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WO2018236221A3 - Esters of a bisphosphonate compound or esters of a calcium chelating compound for use to dissolve neurodegenerative peptide deposit - Google Patents

Esters of a bisphosphonate compound or esters of a calcium chelating compound for use to dissolve neurodegenerative peptide deposit Download PDF

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Publication number
WO2018236221A3
WO2018236221A3 PCT/NL2018/050409 NL2018050409W WO2018236221A3 WO 2018236221 A3 WO2018236221 A3 WO 2018236221A3 NL 2018050409 W NL2018050409 W NL 2018050409W WO 2018236221 A3 WO2018236221 A3 WO 2018236221A3
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WO
WIPO (PCT)
Prior art keywords
esters
compound
neurodegenerative
dissolve
calcium chelating
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/NL2018/050409
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French (fr)
Other versions
WO2018236221A2 (en
Inventor
Thomas Cremers
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.)
Can Holding BV
Original Assignee
Can Holding BV
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Filing date
Publication date
Application filed by Can Holding BV filed Critical Can Holding BV
Publication of WO2018236221A2 publication Critical patent/WO2018236221A2/en
Publication of WO2018236221A3 publication Critical patent/WO2018236221A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A61K31/663—Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/221—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839—Polyphosphonic acids
    • C07F9/3856—Polyphosphonic acids containing halogen or nitro(so) substituents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839—Polyphosphonic acids
    • C07F9/386—Polyphosphonic acids containing hydroxy substituents in the hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839—Polyphosphonic acids
    • C07F9/3865—Polyphosphonic acids containing sulfur substituents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839—Polyphosphonic acids
    • C07F9/3873—Polyphosphonic acids containing nitrogen substituent, e.g. N.....H or N-hydrocarbon group which can be substituted by halogen or nitro(so), N.....O, N.....S, N.....C(=X)- (X =O, S), N.....N, N...C(=X)...N (X =O, S)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
    • C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne un promédicament pour un agent de solubilisation d'ion calcium (Ca2+) ou d'ion magnésium (Mg2+) physiologiquement acceptable, destiné à être utilisé dans un procédé de traitement d'une affection médicale caractérisée par la présence de dépôts de peptides neuropathologiques. Le promédicament est choisi parmi un ester d'un bisphosphonate ou un ester d'un composé chélatant le calcium, et l'affection médicale caractérisée par la présence de dépôts de peptides neuropathologiques peut être la maladie d'Alzheimer, la maladie de Parkinson ou la maladie de Huntington.The invention provides a prodrug for a physiologically acceptable calcium ion (Ca 2+) or magnesium ion (Mg 2+) solubilizing agent for use in a method of treating a medical condition characterized by the presence of neuropathological peptides. The prodrug is selected from an ester of a bisphosphonate or an ester of a calcium chelating compound, and the medical condition characterized by the presence of neuropathological peptide deposits may be Alzheimer's disease, Parkinson's disease or Huntington's disease.

PCT/NL2018/050409 2017-06-03 2018-06-25 DISSOLUTION OF NEURODEGENERATIVE PEPTIDE DEPOSITION Ceased WO2018236221A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
NL2019118 2017-06-03
NL2019118 2017-06-23

Publications (2)

Publication Number Publication Date
WO2018236221A2 WO2018236221A2 (en) 2018-12-27
WO2018236221A3 true WO2018236221A3 (en) 2019-02-21

Family

ID=59521616

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/NL2018/050409 Ceased WO2018236221A2 (en) 2017-06-03 2018-06-25 DISSOLUTION OF NEURODEGENERATIVE PEPTIDE DEPOSITION

Country Status (1)

Country Link
WO (1) WO2018236221A2 (en)

Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0339237A2 (en) * 1988-03-31 1989-11-02 Symphar S.A. Phenol substituted gem-diphosphonate derivatives, process for their preparation and pharmaceutical compositions containing them
WO1998040071A1 (en) * 1997-03-11 1998-09-17 The General Hospital Corporation Identification of agents for use in the treatment of alzheimer's disease
WO1999051613A1 (en) * 1998-04-03 1999-10-14 Medivir Ab Prodrugs of phosphorous-containing pharmaceuticals
WO2003094851A2 (en) * 2002-05-11 2003-11-20 Ilex Products, Inc. 1,1- and 1,2-bisphosphonates as apoliprotein e modulators
WO2004028443A2 (en) * 2002-09-25 2004-04-08 D-Pharm Ltd. Lipophilic diesters of chelating agent for inhibition of enzyme activity
WO2005016229A2 (en) * 2003-08-14 2005-02-24 D-Pharm Ltd. Use of lipophilic diesters of chelating agent for the treatment of amyloidosis and atherosclerosis
US20050209321A1 (en) * 2004-03-15 2005-09-22 Manjari Lal Platinum carboxylate anticancer compounds
WO2007015122A1 (en) * 2005-08-02 2007-02-08 Genexel, Inc. Therapy for alzheimer’s disease
WO2007095178A2 (en) * 2006-02-14 2007-08-23 Eastern Virginia Medical School Methoxypolyethylene glycol thioester chelate and uses thereof
EP2047848A1 (en) * 2006-07-05 2009-04-15 The University of Tokyo Method of treating genetic disease caused by nonsense mutation
WO2012113738A1 (en) * 2011-02-22 2012-08-30 Akzo Nobel Chemicals International B.V. Chelating agent precursors, fluids containing them, and their use
WO2014052896A1 (en) * 2012-09-28 2014-04-03 Tufts University Uridine diphosphate derivatives, prodrugs, compositions and uses thereof
WO2016063297A1 (en) * 2014-10-21 2016-04-28 Council Of Scientific & Industrial Research Alkylidene phosphonate esters as p-glycoprotein inducers

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0339237A2 (en) * 1988-03-31 1989-11-02 Symphar S.A. Phenol substituted gem-diphosphonate derivatives, process for their preparation and pharmaceutical compositions containing them
WO1998040071A1 (en) * 1997-03-11 1998-09-17 The General Hospital Corporation Identification of agents for use in the treatment of alzheimer's disease
WO1999051613A1 (en) * 1998-04-03 1999-10-14 Medivir Ab Prodrugs of phosphorous-containing pharmaceuticals
WO2003094851A2 (en) * 2002-05-11 2003-11-20 Ilex Products, Inc. 1,1- and 1,2-bisphosphonates as apoliprotein e modulators
WO2004028443A2 (en) * 2002-09-25 2004-04-08 D-Pharm Ltd. Lipophilic diesters of chelating agent for inhibition of enzyme activity
WO2005016229A2 (en) * 2003-08-14 2005-02-24 D-Pharm Ltd. Use of lipophilic diesters of chelating agent for the treatment of amyloidosis and atherosclerosis
US20050209321A1 (en) * 2004-03-15 2005-09-22 Manjari Lal Platinum carboxylate anticancer compounds
WO2007015122A1 (en) * 2005-08-02 2007-02-08 Genexel, Inc. Therapy for alzheimer’s disease
WO2007095178A2 (en) * 2006-02-14 2007-08-23 Eastern Virginia Medical School Methoxypolyethylene glycol thioester chelate and uses thereof
EP2047848A1 (en) * 2006-07-05 2009-04-15 The University of Tokyo Method of treating genetic disease caused by nonsense mutation
WO2012113738A1 (en) * 2011-02-22 2012-08-30 Akzo Nobel Chemicals International B.V. Chelating agent precursors, fluids containing them, and their use
WO2014052896A1 (en) * 2012-09-28 2014-04-03 Tufts University Uridine diphosphate derivatives, prodrugs, compositions and uses thereof
WO2016063297A1 (en) * 2014-10-21 2016-04-28 Council Of Scientific & Industrial Research Alkylidene phosphonate esters as p-glycoprotein inducers

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
CADE, J. A.: "Methylenediphosphonates and related compounds. II. Synthesis from .alpha.-oxophosphonates", JOURNAL OF THE CHEMICAL SOCIETY 2272-6 CODEN: JCSOA9; ISSN: 0368-1769, 1959, XP002785069, DOI: 10.1039/JR9590002272 10.1039/JR9590002272 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 1997, CHEN, WEIPING ET AL: "Study on property and acid dissociation constant of .alpha.-hydroxyethylidene-bis(O-alkyl phosphonic acid)", XP002785070, retrieved from STN Database accession no. 1998:347025 *
GIOVANNI B. GIOVENZANA ET AL: "Stevens rearrangement as a tool for the structural modification of polyaminopolycarboxylic ligands", ORGANIC & BIOMOLECULAR CHEMISTRY, vol. 9, no. 3, 1 January 2011 (2011-01-01), pages 679, XP055096726, ISSN: 1477-0520, DOI: 10.1039/c0ob00909a *
JAEGER ET AL: "Surfactant transition metal chelates", COLLOIDS AND SURFACES A: PHYSIOCHEMICAL AND ENGINEERING ASPECTS, ELSEVIER, AMSTERDAM, NL, vol. 302, no. 1-3, 11 May 2007 (2007-05-11), pages 186 - 196, XP022070887, ISSN: 0927-7757, DOI: 10.1016/J.COLSURFA.2007.02.021 *
SUDHAKAR MANDA ET AL: "Design, synthesis and P-gp induction activity of aryl phosphonate esters: identification of tetraethyl-2-phenylethene-1,1-diyldiphosphonate as an orally bioavailable P-gp inducer", MEDCHEMCOMM, vol. 7, no. 10, 1 January 2016 (2016-01-01), United Kingdom, pages 1910 - 1915, XP055507301, ISSN: 2040-2503, DOI: 10.1039/C6MD00300A *

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