KR101734858B1 - 피르페니돈을 합성하기 위한 개선된 방법 - Google Patents

피르페니돈을 합성하기 위한 개선된 방법 Download PDF

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KR101734858B1
KR101734858B1 KR1020117029855A KR20117029855A KR101734858B1 KR 101734858 B1 KR101734858 B1 KR 101734858B1 KR 1020117029855 A KR1020117029855 A KR 1020117029855A KR 20117029855 A KR20117029855 A KR 20117029855A KR 101734858 B1 KR101734858 B1 KR 101734858B1
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KR20120016277A (ko
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라마차드란 라드하크리시난
마이크 시르
사빈 마리-프랑소아즈 브리짓 부테트
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인터뮨, 인크.
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    • 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

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  • 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)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Heart & Thoracic Surgery (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)
KR1020117029855A 2009-06-03 2010-06-02 피르페니돈을 합성하기 위한 개선된 방법 Active KR101734858B1 (ko)

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 (2)

Publication Number Publication Date
KR20120016277A KR20120016277A (ko) 2012-02-23
KR101734858B1 true KR101734858B1 (ko) 2017-05-12

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

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EP2296653B1 (en) 2008-06-03 2016-01-27 Intermune, Inc. 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
EP4059499A1 (en) 2011-01-31 2022-09-21 Avalyn Pharma Inc. Aerosol pirfenidone and pyridone analog compounds and uses thereof
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
JP7066321B2 (ja) 2014-01-10 2022-05-13 アヴァリン ファーマ インク. エアロゾルのピルフェニドン及びピリドンのアナログの化合物、及び、その使用
JP6525437B2 (ja) 2014-04-02 2019-06-05 インターミューン, インコーポレイテッド 抗線維性ピリジノン
BR112017002980A2 (pt) * 2014-08-15 2017-12-12 Pixarbio Corp composição para inibir a inflamação em um indivíduo com um dano na coluna vertebral, método para tratar inflamação em um indivíduo tendo um dano na coluna vertebral e kit para produzir a composição
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
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Also Published As

Publication number Publication date
PT2440543E (pt) 2015-07-03
MA33489B1 (fr) 2012-08-01
TWI434833B (zh) 2014-04-21
US20150065720A1 (en) 2015-03-05
AU2010256693A1 (en) 2012-01-12
BRPI1011015A2 (pt) 2018-02-14
EP2440543B1 (en) 2015-04-15
HN2011003187A (es) 2015-02-02
HRP20150696T1 (hr) 2015-08-28
BRPI1011015B8 (pt) 2021-05-25
TW201043602A (en) 2010-12-16
MY162443A (en) 2017-06-15
JP2016026196A (ja) 2016-02-12
ZA201108794B (en) 2013-03-27
JP5848244B2 (ja) 2016-01-27
PL2440543T3 (pl) 2015-09-30
EP2440543A2 (en) 2012-04-18
NZ596872A (en) 2013-12-20
BRPI1011015B1 (pt) 2020-11-10
IL216565A0 (en) 2012-03-01
US20110003863A1 (en) 2011-01-06
HUE026014T2 (en) 2016-05-30
JP2012528877A (ja) 2012-11-15
AU2010256693B2 (en) 2015-09-17
US20130345430A1 (en) 2013-12-26
CL2011003069A1 (es) 2012-05-25
AP2012006052A0 (en) 2012-02-29
NI201100211A (es) 2012-08-01
GEP20156223B (en) 2015-01-26
UA106759C2 (uk) 2014-10-10
CA2764043C (en) 2018-01-16
MX2011012654A (es) 2012-01-12
US20120016133A1 (en) 2012-01-19
US20150368200A1 (en) 2015-12-24
KR20120016277A (ko) 2012-02-23
TN2011000615A1 (en) 2013-05-24
SI2440543T1 (sl) 2015-06-30
EA201101695A1 (ru) 2012-05-30
EA021826B1 (ru) 2015-09-30
SG176648A1 (en) 2012-01-30
EP2440543A4 (en) 2012-11-21
WO2010141600A3 (en) 2011-04-21
PE20120398A1 (es) 2012-05-13
WO2010141600A2 (en) 2010-12-09
AP3630A (en) 2016-03-08
RS54031B1 (sr) 2015-10-30
ES2538103T3 (es) 2015-06-17
US8519140B2 (en) 2013-08-27
IL216565A (en) 2015-06-30
DK2440543T3 (en) 2015-05-18
US20140221660A1 (en) 2014-08-07
CA2764043A1 (en) 2010-12-09
CN102482255A (zh) 2012-05-30
AR076974A1 (es) 2011-07-20

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