SI2503993T1 - Hidrokloridna sol 4-(2-((5-metil-1-(2-naftalenil)-1h-pirazol-3-il)oksi) etil)morfolina - Google Patents

Hidrokloridna sol 4-(2-((5-metil-1-(2-naftalenil)-1h-pirazol-3-il)oksi) etil)morfolina

Info

Publication number
SI2503993T1
SI2503993T1 SI201031267A SI201031267A SI2503993T1 SI 2503993 T1 SI2503993 T1 SI 2503993T1 SI 201031267 A SI201031267 A SI 201031267A SI 201031267 A SI201031267 A SI 201031267A SI 2503993 T1 SI2503993 T1 SI 2503993T1
Authority
SI
Slovenia
Prior art keywords
naphthalenyl
pyrazol
morpholine
oxy
ethyl
Prior art date
Application number
SI201031267A
Other languages
English (en)
Inventor
Maria Rosa Cuberes-Altisent
- Carandell Lluis Sol
- Couceiro Urko Garcia
Original Assignee
Laboratorios Del Dr. Esteve, S.A.
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
Priority claimed from EP09382261A external-priority patent/EP2335688A1/en
Priority claimed from EP10382025A external-priority patent/EP2361904A1/en
Application filed by Laboratorios Del Dr. Esteve, S.A. filed Critical Laboratorios Del Dr. Esteve, S.A.
Publication of SI2503993T1 publication Critical patent/SI2503993T1/sl

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D231/18One oxygen or sulfur atom
    • C07D231/20One oxygen atom attached in position 3 or 5
    • C07D231/22One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
    • 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/41551,2-Diazoles non condensed 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
    • A61K31/535Heterocyclic 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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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
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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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
    • A61K9/1682Processes
    • A61K9/1694Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • AHUMAN NECESSITIES
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Molecular Biology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Biophysics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
SI201031267A 2009-11-25 2010-11-25 Hidrokloridna sol 4-(2-((5-metil-1-(2-naftalenil)-1h-pirazol-3-il)oksi) etil)morfolina SI2503993T1 (sl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP09382261A EP2335688A1 (en) 2009-11-25 2009-11-25 Pharmaceutical compositions comprising sigma receptor ligands
EP10382025A EP2361904A1 (en) 2010-02-04 2010-02-04 4-[-2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride and crystalline forms thereof
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
EP10782303.1A EP2503993B1 (en) 2009-11-25 2010-11-25 Hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine

Publications (1)

Publication Number Publication Date
SI2503993T1 true SI2503993T1 (sl) 2016-10-28

Family

ID=43629487

Family Applications (1)

Application Number Title Priority Date Filing Date
SI201031267A SI2503993T1 (sl) 2009-11-25 2010-11-25 Hidrokloridna sol 4-(2-((5-metil-1-(2-naftalenil)-1h-pirazol-3-il)oksi) etil)morfolina

Country Status (32)

Country Link
US (1) US20130143884A1 (sl)
EP (1) EP2503993B1 (sl)
JP (1) JP5794999B2 (sl)
KR (2) KR20170096225A (sl)
CN (2) CN102753154A (sl)
AR (1) AR079198A1 (sl)
AU (1) AU2010323116B2 (sl)
BR (1) BR112012012456A2 (sl)
CA (1) CA2781744C (sl)
CO (1) CO6612255A2 (sl)
CY (1) CY1117962T1 (sl)
DK (1) DK2503993T3 (sl)
EC (1) ECSP12011959A (sl)
ES (1) ES2589045T3 (sl)
HR (1) HRP20161128T1 (sl)
HU (1) HUE029283T2 (sl)
IL (1) IL219997A (sl)
LT (1) LT2503993T (sl)
MA (1) MA33835B1 (sl)
ME (1) ME02481B (sl)
MX (1) MX339932B (sl)
MY (1) MY160018A (sl)
NZ (1) NZ600310A (sl)
PT (1) PT2503993T (sl)
RS (1) RS55099B1 (sl)
RU (1) RU2559325C2 (sl)
SI (1) SI2503993T1 (sl)
SM (1) SMT201600304B (sl)
TN (1) TN2012000247A1 (sl)
TW (1) TWI482767B (sl)
WO (1) WO2011064315A1 (sl)
ZA (1) ZA201203771B (sl)

Families Citing this family (14)

* 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
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
EP2792352A1 (en) 2013-04-16 2014-10-22 Laboratorios Del. Dr. Esteve, S.A. Alpha-2 adrenoreceptor and sigma receptor ligand combinations
TW201607538A (zh) 2013-12-17 2016-03-01 以斯提夫博士實驗室股份有限公司 血清素-去甲腎上腺素再攝取抑制劑(SNRIS)和σ受體配體組合物
MA39146A1 (fr) 2013-12-17 2017-11-30 Esteve Labor Dr Combinaisons de gabapentanoïdes et de ligands des récepteurs sigma
EP3344620B1 (en) * 2015-09-02 2022-10-26 Esteve Pharmaceuticals, S.A. 1-(4-(2-((1-(3,4-difluorophenyl)-1h-pyrazol-3-yl)methoxy)ethyl) piperazin-1-yl)ethanone salts
AR108682A1 (es) 2016-06-06 2018-09-12 Esteve Labor Dr Derivados de pirazol-3-iloxi ligandos del receptor sigma
WO2018059420A1 (zh) * 2016-09-27 2018-04-05 苏州科睿思制药有限公司 E52862盐酸盐晶型h及其制备方法
WO2019068771A1 (en) 2017-10-04 2019-04-11 Esteve Pharmaceuticals, S.A. USE OF SIGMA RECEPTOR LIGANDS AGAINST AGE-RELATED COGNITIVE DISORDERS

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2347015C2 (de) * 1973-09-14 1985-12-12 Schering AG, 1000 Berlin und 4709 Bergkamen Neue Pyrazolyloxyessigsäurederivate, Verfahren zu ihrer Herstellung und diese enthaltende Mittel
EP1634872A1 (en) * 2004-08-27 2006-03-15 Laboratorios Del Dr. Esteve, S.A. Pyrazole derivatives as sigma receptor inhibitors
JP5139061B2 (ja) * 2004-08-27 2013-02-06 ラボラトリオス デル ドクトール エステベ エセ.ア. シグマ受容体阻害剤
MX2007002341A (es) * 2004-08-27 2007-09-25 Esteve Labor Dr Inhibidores del receptor sigma.
EP2113501A1 (en) * 2008-04-25 2009-11-04 Laboratorios Del. Dr. Esteve, S.A. 5-Methyl-1-(naphthalen-2-YL)-1H-Pyrazoles useful as sigma receptor inhibitors
EP2335688A1 (en) * 2009-11-25 2011-06-22 Laboratorios Del. Dr. Esteve, S.A. Pharmaceutical compositions comprising sigma receptor ligands

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MY160018A (en) 2017-02-15
CA2781744A1 (en) 2011-06-03
WO2011064315A1 (en) 2011-06-03
ZA201203771B (en) 2013-08-28
ES2589045T3 (es) 2016-11-08
AU2010323116A1 (en) 2012-06-21
RU2559325C2 (ru) 2015-08-10
ME02481B (me) 2017-02-20
RS55099B1 (sr) 2016-12-30
PT2503993T (pt) 2016-09-09
LT2503993T (lt) 2016-09-12
CN105859624A (zh) 2016-08-17
EP2503993B1 (en) 2016-07-13
KR20130004244A (ko) 2013-01-09
TW201129560A (en) 2011-09-01
US20130143884A1 (en) 2013-06-06
HUE029283T2 (en) 2017-02-28
BR112012012456A2 (pt) 2020-08-11
KR20170096225A (ko) 2017-08-23
MX2012006108A (es) 2012-07-03
DK2503993T3 (en) 2016-08-22
JP2013512225A (ja) 2013-04-11
IL219997A0 (en) 2012-07-31
SMT201600304B (it) 2016-11-10
AR079198A1 (es) 2012-01-04
TWI482767B (zh) 2015-05-01
IL219997A (en) 2016-12-29
ECSP12011959A (es) 2012-07-31
NZ600310A (en) 2013-08-30
MX339932B (es) 2016-06-17
CN102753154A (zh) 2012-10-24
RU2012126105A (ru) 2013-12-27
CO6612255A2 (es) 2013-02-01
AU2010323116B2 (en) 2016-03-10
EP2503993A1 (en) 2012-10-03
CY1117962T1 (el) 2017-05-17
HRP20161128T1 (hr) 2016-11-18
TN2012000247A1 (en) 2013-12-12
JP5794999B2 (ja) 2015-10-14
CA2781744C (en) 2017-11-07
MA33835B1 (fr) 2012-12-03

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