ZA201005014B - Method of synthesis of bosentan,its polymorphic forms and its salts - Google Patents

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

Info

Publication number
ZA201005014B
ZA201005014B ZA2010/05014A ZA201005014A ZA201005014B ZA 201005014 B ZA201005014 B ZA 201005014B ZA 2010/05014 A ZA2010/05014 A ZA 2010/05014A ZA 201005014 A ZA201005014 A ZA 201005014A ZA 201005014 B ZA201005014 B ZA 201005014B
Authority
ZA
South Africa
Prior art keywords
bosentan
synthesis
salts
polymorphic forms
polymorphic
Prior art date
Application number
ZA2010/05014A
Other languages
English (en)
Inventor
Ashwini Amol Sawant
Manjinder Singh Phull
Dharmaraj Ramachandra Rao
Rajendra Narayanrao Kankan
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 ZA201005014B publication Critical patent/ZA201005014B/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/69Benzenesulfonamido-pyrimidines
    • 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
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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)
ZA2010/05014A 2008-01-01 2010-07-15 Method of synthesis of bosentan,its polymorphic forms and its salts ZA201005014B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN12MU2008 2008-01-01
IN836MU2008 2008-04-09

Publications (1)

Publication Number Publication Date
ZA201005014B true ZA201005014B (en) 2011-03-30

Family

ID=40424567

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2010/05014A ZA201005014B (en) 2008-01-01 2010-07-15 Method of synthesis of bosentan,its polymorphic forms and its salts

Country Status (9)

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

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2544678C (en) 2003-11-05 2013-12-31 Sunesis Pharmaceuticals, Inc. Modulators of cellular adhesion
EP2248805A3 (en) 2008-01-01 2011-02-23 Cipla Ltd. 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
KR20200108932A (ko) 2012-07-25 2020-09-21 에스에이알코드 바이오사이언스 인코포레이티드 Lfa-1 저해제 및 그의 다형체
EP2890694A4 (en) * 2012-08-31 2015-12-30 Rao Davuluri Ramamohan 4-TERT-BUTYL-N- [6- (2-HYDROXYETHOXY) -5- (2-METHOXYPHENOXY) -2 (2-PYRIMIDINYL) -PYRIMIDIN-4-YL) -BENZENESULFONAMIDE SODIUM
KR102004422B1 (ko) 2012-12-20 2019-07-26 제일약품주식회사 보센탄 일수화물의 제조방법, 이에 사용되는 신규 중간체 및 이의 제조방법
MX2015010725A (es) 2013-02-21 2016-05-31 Adverio Pharma Gmbh Formas de metil {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo [3,4-b] piridino-3-il] pirimidino-5-il} metil carbamato.
KR102259824B1 (ko) * 2018-07-24 2021-06-02 주식회사 마더스제약 보센탄을 함유한 약학 제제
US20250144095A1 (en) * 2022-02-03 2025-05-08 The Johns Hopkins University Compositions and methods for treatment of connective tissue disorders

Family Cites Families (11)

* 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
EP1248869A2 (en) * 2000-01-07 2002-10-16 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
MXPA02007192A (es) 2000-01-25 2002-12-09 Hoffmann La Roche Preparacion de sulfonamidas.
CA2686457A1 (en) * 2007-05-08 2008-11-13 Generics [Uk] Limited Novel polymorphic forms
US8664390B2 (en) * 2007-06-29 2014-03-04 Generics (Uk) Limited Process for the introduction of hydroxyethoxy side chain in bosentan
EP2205591A1 (en) 2007-10-11 2010-07-14 Actavis Group PTC EHF Novel polymorphs of bosentan
NZ585438A (en) 2007-10-24 2012-09-28 Generics Uk Ltd Novel crystalline forms of 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yI]-benzenesulfonamide
EP2248805A3 (en) 2008-01-01 2011-02-23 Cipla Ltd. Method of synthesis of bosentan, its polymorphic forms and its salts
EP2240469A2 (en) 2008-01-24 2010-10-20 Actavis Group PTC EHF Substantially pure and a stable crystalline form of bosentan
EP2294056A1 (en) * 2008-05-23 2011-03-16 Synthon B.V. Bosentan salts

Also Published As

Publication number Publication date
US20110015394A1 (en) 2011-01-20
US8481730B2 (en) 2013-07-09
AU2009203174A1 (en) 2009-07-09
EP2238118A1 (en) 2010-10-13
EP2248805A2 (en) 2010-11-10
WO2009083739A1 (en) 2009-07-09
NZ586900A (en) 2012-10-26
EP2248805A3 (en) 2011-02-23
KR20100113542A (ko) 2010-10-21
JP5535082B2 (ja) 2014-07-02
JP2011508767A (ja) 2011-03-17
AU2009203174B2 (en) 2014-01-30
CA2711043A1 (en) 2009-07-09

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