JP3822601B2 - 安定多形体のフリバンセリン、その製造方法及び薬剤を製造するためのその使用 - Google Patents

安定多形体のフリバンセリン、その製造方法及び薬剤を製造するためのその使用 Download PDF

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JP3822601B2
JP3822601B2 JP2003519029A JP2003519029A JP3822601B2 JP 3822601 B2 JP3822601 B2 JP 3822601B2 JP 2003519029 A JP2003519029 A JP 2003519029A JP 2003519029 A JP2003519029 A JP 2003519029A JP 3822601 B2 JP3822601 B2 JP 3822601B2
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flibanserin
polymorph
water
mixture
pharmaceutical composition
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JP2004537597A (ja
JP2004537597A5 (enExample
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カルロ ボンバルダ
エンリカ デュビーニ
アントワーヌ エザーヤ
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ビダケム ソシエタ ペル アチオニ
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    • 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

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  • 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)
JP2003519029A 2001-08-02 2002-07-30 安定多形体のフリバンセリン、その製造方法及び薬剤を製造するためのその使用 Expired - Fee Related JP3822601B2 (ja)

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 (3)

Publication Number Publication Date
JP2004537597A JP2004537597A (ja) 2004-12-16
JP2004537597A5 JP2004537597A5 (enExample) 2006-02-16
JP3822601B2 true JP3822601B2 (ja) 2006-09-20

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ID=26076670

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Application Number Title Priority Date Filing Date
JP2003519029A Expired - Fee Related JP3822601B2 (ja) 2001-08-02 2002-07-30 安定多形体のフリバンセリン、その製造方法及び薬剤を製造するためのその使用

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

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
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
AU2002331361B2 (en) 2008-06-05
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
AR036208A1 (es) 2004-08-18
EP1414816B1 (en) 2005-02-09
MY127294A (en) 2006-11-30

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