DK2595484T3 - Anvendelse af cykliske amidderivater til behandling af søvnforstyrrelser - Google Patents

Anvendelse af cykliske amidderivater til behandling af søvnforstyrrelser Download PDF

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DK2595484T3
DK2595484T3 DK11810349.8T DK11810349T DK2595484T3 DK 2595484 T3 DK2595484 T3 DK 2595484T3 DK 11810349 T DK11810349 T DK 11810349T DK 2595484 T3 DK2595484 T3 DK 2595484T3
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sleep
compound
schizophrenia
formula
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Lorenzo Pellegrini
Argeris N Karabelas
Remy Henri Luthringer
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Minerva Neurosciences Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/40Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered 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
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04LTRANSMISSION OF DIGITAL INFORMATION, e.g. TELEGRAPHIC COMMUNICATION
    • H04L5/00Arrangements affording multiple use of the transmission path
    • H04L5/0001Arrangements for dividing the transmission path
    • H04L5/0003Two-dimensional division
    • H04L5/0005Time-frequency
    • H04L5/0007Time-frequency the frequencies being orthogonal, e.g. OFDM(A), DMT
    • H04L5/001Time-frequency the frequencies being orthogonal, e.g. OFDM(A), DMT the frequencies being arranged in component carriers
    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04LTRANSMISSION OF DIGITAL INFORMATION, e.g. TELEGRAPHIC COMMUNICATION
    • H04L5/00Arrangements affording multiple use of the transmission path
    • H04L5/0001Arrangements for dividing the transmission path
    • H04L5/0014Three-dimensional division
    • H04L5/0016Time-frequency-code
    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04LTRANSMISSION OF DIGITAL INFORMATION, e.g. TELEGRAPHIC COMMUNICATION
    • H04L5/00Arrangements affording multiple use of the transmission path
    • H04L5/0001Arrangements for dividing the transmission path
    • H04L5/0014Three-dimensional division
    • H04L5/0016Time-frequency-code
    • H04L5/0019Time-frequency-code in which one code is applied, as a temporal sequence, to all frequencies
    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04LTRANSMISSION OF DIGITAL INFORMATION, e.g. TELEGRAPHIC COMMUNICATION
    • H04L5/00Arrangements affording multiple use of the transmission path
    • H04L5/003Arrangements for allocating sub-channels of the transmission path
    • H04L5/0048Allocation of pilot signals, i.e. of signals known to the receiver
    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04LTRANSMISSION OF DIGITAL INFORMATION, e.g. TELEGRAPHIC COMMUNICATION
    • H04L5/00Arrangements affording multiple use of the transmission path
    • H04L5/003Arrangements for allocating sub-channels of the transmission path
    • H04L5/0048Allocation of pilot signals, i.e. of signals known to the receiver
    • H04L5/005Allocation of pilot signals, i.e. of signals known to the receiver of common pilots, i.e. pilots destined for multiple users or terminals
    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04LTRANSMISSION OF DIGITAL INFORMATION, e.g. TELEGRAPHIC COMMUNICATION
    • H04L5/00Arrangements affording multiple use of the transmission path
    • H04L5/003Arrangements for allocating sub-channels of the transmission path
    • H04L5/0053Allocation of signaling, i.e. of overhead other than pilot signals
    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04WWIRELESS COMMUNICATION NETWORKS
    • H04W4/00Services specially adapted for wireless communication networks; Facilities therefor

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Neurosurgery (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Computer Networks & Wireless Communication (AREA)
  • Psychiatry (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (11)

1. Forbindelse med formlen (II) eller farmaceutisk acceptabelt salt, hydrat eller solvat deraf til anvendelse i behandling eller bedring af mindst én søvnforstyrrelse hos en person, der lider af skizofreni: II
2. Forbindelse eller salt, hydrat eller solvat deraf til anvendelse ifølge krav 1, hvor personen lider af mindst ét symptom på skizofreni udvalgt fra gruppen bestående af et positivt symptom på skizofreni, et negativt symptom på skizofreni og et generelt symptom på skizofreni.
3. Forbindelse eller salt, hydrat eller solvat deraf til anvendelse ifølge krav 2, hvor det negative symptom er udvalgt fra gruppen bestående af et primært negativt symptom og et sekundært negativt symptom.
4. Forbindelse eller salt, hydrat eller solvat deraf til anvendelse ifølge krav 1, hvor personen er en effektiv cytochrom P450 2D6-metabolisator.
5. Sammensætning til anvendelse i behandling eller bedring af mindst én søvnforstyrrelse hos en person, der lider af skizofreni, hvilken sammensætning omfatter: (a) en terapeutisk effektiv mængde af en antipsykotisk forbindelse, der ikke er en forbindelse med formlen (I); og (b) en terapeutisk effektiv mængde af en forbindelse med formlen (II) ifølge krav 1, eller et farmaceutisk acceptabelt salt, hydrat eller solvat deraf, hvor den terapeutisk effektive mængde af en antipsykotisk forbindelse, der ikke er en forbindelse med formlen (I), er lavere end den ellers ville være i fravær af forbindelsen med formlen (II), hvor forbindelsen med formlen (I) er
hvor: X repræsenterer en alkylgruppe, en cycloalkyl-substitueret alkylgruppe, en aryl-substitueret alkylgruppe, en aryl-substitueret alkenylgruppe, en aryl-substitueret alkynylgruppe, en monocyklisk eller polycyklisk cycloalkylgruppe, der kan være substitueret med en alkylgruppe, en arylgruppe, en heterocyklisk gruppe eller en substitueret eller usubstitueret aminogruppe; Q repræsenterer en gruppe repræsenteret ved —CO—, —O—, —S—, — CH(OR.7)—, —C(=CH2)— eller — C(=NRs)—, hvor R7 repræsenterer et hydrogenatom, en alkylgruppe, en hydroxyalkylgruppe, eller en acylgruppe, og Rs repræsenterer en hydroxylgruppe, en alkoxylgruppe, en aralkyloxygruppe, en acyloxygruppe, en acylaminogruppe eller en alkoxycarbonylaminogruppe; n repræsenterer et heltal på fra 0 til 5; Ri og R2 hver uafhængigt repræsenterer et hydrogenatom eller en alkylgruppe; B repræsenterer følgende grupper:
hvor R3, R4, Rs og R6 hver uafhængigt repræsenterer en substituent udvalgt fra gruppen bestående af et hydrogenatom, et halogenatom, en nitrogruppe, en alkylgruppe, en halogeneret alkylgruppe, en hydroxylgruppe, en alkoxylgruppe, en halogeneret alkoxylgruppe og en cyangruppe; m repræsenterer 1 eller 2.
6. Forbindelse eller salt, hydrat eller solvat deraf til anvendelse ifølge et hvilket som helst af kravene 1-4, hvor den mindst ene søvnforstyrrelse er udvalgt fra gruppen bestående af latenstid til søvnstart, latenstid til dyb søvn, og fordelingen af slow-wave-søvn over søvnperioden eller ét eller flere segmenter af søvnperioden.
7. Forbindelse eller salt, hydrat eller solvat deraf til anvendelse ifølge et hvilket som helst af kravene 1-4, hvor bedringen omfatter bedring af latenstid til søvnstart eller latenstid til dyb søvn.
8. Forbindelse eller salt, hydrat eller solvat deraf til anvendelse ifølge et hvilket som helst af kravene 1-4, hvor bedringen omfatter en stigning i slow-wave-søvn i den første tredjedel af søvnperioden.
9. Sammensætning til anvendelse ifølge krav 5, hvor den mindst ene søvnforstyrrelse er udvalgt fra gruppen bestående af latenstid til søvnstart, latenstid til dyb søvn, og fordelingen af slow-wave-søvn over søvnperioden eller ét eller flere segmenter af søvnperioden.
10. Sammensætning til anvendelse ifølge krav 5, hvor bedringen omfatter bedring af latenstid til søvnstart eller latenstid til dyb søvn.
11. Sammensætning til anvendelse ifølge krav 5, hvor bedringen omfatter en stigning i slow-wave-søvn i den første tredje del af søvnperioden.
DK11810349.8T 2010-07-20 2011-07-20 Anvendelse af cykliske amidderivater til behandling af søvnforstyrrelser DK2595484T3 (da)

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US36607510P 2010-07-20 2010-07-20
PCT/US2011/044697 WO2012012542A1 (en) 2010-07-20 2011-07-20 Methods of use of cyclic amide derivatives to treat schizophrenia

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DK16181339.9T DK3135286T3 (da) 2010-07-20 2011-07-20 Fremgangsmåder til anvendelse af cykliske amidderivater til behandling af skizofreni og symptomer derpå

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US (2) US20180155318A1 (da)
EP (3) EP3335731A1 (da)
JP (2) JP6053678B2 (da)
KR (1) KR101867633B1 (da)
CN (1) CN103220910B (da)
BR (1) BR112013001303A2 (da)
CA (2) CA3117855C (da)
DK (2) DK2595484T3 (da)
ES (2) ES2963362T3 (da)
FI (1) FI3135286T3 (da)
HR (1) HRP20231446T1 (da)
HU (1) HUE064157T2 (da)
LT (1) LT3135286T (da)
NO (1) NO2595484T3 (da)
PL (2) PL3135286T3 (da)
PT (2) PT2595484T (da)
RS (1) RS64819B1 (da)
RU (1) RU2576611C2 (da)
SI (1) SI3135286T1 (da)
TW (1) TWI583679B (da)
WO (1) WO2012012542A1 (da)

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CA2968977A1 (en) * 2014-12-02 2016-06-09 Minerva Neurosciences, Inc. Compositions comprising 2-((1-(2(4-fluorophenyl)-2-oxoethyl)piperidin-4-yl)methyl)isoindolin-1-one for treating schizophrenia
TWI820001B (zh) * 2016-05-25 2023-11-01 日商田邊三菱製藥股份有限公司 醫藥組成物的用於製造非思覺失調症病患之負性症狀治療劑的用途
CN116492340A (zh) 2017-10-10 2023-07-28 纽罗克里生物科学有限公司 施用某些vmat2抑制剂的方法
AU2019326525A1 (en) * 2018-08-21 2021-03-04 Minerva Neurosciences, Inc. Use of roluperidone to treat negative symptoms and disorders, increase neuroplasticity, and promote neuroprotection

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DE3888340T2 (de) * 1988-01-21 1994-06-30 Merrell Dow Pharma Verwendung von 1,4-disubstituierten-Piperidinyl-Verbindungen zur Herstellung eines Arzneimittels zur Behandlung von Schlaflosigkeit.
KR927002347A (ko) * 1989-10-27 1992-09-03 레이몬드 지. 아너 (n-프탈이미도알킬) 피페리딘
NZ235841A (en) * 1989-10-27 1993-03-26 Du Pont (n-phthalimidoalkyl) piperidine derivatives and pharmaceutical compositions
CA2401711C (en) * 2000-02-29 2008-06-03 Mitsubishi Pharma Corporation Cyclic amide derivatives
US7626056B2 (en) * 2005-06-06 2009-12-01 Merck Sharp & Dohme Limited Cyclohexanesulfonyl derivatives as GlyT1 inhibitors to treat schizophrenia
TW200817400A (en) * 2006-05-30 2008-04-16 Elbion Ag Pyrido [3,2-e] pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them

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US20180155318A1 (en) 2018-06-07
PT2595484T (pt) 2018-01-22
KR20130129905A (ko) 2013-11-29
US20220274951A1 (en) 2022-09-01
EP3335731A1 (en) 2018-06-20
TW201211021A (en) 2012-03-16
CN103220910B (zh) 2016-05-11
TWI583679B (zh) 2017-05-21
KR101867633B1 (ko) 2018-06-15
CA3117855C (en) 2023-01-10
BR112013001303A2 (pt) 2016-05-17
CA2806017C (en) 2021-06-29
EP2595484A4 (en) 2014-04-23
RS64819B1 (sr) 2023-12-29
ES2656313T3 (es) 2018-02-26
RU2013107382A (ru) 2014-08-27
RU2576611C2 (ru) 2016-03-10
CA3117855A1 (en) 2012-01-26
ES2963362T3 (es) 2024-03-26
EP3135286A1 (en) 2017-03-01
NO2595484T3 (da) 2018-03-17
PL3135286T3 (pl) 2024-04-22
JP6053678B2 (ja) 2016-12-27
JP2017031159A (ja) 2017-02-09
FI3135286T3 (fi) 2023-11-15
PT3135286T (pt) 2023-11-28
DK3135286T3 (da) 2023-11-27
SI3135286T1 (sl) 2024-02-29
WO2012012542A1 (en) 2012-01-26
LT3135286T (lt) 2023-11-10
HUE064157T2 (hu) 2024-02-28
CN103220910A (zh) 2013-07-24
PL2595484T3 (pl) 2018-03-30
EP3135286B1 (en) 2023-09-06
JP2013531072A (ja) 2013-08-01
HRP20231446T1 (hr) 2024-03-01
EP2595484A1 (en) 2013-05-29
CA2806017A1 (en) 2012-01-26
JP6200561B2 (ja) 2017-09-20
EP2595484B1 (en) 2017-10-18

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