JP2008510754A5 - - Google Patents
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- Publication number
- JP2008510754A5 JP2008510754A5 JP2007528715A JP2007528715A JP2008510754A5 JP 2008510754 A5 JP2008510754 A5 JP 2008510754A5 JP 2007528715 A JP2007528715 A JP 2007528715A JP 2007528715 A JP2007528715 A JP 2007528715A JP 2008510754 A5 JP2008510754 A5 JP 2008510754A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- lercanidipine
- acid
- acid addition
- addition salt
- 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.)
- Abandoned
Links
- 150000003839 salts Chemical class 0.000 claims 18
- 229960004294 lercanidipine Drugs 0.000 claims 11
- 239000002253 acid Substances 0.000 claims 10
- ZDXUKAKRHYTAKV-UHFFFAOYSA-N lercanidipine Chemical compound 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 claims 10
- JVTAAEKCZFNVCJ-REOHCLBHSA-N L-lactic acid Chemical compound C[C@H](O)C(O)=O JVTAAEKCZFNVCJ-REOHCLBHSA-N 0.000 claims 3
- -1 lercanidipine benzenesulfonate salt Chemical class 0.000 claims 3
- WBYWAXJHAXSJNI-VOTSOKGWSA-M .beta-Phenylacrylic acid Natural products [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 150000002500 ions Chemical class 0.000 claims 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 2
- XTEGVFVZDVNBPF-UHFFFAOYSA-N naphthalene-1,5-disulfonic acid Chemical compound C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1S(O)(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-N 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 2
- WBYWAXJHAXSJNI-SREVYHEPSA-N Cinnamic acid Chemical compound OC(=O)\C=C/C1=CC=CC=C1 WBYWAXJHAXSJNI-SREVYHEPSA-N 0.000 claims 1
- DSLZVSRJTYRBFB-LLEIAEIESA-N D-glucaric acid Chemical compound OC(=O)[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O DSLZVSRJTYRBFB-LLEIAEIESA-N 0.000 claims 1
- 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 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 1
- 239000000010 aprotic solvent Substances 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims 1
- 229940092714 benzenesulfonic acid Drugs 0.000 claims 1
- 229940114081 cinnamate Drugs 0.000 claims 1
- 229930016911 cinnamic acid Natural products 0.000 claims 1
- 235000013985 cinnamic acid Nutrition 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940116871 l-lactate Drugs 0.000 claims 1
- 229960002162 lercanidipine hydrochloride Drugs 0.000 claims 1
- 239000011976 maleic acid Substances 0.000 claims 1
- 229940098895 maleic acid Drugs 0.000 claims 1
- WBYWAXJHAXSJNI-UHFFFAOYSA-N methyl p-hydroxycinnamate Natural products OC(=O)C=CC1=CC=CC=C1 WBYWAXJHAXSJNI-UHFFFAOYSA-N 0.000 claims 1
- XTEGVFVZDVNBPF-UHFFFAOYSA-L naphthalene-1,5-disulfonate(2-) Chemical compound C1=CC=C2C(S(=O)(=O)[O-])=CC=CC2=C1S([O-])(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-L 0.000 claims 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000003586 protic polar solvent Substances 0.000 claims 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims 1
- 229940081974 saccharin Drugs 0.000 claims 1
- 235000019204 saccharin Nutrition 0.000 claims 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 claims 1
- 229960001860 salicylate Drugs 0.000 claims 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 claims 1
- 229960004889 salicylic acid Drugs 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60414904P | 2004-08-24 | 2004-08-24 | |
| PCT/EP2005/009043 WO2006021397A1 (en) | 2004-08-24 | 2005-08-22 | Lercanidipine salts |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008510754A JP2008510754A (ja) | 2008-04-10 |
| JP2008510754A5 true JP2008510754A5 (https=) | 2008-10-09 |
Family
ID=35159792
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007528715A Abandoned JP2008510754A (ja) | 2004-08-24 | 2005-08-22 | レルカニジピンの塩 |
Country Status (19)
| Country | Link |
|---|---|
| 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=) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100926247B1 (ko) * | 2001-02-24 | 2009-11-12 | 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 | 크산틴 유도체를 포함하는 약제학적 조성물 및 이의제조방법 |
| 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 |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| KR101452915B1 (ko) | 2006-05-04 | 2014-10-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 다형태 |
| CA2654230C (en) | 2006-06-12 | 2012-09-11 | Novartis Ag | Process for making a lactate salt of n-hydroxy-3-[4-[[[2-(2-methyl-1h-indol-3-yl)ethyl]amino]methyl]phenyl]-2e-2-propenamide |
| 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 |
| WO2009070311A2 (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 |
| US20100105743A1 (en) * | 2008-08-01 | 2010-04-29 | Gopal Krishna | Pharmaceutical compositions and methods for stabilizing the same |
| PL2320740T3 (pl) * | 2008-08-01 | 2014-09-30 | The Medicines Co | Kompozycje farmaceutyczne klewidypiny oraz sposoby ich wytwarzania z niskim stężeniem zanieczyszczeń |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| CA2736421A1 (en) | 2008-09-10 | 2010-03-18 | Boehringer Ingelheim International Gmbh | Combination therapy for the treatment of diabetes and related conditions |
| 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 |
| JP2012512848A (ja) | 2008-12-23 | 2012-06-07 | 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 | 有機化合物の塩の形態 |
| TW201036975A (en) | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| KR20240090632A (ko) | 2009-11-27 | 2024-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 dpp-iv 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| WO2011121452A2 (en) * | 2010-03-29 | 2011-10-06 | Pliva Hrvatska D.O.O. | Crystal forms of o-desmethylvenlafaxine fumarate |
| CA3070513C (en) | 2010-05-05 | 2023-01-03 | Boehringer Ingelheim International Gmbh | A dpp-4 inhibitor for use in treatment of skin-alterations or necrosis |
| KR20130093012A (ko) | 2010-06-24 | 2013-08-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| DK2731947T3 (en) | 2011-07-15 | 2019-04-23 | Boehringer Ingelheim Int | SUBSTITUTED DIMERIC QUINAZOLINE DERIVATIVE, PREPARATION AND USE thereof IN PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF TYPE I AND TYPE II DIABETES |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| WO2013171167A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
| WO2013171166A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp-4 inhibitor for use in the treatment of sirs and/or sepsis |
| 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 |
| EP4233840A3 (en) | 2016-06-10 | 2023-10-18 | Boehringer Ingelheim International GmbH | Combinations of linagliptin and metformin |
| EP4524132A4 (en) * | 2022-05-10 | 2026-04-22 | Myrodia Therapeutics Co Ltd | 2-METHYL-2-THIAZOLINE SALT |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8403866D0 (en) | 1984-02-14 | 1984-03-21 | Recordati Chem Pharm | Diphenylalkylaminoalkyl esters |
| US5696139A (en) | 1995-05-12 | 1997-12-09 | Recordati S.A., Chemical And Pharmaceutical Company | Use of S-enantiomers of 1,4-dihydropyridine derivatives for treating heart failure |
| IT1275532B (it) * | 1995-07-14 | 1997-08-07 | Recordati Chem Pharm | Uso di derivati 1,4-diidropiridinici per la prevenzione e la terapia della degenerazione aterosclerotica della parete arteriosa |
| US5767136A (en) | 1995-05-12 | 1998-06-16 | Recordati, S.A. Chemical And Pharmaceutical Company | 1,4-Dihydropyridines useful for prevention or reduction of atherosclerotic lesions on arterial walls |
| IT1301759B1 (it) * | 1998-06-19 | 2000-07-07 | Nicox Sa | Sali nitrati di farmaci antiipertensivi |
| US20030069285A1 (en) | 2001-08-06 | 2003-04-10 | Recordati Ireland Limited | Novel solvate and crystalline forms of lercanidipine hydrochloride |
| 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 |
| JP2006504800A (ja) * | 2002-10-16 | 2006-02-09 | レコーダチ アイルランド リミテッド | リシノプリル/レルカニジピンの組み合わせ治療 |
| 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 CA CA002575078A patent/CA2575078A1/en not_active Abandoned
- 2005-08-22 AU AU2005276619A patent/AU2005276619B2/en not_active Ceased
- 2005-08-22 WO PCT/EP2005/009043 patent/WO2006021397A1/en not_active Ceased
- 2005-08-22 NZ NZ553127A patent/NZ553127A/xx not_active IP Right Cessation
- 2005-08-22 CN CNA2005800284676A patent/CN101048379A/zh active Pending
- 2005-08-22 JP JP2007528715A patent/JP2008510754A/ja not_active Abandoned
- 2005-08-22 PE PE2005000963A patent/PE20060629A1/es not_active Application Discontinuation
- 2005-08-22 AR ARP050103516A patent/AR050467A1/es not_active Application Discontinuation
- 2005-08-22 EA EA200700492A patent/EA011773B1/ru not_active IP Right Cessation
- 2005-08-22 ES ES05776228.8T patent/ES2462921T3/es not_active Expired - Lifetime
- 2005-08-22 MX MX2007002141A patent/MX2007002141A/es not_active Application Discontinuation
- 2005-08-22 EP EP05776228.8A patent/EP1799644B1/en not_active Expired - Lifetime
- 2005-08-22 BR BRPI0514606-2A patent/BRPI0514606A/pt not_active IP Right Cessation
- 2005-08-22 KR KR1020077006715A patent/KR20070045351A/ko not_active Withdrawn
- 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
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