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

Info

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
Authority
CN
China
Prior art keywords
polycrystalline
water
sodium
potassium
lithium
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CNB028152263A
Other languages
English (en)
Chinese (zh)
Other versions
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sprout Pharmaceutical Ltd By Share Ltd
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 CN1551879A publication Critical patent/CN1551879A/zh
Application granted granted Critical
Publication of CN1288147C publication Critical patent/CN1288147C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (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 (https=)
JP (1) JP3822601B2 (https=)
KR (1) KR100899297B1 (https=)
CN (1) CN1288147C (https=)
AR (2) AR036208A1 (https=)
AT (1) ATE288911T1 (https=)
AU (1) AU2002331361B2 (https=)
BR (1) BR0211601A (https=)
CA (1) CA2450093C (https=)
CO (1) CO5560572A2 (https=)
DE (1) DE60202958T2 (https=)
DK (1) DK1414816T3 (https=)
EA (1) EA006400B1 (https=)
ES (1) ES2237694T3 (https=)
HR (1) HRP20040107B1 (https=)
HU (1) HU228666B1 (https=)
IL (2) IL159151A0 (https=)
MX (1) MXPA04000913A (https=)
MY (1) MY127294A (https=)
NZ (1) NZ530510A (https=)
PL (1) PL210224B1 (https=)
PT (1) PT1414816E (https=)
RS (1) RS50742B (https=)
SI (1) SI1414816T1 (https=)
UA (1) UA76767C2 (https=)
WO (1) WO2003014079A1 (https=)

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
ES2361994T3 (es) * 2002-05-22 2011-06-27 BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG Nuevas composiciones farmacéuticas que contienen polimorfo a de flibanserina.
EP1904182A2 (en) * 2005-05-06 2008-04-02 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
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
CA2642368A1 (en) * 2006-02-28 2007-09-07 Boehringer Ingelheim International Gmbh Treatment of prevention of valvular heart disease with flibanserin
BRPI0712039A2 (pt) * 2006-05-09 2011-12-20 Boehringer Ingelheim Int 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
EP2054041A2 (en) 2006-08-14 2009-05-06 Boehringer Ingelheim International GmbH Formulations of flibanserin and method for manufacturing the same
IL197129A (en) 2006-08-25 2014-08-31 Boehringer Ingelheim Int Controlled release system and method for production
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
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
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
UA76767C2 (uk) 2006-09-15
HU228666B1 (en) 2013-05-28
IL159151A0 (en) 2004-06-01
ES2237694T3 (es) 2005-08-01
EA200400252A1 (ru) 2004-08-26
MXPA04000913A (es) 2004-10-27
IL159151A (en) 2009-09-22
JP3822601B2 (ja) 2006-09-20
CA2450093A1 (en) 2003-02-20
CO5560572A2 (es) 2005-09-30
WO2003014079A1 (en) 2003-02-20
DE60202958T2 (de) 2006-04-06
EP1414816A1 (en) 2004-05-06
MY127294A (en) 2006-11-30
CN1551879A (zh) 2004-12-01
KR100899297B1 (ko) 2009-05-26
EP1414816B1 (en) 2005-02-09
YU7804A (sh) 2006-08-17
RS50742B (sr) 2010-08-31
EP1518858A1 (en) 2005-03-30
KR20040023704A (ko) 2004-03-18
HUP0401201A2 (hu) 2004-10-28
JP2004537597A (ja) 2004-12-16
PT1414816E (pt) 2005-04-29
PL364598A1 (en) 2004-12-13
NZ530510A (en) 2004-07-30
SI1414816T1 (en) 2005-06-30
DK1414816T3 (da) 2005-04-11
HUP0401201A3 (en) 2004-11-29
AR077416A2 (es) 2011-08-24
ATE288911T1 (de) 2005-02-15
CA2450093C (en) 2008-09-23
WO2003014079A8 (en) 2003-11-20
AR036208A1 (es) 2004-08-18
EA006400B1 (ru) 2005-12-29
HK1070063A1 (en) 2005-06-10
DE60202958D1 (de) 2005-03-17
AU2002331361B2 (en) 2008-06-05
PL210224B1 (pl) 2011-12-30
BR0211601A (pt) 2004-08-24
HRP20040107B1 (hr) 2012-02-29
HRP20040107A2 (en) 2004-06-30

Similar Documents

Publication Publication Date Title
CN1288147C (zh) 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
US7420057B2 (en) Stable polymorph of flibanserin
EP1319003B1 (en) Xanthine phosphodiesterase v inhibitors
AU2002331361A1 (en) Stable polymorph of flibanserin, technical process for its preparation and the use thereof for preparing medicaments
KR20140054068A (ko) 테노포비어 알라펜아미드 헤미푸마레이트
JP2002504549A (ja) ベンジルピペラジニル−およびベンジルピペリジニルエタノン誘導体、その調製、およびドーパミンｄ４受容体アンタゴニストとしてのその使用
CZ183699A3 (cs) 2-Imidazolinylaminobenzoxazolové sloučeniny užitečné jako alfa-2 adrenoceptorové agonisty
JPH0825997B2 (ja) ３−アミノプロピルオキシフェニル誘導体、その製法およびそれらを含有する医薬組成物
CN1125065C (zh) 苯并[g]喹啉衍生物
HK1070063B (en) Stable polymorph of flibanserin, technical process for its preparation and the use thereof for preparing medicaments
CN1944448A (zh) 葛根素衍生物及其药物用途
HK1040399A1 (zh) N-取代的氮雜二環庚烷衍生物及其製備方法和用途
ZA200309586B (en) Stable polymorph of flibanserin technical process for its preparation and the use thereof for preparing medicaments
CN1384817A (zh) 多晶型的n－[3－[[2－(3,4－二甲氧基苯基)乙基]氨基]丙基]－4－硝基苯甲酰胺盐酸化物
BR122012029907B1 (pt) A crystal polymorphine (form a) of flibanserin 1, its use, process for the preparation of flibanserin 1, and pharmaceutical compositions
NO326098B1 (no) Stabil polymorf av flibanserin, teknisk fremgangsmate for fremstilling derav og anvendelse derav for fremstlling av medikamenter
HK1036980A (en) 4-hydroxy-4-phenylpiperidine derivatives and pharmaceuticals containing the same

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1070063

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
ASS Succession or assignment of patent right

Owner name: SPROUT PHARMACEUTICALS, INC.

Free format text: FORMER OWNER: BIDACHEM SPA

Effective date: 20120425

C41 Transfer of patent application or patent right or utility model
TR01 Transfer of patent right

Effective date of registration: 20120425

Address after: North Carolina

Patentee after: Sprout pharmaceutical Limited by Share Ltd

Address before: Italy Bergamo

Patentee before: Bidachem SPA

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20061206

Termination date: 20200730

CF01 Termination of patent right due to non-payment of annual fee