EA200100361A1 - Сложные эфиры (+)-альфа-(2,3-диметоксифенил)-1-[2-(4-фторфенил)этил]-4-пиперидинметанола и их использование в качестве пролекарств антагониста mdl 110907 5htрецепторов - Google Patents

Сложные эфиры (+)-альфа-(2,3-диметоксифенил)-1-[2-(4-фторфенил)этил]-4-пиперидинметанола и их использование в качестве пролекарств антагониста mdl 110907 5htрецепторов

Info

Publication number
EA200100361A1
EA200100361A1 EA200100361A EA200100361A EA200100361A1 EA 200100361 A1 EA200100361 A1 EA 200100361A1 EA 200100361 A EA200100361 A EA 200100361A EA 200100361 A EA200100361 A EA 200100361A EA 200100361 A1 EA200100361 A1 EA 200100361A1
Authority
EA
Eurasian Patent Office
Prior art keywords
antagonist
alpha
ethyl
dimetoxyphenyl
piperidinmethanol
Prior art date
Application number
EA200100361A
Other languages
English (en)
Other versions
EA003667B1 (ru
Inventor
Альберт А. Карр
Хейфте Люк Е. Ван
Рэймонд В. Мл. Косли
Original Assignee
Авентис Фармасьютикалз Инк.
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 Авентис Фармасьютикалз Инк. filed Critical Авентис Фармасьютикалз Инк.
Publication of EA200100361A1 publication Critical patent/EA200100361A1/ru
Publication of EA003667B1 publication Critical patent/EA003667B1/ru

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
    • C07D211/20—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 singly bound oxygen or sulphur atoms
    • C07D211/22—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 singly bound oxygen or sulphur atoms by oxygen atoms
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61P25/18—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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Addiction (AREA)
  • Epidemiology (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Настоящее изобретение относится к сложным эфирам (+)-альфа-(2,3-диметоксифенил)-1-[2-(4-фторфенил)этил]-4-пиперидинметанола формулы Iгде R представляет собой C-C-алкил, фармацевтическим композициям, способам получения и способам использования указанных эфиров, обладающих антагонистическим действием по отношению к воздействию серотонина на 5HT-рецептор и полезных для лечения различных заболеваний, таких, например, как психические расстройства, такие как шизофрения.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200100361A 1998-10-14 1998-10-14 Сложные эфиры (+)-альфа-(2,3-диметоксифенил)-1-[2-(4-фторфенил)этил]-4-пиперидинметанола и их использование в качестве пролекарств антагониста mdl 110907 5htрецепторов EA003667B1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US1998/021608 WO2000021930A1 (en) 1998-10-14 1998-10-14 Esters of (+)-alpha-( 2,3- dimethoxyphenyl) -1-[2-(4- fluorophenyl) ethyl]-4- piperidinemethanol and their use as prodrugs of the 5ht2a receptor antagonist mdl 110,907

Publications (2)

Publication Number Publication Date
EA200100361A1 true EA200100361A1 (ru) 2001-10-22
EA003667B1 EA003667B1 (ru) 2003-08-28

Family

ID=22268079

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200100361A EA003667B1 (ru) 1998-10-14 1998-10-14 Сложные эфиры (+)-альфа-(2,3-диметоксифенил)-1-[2-(4-фторфенил)этил]-4-пиперидинметанола и их использование в качестве пролекарств антагониста mdl 110907 5htрецепторов

Country Status (21)

Country Link
EP (1) EP1121345A1 (ru)
JP (1) JP2002527422A (ru)
KR (1) KR100515429B1 (ru)
CN (1) CN1160333C (ru)
AU (1) AU1083099A (ru)
BR (1) BR9816049A (ru)
CA (1) CA2347469C (ru)
CZ (1) CZ20011331A3 (ru)
EA (1) EA003667B1 (ru)
EE (1) EE200100219A (ru)
HK (1) HK1039332A1 (ru)
HR (1) HRP20010278A2 (ru)
HU (1) HUP0200517A3 (ru)
IL (2) IL142479A0 (ru)
NO (1) NO320417B1 (ru)
NZ (1) NZ510631A (ru)
PL (1) PL193306B1 (ru)
SK (1) SK5082001A3 (ru)
TR (1) TR200101047T2 (ru)
UA (1) UA57859C2 (ru)
WO (1) WO2000021930A1 (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020099076A1 (en) * 2000-05-25 2002-07-25 Richard Scheyer D. Use of (+)-a-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl) ethyl]-4-piperidinemethanol or its prodrug in the treatment of symptoms of dementia and dopamine induced psychosis
CN102241667B (zh) * 2010-05-14 2013-10-23 中国人民解放军军事医学科学院毒物药物研究所 1-[(4-羟基哌啶-4基)甲基]吡啶-2(1h)-酮衍生物及其制备方法和用途
CN106892897A (zh) * 2015-12-21 2017-06-27 上海科胜药物研发有限公司 一种羟哌吡酮游离碱新晶型及其制备方法
CN106928187A (zh) * 2015-12-31 2017-07-07 上海奥博生物医药技术有限公司 一种盐酸羟哌吡酮新晶型及其制备方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100211713B1 (ko) * 1990-06-01 1999-08-02 슈테펜 엘. 네스비트 (+)-알파-(2,3-디메톡시페닐)-1-[2-(4-플루오로페닐)에틸]-4-피페리딘메탄올

Also Published As

Publication number Publication date
AU1083099A (en) 2000-05-01
KR20010106517A (ko) 2001-11-29
HUP0200517A2 (en) 2002-06-29
EP1121345A1 (en) 2001-08-08
CA2347469C (en) 2006-02-28
EE200100219A (et) 2002-08-15
EA003667B1 (ru) 2003-08-28
JP2002527422A (ja) 2002-08-27
HK1039332A1 (en) 2002-04-19
CZ20011331A3 (cs) 2001-08-15
NO20011805L (no) 2001-06-08
NO320417B1 (no) 2005-12-05
WO2000021930A1 (en) 2000-04-20
IL142479A0 (en) 2002-03-10
CN1314887A (zh) 2001-09-26
IL142479A (en) 2006-06-11
UA57859C2 (ru) 2003-07-15
NO20011805D0 (no) 2001-04-09
NZ510631A (en) 2003-07-25
SK5082001A3 (en) 2001-11-06
KR100515429B1 (ko) 2005-09-20
PL347318A1 (en) 2002-03-25
HRP20010278A2 (en) 2002-06-30
CA2347469A1 (en) 2000-04-20
HUP0200517A3 (en) 2002-12-28
CN1160333C (zh) 2004-08-04
TR200101047T2 (tr) 2001-08-21
BR9816049A (pt) 2001-07-03
PL193306B1 (pl) 2007-01-31

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU