JP5683276B2 - ボセンタンの製造方法 - Google Patents
ボセンタンの製造方法 Download PDFInfo
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- JP5683276B2 JP5683276B2 JP2010545563A JP2010545563A JP5683276B2 JP 5683276 B2 JP5683276 B2 JP 5683276B2 JP 2010545563 A JP2010545563 A JP 2010545563A JP 2010545563 A JP2010545563 A JP 2010545563A JP 5683276 B2 JP5683276 B2 JP 5683276B2
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- compound
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- ethylene glycol
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- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 1
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- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
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- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
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- 229910000386 magnesium trisilicate Inorganic materials 0.000 description 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
- 229940043353 maltol Drugs 0.000 description 1
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- 229910052751 metal Inorganic materials 0.000 description 1
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- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
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- 235000011164 potassium chloride Nutrition 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
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- 238000001694 spray drying Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 229960004274 stearic acid Drugs 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229960001367 tartaric acid Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 125000000025 triisopropylsilyl group Chemical group C(C)(C)[Si](C(C)C)(C(C)C)* 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
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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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
-
- 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
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN228/KOL/2008 | 2008-02-08 | ||
| IN228KO2008 | 2008-02-08 | ||
| PCT/GB2009/050120 WO2009098517A1 (en) | 2008-02-08 | 2009-02-06 | Process for preparing bosentan |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011511054A JP2011511054A (ja) | 2011-04-07 |
| JP2011511054A5 JP2011511054A5 (cg-RX-API-DMAC10.html) | 2012-03-22 |
| JP5683276B2 true JP5683276B2 (ja) | 2015-03-11 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010545563A Expired - Fee Related JP5683276B2 (ja) | 2008-02-08 | 2009-02-06 | ボセンタンの製造方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8785461B2 (cg-RX-API-DMAC10.html) |
| EP (1) | EP2245018B1 (cg-RX-API-DMAC10.html) |
| JP (1) | JP5683276B2 (cg-RX-API-DMAC10.html) |
| CN (1) | CN101939301B (cg-RX-API-DMAC10.html) |
| AU (1) | AU2009211159B2 (cg-RX-API-DMAC10.html) |
| CA (1) | CA2712860C (cg-RX-API-DMAC10.html) |
| ES (1) | ES2650247T3 (cg-RX-API-DMAC10.html) |
| NZ (1) | NZ587793A (cg-RX-API-DMAC10.html) |
| PT (1) | PT2245018T (cg-RX-API-DMAC10.html) |
| WO (1) | WO2009098517A1 (cg-RX-API-DMAC10.html) |
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| WO2009004374A1 (en) | 2007-06-29 | 2009-01-08 | Generics [Uk] Limited | Process for introduction of hydroxyethoxy side chain in bosentan |
| US8530488B2 (en) | 2007-10-24 | 2013-09-10 | Generics [Uk] Limited | Crystalline forms of bosentan |
| JP2012507497A (ja) | 2008-11-03 | 2012-03-29 | ジェネリクス・（ユーケー）・リミテッド | ボセンタンおよび関連物質のｈｐｌｃ分析方法、ならびに参照スタンダードまたはマーカーとしてのこれら物質の使用 |
| WO2013098577A1 (en) * | 2011-12-31 | 2013-07-04 | Abdi Ibrahim Ilac Sanayi Ve Ticaret Anonim Sirketi | Pharmaceutical compositions of bosentan |
| CN104487057A (zh) * | 2012-05-11 | 2015-04-01 | 韩诺生物制药株式会社 | 波生坦控释口服制剂 |
| CN112457259B (zh) * | 2020-12-08 | 2024-02-20 | 重庆康乐制药有限公司 | 一种磺胺多辛的制备方法 |
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|---|---|---|---|---|
| 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 |
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| HUP0204069A3 (en) | 1999-12-16 | 2005-01-28 | Teva Pharma | Novel processes for making- and a new crystalline form of- leflunomide and pharmaceutical composition containing it |
| PT1254121E (pt) | 2000-01-25 | 2006-06-30 | Hoffmann La Roche | Preparacao de sulfonamidas |
| US6479692B1 (en) | 2001-05-02 | 2002-11-12 | Nobex Corporation | Methods of synthesizing acylanilides including bicalutamide and derivatives thereof |
| AU2003209669A1 (en) | 2003-02-25 | 2004-09-17 | Hetero Drugs Limited | Amorphous form of losartan potassium |
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| WO2004087660A1 (en) | 2003-04-02 | 2004-10-14 | Hetero Drugs Limited | A novel process for amorphous form of donepezil hydrochloride |
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| US20080188663A1 (en) | 2007-01-29 | 2008-08-07 | Ashok Kumar | Process for the preparation of crystalline clopidogrel hydrogen sulphate Form I |
| BRPI0809171A2 (pt) | 2007-04-02 | 2014-09-16 | Auspex Pharmaceuticals Inc | "composto, composição farmacêutica, método para tratamento,prevençõ ou melhora de um ou mais , sintomas de uma desordem mediada pela endotelina em um sujeito, método de inibição de ligação d euma endotelina a um receptor eta ou etb e método para modular a atividade mediada pelo receptor de endotelina" |
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| 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 |
| ATE530531T1 (de) * | 2007-12-18 | 2011-11-15 | Dipharma Francis Srl | Verfahren zur herstellung von bosentan |
| WO2009095933A2 (en) | 2008-01-10 | 2009-08-06 | Msn Laboratories Limited | Improved and novel process for the preparation of bosentan |
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| WO2009112954A2 (en) | 2008-03-13 | 2009-09-17 | Actavis Group Ptc Ehf | Processes for the preparation of bosentan and related compounds using novel intermediates |
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| JP2012507497A (ja) | 2008-11-03 | 2012-03-29 | ジェネリクス・（ユーケー）・リミテッド | ボセンタンおよび関連物質のｈｐｌｃ分析方法、ならびに参照スタンダードまたはマーカーとしてのこれら物質の使用 |
| IT1393136B1 (it) | 2009-03-11 | 2012-04-11 | Sifa Vitor S R L | Procedimento per la preparazione del bosentan |
-
2009
- 2009-02-06 CA CA2712860A patent/CA2712860C/en not_active Expired - Fee Related
- 2009-02-06 NZ NZ587793A patent/NZ587793A/en not_active IP Right Cessation
- 2009-02-06 JP JP2010545563A patent/JP5683276B2/ja not_active Expired - Fee Related
- 2009-02-06 AU AU2009211159A patent/AU2009211159B2/en not_active Ceased
- 2009-02-06 WO PCT/GB2009/050120 patent/WO2009098517A1/en not_active Ceased
- 2009-02-06 US US12/866,373 patent/US8785461B2/en active Active
- 2009-02-06 CN CN200980104551.XA patent/CN101939301B/zh not_active Expired - Fee Related
- 2009-02-06 EP EP09709282.9A patent/EP2245018B1/en not_active Not-in-force
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Also Published As
| Publication number | Publication date |
|---|---|
| CN101939301B (zh) | 2016-07-06 |
| CN101939301A (zh) | 2011-01-05 |
| CA2712860A1 (en) | 2009-08-13 |
| AU2009211159A1 (en) | 2009-08-13 |
| US20110039871A1 (en) | 2011-02-17 |
| EP2245018A1 (en) | 2010-11-03 |
| PT2245018T (pt) | 2017-12-05 |
| CA2712860C (en) | 2014-11-18 |
| JP2011511054A (ja) | 2011-04-07 |
| NZ587793A (en) | 2012-06-29 |
| EP2245018B1 (en) | 2017-08-30 |
| AU2009211159B2 (en) | 2013-02-07 |
| US8785461B2 (en) | 2014-07-22 |
| WO2009098517A1 (en) | 2009-08-13 |
| ES2650247T3 (es) | 2018-01-17 |
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