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DE60202958D1 - 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
DE60202958D1
DE60202958D1 DE60202958T DE60202958T DE60202958D1 DE 60202958 D1 DE60202958 D1 DE 60202958D1 DE 60202958 T DE60202958 T DE 60202958T DE 60202958 T DE60202958 T DE 60202958T DE 60202958 D1 DE60202958 D1 DE 60202958D1
Authority
DE
Germany
Prior art keywords
production
flibanserin
medicaments
industrial process
stable polymorph
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 - Lifetime
Application number
DE60202958T
Other languages
English (en)
Other versions
DE60202958T2 (de
Inventor
Carlo Bombarda
Enrica Dubini
Antoine Ezhaya
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.)
Bidachem SpA
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 DE60202958D1 publication Critical patent/DE60202958D1/de
Publication of DE60202958T2 publication Critical patent/DE60202958T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/20—Heterocyclic 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
    • C07D233/26—Radicals substituted by carbon atoms having three bonds to hetero 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
    • 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
    • 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
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design 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)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
DE60202958T 2001-08-02 2002-07-30 Stabiles polymorph von flibanserin, industrielles verfahren zu dessen herstellung und dessen verwendung zur herstellung von medikamenten Expired - Lifetime DE60202958T2 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP01118593 2001-08-02
EP01118593 2001-08-02
EP01130180 2001-12-19
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 (2)

Publication Number Publication Date
DE60202958D1 true DE60202958D1 (de) 2005-03-17
DE60202958T2 DE60202958T2 (de) 2006-04-06

Family

ID=26076670

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60202958T Expired - Lifetime DE60202958T2 (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) EP1518858A1 (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
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
CA2483597C (en) * 2002-05-22 2010-02-09 Boehringer Ingelheim Pharma Gmbh & Co. Kg New pharmaceutical compositions containing flibanserin polymorph a
WO2006119884A2 (en) * 2005-05-06 2006-11-16 Boehringer Ingelheim International Gmbh Method for the treatment of drug abuse with flibanserin
US8227476B2 (en) 2005-08-03 2012-07-24 Sprout Pharmaceuticals, Inc. Use of flibanserin in the treatment of obesity
EP1945214A1 (de) 2005-10-29 2008-07-23 Boehringer Ingelheim International GmbH Benzimidazolon-derivate zur behandlung von prämenstruellen und anderen sexuellen störungen der frau
US20070105869A1 (en) * 2005-11-08 2007-05-10 Stephane Pollentier Use of flibanserin for the treatment of pre-menopausal sexual desire disorders
CA2642368A1 (en) * 2006-02-28 2007-09-07 Boehringer Ingelheim International Gmbh Treatment of prevention of valvular heart disease with flibanserin
PL2021006T3 (pl) * 2006-05-09 2015-12-31 Sprout Pharmaceuticals Inc Zastosowanie flibanseryny do leczenia pomenopauzalnych zaburzeń popędu płciowego
ATE456369T1 (de) 2006-06-30 2010-02-15 Boehringer Ingelheim Int Flibanserin zur behandlung von harninkontinenz und assoziierten erkrankungen
AU2007286288A1 (en) 2006-08-14 2008-02-21 Boehringer Ingelheim International Gmbh Formulations of flibanserin and method for manufacturing the same
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
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
US8722682B2 (en) 2006-12-20 2014-05-13 Sprout Pharmaceuticals, Inc. Sulfated benzimidazolone derivatives having mixed serotonin receptor affinity
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
CN108699007A (zh) * 2016-01-31 2018-10-23 孟晓明 氟班色林的新晶型及其制备方法及其用途
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
HK1070063A1 (en) 2005-06-10
JP3822601B2 (ja) 2006-09-20
ES2237694T3 (es) 2005-08-01
MY127294A (en) 2006-11-30
UA76767C2 (uk) 2006-09-15
BR0211601A (pt) 2004-08-24
WO2003014079A8 (en) 2003-11-20
CA2450093A1 (en) 2003-02-20
EA200400252A1 (ru) 2004-08-26
EP1414816B1 (de) 2005-02-09
HUP0401201A3 (en) 2004-11-29
CN1288147C (zh) 2006-12-06
HRP20040107A2 (en) 2004-06-30
EA006400B1 (ru) 2005-12-29
CN1551879A (zh) 2004-12-01
CA2450093C (en) 2008-09-23
EP1518858A1 (de) 2005-03-30
HU228666B1 (en) 2013-05-28
YU7804A (sh) 2006-08-17
IL159151A0 (en) 2004-06-01
KR20040023704A (ko) 2004-03-18
HUP0401201A2 (hu) 2004-10-28
AR036208A1 (es) 2004-08-18
IL159151A (en) 2009-09-22
RS50742B (sr) 2010-08-31
CO5560572A2 (es) 2005-09-30
PL364598A1 (en) 2004-12-13
AR077416A2 (es) 2011-08-24
MXPA04000913A (es) 2004-10-27
KR100899297B1 (ko) 2009-05-26
PT1414816E (pt) 2005-04-29
PL210224B1 (pl) 2011-12-30
WO2003014079A1 (en) 2003-02-20
SI1414816T1 (en) 2005-06-30
DE60202958T2 (de) 2006-04-06
ATE288911T1 (de) 2005-02-15
HRP20040107B1 (en) 2012-02-29
DK1414816T3 (da) 2005-04-11
AU2002331361B2 (en) 2008-06-05
JP2004537597A (ja) 2004-12-16
NZ530510A (en) 2004-07-30
EP1414816A1 (de) 2004-05-06

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8381 Inventor (new situation)

Inventor name: BOMBARDA, CARLO, CHESTER, US

Inventor name: DUBINI, ENRICA, I-ZIP 20135 MILANO, IT

Inventor name: EZHAYA, ANTOINE, I-ZIP 20141 MILANO, IT

Inventor name: SCHNEIDER, HEINRICH, DR., 55218 INGELHEIM, DE