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BRPI1011015B8 - método para sintetizar pirfenidona - Google Patents

método para sintetizar pirfenidona

Info

Publication number
BRPI1011015B8
BRPI1011015B8 BRPI1011015A BRPI1011015A BRPI1011015B8 BR PI1011015 B8 BRPI1011015 B8 BR PI1011015B8 BR PI1011015 A BRPI1011015 A BR PI1011015A BR PI1011015 A BRPI1011015 A BR PI1011015A BR PI1011015 B8 BRPI1011015 B8 BR PI1011015B8
Authority
BR
Brazil
Prior art keywords
pirfenidone
disclosed
synthesizing
butanol
ethyl acetate
Prior art date
Application number
BRPI1011015A
Other languages
English (en)
Inventor
Cyr Mike
Radhakrishnan Ramachandran
Marie-Francoise Brigitte Boutet Sabine
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=BRPI1011015(B8) "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 BRPI1011015A2 publication Critical patent/BRPI1011015A2/pt
Publication of BRPI1011015B1 publication Critical patent/BRPI1011015B1/pt
Publication of BRPI1011015B8 publication Critical patent/BRPI1011015B8/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C07D213/643—2-Phenoxypyridines; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION 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
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/40—Biocides, 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs 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)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Plant Pathology (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (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)

Abstract

método aperfeiçoado para sintetizar pirfenidona. um processo para sintetizar pirfenidona de bromobenzeno tendo menos de cerca de 0,15% em peso de dibromobenzo é divulgado. também são divulgados processo para sintetizar pirfenidona sem usar acetado de etila ou n-butanol e pirfenidona tendo níveis controlados de acetado de etila, n-butanol, di (5-metil-2-piridinona)benzenos e outras impurezas tendo tempos de retenção especificados. também são divulgadas formas de dosagem formuladas incluindo a pirfenidona divulgada.
BRPI1011015A 2009-06-03 2010-06-02 método para sintetizar pirfenidona BRPI1011015B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18358809P 2009-06-03 2009-06-03
US61/183,588 2009-06-03
PCT/US2010/037090 WO2010141600A2 (en) 2009-06-03 2010-06-02 Improved method for synthesizing pirfenidone

Publications (3)

Publication Number Publication Date
BRPI1011015A2 BRPI1011015A2 (pt) 2018-02-14
BRPI1011015B1 BRPI1011015B1 (pt) 2020-11-10
BRPI1011015B8 true BRPI1011015B8 (pt) 2021-05-25

Family

ID=43298478

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI1011015A BRPI1011015B8 (pt) 2009-06-03 2010-06-02 método para sintetizar pirfenidona

Country Status (35)

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

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Publication number Priority date Publication date Assignee Title
CA3034994A1 (en) 2008-06-03 2009-12-10 Intermune, Inc. Substituted aryl-2 pyridone compounds and use thereof 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
EP4491180A1 (en) 2014-01-10 2025-01-15 Avalyn Pharma Inc. Aerosol pirfenidone and pyridone analog compounds and uses thereof
WO2015153683A1 (en) 2014-04-02 2015-10-08 Intermune, Inc. Anti-fibrotic pyridinones
AU2015301530A1 (en) * 2014-08-15 2017-03-02 PixarBio Corporation Compositions for inhibiting inflammation in a subject with a spinal cord injury and methods of using the same
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
IT201600108927A1 (it) * 2016-10-27 2018-04-27 Dipharma Francis Srl Metodo per sintetizzare un farmaco antifibrotico
IT201600071672A1 (it) * 2016-07-08 2018-01-08 Dipharma Francis Srl Metodo per sintetizzare un farmaco immunosoppressore
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
JP7360171B2 (ja) 2017-07-31 2023-10-12 ワシントン・ユニバーシティ Ｂリンパ球活性の調節及び臓器保護のためのピルフェニドン誘導体
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
CN115666533B (zh) * 2020-04-22 2024-08-09 永进药品工业株式会社 具有改善的安全性和稳定性的含吡非尼酮的肠溶包衣制剂及其制备方法

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Also Published As

Publication number Publication date
US20120016133A1 (en) 2012-01-19
AP3630A (en) 2016-03-08
KR20120016277A (ko) 2012-02-23
TN2011000615A1 (en) 2013-05-24
AP2012006052A0 (en) 2012-02-29
MY162443A (en) 2017-06-15
HN2011003187A (es) 2015-02-02
IL216565A (en) 2015-06-30
UA106759C2 (uk) 2014-10-10
WO2010141600A3 (en) 2011-04-21
US20140221660A1 (en) 2014-08-07
SI2440543T1 (sl) 2015-06-30
MX2011012654A (es) 2012-01-12
NZ596872A (en) 2013-12-20
HUE026014T2 (en) 2016-05-30
US20150065720A1 (en) 2015-03-05
US8519140B2 (en) 2013-08-27
IL216565A0 (en) 2012-03-01
PL2440543T3 (pl) 2015-09-30
ZA201108794B (en) 2013-03-27
MA33489B1 (fr) 2012-08-01
CA2764043A1 (en) 2010-12-09
AR076974A1 (es) 2011-07-20
TWI434833B (zh) 2014-04-21
EA201101695A1 (ru) 2012-05-30
US20110003863A1 (en) 2011-01-06
HRP20150696T1 (hr) 2015-08-28
ES2538103T3 (es) 2015-06-17
EA021826B1 (ru) 2015-09-30
GEP20156223B (en) 2015-01-26
KR101734858B1 (ko) 2017-05-12
EP2440543A4 (en) 2012-11-21
PT2440543E (pt) 2015-07-03
RS54031B1 (en) 2015-10-30
BRPI1011015B1 (pt) 2020-11-10
US20150368200A1 (en) 2015-12-24
CA2764043C (en) 2018-01-16
SG176648A1 (en) 2012-01-30
JP2016026196A (ja) 2016-02-12
AU2010256693B2 (en) 2015-09-17
CL2011003069A1 (es) 2012-05-25
PE20120398A1 (es) 2012-05-13
BRPI1011015A2 (pt) 2018-02-14
AU2010256693A1 (en) 2012-01-12
CN102482255A (zh) 2012-05-30
EP2440543B1 (en) 2015-04-15
US20130345430A1 (en) 2013-12-26
NI201100211A (es) 2012-08-01
DK2440543T3 (en) 2015-05-18
TW201043602A (en) 2010-12-16
JP2012528877A (ja) 2012-11-15
JP5848244B2 (ja) 2016-01-27
EP2440543A2 (en) 2012-04-18
WO2010141600A2 (en) 2010-12-09

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