AU2005276619B2 - Lercanidipine salts - Google Patents
Lercanidipine salts Download PDFInfo
- Publication number
- AU2005276619B2 AU2005276619B2 AU2005276619A AU2005276619A AU2005276619B2 AU 2005276619 B2 AU2005276619 B2 AU 2005276619B2 AU 2005276619 A AU2005276619 A AU 2005276619A AU 2005276619 A AU2005276619 A AU 2005276619A AU 2005276619 B2 AU2005276619 B2 AU 2005276619B2
- Authority
- AU
- Australia
- Prior art keywords
- lercanidipine
- salt
- crystalline
- acid
- amorphous
- 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
Links
- ZDXUKAKRHYTAKV-UHFFFAOYSA-N lercanidipine Chemical class COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)(C)CN(C)CCC(C=2C=CC=CC=2)C=2C=CC=CC=2)C1C1=CC=CC([N+]([O-])=O)=C1 ZDXUKAKRHYTAKV-UHFFFAOYSA-N 0.000 title claims description 186
- 229960004294 lercanidipine Drugs 0.000 claims description 133
- 150000003839 salts Chemical class 0.000 claims description 66
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims description 55
- 239000002253 acid Substances 0.000 claims description 49
- 238000000034 method Methods 0.000 claims description 21
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 16
- WMFYOYKPJLRMJI-UHFFFAOYSA-N Lercanidipine hydrochloride Chemical compound Cl.COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)(C)CN(C)CCC(C=2C=CC=CC=2)C=2C=CC=CC=2)C1C1=CC=CC([N+]([O-])=O)=C1 WMFYOYKPJLRMJI-UHFFFAOYSA-N 0.000 claims description 12
- 229960002162 lercanidipine hydrochloride Drugs 0.000 claims description 12
- 238000002360 preparation method Methods 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- XTEGVFVZDVNBPF-UHFFFAOYSA-N naphthalene-1,5-disulfonic acid Chemical class C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1S(O)(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-N 0.000 claims description 8
- WBYWAXJHAXSJNI-VOTSOKGWSA-M trans-cinnamate Chemical compound [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 claims description 7
- 239000003960 organic solvent Substances 0.000 claims description 6
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- 229960001860 salicylate Drugs 0.000 claims description 5
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- CVHZOJJKTDOEJC-UHFFFAOYSA-M 1,1-dioxo-1,2-benzothiazol-3-olate Chemical compound C1=CC=C2C([O-])=NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-M 0.000 claims description 4
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims description 4
- 229940081974 saccharin Drugs 0.000 claims description 4
- 235000019204 saccharin Nutrition 0.000 claims description 4
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 claims description 4
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
- C07D211/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Heart & Thoracic Surgery (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60414904P | 2004-08-24 | 2004-08-24 | |
| US60/604,149 | 2004-08-24 | ||
| PCT/EP2005/009043 WO2006021397A1 (en) | 2004-08-24 | 2005-08-22 | Lercanidipine salts |
Publications (2)
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| AU2005276619A1 AU2005276619A1 (en) | 2006-03-02 |
| AU2005276619B2 true AU2005276619B2 (en) | 2009-04-30 |
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| Application Number | Title | Priority Date | Filing Date |
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Country Status (19)
| Country | Link |
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| US (1) | US7683179B2 (https=) |
| EP (1) | EP1799644B1 (https=) |
| JP (1) | JP2008510754A (https=) |
| KR (1) | KR20070045351A (https=) |
| CN (1) | CN101048379A (https=) |
| AR (1) | AR050467A1 (https=) |
| AU (1) | AU2005276619B2 (https=) |
| BR (1) | BRPI0514606A (https=) |
| CA (1) | CA2575078A1 (https=) |
| EA (1) | EA011773B1 (https=) |
| ES (1) | ES2462921T3 (https=) |
| IL (1) | IL180905A0 (https=) |
| MX (1) | MX2007002141A (https=) |
| NO (1) | NO20071515L (https=) |
| NZ (1) | NZ553127A (https=) |
| PE (1) | PE20060629A1 (https=) |
| TW (1) | TW200613275A (https=) |
| WO (1) | WO2006021397A1 (https=) |
| ZA (1) | ZA200702364B (https=) |
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| EP1368349B1 (de) * | 2001-02-24 | 2007-02-14 | Boehringer Ingelheim Pharma GmbH & Co.KG | Xanthinderivate, deren herstellung und deren verwendung als arzneimittel |
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| AR052918A1 (es) * | 2005-02-25 | 2007-04-11 | Recordati Ireland Ltd | Clorhidrato de lercanidipina amorfo |
| AR053023A1 (es) * | 2005-02-25 | 2007-04-18 | Recordati Ireland Ltd | Base libre de lercanidipina, metodos para su preparacion y composiciones farmaceuticas que las contienen |
| DE102005035891A1 (de) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| EP2540725A1 (de) | 2006-05-04 | 2013-01-02 | Boehringer Ingelheim International GmbH | Polymorphe von 1-((4-Methyl-chinazolin-2-yl)methyl)-3-methyl-7-(2-butin-1-yl)-8-(3-(R)-amino-piperidin-1-yl)xanthin |
| RU2008151724A (ru) | 2006-06-12 | 2010-07-20 | Новартис АГ (CH) | Способ получения солей n-гидрокси-3-[4-[[[2-(2-метил-1н-индол-3-ил)этил]амино]метил]фенил]-2е-2-пропенамида |
| WO2008040367A1 (en) * | 2006-08-01 | 2008-04-10 | Union Quimico-Farmaceutica S.A. | Lercanidipine hydrobromide, a process for its preparation, crystalline forms and compositions thereof |
| US20080175872A1 (en) * | 2006-09-28 | 2008-07-24 | Osmotica Corp. | Controlled Release Dosage Form Containing Lercanidipine and a Performance-enhancing Acid |
| ES2306595B1 (es) * | 2007-02-09 | 2009-09-11 | Laboratorios Almirall S.A. | Sal de napadisilato de 5-(2-((6-(2,2-difluoro-2-feniletoxi)hexil)amino)-1-hidroxietil)-8-hidroxiquinolin-2(1h)-ona como agonista del receptor adrenergico beta2. |
| IN2009DN05509A (https=) * | 2007-03-14 | 2010-04-30 | Teva Pharma | |
| WO2009017813A1 (en) * | 2007-08-02 | 2009-02-05 | Teva Pharmaceutical Industries Ltd. | O-desmethyl venlafaxine saccharinate |
| CA2706775A1 (en) | 2007-11-26 | 2009-06-04 | Teva Pharmaceutical Industries Ltd. | Crystal forms of o-desmethylvenlafaxine fumarate |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| CN102186351A (zh) * | 2008-08-01 | 2011-09-14 | 医药公司 | 药物组合物和用于稳定药物组合物的方法 |
| WO2010014727A1 (en) * | 2008-08-01 | 2010-02-04 | The Medicines Company | Pharmaceutical compositions and methods for producing low impurity concentrations of the same |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| BRPI0916997A2 (pt) | 2008-08-06 | 2020-12-15 | Boehringer Ingelheim International Gmbh | Inibidor de dpp-4 e seu uso |
| CN102149407A (zh) | 2008-09-10 | 2011-08-10 | 贝林格尔.英格海姆国际有限公司 | 治疗糖尿病和相关病症的组合疗法 |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| CN102256976A (zh) | 2008-12-23 | 2011-11-23 | 贝林格尔.英格海姆国际有限公司 | 有机化合物的盐形式 |
| AR074990A1 (es) | 2009-01-07 | 2011-03-02 | Boehringer Ingelheim Int | Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina |
| KR20240090632A (ko) | 2009-11-27 | 2024-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| EP2539313A2 (en) * | 2010-03-29 | 2013-01-02 | Pliva Hrvatska D.O.O. | Crystal forms of o-desmethylvenlafaxine fumarate |
| CN102946875A (zh) | 2010-05-05 | 2013-02-27 | 贝林格尔.英格海姆国际有限公司 | 组合疗法 |
| WO2011161161A1 (en) | 2010-06-24 | 2011-12-29 | Boehringer Ingelheim International Gmbh | Diabetes therapy |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| US8883800B2 (en) | 2011-07-15 | 2014-11-11 | Boehringer Ingelheim International Gmbh | Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| JP6224084B2 (ja) | 2012-05-14 | 2017-11-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 糸球体上皮細胞関連障害及び／又はネフローゼ症候群の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体 |
| JP6218811B2 (ja) | 2012-05-14 | 2017-10-25 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｓｉｒｓ及び／又は敗血症の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体 |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| EP3110449B1 (en) | 2014-02-28 | 2023-06-28 | Boehringer Ingelheim International GmbH | Medical use of a dpp-4 inhibitor |
| CN109310697A (zh) | 2016-06-10 | 2019-02-05 | 勃林格殷格翰国际有限公司 | 利格列汀和二甲双胍的组合 |
| JPWO2023219106A1 (https=) * | 2022-05-10 | 2023-11-16 |
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| US4705797A (en) * | 1984-02-14 | 1987-11-10 | Recordati S.A., Chemical And Pharmaceutical Company | N-(3,3-diphenylpropyl) aminoethyl esters of 1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylic acid, compositions and use |
| WO1997003669A1 (en) * | 1995-07-14 | 1997-02-06 | Recordati S.A., Chemical And Pharmaceutical Company | Use of 1,4-dihydropyridine derivatives in the prevention and therapy of atherosclerotic degradation of arterial walls |
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| US6852737B2 (en) | 2001-08-06 | 2005-02-08 | Recordati Ireland Limited | Crude and crystalline forms of lercanidipine hydrochloride |
| US6699892B2 (en) * | 2002-06-04 | 2004-03-02 | Yung Shin Pharmaceutical Industrial Co., Ltd. | Pharmaceutically acceptable salt of amlodipine and method of preparing the same |
| US20040198789A1 (en) * | 2003-02-28 | 2004-10-07 | Recordati Ireland Limited | Lercanidipine/ARB/diuretic therapeutic combinations |
-
2005
- 2005-08-19 TW TW094128384A patent/TW200613275A/zh unknown
- 2005-08-22 EA EA200700492A patent/EA011773B1/ru not_active IP Right Cessation
- 2005-08-22 AR ARP050103516A patent/AR050467A1/es not_active Application Discontinuation
- 2005-08-22 BR BRPI0514606-2A patent/BRPI0514606A/pt not_active IP Right Cessation
- 2005-08-22 EP EP05776228.8A patent/EP1799644B1/en not_active Expired - Lifetime
- 2005-08-22 WO PCT/EP2005/009043 patent/WO2006021397A1/en not_active Ceased
- 2005-08-22 AU AU2005276619A patent/AU2005276619B2/en not_active Ceased
- 2005-08-22 JP JP2007528715A patent/JP2008510754A/ja not_active Abandoned
- 2005-08-22 NZ NZ553127A patent/NZ553127A/xx not_active IP Right Cessation
- 2005-08-22 MX MX2007002141A patent/MX2007002141A/es not_active Application Discontinuation
- 2005-08-22 CA CA002575078A patent/CA2575078A1/en not_active Abandoned
- 2005-08-22 KR KR1020077006715A patent/KR20070045351A/ko not_active Withdrawn
- 2005-08-22 PE PE2005000963A patent/PE20060629A1/es not_active Application Discontinuation
- 2005-08-22 ES ES05776228.8T patent/ES2462921T3/es not_active Expired - Lifetime
- 2005-08-22 CN CNA2005800284676A patent/CN101048379A/zh active Pending
- 2005-08-24 US US11/211,769 patent/US7683179B2/en not_active Expired - Fee Related
-
2007
- 2007-01-23 IL IL180905A patent/IL180905A0/en unknown
- 2007-03-22 ZA ZA200702364A patent/ZA200702364B/xx unknown
- 2007-03-23 NO NO20071515A patent/NO20071515L/no not_active Application Discontinuation
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4705797A (en) * | 1984-02-14 | 1987-11-10 | Recordati S.A., Chemical And Pharmaceutical Company | N-(3,3-diphenylpropyl) aminoethyl esters of 1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylic acid, compositions and use |
| WO1997003669A1 (en) * | 1995-07-14 | 1997-02-06 | Recordati S.A., Chemical And Pharmaceutical Company | Use of 1,4-dihydropyridine derivatives in the prevention and therapy of atherosclerotic degradation of arterial walls |
| WO2004035051A1 (en) * | 2002-10-16 | 2004-04-29 | Recordati Ireland Limited | Lisinopril/lercanidipine combination therapy |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20070045351A (ko) | 2007-05-02 |
| EA200700492A1 (ru) | 2007-08-31 |
| AR050467A1 (es) | 2006-10-25 |
| CA2575078A1 (en) | 2006-03-02 |
| NZ553127A (en) | 2009-07-31 |
| WO2006021397A8 (en) | 2006-04-27 |
| MX2007002141A (es) | 2007-04-27 |
| ZA200702364B (en) | 2008-09-25 |
| US20060047125A1 (en) | 2006-03-02 |
| IL180905A0 (en) | 2007-07-04 |
| WO2006021397A1 (en) | 2006-03-02 |
| EP1799644A1 (en) | 2007-06-27 |
| EP1799644B1 (en) | 2014-02-12 |
| JP2008510754A (ja) | 2008-04-10 |
| NO20071515L (no) | 2007-05-22 |
| TW200613275A (en) | 2006-05-01 |
| BRPI0514606A (pt) | 2008-06-17 |
| AU2005276619A1 (en) | 2006-03-02 |
| EA011773B1 (ru) | 2009-06-30 |
| ES2462921T3 (es) | 2014-05-26 |
| PE20060629A1 (es) | 2006-08-11 |
| US7683179B2 (en) | 2010-03-23 |
| CN101048379A (zh) | 2007-10-03 |
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