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HRP20040107B1 - Stabilni polimorf flibanserina, tehnički postupak njegova pripravljanja, te njegova primjena u proizvodnji lijekova - Google Patents

Stabilni polimorf flibanserina, tehnički postupak njegova pripravljanja, te njegova primjena u proizvodnji lijekova

Info

Publication number
HRP20040107B1
HRP20040107B1 HR20040107A HRP20040107A HRP20040107B1 HR P20040107 B1 HRP20040107 B1 HR P20040107B1 HR 20040107 A HR20040107 A HR 20040107A HR P20040107 A HRP20040107 A HR P20040107A HR P20040107 B1 HRP20040107 B1 HR P20040107B1
Authority
HR
Croatia
Prior art keywords
polymorph
flibanserine
medicines
stable
preparation
Prior art date
Application number
HR20040107A
Other languages
English (en)
Inventor
Bombarda Carlo
Dubini Enrica
Ezhaya Antoine
Schneider Heinrich
Original Assignee
Bidachem S.P.A.
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 S.P.A. filed Critical Bidachem S.P.A.
Publication of HRP20040107A2 publication Critical patent/HRP20040107A2/hr
Publication of HRP20040107B1 publication Critical patent/HRP20040107B1/hr

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

Abstract

Kristalni polimorf A (oblik A) flibanserina 1naznačen time, da ima endotermni maksimuma od 161°C utvrđen termalnom analizom putem DSC. Patent sadrži još 9 patentnih zahtjeva.
HR20040107A 2001-08-02 2002-07-30 Stabilni polimorf flibanserina, tehnički postupak njegova pripravljanja, te njegova primjena u proizvodnji lijekova HRP20040107B1 (hr)

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 (2)

Publication Number Publication Date
HRP20040107A2 HRP20040107A2 (en) 2004-06-30
HRP20040107B1 true HRP20040107B1 (hr) 2012-02-29

Family

ID=26076670

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20040107A HRP20040107B1 (hr) 2001-08-02 2002-07-30 Stabilni polimorf flibanserina, tehnički postupak njegova pripravljanja, te njegova primjena u proizvodnji lijekova

Country Status (26)

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

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
BRPI0311189B8 (pt) * 2002-05-22 2021-05-25 Boehringer Ingelheim Pharma composições farmacêuticas contendo polimorfo a de flibanserin, bem como seu uso
CA2608249A1 (en) * 2005-05-06 2006-11-16 Boehringer Ingelheim International Gmbh Method for the treatment of drug abuse with flibanserin
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
WO2007048803A1 (en) 2005-10-29 2007-05-03 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
PE20080090A1 (es) * 2006-05-09 2008-03-14 Boehringer Ingelheim Int Flibanserina para el tratamiento de trastornos post-menopausicos del deseo sexual
EP2037927B1 (en) 2006-06-30 2010-01-27 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
CA2660476C (en) 2006-08-14 2015-11-17 Boehringer Ingelheim International Gmbh Formulations of flibanserin and method for manufacturing the same
CN101505736A (zh) 2006-08-25 2009-08-12 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
EP2097389B1 (en) 2006-12-20 2011-09-14 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
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

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
EA006400B1 (ru) 2005-12-29
DE60202958D1 (de) 2005-03-17
KR20040023704A (ko) 2004-03-18
HUP0401201A2 (hu) 2004-10-28
WO2003014079A8 (en) 2003-11-20
DE60202958T2 (de) 2006-04-06
EA200400252A1 (ru) 2004-08-26
PL364598A1 (en) 2004-12-13
NZ530510A (en) 2004-07-30
HUP0401201A3 (en) 2004-11-29
RS50742B (sr) 2010-08-31
HU228666B1 (en) 2013-05-28
PL210224B1 (pl) 2011-12-30
SI1414816T1 (en) 2005-06-30
CN1551879A (zh) 2004-12-01
HRP20040107A2 (en) 2004-06-30
IL159151A0 (en) 2004-06-01
ES2237694T3 (es) 2005-08-01
DK1414816T3 (da) 2005-04-11
IL159151A (en) 2009-09-22
AU2002331361B2 (en) 2008-06-05
BR0211601A (pt) 2004-08-24
YU7804A (sh) 2006-08-17
PT1414816E (pt) 2005-04-29
EP1414816B1 (en) 2005-02-09
CN1288147C (zh) 2006-12-06
JP2004537597A (ja) 2004-12-16
ATE288911T1 (de) 2005-02-15
CA2450093A1 (en) 2003-02-20
KR100899297B1 (ko) 2009-05-26
CA2450093C (en) 2008-09-23
EP1518858A1 (en) 2005-03-30
MXPA04000913A (es) 2004-10-27
JP3822601B2 (ja) 2006-09-20
UA76767C2 (uk) 2006-09-15
HK1070063A1 (en) 2005-06-10
WO2003014079A1 (en) 2003-02-20
EP1414816A1 (en) 2004-05-06
CO5560572A2 (es) 2005-09-30
MY127294A (en) 2006-11-30
AR077416A2 (es) 2011-08-24
AR036208A1 (es) 2004-08-18

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