RU2012126105A - Соли 4-[2-[[5-метил-1-(2-нафталинил)-1н-пиразол-3-ил]окси]этил]морфолина - Google Patents
Соли 4-[2-[[5-метил-1-(2-нафталинил)-1н-пиразол-3-ил]окси]этил]морфолина Download PDFInfo
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- RU2012126105A RU2012126105A RU2012126105/04A RU2012126105A RU2012126105A RU 2012126105 A RU2012126105 A RU 2012126105A RU 2012126105/04 A RU2012126105/04 A RU 2012126105/04A RU 2012126105 A RU2012126105 A RU 2012126105A RU 2012126105 A RU2012126105 A RU 2012126105A
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- hydrochloride salt
- pyrazol
- oxy
- morpholine
- ethyl
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic 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
- C07D231/14—Heterocyclic 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
- C07D231/18—One oxygen or sulfur atom
- C07D231/20—One oxygen atom attached in position 3 or 5
- C07D231/22—One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
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- A61K31/41—Heterocyclic 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
- A61K31/415—1,2-Diazoles
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K9/1605—Excipients; Inactive ingredients
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Abstract
1. Соль 4-[2-[[5-метил-1-(2-нафталинил)-1H-пиразол-3-ил]окси]этил]морфолина, выбранная из этансульфоната, фумарата, гидрохлорида, малата, малеата, малоната и метансульфоната.2. Соль 4-[2-[[5-метил-1-(2-нафталинил)-1H-пиразол-3-ил]окси]этил]морфолина по п.1, где указанная соль представляет собой гидрохлоридную соль 4-[2-[[5-метил-1-(2-нафталинил)-1H-пиразол-3-ил]окси]этил]морфолина.3. Способ получения гидрохлоридной соли по п.2, включающий:a) смешивание 4-[2-[[5-метил-1-(2-нафталинил)-1H-пиразол-3-ил]окси]этил]морфолина и раствора, содержащего хлористоводородную кислоту, иb) выделение полученной гидрохлоридной соли.4. Фармацевтическая композиция, включающая гидрохлоридную соль по п.2.5. Гидрохлоридная соль по п.2 для использования в качестве лекарственного средства.6. Гидрохлоридная соль по п.2, предназначенная для лечения и/или профилактики заболевания или состояния, опосредованного рецептором сигма.7. Гидрохлоридная соль по п.2, предназначенная для лечения и/или профилактики заболевания, выбранного из группы, состоящей из диареи; липопротеиновых нарушений; мигрени; ожирения; артрита; гипертензии; аритмии; язвы; дефицита обучаемости, памяти и внимания; нарушений познавательных способностей; нейродегенеративных заболеваний; демиенилизирующих заболеваний; зависимости от лекарств и химических веществ, включая кокаин, амфетамин, этанол и никотин; поздней дискинезии; ишемического удара; эпилепсии; удара; стресса; рака; психотических состояний, в частности депрессии, страхов или шизофрении; воспалений; или аутоиммунных заболеваний.
Claims (7)
1. Соль 4-[2-[[5-метил-1-(2-нафталинил)-1H-пиразол-3-ил]окси]этил]морфолина, выбранная из этансульфоната, фумарата, гидрохлорида, малата, малеата, малоната и метансульфоната.
2. Соль 4-[2-[[5-метил-1-(2-нафталинил)-1H-пиразол-3-ил]окси]этил]морфолина по п.1, где указанная соль представляет собой гидрохлоридную соль 4-[2-[[5-метил-1-(2-нафталинил)-1H-пиразол-3-ил]окси]этил]морфолина.
3. Способ получения гидрохлоридной соли по п.2, включающий:
a) смешивание 4-[2-[[5-метил-1-(2-нафталинил)-1H-пиразол-3-ил]окси]этил]морфолина и раствора, содержащего хлористоводородную кислоту, и
b) выделение полученной гидрохлоридной соли.
4. Фармацевтическая композиция, включающая гидрохлоридную соль по п.2.
5. Гидрохлоридная соль по п.2 для использования в качестве лекарственного средства.
6. Гидрохлоридная соль по п.2, предназначенная для лечения и/или профилактики заболевания или состояния, опосредованного рецептором сигма.
7. Гидрохлоридная соль по п.2, предназначенная для лечения и/или профилактики заболевания, выбранного из группы, состоящей из диареи; липопротеиновых нарушений; мигрени; ожирения; артрита; гипертензии; аритмии; язвы; дефицита обучаемости, памяти и внимания; нарушений познавательных способностей; нейродегенеративных заболеваний; демиенилизирующих заболеваний; зависимости от лекарств и химических веществ, включая кокаин, амфетамин, этанол и никотин; поздней дискинезии; ишемического удара; эпилепсии; удара; стресса; рака; психотических состояний, в частности депрессии, страхов или шизофрении; воспалений; или аутоиммунных заболеваний.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09382261.7 | 2009-11-25 | ||
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 |
EP10382025.4 | 2010-02-04 | ||
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 (2)
Publication Number | Publication Date |
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RU2012126105A true RU2012126105A (ru) | 2013-12-27 |
RU2559325C2 RU2559325C2 (ru) | 2015-08-10 |
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Application Number | Title | Priority Date | Filing Date |
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RU2012126105/04A RU2559325C2 (ru) | 2009-11-25 | 2010-11-25 | Соли 4-[2-[[5-метил-1-(2-нафталинил)-1н-пиразол-3-ил]окси]этил]морфолина |
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US (1) | US20130143884A1 (ru) |
EP (1) | EP2503993B1 (ru) |
JP (1) | JP5794999B2 (ru) |
KR (2) | KR20130004244A (ru) |
CN (2) | CN105859624A (ru) |
AR (1) | AR079198A1 (ru) |
AU (1) | AU2010323116B2 (ru) |
BR (1) | BR112012012456A2 (ru) |
CA (1) | CA2781744C (ru) |
CO (1) | CO6612255A2 (ru) |
CY (1) | CY1117962T1 (ru) |
DK (1) | DK2503993T3 (ru) |
EC (1) | ECSP12011959A (ru) |
ES (1) | ES2589045T3 (ru) |
HR (1) | HRP20161128T1 (ru) |
HU (1) | HUE029283T2 (ru) |
IL (1) | IL219997A (ru) |
LT (1) | LT2503993T (ru) |
MA (1) | MA33835B1 (ru) |
ME (1) | ME02481B (ru) |
MX (1) | MX339932B (ru) |
MY (1) | MY160018A (ru) |
NZ (1) | NZ600310A (ru) |
PT (1) | PT2503993T (ru) |
RS (1) | RS55099B1 (ru) |
RU (1) | RU2559325C2 (ru) |
SI (1) | SI2503993T1 (ru) |
SM (1) | SMT201600304B (ru) |
TN (1) | TN2012000247A1 (ru) |
TW (1) | TWI482767B (ru) |
WO (1) | WO2011064315A1 (ru) |
ZA (1) | ZA201203771B (ru) |
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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 |
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 |
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 |
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 |
WO2015091508A1 (en) | 2013-12-17 | 2015-06-25 | Laboratorios Del Dr. Esteve, S.A. | SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs) AND SIGMA RECEPTOR LIGANDS COMBINATIONS |
AU2014364644A1 (en) | 2013-12-17 | 2016-06-23 | Laboratorios Del Dr. Esteve, S.A. | Gabapentinoids and Sigma receptor ligands combinations |
US10640468B2 (en) * | 2015-09-02 | 2020-05-05 | Esteve Pharmaceuticals, S.A. | 1-(4-(2-((1-(3,4-difluorophenyl)-1H-pyrazol-3-Yl)methoxy)ethyl)piperazin-1- Yl)ethanone salts |
TW201808300A (zh) | 2016-06-06 | 2018-03-16 | 以斯提夫博士實驗室股份有限公司 | σ受體配體在癌症中的用途 |
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 |
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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 |
PL1781618T3 (pl) * | 2004-08-27 | 2013-03-29 | Esteve Labor Dr | Inhibitory receptora sigma |
EP1634872A1 (en) * | 2004-08-27 | 2006-03-15 | Laboratorios Del Dr. Esteve, S.A. | Pyrazole derivatives as sigma receptor inhibitors |
RU2417987C2 (ru) * | 2004-08-27 | 2011-05-10 | Лабораторьос Дель Др.Эстеве, С.А. | Ингибиторы сигма-рецептора |
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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