RU2003131687A - Камзилат амлодипина, способ его получения и фармацевтическая композиция на его основе - Google Patents
Камзилат амлодипина, способ его получения и фармацевтическая композиция на его основе Download PDFInfo
- Publication number
- RU2003131687A RU2003131687A RU2003131687/04A RU2003131687A RU2003131687A RU 2003131687 A RU2003131687 A RU 2003131687A RU 2003131687/04 A RU2003131687/04 A RU 2003131687/04A RU 2003131687 A RU2003131687 A RU 2003131687A RU 2003131687 A RU2003131687 A RU 2003131687A
- Authority
- RU
- Russia
- Prior art keywords
- amlodipine
- camphorsulfonic acid
- formula
- pharmaceutical composition
- organic solvent
- Prior art date
Links
- HTIQEAQVCYTUBX-UHFFFAOYSA-N amlodipine Chemical compound CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1Cl HTIQEAQVCYTUBX-UHFFFAOYSA-N 0.000 title claims abstract 6
- 229960000528 amlodipine Drugs 0.000 title claims abstract 6
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract 3
- 238000000034 method Methods 0.000 title claims 7
- MIOPJNTWMNEORI-GMSGAONNSA-N (S)-camphorsulfonic acid Chemical compound C1C[C@@]2(CS(O)(=O)=O)C(=O)C[C@@H]1C2(C)C MIOPJNTWMNEORI-GMSGAONNSA-N 0.000 claims abstract 6
- UXKMFEPPKJZDAR-STOWLHSFSA-N [(1r,4s)-7,7-dimethyl-3-oxo-4-bicyclo[2.2.1]heptanyl]methanesulfonic acid;3-o-ethyl 5-o-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate Chemical compound C1C[C@@]2(CS(O)(=O)=O)C(=O)C[C@@H]1C2(C)C.CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1Cl UXKMFEPPKJZDAR-STOWLHSFSA-N 0.000 claims abstract 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims abstract 2
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 239000003960 organic solvent Substances 0.000 claims 3
- 239000007787 solid Substances 0.000 claims 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- MIOPJNTWMNEORI-XVKPBYJWSA-N (R)-camphorsulfonic acid Chemical compound C1C[C@]2(CS(O)(=O)=O)C(=O)C[C@H]1C2(C)C MIOPJNTWMNEORI-XVKPBYJWSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 238000004090 dissolution Methods 0.000 claims 1
- 238000001035 drying Methods 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 238000005406 washing Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 231100000331 toxic Toxicity 0.000 abstract 1
- 230000002588 toxic effect Effects 0.000 abstract 1
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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Heart & Thoracic Surgery (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Medicinal Preparation (AREA)
- Saccharide Compounds (AREA)
Claims (8)
1. Камзилат амлодипина, имеющий структуру формулы (1)
2. Способ получения камзилата амлодипина по п.1, который включает следующие стадии:
1) растворение амлодипина формулы (2) в органическом растворителе;
2) добавление раствора камфорсульфокислоты в органическом растворителе к раствору амлодипина и перемешивание смеси в течение промежутка времени, достаточного для образования твердого вещества;
3) фильтрование, промывание и сушка твердого вещества
3. Способ по п.2, в котором камфорсульфокислоту выбирают из группы, включающей (1S)-(+)-10-камфорсульфокислоту формулы (3), (1R)-(-)-10-камфорсульфокислоту формулы (4) и рацемическую 10-камфорсульфокислоту
4. Способ по п.2, в котором концентрация амлодипина в смеси, используемой на стадии 2), составляет от 3 до 60 мас.%.
5. Способ по п.2, в котором камфорсульфокислоту используют в количестве от 0,1 до 5,0 эквивалентов в расчете на количество амлодипина.
6. Способ по п.2, в котором органический растворитель, использованный на стадии 1) или 2), выбирают из группы, включающей метанол, этанол, изопропанол и ацетонитрил.
7. Способ по п.2, в котором твердое вещество образуется при температуре от –10 до 50°С.
8. Фармацевтическая композиция для лечения сердечно-сосудистых заболеваний, включающая камзилат амлодипина по п.1 в качестве активнодействующего ингредиента.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR2001/16514 | 2001-03-29 | ||
| KR10-2001-0016514A KR100452491B1 (ko) | 2001-03-29 | 2001-03-29 | 신규한 결정형 암로디핀 캠실레이트 염 및 그의 제조방법 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2241701C1 RU2241701C1 (ru) | 2004-12-10 |
| RU2003131687A true RU2003131687A (ru) | 2005-02-27 |
Family
ID=36792806
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2003131687/04A RU2241701C1 (ru) | 2001-03-29 | 2002-03-28 | Камзилат амлодипина, способ его получения и фармацевтическая композиция на его основе |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US6936625B2 (ru) |
| EP (1) | EP1373207B1 (ru) |
| JP (1) | JP4188088B2 (ru) |
| KR (1) | KR100452491B1 (ru) |
| CN (1) | CN1238342C (ru) |
| AT (1) | ATE498612T1 (ru) |
| AU (1) | AU2002243069B2 (ru) |
| BR (1) | BRPI0208468B8 (ru) |
| CA (1) | CA2441613C (ru) |
| CZ (1) | CZ304489B6 (ru) |
| DE (1) | DE60239193D1 (ru) |
| DK (1) | DK1373207T3 (ru) |
| ES (1) | ES2360787T3 (ru) |
| HK (1) | HK1066545A1 (ru) |
| HU (1) | HU227919B1 (ru) |
| IL (2) | IL158082A0 (ru) |
| MX (1) | MXPA03008675A (ru) |
| NZ (1) | NZ528362A (ru) |
| PL (1) | PL207535B1 (ru) |
| PT (1) | PT1373207E (ru) |
| RU (1) | RU2241701C1 (ru) |
| WO (1) | WO2002079158A1 (ru) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070135488A1 (en) * | 2002-04-13 | 2007-06-14 | Chung You S | Amlodipine nicotinate and process for the preparation thereof |
| KR100462304B1 (ko) * | 2002-07-30 | 2004-12-17 | 씨제이 주식회사 | 암로디핀의 유기산염 |
| KR100496436B1 (ko) * | 2002-07-30 | 2005-06-20 | 씨제이 주식회사 | 암로디핀의 유기산염 |
| KR20040011751A (ko) * | 2002-07-30 | 2004-02-11 | 씨제이 주식회사 | 암로디핀의 유기산염 |
| KR100538641B1 (ko) * | 2002-07-30 | 2005-12-22 | 씨제이 주식회사 | 암로디핀의 유기산염 |
| KR100558505B1 (ko) * | 2003-01-27 | 2006-03-07 | 한미약품 주식회사 | 안정한 무정형 암로디핀 캠실레이트, 이의 제조방법 및이를 포함하는 경구투여용 조성물 |
| WO2005042485A1 (en) * | 2003-10-30 | 2005-05-12 | Sk Chemicals, Co., Ltd. | Acid added salts of amlodipine |
| KR100841409B1 (ko) | 2003-12-16 | 2008-06-25 | 에스케이케미칼주식회사 | 암로디핀 겐티세이트 염과 이의 제조방법 |
| KR100632470B1 (ko) * | 2005-02-25 | 2006-10-12 | 민연식 | 결정성 시부트라민 캄실레이트염과 이의 제조방법 |
| KR100913791B1 (ko) * | 2006-07-21 | 2009-08-26 | 한미약품 주식회사 | (ｓ)-(-)-암로디핀 캠실레이트 또는 이의 수화물 및 이를함유하는 약학적 조성물 |
| KR100830003B1 (ko) | 2006-10-31 | 2008-05-15 | 씨제이제일제당 (주) | 결정성 ｓ-(-)-암로디핀 아디핀산 염 무수물 및 이의 제조방법 |
| KR100843401B1 (ko) * | 2006-12-04 | 2008-07-04 | 씨제이제일제당 (주) | 결정성 ｓ-(-)-암로디핀 캠실레이트 무수물 및 이의제조방법 |
| KR100840069B1 (ko) * | 2007-01-23 | 2008-06-20 | 씨제이제일제당 (주) | 결정성 ｓ-(-)-암로디핀 오로테이트 무수물 및 이의제조방법 |
| KR100799821B1 (ko) * | 2007-02-05 | 2008-01-31 | 동화약품공업주식회사 | 신규한 이마티닙 캠실레이트 및 그의 제조방법 |
| US9161933B2 (en) * | 2009-01-23 | 2015-10-20 | Hanmi Science Co., Ltd | Solid pharmaceutical composition comprising amlodipine and losartan and process for producing same |
| US8754072B2 (en) | 2010-02-12 | 2014-06-17 | Pfizer Inc. | Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one |
| US8415483B2 (en) | 2010-12-22 | 2013-04-09 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
| CN102266333B (zh) * | 2011-08-19 | 2012-08-29 | 海南锦瑞制药股份有限公司 | 一种含有左旋氨氯地平和阿托伐他汀钙的全新药用组合物及其制备方法 |
| US9650336B2 (en) | 2011-10-10 | 2017-05-16 | Astrazeneca Ab | Mono-fluoro beta-secretase inhibitors |
| US10548882B2 (en) * | 2012-06-21 | 2020-02-04 | Astrazeneca Ab | Camsylate salt |
| KR101910901B1 (ko) | 2013-11-29 | 2018-10-24 | 한미약품 주식회사 | 암로디핀, 로자탄 및 로수바스타틴을 포함하는 약제학적 복합 제제 |
| KR101914930B1 (ko) | 2015-03-31 | 2018-11-05 | 한미약품 주식회사 | 암로디핀, 로자탄 및 클로르탈리돈을 포함하는 약제학적 복합 제제 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK161312C (da) * | 1982-03-11 | 1991-12-09 | Pfizer | Analogifremgangsmaade til fremstilling af 2-aminoalkoxymethyl-4-phenyl-6-methyl-1,4-dihydropyridin-3,5-dicarboxylsyreestere eller syreadditionssalte deraf samt phthalimidoderivater til anvendelse som udgangsmateriale ved fremgangsmaaden |
| GB8608335D0 (en) * | 1986-04-04 | 1986-05-08 | Pfizer Ltd | Pharmaceutically acceptable salts |
| US6057344A (en) * | 1991-11-26 | 2000-05-02 | Sepracor, Inc. | Methods for treating hypertension, and angina using optically pure (-) amlodipine |
| KR100188391B1 (ko) | 1993-08-27 | 1999-06-01 | 류정열 | 전기자동차의 충전중 표시 장치 |
| KR100374405B1 (ko) * | 2000-06-21 | 2003-03-04 | 한국유나이티드제약 주식회사 | 암로디핀 베실레이트의 제조방법 |
| EP1309556B1 (en) * | 2000-12-29 | 2004-11-24 | Pfizer Limited | Amlodipine fumarate |
-
2001
- 2001-03-29 KR KR10-2001-0016514A patent/KR100452491B1/ko active IP Right Grant
-
2002
- 2002-03-28 EP EP02708811A patent/EP1373207B1/en not_active Expired - Lifetime
- 2002-03-28 CZ CZ2003-2583A patent/CZ304489B6/cs not_active IP Right Cessation
- 2002-03-28 NZ NZ528362A patent/NZ528362A/en not_active IP Right Cessation
- 2002-03-28 AU AU2002243069A patent/AU2002243069B2/en not_active Expired
- 2002-03-28 AT AT02708811T patent/ATE498612T1/de active
- 2002-03-28 RU RU2003131687/04A patent/RU2241701C1/ru active
- 2002-03-28 WO PCT/KR2002/000543 patent/WO2002079158A1/en active IP Right Grant
- 2002-03-28 PL PL362667A patent/PL207535B1/pl unknown
- 2002-03-28 IL IL15808202A patent/IL158082A0/xx unknown
- 2002-03-28 MX MXPA03008675A patent/MXPA03008675A/es active IP Right Grant
- 2002-03-28 ES ES02708811T patent/ES2360787T3/es not_active Expired - Lifetime
- 2002-03-28 HU HU0303639A patent/HU227919B1/hu unknown
- 2002-03-28 CA CA002441613A patent/CA2441613C/en not_active Expired - Lifetime
- 2002-03-28 US US10/473,479 patent/US6936625B2/en not_active Expired - Lifetime
- 2002-03-28 DE DE60239193T patent/DE60239193D1/de not_active Expired - Lifetime
- 2002-03-28 PT PT02708811T patent/PT1373207E/pt unknown
- 2002-03-28 BR BRPI0208468A patent/BRPI0208468B8/pt not_active IP Right Cessation
- 2002-03-28 CN CNB028074432A patent/CN1238342C/zh not_active Expired - Lifetime
- 2002-03-28 DK DK02708811.1T patent/DK1373207T3/da active
- 2002-03-28 JP JP2002577785A patent/JP4188088B2/ja not_active Expired - Lifetime
-
2003
- 2003-09-24 IL IL158082A patent/IL158082A/en unknown
-
2004
- 2004-12-01 HK HK04109527A patent/HK1066545A1/xx not_active IP Right Cessation
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