CA2417081C - Derives benzimidazolone n,n'-disubstitues presentant une affinite pour les recepteurs de la serotonine et de la dopamine - Google Patents

Derives benzimidazolone n,n'-disubstitues presentant une affinite pour les recepteurs de la serotonine et de la dopamine Download PDF

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Publication number
CA2417081C
CA2417081C CA 2417081 CA2417081A CA2417081C CA 2417081 C CA2417081 C CA 2417081C CA 2417081 CA2417081 CA 2417081 CA 2417081 A CA2417081 A CA 2417081A CA 2417081 C CA2417081 C CA 2417081C
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CA
Canada
Prior art keywords
substituted
group selected
alkyl
compound
heterocyclic ring
Prior art date
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Expired - Fee Related
Application number
CA 2417081
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English (en)
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CA2417081A1 (fr
Inventor
Enzo Cereda
Luciano Maiocchi
Alessandro Brambilla
Ettore Giraldo
Eugenia Monferini
Giovanni Battista Schiavi
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Sprout Pharmaceuticals Inc
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Boehringer Ingelheim Pharma GmbH and Co KG
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Publication of CA2417081A1 publication Critical patent/CA2417081A1/fr
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Publication of CA2417081C publication Critical patent/CA2417081C/fr
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P25/22—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

L'invention concerne des dérivés benzimidazolone N,N'disubstitués, pharmacologiquement actifs, de formule générale (I) dans laquelle R?1¿, R?2¿, R?3¿, et A sont définis dans les spécifications et dans les revendications, leurs sels, acceptable sur le plan pharmaceutique, ainsi que leur préparation et leur utilisation à des fins thérapeutiques.
CA 2417081 2000-09-19 2001-09-08 Derives benzimidazolone n,n'-disubstitues presentant une affinite pour les recepteurs de la serotonine et de la dopamine Expired - Fee Related CA2417081C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP00830624.3 2000-09-19
EP00830624 2000-09-19
PCT/EP2001/010376 WO2002024661A2 (fr) 2000-09-19 2001-09-08 Derives benzimidazolone n,n'-disubstitues presentant une affinite pour les recepteurs de la serotonine et de la dopamine

Publications (2)

Publication Number Publication Date
CA2417081A1 CA2417081A1 (fr) 2002-03-28
CA2417081C true CA2417081C (fr) 2008-08-05

Family

ID=8175483

Family Applications (1)

Application Number Title Priority Date Filing Date
CA 2417081 Expired - Fee Related CA2417081C (fr) 2000-09-19 2001-09-08 Derives benzimidazolone n,n'-disubstitues presentant une affinite pour les recepteurs de la serotonine et de la dopamine

Country Status (6)

Country Link
EP (1) EP1322622B1 (fr)
JP (1) JP5062938B2 (fr)
AU (1) AU2002223528A1 (fr)
CA (1) CA2417081C (fr)
MX (1) MXPA03002370A (fr)
WO (1) WO2002024661A2 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US20090181948A1 (en) * 2005-01-31 2009-07-16 Kyowa Hakko Kogyo Co., Ltd. Diamine derivative
MY150958A (en) * 2005-06-16 2014-03-31 Astrazeneca Ab Compounds for the treatment of multi-drug resistant bacterial infections
CA2617546C (fr) 2005-08-03 2014-07-15 Boehringer Ingelheim International Gmbh Utilisation de la flibanserine dans le traitement de l'obesite
CN101277933A (zh) 2005-09-29 2008-10-01 惠氏公司 取代丙胺衍生物和其使用方法
EP2097389B1 (fr) 2006-12-20 2011-09-14 Boehringer Ingelheim International GmbH Dérivés de benzimidazolone sulfatés ayant une affinité mixte au récepteur de la sérotonine
EP2238117A1 (fr) * 2008-01-24 2010-10-13 NeuroSearch A/S Dérivés de 4-phényl-pipérazin-1-yl-alkyl-benzoimidazol-2-one et leur utilisation en tant qu'inhibiteurs de la réabsorption des neurotransmetteurs monoamines
US20120220604A1 (en) * 2009-09-21 2012-08-30 Neurosearch A/S Piperazinyl-alkyl-benzoimidazol-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
YU39992B (en) * 1976-04-02 1985-06-30 Janssen Pharmaceutica Nv Process for obtaining new piperazine and piperidine derivatives
US4200641A (en) * 1976-12-21 1980-04-29 Janssen Pharmaceutica, N.V. 1-[(Heterocyclyl)-alkyl]-4-diarylmethoxy piperidine derivatives
FR2675800A1 (fr) * 1991-04-26 1992-10-30 Rhone Poulenc Rorer Sa Derives heterocycliques antiserotonines leur preparation et les medicaments les contenant.
IT1251144B (it) * 1991-07-30 1995-05-04 Boehringer Ingelheim Italia Derivati del benzimidazolone
ES2204932T3 (es) * 1994-09-12 2004-05-01 Eli Lilly And Company Limited Moduladores serotonergicos.
US5883094A (en) * 1995-04-24 1999-03-16 Pfizer Inc. Benzimidazolone derivatives with central dopaminergic activity
GB9613423D0 (en) * 1996-06-26 1996-08-28 Lilly Industries Ltd Pharmaceutical compounds

Also Published As

Publication number Publication date
WO2002024661A2 (fr) 2002-03-28
EP1322622A2 (fr) 2003-07-02
AU2002223528A1 (en) 2002-04-02
MXPA03002370A (es) 2003-10-15
CA2417081A1 (fr) 2002-03-28
EP1322622B1 (fr) 2012-10-31
JP5062938B2 (ja) 2012-10-31
WO2002024661A3 (fr) 2002-07-18
JP2004509872A (ja) 2004-04-02

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