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AU2001293804A1 - New benzimidazolone derivatives displaying affinity at the serotonin and dopamine receptors - Google Patents

New benzimidazolone derivatives displaying affinity at the serotonin and dopamine receptors

Info

Publication number
AU2001293804A1
AU2001293804A1 AU2001293804A AU9380401A AU2001293804A1 AU 2001293804 A1 AU2001293804 A1 AU 2001293804A1 AU 2001293804 A AU2001293804 A AU 2001293804A AU 9380401 A AU9380401 A AU 9380401A AU 2001293804 A1 AU2001293804 A1 AU 2001293804A1
Authority
AU
Australia
Prior art keywords
serotonin
dopamine receptors
benzimidazolone derivatives
displaying affinity
new
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.)
Abandoned
Application number
AU2001293804A
Inventor
Dr. Alessandro Brambilla
Enzo Cereda
Ettore Giraldo
Luciano Maiocchi
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.)
Boehringer Ingelheim Pharma GmbH and Co KG
Original Assignee
Boehringer Ingelheim Pharma GmbH and Co KG
Boehringer Ingelheim Pharmaceuticals Inc
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 Pharma GmbH and Co KG, Boehringer Ingelheim Pharmaceuticals Inc filed Critical Boehringer Ingelheim Pharma GmbH and Co KG
Publication of AU2001293804A1 publication Critical patent/AU2001293804A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; 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
    • C07D235/26Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems

Landscapes

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

N, N'-Disubtituted benzimidazolone derivatives of general formula (I) wherein R<1> is hydrogen, alkyl or cycloaljylalkyl, A is alkenylene and R<2> and R<3> together with N form sepecified cyclic system are serotonine or dopamine receptor ligands useful in the treatment of anxiety and affective disorders.
AU2001293804A 2000-09-19 2001-09-11 New benzimidazolone derivatives displaying affinity at the serotonin and dopamine receptors Abandoned AU2001293804A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP00830625 2000-09-19
EP00830625 2000-09-19
PCT/EP2001/010465 WO2002024662A1 (en) 2000-09-19 2001-09-11 New benzimidazolone derivatives displaying affinity at the serotonin and dopamine receptors

Publications (1)

Publication Number Publication Date
AU2001293804A1 true AU2001293804A1 (en) 2002-04-02

Family

ID=8175484

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001293804A Abandoned AU2001293804A1 (en) 2000-09-19 2001-09-11 New benzimidazolone derivatives displaying affinity at the serotonin and dopamine receptors

Country Status (9)

Country Link
EP (1) EP1322621B1 (en)
JP (1) JP5062939B2 (en)
AT (1) ATE341538T1 (en)
AU (1) AU2001293804A1 (en)
CA (1) CA2417082C (en)
DE (1) DE60123643T2 (en)
ES (1) ES2273891T3 (en)
MX (1) MXPA03002329A (en)
WO (1) WO2002024662A1 (en)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7183410B2 (en) 2001-08-02 2007-02-27 Bidachem S.P.A. Stable polymorph of flibanserin
US7087593B2 (en) 2001-10-02 2006-08-08 Acadia Pharmaceuticals Inc. Benzimidazolidinone derivatives as muscarinic agents
US6951849B2 (en) 2001-10-02 2005-10-04 Acadia Pharmaceuticals Inc. Benzimidazolidinone derivatives as muscarinic agents
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
ES2646326T3 (en) 2005-08-03 2017-12-13 Sprout Pharmaceuticals, Inc. Use of flibanserin in the treatment of obesity
CA2626134C (en) 2005-10-29 2013-12-24 Boehringer Ingelheim International Gmbh Benzimidazolone derivatives for the treatment of premenstrual and other female sexual disorders
EP2024364A1 (en) * 2006-05-26 2009-02-18 Neuromed Pharmaceuticals, Ltd. Heterocyclic compounds as calcium channel blockers
ATE456369T1 (en) 2006-06-30 2010-02-15 Boehringer Ingelheim Int FLIBANSERIN FOR THE TREATMENT OF URINARY INCONTINENCE AND ASSOCIATED DISEASES
AU2007286288A1 (en) 2006-08-14 2008-02-21 Boehringer Ingelheim International Gmbh Formulations of flibanserin and method for manufacturing the same
BRPI0716436B8 (en) 2006-08-25 2021-05-25 Boehringer Ingelheim Int controlled release system and method for manufacturing it
KR100871077B1 (en) 2007-05-11 2008-11-28 한국화학연구원 Aryl piperidine group-containing imidazole derivatives, preparation method thereof and pharmaceutical composition comprising the same as an active ingredient
JP5514716B2 (en) * 2007-05-11 2014-06-04 コリア・リサーチ・インスティテュート・オブ・ケミカル・テクノロジー Imidazole derivative having arylpiperidine substituent, method for producing the same, and pharmaceutical composition containing the same
CL2008002693A1 (en) 2007-09-12 2009-10-16 Boehringer Ingelheim Int Use of flibanserin for the treatment of selected vasomotor symptoms of hot flashes, night sweats, mood swings, and irritability
CN116444484B (en) * 2021-10-25 2025-07-15 江苏恩华药业股份有限公司 Salts of 1,5-dihydro-2,4-benzodiazepine-3-one derivatives and their applications

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2675800A1 (en) * 1991-04-26 1992-10-30 Rhone Poulenc Rorer Sa HETEROCYCLIC ANTISEROTONINE DERIVATIVES AND PREPARATION AND MEDICAMENTS CONTAINING SAME.
IT1251144B (en) * 1991-07-30 1995-05-04 Boehringer Ingelheim Italia BENZIMIDAZOLONE DERIVATIVES
ES2163506T3 (en) * 1994-06-14 2002-02-01 Pfizer DERIVATIVES OF BENCIMIDAZOLONA WITH CENTRAL DOPAMINERGIC ACTIVITY.
DE69531476T2 (en) * 1994-09-12 2004-06-09 Lilly Industries Ltd., Basingstoke Serotonergic modulators

Also Published As

Publication number Publication date
JP2004509873A (en) 2004-04-02
ATE341538T1 (en) 2006-10-15
CA2417082A1 (en) 2002-03-28
DE60123643T2 (en) 2007-08-16
DE60123643D1 (en) 2006-11-16
WO2002024662A1 (en) 2002-03-28
JP5062939B2 (en) 2012-10-31
EP1322621A1 (en) 2003-07-02
ES2273891T3 (en) 2007-05-16
MXPA03002329A (en) 2003-10-15
EP1322621B1 (en) 2006-10-04
CA2417082C (en) 2009-11-17

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