SI2419104T1 - Kombinacije 5-HT4 receptorskih agonistov in acetilholinesteraznih inhibitorjev za zdravljenje kognitivnih motenj - Google Patents

Kombinacije 5-HT4 receptorskih agonistov in acetilholinesteraznih inhibitorjev za zdravljenje kognitivnih motenj Download PDF

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SI2419104T1
SI2419104T1 SI201031632T SI201031632T SI2419104T1 SI 2419104 T1 SI2419104 T1 SI 2419104T1 SI 201031632 T SI201031632 T SI 201031632T SI 201031632 T SI201031632 T SI 201031632T SI 2419104 T1 SI2419104 T1 SI 2419104T1
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Prior art keywords
treatment
acetylcholinesterase inhibitor
compound
disease
pharmaceutically acceptable
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SI201031632T
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English (en)
Inventor
David Beattie
Fei Shen
Jacqueline A. M. Smith
Robert Murray Mckinnell
Ray Chang
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Theravance Biopharma R&D Ip, Llc
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Publication of SI2419104T1 publication Critical patent/SI2419104T1/sl

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy

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  • Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (10)

  1. Kombinacije 5-HT4 receptorskih agonistov in acetilholinesteraznih inhibitorjev za zdravljenje kognitivnih motenj Patentni zahtevki 1. {(liS,3^,5Z?)-8-[(^)-2-hidroksi-3-(metansulfonil-metil-amino)propil]-8-azabiciklo[3.2.1 ]okt-3-il} amid 1 -izopropil-2-okso-1,2-dihidrokinolin-3-karboksilne kisline ali njegova farmacevtsko sprejemljiva sol za uporabo v kombinaciji z acetilholinesteraznim inhibitorjem za zdravljenje Alzheimerjeve bolezni ali kognitivne motnje.
  2. 2. Spojina za uporabo po zahtevku 1, kjer sta v navedenem zdravljenju navedena spojina in navedeni acetilholinesterazni inhibitor vsak prisotna v odmerku, ki je pod-učinkovit za zdravljenje Alzheimerjeve bolezni ali kognitivne motnje, kadar se ju daje sama.
  3. 3. Spojina za uporabo po zahtevku 1 ali zahtevku 2, kjer je acetilholinesterazni inhibitor donepezilijev hidroklorid.
  4. 4. Spojina po zahtevku 1 za uporabo v kombinaciji z acetilholinesteraznim inhibitorjem za izboljšanje spomina pri bolniku, ki ima spominski deficit.
  5. 5. Spojina za uporabo po zahtevku 4, kjer sta v navedenem zdravljenju navedena spojina in navedeni acetilholinesterazni inhibitor vsak prisotna v odmerku, ki je pod-učinkovit za izboljšanje spomina pri bolniku, ki doživlja spominski deficit, kadar se ju daje sama.
  6. 6. {(15,3/?,5/?)-8-[(i?)-2-hidroksi-3-(metansulfonil-metil-amino)propil]-8-azabiciklo[3.2.1]okt-3-il}amid l-izopropil-2-okso-l,2-dihidrokinolin-3-karboksilne kisline ali njegova farmacevtsko sprejemljiva sol za uporabo v povečanju učinkovitosti acetilholinesteraznega inhibitorja za zdravljenje Alzheimerjeve bolezni ali kognitivne motnje.
  7. 7. Farmacevtski sestavek, ki obsega acetilholinesterazni inhibitor, {(lS,3R,5R)-8-[(i?)-2-hidroksi-3-(metansulfonil-metil-amino)propil]-8-azabiciklo[3.2.1]okt-3-iljamid l-izopropil-2-okso-l,2-dihidrokinolin-3-karboksilne kisline ali njegovo farmacevtsko sprejemljivo sol in farmacevtsko sprejemljiv nosilec.
  8. 8. Farmacevtski sestavek po zahtevku 7, kjer je acetilholinesterazni inhibitor donepezilijev hidroklorid.
  9. 9. Uporaba {(lS,3/?,5/?)-8-[(/?)-2-hidroksi-3-(metansulfonil-metil-amino)propil]-8-azabiciklo[3.2.1]okt-3-il}amida l-izopropil-2-okso-l,2-dihidrokinolin-3-karboksilne kisline ali njegove farmacevtsko sprejemljive soli v izdelavi zdravila za zdravljenje Alzheimerjeve bolezni ali kognitivne motnje pri pacientu, pri čemer navedeno zdravljenje obsega dajanje navedene spojine v kombinaciji z acetilholinesteraznim inhibitorjem.
  10. 10. Uporaba po zahtevku 9, kjer se zdravilo uporabi v odmerku navedene spojine in navedenega acetilholinesteraznega inhbitorja, ki je pod-učinkovit za zdravljenje Alzheimerjeve bolezni ali kognitivne motnje, kadar se ju daje sama.
SI201031632T 2009-04-13 2010-04-12 Kombinacije 5-HT4 receptorskih agonistov in acetilholinesteraznih inhibitorjev za zdravljenje kognitivnih motenj SI2419104T1 (sl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US16874109P 2009-04-13 2009-04-13
US29255910P 2010-01-06 2010-01-06
PCT/US2010/030760 WO2010120695A2 (en) 2009-04-13 2010-04-12 5-ht4 receptor agonist compounds for treatment of cognitive disorders
EP10713790.3A EP2419104B1 (en) 2009-04-13 2010-04-12 Combinations of 5-ht4 receptor agonists and acetylcholinesterase inhibitors for treatment of cognitive disorders

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SI2419104T1 true SI2419104T1 (sl) 2018-03-30

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US (2) US8404711B2 (sl)
EP (1) EP2419104B1 (sl)
JP (1) JP2012523437A (sl)
KR (1) KR20120017421A (sl)
CN (2) CN102395371A (sl)
AU (1) AU2010236734B2 (sl)
BR (1) BRPI1013777A8 (sl)
CA (1) CA2758321A1 (sl)
CY (1) CY1119800T1 (sl)
DK (1) DK2419104T3 (sl)
ES (1) ES2654930T3 (sl)
HR (1) HRP20180018T1 (sl)
HU (1) HUE038141T2 (sl)
IL (1) IL215660A0 (sl)
LT (1) LT2419104T (sl)
MX (1) MX2011010782A (sl)
NO (1) NO2419104T3 (sl)
PL (1) PL2419104T3 (sl)
PT (1) PT2419104T (sl)
RU (1) RU2569056C2 (sl)
SI (1) SI2419104T1 (sl)
WO (1) WO2010120695A2 (sl)
ZA (1) ZA201107490B (sl)

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DK3029039T3 (en) 2010-05-17 2017-12-04 Forum Pharmaceuticals Inc PHARMACEUTICAL FORMS CONTAINING CRYSTALLINIC FORMS OF (R) -7-CHLOR-N- (QUINUCLIDIN-3-YL) BENZO (B) THIOPHEN-2-CARBOXAMIDE HYDROCHLORIDE MONOHYDRATE
WO2013169646A1 (en) 2012-05-08 2013-11-14 Envivo Pharmaceuticals, Inc. Methods of maintaining, treating or improving cognitive function
US10874701B2 (en) 2012-08-16 2020-12-29 University-Industry Cooperation Group Of Kyung Hee University Lactic acid bacteria capable of preventing and/or treating senescence and dementia
JP6009080B2 (ja) 2012-08-16 2016-10-19 ユニバーシティ−インダストリー コオペレーション グループ オブ キョン ヒ ユニバーシティUniversity−Industry Cooperation Group Of Kyung Hee University 老化及び認知症の予防及び/または治療活性を有する乳酸菌
CN111032038A (zh) 2017-05-24 2020-04-17 H.隆德贝克有限公司 用于治疗阿尔茨海默氏病的药物组合
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NZ759585A (en) 2017-06-02 2022-02-25 Fujifilm Toyama Chemical Co Ltd Agent for preventing or treating brain atrophy
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PT1311272E (pt) * 2000-03-03 2007-02-28 Eisai R&D Man Co Ltd Novos métodos utilizando inibidores de colinesterase
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DK2419104T3 (en) 2018-02-05
LT2419104T (lt) 2018-02-12
ZA201107490B (en) 2012-06-27
WO2010120695A2 (en) 2010-10-21
CY1119800T1 (el) 2018-06-27
PL2419104T3 (pl) 2018-04-30
US20100261752A1 (en) 2010-10-14
BRPI1013777A8 (pt) 2017-09-19
CN105832735A (zh) 2016-08-10
EP2419104A2 (en) 2012-02-22
RU2011146032A (ru) 2013-05-20
KR20120017421A (ko) 2012-02-28
ES2654930T3 (es) 2018-02-15
IL215660A0 (en) 2012-01-31
JP2012523437A (ja) 2012-10-04
US20140057939A1 (en) 2014-02-27
CN102395371A (zh) 2012-03-28
AU2010236734A1 (en) 2011-11-03
EP2419104B1 (en) 2017-11-08
AU2010236734A8 (en) 2012-02-16
US8404711B2 (en) 2013-03-26
MX2011010782A (es) 2012-01-20
HRP20180018T1 (hr) 2018-02-09
HUE038141T2 (hu) 2018-10-29
WO2010120695A3 (en) 2010-12-02
PT2419104T (pt) 2018-01-31
CA2758321A1 (en) 2010-10-21
NO2419104T3 (sl) 2018-04-07
BRPI1013777A2 (pt) 2016-04-05
RU2569056C2 (ru) 2015-11-20
AU2010236734B2 (en) 2015-06-11

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