AU2009203174B2 - Method of synthesis of bosentan, its polymorphic forms and its salts - Google Patents

Method of synthesis of bosentan, its polymorphic forms and its salts Download PDF

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Publication number
AU2009203174B2
AU2009203174B2 AU2009203174A AU2009203174A AU2009203174B2 AU 2009203174 B2 AU2009203174 B2 AU 2009203174B2 AU 2009203174 A AU2009203174 A AU 2009203174A AU 2009203174 A AU2009203174 A AU 2009203174A AU 2009203174 B2 AU2009203174 B2 AU 2009203174B2
Authority
AU
Australia
Prior art keywords
bosentan
anhydrous
anhydrous bosentan
bosentan form
solvent
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2009203174A
Other languages
English (en)
Other versions
AU2009203174A1 (en
Inventor
Rajendra Narayanrao Kankan
Manjinder Singh Phull
Dharmaraj Ramachandra Rao
Ashwini Amol Sawant
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cipla Ltd
Original Assignee
Cipla Ltd
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 Cipla Ltd filed Critical Cipla Ltd
Publication of AU2009203174A1 publication Critical patent/AU2009203174A1/en
Application granted granted Critical
Publication of AU2009203174B2 publication Critical patent/AU2009203174B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/69—Benzenesulfonamido-pyrimidines
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/12—Antihypertensives

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
AU2009203174A 2008-01-01 2009-01-02 Method of synthesis of bosentan, its polymorphic forms and its salts Ceased AU2009203174B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
IN12/MUM/2008 2008-01-01
IN12MU2008 2008-01-01
IN836/MUM/2008 2008-04-09
IN836MU2008 2008-04-09
PCT/GB2009/000009 WO2009083739A1 (en) 2008-01-01 2009-01-02 Method of synthesis of bosentan, its polymorphic forms and its salts

Publications (2)

Publication Number Publication Date
AU2009203174A1 AU2009203174A1 (en) 2009-07-09
AU2009203174B2 true AU2009203174B2 (en) 2014-01-30

Family

ID=40424567

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2009203174A Ceased AU2009203174B2 (en) 2008-01-01 2009-01-02 Method of synthesis of bosentan, its polymorphic forms and its salts

Country Status (9)

Country Link
US (1) US8481730B2 (enExample)
EP (2) EP2248805A3 (enExample)
JP (1) JP5535082B2 (enExample)
KR (1) KR20100113542A (enExample)
AU (1) AU2009203174B2 (enExample)
CA (1) CA2711043A1 (enExample)
NZ (1) NZ586900A (enExample)
WO (1) WO2009083739A1 (enExample)
ZA (1) ZA201005014B (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2004287875B2 (en) 2003-11-05 2011-06-02 Bausch + Lomb Ireland Limited Modulators of cellular adhesion
AU2009203174B2 (en) 2008-01-01 2014-01-30 Cipla Limited Method of synthesis of bosentan, its polymorphic forms and its salts
CA2781541A1 (en) 2009-11-12 2011-05-19 Ranbaxy Laboratories Limited Crystalline forms of bosentan salt and processes for their preparation
JP5356323B2 (ja) * 2010-07-01 2013-12-04 富士化学工業株式会社 新規な非晶質ボセンタン及びその製造方法
WO2012002547A1 (ja) * 2010-07-02 2012-01-05 富士化学工業株式会社 ボセンタン固体分散体
JP5850576B2 (ja) * 2010-07-06 2016-02-03 富士化学工業株式会社 ボセンタン固体分散体
US20130245259A1 (en) 2012-03-16 2013-09-19 Natco Pharma Limited Process for the preparation of bosentan monohydrate
ITMI20120701A1 (it) 2012-04-27 2013-10-28 Dipharma Francis Srl Procedimento per la purificazione di un composto benzensolfonammidico
EP2877465A4 (en) 2012-07-25 2016-05-11 Sarcode Bioscience Inc LFA-1 HEMMER AND POLYMORPH THEREOF
WO2014033758A1 (en) * 2012-08-31 2014-03-06 Rao Davuluri Ramamohan 4-tert-butyl-n-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2(2-pyrimidinyl)-pyrimidine-4-yl)-benzen esulfonamide sodium
KR102004422B1 (ko) 2012-12-20 2019-07-26 제일약품주식회사 보센탄 일수화물의 제조방법, 이에 사용되는 신규 중간체 및 이의 제조방법
CA2901636A1 (en) 2013-02-21 2014-08-28 Adverio Pharma Gmbh Forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methyl carbamate
KR102259824B1 (ko) * 2018-07-24 2021-06-02 주식회사 마더스제약 보센탄을 함유한 약학 제제
WO2023150702A2 (en) * 2022-02-03 2023-08-10 The Johns Hopkins University Compositions and methods for treatment of connective tissue disorders

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001055120A1 (en) * 2000-01-25 2001-08-02 F. Hoffmann-La Roche Ag Preparation of sulfonamides

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2086544C1 (ru) 1991-06-13 1997-08-10 Хоффманн-Ля Рош АГ Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина
US6136971A (en) * 1998-07-17 2000-10-24 Roche Colorado Corporation Preparation of sulfonamides
IL150524A0 (en) * 2000-01-07 2003-02-12 Transform Pharmaceuticals Inc High-throughput formation, identification, and analysis of diverse solid-forms
WO2008135795A2 (en) * 2007-05-08 2008-11-13 Generics [Uk] Limited Polymorphic forms of bosentan
WO2009004374A1 (en) * 2007-06-29 2009-01-08 Generics [Uk] Limited Process for introduction of hydroxyethoxy side chain in bosentan
EP2205591A1 (en) * 2007-10-11 2010-07-14 Actavis Group PTC EHF Novel polymorphs of bosentan
US8530488B2 (en) * 2007-10-24 2013-09-10 Generics [Uk] Limited Crystalline forms of bosentan
AU2009203174B2 (en) 2008-01-01 2014-01-30 Cipla Limited Method of synthesis of bosentan, its polymorphic forms and its salts
US20110021547A1 (en) * 2008-01-24 2011-01-27 Actavis Group Ptc Ehf Substantially Pure and a Stable Crystalline Form of Bosentan
WO2009141167A1 (en) * 2008-05-23 2009-11-26 Synthon B.V. Bosentan salts

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001055120A1 (en) * 2000-01-25 2001-08-02 F. Hoffmann-La Roche Ag Preparation of sulfonamides

Also Published As

Publication number Publication date
JP2011508767A (ja) 2011-03-17
EP2238118A1 (en) 2010-10-13
US8481730B2 (en) 2013-07-09
JP5535082B2 (ja) 2014-07-02
EP2248805A2 (en) 2010-11-10
AU2009203174A1 (en) 2009-07-09
US20110015394A1 (en) 2011-01-20
KR20100113542A (ko) 2010-10-21
ZA201005014B (en) 2011-03-30
EP2248805A3 (en) 2011-02-23
CA2711043A1 (en) 2009-07-09
WO2009083739A1 (en) 2009-07-09
NZ586900A (en) 2012-10-26

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Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired
NA Applications received for extensions of time, section 223

Free format text: AN APPLICATION TO EXTEND THE TIME FROM 02 JAN 2015 TO 02 SEP 2015 IN WHICH TO PAY A RENEWAL FEE HAS BEEN FILED .

NB Applications allowed - extensions of time section 223(2)

Free format text: THE TIME IN WHICH TO PAY A RENEWAL FEE HAS BEEN EXTENDED TO 02 SEP 2015 .

MK14 Patent ceased section 143(a) (annual fees not paid) or expired