JP5433413B2 - 短時間作用型ベンゾジアゼピンの塩およびそれらの多形形態 - Google Patents

短時間作用型ベンゾジアゼピンの塩およびそれらの多形形態 Download PDF

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JP5433413B2
JP5433413B2 JP2009518952A JP2009518952A JP5433413B2 JP 5433413 B2 JP5433413 B2 JP 5433413B2 JP 2009518952 A JP2009518952 A JP 2009518952A JP 2009518952 A JP2009518952 A JP 2009518952A JP 5433413 B2 JP5433413 B2 JP 5433413B2
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besylate
salt
compound
formula
shows
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JP2009542785A5 (enExample
JP2009542785A (ja
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ゲイリー スチュワート ティルブルック，
ルイザ ジェーン キュービット，
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パイオン ユーケー リミテッド
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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
    • 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
    • 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
    • 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)
JP2009518952A 2006-07-10 2007-07-10 短時間作用型ベンゾジアゼピンの塩およびそれらの多形形態 Active JP5433413B2 (ja)

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

Related Child Applications (1)

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JP2012235328A Division JP5785923B2 (ja) 2006-07-10 2012-10-25 短時間作用型ベンゾジアゼピンの塩およびそれらの多形形態

Publications (3)

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JP2009542785A JP2009542785A (ja) 2009-12-03
JP2009542785A5 JP2009542785A5 (enExample) 2011-07-28
JP5433413B2 true JP5433413B2 (ja) 2014-03-05

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JP2009518952A Active JP5433413B2 (ja) 2006-07-10 2007-07-10 短時間作用型ベンゾジアゼピンの塩およびそれらの多形形態
JP2012235328A Active JP5785923B2 (ja) 2006-07-10 2012-10-25 短時間作用型ベンゾジアゼピンの塩およびそれらの多形形態

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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)
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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
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