BR9816049A - (+) - alpha- (2,3-dimethoxyphenyl) -1- [2- (4-fluorophenyl) ethyl] -4-pi peridinomethanol esters and their use as prodrugs of the 5ht2a mdl receptor antagonist 110,907 - Google Patents

(+) - alpha- (2,3-dimethoxyphenyl) -1- [2- (4-fluorophenyl) ethyl] -4-pi peridinomethanol esters and their use as prodrugs of the 5ht2a mdl receptor antagonist 110,907

Info

Publication number
BR9816049A
BR9816049A BR9816049-4A BR9816049A BR9816049A BR 9816049 A BR9816049 A BR 9816049A BR 9816049 A BR9816049 A BR 9816049A BR 9816049 A BR9816049 A BR 9816049A
Authority
BR
Brazil
Prior art keywords
esters
alpha
peridinomethanol
5ht2a
dimethoxyphenyl
Prior art date
Application number
BR9816049-4A
Other languages
Portuguese (pt)
Inventor
Albert A Carr
Luc E Van Hijfte
Raymond W Kosley Jr
Original Assignee
Aventis Pharma Inc
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 Aventis Pharma Inc filed Critical Aventis Pharma Inc
Publication of BR9816049A publication Critical patent/BR9816049A/en

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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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Epidemiology (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Patente de Invenção: <B>"éSTERES DE (+)-ALFA-(2,3-DIMETOXIFENIL)-1-[2-(4-FLUOROFENIL)ETIL]-4-PI PERIDINOMETANOL E SEU USO COMO PRó-DROGAS DO ANTAGONISTA DE RECEPTOR 5HT2A MDL 110.907"<D>. A presente invenção é direcionada a ésteres de (+)-alfa-(2,3-dimetoxifenil)-1-[2-(4-fluorofenil)etil]-4-piperidino metanol, de fórmula (I) onde R é C~ 4-20~ alquila, formulações farmacêuticas, métodos de fabricação e métodos de uso destes ésteres. Estes compostos antagonizamos efeitos de serotonina no receptor 5HT~ 2A~ e são úteis no tratamento de várias condições tais como, por exemplo, psicoses tais como esquizofrenia.Invention Patent: <B> "(+) - ALPHA- (2,3-DIMETOXYphenyl) -1- [2- (4-FLUOROFENYL) ETHERS] -4-PI PERIDINOMETHANOL ESTERS AND THEIR USE AS ANTAGONIST PRO-DRUGS RECEIVER 5HT2A CDM 110.907 "<D>. The present invention is directed to esters of (+) - alpha- (2,3-dimethoxyphenyl) -1- [2- (4-fluorophenyl) ethyl] -4-piperidine methanol, of formula (I) where R is C ~ 4-20 ~ alkyl, pharmaceutical formulations, manufacturing methods and methods of using these esters. These compounds antagonize serotonin effects at the 5HT ~ 2A ~ receptor and are useful in the treatment of various conditions such as, for example, psychoses such as schizophrenia.

BR9816049-4A 1998-10-14 1998-10-14 (+) - alpha- (2,3-dimethoxyphenyl) -1- [2- (4-fluorophenyl) ethyl] -4-pi peridinomethanol esters and their use as prodrugs of the 5ht2a mdl receptor antagonist 110,907 BR9816049A (en)

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 (1)

Publication Number Publication Date
BR9816049A true BR9816049A (en) 2001-07-03

Family

ID=22268079

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9816049-4A BR9816049A (en) 1998-10-14 1998-10-14 (+) - alpha- (2,3-dimethoxyphenyl) -1- [2- (4-fluorophenyl) ethyl] -4-pi peridinomethanol esters and their use as prodrugs of the 5ht2a mdl receptor antagonist 110,907

Country Status (21)

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

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 (en) * 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-hydroxypiperidine-4-yl) methyl] pyridine-2(1H)-one derivatives, preparation method and use thereof
CN106892897A (en) * 2015-12-21 2017-06-27 上海科胜药物研发有限公司 A kind of hydroxyl piperazine pyrrone free alkali novel crystal forms and preparation method thereof
CN106928187A (en) * 2015-12-31 2017-07-07 上海奥博生物医药技术有限公司 A kind of hydrochloric acid hydroxyl piperazine pyrrone novel crystal forms and preparation method thereof

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU652759B2 (en) * 1990-06-01 1994-09-08 Aventisub Ii Inc. (+)-alpha-(2,3-dimethoxyphenyl)-1-(2-(4-fluorophenyl)ethyl)- 4-piperidinemethanol

Also Published As

Publication number Publication date
PL193306B1 (en) 2007-01-31
SK5082001A3 (en) 2001-11-06
EE200100219A (en) 2002-08-15
NZ510631A (en) 2003-07-25
NO20011805L (en) 2001-06-08
HUP0200517A3 (en) 2002-12-28
NO320417B1 (en) 2005-12-05
CN1160333C (en) 2004-08-04
CN1314887A (en) 2001-09-26
KR20010106517A (en) 2001-11-29
PL347318A1 (en) 2002-03-25
WO2000021930A1 (en) 2000-04-20
CZ20011331A3 (en) 2001-08-15
EA003667B1 (en) 2003-08-28
HRP20010278A2 (en) 2002-06-30
JP2002527422A (en) 2002-08-27
AU1083099A (en) 2000-05-01
CA2347469A1 (en) 2000-04-20
HUP0200517A2 (en) 2002-06-29
UA57859C2 (en) 2003-07-15
CA2347469C (en) 2006-02-28
IL142479A (en) 2006-06-11
HK1039332A1 (en) 2002-04-19
EP1121345A1 (en) 2001-08-08
TR200101047T2 (en) 2001-08-21
NO20011805D0 (en) 2001-04-09
EA200100361A1 (en) 2001-10-22
IL142479A0 (en) 2002-03-10
KR100515429B1 (en) 2005-09-20

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Legal Events

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B06G Technical and formal requirements: other requirements [chapter 6.7 patent gazette]

Free format text: FOI APRESENTADA ATRAVES DA PETICAO NO 40022 DE 17/08/2001 O PEDIDO DE EXAME CONTENDO UM TOTAL DE 55 REIVINDICACOES, ENTRETANTO O REQUERENTE ANEXOU UMA NOVA FOLHA 5 AO QUADRO REIVINDICATORIO, A QUAL ADICIONA UMA REIVINDICACAO AO QUADRO, PERFAZENDO UM TOTAL DE 56 REIVINDICACOES, PELO EXPOSTO, SOLICITA-SE QUE O REQUERENTE DEFINA QUAL QUADRO REIVINDICATORIO DEVE SER AXAMINADO, E QUE CASO SEJA DEFINIDO O QUE POSSUI 56 REINVIDICACOES QUE SEJA EFETUADO O PAGAMENTO DA 56O. O DEPOSITANTE DEVE TOMAR CONHECIMENTO DESTE PARECER, PODENDO MANIFESTAR-SE NO PRAZO DE 60 DIAS, CONTADOS DA DATA DA PUBLICACAO DESTE RPI.

B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: INDEFERIMENTO DO PRESENTE PEDIDO, UMA VEZ QUE NAO ATENDE AOS ARTIGOS 8O E 13 DA LPI.

B09B Patent application refused [chapter 9.2 patent gazette]

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