AU759219B2 - Stabilization of macrolides - Google Patents

Stabilization of macrolides Download PDF

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Publication number
AU759219B2
AU759219B2 AU16573/00A AU1657300A AU759219B2 AU 759219 B2 AU759219 B2 AU 759219B2 AU 16573/00 A AU16573/00 A AU 16573/00A AU 1657300 A AU1657300 A AU 1657300A AU 759219 B2 AU759219 B2 AU 759219B2
Authority
AU
Australia
Prior art keywords
rapamycin
antioxidant
mixture
process according
derivative
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
Application number
AU16573/00A
Other languages
English (en)
Other versions
AU1657300A (en
Inventor
Francois Navarro
Samuel Petit
Guy Stone
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.)
Novartis AG
Original Assignee
Novartis AG
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26314797&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU759219(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis AG filed Critical Novartis AG
Publication of AU1657300A publication Critical patent/AU1657300A/en
Priority to AU2003200370A priority Critical patent/AU2003200370B2/en
Application granted granted Critical
Publication of AU759219B2 publication Critical patent/AU759219B2/en
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P35/00—Antineoplastic 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
AU16573/00A 1998-12-07 1999-12-06 Stabilization of macrolides Expired AU759219B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003200370A AU2003200370B2 (en) 1998-12-07 2003-02-05 Stabilization of macrolides

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB9826882.4A GB9826882D0 (en) 1998-12-07 1998-12-07 Organic compounds
GB9826882 1998-12-07
GBGB9904934.8A GB9904934D0 (en) 1998-12-07 1999-03-04 Organic compounds
GB9904934 1999-03-04
PCT/EP1999/009521 WO2000033878A2 (en) 1998-12-07 1999-12-06 Stabilization of macrolides

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2003200370A Division AU2003200370B2 (en) 1998-12-07 2003-02-05 Stabilization of macrolides

Publications (2)

Publication Number Publication Date
AU1657300A AU1657300A (en) 2000-06-26
AU759219B2 true AU759219B2 (en) 2003-04-10

Family

ID=26314797

Family Applications (1)

Application Number Title Priority Date Filing Date
AU16573/00A Expired AU759219B2 (en) 1998-12-07 1999-12-06 Stabilization of macrolides

Country Status (38)

Country Link
US (5) US6605613B2 (enExample)
EP (4) EP2269651A3 (enExample)
JP (3) JP3805625B2 (enExample)
KR (2) KR20060096477A (enExample)
CN (2) CN1876657B (enExample)
AR (3) AR026102A1 (enExample)
AT (1) ATE365051T1 (enExample)
AU (1) AU759219B2 (enExample)
BE (1) BE1012869A3 (enExample)
BR (1) BR9915986A (enExample)
CA (3) CA2351580C (enExample)
CO (1) CO4980847A1 (enExample)
CY (1) CY1106870T1 (enExample)
CZ (2) CZ303006B6 (enExample)
DE (1) DE69936352T3 (enExample)
DK (1) DK1137439T4 (enExample)
ES (1) ES2288033T5 (enExample)
FR (1) FR2786771B1 (enExample)
GB (2) GB9826882D0 (enExample)
HK (1) HK1038889B (enExample)
HU (2) HU230174B1 (enExample)
ID (1) ID29250A (enExample)
IL (1) IL143092A0 (enExample)
IT (1) IT1319701B1 (enExample)
MY (2) MY127579A (enExample)
NO (2) NO332698B1 (enExample)
NZ (2) NZ511936A (enExample)
PE (1) PE20001333A1 (enExample)
PL (2) PL208854B1 (enExample)
PT (1) PT1137439E (enExample)
RU (1) RU2243769C2 (enExample)
SG (1) SG151072A1 (enExample)
SI (1) SI1137439T2 (enExample)
SK (2) SK286688B6 (enExample)
TR (2) TR200101416T2 (enExample)
TW (2) TWI248938B (enExample)
WO (1) WO2000033878A2 (enExample)
ZA (1) ZA200104360B (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007075621A1 (en) * 2005-12-20 2007-07-05 Wyeth Control of cci-779 dosage form stability through control of drug substance impurities
US8026276B2 (en) 2002-07-30 2011-09-27 Wyeth Llc Parenteral CCI-779 formulations containing cosolvents, an antioxidant, and a surfactant

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US20070032853A1 (en) 2002-03-27 2007-02-08 Hossainy Syed F 40-O-(2-hydroxy)ethyl-rapamycin coated stent
US7452692B2 (en) 2002-02-13 2008-11-18 Teva Gyógyszergyár Zártkörüen Müködö Részvénytársaság Method for extracting a macrolide from biomatter
ZA200406350B (en) 2002-02-13 2006-11-29 Teva Gyogyszergyar Reszveny Tarsasag Method for extracting a macrolide from biomatter
KR20050114262A (ko) * 2003-03-31 2005-12-05 테바 기오기스제르갸르 레스즈베니타르사사그 마크로라이드의 결정화 및 정제
US20050118344A1 (en) 2003-12-01 2005-06-02 Pacetti Stephen D. Temperature controlled crimping
ATE378345T1 (de) 2003-07-24 2007-11-15 Teva Gyogyszergyar Zartkoeruee Verfahren zur aufreinigung von makroliden
JP2007505932A (ja) 2003-09-18 2007-03-15 マクサイト， インコーポレイテッド 経強膜送達
US9114198B2 (en) * 2003-11-19 2015-08-25 Advanced Cardiovascular Systems, Inc. Biologically beneficial coatings for implantable devices containing fluorinated polymers and methods for fabricating the same
JP2007520262A (ja) * 2003-12-10 2007-07-26 アクルックス・ディ・ディ・エス・プロプライエタリー・リミテッド 経皮または局所薬物輸送に伴う副作用の処置方法
US8551512B2 (en) * 2004-03-22 2013-10-08 Advanced Cardiovascular Systems, Inc. Polyethylene glycol/poly(butylene terephthalate) copolymer coated devices including EVEROLIMUS
KR20070083839A (ko) * 2004-09-29 2007-08-24 코디스 코포레이션 안정한 무정형 라파마이신 유사 화합물의 약학적 투약 형태
AU2006213673A1 (en) 2005-02-09 2006-08-17 Santen Pharmaceutical Co., Ltd. Formulations for ocular treatment
AR058283A1 (es) * 2005-12-07 2008-01-30 Wyeth Corp Metodos para la preparacion de rapamicina cristalina y para la medicion de la cristalinidad de los compuestos de rapamicina utilizando calorimetria diferencial de barrido
US7700614B2 (en) * 2005-12-14 2010-04-20 Abbott Laboratories One pot synthesis of tetrazole derivatives of rapamycin
BRPI0707612B8 (pt) * 2006-02-09 2021-05-25 Macusight Inc vaso lacrado e formulações líquidas contidas no mesmo
US8222271B2 (en) 2006-03-23 2012-07-17 Santen Pharmaceutical Co., Ltd. Formulations and methods for vascular permeability-related diseases or conditions
AU2011260016B2 (en) 2010-06-02 2013-08-22 Fresenius Kabi Oncology Ltd. Stable pharmaceutical compositions of Rapamycin esters
WO2011156025A1 (en) * 2010-06-07 2011-12-15 Telik, Inc. Crystalline Ezatiostat Hydrochloride Ansolvate
US9321782B2 (en) * 2010-08-04 2016-04-26 Meril Life Sciences Pvt. Ltd. Process for preparation of novel 42-O-(heteroalkoxyalkyl) rapamicin compounds with anti-proliferative properties
EP2640730B1 (en) 2010-11-19 2019-08-07 Biocon Limited Processes for preparation of everolimus and intermediates thereof
US8809562B2 (en) 2011-06-06 2014-08-19 Chevron Phillips Chemical Company Lp Use of metallocene compounds for cancer treatment
WO2013022201A1 (en) * 2011-08-11 2013-02-14 Dong-A Pharm. Co., Ltd. Process of preparing a stabilized and solubilized formulation of sirolimus derivatives
US9610385B2 (en) 2013-03-07 2017-04-04 Abbott Cardiovascular Systems Inc. Method of fabricating an implantable medical device comprising a rapamycin derivative
IN2013MU02532A (enExample) 2013-07-31 2015-06-26 Sahajanand Medical Technologies Pvt Ltd
CN104721158B (zh) * 2013-12-24 2018-01-30 正大天晴药业集团股份有限公司 一种稳定的依维莫司片剂
CN104892632B (zh) * 2015-06-03 2017-12-26 道中道（菏泽）制药有限公司 一种晶体形式的依维莫司及其制备方法
US10383860B2 (en) 2015-07-28 2019-08-20 Nippon Kayaku Kabushiki Kaisha Pharmaceutical composition comprising rapamycin or derivative thereof, and method for producing the same
US20190015513A1 (en) * 2015-08-28 2019-01-17 Nippon Kayaku Kabushiki Kaisha Pharmaceutical composition comprising rapamycin or derivative thereof
JP7020914B2 (ja) * 2015-09-18 2022-02-16 日本化薬株式会社 ラパマイシン又はその誘導体を含有する医薬組成物
WO2017129772A1 (en) 2016-01-29 2017-08-03 Xellia Phamaceuticals Aps Stable pharmaceutical compositions of temsirolimus
EP3466424A1 (en) 2016-05-27 2019-04-10 Nippon Kayaku Kabushiki Kaisha Pharmaceutical composition comprizing rapamycin or derivative thereof
KR102051806B1 (ko) * 2018-01-12 2019-12-04 주식회사 종근당 에베로리무스를 포함하는 안정화된 약제학적 제제
JP2023519875A (ja) * 2020-03-27 2023-05-15 ボストン サイエンティフィック サイムド，インコーポレイテッド 薬品の結晶化のための方法
JP2023028473A (ja) * 2021-08-19 2023-03-03 日本マイクロバイオファーマ株式会社 エベロリムスの製造方法

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JPH04230389A (ja) * 1990-07-16 1992-08-19 American Home Prod Corp ラパマイシン誘導体
FI97472C (fi) * 1991-05-07 1996-12-27 American Home Prod Menetelmä terapeuttisesti käyttökelpoisten rapamysiinijohdannaisten valmistamiseksi anti-inflammatorisina ja antifungaalisina aineina
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US5302584A (en) * 1992-10-13 1994-04-12 American Home Products Corporation Carbamates of rapamycin
RU2181054C2 (ru) * 1994-11-02 2002-04-10 Новартис Аг Микроэмульсионный предконцентрат
RU2158267C2 (ru) * 1995-06-09 2000-10-27 Новартис Аг Производные рапамицина и фармацевтическая композиция на их основе
BE1009856A5 (fr) * 1995-07-14 1997-10-07 Sandoz Sa Composition pharmaceutique sous la forme d'une dispersion solide comprenant un macrolide et un vehicule.
ATE222502T1 (de) * 1996-07-30 2002-09-15 Novartis Ag Kombinationspräparat mit hemmender wirkung auf die abstossung von transplantaten, autoimmunerkrankungen und entzündungen, welches cyclosporin a und 40-0-(2-hydroxyethyl)-rapamycin enthält
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EP0975330A1 (en) 1997-02-04 2000-02-02 Abbott Laboratories Pain reducing parenteral liposome formulation

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8026276B2 (en) 2002-07-30 2011-09-27 Wyeth Llc Parenteral CCI-779 formulations containing cosolvents, an antioxidant, and a surfactant
US8299116B2 (en) 2002-07-30 2012-10-30 Wyeth Llc CCI-779 concentrate formulations
WO2007075621A1 (en) * 2005-12-20 2007-07-05 Wyeth Control of cci-779 dosage form stability through control of drug substance impurities

Also Published As

Publication number Publication date
NZ527781A (en) 2004-11-26
TR200201428T2 (tr) 2002-12-23
KR100695834B1 (ko) 2007-03-19
EP1137439A2 (en) 2001-10-04
BR9915986A (pt) 2001-09-04
HU230174B1 (hu) 2015-09-28
TWI248938B (en) 2006-02-11
NZ511936A (en) 2003-10-31
AR054444A2 (es) 2007-06-27
JP5043308B2 (ja) 2012-10-10
FR2786771A1 (fr) 2000-06-09
US7572804B2 (en) 2009-08-11
PE20001333A1 (es) 2000-12-12
PL348333A1 (en) 2002-05-20
EP2269651A2 (en) 2011-01-05
NO20012424L (no) 2001-05-16
CA2351580C (en) 2012-03-20
ES2288033T3 (es) 2007-12-16
TWI270550B (en) 2007-01-11
US7741338B2 (en) 2010-06-22
CZ302210B6 (cs) 2010-12-22
US20090270441A1 (en) 2009-10-29
EP1137439B2 (en) 2011-11-23
SI1137439T2 (sl) 2012-05-31
CO4980847A1 (es) 2000-11-27
GB9904934D0 (en) 1999-04-28
CA2732620A1 (en) 2000-06-15
US20080161334A1 (en) 2008-07-03
DE69936352T2 (de) 2008-02-14
DE69936352D1 (de) 2007-08-02
CN1876657A (zh) 2006-12-13
SK7662001A3 (en) 2001-12-03
CA2651609A1 (en) 2000-06-15
ITMI992520A1 (it) 2001-06-02
CN1261163C (zh) 2006-06-28
JP3805625B2 (ja) 2006-08-02
MY120594A (en) 2005-11-30
SK287325B6 (sk) 2010-07-07
CA2351580A1 (en) 2000-06-15
US20030191148A1 (en) 2003-10-09
WO2000033878A3 (en) 2000-11-02
JP2002531527A (ja) 2002-09-24
JP2006111637A (ja) 2006-04-27
NO20012424D0 (no) 2001-05-16
TW200540179A (en) 2005-12-16
US20050107418A1 (en) 2005-05-19
AR026102A1 (es) 2003-01-29
RU2243769C2 (ru) 2005-01-10
CA2732620C (en) 2013-08-06
KR20010101128A (ko) 2001-11-14
PL196627B1 (pl) 2008-01-31
NO332698B1 (no) 2012-12-10
AU1657300A (en) 2000-06-26
US7297703B2 (en) 2007-11-20
SI1137439T1 (sl) 2008-06-30
CY1106870T1 (el) 2012-09-26
KR20060096477A (ko) 2006-09-11
EP1743657A3 (en) 2007-03-28
SK286688B6 (sk) 2009-03-05
CZ20012001A3 (cs) 2001-09-12
HK1038889A1 (en) 2002-04-04
EP1137439B1 (en) 2007-06-20
AR048073A2 (es) 2006-03-29
MY127579A (en) 2006-12-29
BE1012869A3 (fr) 2001-04-03
WO2000033878A2 (en) 2000-06-15
CZ303006B6 (cs) 2012-02-22
PT1137439E (pt) 2007-09-25
JP2005200429A (ja) 2005-07-28
PL208854B1 (pl) 2011-06-30
ID29250A (id) 2001-08-16
HK1038889B (en) 2008-01-25
CN1876657B (zh) 2013-01-09
US6605613B2 (en) 2003-08-12
HU228939B1 (en) 2013-07-29
ITMI992520A0 (it) 1999-12-02
ZA200104360B (en) 2002-01-16
NO20121113L (no) 2001-05-16
DK1137439T4 (da) 2012-03-19
JP5165199B2 (ja) 2013-03-21
NO334612B1 (no) 2014-04-22
EP2269651A3 (en) 2011-03-09
ATE365051T1 (de) 2007-07-15
EP2279751A2 (en) 2011-02-02
HUP0104489A2 (hu) 2002-03-28
DK1137439T3 (da) 2007-09-10
US6852729B2 (en) 2005-02-08
ES2288033T5 (es) 2012-04-10
DE69936352T3 (de) 2012-05-03
US20020032213A1 (en) 2002-03-14
SG151072A1 (en) 2009-06-29
TR200101416T2 (tr) 2002-01-21
IL143092A0 (en) 2002-04-21
GB9826882D0 (en) 1999-01-27
HUP0104489A3 (en) 2004-05-28
EP1743657A2 (en) 2007-01-17
IT1319701B1 (it) 2003-10-27
CN1374872A (zh) 2002-10-16
FR2786771B1 (fr) 2002-12-27
EP2279751A3 (en) 2011-02-16

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