ES2651389T3 - Composiciones que comprenden benzodiazepinas de acción corta - Google Patents
Composiciones que comprenden benzodiazepinas de acción corta Download PDFInfo
- Publication number
- ES2651389T3 ES2651389T3 ES13730128.9T ES13730128T ES2651389T3 ES 2651389 T3 ES2651389 T3 ES 2651389T3 ES 13730128 T ES13730128 T ES 13730128T ES 2651389 T3 ES2651389 T3 ES 2651389T3
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- ES
- Spain
- Prior art keywords
- compositions
- short
- hydroxyalkyl
- alkyl
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
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- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
- C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
- C07D243/24—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/40—Cyclodextrins; Derivatives thereof
Abstract
Una composición liofilizada o secada por pulverización que comprende al menos una benzodiazepina de acuerdo con la fórmula (I) **Fórmula** con W es H; X es CH2; n es 1; Y es CH2; m es 1; Z es O; R1 es CH3, CH2CH3, CH2CH2CH3, CH(CH3)2 o CH2CH(CH3)2; R2 es 2-fluorofenilo, 2-clorofenilo o 2-piridilo; R3 es Cl o Br; R4, R5 y R8 forman el grupo -CR8>=U-V>= en donde R8 es hidrógeno, alquilo C1-4 o hidroxialquilo C1-3, U es N o CR9 en donde R9 es H, alquilo C1-4, hidroxialquilo C1-3 o alcoxi C1-4, V es N o CH y p es cero o una sal farmacéuticamente aceptable de esta, en donde la composición comprende al menos un excipiente higroscópico farmacéuticamente aceptable, en donde el excipiente 30 higroscópico es un carbohidrato seleccionado del grupo que consiste en disacáridos y dextrano y opcionalmente la composición es al menos en parte amorfa.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12168968 | 2012-05-22 | ||
| EP12168968 | 2012-05-22 | ||
| PCT/EP2013/060543 WO2013174883A1 (en) | 2012-05-22 | 2013-05-22 | Compositions comprising short-acting benzodiazepines |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2651389T3 true ES2651389T3 (es) | 2018-01-26 |
Family
ID=48669863
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES13730128.9T Active ES2651389T3 (es) | 2012-05-22 | 2013-05-22 | Composiciones que comprenden benzodiazepinas de acción corta |
Country Status (42)
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2081921E (pt) | 2006-07-10 | 2010-12-10 | Paion Uk Ltd | Sais de benzodiazepina de acção curta e suas formas polimórficas |
| EP2305647A1 (en) | 2009-09-18 | 2011-04-06 | PAION UK Limited | Process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4 H-imidazo[1,2-a][1,4]benzodiazepine-4-yl] propionic acid methyl ester or the benzene sulfonate salt thereof, and compounds useful in that process |
| EP2450039A1 (en) | 2010-11-08 | 2012-05-09 | PAION UK Ltd. | Dosing regimen for sedation with CNS 7056 (Remimazolam) |
| AR094963A1 (es) | 2013-03-04 | 2015-09-09 | Ono Pharmaceutical Co | Reacción de oxidación excelente en el índice de conversión |
| WO2015076340A1 (ja) * | 2013-11-21 | 2015-05-28 | 小野薬品工業株式会社 | 全身麻酔および／または鎮静のための注射用組成物 |
| MX370298B (es) | 2014-02-10 | 2019-12-09 | Biolumic Ltd | Mejoras en, y relacionadas con, características de control de organismos fotosintéticos. |
| CN111615947B (zh) | 2014-03-14 | 2021-08-17 | 拜欧卢米克有限公司 | 提高作物产量和/或质量的方法 |
| US9994578B2 (en) | 2014-07-23 | 2018-06-12 | Jiangsu Nhwaluokang Pharmceutical Research And Development Co., Ltd | Benzodiazepine derivative and use thereof |
| CN107105625A (zh) | 2014-09-17 | 2017-08-29 | 拜欧卢米克有限公司 | 种子处理的方法及所得产物 |
| CN105726495B (zh) * | 2014-12-12 | 2019-03-29 | 宜昌人福药业有限责任公司 | 一种注射用短效苯并二氮杂卓盐药物组合物及其制备方法 |
| CN107198691A (zh) * | 2016-03-17 | 2017-09-26 | 江苏恒瑞医药股份有限公司 | 一种瑞马唑仑的药物组合物 |
| US20190175613A1 (en) * | 2016-04-14 | 2019-06-13 | Paion Uk Limited | Orally inhaled and nasal benzodiazepines |
| CN108289897B (zh) * | 2016-05-20 | 2020-07-28 | 江苏恒瑞医药股份有限公司 | 一种瑞马唑仑的药物组合物 |
| US11147221B2 (en) | 2016-08-22 | 2021-10-19 | Biolumic Limited | Methods of seed treatment and resulting products |
| CN108503644B (zh) | 2016-12-09 | 2019-06-14 | 成都倍特药业有限公司 | 一种苯并二氮杂*衍生物的氢溴酸盐及其制备方法和用途 |
| EP3714884A1 (en) | 2019-03-27 | 2020-09-30 | Paion UK Limited | Medical uses for benzodiazepines with a particular eeg pattern |
| CN112209932B (zh) * | 2019-07-12 | 2023-03-24 | 成都倍特药业股份有限公司 | 一种化合物氢溴酸盐的新固体形态及其制备方法和用途 |
| ES2803099B2 (es) * | 2019-07-22 | 2021-11-08 | Moehs Iberica Sl | Procedimiento de obtención de besilato de remimazolam amorfo |
| CN114478535B (zh) * | 2020-10-23 | 2024-02-09 | 成都苑东生物制药股份有限公司 | 一种苯磺酸瑞马唑仑ii晶型的制备方法 |
| CN112462015B (zh) * | 2020-11-18 | 2022-07-12 | 海南倍特药业有限公司 | 一种氢溴酸瑞马唑仑细菌内毒素的检测方法 |
| CN114624351B (zh) * | 2020-12-14 | 2024-04-09 | 宜昌人福药业有限责任公司 | 苯磺酸瑞马唑仑原料药中(r)-(-)-1-氨基-2-丙醇残留的分析方法 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3520877A (en) * | 1967-10-02 | 1970-07-21 | Hoffmann La Roche | 3-carbonyl amino acetic acid ethyl ester substituted benzodiazepines |
| CA2143246C (en) | 1994-03-16 | 2000-08-22 | Thierry Godel | Imidazodiazepines |
| CN1168140A (zh) | 1995-01-06 | 1997-12-17 | 弗·哈夫曼-拉罗切有限公司 | 羟甲基咪唑并二氮杂䓬及其酯 |
| WO1996023790A1 (de) | 1995-02-02 | 1996-08-08 | F. Hoffmann-La Roche Ag | Acetylimidazobenzodiazepine |
| JPH0971533A (ja) * | 1995-06-30 | 1997-03-18 | Takeda Chem Ind Ltd | 凍結乾燥製剤 |
| GB9911152D0 (en) * | 1999-05-14 | 1999-07-14 | Glaxo Group Ltd | Short-acting benzodiazepines |
| US7160880B1 (en) * | 1999-05-14 | 2007-01-09 | Cenes Limited | Short-acting benzodiazepines |
| TWI233805B (en) * | 1999-07-01 | 2005-06-11 | Fujisawa Pharmaceutical Co | Stabilized pharmaceutical composition in lyophilized form as antifungal agent |
| EP1161949A1 (en) * | 2000-06-09 | 2001-12-12 | Warner-Lambert Company | Use od diazepinoindoles for the treatment of chronic obstructive pulmonary disease |
| EP1853234A2 (en) * | 2005-02-15 | 2007-11-14 | Elan Pharma International Limited | Aerosol and injectable formulations of nanoparticulate benzodiazepine |
| PT2081921E (pt) | 2006-07-10 | 2010-12-10 | Paion Uk Ltd | Sais de benzodiazepina de acção curta e suas formas polimórficas |
| GB0613693D0 (en) * | 2006-07-10 | 2006-08-16 | Cenes Ltd | Benzodiazepine salts (3) |
| GB0613692D0 (en) * | 2006-07-10 | 2006-08-16 | Cenes Ltd | Benzodiazepine salts |
| CN101352422B (zh) * | 2008-09-17 | 2011-04-20 | 厦门朝阳生物工程有限公司 | 河豚毒素冻干粉针制剂及其制备方法 |
| ME02356B (me) * | 2009-11-05 | 2016-06-20 | Glaxosmithkline Llc | Inhibitor bromodomena benzodiazepina |
| EP2450039A1 (en) * | 2010-11-08 | 2012-05-09 | PAION UK Ltd. | Dosing regimen for sedation with CNS 7056 (Remimazolam) |
| CN102964349A (zh) * | 2011-08-31 | 2013-03-13 | 江苏恒瑞医药股份有限公司 | 苯并二氮杂*衍生物的托西酸盐及其多晶型、它们的制备方法和用途 |
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2013
- 2013-05-22 MX MX2014014225A patent/MX368854B/es active IP Right Grant
- 2013-05-22 MY MYPI2014003222A patent/MY185117A/en unknown
- 2013-05-22 EP EP13730128.9A patent/EP2852389B1/en active Active
- 2013-05-22 AP AP2014008084A patent/AP2014008084A0/xx unknown
- 2013-05-22 US US14/402,590 patent/US20150148338A1/en not_active Abandoned
- 2013-05-22 DK DK13730128.9T patent/DK2852389T3/en active
- 2013-05-22 SI SI201330840T patent/SI2852389T1/en unknown
- 2013-05-22 BR BR112014029108-0A patent/BR112014029108B1/pt active IP Right Grant
- 2013-05-22 EA EA201492160A patent/EA032119B1/ru unknown
- 2013-05-22 HU HUE13730128A patent/HUE037734T2/hu unknown
- 2013-05-22 WO PCT/EP2013/060543 patent/WO2013174883A1/en active Application Filing
- 2013-05-22 MA MA37581A patent/MA37581B1/fr unknown
- 2013-05-22 AR ARP130101779A patent/AR092008A1/es not_active Application Discontinuation
- 2013-05-22 NZ NZ702063A patent/NZ702063A/en unknown
- 2013-05-22 CN CN201810206738.1A patent/CN108578413A/zh active Pending
- 2013-05-22 NO NO13730128A patent/NO2852389T3/no unknown
- 2013-05-22 JP JP2015513164A patent/JP6313286B2/ja active Active
- 2013-05-22 SG SG11201407710VA patent/SG11201407710VA/en unknown
- 2013-05-22 TW TW102118175A patent/TWI590826B/zh active
- 2013-05-22 ES ES13730128.9T patent/ES2651389T3/es active Active
- 2013-05-22 RS RS20171260A patent/RS56660B1/sr unknown
- 2013-05-22 CN CN201380036582.2A patent/CN104968348B/zh active Active
- 2013-05-22 GE GEAP201313666A patent/GEP20186852B/en unknown
- 2013-05-22 PL PL13730128T patent/PL2852389T4/pl unknown
- 2013-05-22 PT PT137301289T patent/PT2852389T/pt unknown
- 2013-05-22 KR KR1020147036021A patent/KR102116737B1/ko active Protection Beyond IP Right Term
- 2013-05-22 AU AU2013265295A patent/AU2013265295B2/en active Active
- 2013-05-22 CA CA2874247A patent/CA2874247C/en active Active
- 2013-05-22 UA UAA201413655A patent/UA115063C2/uk unknown
- 2013-05-22 PE PE2014002207A patent/PE20150683A1/es active IP Right Grant
- 2013-05-22 LT LTEP13730128.9T patent/LT2852389T/lt unknown
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2014
- 2014-11-18 ZA ZA2014/08412A patent/ZA201408412B/en unknown
- 2014-11-18 TN TN2014000479A patent/TN2014000479A1/fr unknown
- 2014-11-19 IL IL235789A patent/IL235789B/en active IP Right Grant
- 2014-11-21 PH PH12014502608A patent/PH12014502608A1/en unknown
- 2014-11-21 CL CL2014003171A patent/CL2014003171A1/es unknown
- 2014-11-24 CO CO14258220A patent/CO7151503A2/es unknown
- 2014-12-19 EC ECIEPI201432553A patent/ECSP14032553A/es unknown
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2015
- 2015-09-09 HK HK15108782.8A patent/HK1208164A1/xx unknown
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2017
- 2017-12-04 HR HRP20171872TT patent/HRP20171872T1/hr unknown
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2021
- 2021-08-16 US US17/402,730 patent/US20220040198A1/en active Pending
- 2021-09-17 LT LTPA2021521C patent/LTPA2021521I1/lt unknown
- 2021-09-20 LU LU00230C patent/LUC00230I2/fr unknown
- 2021-09-20 HU HUS2100040C patent/HUS2100040I1/hu unknown
- 2021-09-20 FR FR21C1043C patent/FR21C1043I2/fr active Active
- 2021-09-20 NO NO2021041C patent/NO2021041I1/no unknown
- 2021-09-21 NL NL301130C patent/NL301130I2/nl unknown
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