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WO2017076356A1 - Nouvelle forme cristalline de la flibansérine et son procédé de préparation - Google Patents

Nouvelle forme cristalline de la flibansérine et son procédé de préparation Download PDF

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Publication number
WO2017076356A1
WO2017076356A1 PCT/CN2016/104735 CN2016104735W WO2017076356A1 WO 2017076356 A1 WO2017076356 A1 WO 2017076356A1 CN 2016104735 W CN2016104735 W CN 2016104735W WO 2017076356 A1 WO2017076356 A1 WO 2017076356A1
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WO
WIPO (PCT)
Prior art keywords
crystal form
ray powder
powder diffraction
diffraction pattern
crystal
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.)
Ceased
Application number
PCT/CN2016/104735
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English (en)
Chinese (zh)
Inventor
陈敏华
张炎锋
邹坡
张晓宇
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.)
Crystal Pharmatech Co Ltd
Original Assignee
Crystal Pharmatech Co Ltd
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 Crystal Pharmatech Co Ltd filed Critical Crystal Pharmatech Co Ltd
Publication of WO2017076356A1 publication Critical patent/WO2017076356A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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

Definitions

  • the patent CN1288147C discloses two crystal forms of Fluboxerin, Form A and Form B.
  • Form B exhibits lower stability under the influence of mechanical stress caused by grinding, and only Form A is a crystal form that meets the requirements for polishing stability. Therefore, it is necessary to develop a new crystalline form of flurbinerine suitable for storage and industrial production, providing more and better choices for the subsequent development of drugs.
  • the inventors of the present invention found that there are two other crystal forms which have better properties, and the two crystal forms have higher stability, higher solubility than the existing crystal forms, and higher bioavailability.
  • the invented crystal form has an unexpected technical effect and is of great significance for future drug development.
  • the crystalline form I provided by the present invention has a weight loss gradient of about 3.2% when heated to 98 ° C, and the thermogravimetric analysis chart is shown in FIG.
  • the X-ray powder diffraction pattern of Form II also has a diffraction peak at a 2theta value of 15.3 ° ⁇ 0.2 °, 20.0 ° ⁇ 0.2 °, 23.0 ° ⁇ 0.2 °.
  • Form II its X-ray powder diffraction pattern (CuK ⁇ radiation) at 25 ° C has a characteristic peak at a value of 16.2 ° ⁇ 0.2 °, 8.8 ° ⁇ 0.2 °, 12.8 ° ⁇ 0.2 ° at 17.4 °.
  • ⁇ 0.2°, 19.0° ⁇ 0.2°, 9.6° ⁇ 0.2°, 15.3° ⁇ 0.2°, 20.0° ⁇ 0.2°, and 23.0° ⁇ 0.2° have diffraction peaks.
  • D90 indicates the particle size distribution (volume distribution) accounts for 90% of the particle size

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne une nouvelle forme cristalline de la flibansérine et son procédé de préparation. La nouvelle forme cristalline de la flibansérine de la présente invention consiste en une forme cristalline I et une forme cristalline II. Par rapport à une forme cristalline existante, la nouvelle forme cristalline présente une stabilité, une solubilité et une biodisponibilité élevées. La forme cristalline I, la forme cristalline II, ou un mélange de la forme cristalline I et de la forme cristalline II de la présente invention peuvent être utilisés pour l'élaboration de préparations pharmaceutiques destinées au traitement de la dépression, de la schizophrénie, de troubles de l'anxiété, de troubles du sommeil, ds troubles mentaux et sexuels et de troubles de la mémoire liés à l'âge; en particulier, elles peuvent être utilisées pour l'élaboration de préparations pharmaceutiques destinées au traitement d'une baisse du désir sexuel (HSDD).
PCT/CN2016/104735 2015-11-05 2016-11-04 Nouvelle forme cristalline de la flibansérine et son procédé de préparation Ceased WO2017076356A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201510751851 2015-11-05
CN201510751851.4 2015-11-05

Publications (1)

Publication Number Publication Date
WO2017076356A1 true WO2017076356A1 (fr) 2017-05-11

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ID=58661833

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2016/104735 Ceased WO2017076356A1 (fr) 2015-11-05 2016-11-04 Nouvelle forme cristalline de la flibansérine et son procédé de préparation

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WO (1) WO2017076356A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11492343B2 (en) * 2016-01-31 2022-11-08 Xiaoming Meng Polymorph of flibanserin and preparation method thereof and use of same

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0526434A1 (fr) * 1991-07-30 1993-02-03 BOEHRINGER INGELHEIM ITALIA S.p.A. Dérivés de benzimidazolone comme antagonistes de 5-HT1A et 5-HT2
CN1551879A (zh) * 2001-08-02 2004-12-01 ���������ﻯѧ���޹�˾ 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
WO2010079045A2 (fr) * 2008-12-15 2010-07-15 Boehringer Ingelheim International Gmbh Nouveaux sels
WO2010146595A2 (fr) * 2009-06-16 2010-12-23 Symed Labs Limited Nouveaux polymorphes d'hydrochlorure de flibansérine

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0526434A1 (fr) * 1991-07-30 1993-02-03 BOEHRINGER INGELHEIM ITALIA S.p.A. Dérivés de benzimidazolone comme antagonistes de 5-HT1A et 5-HT2
CN1551879A (zh) * 2001-08-02 2004-12-01 ���������ﻯѧ���޹�˾ 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
WO2010079045A2 (fr) * 2008-12-15 2010-07-15 Boehringer Ingelheim International Gmbh Nouveaux sels
WO2010146595A2 (fr) * 2009-06-16 2010-12-23 Symed Labs Limited Nouveaux polymorphes d'hydrochlorure de flibansérine

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11492343B2 (en) * 2016-01-31 2022-11-08 Xiaoming Meng Polymorph of flibanserin and preparation method thereof and use of same

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