ATE469908T1 - Verfahren zur herstellung von pimecrolimus - Google Patents

Verfahren zur herstellung von pimecrolimus

Info

Publication number: ATE469908T1
Authority: AT; Austria
Prior art keywords: pimecrolimus; producing; macrolides; tacrolimus; crystallization
Prior art date: 2004-12-01

Application number

AT05848723T

Other languages

English (en)

Inventor

Viktor Gyollai

Csaba Szabo

Original Assignee

Teva Gyogyszergyar Zartkoeruen

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.)

2004-12-01

Filing date

2005-12-01

Publication date

2010-06-15

2005-12-01 Application filed by Teva Gyogyszergyar Zartkoeruen filed Critical Teva Gyogyszergyar Zartkoeruen

2010-06-15 Application granted granted Critical

2010-06-15 Publication of ATE469908T1 publication Critical patent/ATE469908T1/de

Links

KASDHRXLYQOAKZ-ZPSXYTITSA-N pimecrolimus Chemical compound C/C([C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@H](C(C[C@H](O)[C@H]1C)=O)CC)=C\[C@@H]1CC[C@@H](Cl)[C@H](OC)C1 KASDHRXLYQOAKZ-ZPSXYTITSA-N 0.000 title abstract 2
229960005330 pimecrolimus Drugs 0.000 title abstract 2
238000004519 manufacturing process Methods 0.000 title 1
QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 abstract 1
238000002425 crystallisation Methods 0.000 abstract 1
230000008025 crystallization Effects 0.000 abstract 1
239000003120 macrolide antibiotic agent Substances 0.000 abstract 1
229940041033 macrolides Drugs 0.000 abstract 1
238000000034 method Methods 0.000 abstract 1
229960001967 tacrolimus Drugs 0.000 abstract 1
QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1688—Processes resulting in pure drug agglomerate optionally containing up to 5% of excipient
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/14—Ortho-condensed systems
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/01—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing oxygen

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Immunology (AREA)
Epidemiology (AREA)
Communicable Diseases (AREA)
Biochemistry (AREA)
Oncology (AREA)
Molecular Biology (AREA)
Genetics & Genomics (AREA)
Biotechnology (AREA)
Dermatology (AREA)
Transplantation (AREA)
Pulmonology (AREA)
Rheumatology (AREA)
Pain & Pain Management (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Saccharide Compounds (AREA)
Solid-Sorbent Or Filter-Aiding Compositions (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Preparation Of Compounds By Using Micro-Organisms (AREA)

AT05848723T 2004-12-01 2005-12-01 Verfahren zur herstellung von pimecrolimus ATE469908T1 (de)

Applications Claiming Priority (9)

Application Number	Priority Date	Filing Date	Title
US63237204P	2004-12-01	2004-12-01
US63392604P	2004-12-06	2004-12-06
US64186905P	2005-01-05	2005-01-05
US64186805P	2005-01-05	2005-01-05
US64169705P	2005-01-05	2005-01-05
US66244005P	2005-03-16	2005-03-16
US70568105P	2005-08-03	2005-08-03
US70916005P	2005-08-17	2005-08-17
PCT/US2005/043541 WO2006060614A1 (en)	2004-12-01	2005-12-01	Methods for preparing pimecrolimus

Publications (1)

Publication Number	Publication Date
ATE469908T1 true ATE469908T1 (de)	2010-06-15

Family

ID=36097009

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AT05848723T ATE469908T1 (de)	2004-12-01	2005-12-01	Verfahren zur herstellung von pimecrolimus

Country Status (11)

Country	Link
US (5)	US7645876B2 (de)
EP (4)	EP1817314A1 (de)
JP (4)	JP2007519758A (de)
KR (1)	KR20070060144A (de)
AT (1)	ATE469908T1 (de)
CA (4)	CA2584358A1 (de)
DE (1)	DE602005021684D1 (de)
IL (4)	IL182871A0 (de)
MX (2)	MX2007005222A (de)
TW (3)	TWI315310B (de)
WO (4)	WO2006060615A1 (de)

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US7820812B2 (en)	2006-07-25	2010-10-26	Abbott Laboratories	Methods of manufacturing crystalline forms of rapamycin analogs
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CN102282457A (zh) *	2009-01-21	2011-12-14	拜康有限公司	确定西罗莫司稳定性的方法和制备其稳定形式的工艺
IT1394309B1 (it)	2009-05-22	2012-06-06	Poli Ind Chimica Spa	Nuovo approccio chimico-enzimatico alla sintesi del pimecrolimus
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JP5440692B2 (ja) *	2010-03-29	2014-03-12	ダイキン工業株式会社	３−クロロ−ペンタフルオロプロペンの製造方法
WO2012011877A2 (en)	2010-07-23	2012-01-26	Curiox Biosystems Pte Ltd	Apparatus and method for multiple reactions in small volumes
WO2012017449A1 (en)	2010-08-04	2012-02-09	Meril Life Sciences Pvt. Ltd	Process for preparation of novel 42-0-(heteroalkoxyalkyl) rapamycin compounds with anti-proliferative properties"
EP2611476B1 (de)	2010-09-02	2016-08-10	Boston Scientific Scimed, Inc.	Beschichtungsverfahren für wirkstofffreisetzungsballons mit wärmeinduziertem rewrap-gedächtnis
US9327264B2 (en) *	2011-01-31	2016-05-03	Uchicago Argonne, Llc	Containerless synthesis of amorphous and nanophase organic materials
WO2013022458A1 (en)	2011-08-05	2013-02-14	Boston Scientific Scimed, Inc.	Methods of converting amorphous drug substance into crystalline form
US9056152B2 (en)	2011-08-25	2015-06-16	Boston Scientific Scimed, Inc.	Medical device with crystalline drug coating
WO2014145780A1 (en)	2013-03-15	2014-09-18	Biosensors International Group, Ltd.	Purification of rapamycin derivatives
EP3578546A1 (de)	2013-11-15	2019-12-11	Akebia Therapeutics Inc.	Feste formen von {[5-(3-chlorophenyl)-3-hydroxypyridin-2-carbonyl]amino}essigsäure, zusammensetzungen und verwendungen davon
US20170072058A1 (en)	2014-11-21	2017-03-16	Solipharma Llc	Pharmaceutical composition containing tacrolimus and preparation methods thereof
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EP3178824A1 (de)	2015-12-08	2017-06-14	Medichem, S.A.	Verfahren zur herstellung von pimecrolimus
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CN108948046B (zh) *	2017-05-20	2020-11-10	鲁南制药集团股份有限公司	一种替西罗莫司的中间体及其制备方法
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US7589128B2 (en)	2004-06-01	2009-09-15	Teva Gyógyszergyár Zártkörüen Müködö Részvénytársaság	Process for preparation of amorphous form of a drug
US20080312447A1 (en) *	2004-09-10	2008-12-18	Ivax Pharmaceuticals S.R.O.	Process for Isolation of Crystalline Tacrolimus
WO2006031661A2 (en) *	2004-09-10	2006-03-23	Ivax Pharmaceuticals S.R.O.	Process for isolation of macrolide compounds
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CA2584358A1 (en) *	2004-12-01	2006-06-08	Teva Gyogyszergyar Zartkoeruen Mukoedo Reszvenytarsasag	Non-hygroscopic and powdery amorphous pimecrolimus

2005
- 2005-12-01 CA CA002584358A patent/CA2584358A1/en not_active Abandoned
- 2005-12-01 DE DE602005021684T patent/DE602005021684D1/de not_active Expired - Lifetime
- 2005-12-01 CA CA002584365A patent/CA2584365A1/en not_active Abandoned
- 2005-12-01 WO PCT/US2005/043542 patent/WO2006060615A1/en not_active Ceased
- 2005-12-01 WO PCT/US2005/043543 patent/WO2006060616A1/en not_active Ceased
- 2005-12-01 EP EP05826343A patent/EP1817314A1/de not_active Withdrawn
- 2005-12-01 EP EP05848723A patent/EP1817317B1/de not_active Expired - Lifetime
- 2005-12-01 TW TW094142290A patent/TWI315310B/zh not_active IP Right Cessation
- 2005-12-01 WO PCT/US2005/043544 patent/WO2006060617A1/en not_active Ceased
- 2005-12-01 EP EP05848588A patent/EP1817316A1/de not_active Withdrawn
- 2005-12-01 WO PCT/US2005/043541 patent/WO2006060614A1/en not_active Ceased
- 2005-12-01 CA CA002584430A patent/CA2584430A1/en not_active Abandoned
- 2005-12-01 JP JP2006551654A patent/JP2007519758A/ja active Pending
- 2005-12-01 JP JP2006551652A patent/JP2007519757A/ja active Pending
- 2005-12-01 US US11/293,747 patent/US7645876B2/en not_active Expired - Fee Related
- 2005-12-01 US US11/293,286 patent/US7439252B2/en not_active Expired - Fee Related
- 2005-12-01 US US11/293,283 patent/US7589100B2/en not_active Expired - Fee Related
- 2005-12-01 KR KR1020077010037A patent/KR20070060144A/ko not_active Ceased
- 2005-12-01 US US11/293,353 patent/US7279571B2/en not_active Expired - Fee Related
- 2005-12-01 TW TW094142326A patent/TW200628483A/zh unknown
- 2005-12-01 JP JP2006551655A patent/JP2007523896A/ja active Pending
- 2005-12-01 MX MX2007005222A patent/MX2007005222A/es unknown
- 2005-12-01 AT AT05848723T patent/ATE469908T1/de not_active IP Right Cessation
- 2005-12-01 JP JP2006551653A patent/JP2007523069A/ja active Pending
- 2005-12-01 CA CA002584360A patent/CA2584360A1/en not_active Abandoned
- 2005-12-01 TW TW094142291A patent/TW200631955A/zh unknown
- 2005-12-01 EP EP05848573A patent/EP1817315A1/de not_active Withdrawn
- 2005-12-01 MX MX2007005221A patent/MX2007005221A/es unknown
2007
- 2007-04-30 IL IL182871A patent/IL182871A0/en unknown
- 2007-04-30 IL IL182872A patent/IL182872A0/en unknown
- 2007-04-30 IL IL182869A patent/IL182869A0/en unknown
- 2007-04-30 IL IL182870A patent/IL182870A0/en unknown
- 2007-07-24 US US11/881,033 patent/US20070270451A1/en not_active Abandoned

Also Published As

Publication number	Publication date
WO2006060616A1 (en)	2006-06-08
WO2006060614A9 (en)	2006-08-31
IL182870A0 (en)	2007-08-19
US7279571B2 (en)	2007-10-09
EP1817316A1 (de)	2007-08-15
WO2006060615A1 (en)	2006-06-08
CA2584430A1 (en)	2006-06-08
US7645876B2 (en)	2010-01-12
DE602005021684D1 (de)	2010-07-15
CA2584358A1 (en)	2006-06-08
US20060155119A1 (en)	2006-07-13
US20060147540A1 (en)	2006-07-06
US20070270451A1 (en)	2007-11-22
TW200626604A (en)	2006-08-01
IL182872A0 (en)	2007-08-19
JP2007519758A (ja)	2007-07-19
CA2584365A1 (en)	2006-06-08
MX2007005221A (es)	2007-06-22
US7439252B2 (en)	2008-10-21
JP2007519757A (ja)	2007-07-19
TW200631955A (en)	2006-09-16
IL182869A0 (en)	2007-08-19
EP1817314A1 (de)	2007-08-15
US7589100B2 (en)	2009-09-15
EP1817317B1 (de)	2010-06-02
EP1817317A1 (de)	2007-08-15
CA2584360A1 (en)	2006-06-08
JP2007523896A (ja)	2007-08-23
JP2007523069A (ja)	2007-08-16
WO2006060617A1 (en)	2006-06-08
IL182871A0 (en)	2007-08-19
EP1817315A1 (de)	2007-08-15
TWI315310B (en)	2009-10-01
WO2006060614A1 (en)	2006-06-08
US20060142564A1 (en)	2006-06-29
US20060135548A1 (en)	2006-06-22
MX2007005222A (es)	2007-06-26
KR20070060144A (ko)	2007-06-12
TW200628483A (en)	2006-08-16

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Date	Code	Title	Description
2010-12-15	RER	Ceased as to paragraph 5 lit. 3 law introducing patent treaties

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