AR080133A1 - Clorhidrato de 4-(-2-((5-metil-1-(2-naftalenil)-1h-pirazol-3-il)oxi)etil)morfolina y formas cristalinas del mismo - Google Patents
Clorhidrato de 4-(-2-((5-metil-1-(2-naftalenil)-1h-pirazol-3-il)oxi)etil)morfolina y formas cristalinas del mismoInfo
- Publication number
- AR080133A1 AR080133A1 ARP110100380A ARP110100380A AR080133A1 AR 080133 A1 AR080133 A1 AR 080133A1 AR P110100380 A ARP110100380 A AR P110100380A AR P110100380 A ARP110100380 A AR P110100380A AR 080133 A1 AR080133 A1 AR 080133A1
- Authority
- AR
- Argentina
- Prior art keywords
- 2theta
- degrees
- approximately
- diffraction pattern
- ray powder
- Prior art date
Links
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 title 2
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 6
- 239000012453 solvate Substances 0.000 abstract 3
- 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 abstract 2
- 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 abstract 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 abstract 2
- 239000007787 solid Substances 0.000 abstract 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 abstract 1
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 abstract 1
- 229910052802 copper Inorganic materials 0.000 abstract 1
- 239000010949 copper Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000005855 radiation Effects 0.000 abstract 1
Classifications
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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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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
La presente se refiere a polimorfos y solvatos de la sal de clorhidrato de 4-[2-[[5-metil-1-(2-naftalenil)-1H-pirazol-3-il]oxi]etil]morfolina (P027), a procedimientos para su preparacion, a su uso para preparar la forma de fase I, y a composiciones farmacéuticas que los comprenden. Reivindicacion 1: Forma solida polimorfica o solvatada de la sal de clorhidrato de 4-[2-[[5-metil-1-(2-naftalenil)-1H-pirazol-3-il]oxi]etil]morfolina. Reivindicacion 2: Forma solida segun la reivindicacion 1 seleccionada del grupo que consiste en: a) una forma de fase I polimorfica, que tiene un patron de difraccion de polvo de rayos X que muestra picos característicos a un ángulo de reflexion [2theta en grados] de aproximadamente 5,9, 8,1, 11,3, 11,7, 14,2, 15,1, 15,8, 16,3, 16,8, 17,8, 18,1, 18,6, 19,8, 20,9, 21,9, 22,8, 23,0, 23,2, 23,6, 23,9, 24,3, 25,0, 25,1, 28,0, 28,3, 28,6, 29,0, 29,2, 30,7 y 30,9; b) una forma de fase II polimorfica, que tiene un patron de difraccion de polvo de rayos X que muestra picos característicos a un ángulo de reflexion [2theta en grados] de aproximadamente 5,776, 11,629, 14,558, 15,737, 15,891, 16,420, 16,740, 17,441, 17,635, 18, 056, 18,219, 19,232, 19, 712, 20, 140, 20,685, 21,135, 21,889, 22,108, 22,478, 22,763, 23,219, 23,454, 23,782, 24,689, 25,065 y 25,671; c) una forma de fase III polimorfica, que tiene un patron de difraccion de polvo de rayos X que muestra picos característicos a un ángulo de reflexion [2theta en grados] de aproximadamente 5,437, 5,714, 10,918, 11,546, 12,704, 13,344, 13,984, 14,505, 15,606, 15,824, 16,164, 16,646, 17,333, 17,837, 18,719, 18,878, 19,236, 19,533, 20,142, 20,689, 21,337, 22,008, 22,929, 23,596, 24,748, 25,064, 25,207, 25, 737 y 26, 148; d) una forma de fase IV polimorfica, que tiene un patron de difraccion de polvo de rayos X que muestra picos característicos a un ángulo de reflexion [2theta en grados] de aproximadamente 5,805, 11,685, 15,559, 15,804, 16,397, 16,879, 17,357, 17,465, 17,621, 19,112, 19,435, 19,923, 21,224, 21,987, 22,167, 22,412, 22,852, 23,059, 23,359, 23,855, 24,092, 25,722, 26,054, 26,649 y 27,780; e) un solvato de dioxano que tiene un patron de difraccion de polvo de rayos X que muestra picos característicos a un ángulo de reflexion [2theta en grados] de aproximadamente 4,734, 9,317, 11,390, 13,614, 14,290, 14,815, 16,211, 16,432, 16,782, 17, 741, 18, 056, 18, 329, 18, 724, 19, 070, 19, 494, 20,436, 20,762, 21,587, 22,000, 22,935, 23,084, 23,551, 23,891, 24,721 y 25,078; y f) un solvato de cloroformo que tiene un patron de difraccion de polvo de rayos X que muestra picos característicos a un ángulo de reflexion [2theta en grados] de aproximadamente 11,370, 13,396, 14,048, 15, 010, 15, 303, 16,117, 16, 804, 17, 040, 17, 830, 18,029, 18,661, 18,859, 19,190, 20,150, 20,434, 21,424, 22,279, 22,871, 23,449, 23,918, 24,343, 24,709, 24,820, 25,459 y 26,199; obteniéndose los valores de 2theta usando radiacion de cobre (CuKalfa1 1,54060 L).
Applications Claiming Priority (2)
| 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080133A1 true AR080133A1 (es) | 2012-03-14 |
Family
ID=43897079
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100380A AR080133A1 (es) | 2010-02-04 | 2011-02-04 | Clorhidrato de 4-(-2-((5-metil-1-(2-naftalenil)-1h-pirazol-3-il)oxi)etil)morfolina y formas cristalinas del mismo |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US9051275B2 (es) |
| EP (1) | EP2531177B8 (es) |
| JP (1) | JP5894086B2 (es) |
| KR (2) | KR20120123532A (es) |
| CN (1) | CN102753155B (es) |
| AR (1) | AR080133A1 (es) |
| AU (1) | AU2011212476B2 (es) |
| BR (1) | BR112012018958A8 (es) |
| CA (1) | CA2788024C (es) |
| CO (1) | CO6592093A2 (es) |
| CY (1) | CY1117886T1 (es) |
| DK (1) | DK2531177T3 (es) |
| EC (1) | ECSP12012039A (es) |
| ES (1) | ES2586212T3 (es) |
| HR (1) | HRP20160937T1 (es) |
| HU (1) | HUE029738T2 (es) |
| IL (1) | IL221277A (es) |
| MA (1) | MA34047B1 (es) |
| ME (1) | ME02483B (es) |
| MX (1) | MX339193B (es) |
| NZ (1) | NZ601316A (es) |
| PH (1) | PH12012501510A1 (es) |
| PL (1) | PL2531177T3 (es) |
| PT (1) | PT2531177T (es) |
| RS (1) | RS55046B1 (es) |
| RU (1) | RU2560150C2 (es) |
| SG (2) | SG10201500832PA (es) |
| SI (1) | SI2531177T1 (es) |
| SM (1) | SMT201600264B (es) |
| TN (1) | TN2012000347A1 (es) |
| TW (1) | TWI568729B (es) |
| WO (1) | WO2011095579A1 (es) |
Families Citing this family (18)
| 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 |
| 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 |
| 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 |
| TW201206893A (en) | 2010-07-09 | 2012-02-16 | Abbott Healthcare Products Bv | Bisaryl (thio) morpholine derivatives as S1P modulators |
| 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 |
| 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 |
| CA2933511A1 (en) | 2013-12-17 | 2015-06-25 | Laboratorios Del Dr. Esteve, S.A. | Serotonin-norepinephrine reuptake inhibitors (snris) and sigma receptor ligands combinations |
| 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 |
| EP4051683A1 (en) | 2019-10-31 | 2022-09-07 | Escape Bio, Inc. | Solid forms of an s1p-receptor modulator |
Family Cites Families (6)
| 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 |
| US7696199B2 (en) * | 2004-08-27 | 2010-04-13 | Laboratorios Del Dr. Esteve, S.A. | Sigma receptor inhibitors |
| JP2009528315A (ja) * | 2006-03-01 | 2009-08-06 | 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 | シグマ受容体阻害剤としてのピラゾール誘導体 |
| 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 |
-
2011
- 2011-02-04 HU HUE11702056A patent/HUE029738T2/en unknown
- 2011-02-04 AR ARP110100380A patent/AR080133A1/es unknown
- 2011-02-04 ME MEP-2016-154A patent/ME02483B/me unknown
- 2011-02-04 RS RS20160612A patent/RS55046B1/sr unknown
- 2011-02-04 US US13/577,078 patent/US9051275B2/en not_active Ceased
- 2011-02-04 KR KR1020127023081A patent/KR20120123532A/ko not_active Ceased
- 2011-02-04 JP JP2012551631A patent/JP5894086B2/ja active Active
- 2011-02-04 AU AU2011212476A patent/AU2011212476B2/en not_active Ceased
- 2011-02-04 EP EP11702056.0A patent/EP2531177B8/en active Active
- 2011-02-04 WO PCT/EP2011/051630 patent/WO2011095579A1/en not_active Ceased
- 2011-02-04 MA MA35183A patent/MA34047B1/fr unknown
- 2011-02-04 CN CN201180008354.5A patent/CN102753155B/zh active Active
- 2011-02-04 BR BR112012018958A patent/BR112012018958A8/pt not_active Application Discontinuation
- 2011-02-04 PT PT117020560T patent/PT2531177T/pt unknown
- 2011-02-04 SI SI201130895A patent/SI2531177T1/sl unknown
- 2011-02-04 ES ES11702056.0T patent/ES2586212T3/es active Active
- 2011-02-04 DK DK11702056.0T patent/DK2531177T3/en active
- 2011-02-04 NZ NZ601316A patent/NZ601316A/en not_active IP Right Cessation
- 2011-02-04 RU RU2012137495/04A patent/RU2560150C2/ru not_active IP Right Cessation
- 2011-02-04 SG SG10201500832PA patent/SG10201500832PA/en unknown
- 2011-02-04 PL PL11702056.0T patent/PL2531177T3/pl unknown
- 2011-02-04 CA CA2788024A patent/CA2788024C/en not_active Expired - Fee Related
- 2011-02-04 US US15/616,347 patent/USRE47214E1/en active Active
- 2011-02-04 MX MX2012009018A patent/MX339193B/es active IP Right Grant
- 2011-02-04 HR HRP20160937TT patent/HRP20160937T1/hr unknown
- 2011-02-04 PH PH1/2012/501510A patent/PH12012501510A1/en unknown
- 2011-02-04 KR KR1020187015725A patent/KR20180063379A/ko not_active Ceased
- 2011-02-04 SG SG2012053724A patent/SG182628A1/en unknown
- 2011-02-08 TW TW100104115A patent/TWI568729B/zh not_active IP Right Cessation
-
2012
- 2012-07-04 TN TNP2012000347A patent/TN2012000347A1/en unknown
- 2012-07-13 EC ECSP12012039 patent/ECSP12012039A/es unknown
- 2012-08-02 IL IL221277A patent/IL221277A/en not_active IP Right Cessation
- 2012-09-04 CO CO12151303A patent/CO6592093A2/es not_active Application Discontinuation
-
2016
- 2016-08-04 SM SM201600264T patent/SMT201600264B/it unknown
- 2016-08-08 CY CY20161100779T patent/CY1117886T1/el unknown
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