ES2225330T3 - Compuesto de piperidina y piperacina para empleo en el tratamiento de alzheimer. - Google Patents

Compuesto de piperidina y piperacina para empleo en el tratamiento de alzheimer.

Info

Publication number
ES2225330T3
ES2225330T3 ES01105498T ES01105498T ES2225330T3 ES 2225330 T3 ES2225330 T3 ES 2225330T3 ES 01105498 T ES01105498 T ES 01105498T ES 01105498 T ES01105498 T ES 01105498T ES 2225330 T3 ES2225330 T3 ES 2225330T3
Authority
ES
Spain
Prior art keywords
halogen
alkyl
hydrogen
compounds
independently
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES01105498T
Other languages
English (en)
Inventor
Yvo Crameri
Michelangelo Scalone
Pius Waldmeier
Ulrich Widmer
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Application granted granted Critical
Publication of ES2225330T3 publication Critical patent/ES2225330T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/02—Preparation by ring-closure or hydrogenation
    • 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
    • C07D211/36—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/42—Oxygen atoms attached in position 3 or 5
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D211/68—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—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 one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (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)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un método para la preparación de compuestos de las **fórmulas** caracterizado porque R1-R4 son independientemente uno del otro, hidrógeno, halógeno hidroxi, amino, nitro, sulfonilamido alquilo C1-5, o acetamido; R5-R8 son independientemente uno del otro, hidrógeno, alquilo C1-5, halógeno, trifluorometilo o alcoxi C1- 5; y sus sales de adición ácidas farmacéuticamente aceptables; cuyo proceso comprende a) hacer reaccionar un éster de ácido amino protegido (1) con un derivado de ácido butírico 4 sustituido (2) en donde R9 es un grupo amino protector, preferiblemente bencilo; R10 y R10¿ son independientemente un grupo protector de ácido carboxílico; y Y representa un grupo de partida; en presencia de una base; b) ciclizar el derivado de ácido butírico alcoxicarbonilmetil amino protegido c) bencilar la sal de carboxilato alquil 3-oxo- piperidina protegida en donde AZ significa un ácido mineral o un ácido orgánico fuerte; d) descarboxilar el carboxilato del alquil 3-oxo- piperidina benciladoprotegido.
ES01105498T 2000-03-22 2001-03-15 Compuesto de piperidina y piperacina para empleo en el tratamiento de alzheimer. Expired - Lifetime ES2225330T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP00106210 2000-03-22

Publications (1)

Publication Number Publication Date
ES2225330T3 true ES2225330T3 (es) 2005-03-16

Family

ID=8168189

Family Applications (1)

Application Number Title Priority Date Filing Date
ES01105498T Expired - Lifetime ES2225330T3 (es) 2000-03-22 2001-03-15 Compuesto de piperidina y piperacina para empleo en el tratamiento de alzheimer.

Country Status (12)

Country Link
US (1) US6605723B2 (es)
EP (1) EP1136475B1 (es)
JP (1) JP3598277B2 (es)
KR (1) KR100378331B1 (es)
CN (1) CN1218941C (es)
AT (1) ATE273953T1 (es)
CA (1) CA2341010C (es)
DE (1) DE60104923T2 (es)
DK (1) DK1136475T3 (es)
ES (1) ES2225330T3 (es)
JO (1) JO2275B1 (es)
MX (1) MXPA01002945A (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0204129D0 (en) * 2002-02-21 2002-04-10 Novartis Ag Process for the manufacture of organic compounds
US7569691B2 (en) * 2005-04-20 2009-08-04 Shin-Etsu Chemical Co., Ltd. Protected piperazino group-bearing organoxysilane compound and making method
CN101796050B (zh) 2007-09-06 2015-08-12 日本曹达株式会社 光学活性3-奎核醇衍生物的制造方法
EP2264000B1 (en) * 2008-04-07 2016-05-11 Nippon Soda Co., Ltd. Method for producing optically active aminoalcohol compound using ruthenium compound
CN102126995A (zh) * 2010-12-14 2011-07-20 台州市华南医化有限公司 一种改进的苯基乙烯基砜的制备工艺
CN102617451B (zh) * 2012-02-22 2014-01-22 华东理工大学 具有杀虫活性的哌啶醇衍生物、及其制备和用途
CN110240561B (zh) * 2018-03-07 2020-08-04 新发药业有限公司 一种低成本的3-羟基吡啶的制备方法
CN110734393B (zh) * 2019-11-11 2022-02-25 南京恒远科技开发有限公司 N-苄基-3-氧代哌啶-4-羧酸乙酯盐酸盐的制备方法
CN119039289A (zh) * 2024-07-30 2024-11-29 安庆多辉生物科技有限公司 一种阿达格西布合成用新型中间体及制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4410822A1 (de) * 1994-03-24 1995-09-28 Schering Ag Neue Piperidin-Derivate
DE69518497T2 (de) 1994-12-07 2001-04-19 Japan Science And Technology Corp., Kawaguchi Verfahren zur Herstellung eines Alkohols
JP4144814B2 (ja) 1997-09-05 2008-09-03 長谷川香料株式会社 光学活性アルコール化合物の製造方法
TWI254043B (en) 1999-06-08 2006-05-01 Hoffmann La Roche Ethanesulfonyl-piperidine derivatives having good affinity to N-methyl-D-aspartate (NMDA) receptor

Also Published As

Publication number Publication date
EP1136475A1 (en) 2001-09-26
DE60104923D1 (de) 2004-09-23
DE60104923T2 (de) 2005-08-25
US6605723B2 (en) 2003-08-12
MXPA01002945A (es) 2002-08-06
ATE273953T1 (de) 2004-09-15
JO2275B1 (en) 2005-04-07
JP3598277B2 (ja) 2004-12-08
CN1218941C (zh) 2005-09-14
DK1136475T3 (da) 2004-12-27
CA2341010A1 (en) 2001-09-22
CN1315319A (zh) 2001-10-03
KR20010100822A (ko) 2001-11-14
JP2001270865A (ja) 2001-10-02
EP1136475B1 (en) 2004-08-18
US20010037026A1 (en) 2001-11-01
CA2341010C (en) 2009-09-08
KR100378331B1 (ko) 2003-05-09

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