AU2002331361B2 - Stable polymorph of flibanserin, technical process for its preparation and the use thereof for preparing medicaments - Google Patents

Stable polymorph of flibanserin, technical process for its preparation and the use thereof for preparing medicaments Download PDF

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Publication number
AU2002331361B2
AU2002331361B2 AU2002331361A AU2002331361A AU2002331361B2 AU 2002331361 B2 AU2002331361 B2 AU 2002331361B2 AU 2002331361 A AU2002331361 A AU 2002331361A AU 2002331361 A AU2002331361 A AU 2002331361A AU 2002331361 B2 AU2002331361 B2 AU 2002331361B2
Authority
AU
Australia
Prior art keywords
flibanserin
polymorph
medicament
water
preferred
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
Application number
AU2002331361A
Other languages
English (en)
Other versions
AU2002331361A1 (en
Inventor
Carlo Bombarda
Enrica Dubini
Antoine Ezhaya
Heinrich Schneider
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
Sprout 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 Sprout Pharmaceuticals Inc filed Critical Sprout Pharmaceuticals Inc
Publication of AU2002331361A1 publication Critical patent/AU2002331361A1/en
Application granted granted Critical
Publication of AU2002331361B2 publication Critical patent/AU2002331361B2/en
Assigned to SPROUT PHARMACEUTICALS, INC. reassignment SPROUT PHARMACEUTICALS, INC. Request for Assignment Assignors: BIDACHEM S.P.A.
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

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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)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (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)
AU2002331361A 2001-08-02 2002-07-30 Stable polymorph of flibanserin, technical process for its preparation and the use thereof for preparing medicaments Expired AU2002331361B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP01118593.1 2001-08-02
EP01118593 2001-08-02
EP01130180.1 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
AU2002331361A1 AU2002331361A1 (en) 2003-06-19
AU2002331361B2 true AU2002331361B2 (en) 2008-06-05

Family

ID=26076670

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2002331361A Expired AU2002331361B2 (en) 2001-08-02 2002-07-30 Stable polymorph of flibanserin, technical process for its preparation and the use thereof for preparing medicaments

Country Status (26)

Country Link
EP (2) EP1518858A1 (enExample)
JP (1) JP3822601B2 (enExample)
KR (1) KR100899297B1 (enExample)
CN (1) CN1288147C (enExample)
AR (2) AR036208A1 (enExample)
AT (1) ATE288911T1 (enExample)
AU (1) AU2002331361B2 (enExample)
BR (1) BR0211601A (enExample)
CA (1) CA2450093C (enExample)
CO (1) CO5560572A2 (enExample)
DE (1) DE60202958T2 (enExample)
DK (1) DK1414816T3 (enExample)
EA (1) EA006400B1 (enExample)
ES (1) ES2237694T3 (enExample)
HR (1) HRP20040107B1 (enExample)
HU (1) HU228666B1 (enExample)
IL (2) IL159151A0 (enExample)
MX (1) MXPA04000913A (enExample)
MY (1) MY127294A (enExample)
NZ (1) NZ530510A (enExample)
PL (1) PL210224B1 (enExample)
PT (1) PT1414816E (enExample)
RS (1) RS50742B (enExample)
SI (1) SI1414816T1 (enExample)
UA (1) UA76767C2 (enExample)
WO (1) WO2003014079A1 (enExample)

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
HRP20041092B1 (hr) * 2002-05-22 2013-05-31 Boehringer Ingelheim Pharma Gmbh & Co.Kg Novi farmaceutski pripravci flibanserina
WO2006119884A2 (en) * 2005-05-06 2006-11-16 Boehringer Ingelheim International Gmbh Method for the treatment of drug abuse with flibanserin
PL1912650T3 (pl) 2005-08-03 2018-01-31 Sprout Pharmaceuticals Inc Zastosowanie flibanseryny w leczeniu otyłości
CA2626134C (en) 2005-10-29 2013-12-24 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
JP2009528322A (ja) * 2006-02-28 2009-08-06 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 フリバンセリンによる弁膜性心疾患の治療又は予防
EA200802208A1 (ru) * 2006-05-09 2009-04-28 Бёрингер Ингельхайм Интернациональ Гмбх Применение флибансерина для лечения расстройств полового влечения в постклимактерический период
EP2037927B1 (en) 2006-06-30 2010-01-27 Boehringer Ingelheim International GmbH Flibanserin for the treatment of urinary incontinence and related diseases
AR062320A1 (es) 2006-08-14 2008-10-29 Boehringer Ingelheim Int Formulaciones de flibanserina y metodo para fabricarlas
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 (en) * 2007-02-08 2008-08-13 Boehringer Ingelheim Pharma GmbH & Co. KG Use of flibanserin for the treatment of insomnia
CL2008002693A1 (es) 2007-09-12 2009-10-16 Boehringer Ingelheim Int Uso de flibanserina para el tratamiento de sintomas vasomotores seleccionados de sofocos, sudores nocturnos, cambios de estado de animo e irritabilidad
EP2090297A1 (en) 2008-02-13 2009-08-19 Boehringer Ingelheim International GmbH Formulations of 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
WO2017128932A1 (zh) * 2016-01-31 2017-08-03 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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0526434A1 (en) * 1991-07-30 1993-02-03 BOEHRINGER INGELHEIM ITALIA S.p.A. Benzimidazolone derivatives as 5-HT1A and 5-HT2 antagonists

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0526434A1 (en) * 1991-07-30 1993-02-03 BOEHRINGER INGELHEIM ITALIA S.p.A. Benzimidazolone derivatives as 5-HT1A and 5-HT2 antagonists

Also Published As

Publication number Publication date
PL210224B1 (pl) 2011-12-30
JP2004537597A (ja) 2004-12-16
RS50742B (sr) 2010-08-31
EA200400252A1 (ru) 2004-08-26
CN1551879A (zh) 2004-12-01
PL364598A1 (en) 2004-12-13
IL159151A0 (en) 2004-06-01
HK1070063A1 (en) 2005-06-10
EP1414816A1 (en) 2004-05-06
WO2003014079A1 (en) 2003-02-20
HRP20040107A2 (en) 2004-06-30
HUP0401201A2 (hu) 2004-10-28
EA006400B1 (ru) 2005-12-29
EP1518858A1 (en) 2005-03-30
NZ530510A (en) 2004-07-30
CN1288147C (zh) 2006-12-06
CA2450093C (en) 2008-09-23
PT1414816E (pt) 2005-04-29
WO2003014079A8 (en) 2003-11-20
HU228666B1 (en) 2013-05-28
DE60202958D1 (de) 2005-03-17
UA76767C2 (uk) 2006-09-15
YU7804A (sh) 2006-08-17
HUP0401201A3 (en) 2004-11-29
KR20040023704A (ko) 2004-03-18
AR077416A2 (es) 2011-08-24
HRP20040107B1 (hr) 2012-02-29
ATE288911T1 (de) 2005-02-15
CA2450093A1 (en) 2003-02-20
ES2237694T3 (es) 2005-08-01
SI1414816T1 (en) 2005-06-30
MXPA04000913A (es) 2004-10-27
CO5560572A2 (es) 2005-09-30
KR100899297B1 (ko) 2009-05-26
IL159151A (en) 2009-09-22
DK1414816T3 (da) 2005-04-11
DE60202958T2 (de) 2006-04-06
BR0211601A (pt) 2004-08-24
JP3822601B2 (ja) 2006-09-20
AR036208A1 (es) 2004-08-18
EP1414816B1 (en) 2005-02-09
MY127294A (en) 2006-11-30

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Legal Events

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DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: ADD CO-INVENTOR SCHNEIDER, HEINRICH

FGA Letters patent sealed or granted (standard patent)
PC Assignment registered

Owner name: SPROUT PHARMACEUTICALS, INC.

Free format text: FORMER OWNER WAS: BIDACHEM S.P.A.

MK14 Patent ceased section 143(a) (annual fees not paid) or expired