ATE288911T1 - Stabiles polymorph von flibanserin, industrielles verfahren zu dessen herstellung und dessen verwendung zur herstellung von medikamenten - Google Patents

Stabiles polymorph von flibanserin, industrielles verfahren zu dessen herstellung und dessen verwendung zur herstellung von medikamenten

Info

Publication number
ATE288911T1
ATE288911T1 AT02767277T AT02767277T ATE288911T1 AT E288911 T1 ATE288911 T1 AT E288911T1 AT 02767277 T AT02767277 T AT 02767277T AT 02767277 T AT02767277 T AT 02767277T AT E288911 T1 ATE288911 T1 AT E288911T1
Authority
AT
Austria
Prior art keywords
production
polymorphoe
flibanserin
medications
stable
Prior art date
Application number
AT02767277T
Other languages
English (en)
Inventor
Carlo Bombarda
Enrica Dubini
Antoine Ezhaya
Original Assignee
Bidachem Spa
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 Bidachem Spa filed Critical Bidachem Spa
Application granted granted Critical
Publication of ATE288911T1 publication Critical patent/ATE288911T1/de

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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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/26Radicals substituted by carbon atoms having three bonds to hetero atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P25/14Drugs 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
    • A61P25/20Hypnotics; Sedatives
    • 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
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
AT02767277T 2001-08-02 2002-07-30 Stabiles polymorph von flibanserin, industrielles verfahren zu dessen herstellung und dessen verwendung zur herstellung von medikamenten ATE288911T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP01118593 2001-08-02
EP01130180 2001-12-19
PCT/EP2002/008466 WO2003014079A1 (en) 2001-08-02 2002-07-30 Stable polymorph of flibanserin, technical process for its preparation and the use thereof for preparing medicaments

Publications (1)

Publication Number Publication Date
ATE288911T1 true ATE288911T1 (de) 2005-02-15

Family

ID=26076670

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02767277T ATE288911T1 (de) 2001-08-02 2002-07-30 Stabiles polymorph von flibanserin, industrielles verfahren zu dessen herstellung und dessen verwendung zur herstellung von medikamenten

Country Status (27)

Country Link
EP (2) EP1414816B1 (de)
JP (1) JP3822601B2 (de)
KR (1) KR100899297B1 (de)
CN (1) CN1288147C (de)
AR (2) AR036208A1 (de)
AT (1) ATE288911T1 (de)
AU (1) AU2002331361B2 (de)
BR (1) BR0211601A (de)
CA (1) CA2450093C (de)
CO (1) CO5560572A2 (de)
DE (1) DE60202958T2 (de)
DK (1) DK1414816T3 (de)
EA (1) EA006400B1 (de)
ES (1) ES2237694T3 (de)
HK (1) HK1070063A1 (de)
HR (1) HRP20040107B1 (de)
HU (1) HU228666B1 (de)
IL (2) IL159151A0 (de)
MX (1) MXPA04000913A (de)
MY (1) MY127294A (de)
NZ (1) NZ530510A (de)
PL (1) PL210224B1 (de)
PT (1) PT1414816E (de)
RS (1) RS50742B (de)
SI (1) SI1414816T1 (de)
UA (1) UA76767C2 (de)
WO (1) WO2003014079A1 (de)

Families Citing this family (26)

* 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
DE10138273A1 (de) * 2001-08-10 2003-02-27 Boehringer Ingelheim Pharma Arzneimittel mit neuroprotektiver Wirkung
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
RS51718B (en) * 2002-05-22 2011-10-31 Boehringer Ingelheim Pharma Gmbh. & Co.Kg. NEW PHARMACEUTICAL COMPOSITIONS CONTAINING FLIBANSERINE POLYMORF A
JP2008540356A (ja) * 2005-05-06 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 薬物乱用の治療方法
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
WO2007048803A1 (en) 2005-10-29 2007-05-03 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
EP1991228A1 (de) * 2006-02-28 2008-11-19 Boehringer Ingelheim International GmbH Präventionsbehandlung für herzklappenfehler mit flibanserin
JP2009536176A (ja) * 2006-05-09 2009-10-08 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 閉経後の性的欲求障害の治療のためのフリバンセリンの使用
ES2336719T3 (es) 2006-06-30 2010-04-15 Boehringer Ingelheim International Gmbh Flibanserina para el tratamiento de la incontinencia urinaria y las enfermedades relacionadas.
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
WO2008019996A2 (en) 2006-08-14 2008-02-21 Boehringer Ingelheim International Gmbh Formulations of flibanserin and method for manufacturing the same
WO2008022932A2 (en) 2006-08-25 2008-02-28 Boehringer Ingelheim International Gmbh Controlled release system and method for manufacturing the same
WO2008061966A2 (en) * 2006-11-22 2008-05-29 Boehringer Ingelheim International Gmbh New use of flibanserin
ATE524446T1 (de) 2006-12-20 2011-09-15 Boehringer Ingelheim Int Sulfatierte benzimidazolon-derivate mit gemischter serotonin-rezeptor-affinität
EP1955699A1 (de) * 2007-02-08 2008-08-13 Boehringer Ingelheim Pharma GmbH & Co. KG Verwendung von Flibanserin zur Behandlung von Schlaflosigkeit
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
EP2090297A1 (de) 2008-02-13 2009-08-19 Boehringer Ingelheim International GmbH Formulierungen aus Flibanserin
CA2686480A1 (en) * 2008-12-15 2010-06-15 Boehringer Ingelheim International Gmbh New salts
CN104926734B (zh) * 2015-07-07 2017-04-05 苏州立新制药有限公司 氟班色林的制备方法
WO2017076356A1 (zh) * 2015-11-05 2017-05-11 苏州晶云药物科技有限公司 氟班色林的新晶型及其制备方法
US11492343B2 (en) 2016-01-31 2022-11-08 Xiaoming Meng Polymorph of flibanserin and preparation method thereof and use of same
CN111303043A (zh) * 2019-04-19 2020-06-19 武汉万知化工医药有限公司 一种氟班色林盐酸盐的制备方法
CN115919860B (zh) * 2022-12-05 2023-11-10 中国药科大学 氟班色林在制备治疗雄激素脱发药物中的用途

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1251144B (it) * 1991-07-30 1995-05-04 Boehringer Ingelheim Italia Derivati del benzimidazolone

Also Published As

Publication number Publication date
DK1414816T3 (da) 2005-04-11
HRP20040107A2 (en) 2004-06-30
ES2237694T3 (es) 2005-08-01
PL364598A1 (en) 2004-12-13
UA76767C2 (uk) 2006-09-15
WO2003014079A1 (en) 2003-02-20
IL159151A (en) 2009-09-22
KR20040023704A (ko) 2004-03-18
HK1070063A1 (en) 2005-06-10
AR077416A2 (es) 2011-08-24
HRP20040107B1 (en) 2012-02-29
HU228666B1 (en) 2013-05-28
CA2450093C (en) 2008-09-23
CA2450093A1 (en) 2003-02-20
AR036208A1 (es) 2004-08-18
EA200400252A1 (ru) 2004-08-26
HUP0401201A3 (en) 2004-11-29
JP3822601B2 (ja) 2006-09-20
DE60202958T2 (de) 2006-04-06
NZ530510A (en) 2004-07-30
JP2004537597A (ja) 2004-12-16
WO2003014079A8 (en) 2003-11-20
YU7804A (sh) 2006-08-17
CN1288147C (zh) 2006-12-06
MXPA04000913A (es) 2004-10-27
CO5560572A2 (es) 2005-09-30
HUP0401201A2 (hu) 2004-10-28
SI1414816T1 (en) 2005-06-30
EP1518858A1 (de) 2005-03-30
DE60202958D1 (de) 2005-03-17
PL210224B1 (pl) 2011-12-30
MY127294A (en) 2006-11-30
IL159151A0 (en) 2004-06-01
EP1414816B1 (de) 2005-02-09
AU2002331361B2 (en) 2008-06-05
RS50742B (sr) 2010-08-31
EP1414816A1 (de) 2004-05-06
KR100899297B1 (ko) 2009-05-26
EA006400B1 (ru) 2005-12-29
CN1551879A (zh) 2004-12-01
BR0211601A (pt) 2004-08-24
PT1414816E (pt) 2005-04-29

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