CN103649104A - 用于制备氟替卡松丙酸酯形式1的方法 - Google Patents

用于制备氟替卡松丙酸酯形式1的方法 Download PDF

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Publication number
CN103649104A
CN103649104A CN201280034030.3A CN201280034030A CN103649104A CN 103649104 A CN103649104 A CN 103649104A CN 201280034030 A CN201280034030 A CN 201280034030A CN 103649104 A CN103649104 A CN 103649104A
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CN
China
Prior art keywords
fluticasone propionate
solvent
solution
slurry
acetone
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.)
Pending
Application number
CN201280034030.3A
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English (en)
Chinese (zh)
Inventor
M.D.泰斯赫斯特
I.马奇亚诺
E.库古洛斯
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.)
Pfizer Ltd Great Britain
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Pfizer Ltd Great Britain
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Filing date
Publication date
Application filed by Pfizer Ltd Great Britain filed Critical Pfizer Ltd Great Britain
Priority to CN201610951505.5A priority Critical patent/CN106977575A/zh
Publication of CN103649104A publication Critical patent/CN103649104A/zh
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • YGENERAL 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
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10TTECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T428/00Stock material or miscellaneous articles
    • Y10T428/29Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
    • Y10T428/2982Particulate matter [e.g., sphere, flake, etc.]

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (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 Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201280034030.3A 2011-07-08 2012-07-06 用于制备氟替卡松丙酸酯形式1的方法 Pending CN103649104A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610951505.5A CN106977575A (zh) 2011-07-08 2012-07-06 用于制备氟替卡松丙酸酯形式1的方法

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161505612P 2011-07-08 2011-07-08
US61/505,612 2011-07-08
PCT/US2012/045660 WO2013009591A1 (en) 2011-07-08 2012-07-06 Process for the preparation of fluticasone propionate form 1

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201610951505.5A Division CN106977575A (zh) 2011-07-08 2012-07-06 用于制备氟替卡松丙酸酯形式1的方法

Publications (1)

Publication Number Publication Date
CN103649104A true CN103649104A (zh) 2014-03-19

Family

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Family Applications (2)

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CN201280034030.3A Pending CN103649104A (zh) 2011-07-08 2012-07-06 用于制备氟替卡松丙酸酯形式1的方法
CN201610951505.5A Pending CN106977575A (zh) 2011-07-08 2012-07-06 用于制备氟替卡松丙酸酯形式1的方法

Family Applications After (1)

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CN201610951505.5A Pending CN106977575A (zh) 2011-07-08 2012-07-06 用于制备氟替卡松丙酸酯形式1的方法

Country Status (10)

Country Link
US (2) US10370402B2 (cg-RX-API-DMAC7.html)
EP (1) EP2729480A4 (cg-RX-API-DMAC7.html)
JP (2) JP2014520848A (cg-RX-API-DMAC7.html)
KR (3) KR20140048237A (cg-RX-API-DMAC7.html)
CN (2) CN103649104A (cg-RX-API-DMAC7.html)
AU (1) AU2012282936B2 (cg-RX-API-DMAC7.html)
CA (1) CA2840401C (cg-RX-API-DMAC7.html)
MX (2) MX376564B (cg-RX-API-DMAC7.html)
WO (1) WO2013009591A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201309531B (cg-RX-API-DMAC7.html)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111662353A (zh) * 2019-03-05 2020-09-15 上海谷森医药有限公司 一种糠酸氟替卡松晶型1的制备方法

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX376564B (es) * 2011-07-08 2025-03-07 Pfizer Ltd Proceso para la preparación de la forma 1 del propionato de fluticasona.
ES2727474T3 (es) 2012-05-08 2019-10-16 Nicox Ophthalmics Inc Nanocristales de propionato de fluticasona
US9796750B2 (en) 2014-02-07 2017-10-24 Mylan Laboratories Ltd. Process for the purification of fluticasone propionate using a ketone solvent and water as anti-solvent
US20220168665A1 (en) * 2019-04-10 2022-06-02 Eupraxia Pharmaceuticals Inc. Process for making drug crystals of desired size distribution and morphology
CN110759960B (zh) * 2019-10-30 2021-03-23 山东赛托生物科技股份有限公司 一种丙酸氟替卡松的精制方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1409627A (zh) * 1999-11-03 2003-04-09 葛兰素集团有限公司 制备晶粒的新装置和方法
WO2004001369A2 (en) * 2002-06-20 2003-12-31 Sun Pharmaceutical Industries Limited Convenient synthesis of s-fluoromethyl 6alpha, 9alpha-difluoro-11beta-hydroxy-16alpha- methyl-17alpha-propionyloxy-3-oxoandrosta-1, 4-diene-17beta-carbothioate
CN100338087C (zh) * 2002-02-04 2007-09-19 葛兰素集团有限公司 制备氟替卡松丙酸酯,尤其是多晶型的晶形1的新方法

Family Cites Families (11)

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GB2088877B (en) 1980-02-15 1984-07-04 Glaxo Group Ltd Androstane 17 carbothioates
GB9001635D0 (en) * 1990-01-24 1990-03-21 Ganderton David Aerosol carriers
SE9501384D0 (sv) * 1995-04-13 1995-04-13 Astra Ab Process for the preparation of respirable particles
GB9622173D0 (en) * 1996-10-24 1996-12-18 Glaxo Group Ltd Particulate Products
GB9828721D0 (en) * 1998-12-24 1999-02-17 Glaxo Group Ltd Novel apparatus and process
GB0015981D0 (en) * 2000-06-29 2000-08-23 Glaxo Group Ltd Novel process for preparing crystalline particles
GB0125604D0 (en) * 2001-10-25 2001-12-19 Glaxo Group Ltd Novel process
GB0201400D0 (en) * 2002-01-22 2002-03-13 Glaxo Group Ltd Novel apparatus and process
GB0315509D0 (en) 2003-07-02 2003-08-06 Meridica Ltd Dispensing device
US7314516B2 (en) * 2004-12-29 2008-01-01 Five Star Technologies, Inc. Hydrodynamic cavitation crystallization device and process
MX376564B (es) * 2011-07-08 2025-03-07 Pfizer Ltd Proceso para la preparación de la forma 1 del propionato de fluticasona.

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1409627A (zh) * 1999-11-03 2003-04-09 葛兰素集团有限公司 制备晶粒的新装置和方法
CN100338087C (zh) * 2002-02-04 2007-09-19 葛兰素集团有限公司 制备氟替卡松丙酸酯,尤其是多晶型的晶形1的新方法
WO2004001369A2 (en) * 2002-06-20 2003-12-31 Sun Pharmaceutical Industries Limited Convenient synthesis of s-fluoromethyl 6alpha, 9alpha-difluoro-11beta-hydroxy-16alpha- methyl-17alpha-propionyloxy-3-oxoandrosta-1, 4-diene-17beta-carbothioate

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
HARTWIG STECKEL ET AL.: "In vitro characterization of jet-milled and in-situ-micronized fluticasone-17-propionate", 《INTERNATIONAL JOURNAL OF PHARMACEUTICS 》, vol. 258, 31 December 2003 (2003-12-31) *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111662353A (zh) * 2019-03-05 2020-09-15 上海谷森医药有限公司 一种糠酸氟替卡松晶型1的制备方法

Also Published As

Publication number Publication date
MX2014000192A (es) 2014-04-25
US20200024298A1 (en) 2020-01-23
AU2012282936B2 (en) 2016-11-10
MX2020011330A (es) 2020-11-24
ZA201309531B (en) 2014-08-27
CA2840401C (en) 2016-05-17
JP2017031161A (ja) 2017-02-09
KR20140048237A (ko) 2014-04-23
CA2840401A1 (en) 2013-01-17
WO2013009591A1 (en) 2013-01-17
MX376564B (es) 2025-03-07
KR102163368B1 (ko) 2020-10-08
US20140141247A1 (en) 2014-05-22
CN106977575A (zh) 2017-07-25
US10370402B2 (en) 2019-08-06
KR20200117056A (ko) 2020-10-13
EP2729480A1 (en) 2014-05-14
AU2012282936A1 (en) 2014-01-16
KR20190107165A (ko) 2019-09-18
JP2014520848A (ja) 2014-08-25
EP2729480A4 (en) 2014-12-31

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Application publication date: 20140319