RU2470935C2 - Бензодиазепиновые соли кратковременного действия и их полиморфные формы - Google Patents

Бензодиазепиновые соли кратковременного действия и их полиморфные формы Download PDF

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RU2470935C2
RU2470935C2 RU2009104311/04A RU2009104311A RU2470935C2 RU 2470935 C2 RU2470935 C2 RU 2470935C2 RU 2009104311/04 A RU2009104311/04 A RU 2009104311/04A RU 2009104311 A RU2009104311 A RU 2009104311A RU 2470935 C2 RU2470935 C2 RU 2470935C2
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besylate
salt
formula
compound
crystalline
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RU2009104311/04A
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Russian (ru)
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RU2009104311A (ru
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Гэри Стюарт ТИЛБРУК
Луиза Джейн КЬЮБИТТ
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ПАЙОН ЮКей ЛИМИТЕД
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Priority claimed from GB0613694A external-priority patent/GB0613694D0/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Anesthesiology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Developing Agents For Electrophotography (AREA)
  • Steroid Compounds (AREA)
RU2009104311/04A 2006-07-10 2007-07-10 Бензодиазепиновые соли кратковременного действия и их полиморфные формы RU2470935C2 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB0613694.9 2006-07-10
GB0613692A GB0613692D0 (en) 2006-07-10 2006-07-10 Benzodiazepine salts
GB0613694A GB0613694D0 (en) 2006-07-10 2006-07-10 Benzodiazepine salts
GB0613692.3 2006-07-10
PCT/GB2007/002565 WO2008007071A1 (en) 2006-07-10 2007-07-10 Short-acting benzodiazepine salts and their polymorphic forms

Publications (2)

Publication Number Publication Date
RU2009104311A RU2009104311A (ru) 2010-08-20
RU2470935C2 true RU2470935C2 (ru) 2012-12-27

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RU2009104311/04A RU2470935C2 (ru) 2006-07-10 2007-07-10 Бензодиазепиновые соли кратковременного действия и их полиморфные формы

Country Status (17)

Country Link
US (7) US9193730B2 (enExample)
EP (1) EP2081921B1 (enExample)
JP (2) JP5433413B2 (enExample)
KR (3) KR20090045233A (enExample)
CN (3) CN103288834B (enExample)
AT (1) ATE480532T1 (enExample)
AU (1) AU2007274054B2 (enExample)
BR (1) BRPI0714886B8 (enExample)
CA (1) CA2657347C (enExample)
DE (1) DE602007009128D1 (enExample)
DK (1) DK2081921T3 (enExample)
MX (1) MX2009000404A (enExample)
PL (1) PL2081921T3 (enExample)
PT (1) PT2081921E (enExample)
RU (1) RU2470935C2 (enExample)
SI (1) SI2081921T1 (enExample)
WO (1) WO2008007071A1 (enExample)

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GB0613693D0 (en) 2006-07-10 2006-08-16 Cenes Ltd Benzodiazepine salts (3)
BRPI0714886B8 (pt) 2006-07-10 2021-05-25 Paion Uk Ltd sais de benzodiazepina, seus usos e seus processos de preparação, e composição farmacêutica
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
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AU2013309860B2 (en) * 2012-08-31 2017-12-21 Paion Uk Limited Method for administering hypnotic/sedative agent
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CN106804107B (zh) * 2014-07-23 2019-03-12 江苏恩华络康药物研发有限公司 新的苯并二氮杂*类衍生物及其用途
US20170081954A1 (en) * 2015-09-23 2017-03-23 Tesco Corporation Pipe joint location detection system and method
CN110511224A (zh) * 2016-04-08 2019-11-29 四川科伦药物研究院有限公司 苯并二氮杂*衍生物的盐及其晶体形式、制备方法和用途
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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
EP3580219B1 (en) 2017-02-09 2022-04-13 Assia Chemical Industries Ltd. Process for the preparation of remimazolam and solid state forms of remimazolam salts
CN108948018B (zh) * 2017-05-17 2021-03-30 四川科伦博泰生物医药股份有限公司 苯并二氮*衍生物及其盐和相关晶体形式、制备方法和用途
JP7410036B2 (ja) 2018-02-13 2024-01-09 ジャンスー、エンファルオカン、ファーマシューティカル、リサーチ、アンド、ディベロップメント、カンパニー、リミテッド ベンゾジアゼピン誘導体塩酸塩および結晶形、その製造方法および用途
CN110398514B (zh) * 2018-04-24 2023-04-28 恒天纤维集团有限公司 一种快速判断纤维素胶液中金属杂质含量的方法
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
WO2023037237A1 (en) * 2021-09-09 2023-03-16 Wavelength Enterprises Ltd Process for the preparation of remimazolam
WO2023194945A1 (en) 2022-04-08 2023-10-12 Fresenius Kabi Oncology Ltd. An improved process for the preparation of remimazolam
CN115448927A (zh) * 2022-10-20 2022-12-09 重庆瑞泊莱医药科技有限公司 一种氢溴酸依匹斯汀晶型ii及其制备方法
WO2025052259A1 (en) 2023-09-05 2025-03-13 Reena Patel Ready to use compositions of remimazolam

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