RU2006122472A - Амлодипина гентизат и способ его получения - Google Patents
Амлодипина гентизат и способ его полученияInfo
- Publication number
- RU2006122472A RU2006122472A RU2006122472/04A RU2006122472A RU2006122472A RU 2006122472 A RU2006122472 A RU 2006122472A RU 2006122472/04 A RU2006122472/04 A RU 2006122472/04A RU 2006122472 A RU2006122472 A RU 2006122472A RU 2006122472 A RU2006122472 A RU 2006122472A
- Authority
- RU
- Russia
- Prior art keywords
- amlodipine
- formula
- specified
- gentisate
- amlodipine gentisate
- 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 13
- 229960000528 amlodipine Drugs 0.000 title claims abstract 13
- 238000004519 manufacturing process Methods 0.000 title 1
- WXTMDXOMEHJXQO-UHFFFAOYSA-N 2,5-dihydroxybenzoic acid Chemical compound OC(=O)C1=CC(O)=CC=C1O WXTMDXOMEHJXQO-UHFFFAOYSA-N 0.000 claims abstract description 23
- 229940114119 gentisate Drugs 0.000 claims abstract 8
- 238000000034 method Methods 0.000 claims abstract 7
- 229960005219 gentisic acid Drugs 0.000 claims abstract 3
- 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- 230000003993 interaction Effects 0.000 claims 2
- 239000011541 reaction mixture Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000008280 blood Substances 0.000 abstract 1
- 210000004369 blood Anatomy 0.000 abstract 1
- 230000005923 long-lasting effect Effects 0.000 abstract 1
- 231100000053 low toxicity Toxicity 0.000 abstract 1
- 0 CCOC(C1=C(COCCN)NC(C)=C(*)C1c1ccccc1Cl)=O Chemical compound CCOC(C1=C(COCCN)NC(C)=C(*)C1c1ccccc1Cl)=O 0.000 description 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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
-
- 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
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Claims (11)
1. Амлодипина гентизат формулы 1
2. Амлодипина гентизат по п.1, где указанное соединение представляет собой (S)-(-)-изомер.
3. Способ получения амлодипина гентизата формулы 1, включающий взаимодействие амлодипина формулы 2 с гентизиновой кислотой формулы 3
4. Способ по п.3, где амлодипин содержится в указанной реакционной смеси в диапазоне концентраций от примерно 3 до примерно 60 мас.%.
5. Способ по п.3, где гентизиновую кислоту используют в количественном диапазоне от примерно 0,1 до примерно 5,0 эквивалентов относительно количества амлодипина.
6. Способ по п.3, где указанное взаимодействие проводят в диапазоне температур от примерно -10 до примерно 60°С.
7. Способ по п.3, где растворитель в указанной реакционной смеси представлет собой по меньшей мере один растворитель, выбранный из группы, состоящей из воды, метанола, этанола, изопропанола и ацетонитрила, или их смесь.
8. Способ по п.3, где указанный амлодипина гентизат формулы 1 представляет собой (S)-(-)-изомер
9. Фармацевтическая композиция для лечения сердечно-сосудистых заболеваний, где в качестве активного ингредиента использован амлодипина гентизат формулы 1
10. Фармацевтическая композиция по п.9, где указанный амлодипина гентизат формулы 1 представляет собой (S)-(-)-изомер
11. Фармацевтическая композиция по п.9 или 10, которая изготовлена в форме таблеток, капсул или растворов для инъекций.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20030092001 | 2003-12-16 | ||
| KR10-2003-0092001 | 2003-12-16 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2006122472A true RU2006122472A (ru) | 2008-01-27 |
| RU2330843C2 RU2330843C2 (ru) | 2008-08-10 |
Family
ID=36660050
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2006122472/04A RU2330843C2 (ru) | 2003-12-16 | 2004-12-15 | Амлодипина гентизат и способ его получения |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US7442714B2 (ru) |
| EP (1) | EP1694645B1 (ru) |
| JP (1) | JP4740875B2 (ru) |
| KR (1) | KR100841409B1 (ru) |
| CN (1) | CN100591669C (ru) |
| AT (1) | ATE491686T1 (ru) |
| AU (1) | AU2004299412B2 (ru) |
| BR (1) | BRPI0417179A (ru) |
| CA (1) | CA2549832C (ru) |
| DE (1) | DE602004030616D1 (ru) |
| ES (1) | ES2357433T3 (ru) |
| MX (1) | MXPA06006922A (ru) |
| RU (1) | RU2330843C2 (ru) |
| WO (1) | WO2005058825A1 (ru) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2413717C2 (ru) * | 2008-08-08 | 2011-03-10 | Вадим Алексеевич Козловский | Антигипертензивная органическая соль |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101235116B1 (ko) * | 2005-10-17 | 2013-02-20 | 에스케이케미칼주식회사 | 광학활성 암로디핀 겐티세이트 염의 제조방법 |
| JP2008013489A (ja) * | 2006-07-06 | 2008-01-24 | Ohara Yakuhin Kogyo Kk | ベシル酸アムロジピン含有錠剤 |
| 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 |
| MX2020003730A (es) * | 2017-10-09 | 2020-08-03 | Teva Pharma | Nueva sal y formas en estado solido de escitalopram. |
| KR102178355B1 (ko) * | 2018-10-19 | 2020-11-11 | 전남대학교산학협력단 | 심장 질환 치료용 조성물 |
| CN110372575A (zh) * | 2019-07-10 | 2019-10-25 | 复旦大学 | 一种二氢吡啶钙拮抗剂共晶体及其制备方法和应用 |
| CN117024292B (zh) * | 2023-08-08 | 2024-09-24 | 深圳杉海创新技术有限公司 | 一种龙胆酸离子盐、其制备方法及日化产品或食品或药品 |
Family Cites Families (9)
| 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 |
| KR950007228B1 (ko) | 1987-08-05 | 1995-07-07 | 화이자 인코포레이티드 | 암로디핀의 베실레이트염 |
| AP1057A (en) * | 1997-10-10 | 2002-04-08 | Aventis Pharmaceuticals Products Inc | Process for the preparation of azacycloalkylalkanoyl pseudotetrapeptides. |
| UA33033A (ru) * | 1998-10-16 | 2001-02-15 | Др.Редіс Леборетрис Лтд | Способ получения бензилата амлодипина |
| US20020045613A1 (en) * | 2000-04-27 | 2002-04-18 | Heinz Pauls | 1-aroyl-piperidinyl benzamidines |
| KR100452491B1 (ko) * | 2001-03-29 | 2004-10-12 | 한미약품 주식회사 | 신규한 결정형 암로디핀 캠실레이트 염 및 그의 제조방법 |
| EP1499592A4 (en) * | 2002-04-13 | 2010-01-13 | Hanlim Pharmaceutical Co Ltd | AMLODIPINNICOTINATE AND METHOD FOR THE PRODUCTION THEREOF |
| KR100517383B1 (ko) | 2003-05-23 | 2005-09-26 | 동아제약주식회사 | 신규한 암로디핀 젠티세이트 염, 그의 제조방법 및 그의 약제학적 조성물 |
-
2004
- 2004-12-13 KR KR1020040105083A patent/KR100841409B1/ko not_active Expired - Fee Related
- 2004-12-15 MX MXPA06006922A patent/MXPA06006922A/es active IP Right Grant
- 2004-12-15 BR BRPI0417179-9A patent/BRPI0417179A/pt not_active IP Right Cessation
- 2004-12-15 AU AU2004299412A patent/AU2004299412B2/en not_active Ceased
- 2004-12-15 RU RU2006122472/04A patent/RU2330843C2/ru not_active IP Right Cessation
- 2004-12-15 JP JP2006545234A patent/JP4740875B2/ja not_active Expired - Fee Related
- 2004-12-15 WO PCT/KR2004/003309 patent/WO2005058825A1/en not_active Ceased
- 2004-12-15 CN CN200480041687A patent/CN100591669C/zh not_active Expired - Fee Related
- 2004-12-15 EP EP04808440A patent/EP1694645B1/en not_active Expired - Lifetime
- 2004-12-15 AT AT04808440T patent/ATE491686T1/de not_active IP Right Cessation
- 2004-12-15 CA CA2549832A patent/CA2549832C/en not_active Expired - Fee Related
- 2004-12-15 ES ES04808440T patent/ES2357433T3/es not_active Expired - Lifetime
- 2004-12-15 US US10/583,438 patent/US7442714B2/en not_active Expired - Fee Related
- 2004-12-15 DE DE602004030616T patent/DE602004030616D1/de not_active Expired - Lifetime
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2413717C2 (ru) * | 2008-08-08 | 2011-03-10 | Вадим Алексеевич Козловский | Антигипертензивная органическая соль |
Also Published As
| Publication number | Publication date |
|---|---|
| MXPA06006922A (es) | 2006-08-23 |
| EP1694645A1 (en) | 2006-08-30 |
| CN1956956A (zh) | 2007-05-02 |
| KR20050061317A (ko) | 2005-06-22 |
| KR100841409B1 (ko) | 2008-06-25 |
| CA2549832A1 (en) | 2005-06-30 |
| RU2330843C2 (ru) | 2008-08-10 |
| AU2004299412A1 (en) | 2005-06-30 |
| ATE491686T1 (de) | 2011-01-15 |
| ES2357433T3 (es) | 2011-04-26 |
| JP2007513997A (ja) | 2007-05-31 |
| BRPI0417179A (pt) | 2007-03-06 |
| CA2549832C (en) | 2010-10-05 |
| US7442714B2 (en) | 2008-10-28 |
| EP1694645A4 (en) | 2009-03-04 |
| CN100591669C (zh) | 2010-02-24 |
| AU2004299412B2 (en) | 2011-08-18 |
| JP4740875B2 (ja) | 2011-08-03 |
| US20070135495A1 (en) | 2007-06-14 |
| DE602004030616D1 (de) | 2011-01-27 |
| WO2005058825A1 (en) | 2005-06-30 |
| EP1694645B1 (en) | 2010-12-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20131216 |