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
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 - Fee Related
Application number
CA 2417081
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English (en)
Other versions
CA2417081A1 (fr
Inventor
Enzo Cereda
Luciano Maiocchi
Alessandro Brambilla
Ettore Giraldo
Eugenia Monferini
Giovanni Battista Schiavi
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.)
Sprout Pharmaceuticals Inc
Original Assignee
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
US10675280B2 (en) 2001-10-20 2020-06-09 Sprout Pharmaceuticals, Inc. Treating sexual desire disorders with flibanserin
UA78974C2 (en) 2001-10-20 2007-05-10 Boehringer Ingelheim Pharma Use of flibanserin for treating disorders of sexual desire
EP1847530A1 (fr) * 2005-01-31 2007-10-24 Kyowa Hakko Kogyo Co., Ltd. Derive diamine
MY150958A (en) * 2005-06-16 2014-03-31 Astrazeneca Ab Compounds for the treatment of multi-drug resistant bacterial infections
JP2009503020A (ja) 2005-08-03 2009-01-29 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 肥満症の治療におけるフリバンセリンの使用
AR056097A1 (es) * 2005-09-29 2007-09-19 Wyeth Corp Derivados de propilamina sustituida y metodos para su utilizacion
ATE524446T1 (de) 2006-12-20 2011-09-15 Boehringer Ingelheim Int Sulfatierte benzimidazolon-derivate mit gemischter serotonin-rezeptor-affinität
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
WO2011032903A1 (fr) * 2009-09-21 2011-03-24 Neurosearch A/S Dérivés de pipérazinyl-alkyl-benzoimidazol-2-one et leur utilisation comme inhibiteurs de recaptage de neurotransmetteurs monoamines

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
DE69531476T2 (de) * 1994-09-12 2004-06-09 Lilly Industries Ltd., Basingstoke Serotonergische Modulatoren
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
EP1322622A2 (fr) 2003-07-02
WO2002024661A2 (fr) 2002-03-28
EP1322622B1 (fr) 2012-10-31
JP2004509872A (ja) 2004-04-02
CA2417081A1 (fr) 2002-03-28
JP5062938B2 (ja) 2012-10-31
AU2002223528A1 (en) 2002-04-02
WO2002024661A3 (fr) 2002-07-18
MXPA03002370A (es) 2003-10-15

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