ES2733905T3 - Composiciones farmacéuticas que comprenden (3-(1-(1H-imidazol-4-il)etil)-2-metilfenil)metanol - Google Patents
Composiciones farmacéuticas que comprenden (3-(1-(1H-imidazol-4-il)etil)-2-metilfenil)metanol Download PDFInfo
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- ES2733905T3 ES2733905T3 ES17174959T ES17174959T ES2733905T3 ES 2733905 T3 ES2733905 T3 ES 2733905T3 ES 17174959 T ES17174959 T ES 17174959T ES 17174959 T ES17174959 T ES 17174959T ES 2733905 T3 ES2733905 T3 ES 2733905T3
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 28
- HTQCEFAVROSRIW-UHFFFAOYSA-N [3-[1-(1h-imidazol-5-yl)ethyl]-2-methylphenyl]methanol Chemical compound C=1C=CC(CO)=C(C)C=1C(C)C1=CNC=N1 HTQCEFAVROSRIW-UHFFFAOYSA-N 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 52
- 208000002193 Pain Diseases 0.000 claims abstract description 45
- 230000036407 pain Effects 0.000 claims abstract description 29
- 150000003839 salts Chemical class 0.000 claims abstract description 17
- 238000000034 method Methods 0.000 claims abstract description 16
- 208000009935 visceral pain Diseases 0.000 claims abstract description 15
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 7
- 239000000203 mixture Substances 0.000 claims description 27
- 230000001684 chronic effect Effects 0.000 claims description 5
- 206010064147 Gastrointestinal inflammation Diseases 0.000 claims description 4
- 208000004998 Abdominal Pain Diseases 0.000 claims description 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 2
- 206010010774 Constipation Diseases 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- 208000007882 Gastritis Diseases 0.000 claims description 2
- 208000005577 Gastroenteritis Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 2
- 208000007784 diverticulitis Diseases 0.000 claims description 2
- 201000006549 dyspepsia Diseases 0.000 claims description 2
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims description 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Substances OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 22
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- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 16
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- 230000003042 antagnostic effect Effects 0.000 description 1
- 239000008346 aqueous phase Substances 0.000 description 1
- 150000004945 aromatic hydrocarbons Chemical class 0.000 description 1
- 239000012752 auxiliary agent Substances 0.000 description 1
- 230000002146 bilateral effect Effects 0.000 description 1
- 230000036983 biotransformation Effects 0.000 description 1
- 230000005587 bubbling Effects 0.000 description 1
- 239000007975 buffered saline Substances 0.000 description 1
- 229960001948 caffeine Drugs 0.000 description 1
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229940126214 compound 3 Drugs 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- JXMXDKHEZLKQPB-UHFFFAOYSA-N detomidine Chemical compound CC1=CC=CC(CC=2[N]C=NC=2)=C1C JXMXDKHEZLKQPB-UHFFFAOYSA-N 0.000 description 1
- 229960001894 detomidine Drugs 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 229920001971 elastomer Polymers 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 230000001804 emulsifying effect Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 150000002169 ethanolamines Chemical class 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000006260 foam Substances 0.000 description 1
- 235000019256 formaldehyde Nutrition 0.000 description 1
- 239000012458 free base Substances 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- 229960002870 gabapentin Drugs 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 229940074045 glyceryl distearate Drugs 0.000 description 1
- 229940075507 glyceryl monostearate Drugs 0.000 description 1
- 230000009931 harmful effect Effects 0.000 description 1
- 125000000623 heterocyclic group Chemical group 0.000 description 1
- 150000003840 hydrochlorides Chemical class 0.000 description 1
- 230000033444 hydroxylation Effects 0.000 description 1
- 238000005805 hydroxylation reaction Methods 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 150000007529 inorganic bases Chemical class 0.000 description 1
- 229910001410 inorganic ion Inorganic materials 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 229910052744 lithium Inorganic materials 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- CCERQOYLJJULMD-UHFFFAOYSA-M magnesium;carbanide;chloride Chemical compound [CH3-].[Mg+2].[Cl-] CCERQOYLJJULMD-UHFFFAOYSA-M 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000005399 mechanical ventilation Methods 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- GBMDVOWEEQVZKZ-UHFFFAOYSA-N methanol;hydrate Chemical compound O.OC GBMDVOWEEQVZKZ-UHFFFAOYSA-N 0.000 description 1
- -1 mono- Chemical class 0.000 description 1
- 210000001640 nerve ending Anatomy 0.000 description 1
- 210000000929 nociceptor Anatomy 0.000 description 1
- 108091008700 nociceptors Proteins 0.000 description 1
- 229960002748 norepinephrine Drugs 0.000 description 1
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 description 1
- 239000010502 orange oil Substances 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- 239000006179 pH buffering agent Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 238000005192 partition Methods 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229920001983 poloxamer Polymers 0.000 description 1
- 229920001515 polyalkylene glycol Polymers 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 229940087659 precedex Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 229940125723 sedative agent Drugs 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 229940035044 sorbitan monolaurate Drugs 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000012257 stirred material Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 125000003944 tolyl group Chemical group 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- 125000005270 trialkylamine group Chemical group 0.000 description 1
- 229940117013 triethanolamine oleate Drugs 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 229960004418 trolamine Drugs 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 208000019206 urinary tract infection Diseases 0.000 description 1
- 210000001835 viscera Anatomy 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
-
- 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
- A61K31/4164—1,3-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- 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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15249409P | 2009-02-13 | 2009-02-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2733905T3 true ES2733905T3 (es) | 2019-12-03 |
Family
ID=42083967
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES17174959T Active ES2733905T3 (es) | 2009-02-13 | 2010-02-12 | Composiciones farmacéuticas que comprenden (3-(1-(1H-imidazol-4-il)etil)-2-metilfenil)metanol |
| ES19168102T Active ES2880578T3 (es) | 2009-02-13 | 2010-02-12 | Composiciones farmacéuticas que comprenden (3-(1-(1H-imidazol-4-il)etil)-2-metilfenil)metanol |
| ES10706824.9T Active ES2649018T3 (es) | 2009-02-13 | 2010-02-12 | Composiciones farmacéuticas que comprenden (3-(1-(1H-imidazol-4-il)etil)-2-metilfenil)metanol |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES19168102T Active ES2880578T3 (es) | 2009-02-13 | 2010-02-12 | Composiciones farmacéuticas que comprenden (3-(1-(1H-imidazol-4-il)etil)-2-metilfenil)metanol |
| ES10706824.9T Active ES2649018T3 (es) | 2009-02-13 | 2010-02-12 | Composiciones farmacéuticas que comprenden (3-(1-(1H-imidazol-4-il)etil)-2-metilfenil)metanol |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US20110301214A1 (https=) |
| EP (3) | EP3241553B1 (https=) |
| JP (1) | JP2012518007A (https=) |
| AU (1) | AU2010213580A1 (https=) |
| CA (1) | CA2752148A1 (https=) |
| DK (1) | DK3566703T3 (https=) |
| ES (3) | ES2733905T3 (https=) |
| HK (1) | HK1246204B (https=) |
| WO (1) | WO2010093930A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8653123B2 (en) * | 2010-09-16 | 2014-02-18 | Allergan, Inc. | Ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl] methanol for treating retinal diseases |
| CA2818144C (en) | 2010-11-16 | 2020-09-22 | Allergan, Inc. | Pharmaceutical compositions comprising (3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl)methanol |
| JP2014521643A (ja) * | 2011-07-22 | 2014-08-28 | アラーガン インコーポレイテッド | 眼の中枢視覚投影によって媒介される視覚障害を治療するためのα−2アドレナリン調節剤 |
| AU2012340806B2 (en) | 2011-11-21 | 2017-10-19 | Allergan, Inc. | Pharmaceutical compositions comprising 4-[1-(2,3-dimethylphenyl)ethyl]-3H-imidazole derivatives for treating retinal diseases |
| EP4642453A1 (en) * | 2022-12-27 | 2025-11-05 | Alceptor Therapeutics, Inc. | (s)-(3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl)methanol for treatment of agitation |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4166452A (en) | 1976-05-03 | 1979-09-04 | Generales Constantine D J Jr | Apparatus for testing human responses to stimuli |
| US4256108A (en) | 1977-04-07 | 1981-03-17 | Alza Corporation | Microporous-semipermeable laminated osmotic system |
| US4265874A (en) | 1980-04-25 | 1981-05-05 | Alza Corporation | Method of delivering drug with aid of effervescent activity generated in environment of use |
| GB2215206B (en) * | 1988-02-29 | 1991-07-03 | Farmos Oy | 4-substituted imidazole derivatives useful in perioperative care |
| US5344840A (en) | 1988-02-29 | 1994-09-06 | Orion-Yhtyma Oy | 4-substituted imidazole derivatives useful in perioperative care |
| FI894911A0 (fi) | 1989-10-17 | 1989-10-17 | Farmos Oy | En terapeutiskt vaerdefull foerening. |
| UA78529C2 (en) * | 2001-10-10 | 2007-04-10 | Wyeth Corp | Derivatives of [[2-(amino-3,4-dioxo-1-cyclobutene-1-yl)amino]alkyl] acid for treating pain |
| US8653123B2 (en) * | 2010-09-16 | 2014-02-18 | Allergan, Inc. | Ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl] methanol for treating retinal diseases |
| CA2818144C (en) | 2010-11-16 | 2020-09-22 | Allergan, Inc. | Pharmaceutical compositions comprising (3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl)methanol |
| AU2012340806B2 (en) | 2011-11-21 | 2017-10-19 | Allergan, Inc. | Pharmaceutical compositions comprising 4-[1-(2,3-dimethylphenyl)ethyl]-3H-imidazole derivatives for treating retinal diseases |
-
2010
- 2010-02-12 ES ES17174959T patent/ES2733905T3/es active Active
- 2010-02-12 EP EP17174959.1A patent/EP3241553B1/en active Active
- 2010-02-12 ES ES19168102T patent/ES2880578T3/es active Active
- 2010-02-12 DK DK19168102.2T patent/DK3566703T3/da active
- 2010-02-12 US US13/147,760 patent/US20110301214A1/en not_active Abandoned
- 2010-02-12 CA CA2752148A patent/CA2752148A1/en not_active Abandoned
- 2010-02-12 EP EP19168102.2A patent/EP3566703B1/en active Active
- 2010-02-12 EP EP10706824.9A patent/EP2395999B1/en active Active
- 2010-02-12 JP JP2011550276A patent/JP2012518007A/ja active Pending
- 2010-02-12 ES ES10706824.9T patent/ES2649018T3/es active Active
- 2010-02-12 AU AU2010213580A patent/AU2010213580A1/en not_active Abandoned
- 2010-02-12 WO PCT/US2010/024111 patent/WO2010093930A1/en not_active Ceased
-
2014
- 2014-11-21 US US14/550,647 patent/US9193690B2/en active Active
-
2015
- 2015-10-19 US US14/886,457 patent/US9555021B2/en active Active
-
2018
- 2018-05-08 HK HK18105920.4A patent/HK1246204B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2010213580A1 (en) | 2011-09-08 |
| US9555021B2 (en) | 2017-01-31 |
| JP2012518007A (ja) | 2012-08-09 |
| ES2880578T3 (es) | 2021-11-24 |
| US20110301214A1 (en) | 2011-12-08 |
| EP3566703B1 (en) | 2021-04-07 |
| WO2010093930A1 (en) | 2010-08-19 |
| US9193690B2 (en) | 2015-11-24 |
| ES2649018T3 (es) | 2018-01-09 |
| CA2752148A1 (en) | 2010-08-19 |
| DK3566703T3 (da) | 2021-07-05 |
| EP2395999A1 (en) | 2011-12-21 |
| EP3241553B1 (en) | 2019-04-10 |
| EP3241553A1 (en) | 2017-11-08 |
| US20160038466A1 (en) | 2016-02-11 |
| EP3566703A1 (en) | 2019-11-13 |
| HK1246204B (en) | 2020-02-07 |
| EP2395999B1 (en) | 2017-09-13 |
| US20150080445A1 (en) | 2015-03-19 |
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