CN103288834B - 短效苯并二氮杂*盐及其多晶型 - Google Patents

短效苯并二氮杂*盐及其多晶型 Download PDF

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Publication number
CN103288834B
CN103288834B CN201310166860.8A CN201310166860A CN103288834B CN 103288834 B CN103288834 B CN 103288834B CN 201310166860 A CN201310166860 A CN 201310166860A CN 103288834 B CN103288834 B CN 103288834B
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besylate
compound
salt
general formula
crystal
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CN103288834A (zh
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G·S·蒂尔布鲁克
L·J·丘比特
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Wuhan Humanwell Innovative Drug Research and Development Center Ltd Co
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Paion UK Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (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)
CN201310166860.8A 2006-07-10 2007-07-10 短效苯并二氮杂*盐及其多晶型 Active CN103288834B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB0613692.3 2006-07-10
GB0613694A GB0613694D0 (en) 2006-07-10 2006-07-10 Benzodiazepine salts
GB0613694.9 2006-07-10
GB0613692A GB0613692D0 (en) 2006-07-10 2006-07-10 Benzodiazepine salts
CN200780028964.5A CN101501019B (zh) 2006-07-10 2007-07-10 短效苯并二氮杂*盐及其多晶型

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN200780028964.5A Division CN101501019B (zh) 2006-07-10 2007-07-10 短效苯并二氮杂*盐及其多晶型

Publications (2)

Publication Number Publication Date
CN103288834A CN103288834A (zh) 2013-09-11
CN103288834B true CN103288834B (zh) 2015-07-15

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CN201310166860.8A Active CN103288834B (zh) 2006-07-10 2007-07-10 短效苯并二氮杂*盐及其多晶型
CN201410147318.2A Active CN104059072B (zh) 2006-07-10 2007-07-10 短效苯并二氮杂*盐及其多晶型
CN201410147078.6A Active CN104059071B (zh) 2006-07-10 2007-07-10 短效苯并二氮杂*盐及其多晶型

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CN201410147078.6A Active CN104059071B (zh) 2006-07-10 2007-07-10 短效苯并二氮杂*盐及其多晶型

Country Status (17)

Country Link
US (7) US9193730B2 (https=)
EP (1) EP2081921B1 (https=)
JP (2) JP5433413B2 (https=)
KR (3) KR20150081370A (https=)
CN (3) CN103288834B (https=)
AT (1) ATE480532T1 (https=)
AU (1) AU2007274054B2 (https=)
BR (1) BRPI0714886B8 (https=)
CA (1) CA2657347C (https=)
DE (1) DE602007009128D1 (https=)
DK (1) DK2081921T3 (https=)
MX (1) MX2009000404A (https=)
PL (1) PL2081921T3 (https=)
PT (1) PT2081921E (https=)
RU (1) RU2470935C2 (https=)
SI (1) SI2081921T1 (https=)
WO (1) WO2008007071A1 (https=)

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EP2450039A1 (en) 2010-11-08 2012-05-09 PAION UK Ltd. Dosing regimen for sedation with CNS 7056 (Remimazolam)
NZ702063A (en) * 2012-05-22 2016-11-25 Paion Uk Ltd Compositions comprising short-acting benzodiazepines
UA116452C2 (uk) * 2012-08-31 2018-03-26 ПАЙОН ЮКей ЛІМІТЕД Режим дозування седативного засобу
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HUE047450T2 (hu) 2014-07-23 2020-04-28 Jiangsu Nhwaluokang Pharmaceutical Res And Development Co Ltd Új benzodiazepin származék és alkalmazása
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
EP3442539B1 (en) * 2016-04-14 2025-04-09 Paion UK Limited Orally inhaled and nasal benzodiazepines
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
WO2018148361A1 (en) 2017-02-09 2018-08-16 Watson Laboratories Inc. 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
EA202091927A1 (ru) 2018-02-13 2020-12-07 Цзянсу Нхвалокан Фармасьютикал Рисерч Энд Дивелопмент Ко., Лтд. Гидрохлорид производного бензодиазепина и кристаллическая форма, способ их получения и применения
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
US12540140B2 (en) 2022-04-08 2026-02-03 Fresenius Kabi Oncology Ltd. 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
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