UA112055C2 - Солі 4-[2-[[5-метил-1-(2-нафталініл)-1h-піразол-3-іл]оксі]етил]морфоліну - Google Patents

Солі 4-[2-[[5-метил-1-(2-нафталініл)-1h-піразол-3-іл]оксі]етил]морфоліну

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Publication number
UA112055C2
UA112055C2 UAA201207654A UAA201207654A UA112055C2 UA 112055 C2 UA112055 C2 UA 112055C2 UA A201207654 A UAA201207654 A UA A201207654A UA A201207654 A UAA201207654 A UA A201207654A UA 112055 C2 UA112055 C2 UA 112055C2
Authority
UA
Ukraine
Prior art keywords
naphthalinyl
pyrazol
morpholine
oxy
salts
Prior art date
Application number
UAA201207654A
Other languages
English (en)
Inventor
Марія Роза Куберес-Алтісент
Льюіс Сола-Карандель
Урко Гарсія-Коусейро
Original Assignee
Лабораторьос Дель Др. Естеве, С.А.
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 Лабораторьос Дель Др. Естеве, С.А. filed Critical Лабораторьос Дель Др. Естеве, С.А.
Priority claimed from PCT/EP2010/068256 external-priority patent/WO2011064315A1/en
Publication of UA112055C2 publication Critical patent/UA112055C2/uk

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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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41521,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
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    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
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    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
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    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • A61K9/1694Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
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  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
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Abstract

Даний винахід стосується солей 4-[-2-[[5-метил-1-(2-нафталініл)-1Н-піразол-3-іл]оксі]етил]морфоліну, особливо гідрохлориду, фармацевтичних композицій, що їх містять, і їх використання для лікування і/або профілактики захворювань, пов'язаних з сигма-рецептором.
UAA201207654A 2009-11-25 2010-11-25 Солі 4-[2-[[5-метил-1-(2-нафталініл)-1h-піразол-3-іл]оксі]етил]морфоліну UA112055C2 (uk)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09382261A EP2335688A1 (en) 2009-11-25 2009-11-25 Pharmaceutical compositions comprising sigma receptor ligands
PCT/EP2010/068256 WO2011064315A1 (en) 2009-11-25 2010-11-25 4-[2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine salts

Publications (1)

Publication Number Publication Date
UA112055C2 true UA112055C2 (uk) 2016-07-25

Family

ID=42077699

Family Applications (2)

Application Number Title Priority Date Filing Date
UAA201207654A UA112055C2 (uk) 2009-11-25 2010-11-25 Солі 4-[2-[[5-метил-1-(2-нафталініл)-1h-піразол-3-іл]оксі]етил]морфоліну
UAA201207655A UA109421C2 (uk) 2009-11-25 2010-11-25 Фармацевтична композиція, яка містить ліганди сигма-рецептора

Family Applications After (1)

Application Number Title Priority Date Filing Date
UAA201207655A UA109421C2 (uk) 2009-11-25 2010-11-25 Фармацевтична композиція, яка містить ліганди сигма-рецептора

Country Status (33)

Country Link
US (1) US9241927B2 (uk)
EP (2) EP2335688A1 (uk)
JP (1) JP5827236B2 (uk)
KR (1) KR101794579B1 (uk)
CN (2) CN105560250A (uk)
AR (1) AR079199A1 (uk)
AU (1) AU2010323097B2 (uk)
BR (1) BR112012012457A2 (uk)
CA (1) CA2781726C (uk)
CO (1) CO6501134A2 (uk)
CY (1) CY1119357T1 (uk)
DK (1) DK2503994T3 (uk)
EC (1) ECSP12011958A (uk)
ES (1) ES2641637T3 (uk)
HR (1) HRP20171448T1 (uk)
HU (1) HUE036377T2 (uk)
IL (1) IL219996A (uk)
LT (1) LT2503994T (uk)
MA (1) MA33836B1 (uk)
ME (1) ME02876B (uk)
MX (1) MX351570B (uk)
NZ (1) NZ600231A (uk)
PL (2) PL2503994T3 (uk)
PT (1) PT2503994T (uk)
RS (1) RS56382B1 (uk)
RU (1) RU2549882C2 (uk)
SG (1) SG10201407504YA (uk)
SI (1) SI2503994T1 (uk)
TN (1) TN2012000246A1 (uk)
TW (1) TWI526207B (uk)
UA (2) UA112055C2 (uk)
WO (1) WO2011064296A1 (uk)
ZA (1) ZA201203774B (uk)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2116539A1 (en) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof
EP2503993B1 (en) * 2009-11-25 2016-07-13 Laboratorios Del. Dr. Esteve, S.A. Hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine
EP2353598A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for use in the prevention and/or treatment of postoperative pain
EP2353591A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
EP2388005A1 (en) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
EP2415471A1 (en) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
EP2426111A1 (en) * 2010-08-09 2012-03-07 Laboratorios Del. Dr. Esteve, S.A. 4-[-2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride amorphous solid forms
EP2524694A1 (en) 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
HUE051406T2 (hu) 2012-11-14 2021-03-01 Grace W R & Co Biológiailag aktív anyagot és rendezetlen szervetlen oxidot tartalmazó kompozíciók
EP2792352A1 (en) 2013-04-16 2014-10-22 Laboratorios Del. Dr. Esteve, S.A. Alpha-2 adrenoreceptor and sigma receptor ligand combinations
TN2016000229A1 (en) 2013-12-17 2017-10-06 Esteve Labor Dr Gabapentinoids and sigma receptor ligands combinations.
SG11201604480PA (en) 2013-12-17 2016-07-28 Esteve Labor Dr SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs) AND SIGMA RECEPTOR LIGANDS COMBINATIONS
EP2929883A1 (en) * 2014-04-08 2015-10-14 Institut Pasteur Pyrazole derivatives as dihydroorotate dehydrogenase (DHODH) inhibitors
MA41177A (fr) * 2014-12-15 2017-10-24 Esteve Labor Dr Utilisation de ligands des récepteurs sigma dans l'arthrose
AU2019387370A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
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

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7696199B2 (en) * 2004-08-27 2010-04-13 Laboratorios Del Dr. Esteve, S.A. Sigma receptor inhibitors
EP1634872A1 (en) * 2004-08-27 2006-03-15 Laboratorios Del Dr. Esteve, S.A. Pyrazole derivatives as sigma receptor inhibitors
SI1781618T1 (sl) * 2004-08-27 2013-01-31 Laboratorios Del Dr. Esteve, S.A. Inhibitorji sigma receptorja
EP2116539A1 (en) * 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof

Also Published As

Publication number Publication date
WO2011064296A9 (en) 2011-07-21
US20120283262A1 (en) 2012-11-08
JP2013512219A (ja) 2013-04-11
CN105560250A (zh) 2016-05-11
ZA201203774B (en) 2013-08-28
AU2010323097B2 (en) 2016-03-24
CY1119357T1 (el) 2018-02-14
MX351570B (es) 2017-10-19
AU2010323097A1 (en) 2012-06-14
US9241927B2 (en) 2016-01-26
KR101794579B1 (ko) 2017-12-01
SI2503994T1 (sl) 2017-11-30
TN2012000246A1 (en) 2013-12-12
CA2781726C (en) 2018-09-04
KR20120109522A (ko) 2012-10-08
IL219996A0 (en) 2012-07-31
IL219996A (en) 2017-10-31
RU2012126126A (ru) 2013-12-27
HUE036377T2 (hu) 2018-07-30
HRP20171448T1 (hr) 2017-11-03
EP2503994B1 (en) 2017-07-05
MA33836B1 (fr) 2012-12-03
TWI526207B (zh) 2016-03-21
RU2549882C2 (ru) 2015-05-10
SG10201407504YA (en) 2014-12-30
NZ600231A (en) 2013-06-28
ECSP12011958A (es) 2012-07-31
WO2011064296A1 (en) 2011-06-03
CN102711736A (zh) 2012-10-03
LT2503994T (lt) 2017-09-25
ES2641637T3 (es) 2017-11-10
PL2503994T3 (pl) 2017-11-30
UA109421C2 (uk) 2015-08-25
CA2781726A1 (en) 2011-06-03
EP2335688A1 (en) 2011-06-22
DK2503994T3 (en) 2017-10-02
RS56382B1 (sr) 2017-12-29
JP5827236B2 (ja) 2015-12-02
EP2503994A1 (en) 2012-10-03
MX2012006106A (es) 2012-07-03
AR079199A1 (es) 2012-01-04
PT2503994T (pt) 2017-10-06
BR112012012457A2 (pt) 2020-08-11
CO6501134A2 (es) 2012-08-15
PL2503993T3 (pl) 2017-09-29
TW201127377A (en) 2011-08-16
ME02876B (me) 2018-04-20

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