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CO5560572A2 - Compuesto polimorfo estable de flibanserina, procedimiento industrial para su preparacion, y uso del mismo para preparar medicamentos - Google Patents

Compuesto polimorfo estable de flibanserina, procedimiento industrial para su preparacion, y uso del mismo para preparar medicamentos

Info

Publication number
CO5560572A2
CO5560572A2 CO04016766A CO04016766A CO5560572A2 CO 5560572 A2 CO5560572 A2 CO 5560572A2 CO 04016766 A CO04016766 A CO 04016766A CO 04016766 A CO04016766 A CO 04016766A CO 5560572 A2 CO5560572 A2 CO 5560572A2
Authority
CO
Colombia
Prior art keywords
same
flibanserin
preparation
flibanserine
water
Prior art date
Application number
CO04016766A
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
Publication of CO5560572A2 publication Critical patent/CO5560572A2/es

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
    • C07D401/06Heterocyclic 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (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)

Abstract

1.- El compuesto polimorfo A cristalino (forma A) de flibanserina 1, que tiene un máximo endotérmico a 161°C que se produce durante un análisis térmico usando DSC.2.- La flibanserina 1 que comprende la forma A de acuerdo con la reivindicación 1.3.- Un procedimiento para la preparación industrial de flibanserina 1 de acuerdo con la reivindicación 1 ó 2, caracterizado porque, en una primera operación de reacción, una benzoimidazolona 2 en la que R representa un grupo protector de aminas adecuado, es hecha reaccionar con una piperazina 3 en la que X es un grupo lábil seleccionado entre cloro, bromo, yodo, metanosulfonato, trifluorometanosulfonato y para-toluenosulfonato, en un disolvente adecuado seleccionado entre agua, alcoholes, mezclas de agua con alcoholes, disolventes apróticos polares y mezclas de los mismos con agua, en presencia de una base adecuada, y porque, en una segunda operación de reacción, el grupo protector R de aminas es escindido bajo unas condiciones de escisión adecuadas.
CO04016766A 2001-08-02 2004-02-25 Compuesto polimorfo estable de flibanserina, procedimiento industrial para su preparacion, y uso del mismo para preparar medicamentos CO5560572A2 (es)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
CO5560572A2 true CO5560572A2 (es) 2005-09-30

Family

ID=26076670

Family Applications (1)

Application Number Title Priority Date Filing Date
CO04016766A CO5560572A2 (es) 2001-08-02 2004-02-25 Compuesto polimorfo estable de flibanserina, procedimiento industrial para su preparacion, y uso del mismo para preparar medicamentos

Country Status (26)

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

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 (sr) * 2002-05-22 2011-10-31 Boehringer Ingelheim Pharma Gmbh. & Co.Kg. Nove farmaceutske kompozicije koje sadrže flibanserin polimorf a
CA2608249A1 (en) * 2005-05-06 2006-11-16 Boehringer Ingelheim International Gmbh Method for the treatment of drug abuse with flibanserin
EP1912650B8 (en) 2005-08-03 2017-10-18 Sprout Pharmaceuticals, Inc. Use of flibanserin in the treatment of obesity
EP1945214A1 (en) 2005-10-29 2008-07-23 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
CA2642368A1 (en) * 2006-02-28 2007-09-07 Boehringer Ingelheim International Gmbh Treatment of prevention of valvular heart disease with flibanserin
PT2021006E (pt) * 2006-05-09 2015-11-12 Sprout Pharmaceuticals Inc Uso de flibanserina para o tratamento de distúrbios de desejo sexual pós-menopausa
JP2009541443A (ja) 2006-06-30 2009-11-26 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 尿失禁及び関連疾患の治療のためのフリバンセリン
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
KR20090042967A (ko) 2006-08-14 2009-05-04 베링거 인겔하임 인터내셔날 게엠베하 플리반세린 제형 및 이의 제조방법
CN104721168A (zh) 2006-08-25 2015-06-24 贝林格尔·英格海姆国际有限公司 控制释放系统及其制造方法
WO2008061966A2 (en) * 2006-11-22 2008-05-29 Boehringer Ingelheim International Gmbh New use of flibanserin
WO2008074795A1 (en) 2006-12-20 2008-06-26 Boehringer Ingelheim International Gmbh Sulfated benzimidazolone derivatives having mixed serotonine 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
DK1414816T3 (da) 2005-04-11
IL159151A0 (en) 2004-06-01
HU228666B1 (en) 2013-05-28
YU7804A (sh) 2006-08-17
ATE288911T1 (de) 2005-02-15
KR100899297B1 (ko) 2009-05-26
HRP20040107A2 (en) 2004-06-30
DE60202958T2 (de) 2006-04-06
EP1518858A1 (en) 2005-03-30
WO2003014079A1 (en) 2003-02-20
MXPA04000913A (es) 2004-10-27
NZ530510A (en) 2004-07-30
UA76767C2 (uk) 2006-09-15
JP2004537597A (ja) 2004-12-16
MY127294A (en) 2006-11-30
HUP0401201A3 (en) 2004-11-29
PL364598A1 (en) 2004-12-13
PT1414816E (pt) 2005-04-29
EA006400B1 (ru) 2005-12-29
RS50742B (sr) 2010-08-31
WO2003014079A8 (en) 2003-11-20
PL210224B1 (pl) 2011-12-30
HRP20040107B1 (hr) 2012-02-29
ES2237694T3 (es) 2005-08-01
EA200400252A1 (ru) 2004-08-26
CN1288147C (zh) 2006-12-06
AR036208A1 (es) 2004-08-18
JP3822601B2 (ja) 2006-09-20
IL159151A (en) 2009-09-22
HK1070063A1 (en) 2005-06-10
AU2002331361B2 (en) 2008-06-05
AR077416A2 (es) 2011-08-24
BR0211601A (pt) 2004-08-24
HUP0401201A2 (hu) 2004-10-28
CN1551879A (zh) 2004-12-01
KR20040023704A (ko) 2004-03-18
CA2450093C (en) 2008-09-23
DE60202958D1 (de) 2005-03-17
SI1414816T1 (en) 2005-06-30
CA2450093A1 (en) 2003-02-20
EP1414816B1 (en) 2005-02-09
EP1414816A1 (en) 2004-05-06

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