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PE20010600A1 - Derivados de bencimidazolonas que tienen afinidad para receptores mezclados de serotonina y dopamina - Google Patents

Derivados de bencimidazolonas que tienen afinidad para receptores mezclados de serotonina y dopamina

Info

Publication number
PE20010600A1
PE20010600A1 PE2000000977A PE0009772000A PE20010600A1 PE 20010600 A1 PE20010600 A1 PE 20010600A1 PE 2000000977 A PE2000000977 A PE 2000000977A PE 0009772000 A PE0009772000 A PE 0009772000A PE 20010600 A1 PE20010600 A1 PE 20010600A1
Authority
PE
Peru
Prior art keywords
ona
piperazin
trifluoromethyl
hydroxy
phenyl
Prior art date
Application number
PE2000000977A
Other languages
English (en)
Inventor
Enzo Cereda
Maura Bignotti
Giovanni Battista Schiavi
Original Assignee
Boehringer Ingelheim Italia
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 Boehringer Ingelheim Italia filed Critical Boehringer Ingelheim Italia
Publication of PE20010600A1 publication Critical patent/PE20010600A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/26—Oxygen atoms
    • 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
    • A61P25/14—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
    • A61P25/24—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

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)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A 1,3-DIHIDROBENCIMIDAZOL-2-ONA SUSTITUIDOS DE FORMULA I, DONDE R1, R2, R3, R4 SON H, OH, CON LA CONDICION QUE R1, R2, R3, R4 NO SON A LA VEZ H; SON COMPUESTOS PREFERIDOS 5-HIDROXI-1-{2-[4-(3-TRIFLUOROMETIL-FENIL)-PIPERAZIN-1-IL]ETIL}-1,3-DIHIDROBENCIMIDAZOL-2-ONA, 6-HIDROXI-1-{2-[4-(3-TRIFLUOROMETIL-FENIL)-PIPERAZIN-1-IL]-ETIL}-1,3-DIHIDROBENCIMIDAZOL-2-ONA, 4-HIDROXI-1-{2-[4-(3-TRIFLUOROMETIL-FENIL)-PIPERAZIN-1-IL]-ETIL}-1,3-DIHIDROBENCIMIDAZOL-2-ONA, 7-HIDROXI-1-{2-[4-(3-TRIFLUOROMETIL-FENIL)PIPERAZIN-1-IL]-ETIL}-1,3-DIHIDROBENCIMIDAZOL-2-ONA, 1-{2-[4-(4-HIDROXI-5-TRIFLUOROMETIL-FENIL-PIPERAZIN-1-IL]-ETIL}-1,3-DIHIDROBENCIMIDAZOL-2-ONA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION QUE COMPRENDE LA LIBERACION DEL GRUPO HIDROXI POR DISOCIACION DEL GRUPO PROTECTOR, LA DESPROTECCION DEL GRUPO HIDROXI SE DA POR TRATAMIENTO CON ACIDOS ACUOSOS FUERTES COMO ACIDO BROMHIDRICO A ALTAS TEMPERATURAS O POR TRATAMIENTO CON DERIVADOS DE BORO (BBr3) A BAJAS TEMPERATURAS EN DISOLVENTES CLORADOS. LOS COMPUESTOS I SE FIJAN A LOS RECEPTORES DE SEROTONINA Y DOPAMINA Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE TRASTORNOS DEL SNC COMO DEPRESION, ESQUIZOFRENIA, ENFERMEDAD DE PARKINSON, ANSIEDAD, PERTURBACIONES DEL SUENO, TRASTORNOS SEXUALES
PE2000000977A 1999-09-22 2000-09-20 Derivados de bencimidazolonas que tienen afinidad para receptores mezclados de serotonina y dopamina PE20010600A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT1999MI001964A IT1313625B1 (it) 1999-09-22 1999-09-22 Derivati benzimidazolonici aventi affinita' mista per i recettori diserotonina e dopamina.

Publications (1)

Publication Number Publication Date
PE20010600A1 true PE20010600A1 (es) 2001-06-04

Family

ID=11383635

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000977A PE20010600A1 (es) 1999-09-22 2000-09-20 Derivados de bencimidazolonas que tienen afinidad para receptores mezclados de serotonina y dopamina

Country Status (16)

Country Link
US (1) US6281218B1 (es)
EP (1) EP1218352B1 (es)
JP (2) JP4989002B2 (es)
AR (1) AR025739A1 (es)
AT (1) ATE266644T1 (es)
AU (1) AU7653700A (es)
CA (1) CA2381819C (es)
CO (1) CO5210864A1 (es)
DE (1) DE60010732T2 (es)
DK (1) DK1218352T3 (es)
ES (1) ES2220541T3 (es)
IT (1) IT1313625B1 (es)
MX (1) MXPA02001986A (es)
PE (1) PE20010600A1 (es)
PT (1) PT1218352E (es)
WO (1) WO2001021593A1 (es)

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IT1313625B1 (it) * 1999-09-22 2002-09-09 Boehringer Ingelheim Italia Derivati benzimidazolonici aventi affinita' mista per i recettori diserotonina e dopamina.
US7183410B2 (en) * 2001-08-02 2007-02-27 Bidachem S.P.A. Stable polymorph of flibanserin
US20030060475A1 (en) * 2001-08-10 2003-03-27 Boehringer Ingelheim Pharma Kg Method of using flibanserin for neuroprotection
UA78974C2 (en) * 2001-10-20 2007-05-10 Boehringer Ingelheim Pharma Use of flibanserin for treating disorders of sexual desire
US10675280B2 (en) 2001-10-20 2020-06-09 Sprout Pharmaceuticals, Inc. Treating sexual desire disorders with flibanserin
US7033345B2 (en) * 2002-05-21 2006-04-25 Advanced Cardiovascular Systems, Inc. Deflectable microimplant delivery system
US20040048877A1 (en) * 2002-05-22 2004-03-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions containing flibanserin
WO2005021545A1 (en) * 2003-09-03 2005-03-10 Galapagos Nv IMIDAZO[1,5-a]PYRIDINE OR IMIDAZO[1,5-a]PIPERIDINE DERIVATIVES AND THEIR USE FOR THE PREPARATION OF MEDICAMENT AGAINST 5-HT2A RECEPTOR-RELATED DISORDERS
US20050215589A1 (en) * 2003-09-03 2005-09-29 Roger Crossley Inhibitors of 5-HT2A receptor
TW200533348A (en) * 2004-02-18 2005-10-16 Theravance Inc Indazole-carboxamide compounds as 5-ht4 receptor agonists
US7728006B2 (en) * 2004-04-07 2010-06-01 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
TWI351282B (en) 2004-04-07 2011-11-01 Theravance Inc Quinolinone-carboxamide compounds as 5-ht4 recepto
US8309575B2 (en) 2004-04-07 2012-11-13 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
WO2005102342A1 (en) * 2004-04-22 2005-11-03 Boehringer Ingelheim International Gmbh New pharmaceutical compositions for the treatment of sexual disorders ii
US20050239798A1 (en) * 2004-04-22 2005-10-27 Boehringer Ingelheim Pharmaceuticals, Inc. Method for the treatment of premenstrual and other female sexual disorders
US20060025420A1 (en) * 2004-07-30 2006-02-02 Boehringer Ingelheimn International GmbH Pharmaceutical compositions for the treatment of female sexual disorders
CA2576812A1 (en) * 2004-09-03 2006-03-09 Boehringer Ingelheim International Gmbh Method for the treatment of attention deficit hyperactivity disorder
ES2332808T3 (es) * 2004-11-05 2010-02-12 Theravance, Inc. Compuestos agonistas del receptor 5-ht4.
JP5042028B2 (ja) * 2004-11-05 2012-10-03 セラヴァンス， インコーポレーテッド キノリノン−カルボキサミド化合物
US7419989B2 (en) * 2004-12-22 2008-09-02 Theravance, Inc. Indazole-carboxamide compounds
NZ560828A (en) * 2005-03-02 2011-01-28 Theravance Inc Quinolinone compounds as 5-HT4 receptor agonists
WO2006096439A2 (en) * 2005-03-04 2006-09-14 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for the treatment and/or prevention of schizophrenia and related diseases
EP1858516A1 (en) * 2005-03-04 2007-11-28 Boehringer Ingelheim International GmbH Pharmaceutical compositions for the treatment and/or prevention of depression
EP1858515A2 (en) * 2005-03-04 2007-11-28 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for the treatment and/or prevention of anxiety disorders
EP1904182A2 (en) * 2005-05-06 2008-04-02 Boehringer Ingelheim International GmbH Method for the treatment of drug abuse with flibanserin
WO2006125041A1 (en) * 2005-05-19 2006-11-23 Boehringer Ingelheim International Gmbh Method for the treatment of sexual dysfunctions due to medical conditions
JP2008540673A (ja) * 2005-05-19 2008-11-20 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 薬剤誘発性性機能不全の治療方法
ATE495171T1 (de) * 2005-06-07 2011-01-15 Theravance Inc Benzimidazoloncarbonsäureamidverbindungen als agonisten des 5-ht4-rezeptors
US8227476B2 (en) 2005-08-03 2012-07-24 Sprout Pharmaceuticals, Inc. Use of flibanserin in the treatment of obesity
US20070123540A1 (en) * 2005-10-29 2007-05-31 Angelo Ceci Sexual desire enhancing medicaments comprising benzimidazolone derivatives
EP1945214A1 (en) * 2005-10-29 2008-07-23 Boehringer Ingelheim International GmbH Benzimidazolone derivatives for the treatment of premenstrual and other female sexual disorders
US20070105869A1 (en) * 2005-11-08 2007-05-10 Stephane Pollentier Use of flibanserin for the treatment of pre-menopausal sexual desire disorders
MY143574A (en) * 2005-11-22 2011-05-31 Theravance Inc Carbamate compounds as 5-ht4 receptor agonists
WO2007096300A1 (en) * 2006-02-20 2007-08-30 Boehringer Ingelheim International Gmbh Benzimidazolone derivatives for the treatment of urinary incontinence
CA2649938A1 (en) * 2006-05-09 2007-11-15 Boehringer Ingelheim International Gmbh Use of flibanserin for the treatment of post-menopausal sexual desire disorders
ES2336719T3 (es) 2006-06-30 2010-04-15 Boehringer Ingelheim International Gmbh Flibanserina para el tratamiento de la incontinencia urinaria y las enfermedades relacionadas.
US20090318469A1 (en) * 2006-07-14 2009-12-24 Boehringer Ingelheim International Gmbh Use of Flibanserin for the Treatment of Sexual Disorders in Females
JP5793828B2 (ja) * 2006-08-14 2015-10-14 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング フリバンセリンの製剤及びその製造方法
CL2007002214A1 (es) * 2006-08-14 2008-03-07 Boehringer Ingelheim Int Composicion farmaceutica en la forma de comprimido, donde al menos la longitud del comprimido en el estado anterior de la aplicacion es al menos 7/12 del diametro pilorico del paciente y despues de ingerirlo en estado alimentado, la longitud del comp
AR062321A1 (es) * 2006-08-25 2008-10-29 Boehringer Ingelheim Int Sistema de liberacion controlada y metodo para fabricarlo
WO2008061968A1 (en) * 2006-11-22 2008-05-29 Boehringer Ingelheim International Gmbh Benzimidazolone derivates in the treatment of pulmonary arterial hypertension
EP2097389B1 (en) * 2006-12-20 2011-09-14 Boehringer Ingelheim International GmbH Sulfated benzimidazolone derivatives having mixed serotonine receptor affinity
JP5087011B2 (ja) * 2007-01-23 2012-11-28 馨 井上 眼疾患モデル用非ヒト動物
PE20091188A1 (es) 2007-09-12 2009-08-31 Boehringer Ingelheim Int Compuesto 1-[2-(4-(3-trifluorometil-fenil)piperazin-1-il)etil]-2,3-dihidro-1h-benzimidazol-2-ona (flibanserina), sus sales de adicion y composiciones farmaceuticas que los contienen
WO2009092720A1 (en) * 2008-01-24 2009-07-30 Neurosearch A/S 4-phenyl-piperazin-1-yl-alkyl-benzoimidazol-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
CA2686480A1 (en) 2008-12-15 2010-06-15 Boehringer Ingelheim International Gmbh New salts
BRPI1003506B1 (pt) 2010-09-24 2019-12-03 Ache Int Bvi Ltd composto alquil-piperazino-fenil-4(3h)quinazolinonas e uso do composto alquil-piperazino-fenil-4(3h)quinazolinonas associado aos receptores serotoninérgicos 5-ht1a e 5-ht2a

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IT1251144B (it) * 1991-07-30 1995-05-04 Boehringer Ingelheim Italia Derivati del benzimidazolone
IT1313625B1 (it) * 1999-09-22 2002-09-09 Boehringer Ingelheim Italia Derivati benzimidazolonici aventi affinita' mista per i recettori diserotonina e dopamina.

Also Published As

Publication number Publication date
EP1218352B1 (en) 2004-05-12
CO5210864A1 (es) 2002-10-30
US6281218B1 (en) 2001-08-28
EP1218352A1 (en) 2002-07-03
PT1218352E (pt) 2004-09-30
DE60010732D1 (de) 2004-06-17
ITMI991964A1 (it) 2001-03-22
JP2012067105A (ja) 2012-04-05
CA2381819A1 (en) 2001-03-29
CA2381819C (en) 2007-03-13
AR025739A1 (es) 2002-12-11
JP2003509496A (ja) 2003-03-11
DK1218352T3 (da) 2004-06-28
ATE266644T1 (de) 2004-05-15
ES2220541T3 (es) 2004-12-16
JP4989002B2 (ja) 2012-08-01
DE60010732T2 (de) 2005-05-25
IT1313625B1 (it) 2002-09-09
ITMI991964A0 (it) 1999-09-22
MXPA02001986A (es) 2002-10-31
WO2001021593A1 (en) 2001-03-29
AU7653700A (en) 2001-04-24

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