CA2433366A1 - Amlodipine free base - Google Patents

Amlodipine free base Download PDF

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Publication number
CA2433366A1
CA2433366A1 CA002433366A CA2433366A CA2433366A1 CA 2433366 A1 CA2433366 A1 CA 2433366A1 CA 002433366 A CA002433366 A CA 002433366A CA 2433366 A CA2433366 A CA 2433366A CA 2433366 A1 CA2433366 A1 CA 2433366A1
Authority
CA
Canada
Prior art keywords
free base
amlodipine free
amlodipine
tablet
formulated
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.)
Granted
Application number
CA002433366A
Other languages
French (fr)
Other versions
CA2433366C (en
Inventor
Theodorus Hendricus Antonius Peters
Franciscus Bernardus Gemma Benneker
Jacobus Maria Lemmens
Rolf Keltjens
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.)
Pfizer Ltd
Original Assignee
Individual
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=CA2433366(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Individual filed Critical Individual
Publication of CA2433366A1 publication Critical patent/CA2433366A1/en
Application granted granted Critical
Publication of CA2433366C publication Critical patent/CA2433366C/en
Anticipated expiration legal-status Critical
Expired - Fee Related 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)
  • Inks, Pencil-Leads, Or Crayons (AREA)
  • Medicinal Preparation (AREA)

Abstract

Amlodipine free base can be formulated into a convenient oral dosage form, especially a tablet, without excessive stickiness or tablet punch residue. The amlodipine free base can be crystalline Form I or a novel Form II. Methods of making and using the amlodipine free base are set forth.
CA002433366A 2000-12-29 2001-12-31 Amlodipine free base Expired - Fee Related CA2433366C (en)

Applications Claiming Priority (5)

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
PCT/NL2001/000947 WO2002053135A1 (en) 2000-12-29 2001-12-31 Amlodipine free base

Publications (2)

Publication Number Publication Date
CA2433366A1 true CA2433366A1 (en) 2002-07-11
CA2433366C CA2433366C (en) 2006-01-24

Family

ID=26946752

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002433366A Expired - Fee Related CA2433366C (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
GB2371862B (en) 2000-12-29 2004-07-14 Bioorg Bv Reference standards for determining the purity or stability of amlodipine maleate and processes therefor
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
AR037565A1 (en) * 2001-11-21 2004-11-17 Synthon Bv FORMS OF AMLODIPINE SALTS AND PROCEDURES TO PREPARE 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

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK161312C (en) * 1982-03-11 1991-12-09 Pfizer CHANGES FOR THE PREPARATION FOR THE PREPARATION OF 2-Amino-CO-Methyl-4-Methyl-4-Methyl-4-Methyl-4-Methyl-4-Methyl-4-Methyl-2-D-Hydroxy
US4572908A (en) 1982-12-21 1986-02-25 Pfizer Inc. Dihydropyridines
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
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

Also Published As

Publication number Publication date
WO2002053535A2 (en) 2002-07-11
WO2002053535A3 (en) 2003-01-23
WO2002053135A1 (en) 2002-07-11
DE60125981T2 (en) 2007-10-18
AU2001294354A8 (en) 2005-10-06
MXPA03005888A (en) 2005-04-19
DE20116723U1 (en) 2002-01-17
EP1345901A2 (en) 2003-09-24
AU2001294354A1 (en) 2002-07-16
ES2277960T3 (en) 2007-08-01
CZ20031779A3 (en) 2004-10-13
DE60125981D1 (en) 2007-02-22
BR0116558A (en) 2003-10-28
CA2433366C (en) 2006-01-24

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EEER Examination request
MKLA Lapsed

Effective date: 20191231