ES2303674T3 - Procedimiento para la preparacion de 3-amino-8-(1-piperazinil)-2h-1-benzopiran-2-ona y sales e hidratos de la misma. - Google Patents

Procedimiento para la preparacion de 3-amino-8-(1-piperazinil)-2h-1-benzopiran-2-ona y sales e hidratos de la misma. Download PDF

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Publication number
ES2303674T3
ES2303674T3 ES05717126T ES05717126T ES2303674T3 ES 2303674 T3 ES2303674 T3 ES 2303674T3 ES 05717126 T ES05717126 T ES 05717126T ES 05717126 T ES05717126 T ES 05717126T ES 2303674 T3 ES2303674 T3 ES 2303674T3
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Spain
Prior art keywords
formula
see formula
compound
see
amide
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.)
Active
Application number
ES05717126T
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English (en)
Inventor
Cornelis Bakker
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.)
Abbott Healthcare Products BV
Original Assignee
Solvay Pharmaceuticals BV
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Filing date
Publication date
Application filed by Solvay Pharmaceuticals BV filed Critical Solvay Pharmaceuticals BV
Application granted granted Critical
Publication of ES2303674T3 publication Critical patent/ES2303674T3/es
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/06—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2
    • C07D311/08—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring
    • C07D311/18—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted otherwise than in position 3 or 7
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P25/04—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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/28—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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Neurosurgery (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Un procedimiento para la preparación de un compuesto de fórmula (7): (Ver fórmula) caracterizado porque un compuesto de fórmula (1): (Ver fórmula) donde Hal es F, Cl, Br o I, se nitra para proporcionar 5-halógeno-2-hidroxi-3-nitrobenzaldehído (2), (Ver fórmula) seguido por una condensación de Erlenmeyer de (2) con un derivado de glicina de fórmula: (Ver fórmula) donde R representa un alquilo(C1-6) o un grupo arilo, para proporcionar una N-(6-halógeno-8-nitro-2-oxo-2H-1benzopiran-3-il)amida (3): (Ver fórmula) y una hidrogenación catalítica subsecuente de (3) para proporcionar una N-(8-amino-2-oxo-2H-1-benzopiran-3-il) amida (4), (Ver fórmula) después de lo cual el compuesto (4) obtenido se alquila con un compuesto de fórmula (Ver fórmula) donde L es un grupo saliente, para proporcionar una N-(8-(1-piperazinil)-2-oxo-2H-1-benzopiran-3-il)amida (5), (Ver fórmula) después de lo cual la función amida de (5) se hidroliza empleando un ácido, dando como resultando la sal ácida (6) correspondiente, en la cual n es 1, 2 ó 3, (Ver fórmula) después de lo cual el compuesto de fórmula (6) se neutraliza parcialmente con una base para producir el producto representado por la fórmula (7) (Ver fórmula) donde n* puede tener el valor 1 cuando n = 2 ó n = 3, o el valor 2 cuando n = 3, y m puede tener el valor 1, 2 ó 3.
ES05717126T 2004-03-25 2005-03-23 Procedimiento para la preparacion de 3-amino-8-(1-piperazinil)-2h-1-benzopiran-2-ona y sales e hidratos de la misma. Active ES2303674T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US55595804P 2004-03-25 2004-03-25
EP04101228 2004-03-25

Publications (1)

Publication Number Publication Date
ES2303674T3 true ES2303674T3 (es) 2008-08-16

Family

ID=34928926

Family Applications (1)

Application Number Title Priority Date Filing Date
ES05717126T Active ES2303674T3 (es) 2004-03-25 2005-03-23 Procedimiento para la preparacion de 3-amino-8-(1-piperazinil)-2h-1-benzopiran-2-ona y sales e hidratos de la misma.

Country Status (12)

Country Link
US (2) US7776860B2 (es)
EP (1) EP1732556B1 (es)
JP (1) JP2007530507A (es)
AR (1) AR049478A1 (es)
AT (1) ATE388709T1 (es)
CA (1) CA2554041A1 (es)
DE (1) DE602005005308T2 (es)
ES (1) ES2303674T3 (es)
PL (1) PL1732556T3 (es)
SA (1) SA05260061B1 (es)
TW (1) TWI340136B (es)
WO (1) WO2005092338A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR048112A1 (es) * 2004-03-25 2006-03-29 Solvay Pharm Bv Derivados de 1-(2h-1-benzopiran-2-on-8-il)-piperazina para el tratamiento de dolor
JP6061373B2 (ja) * 2012-07-24 2017-01-18 国立研究開発法人産業技術総合研究所 ２−ヒドロキシベンズアルデヒド化合物、これを含有するコラーゲン細胞外分泌阻害剤及び医薬品組成物
WO2020183011A1 (en) 2019-03-14 2020-09-17 Institut Curie Htr1d inhibitors and uses thereof in the treatment of cancer

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE81975T1 (de) 1984-12-21 1992-11-15 Duphar Int Res Arzneimittel mit psychotroper wirkung.
DK611489A (da) 1988-12-08 1990-06-09 Duphar Int Res Anxiolytisk aktive piperazinderivater og farmaceutiske praeparater med indhold af saadanne forbindelser
US5009895A (en) * 1990-02-02 1991-04-23 Merck & Co., Inc. Sustained release with high and low viscosity HPMC
FR2670491B1 (fr) * 1990-12-14 1993-02-05 Adir Nouvelles piperazines 1,4-disubstituees, leur procede de preparation et les compositions pharmaceutiques les renfermant.
ATE204262T1 (de) 1991-09-18 2001-09-15 Glaxo Group Ltd Benzanilidderivate als 5-ht1d-antagonisten
WO1993013766A1 (en) 1992-01-07 1993-07-22 Merrell Dow Pharmaceuticals Inc. Treatment of involuntary movements with 5ht1a receptor agonists
EP0650964A1 (en) 1993-11-02 1995-05-03 Duphar International Research B.V 1 2H-1-benzopyran-2-one-8-yl -piperazine derivatives
US5478572A (en) * 1994-09-06 1995-12-26 Bristol-Myers Squibb Co. Gepirone dosage form
NL9401572A (nl) * 1994-09-27 1996-05-01 Avebe Coop Verkoop Prod Zetmeelprodukten als tabletteerhulpstof, werkwijze voor het bereiden daarvan alsmede werkwijze voor het maken van tabletten.
BRPI9708389B8 (pt) 1996-03-29 2015-12-08 Duphar Int Res compostos de piperazina e piperidina, composições farmacêuticas.
GB9706089D0 (en) 1997-03-24 1997-05-14 Scherer Ltd R P Pharmaceutical composition
PA8469101A1 (es) 1998-04-09 2000-09-29 Pfizer Prod Inc Ligandos azabiciclicos de receptores 5ht1
US6376494B1 (en) * 1998-06-15 2002-04-23 American Home Products Corporation Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
US6312717B1 (en) * 1998-07-07 2001-11-06 Bristol-Myers Squibb Company Method for treatment of anxiety and depression
UA62015C2 (en) 1998-12-28 2003-12-15 Pfizer Prod Inc Benzoizoxazol derivatives, a pharmaceutical composition (variants) based thereon (variants) and a method for treatment (variants)
GB0008563D0 (en) * 2000-04-07 2000-05-24 Cambridge Discovery Chemistry Investigating different physical and/or chemical forms of materials
JP2004231514A (ja) 2000-08-31 2004-08-19 Meiji Seika Kaisha Ltd ５−ｈｔ７受容体結合能を有し、かつ代謝的に安定なテトラヒドロベンズインドール誘導体
US20030008880A1 (en) * 2001-05-02 2003-01-09 Pfizer Inc. 4-(2-Pyridyl) piperizines having 5HT7 receptor agonist activity
US6696496B2 (en) * 2002-03-28 2004-02-24 Synthon Bv Low water-soluble venlafaxine salts
FR2837822B1 (fr) * 2002-03-29 2004-06-04 Bioprojet Soc Civ Formes polymorphes du fasidotril, leurs procedes de preparation et compositions pharmaceutiques les contenant
AR048112A1 (es) * 2004-03-25 2006-03-29 Solvay Pharm Bv Derivados de 1-(2h-1-benzopiran-2-on-8-il)-piperazina para el tratamiento de dolor
US20050215551A1 (en) * 2004-03-25 2005-09-29 Solvay Pharmaceuticals B.V. 1-[2H-1-benzopyran-2-one-8-yl]- piperazine derivatives for the treatment of movement disorders

Also Published As

Publication number Publication date
JP2007530507A (ja) 2007-11-01
EP1732556A1 (en) 2006-12-20
EP1732556B1 (en) 2008-03-12
US7776860B2 (en) 2010-08-17
US8173660B2 (en) 2012-05-08
US20050215566A1 (en) 2005-09-29
TW200611900A (en) 2006-04-16
AR049478A1 (es) 2006-08-09
ATE388709T1 (de) 2008-03-15
US20110003830A1 (en) 2011-01-06
DE602005005308D1 (de) 2008-04-24
PL1732556T3 (pl) 2008-09-30
SA05260061B1 (ar) 2009-01-19
WO2005092338A1 (en) 2005-10-06
TWI340136B (en) 2011-04-11
CA2554041A1 (en) 2005-10-06
DE602005005308T2 (de) 2009-10-08

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