) US20110003863A1 (https=)
EP (1) EP2440543B1 (https=)
JP (2) JP5848244B2 (https=)
KR (1) KR101734858B1 (https=)
CN (1) CN102482255A (https=)
AP (1) AP3630A (https=)
AR (1) AR076974A1 (https=)
AU (1) AU2010256693B2 (https=)
BR (1) BRPI1011015B8 (https=)
CA (1) CA2764043C (https=)
CL (1) CL2011003069A1 (https=)
DK (1) DK2440543T3 (https=)
EA (1) EA021826B1 (https=)
ES (1) ES2538103T3 (https=)
GE (1) GEP20156223B (https=)
HN (1) HN2011003187A (https=)
HR (1) HRP20150696T1 (https=)
HU (1) HUE026014T2 (https=)
IL (1) IL216565A (https=)
MA (1) MA33489B1 (https=)
MX (1) MX2011012654A (https=)
MY (1) MY162443A (https=)
NI (1) NI201100211A (https=)
NZ (1) NZ596872A (https=)
PE (1) PE20120398A1 (https=)
PL (1) PL2440543T3 (https=)
PT (1) PT2440543E (https=)
RS (1) RS54031B1 (https=)
SG (1) SG176648A1 (https=)
SI (1) SI2440543T1 (https=)
TN (1) TN2011000615A1 (https=)
TW (1) TWI434833B (https=)
UA (1) UA106759C2 (https=)
WO (1) WO2010141600A2 (https=)
ZA (1) ZA201108794B (https=)

Families Citing this family (26)

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Publication number Priority date Publication date Assignee Title
CA2726588C (en) 2008-06-03 2019-04-16 Karl Kossen Compounds and methods for treating inflammatory and fibrotic disorders
US10105356B2 (en) 2011-01-31 2018-10-23 Avalyn Pharma Inc. Aerosol pirfenidone and pyridone analog compounds and uses thereof
JP6021117B2 (ja) 2011-01-31 2016-11-02 ジェノア ファーマシューティカルズ,インク. エアロゾルのピルフェニドンおよびピリドンアナログの化合物、および、その使用
MX2011007675A (es) 2011-07-19 2012-07-11 Cell Therapy And Technology S A De C V Procedimiento para la fabricacion de una composicion farmaceutica en forma de tabletas de liberacion prolongada conteniendo pirfenidona y su aplicacion en la regresion de la insuficiencia renal cronica, contractura capsular mamaria y fibrosis hepatica humanas.
MX356551B (es) 2012-08-23 2018-06-04 Grupo Medifarma S A De C V Star Composición antiséptica, antiseborreica y exfoliante para eliminar o prevenir el acné.
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
NZ760541A (en) 2014-01-10 2022-08-26 Avalyn Pharma Inc Aerosol pirfenidone and pyridone analog compounds and uses thereof
MX382781B (es) 2014-04-02 2025-03-13 Intermune Inc Piridinonas anti-fibroticas.
CN107073112A (zh) * 2014-08-15 2017-08-18 皮克萨尔比奥公司 用于在患有脊髓损伤的对象中抑制炎症的组合物及其使用方法
EP3307714A1 (en) 2015-01-26 2018-04-18 Ulkar Kimya Sanayii Ve Ticaret A. S. An improved method for the synthesis and purification of pirfenidone
ITUB20154832A1 (it) 2015-10-29 2017-04-29 Procos Spa Processo per la sintesi di pirfenidone
CN105315198A (zh) * 2015-11-02 2016-02-10 重庆康乐制药有限公司 一种吡非尼酮的晶型及其制备方法
CN105330598B (zh) * 2015-12-02 2017-11-14 新发药业有限公司 一种吡非尼酮的制备方法
WO2017122139A1 (en) * 2016-01-14 2017-07-20 Laurus Labs Limited An improved process for the preparation of pirfenidone
US11066368B2 (en) 2016-01-14 2021-07-20 Laurus Labs Limited Process for the preparation and particle size reduction of pirfenidone
WO2017130166A1 (en) * 2016-01-31 2017-08-03 Granules India Limited An improved process for the preparation of highly pure anti-fibrotic drug
CA2937365C (en) 2016-03-29 2018-09-18 F. Hoffmann-La Roche Ag Granulate formulation of 5-methyl-1-phenyl-2-(1h)-pyridone and method of making the same
IT201600071672A1 (it) * 2016-07-08 2018-01-08 Dipharma Francis Srl Metodo per sintetizzare un farmaco immunosoppressore
IT201600108927A1 (it) * 2016-10-27 2018-04-27 Dipharma Francis Srl Metodo per sintetizzare un farmaco antifibrotico
US20180009753A1 (en) * 2016-07-08 2018-01-11 Dipharma Francis S.R.L. Method for preparing an antifibrotic agent
WO2018083709A1 (en) * 2016-11-07 2018-05-11 Msn Laboratories Private Limited, R&D Center Improved process for the preparation of pure 5-methyl-1-phenyl-2-1 (h)-pyridone
WO2018178996A1 (en) * 2017-03-28 2018-10-04 Natco Pharma Limited Improved process for the preparation of pirfenidone
WO2019028062A1 (en) 2017-07-31 2019-02-07 Washington University PIRFENIDONE DERIVATIVES FOR MODULATION OF B-LYMPHOCYTE ACTIVITY AND PROTECTION OF ORGANS
ES2886152T3 (es) 2017-12-11 2021-12-16 Laurus Labs Ltd Un procedimiento mejorado para la preparación de pirfenidona
CN112409246B (zh) * 2019-08-21 2023-04-07 北京凯因科技股份有限公司 一种吡非尼酮的晶型及其制备方法
JP7490813B2 (ja) * 2020-04-22 2024-05-27 ユンジン ファーム.カンパニー、リミテッド 安全性と安定性が改善されたピルフェニドンを含む腸溶性製剤およびその製造方法

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US3839346A (en) * 1972-12-18 1974-10-01 Affiliated Med Res N-substituted pyridone and general method for preparing pyridones
CA2099868C (en) * 1991-01-31 2002-04-02 Thomas Richard Belliotti Substituted 4,6-di-tertiary-butyl-5-hydroxy-pyrimidines
WO2002085858A1 (en) * 2001-04-20 2002-10-31 Asahi Glass Company, Limited Process for producing purified piperidine derivative
WO2003014087A1 (fr) * 2001-08-06 2003-02-20 Asahi Glass Company, Limited Procede de preparation de 5-methyl-1-phenyl-2(1h)-pyridinone
CN1218942C (zh) 2002-06-11 2005-09-14 中南大学湘雅医学院 抗纤维化吡啶酮化合物及其生产工艺方法
CN100396669C (zh) * 2006-03-15 2008-06-25 浙江省医学科学院 一种抗纤维化药物吡非尼酮的制备方法
MX2007006349A (es) 2007-05-29 2009-02-18 Cell Therapy And Technology S Nuevo proceso de sintesis para la obtencion de 5-metil-1-fenil-2-(ih)-piridona, composicion y uso de la misma.
JP5587184B2 (ja) * 2007-06-20 2014-09-10 オースペックス・ファーマシューティカルズ・インコーポレイテッド 繊維症阻害剤としての置換n−アリールピリジノン
US20090131485A1 (en) * 2007-09-10 2009-05-21 Concert Pharmaceuticals, Inc. Deuterated pirfenidone

Also Published As

Publication number Publication date
PT2440543E (pt) 2015-07-03
AU2010256693B2 (en) 2015-09-17
US8519140B2 (en) 2013-08-27
CN102482255A (zh) 2012-05-30
AP3630A (en) 2016-03-08
US20120016133A1 (en) 2012-01-19
EP2440543A4 (en) 2012-11-21
EA201101695A1 (ru) 2012-05-30
BRPI1011015A2 (pt) 2018-02-14
CA2764043A1 (en) 2010-12-09
BRPI1011015B1 (pt) 2020-11-10
AU2010256693A1 (en) 2012-01-12
HRP20150696T1 (hr) 2015-08-28
MA33489B1 (fr) 2012-08-01
HUE026014T2 (en) 2016-05-30
WO2010141600A2 (en) 2010-12-09
SI2440543T1 (sl) 2015-06-30
BRPI1011015B8 (pt) 2021-05-25
MY162443A (en) 2017-06-15
KR101734858B1 (ko) 2017-05-12
EP2440543A2 (en) 2012-04-18
EP2440543B1 (en) 2015-04-15
US20150368200A1 (en) 2015-12-24
NZ596872A (en) 2013-12-20
US20140221660A1 (en) 2014-08-07
GEP20156223B (en) 2015-01-26
ZA201108794B (en) 2013-03-27
EA021826B1 (ru) 2015-09-30
HN2011003187A (es) 2015-02-02
PL2440543T3 (pl) 2015-09-30
AP2012006052A0 (en) 2012-02-29
NI201100211A (es) 2012-08-01
TW201043602A (en) 2010-12-16
JP5848244B2 (ja) 2016-01-27
RS54031B1 (sr) 2015-10-30
TWI434833B (zh) 2014-04-21
CA2764043C (en) 2018-01-16
MX2011012654A (es) 2012-01-12
ES2538103T3 (es) 2015-06-17
KR20120016277A (ko) 2012-02-23
CL2011003069A1 (es) 2012-05-25
JP2016026196A (ja) 2016-02-12
PE20120398A1 (es) 2012-05-13
IL216565A0 (en) 2012-03-01
US20150065720A1 (en) 2015-03-05
DK2440543T3 (en) 2015-05-18
WO2010141600A3 (en) 2011-04-21
SG176648A1 (en) 2012-01-30
AR076974A1 (es) 2011-07-20
UA106759C2 (uk) 2014-10-10
US20110003863A1 (en) 2011-01-06
IL216565A (en) 2015-06-30
US20130345430A1 (en) 2013-12-26
JP2012528877A (ja) 2012-11-15

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