CN101397270B - 多奈哌齐盐的多晶型物及其制备和应用 - Google Patents

多奈哌齐盐的多晶型物及其制备和应用 Download PDF

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Publication number
CN101397270B
CN101397270B CN2008102117315A CN200810211731A CN101397270B CN 101397270 B CN101397270 B CN 101397270B CN 2008102117315 A CN2008102117315 A CN 2008102117315A CN 200810211731 A CN200810211731 A CN 200810211731A CN 101397270 B CN101397270 B CN 101397270B
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Prior art keywords
donepezil
acid
formula
solution
tablet
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CN2008102117315A
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Chinese (zh)
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CN101397270A (zh
Inventor
张和胜
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HAINAN HAILING CHEMICAL PHARMACEUTICAL CO Ltd
TIANJIN HEMEI BIOTECHNOLOGY CO Ltd
Original Assignee
HAINAN HAILING CHEMICAL PHARMACEUTICAL CO Ltd
Tianjin Hemay Biotechnology Co Ltd
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Priority to EP08800639A priority Critical patent/EP2204364B1/en
Priority to HK11100149.7A priority patent/HK1146047B/en
Priority to JP2010526129A priority patent/JP5426554B2/ja
Priority to ES08800639T priority patent/ES2415166T3/es
Priority to CN2008102117315A priority patent/CN101397270B/zh
Priority to PCT/CN2008/001646 priority patent/WO2009049479A1/zh
Priority to DK08800639.0T priority patent/DK2204364T3/da
Application filed by HAINAN HAILING CHEMICAL PHARMACEUTICAL CO Ltd, Tianjin Hemay Biotechnology Co Ltd filed Critical HAINAN HAILING CHEMICAL PHARMACEUTICAL CO Ltd
Publication of CN101397270A publication Critical patent/CN101397270A/zh
Priority to US12/748,248 priority patent/US8501779B2/en
Application granted granted Critical
Publication of CN101397270B publication Critical patent/CN101397270B/zh
Priority to US13/935,927 priority patent/US20130296283A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/145Maleic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/03Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring
    • C07C65/05Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring o-Hydroxy carboxylic acids
    • C07C65/10Salicylic acid

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN2008102117315A 2007-09-28 2008-09-24 多奈哌齐盐的多晶型物及其制备和应用 Active CN101397270B (zh)

Priority Applications (9)

Application Number Priority Date Filing Date Title
JP2010526129A JP5426554B2 (ja) 2007-09-28 2008-09-24 ドネペジル塩、その多形体、その製造方法、応用方法および組成物
ES08800639T ES2415166T3 (es) 2007-09-28 2008-09-24 Polímorfos de sales de Donepezilo, métodos de preparación y usos de los mismos
CN2008102117315A CN101397270B (zh) 2007-09-28 2008-09-24 多奈哌齐盐的多晶型物及其制备和应用
PCT/CN2008/001646 WO2009049479A1 (en) 2007-09-28 2008-09-24 Polymorphs of donepezil salts, preparation methods and uses thereof
EP08800639A EP2204364B1 (en) 2007-09-28 2008-09-24 Polymorphs of donepezil salts, preparation methods and uses thereof
HK11100149.7A HK1146047B (en) 2007-09-28 2008-09-24 Polymorphs of donepezil salts, preparation methods and uses thereof
DK08800639.0T DK2204364T3 (da) 2007-09-28 2008-09-24 Polymorfer af donepezil-salte, fremgangsmåder til fremstilling og anvendelser deraf
US12/748,248 US8501779B2 (en) 2007-09-28 2010-03-26 Polymorphs of donepezil salts, preparation methods and uses thereof
US13/935,927 US20130296283A1 (en) 2007-09-28 2013-07-05 Polymorphs of donepezil salts, preparation methods and uses thereof

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN200710061212.0 2007-09-28
CN200710061212 2007-09-28
CN200810052067.4 2008-01-15
CN200810052067 2008-01-15
CN2008102117315A CN101397270B (zh) 2007-09-28 2008-09-24 多奈哌齐盐的多晶型物及其制备和应用

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN2012100165448A Division CN102603612A (zh) 2007-09-28 2008-09-24 多奈哌齐盐的多晶型物及其制备和应用

Publications (2)

Publication Number Publication Date
CN101397270A CN101397270A (zh) 2009-04-01
CN101397270B true CN101397270B (zh) 2012-03-28

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CN2012100165448A Pending CN102603612A (zh) 2007-09-28 2008-09-24 多奈哌齐盐的多晶型物及其制备和应用

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Country Status (7)

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US (2) US8501779B2 (enExample)
EP (1) EP2204364B1 (enExample)
JP (1) JP5426554B2 (enExample)
CN (2) CN101397270B (enExample)
DK (1) DK2204364T3 (enExample)
ES (1) ES2415166T3 (enExample)
WO (1) WO2009049479A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100113793A1 (en) * 2006-03-20 2010-05-06 Ind-Swift Laboratories Limited Process for the Preparation of Highly Pure Donepezil
JP5563841B2 (ja) * 2010-02-05 2014-07-30 沢井製薬株式会社 薬物の不快な味をマスキングした経口医薬組成物
GB201411802D0 (en) * 2014-07-02 2014-08-13 Univ Bradford Effervescent compositions
CN104958254A (zh) * 2015-06-27 2015-10-07 万特制药(海南)有限公司 一种盐酸多奈哌齐口服溶液及其制备方法
EP3888636A4 (en) * 2018-11-26 2022-08-17 Ebabio Inc. EUTECTIC MIXTURE OF DONEPEZIL AND ITS USE
KR102318249B1 (ko) * 2018-11-26 2021-10-27 에바바이오 주식회사 도네페질 이온성 액체 및 이의 용도
EP4087395A4 (en) * 2020-01-10 2023-12-27 President And Fellows Of Harvard College METHOD FOR BIOSTASIS INDUCTION IN A CELL, TISSUE OR ORGAN

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1759836A (zh) * 2004-10-12 2006-04-19 天津和美生物技术有限公司 多奈哌齐及其衍生物的舌下含片

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI95572C (fi) 1987-06-22 1996-02-26 Eisai Co Ltd Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi
JPH1053576A (ja) * 1996-06-07 1998-02-24 Eisai Co Ltd 塩酸ドネペジルの多形結晶およびその製造法
SI9720038B (sl) * 1996-06-07 2010-06-30 Eisai Co Ltd Polimorfi donepezil hidroklorida in postopek izdelave
US20050288330A1 (en) * 2004-06-29 2005-12-29 Avinash Naidu Process for producing a polymorphic form of (1-Benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl] methyl piperidine hydrochloride (donepezil hydrochloride)
US7439365B2 (en) 2003-11-17 2008-10-21 Usv, Ltd. Pharmaceutical salt of (1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl] methyl piperidine (Donepezil)
HUP0401850A3 (en) * 2004-09-15 2008-03-28 Egis Gyogyszergyar Nyilvanosan Donepezil salts for producing pharmaceutical composition
DE102004046497A1 (de) * 2004-09-23 2006-04-06 Helm Ag Donepezil-Salze
CA2581926A1 (en) * 2004-09-29 2006-04-06 Chemagis Ltd. Use of purified donepezil maleate for preparing pharmaceutically pure amorphous donepezil hydrochloride
WO2007010910A1 (en) * 2005-07-15 2007-01-25 Eisai R & D Management Co., Ltd. 1-benzyl-4-[(5, 6-dimethoxy-1-indanon)-2-yl]-methyl piperidine p-toluenesulfonate or crystal thereof
HU227474B1 (en) * 2005-12-20 2011-07-28 Richter Gedeon Nyrt Process for industrial scale production of high purity donepezil hydrochloride polymorph i.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1759836A (zh) * 2004-10-12 2006-04-19 天津和美生物技术有限公司 多奈哌齐及其衍生物的舌下含片

Also Published As

Publication number Publication date
EP2204364A4 (en) 2011-08-10
CN101397270A (zh) 2009-04-01
HK1146047A1 (en) 2011-05-13
US20130296283A1 (en) 2013-11-07
US20100311793A1 (en) 2010-12-09
EP2204364A1 (en) 2010-07-07
JP5426554B2 (ja) 2014-02-26
CN102603612A (zh) 2012-07-25
US8501779B2 (en) 2013-08-06
WO2009049479A1 (en) 2009-04-23
JP2010540470A (ja) 2010-12-24
EP2204364B1 (en) 2013-03-20
DK2204364T3 (da) 2013-06-03
ES2415166T3 (es) 2013-07-24

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C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
ASS Succession or assignment of patent right

Owner name: HAINAN HAILING CHEMICAL PHARMACEUTICAL CO., LTD.

C41 Transfer of patent application or patent right or utility model
TA01 Transfer of patent application right

Effective date of registration: 20110118

Address after: 300457 Tianjin City, Tianjin economic and Technological Development Zone Xiaoyuan village 31-101

Applicant after: Tianjin Hemei Biotechnology Co., Ltd.

Co-applicant after: Hainan Hailing Chemical Pharmaceutical Co., Ltd.

Address before: 300457 Tianjin City, Tianjin economic and Technological Development Zone Xiaoyuan village 31-101

Applicant before: Tianjin Hemei Biotechnology Co., Ltd.

C14 Grant of patent or utility model
GR01 Patent grant