HRP20161128T1 - 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 Download PDFInfo
- Publication number
- HRP20161128T1 HRP20161128T1 HRP20161128TT HRP20161128T HRP20161128T1 HR P20161128 T1 HRP20161128 T1 HR P20161128T1 HR P20161128T T HRP20161128T T HR P20161128TT HR P20161128 T HRP20161128 T HR P20161128T HR P20161128 T1 HRP20161128 T1 HR P20161128T1
- Authority
- HR
- Croatia
- Prior art keywords
- hydrochloride salt
- naphthalenyl
- pyrazol
- morpholine
- oxy
- Prior art date
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- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 title claims 8
- DGPGXHRHNRYVDH-UHFFFAOYSA-N 4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine Chemical compound N=1N(C=2C=C3C=CC=CC3=CC=2)C(C)=CC=1OCCN1CCOCC1 DGPGXHRHNRYVDH-UHFFFAOYSA-N 0.000 title claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 238000011321 prophylaxis Methods 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims 1
- KWTSXDURSIMDCE-QMMMGPOBSA-N (S)-amphetamine Chemical compound C[C@H](N)CC1=CC=CC=C1 KWTSXDURSIMDCE-QMMMGPOBSA-N 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000016192 Demyelinating disease Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 108090001030 Lipoproteins Proteins 0.000 claims 1
- 102000004895 Lipoproteins Human genes 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims 1
- 229940025084 amphetamine Drugs 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229960003920 cocaine Drugs 0.000 claims 1
- 230000003920 cognitive function Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010013663 drug dependence Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 229960004756 ethanol Drugs 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 229960002715 nicotine Drugs 0.000 claims 1
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 108010085082 sigma receptors Proteins 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- 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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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
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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
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic 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
- A61K31/5375—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
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
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- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/12—Heterocyclic 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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- Health & Medical Sciences (AREA)
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- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Child & Adolescent Psychology (AREA)
- Transplantation (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (6)
1. Hidrokloridna sol, naznačena time što je sol 4-[2-[[5-metil-1-(2-naftalenil)-1H-pirazol-3-il]oksi]etil]morfolina.
2. Postupak priprave hidrokloridne soli u skladu s patentnim zahtjevom 1, naznačen time što obuhvaća:
a) miješanje 4-[2-[[5-metil-1-(2-naftalenil)-1H-pirazol-3-il]oksi]etil]morfolina s otopinom koja sadrži klorovodičnu kiselinu, i
b) izdvajanje dobivene hidrokloridne soli.
3. Farmaceutski pripravak, naznačen time što sadrži hidrokloridnu sol u skladu s patentnim zahtjevom 1.
4. Hidrokloridna sol u skladu s patentnim zahtjevom 1, naznačena time što je namijenjena upotrebi kao medikament.
5. Hidrokloridna sol u skladu s patentnim zahtjevom 1, naznačena time što je namijenjena upotrebi u liječenju i/ili profilaksi bolesti ili stanja kod kojeg posreduje sigma receptor.
6. Hidrokloridna sol u skladu s patentnim zahtjevom 1, naznačena time što je namijenjena upotrebi u liječenju i/ili profilaksi bolesti koju se bira iz skupine koju čine dijareja; lipoproteinski poremećaji; migrena; pretilost; artritis; hipertenzija; aritmija; vrijed; poremećaji učenja, pamćenja i pažnje; poremećaji kognitivnih funkcija; neurodegenerativne bolesti; demijelinizirajuće bolesti; ovisnost o drogama i kemijskim tvarima, uključujući kokain, amfetamin, etanol i nikotin; tardivna diskinezija; ishemijski inzult; epilepsija; inzult; stres; rak; psihotična stanja, osobito depresija, anksioznost ili shizofrenija; upala; ili autoimune bolesti.
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 |
|---|---|
| HRP20161128T1 true HRP20161128T1 (hr) | 2016-11-18 |
Family
ID=43629487
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20161128TT HRP20161128T1 (hr) | 2009-11-25 | 2016-09-02 | Hidrokloridna sol 4-[2-[[5-metil-1-(2-naftalenil)-1h-pirazol-3-il]oksi]etil]morfolina |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US20130143884A1 (hr) |
| EP (1) | EP2503993B1 (hr) |
| JP (1) | JP5794999B2 (hr) |
| KR (2) | KR20170096225A (hr) |
| CN (2) | CN102753154A (hr) |
| AR (1) | AR079198A1 (hr) |
| AU (1) | AU2010323116B2 (hr) |
| BR (1) | BR112012012456A2 (hr) |
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| MY (1) | MY160018A (hr) |
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| RS (1) | RS55099B1 (hr) |
| RU (1) | RU2559325C2 (hr) |
| SI (1) | SI2503993T1 (hr) |
| SM (1) | SMT201600304B (hr) |
| TN (1) | TN2012000247A1 (hr) |
| TW (1) | TWI482767B (hr) |
| WO (1) | WO2011064315A1 (hr) |
| ZA (1) | ZA201203771B (hr) |
Families Citing this family (14)
| 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 |
| KR20160097366A (ko) | 2013-12-17 | 2016-08-17 | 라보라토리오스 델 드라. 에스테브.에스.에이. | 세로토닌-노르에피네프린 재흡수 억제제들(SNRIs) 및 시그마 리셉터 리간드들 조합 |
| WO2015091505A1 (en) | 2013-12-17 | 2015-06-25 | Laboratorios Del Dr. Esteve, S.A. | Gabapentinoids and sigma receptor ligands combinations |
| KR20180048923A (ko) * | 2015-09-02 | 2018-05-10 | 라보라토리오스 델 드라. 에스테브.에스.에이. | 1-(4-(2-((1-(3,4-디플루오로페닐)-1h-피라졸-3-일)메톡시)에틸)피페라진-1- 일)에타논 염들 |
| JP7094231B2 (ja) | 2016-06-06 | 2022-07-01 | エスティーブ ファーマシューティカルズ エス エイ | がんにおけるシグマ受容体リガンドの使用 |
| 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)
| 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 |
| MX2007002341A (es) * | 2004-08-27 | 2007-09-25 | Esteve Labor Dr | Inhibidores del receptor sigma. |
| BRPI0514692A (pt) * | 2004-08-27 | 2008-06-17 | Esteve Labor Dr | inibidores do receptor sigma |
| EP1634872A1 (en) * | 2004-08-27 | 2006-03-15 | Laboratorios Del Dr. Esteve, S.A. | Pyrazole derivatives as sigma receptor inhibitors |
| 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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- 2010-11-25 CN CN2010800608479A patent/CN102753154A/zh active Pending
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- 2010-11-25 ES ES10782303.1T patent/ES2589045T3/es active Active
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- 2010-11-25 BR BR112012012456-0A patent/BR112012012456A2/pt not_active IP Right Cessation
- 2010-11-25 WO PCT/EP2010/068256 patent/WO2011064315A1/en active Application Filing
- 2010-11-25 SI SI201031267A patent/SI2503993T1/sl unknown
- 2010-11-25 CA CA2781744A patent/CA2781744C/en not_active Expired - Fee Related
- 2010-11-25 KR KR1020177022538A patent/KR20170096225A/ko not_active Application Discontinuation
- 2010-11-25 KR KR1020127016392A patent/KR20130004244A/ko not_active Application Discontinuation
- 2010-11-25 AU AU2010323116A patent/AU2010323116B2/en not_active Ceased
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- 2010-11-25 EP EP10782303.1A patent/EP2503993B1/en active Active
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- 2010-11-25 US US13/511,715 patent/US20130143884A1/en not_active Abandoned
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2012
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- 2012-06-25 CO CO12106023A patent/CO6612255A2/es not_active Application Discontinuation
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