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WO2002053535A3 - Process for making amlodipine, derivatives thereof, and precursors therefor - Google Patents

Process for making amlodipine, derivatives thereof, and precursors therefor Download PDF

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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
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
Application number
PCT/NL2001/000601
Other languages
French (fr)
Other versions
WO2002053535A2 (en
Inventor
Theodorus Hendricus Ant Peters
Franciscus Bernardus Benneker
Pavel Slanina
Jiri Bartl
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
BIOORGANICS BV
BIOORG BV
Original Assignee
BIOORGANICS BV
BIOORG BV
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26946752&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2002053535(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by BIOORGANICS BV, BIOORG BV filed Critical BIOORGANICS BV
Priority to AU2001294354A priority Critical patent/AU2001294354A1/en
Priority to EP01974983A priority patent/EP1345901A2/en
Publication of WO2002053535A2 publication Critical patent/WO2002053535A2/en
Publication of WO2002053535A3 publication Critical patent/WO2002053535A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Inorganic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicinal Preparation (AREA)
  • Inks, Pencil-Leads, Or Crayons (AREA)

Abstract

Amlodipine and related analogues thereof are prepared by the following general reaction scheme: R1 and R2 each independently represent a C1-C4 alkyl group. The process provides for the formation of compounds of formula (1) in good yield and purity. Further, the compounds of formula (1) can be used as calcium channel blockers or as reference standards or reference markers for checking the purity of amlodipine.
PCT/NL2001/000601 2000-12-29 2001-08-15 Process for making amlodipine, derivatives thereof, and precursors therefor Ceased WO2002053535A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2001294354A AU2001294354A1 (en) 2000-12-29 2001-08-15 Process for making amlodipine, derivatives thereof, and precursors therefor
EP01974983A EP1345901A2 (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 Ceased WO2002053535A2 (en) 2000-12-29 2001-08-15 Process for making amlodipine, derivatives thereof, and precursors therefor
PCT/NL2001/000947 Ceased 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 Ceased 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)

* Cited by examiner, † Cited by third party
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
EP1346214A2 (en) 2000-12-29 2003-09-24 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.
US20060128763A1 (en) * 2003-01-27 2006-06-15 Moon Young H Stable amorphous amlodipine camsylate, process for preparing same and composition for oral administration thereof
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 Oral fast disintegrating tablet containing amlodipine free base and compositions thereof
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT77842B (en) 1982-12-21 1986-05-05 Pfizer Process for preparing dihydropyridines
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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
DE20116723U1 (en) 2002-01-17
WO2002053535A2 (en) 2002-07-11
DE60125981T2 (en) 2007-10-18
MXPA03005888A (en) 2005-04-19
EP1345901A2 (en) 2003-09-24
AU2001294354A8 (en) 2005-10-06
CA2433366C (en) 2006-01-24
CA2433366A1 (en) 2002-07-11
ES2277960T3 (en) 2007-08-01
CZ20031779A3 (en) 2004-10-13
WO2002053135A1 (en) 2002-07-11
BR0116558A (en) 2003-10-28
DE60125981D1 (en) 2007-02-22
AU2001294354A1 (en) 2002-07-16

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