GR1008233B - Βελτιωση και θεραπευτικη αξιοποιηση της συμπτωματικης αντιμετωπισης της ασθενειας του alzheimer με rivastigmine, galantamine ή donepezil, δια επιλεγμενων αμινοτετραϋδροφουρανιων που δρουν σαν μικτοι σιγμα-1/ μουσκαρινικοι προσδετες - Google Patents

Βελτιωση και θεραπευτικη αξιοποιηση της συμπτωματικης αντιμετωπισης της ασθενειας του alzheimer με rivastigmine, galantamine ή donepezil, δια επιλεγμενων αμινοτετραϋδροφουρανιων που δρουν σαν μικτοι σιγμα-1/ μουσκαρινικοι προσδετες

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Publication number
GR1008233B
GR1008233B GR20130100181A GR20130100181A GR1008233B GR 1008233 B GR1008233 B GR 1008233B GR 20130100181 A GR20130100181 A GR 20130100181A GR 20130100181 A GR20130100181 A GR 20130100181A GR 1008233 B GR1008233 B GR 1008233B
Authority
GR
Greece
Prior art keywords
rivastigmine
donepezil
drugs
aminotetrafurans
valorization
Prior art date
Application number
GR20130100181A
Other languages
English (en)
Inventor
Αλεξανδρος Δημητριου Βαμβακιδης
Original Assignee
Αλεξανδρος Δημητριου Βαμβακιδης
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
Application filed by Αλεξανδρος Δημητριου Βαμβακιδης filed Critical Αλεξανδρος Δημητριου Βαμβακιδης
Priority to GR20130100181A priority Critical patent/GR1008233B/el
Priority to US14/395,581 priority patent/US20150073046A1/en
Priority to PCT/GR2013/000018 priority patent/WO2014155138A1/en
Priority to US13/940,352 priority patent/US9750746B2/en
Publication of GR1008233B publication Critical patent/GR1008233B/el
Priority to US14/865,862 priority patent/US20160009674A1/en
Priority to US15/695,170 priority patent/US20170360798A1/en

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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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/13—Amines
    • 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
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • 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
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/10—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/14—Radicals substituted by nitrogen atoms not forming part of a nitro radical

Abstract

Η παρούσα εφεύρεση αφορά τα επιλεγμένα αμινοτετραϋδροφουράνια ΑΕ37, AE37Met, ΑΕ14 και τα εναντιομερή τους που, σαν πρωτότυποι μικτοί σίγμα-1/μου-σκαρινικοί προσδέτες, προτείνονται για την βελτίωση της δράσης των αντίχο-λινεστερασικών φαρμάκων (ΑΧΕασες) και πιο ειδικά των Donepezil, Galantamine και Rivastigmine. Πράγματι, αυτά τα αμινοτετραϋδροφουράνια παρουσιάζουν ανταγωνιστική δράση κατά των Μ2 και M3 μουσκαρινικών υποδοχέων, η οποία δρα κατά των χολινεργικών ανεπιθύμητων ενεργειών, των ως άνω φαρμάκων, οι οποίες αποτελούν τον πλέον περιοριστικό παράγοντα στην χρήση των κατά την συμπτωματική αντιμετώπιση της ασθένειας του Alzheimer (ΑΑ). Επιπλέον, διά του ανταγωνισμού των επί των προσυναπτικών μουσκαρινικών M2 αυτοϋποδοχέων και την λίαν επιλεκτική σίγμα-1 αγωνιστική δράση των αποτελούν δυνατότητα αξιοποίησης των ΑΧΕασες, και πιο ειδικά των Donepezil, Galantamine ή Rivastigmine, από την σημερινή τους χρήση κατά των συμπτωμάτων της ΑΑ προς την προοπτική θεραπευτικής χρήσης των κατά της εξέλιξης της ΑΑ.
GR20130100181A 2013-03-28 2013-03-28 Βελτιωση και θεραπευτικη αξιοποιηση της συμπτωματικης αντιμετωπισης της ασθενειας του alzheimer με rivastigmine, galantamine ή donepezil, δια επιλεγμενων αμινοτετραϋδροφουρανιων που δρουν σαν μικτοι σιγμα-1/ μουσκαρινικοι προσδετες GR1008233B (el)

Priority Applications (6)

Application Number Priority Date Filing Date Title
GR20130100181A GR1008233B (el) 2013-03-28 2013-03-28 Βελτιωση και θεραπευτικη αξιοποιηση της συμπτωματικης αντιμετωπισης της ασθενειας του alzheimer με rivastigmine, galantamine ή donepezil, δια επιλεγμενων αμινοτετραϋδροφουρανιων που δρουν σαν μικτοι σιγμα-1/ μουσκαρινικοι προσδετες
US14/395,581 US20150073046A1 (en) 2013-03-28 2013-04-03 Optimization and therapeutic valorization of the symptomatic treatment of alzheimer's disease with rivastigmine, galantamine or donepezil, by selected aminotetrahydrofurans acting as mixed sigma-1 / muscarinic ligands
PCT/GR2013/000018 WO2014155138A1 (en) 2013-03-28 2013-04-03 Optimization and therapeutic valorization of the symptomatic treatment of alzheimer's disease with rivastigmine, galantamine or donepezil, by selected aminotetrahydrofurans acting as mixed sigma-1 / muscarinic ligands
US13/940,352 US9750746B2 (en) 2013-03-28 2013-07-12 ANAVEX2-73 and certain anticholinesterase inhibitors composition and method for neuroprotection
US14/865,862 US20160009674A1 (en) 2013-03-28 2015-09-25 Prototypical brain protective activity of tetrahydro-n-methyl-2,2-diphenyl-3-furanomethanamine (ae37met)
US15/695,170 US20170360798A1 (en) 2013-03-28 2017-09-05 Anavex2-73 and certain anticholinesterase inhibitors composition and method for neuroprotection

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GR20130100181A GR1008233B (el) 2013-03-28 2013-03-28 Βελτιωση και θεραπευτικη αξιοποιηση της συμπτωματικης αντιμετωπισης της ασθενειας του alzheimer με rivastigmine, galantamine ή donepezil, δια επιλεγμενων αμινοτετραϋδροφουρανιων που δρουν σαν μικτοι σιγμα-1/ μουσκαρινικοι προσδετες

Publications (1)

Publication Number Publication Date
GR1008233B true GR1008233B (el) 2014-06-23

Family

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Family Applications (1)

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GR20130100181A GR1008233B (el) 2013-03-28 2013-03-28 Βελτιωση και θεραπευτικη αξιοποιηση της συμπτωματικης αντιμετωπισης της ασθενειας του alzheimer με rivastigmine, galantamine ή donepezil, δια επιλεγμενων αμινοτετραϋδροφουρανιων που δρουν σαν μικτοι σιγμα-1/ μουσκαρινικοι προσδετες

Country Status (3)

Country Link
US (4) US20150073046A1 (el)
GR (1) GR1008233B (el)
WO (1) WO2014155138A1 (el)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GR1009143B (el) * 2016-07-14 2017-10-20 Αλεξανδρος Δημητριου Βαμβακιδης Πρωτοτυπη θεραπευτικη δραση επιλεγμενων αμινοτετραϋδροφουρανιων κατα των νευροεκφυλιστικων και των διαχυτων νευροαναπτυξιακων ασθενειων
US11617734B2 (en) 2015-07-22 2023-04-04 Anavex Life Sciences Corp. Enantiomers of A2-73, analogues, and sigma agonist activity

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* Cited by examiner, † Cited by third party
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US9517232B2 (en) 2013-11-02 2016-12-13 Medi Synergics, LLC Compounds for treatment of alzheimer's disease
JP2017531043A (ja) * 2014-10-20 2017-10-19 アナベックス ライフ サイエンシズ コーポレイション 抗発作治療のためのａ１９−１４４、ａ２−７３およびある特定の抗コリンエステラーゼ阻害剤、組成物および方法
JP7304043B2 (ja) 2015-07-22 2023-07-06 アナベックス ライフ サイエンシズ コーポレイション テトラヒドロ－ｎ，ｎ－ジメチル－２，２－ジフェニル－３－フランメタンアミンヒドロクロリドの結晶形態、かかる形態の作製方法およびその薬学的組成物
US11337953B2 (en) 2016-07-27 2022-05-24 Anavex Life Sciences Corp. A2-73 as a therapeutic for insomnia, anxiety, and agitation
US10426754B2 (en) 2017-06-14 2019-10-01 Anavex Life Sciences Corp. Crystalline form of ANAVEX2-73 for the treatment of Alzheimer's disease
EP3638225A1 (en) * 2017-06-14 2020-04-22 Anavex Life Sciences Corp. Anavex2-73 for the treatment of alzheimer's disease
WO2019023239A1 (en) * 2017-07-25 2019-01-31 William Beaumont Hospital METHODS FOR DIAGNOSING AND TREATING ALZHEIMER'S DISEASE
AU2018351088B2 (en) * 2017-10-20 2024-02-01 Anavex Life Sciences Corp. Treatment of cardiac dysfunction
CN112105349A (zh) * 2018-04-12 2020-12-18 阿纳韦克斯生命科学公司 A2-73结晶多晶型物质组合物及其使用方法
AU2019269739A1 (en) 2018-05-18 2020-12-10 Anavex Life Sciences Corp. Optimized sigma-1 agonist method of responder selection and treatment
US20220249427A1 (en) * 2019-07-22 2022-08-11 Anavex Life Sciences Corp. Anavex2-73 for the treatment of genetic neurodevelopmental disorders
EP4124338A1 (en) 2021-07-30 2023-02-01 Université de Montpellier Sigma-1 receptor activator for use in the treatment of a pathology associated with wfs1 mutation
WO2024026480A1 (en) * 2022-07-29 2024-02-01 Anavex Life Sciences Corp. Compositions and methods for prevention of cognitive decline caused by degenerative diseases

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GR1005865B (el) 2007-01-17 2008-04-07 Anavex Life Sciences Corp. Νεοι συνδετες των σιγμα υποδοχεων με αντι-αποπτωτικες και/η προ-αποπτωτικες ιδιοτητες επι των κυτταρικων βιοχημικων μηχανισμων, με νευρο-προστατευτικη, αντικαρκινικη, αντι-μεταστατικη και αντι- αντι-(χρονιο)φλεγμονικη δραση.
US7786171B2 (en) * 2008-04-04 2010-08-31 Abbott Laboratories Amide derivatives as positive allosteric modulators and methods of use thereof

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11617734B2 (en) 2015-07-22 2023-04-04 Anavex Life Sciences Corp. Enantiomers of A2-73, analogues, and sigma agonist activity
GR1009143B (el) * 2016-07-14 2017-10-20 Αλεξανδρος Δημητριου Βαμβακιδης Πρωτοτυπη θεραπευτικη δραση επιλεγμενων αμινοτετραϋδροφουρανιων κατα των νευροεκφυλιστικων και των διαχυτων νευροαναπτυξιακων ασθενειων

Also Published As

Publication number Publication date
US9750746B2 (en) 2017-09-05
US20140296211A1 (en) 2014-10-02
US20150073046A1 (en) 2015-03-12
US20160009674A1 (en) 2016-01-14
WO2014155138A1 (en) 2014-10-02
US20170360798A1 (en) 2017-12-21

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