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UA106759C2 - Спосіб синтезу пірфенідону - Google Patents

Спосіб синтезу пірфенідону

Info

Publication number
UA106759C2
UA106759C2 UAA201115405A UAA201115405A UA106759C2 UA 106759 C2 UA106759 C2 UA 106759C2 UA A201115405 A UAA201115405 A UA A201115405A UA A201115405 A UAA201115405 A UA A201115405A UA 106759 C2 UA106759 C2 UA 106759C2
Authority
UA
Ukraine
Prior art keywords
pirfenidone
disclosed
synthesizing
butanol
ethyl acetate
Prior art date
Application number
UAA201115405A
Other languages
English (en)
Russian (ru)
Inventor
Рамачандран Радхакрішнан
Майк Сір
Сабін Марі-Франсуаз Бріжитт Буте
Original Assignee
Інтерм'Юн, Інк.
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=UA106759(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Інтерм'Юн, Інк. filed Critical Інтерм'Юн, Інк.
Publication of UA106759C2 publication Critical patent/UA106759C2/uk

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)
  • 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)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Agronomy & Crop Science (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (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)

Abstract

Описано спосіб синтезу пірфенідону із бромбензолу, що містить менше ніж приблизно 0,15 % за масою дибромбензолу.Також описані способи синтезу: пірфенідону без використання етилацетату або н-бутанолу, і пірфенідон, що містить: контрольовані рівні етилацетату, н-бутанолу, ди(2-піридинон)бензолів, і інших домішок, що мають зазначені часи втримання.Також описані складені в композиції лікарські форми, що містять описаний пірфенідон.
UAA201115405A 2009-06-03 2010-06-02 Спосіб синтезу пірфенідону UA106759C2 (uk)

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
UA106759C2 true UA106759C2 (uk) 2014-10-10

Family

ID=43298478

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201115405A UA106759C2 (uk) 2009-06-03 2010-06-02 Спосіб синтезу пірфенідону

Country Status (35)

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

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102099036B (zh) 2008-06-03 2015-05-27 英特芒尼公司 用于治疗炎性疾患和纤维化疾患的化合物和方法
US10105356B2 (en) 2011-01-31 2018-10-23 Avalyn Pharma Inc. Aerosol pirfenidone and pyridone analog compounds and uses thereof
HUE058753T2 (hu) 2011-01-31 2022-09-28 Avalyn Pharma Inc Aeroszol formájú pirfenidon- és piridon-analóg vegyületek és alkalmazásaik
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
KR102373700B1 (ko) 2014-04-02 2022-03-11 인터뮨, 인크. 항섬유성 피리디논
JP2017527611A (ja) * 2014-08-15 2017-09-21 ピクサーバイオ コーポレーション 脊髄損傷を有する患者において炎症を阻害するための組成物、及びそれを使用する方法
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
US20180009753A1 (en) * 2016-07-08 2018-01-11 Dipharma Francis S.R.L. Method for preparing an antifibrotic agent
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
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
CA3108048A1 (en) 2017-07-31 2019-02-07 Washington University Pirfenidone derivatives for modulation of b lymphocyte activity and organ protection
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
US20230158004A1 (en) * 2020-04-22 2023-05-25 Yungjin Pharm. Co., Ltd. Enteric-coated preparation comprising pirfenidone having improved safety and stability, and method for preparing same

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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
JPWO2002085858A1 (ja) * 2001-04-20 2004-08-12 旭硝子株式会社 精製されたピペリジン誘導体の製造方法
KR100898888B1 (ko) * 2001-08-06 2009-05-21 시오노기세이야쿠가부시키가이샤 5-메틸-1-페닐-2(1ｈ)피리디논의 제조 방법
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CN101842355A (zh) * 2007-06-20 2010-09-22 奥斯拜客斯制药有限公司 作为纤维化抑制剂的取代的n-芳基吡啶酮
US20090131485A1 (en) * 2007-09-10 2009-05-21 Concert Pharmaceuticals, Inc. Deuterated pirfenidone

Also Published As

Publication number Publication date
CA2764043A1 (en) 2010-12-09
ES2538103T3 (es) 2015-06-17
TWI434833B (zh) 2014-04-21
SG176648A1 (en) 2012-01-30
EA201101695A1 (ru) 2012-05-30
IL216565A (en) 2015-06-30
ZA201108794B (en) 2013-03-27
AU2010256693B2 (en) 2015-09-17
US20150368200A1 (en) 2015-12-24
GEP20156223B (en) 2015-01-26
MA33489B1 (fr) 2012-08-01
TW201043602A (en) 2010-12-16
TN2011000615A1 (en) 2013-05-24
NI201100211A (es) 2012-08-01
IL216565A0 (en) 2012-03-01
AP3630A (en) 2016-03-08
RS54031B1 (en) 2015-10-30
AU2010256693A1 (en) 2012-01-12
CA2764043C (en) 2018-01-16
PE20120398A1 (es) 2012-05-13
AR076974A1 (es) 2011-07-20
KR20120016277A (ko) 2012-02-23
JP2012528877A (ja) 2012-11-15
MX2011012654A (es) 2012-01-12
PT2440543E (pt) 2015-07-03
BRPI1011015B8 (pt) 2021-05-25
CN102482255A (zh) 2012-05-30
JP2016026196A (ja) 2016-02-12
WO2010141600A3 (en) 2011-04-21
CL2011003069A1 (es) 2012-05-25
SI2440543T1 (sl) 2015-06-30
EA021826B1 (ru) 2015-09-30
BRPI1011015B1 (pt) 2020-11-10
US20120016133A1 (en) 2012-01-19
MY162443A (en) 2017-06-15
HRP20150696T1 (hr) 2015-08-28
DK2440543T3 (en) 2015-05-18
PL2440543T3 (pl) 2015-09-30
AP2012006052A0 (en) 2012-02-29
US20140221660A1 (en) 2014-08-07
EP2440543A4 (en) 2012-11-21
HN2011003187A (es) 2015-02-02
US20130345430A1 (en) 2013-12-26
BRPI1011015A2 (pt) 2018-02-14
EP2440543A2 (en) 2012-04-18
US20150065720A1 (en) 2015-03-05
NZ596872A (en) 2013-12-20
US20110003863A1 (en) 2011-01-06
JP5848244B2 (ja) 2016-01-27
WO2010141600A2 (en) 2010-12-09
EP2440543B1 (en) 2015-04-15
HUE026014T2 (en) 2016-05-30
US8519140B2 (en) 2013-08-27
KR101734858B1 (ko) 2017-05-12

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