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 PDFInfo
- 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
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- esters
- compound
- neurodegenerative
- dissolve
- calcium chelating
- Prior art date
Links
- 150000002148 esters Chemical class 0.000 title abstract 4
- 108090000765 processed proteins & peptides Proteins 0.000 title abstract 3
- 229940122361 Bisphosphonate Drugs 0.000 title abstract 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 title abstract 2
- 229910052791 calcium Inorganic materials 0.000 title abstract 2
- 239000011575 calcium Substances 0.000 title abstract 2
- 239000002738 chelating agent Substances 0.000 title abstract 2
- -1 bisphosphonate compound Chemical class 0.000 title 1
- 230000000626 neurodegenerative effect Effects 0.000 title 1
- BHPQYMZQTOCNFJ-UHFFFAOYSA-N Calcium cation Chemical compound [Ca+2] BHPQYMZQTOCNFJ-UHFFFAOYSA-N 0.000 abstract 2
- JLVVSXFLKOJNIY-UHFFFAOYSA-N Magnesium ion Chemical compound [Mg+2] JLVVSXFLKOJNIY-UHFFFAOYSA-N 0.000 abstract 2
- 229910001424 calcium ion Inorganic materials 0.000 abstract 2
- 229910001425 magnesium ion Inorganic materials 0.000 abstract 2
- 230000002981 neuropathic effect Effects 0.000 abstract 2
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000023105 Huntington disease Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 150000004663 bisphosphonates Chemical class 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
Classifications
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- 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)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention pertains to a prodrug for a physiologically acceptable calcium ion (Ca2+) or magnesium ion (Mg2+) solubilizer, for use in a method of treating a medical condition characterized by the presence of deposits of neuropath ological 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 deposits of neuropath ological peptides can be Alzheimer's disease, Parkinson's disease or Huntington's disease.
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 |
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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 WO2018236221A2 (en) | 2017-06-03 | 2018-06-25 | Neurodegenerative peptide deposit dissolution |
Country Status (1)
Country | Link |
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WO (1) | WO2018236221A2 (en) |
Citations (13)
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 |
-
2018
- 2018-06-25 WO PCT/NL2018/050409 patent/WO2018236221A2/en active Application Filing
Patent Citations (13)
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)
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 * |
Also Published As
Publication number | Publication date |
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WO2018236221A2 (en) | 2018-12-27 |
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