CN1288147C - 氟立班丝氨(flibanserin)的稳定多晶体,其制备的技术法及其在药物制备的用途 - Google Patents

氟立班丝氨(flibanserin)的稳定多晶体,其制备的技术法及其在药物制备的用途 Download PDF

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Publication number
CN1288147C
CN1288147C CNB028152263A CN02815226A CN1288147C CN 1288147 C CN1288147 C CN 1288147C CN B028152263 A CNB028152263 A CN B028152263A CN 02815226 A CN02815226 A CN 02815226A CN 1288147 C CN1288147 C CN 1288147C
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China
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polycrystalline
water
sodium
potassium
lithium
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Expired - Fee Related
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CNB028152263A
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English (en)
Chinese (zh)
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CN1551879A (zh
Inventor
卡洛·博姆巴达
恩里卡·杜比尼
安托万·伊扎亚
海因里希·施奈德
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Sprout Pharmaceutical Ltd By Share Ltd
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Bidachem SpA
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    • 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

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  • 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)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Psychology (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)
CNB028152263A 2001-08-02 2002-07-30 氟立班丝氨(flibanserin)的稳定多晶体,其制备的技术法及其在药物制备的用途 Expired - Fee Related CN1288147C (zh)

Applications Claiming Priority (4)

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

Publications (2)

Publication Number Publication Date
CN1551879A CN1551879A (zh) 2004-12-01
CN1288147C true CN1288147C (zh) 2006-12-06

Family

ID=26076670

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB028152263A Expired - Fee Related CN1288147C (zh) 2001-08-02 2002-07-30 氟立班丝氨(flibanserin)的稳定多晶体,其制备的技术法及其在药物制备的用途

Country Status (26)

Country Link
EP (2) EP1414816B1 (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
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
NZ537253A (en) * 2002-05-22 2007-09-28 Boehringer Ingelheim Pharma Coated pharmaceutical compositions containing flibanserin polymorph A
CA2608249A1 (en) * 2005-05-06 2006-11-16 Boehringer Ingelheim International Gmbh Method for the treatment of drug abuse with flibanserin
ES2646326T3 (es) 2005-08-03 2017-12-13 Sprout Pharmaceuticals, Inc. Uso de flibanserina en el tratamiento de la obesidad
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
US20090247546A1 (en) * 2006-02-28 2009-10-01 Boehringer Ingelheim International Gmbh Treatment of Prevention of Valvular Heart Disease with Flibanserin
JP2009536176A (ja) * 2006-05-09 2009-10-08 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 閉経後の性的欲求障害の治療のためのフリバンセリンの使用
EP2037927B1 (en) 2006-06-30 2010-01-27 Boehringer Ingelheim International GmbH Flibanserin for the treatment of urinary incontinence and related diseases
WO2008019996A2 (en) 2006-08-14 2008-02-21 Boehringer Ingelheim International Gmbh Formulations of flibanserin and method for manufacturing the same
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
JP5220746B2 (ja) 2006-08-25 2013-06-26 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 制御放出システム及びその製造方法
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
PE20091188A1 (es) 2007-09-12 2009-08-31 Boehringer Ingelheim Int Compuesto 1-[2-(4-(3-trifluorometil-fenil)piperazin-1-il)etil]-2,3-dihidro-1h-benzimidazol-2-ona (flibanserina), sus sales de adicion y composiciones farmaceuticas que los contienen
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
CN108699007A (zh) * 2016-01-31 2018-10-23 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
CN1551879A (zh) 2004-12-01
PT1414816E (pt) 2005-04-29
IL159151A0 (en) 2004-06-01
DE60202958T2 (de) 2006-04-06
PL364598A1 (en) 2004-12-13
SI1414816T1 (en) 2005-06-30
KR20040023704A (ko) 2004-03-18
EA006400B1 (ru) 2005-12-29
DE60202958D1 (de) 2005-03-17
EP1518858A1 (en) 2005-03-30
CO5560572A2 (es) 2005-09-30
HRP20040107B1 (hr) 2012-02-29
MXPA04000913A (es) 2004-10-27
IL159151A (en) 2009-09-22
HRP20040107A2 (en) 2004-06-30
ES2237694T3 (es) 2005-08-01
JP2004537597A (ja) 2004-12-16
DK1414816T3 (da) 2005-04-11
WO2003014079A8 (en) 2003-11-20
CA2450093A1 (en) 2003-02-20
AU2002331361B2 (en) 2008-06-05
BR0211601A (pt) 2004-08-24
EA200400252A1 (ru) 2004-08-26
ATE288911T1 (de) 2005-02-15
KR100899297B1 (ko) 2009-05-26
YU7804A (sh) 2006-08-17
UA76767C2 (uk) 2006-09-15
RS50742B (sr) 2010-08-31
EP1414816A1 (en) 2004-05-06
MY127294A (en) 2006-11-30
NZ530510A (en) 2004-07-30
AR077416A2 (es) 2011-08-24
EP1414816B1 (en) 2005-02-09
JP3822601B2 (ja) 2006-09-20
AR036208A1 (es) 2004-08-18
HU228666B1 (en) 2013-05-28
HUP0401201A2 (hu) 2004-10-28
HK1070063A1 (en) 2005-06-10
PL210224B1 (pl) 2011-12-30
WO2003014079A1 (en) 2003-02-20
CA2450093C (en) 2008-09-23
HUP0401201A3 (en) 2004-11-29

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