ZA201005014B - Method of synthesis of bosentan,its polymorphic forms and its salts - Google Patents
Method of synthesis of bosentan,its polymorphic forms and its saltsInfo
- 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
Links
- 230000015572 biosynthetic process Effects 0.000 title 1
- GJPICJJJRGTNOD-UHFFFAOYSA-N bosentan Chemical compound COC1=CC=CC=C1OC(C(=NC(=N1)C=2N=CC=CN=2)OCCO)=C1NS(=O)(=O)C1=CC=C(C(C)(C)C)C=C1 GJPICJJJRGTNOD-UHFFFAOYSA-N 0.000 title 1
- 229960003065 bosentan Drugs 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 150000003839 salts Chemical class 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
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
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
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 (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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004287875B2 (en) | 2003-11-05 | 2011-06-02 | Bausch + Lomb Ireland Limited | Modulators of cellular adhesion |
| CA2711043A1 (en) | 2008-01-01 | 2009-07-09 | Cipla Limited | Method of synthesis of bosentan, its polymorphic forms and its salts |
| US8716477B2 (en) | 2009-11-12 | 2014-05-06 | Ranbaxy Laboratories Limited | Crystalline forms of bosentan salts 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 |
| EP4406950A3 (en) | 2012-07-25 | 2025-04-23 | Bausch + Lomb Ireland Limited | Lfa-1 inhibitor and polymorph thereof |
| 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 |
| EP2958914B1 (en) | 2013-02-21 | 2020-07-15 | 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 |
| 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)
| 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 |
| MXPA02006660A (es) * | 2000-01-07 | 2002-12-13 | Transform Pharmaceuticals Inc | Formacion, identificacion y analisis de diversas formas solidas de alto rendimiento. |
| WO2001055120A1 (en) | 2000-01-25 | 2001-08-02 | F. Hoffmann-La Roche Ag | Preparation of sulfonamides |
| US8288401B2 (en) * | 2007-05-08 | 2012-10-16 | Generics [Uk] Limited | Polymorphic forms |
| AU2008272685B2 (en) * | 2007-06-29 | 2013-04-18 | 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 |
| JP2011500780A (ja) * | 2007-10-24 | 2011-01-06 | ジェネリクス・(ユーケー)・リミテッド | 新規結晶形 |
| CA2711043A1 (en) | 2008-01-01 | 2009-07-09 | Cipla Limited | Method of synthesis of bosentan, its polymorphic forms and its salts |
| WO2009093127A2 (en) * | 2008-01-24 | 2009-07-30 | 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 |
-
2009
- 2009-01-02 CA CA2711043A patent/CA2711043A1/en not_active Abandoned
- 2009-01-02 NZ NZ586900A patent/NZ586900A/xx not_active IP Right Cessation
- 2009-01-02 WO PCT/GB2009/000009 patent/WO2009083739A1/en not_active Ceased
- 2009-01-02 EP EP10172685A patent/EP2248805A3/en not_active Withdrawn
- 2009-01-02 AU AU2009203174A patent/AU2009203174B2/en not_active Ceased
- 2009-01-02 KR KR1020107017092A patent/KR20100113542A/ko not_active Abandoned
- 2009-01-02 EP EP09700123A patent/EP2238118A1/en not_active Withdrawn
- 2009-01-02 JP JP2010541098A patent/JP5535082B2/ja not_active Expired - Fee Related
- 2009-01-02 US US12/811,279 patent/US8481730B2/en not_active Expired - Fee Related
-
2010
- 2010-07-15 ZA ZA2010/05014A patent/ZA201005014B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2711043A1 (en) | 2009-07-09 |
| EP2248805A3 (en) | 2011-02-23 |
| WO2009083739A1 (en) | 2009-07-09 |
| AU2009203174A1 (en) | 2009-07-09 |
| KR20100113542A (ko) | 2010-10-21 |
| EP2248805A2 (en) | 2010-11-10 |
| JP5535082B2 (ja) | 2014-07-02 |
| EP2238118A1 (en) | 2010-10-13 |
| AU2009203174B2 (en) | 2014-01-30 |
| US20110015394A1 (en) | 2011-01-20 |
| JP2011508767A (ja) | 2011-03-17 |
| US8481730B2 (en) | 2013-07-09 |
| NZ586900A (en) | 2012-10-26 |
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