EA032119B1 - Композиции, содержащие бензодиазепины короткого действия - Google Patents

Композиции, содержащие бензодиазепины короткого действия Download PDF

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Publication number
EA032119B1
EA032119B1 EA201492160A EA201492160A EA032119B1 EA 032119 B1 EA032119 B1 EA 032119B1 EA 201492160 A EA201492160 A EA 201492160A EA 201492160 A EA201492160 A EA 201492160A EA 032119 B1 EA032119 B1 EA 032119B1
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EA
Eurasian Patent Office
Prior art keywords
composition
dextran
lyophilized
lactose
benzodiazepine
Prior art date
Application number
EA201492160A
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English (en)
Russian (ru)
Other versions
EA201492160A1 (ru
Inventor
Джон Эйткен Грэхем
Алан Джеймс Бэйлли
Кевин Ричард Уорд
Томас Пикок
Original Assignee
ПАЙОН ЮКей ЛИМИТЕД
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Application filed by ПАЙОН ЮКей ЛИМИТЕД filed Critical ПАЙОН ЮКей ЛИМИТЕД
Publication of EA201492160A1 publication Critical patent/EA201492160A1/ru
Publication of EA032119B1 publication Critical patent/EA032119B1/ru

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Classifications

    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
EA201492160A 2012-05-22 2013-05-22 Композиции, содержащие бензодиазепины короткого действия EA032119B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12168968 2012-05-22
PCT/EP2013/060543 WO2013174883A1 (en) 2012-05-22 2013-05-22 Compositions comprising short-acting benzodiazepines

Publications (2)

Publication Number Publication Date
EA201492160A1 EA201492160A1 (ru) 2015-10-30
EA032119B1 true EA032119B1 (ru) 2019-04-30

Family

ID=48669863

Family Applications (1)

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EA201492160A EA032119B1 (ru) 2012-05-22 2013-05-22 Композиции, содержащие бензодиазепины короткого действия

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Country Link
US (2) US20150148338A1 (enExample)
EP (1) EP2852389B1 (enExample)
JP (1) JP6313286B2 (enExample)
KR (1) KR102116737B1 (enExample)
CN (2) CN108578413A (enExample)
AP (1) AP2014008084A0 (enExample)
AR (1) AR092008A1 (enExample)
AU (1) AU2013265295B2 (enExample)
BR (1) BR112014029108B1 (enExample)
CA (1) CA2874247C (enExample)
CL (1) CL2014003171A1 (enExample)
CO (1) CO7151503A2 (enExample)
DK (1) DK2852389T3 (enExample)
EA (1) EA032119B1 (enExample)
EC (1) ECSP14032553A (enExample)
ES (1) ES2651389T3 (enExample)
FR (1) FR21C1043I2 (enExample)
GE (1) GEP20186852B (enExample)
HR (1) HRP20171872T1 (enExample)
HU (2) HUE037734T2 (enExample)
IL (1) IL235789B (enExample)
LT (2) LT2852389T (enExample)
LU (1) LUC00230I2 (enExample)
MA (1) MA37581B1 (enExample)
MX (1) MX368854B (enExample)
MY (1) MY185117A (enExample)
NL (1) NL301130I2 (enExample)
NO (2) NO2852389T3 (enExample)
NZ (1) NZ702063A (enExample)
PE (1) PE20150683A1 (enExample)
PH (1) PH12014502608B1 (enExample)
PL (1) PL2852389T4 (enExample)
PT (1) PT2852389T (enExample)
RS (1) RS56660B1 (enExample)
SG (1) SG11201407710VA (enExample)
SI (1) SI2852389T1 (enExample)
TN (1) TN2014000479A1 (enExample)
TW (1) TWI590826B (enExample)
UA (1) UA115063C2 (enExample)
WO (1) WO2013174883A1 (enExample)
ZA (1) ZA201408412B (enExample)

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DK2081921T3 (da) 2006-07-10 2011-01-03 Paion Uk Ltd Korttidsvirkende benzodiazepinsalte og deres polymorfe former
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
JP6767881B2 (ja) 2014-02-10 2020-10-14 バイオルミック リミテッド 光合成生物の特徴の改善、及びそれに関する制御
AU2015230049B2 (en) 2014-03-14 2018-07-26 Biolumic Limited Method to improve crop yield and/or quality
PL3162804T3 (pl) * 2014-07-23 2020-04-30 Jiangsu Nhwaluokang Pharmaceutical Research And Development Co., Ltd. Nowa pochodna benzodiazepiny i jej zastosowanie
JP2017529076A (ja) 2014-09-17 2017-10-05 バイオルミック リミテッド 種子処理の方法およびその結果として得られる生産物
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
WO2017178663A1 (en) * 2016-04-14 2017-10-19 Paion Uk Limited Orally inhaled and nasal benzodiazepines
WO2017198224A1 (zh) * 2016-05-20 2017-11-23 江苏恒瑞医药股份有限公司 一种瑞马唑仑的药物组合物
WO2018037281A1 (en) 2016-08-22 2018-03-01 Biolumic Limited System, device and methods of seed treatment
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
MX2019015877A (es) 2017-06-29 2020-08-06 Biolumic Ltd Método para mejorar el rendimiento o la calidad de los cultivos.
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
EP4633600A1 (en) * 2022-12-16 2025-10-22 LTS Lohmann Therapie-Systeme AG Oromucosal delivery system containing remimazolam
CN119101054A (zh) * 2023-06-09 2024-12-10 成都麻沸散医药科技有限公司 一种氮杂䓬类化合物及其组合物和应用
WO2025052259A1 (en) 2023-09-05 2025-03-13 Reena Patel Ready to use compositions of remimazolam

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GREGORY J. PACOFSKY, JEFFREY A. STAFFORD, RICHARD F. COX, JILL R. COWAN, GEORGE F. DORSEY, STEPHEN S. GONZALES, ISTVAN KALDOR, GEO: "Relating the Structure, Activity, and Physical Properties of Ultrashort-Acting Benzodiazepine Receptor Agonists", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, vol. 12, no. 21, 1 November 2002 (2002-11-01), pages 3219 - 3222, XP055039974, ISSN: 0960894X, DOI: 10.1016/S0960-894X(02)00513-9 *
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