CY1117886T1 - Υδροχλωρικη 4-[2-[[5-μεθυλ-1-(2-ναφθαλενυλ)-1η-πυραζολ-3-υλ]οξυ]αιθυλ]μορφολινη και επιδιαλυτωματα - Google Patents

Υδροχλωρικη 4-[2-[[5-μεθυλ-1-(2-ναφθαλενυλ)-1η-πυραζολ-3-υλ]οξυ]αιθυλ]μορφολινη και επιδιαλυτωματα

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Publication number
CY1117886T1
CY1117886T1 CY20161100779T CY161100779T CY1117886T1 CY 1117886 T1 CY1117886 T1 CY 1117886T1 CY 20161100779 T CY20161100779 T CY 20161100779T CY 161100779 T CY161100779 T CY 161100779T CY 1117886 T1 CY1117886 T1 CY 1117886T1
Authority
CY
Cyprus
Prior art keywords
naphthalenyl
pyrazol
oxy
ethyl
methyl
Prior art date
Application number
CY20161100779T
Other languages
English (en)
Inventor
Maimó Ramón Berenguer
Rupérez Jorge Medrano
Buchholz Jordi Benet
Fernandez Laura Puig
Puxeu Laia Pellejà
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 EP10382025A external-priority patent/EP2361904A1/en
Priority claimed from EP10382226A external-priority patent/EP2426112A1/en
Application filed by Laboratorios Del Dr. Esteve, S.A. filed Critical Laboratorios Del Dr. Esteve, S.A.
Publication of CY1117886T1 publication Critical patent/CY1117886T1/el

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Classifications

    • CCHEMISTRY; METALLURGY
    • 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
    • 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
    • A61K31/41Heterocyclic 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
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Η παρούσα εφεύρεση αναφέρεται σε πολύμορφα και επιδιαλυτώματα του υδροχλωρικού άλατος της 4-[2-[[5-μεθυλ- 1-(2-ναφθαλενυλ)-1Η-πυραζολ-3-υλ]οξυ]αιθυλ]μορφολίνης(Ρ027), σε διεργασίες για την παρασκευή τους και σε φαρμακευτικές συνθέσεις που τα περιέχουν.
CY20161100779T 2010-02-04 2016-08-08 Υδροχλωρικη 4-[2-[[5-μεθυλ-1-(2-ναφθαλενυλ)-1η-πυραζολ-3-υλ]οξυ]αιθυλ]μορφολινη και επιδιαλυτωματα CY1117886T1 (el)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
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
EP10382226A EP2426112A1 (en) 2010-08-09 2010-08-09 4-[-2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride polymorphs and solvates
EP11702056.0A EP2531177B8 (en) 2010-02-04 2011-02-04 4-[2-[[5-methyl-1-(2-naphthalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride polymorphs and solvates
PCT/EP2011/051630 WO2011095579A1 (en) 2010-02-04 2011-02-04 4-[-2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride polymorphs and solvates

Publications (1)

Publication Number Publication Date
CY1117886T1 true CY1117886T1 (el) 2017-05-17

Family

ID=43897079

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20161100779T CY1117886T1 (el) 2010-02-04 2016-08-08 Υδροχλωρικη 4-[2-[[5-μεθυλ-1-(2-ναφθαλενυλ)-1η-πυραζολ-3-υλ]οξυ]αιθυλ]μορφολινη και επιδιαλυτωματα

Country Status (31)

Country Link
US (2) US9051275B2 (el)
EP (1) EP2531177B8 (el)
JP (1) JP5894086B2 (el)
KR (2) KR20120123532A (el)
CN (1) CN102753155B (el)
AR (1) AR080133A1 (el)
AU (1) AU2011212476B2 (el)
BR (1) BR112012018958A8 (el)
CA (1) CA2788024C (el)
CO (1) CO6592093A2 (el)
CY (1) CY1117886T1 (el)
DK (1) DK2531177T3 (el)
EC (1) ECSP12012039A (el)
ES (1) ES2586212T3 (el)
HR (1) HRP20160937T1 (el)
HU (1) HUE029738T2 (el)
IL (1) IL221277A (el)
MA (1) MA34047B1 (el)
ME (1) ME02483B (el)
MX (1) MX339193B (el)
NZ (1) NZ601316A (el)
PL (1) PL2531177T3 (el)
PT (1) PT2531177T (el)
RS (1) RS55046B1 (el)
RU (1) RU2560150C2 (el)
SG (2) SG10201500832PA (el)
SI (1) SI2531177T1 (el)
SM (1) SMT201600264B (el)
TN (1) TN2012000347A1 (el)
TW (1) TWI568729B (el)
WO (1) WO2011095579A1 (el)

Families Citing this family (18)

* 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
TWI522361B (zh) 2010-07-09 2016-02-21 艾伯維公司 作為s1p調節劑的稠合雜環衍生物
TW201643169A (zh) 2010-07-09 2016-12-16 艾伯維股份有限公司 作為s1p調節劑的螺-哌啶衍生物
TW201206893A (en) 2010-07-09 2012-02-16 Abbott Healthcare Products Bv Bisaryl (thio) morpholine derivatives as S1P modulators
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
EP3082790A1 (en) 2013-12-17 2016-10-26 Laboratorios Del. Dr. Esteve, S.A. Gabapentinoids and sigma receptor ligands combinations
JP2016540771A (ja) 2013-12-17 2016-12-28 ラボラトリオス・デル・ドクトル・エステベ・ソシエダッド・アノニマ セロトニン−ノルアドレナリン再取り込み阻害薬(snri)およびシグマ受容体リガンドの組み合わせ
US20190142840A1 (en) 2016-06-06 2019-05-16 Esteve Pharmaceuticals, S.A. Use of sigma receptor ligands in cancer
AR109024A1 (es) 2016-07-12 2018-10-17 Esteve Labor Dr Uso de ligandos del receptor sigma en el dolor post-herpético
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
JP2022553802A (ja) 2019-10-31 2022-12-26 エスケープ・バイオ・インコーポレイテッド S1p受容体モジュレーターの固体形態

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ243065A (en) * 1991-06-13 1995-07-26 Lundbeck & Co As H Piperidine derivatives and pharmaceutical compositions
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
US8202872B2 (en) * 2006-03-01 2012-06-19 Laboratorios Del Dr. Esteve, S.A. Pyrazole derivatives as sigma receptor inhibitors
US7695199B2 (en) 2006-07-20 2010-04-13 Finisar Corporation Optical subassembly having insertable cylindrical sleeve
CN101328155B (zh) * 2007-06-20 2010-11-03 上海医药工业研究院 噁唑烷衍生物及其制备方法和应用
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

Also Published As

Publication number Publication date
CN102753155B (zh) 2015-11-25
IL221277A0 (en) 2012-10-31
DK2531177T3 (en) 2016-08-22
CN102753155A (zh) 2012-10-24
NZ601316A (en) 2013-12-20
BR112012018958A2 (pt) 2016-04-12
TN2012000347A1 (en) 2014-01-30
SI2531177T1 (sl) 2016-10-28
US20120316336A1 (en) 2012-12-13
RU2560150C2 (ru) 2015-08-20
MX339193B (es) 2016-05-16
EP2531177A1 (en) 2012-12-12
BR112012018958A8 (pt) 2017-12-19
HUE029738T2 (en) 2017-04-28
MX2012009018A (es) 2012-09-07
MA34047B1 (fr) 2013-03-05
EP2531177B1 (en) 2016-05-11
JP2013518857A (ja) 2013-05-23
RS55046B1 (sr) 2016-12-30
PL2531177T3 (pl) 2016-11-30
KR20180063379A (ko) 2018-06-11
AU2011212476A1 (en) 2012-08-09
US9051275B2 (en) 2015-06-09
RU2012137495A (ru) 2014-03-10
CA2788024A1 (en) 2011-08-11
HRP20160937T1 (hr) 2016-10-07
SMT201600264B (it) 2016-08-31
TWI568729B (zh) 2017-02-01
KR20120123532A (ko) 2012-11-08
CO6592093A2 (es) 2013-01-02
ES2586212T3 (es) 2016-10-13
ECSP12012039A (es) 2012-08-31
SG182628A1 (en) 2012-08-30
ME02483B (me) 2017-02-20
PT2531177T (pt) 2016-08-17
TW201136923A (en) 2011-11-01
JP5894086B2 (ja) 2016-03-23
USRE47214E1 (en) 2019-01-29
IL221277A (en) 2017-06-29
SG10201500832PA (en) 2015-04-29
WO2011095579A1 (en) 2011-08-11
AU2011212476B2 (en) 2016-03-31
CA2788024C (en) 2018-03-13
EP2531177B8 (en) 2016-10-12
AR080133A1 (es) 2012-03-14

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