HUP0103253A2 - Új eljárás és új intermedierek Donepezil és származékai előállítására - Google Patents

Új eljárás és új intermedierek Donepezil és származékai előállítására

Info

Publication number
HUP0103253A2
HUP0103253A2 HU0103253A HUP0103253A HUP0103253A2 HU P0103253 A2 HUP0103253 A2 HU P0103253A2 HU 0103253 A HU0103253 A HU 0103253A HU P0103253 A HUP0103253 A HU P0103253A HU P0103253 A2 HUP0103253 A2 HU P0103253A2
Authority
HU
Hungary
Prior art keywords
piperidyl
group
general formula
derivatized
compounds
Prior art date
Application number
HU0103253A
Other languages
English (en)
Inventor
L. Arie Gutman
Genady Nisnevich
Eleonora Shkolnik
Boris Tishin
Igor Zaltzman
Original Assignee
Finetech Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Finetech Ltd. filed Critical Finetech Ltd.
Publication of HUP0103253A2 publication Critical patent/HUP0103253A2/hu
Publication of HUP0103253A3 publication Critical patent/HUP0103253A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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
    • C07D211/18—Heterocyclic 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
    • C07D211/30—Heterocyclic 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
    • C07D211/32—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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
    • C07D211/18—Heterocyclic 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
    • C07D211/34—Heterocyclic 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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

A találmány tárgya új eljárás az (I) általános képletű vegyületekelőállítására a (II) általános képletű új vegyületeknek adott esetbensavak és/vagy oldószerek jelenlétében végzett gyűrűzárásával. Aképletekben R1 jelentése N-acil-4-piperidilcsoport, N-(alkoxi-karbonil)-4-piperidilcsoport, 4-piperidilcsoport, N-alkil-4-piperidilcsoport, N-benzil-4-piperidilcsoport, N-(w-aralkil)-4-piperidilcsoport vagy 4-piridilcsoport; R4, R5, R6 és R7 jelentéseazonos vagy különböző, és mindegyikük jelentése hidrogénatom,alkilcsoport, arilcsoport, hidroxicsoport, alkoxicsoport, aril-oxicsoport, benzil-oxicsoport, acil-oxicsoport, alkil-tiocsoport,aril-tiocsoport, benzil-tiocsoport, acil-aminocsoport,ftálimidocsoport vagy halogénatom; n értéke 1, 2 vagy 3; m értéke 1,2, 3, 4 vagy 5; R2 jelentése származékká alakított vagy származékkánem alakított karboxicsoport, cianocsoport, N-szubsztituált amino-karbonilcsoport vagy hidrogénatom; és R3 jelentése származékkáalakított vagy származékká nem alakított karboxicsoport, cianocsoport,N-szubsztituált amino-karbonilcsoportot. A találmány tárgyát képezik a(II) általános képletű új vegyületek és azok előállítási eljárása. Az(I) általános képletű vegyületek körébe tartozik a donepezil, amelyhatékony acetil-kolin-észteráz inhibitor, és így az Alzheimer típusúsenilis dementia kezelésében alkalmazható. Ó
HU0103253A 1998-08-17 1999-08-11 Novel process and intermediates for production of donepezil and related compounds HUP0103253A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IL12580998A IL125809A (en) 1998-08-17 1998-08-17 Process and intermediates for production of donepezil and related compounds
PCT/IL1999/000436 WO2000009483A2 (en) 1998-08-17 1999-08-11 Process and intermediates for production of donepezil and related compounds

Publications (2)

Publication Number Publication Date
HUP0103253A2 true HUP0103253A2 (hu) 2002-01-28
HUP0103253A3 HUP0103253A3 (en) 2002-02-28

Family

ID=11071859

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0103253A HUP0103253A3 (en) 1998-08-17 1999-08-11 Novel process and intermediates for production of donepezil and related compounds

Country Status (7)

Country Link
US (1) US6492522B1 (hu)
EP (1) EP1129073A2 (hu)
JP (1) JP2002525264A (hu)
AU (1) AU5191099A (hu)
HU (1) HUP0103253A3 (hu)
IL (1) IL125809A (hu)
WO (1) WO2000009483A2 (hu)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL150982A (en) * 2002-07-30 2007-02-11 Ori Lerman Process for making Donafzil
US20040192919A1 (en) * 2002-08-14 2004-09-30 Finetech Laboratories, Ltd. Process for production of highly pure donepezil hydrochloride
IL151253A0 (en) * 2002-08-14 2003-04-10 Finetech Lab Ltd Process for production of highly pure donepezil hydrochloride
ATE487492T1 (de) * 2003-02-27 2010-11-15 Eisai R&D Man Co Ltd Pharmazeutische zusammensetzung zur behandlung von drogenabhängigkeit
AU2003247158A1 (en) * 2003-07-01 2005-01-21 Hetero Drugs Limited Preparation of intermediates for acetyl cholinesterase inhibitors
JP2007519733A (ja) * 2004-01-26 2007-07-19 コーテックス ファーマシューティカルズ インコーポレーティッド アンパカインにより誘導されるシナプス応答促通のコリンエステラーゼ阻害剤による増強方法
US20060122226A1 (en) * 2004-12-08 2006-06-08 Itai Adin Crystalline forms of Donepezil base
CN100436416C (zh) * 2005-07-29 2008-11-26 西南合成制药股份有限公司 盐酸多奈哌齐合成工艺
GB0515803D0 (en) 2005-07-30 2005-09-07 Pliva Hrvatska D O O Intermediate compounds
HU227474B1 (en) * 2005-12-20 2011-07-28 Richter Gedeon Nyrt Process for industrial scale production of high purity donepezil hydrochloride polymorph i.
EP1973878B1 (en) 2006-01-04 2010-11-24 Cipla Limited Process and intermediate for preparation of donepezil
US20100113793A1 (en) * 2006-03-20 2010-05-06 Ind-Swift Laboratories Limited Process for the Preparation of Highly Pure Donepezil
EP2089383B1 (en) 2006-11-09 2015-09-16 Probiodrug AG 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
CN101626688A (zh) 2006-12-11 2010-01-13 雷维瓦药品公司 茚满酮基胆碱酯酶抑制剂的组合物、合成和使用方法
MX2009009234A (es) 2007-03-01 2009-12-01 Probiodrug Ag Uso nuevo de inhibidores de ciclasa de glutaminilo.
WO2008128985A1 (en) 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
EA037187B1 (ru) 2010-02-09 2021-02-17 Дзе Джонс Хопкинс Юниверсити Способ и композиция для лечения когнитивного расстройства
US9181233B2 (en) 2010-03-03 2015-11-10 Probiodrug Ag Inhibitors of glutaminyl cyclase
CA2789440C (en) 2010-03-10 2020-03-24 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
JP5945532B2 (ja) 2010-04-21 2016-07-05 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
WO2011151359A1 (en) 2010-06-02 2011-12-08 Noscira, S.A. Combined treatment with a cholinesterase inhibitor and a thiadiazolidinedione derivative
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
CN103524515B (zh) 2012-07-03 2016-07-06 浙江海正药业股份有限公司 具有乙酰胆碱酯酶抑制活性的苯并间二氧杂环戊烯衍生物及其制备方法和用途
US10154988B2 (en) 2012-11-14 2018-12-18 The Johns Hopkins University Methods and compositions for treating schizophrenia
WO2014144801A1 (en) 2013-03-15 2014-09-18 Agenebio Inc. Methods and compositions for improving cognitive function
WO2014144663A1 (en) 2013-03-15 2014-09-18 The Johns Hopkins University Methods and compositions for improving cognitive function
US10925834B2 (en) 2015-05-22 2021-02-23 Agenebio, Inc. Extended release pharmaceutical compositions of levetiracetam
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3476759A (en) * 1967-05-02 1969-11-04 Mcneilab Inc 2- and 3-(4-piperidyl) indanes and indanols
FI95572C (fi) 1987-06-22 1996-02-26 Eisai Co Ltd Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi
JP2893893B2 (ja) * 1990-02-02 1999-05-24 三菱化学株式会社 環状ケトン類の製造方法
NZ318843A (en) 1995-12-15 2000-01-28 Pfizer Processes and intermediates for preparing 1-benzyl-4-((5,6-dimethoxy-1-indanon)-2-yl)methylpiperidine

Also Published As

Publication number Publication date
EP1129073A2 (en) 2001-09-05
JP2002525264A (ja) 2002-08-13
US6492522B1 (en) 2002-12-10
AU5191099A (en) 2000-03-06
WO2000009483A2 (en) 2000-02-24
IL125809A0 (en) 1999-04-11
IL125809A (en) 2005-08-31
WO2000009483A3 (en) 2001-06-21
HUP0103253A3 (en) 2002-02-28

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