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AR036208A1 - 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
AR036208A1
AR036208A1 ARP020102942A ARP020102942A AR036208A1 AR 036208 A1 AR036208 A1 AR 036208A1 AR P020102942 A ARP020102942 A AR P020102942A AR P020102942 A ARP020102942 A AR P020102942A AR 036208 A1 AR036208 A1 AR 036208A1
Authority
AR
Argentina
Prior art keywords
preparation
compound
flibanserin
flibanserine
same
Prior art date
Application number
ARP020102942A
Other languages
English (en)
Inventor
Dubini Enrica Dr
Ezhaya Antoine Dr
Bombarda Carlo Dr
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 AR036208A1 publication Critical patent/AR036208A1/es

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)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (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

Se describe un compuesto polimorfo cristalino (forma A) de flibanserina (1-[2-(4-(3-trifluorometil-fenil)piperazin-1-il)etil]-2,3-dihidro-1H-benzoimidazol-2-ona] fórmula (1) que tiene un máximo endotérmico a 161°C que se produce durante el análisis térmico usando DSC. También se describe un procedimiento industrial para la preparación de dicho compuesto polimorfo A de flibanserina, las composiciones farmacéuticas que lo comprenden y el uso del mismo para la preparación de medicamentos destinados a tratar enfermedades en las que el uso de cantidades terapéuticas eficaces de compuestos que presentan afinidad por los receptores 5-HT1A y 5-HT2, presenta un beneficio terapéutico. Entre estas enfermedades se encuentra la depresión, la esquizofrenia, la enfermedad de Parkinson, la ansiedad, las alteraciones del sueno, los trastornos sexuales y mentales y el deterioro de la memoria asociado con la edad. Esta forma cristalina polimorfa del compuesto flibanserina supera a otras formas menos estables del mismo medicamento en su estabilidad física y química, pureza y distribución uniforme en la formulación.
ARP020102942A 2001-08-02 2002-08-02 Compuesto polimorfo estable de flibanserina, procedimiento industrial para su preparacion, y uso del mismo para preparar medicamentos AR036208A1 (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
AR036208A1 true AR036208A1 (es) 2004-08-18

Family

ID=26076670

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP020102942A AR036208A1 (es) 2001-08-02 2002-08-02 Compuesto polimorfo estable de flibanserina, procedimiento industrial para su preparacion, y uso del mismo para preparar medicamentos
ARP100102577A AR077416A2 (es) 2001-08-02 2010-07-15 Compuesto polimorfo estable de flibanserina , procedimiento industrial para su preparacion y uso del mismo para preparar medicamentos

Family Applications After (1)

Application Number Title Priority Date Filing Date
ARP100102577A AR077416A2 (es) 2001-08-02 2010-07-15 Compuesto polimorfo estable de flibanserina , procedimiento industrial para su preparacion y uso del mismo para preparar medicamentos

Country Status (26)

Country Link
EP (2) EP1518858A1 (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
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
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
JP2009513604A (ja) 2005-10-29 2009-04-02 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 月経前障害及び他の女性の性的障害治療用のベンゾイミダゾロン誘導体
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
KR20090005371A (ko) * 2006-05-09 2009-01-13 베링거 인겔하임 인터내셔날 게엠베하 폐경후 성욕 장애의 치료를 위한 플리반세린의 용도
WO2008000760A1 (en) 2006-06-30 2008-01-03 Boehringer Ingelheim International Gmbh Flibanserin for the treatment of urinary incontinence and related diseases
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
MX2009001551A (es) 2006-08-14 2009-02-20 Boehringer Ingelheim Int Formulaciones de flibanserina y metodo para fabricarlas.
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
JP2010513390A (ja) 2006-12-20 2010-04-30 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 混合セロトニン受容体親和性を有する硫酸化ベンズイミダゾロン誘導体
EP1955699A1 (en) * 2007-02-08 2008-08-13 Boehringer Ingelheim Pharma GmbH & Co. KG Use of flibanserin for the treatment of insomnia
UY31335A1 (es) 2007-09-12 2009-04-30 Tratamiento de sintomas vasomotores
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
CN113683570A (zh) * 2016-01-31 2021-11-23 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
DE60202958D1 (de) 2005-03-17
UA76767C2 (uk) 2006-09-15
WO2003014079A1 (en) 2003-02-20
HRP20040107B1 (hr) 2012-02-29
HU228666B1 (en) 2013-05-28
BR0211601A (pt) 2004-08-24
HUP0401201A3 (en) 2004-11-29
CO5560572A2 (es) 2005-09-30
EA200400252A1 (ru) 2004-08-26
HRP20040107A2 (en) 2004-06-30
ATE288911T1 (de) 2005-02-15
RS50742B (sr) 2010-08-31
JP3822601B2 (ja) 2006-09-20
KR100899297B1 (ko) 2009-05-26
EP1518858A1 (en) 2005-03-30
YU7804A (sh) 2006-08-17
ES2237694T3 (es) 2005-08-01
DE60202958T2 (de) 2006-04-06
HUP0401201A2 (hu) 2004-10-28
CA2450093C (en) 2008-09-23
CN1288147C (zh) 2006-12-06
EP1414816B1 (en) 2005-02-09
CA2450093A1 (en) 2003-02-20
NZ530510A (en) 2004-07-30
IL159151A (en) 2009-09-22
SI1414816T1 (en) 2005-06-30
JP2004537597A (ja) 2004-12-16
MY127294A (en) 2006-11-30
WO2003014079A8 (en) 2003-11-20
PT1414816E (pt) 2005-04-29
PL364598A1 (en) 2004-12-13
CN1551879A (zh) 2004-12-01
AR077416A2 (es) 2011-08-24
EA006400B1 (ru) 2005-12-29
HK1070063A1 (en) 2005-06-10
PL210224B1 (pl) 2011-12-30
DK1414816T3 (da) 2005-04-11
AU2002331361B2 (en) 2008-06-05
IL159151A0 (en) 2004-06-01
KR20040023704A (ko) 2004-03-18
EP1414816A1 (en) 2004-05-06
MXPA04000913A (es) 2004-10-27

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