WO2002053535A3 - Process for making amlodipine, derivatives thereof, and precursors therefor - Google Patents
Process for making amlodipine, derivatives thereof, and precursors therefor Download PDFInfo
- Publication number
- WO2002053535A3 WO2002053535A3 PCT/NL2001/000601 NL0100601W WO02053535A3 WO 2002053535 A3 WO2002053535 A3 WO 2002053535A3 NL 0100601 W NL0100601 W NL 0100601W WO 02053535 A3 WO02053535 A3 WO 02053535A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- amlodipine
- derivatives
- precursors therefor
- purity
- compounds
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
- C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Inorganic Chemistry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicinal Preparation (AREA)
- Inks, Pencil-Leads, Or Crayons (AREA)
Abstract
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP01974983A EP1345901A2 (en) | 2000-12-29 | 2001-08-15 | Process for making amlodipine, derivatives thereof, and precursors therefor |
AU2001294354A AU2001294354A1 (en) | 2000-12-29 | 2001-08-15 | Process for making amlodipine, derivatives thereof, and precursors therefor |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US25861300P | 2000-12-29 | 2000-12-29 | |
US60/258,613 | 2000-12-29 | ||
US80935101A | 2001-03-16 | 2001-03-16 | |
US09/809,351 | 2001-03-16 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2002053535A2 WO2002053535A2 (en) | 2002-07-11 |
WO2002053535A3 true WO2002053535A3 (en) | 2003-01-23 |
Family
ID=26946752
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/NL2001/000601 WO2002053535A2 (en) | 2000-12-29 | 2001-08-15 | Process for making amlodipine, derivatives thereof, and precursors therefor |
PCT/NL2001/000947 WO2002053135A1 (en) | 2000-12-29 | 2001-12-31 | Amlodipine free base |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/NL2001/000947 WO2002053135A1 (en) | 2000-12-29 | 2001-12-31 | Amlodipine free base |
Country Status (9)
Country | Link |
---|---|
EP (1) | EP1345901A2 (en) |
AU (1) | AU2001294354A1 (en) |
BR (1) | BR0116558A (en) |
CA (1) | CA2433366C (en) |
CZ (1) | CZ20031779A3 (en) |
DE (2) | DE20116723U1 (en) |
ES (1) | ES2277960T3 (en) |
MX (1) | MXPA03005888A (en) |
WO (2) | WO2002053535A2 (en) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BE1014450A6 (en) * | 2000-12-29 | 2003-10-07 | Bioorg Bv | New alkyl 2-(2-chlorobenzylidene)-4-(2-phthalimidoethoxy)-acetoacetates, useful as intermediates for the antianginal and antihypertensive agent amlodipine |
WO2002054062A2 (en) | 2000-12-29 | 2002-07-11 | Pfizer Limited | Reference standards and processes for determining the purity or stability of amlodipine maleate |
US6828339B2 (en) * | 2001-11-21 | 2004-12-07 | Synthon Bv | Amlodipine salt forms and processes for preparing them |
NL1019882C2 (en) * | 2002-02-01 | 2003-08-04 | Synthon Licensing | Pharmaceutical tablet composition useful for treating or preventing hypertension, angina or congestive heart failure comprises amlodipine free base |
ES2211317B1 (en) * | 2002-11-18 | 2005-10-16 | Finaf 92, S.A. | INTERMEDIATE COMPOUNDS FOR OBTAINING ANTIHIPERTENSIVE ACTIVE PRINCIPLES AND CORRESPONDING PROCEDURES. |
ES2500292T3 (en) * | 2003-01-27 | 2014-09-30 | Hanmi Science Co., Ltd. | Amorphous amlodipine camsilate, stable, repair procedure and composition for oral administration |
WO2004075825A2 (en) * | 2003-02-28 | 2004-09-10 | Ranbaxy Laboratories Limited | Dosage forms of amlodipine and processes for their preparation |
CH697952B1 (en) * | 2003-07-25 | 2009-03-31 | Siegfried Generics Int Ag | A process for purification of free amlodipine base. |
WO2005023769A1 (en) * | 2003-09-04 | 2005-03-17 | Cipla Limited | Process for the preparation of amlodipine salts |
KR100604034B1 (en) * | 2003-10-08 | 2006-07-24 | 주식회사유한양행 | A composition of fast dissolving tablets containing amlodipine free base |
WO2007131759A1 (en) * | 2006-05-15 | 2007-11-22 | Lek Pharmaceuticals D.D. | A process for the preparation of amlodipine benzenesulfonate |
EP1975167A1 (en) | 2007-03-30 | 2008-10-01 | Esteve Quimica, S.A. | Acetone solvate of phthaloyl amlodipine |
WO2011117876A1 (en) | 2010-03-26 | 2011-09-29 | Fdc Limited | An improved process for the preparation of amlodipine free base and acid addition salts thereof |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0089167A2 (en) * | 1982-03-11 | 1983-09-21 | Pfizer Limited | Dihydropyridine anti-ischaemic and antihypertensive agents, processes for their production, and pharmaceutical compositions containing them |
DE3544211A1 (en) * | 1985-12-13 | 1987-06-19 | Bayer Ag | NEW, FLUORINE 1,4-DIHYDROPYRIDINE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS |
DE4305454A1 (en) * | 1993-02-23 | 1994-08-25 | Bayer Ag | Padding process with a phthalocyanine mixture |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PL140069B1 (en) | 1982-12-21 | 1987-03-31 | Pfizer | Method of obtaining new derivatives of dihydropiridine |
GB9317773D0 (en) * | 1993-08-26 | 1993-10-13 | Pfizer Ltd | Therapeutic compound |
GB0008332D0 (en) * | 2000-04-04 | 2000-05-24 | Pfizer Ltd | Treament |
GB0020842D0 (en) * | 2000-08-23 | 2000-10-11 | Pfizer Ltd | Therapeutic compositions |
-
2001
- 2001-08-15 EP EP01974983A patent/EP1345901A2/en not_active Withdrawn
- 2001-08-15 CZ CZ20031779A patent/CZ20031779A3/en unknown
- 2001-08-15 WO PCT/NL2001/000601 patent/WO2002053535A2/en not_active Application Discontinuation
- 2001-08-15 AU AU2001294354A patent/AU2001294354A1/en not_active Abandoned
- 2001-10-04 DE DE20116723U patent/DE20116723U1/en not_active Ceased
- 2001-12-31 ES ES01995820T patent/ES2277960T3/en not_active Expired - Lifetime
- 2001-12-31 DE DE60125981T patent/DE60125981T2/en not_active Expired - Fee Related
- 2001-12-31 BR BR0116558-5A patent/BR0116558A/en not_active Application Discontinuation
- 2001-12-31 WO PCT/NL2001/000947 patent/WO2002053135A1/en active IP Right Grant
- 2001-12-31 MX MXPA03005888A patent/MXPA03005888A/en active IP Right Grant
- 2001-12-31 CA CA002433366A patent/CA2433366C/en not_active Expired - Fee Related
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0089167A2 (en) * | 1982-03-11 | 1983-09-21 | Pfizer Limited | Dihydropyridine anti-ischaemic and antihypertensive agents, processes for their production, and pharmaceutical compositions containing them |
DE3544211A1 (en) * | 1985-12-13 | 1987-06-19 | Bayer Ag | NEW, FLUORINE 1,4-DIHYDROPYRIDINE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS |
DE4305454A1 (en) * | 1993-02-23 | 1994-08-25 | Bayer Ag | Padding process with a phthalocyanine mixture |
Non-Patent Citations (3)
Title |
---|
ARROWSMITH J E ET AL: "LONG-ACTING DIHYDROPYRIDINE CALCIUM ANTAGONISTS. 1. 2-ALKOXYMETHYL DERIVATIVES INCORPORATING BASIC SUBSTITUENTS", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 29, no. 9, 1986, pages 1696 - 1702, XP002070765, ISSN: 0022-2623 * |
See also references of EP1345901A2 * |
SZIKSZAY, ZOLTAN ET AL: "Quantitative purity test for phthaloyl-amlodipine by personal OPLC", J. PLANAR CHROMATOGR.--MOD. TLC (1998), 11(6), 428-432, XP008007919 * |
Also Published As
Publication number | Publication date |
---|---|
BR0116558A (en) | 2003-10-28 |
DE60125981D1 (en) | 2007-02-22 |
WO2002053535A2 (en) | 2002-07-11 |
MXPA03005888A (en) | 2005-04-19 |
AU2001294354A1 (en) | 2002-07-16 |
CZ20031779A3 (en) | 2004-10-13 |
AU2001294354A8 (en) | 2005-10-06 |
CA2433366C (en) | 2006-01-24 |
DE20116723U1 (en) | 2002-01-17 |
ES2277960T3 (en) | 2007-08-01 |
EP1345901A2 (en) | 2003-09-24 |
CA2433366A1 (en) | 2002-07-11 |
DE60125981T2 (en) | 2007-10-18 |
WO2002053135A1 (en) | 2002-07-11 |
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