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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (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
GB9826882 1998-12-07
GBGB9826882.4A GB9826882D0 (en) 1998-12-07 1998-12-07 Organic compounds
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 (https=)
EP (4) EP2269651A3 (https=)
JP (3) JP3805625B2 (https=)
KR (2) KR100695834B1 (https=)
CN (2) CN1876657B (https=)
AR (3) AR026102A1 (https=)
AT (1) ATE365051T1 (https=)
AU (1) AU759219B2 (https=)
BE (1) BE1012869A3 (https=)
BR (1) BR9915986A (https=)
CA (3) CA2351580C (https=)
CO (1) CO4980847A1 (https=)
CY (1) CY1106870T1 (https=)
CZ (2) CZ302210B6 (https=)
DE (1) DE69936352T3 (https=)
DK (1) DK1137439T4 (https=)
ES (1) ES2288033T5 (https=)
FR (1) FR2786771B1 (https=)
GB (2) GB9826882D0 (https=)
HK (1) HK1038889B (https=)
HU (2) HU230174B1 (https=)
ID (1) ID29250A (https=)
IL (1) IL143092A0 (https=)
IT (1) IT1319701B1 (https=)
MY (2) MY127579A (https=)
NO (2) NO332698B1 (https=)
NZ (2) NZ511936A (https=)
PE (1) PE20001333A1 (https=)
PL (2) PL196627B1 (https=)
PT (1) PT1137439E (https=)
RU (1) RU2243769C2 (https=)
SG (1) SG151072A1 (https=)
SI (1) SI1137439T2 (https=)
SK (2) SK286688B6 (https=)
TR (2) TR200101416T2 (https=)
TW (2) TWI248938B (https=)
WO (1) WO2000033878A2 (https=)
ZA (1) ZA200104360B (https=)

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

Families Citing this family (34)

* Cited by examiner, † Cited by third party
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US20070032853A1 (en) 2002-03-27 2007-02-08 Hossainy Syed F 40-O-(2-hydroxy)ethyl-rapamycin coated stent
MXPA04007847A (es) 2002-02-13 2005-02-24 Biogal Gyogyszergyar Metodo para extraer un macrolido de biomateria.
US7452692B2 (en) 2002-02-13 2008-11-18 Teva Gyógyszergyár Zártkörüen Müködö Részvénytársaság Method for extracting a macrolide from biomatter
WO2004089958A2 (en) * 2003-03-31 2004-10-21 TEVA Gyógyszergyár Részvénytársaság Crystallization and purification of macrolides
US20050118344A1 (en) 2003-12-01 2005-06-02 Pacetti Stephen D. Temperature controlled crimping
PL1558622T3 (pl) 2003-07-24 2008-06-30 Teva Gyogyszergyar Zartkoerueen Muekoedoe Reszvenytarsasag Sposób oczyszczania makrolidów
KR20060085246A (ko) 2003-09-18 2006-07-26 마커사이트, 인코포레이티드 경공막 전달
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
KR20060126701A (ko) * 2003-12-10 2006-12-08 애크럭스 디디에스 피티와이 리미티드 경피 또는 국소 약물 전달에 따른 원치않는 효과의치료방법
US8551512B2 (en) * 2004-03-22 2013-10-08 Advanced Cardiovascular Systems, Inc. Polyethylene glycol/poly(butylene terephthalate) copolymer coated devices including EVEROLIMUS
MX2007003731A (es) * 2004-09-29 2007-08-14 Johnson & Johnson Formas de dosis farmaceuticas de compuestos similares a rapamicina amorfos estables.
DK1848431T3 (en) 2005-02-09 2016-04-18 Santen Pharmaceutical Co Ltd LIQUID FORMULATIONS FOR TREATMENT OF DISEASES OR CONDITIONS
WO2007067566A2 (en) * 2005-12-07 2007-06-14 Wyeth Methods for preparing crystalline rapamycin and for measuring crystallinity of rapamycin compounds using differential scanning calorimetry
US7700614B2 (en) * 2005-12-14 2010-04-20 Abbott Laboratories One pot synthesis of tetrazole derivatives of rapamycin
KR20140093764A (ko) * 2006-02-09 2014-07-28 산텐 세이야꾸 가부시키가이샤 안정한 제제와 그 제조 및 사용 방법
ES2563288T3 (es) 2006-03-23 2016-03-14 Santen Pharmaceutical Co., Ltd Rapamicina en dosis bajas para el tratamiento de enfermedades relacionadas con la permeabilidad vascular
JP2013527223A (ja) 2010-06-02 2013-06-27 フレゼニウス・カビ・オンコロジー・リミテッド ラパマイシンエステルの安定な医薬組成物
CN103025753A (zh) * 2010-06-07 2013-04-03 泰立克公司 晶体盐酸依泽替米贝非溶剂化物
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"
ES2753529T3 (es) 2010-11-19 2020-04-13 Biocon Ltd Procesos para la preparación de everolimús y productos intermedios del mismo
JP2014516075A (ja) 2011-06-06 2014-07-07 シェブロン フィリップス ケミカル カンパニー エルピー 癌治療のためのメタロセン化合物の使用
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 (https=) 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
EP3329916A4 (en) 2015-07-28 2019-03-20 Nippon Kayaku Kabushiki Kaisha PHARMACEUTICAL COMPOSITION COMPRISING RAPAMYCIN OR A DERIVATIVE THEREOF, AND PROCESS FOR PRODUCING THE SAME
JP6793651B2 (ja) * 2015-08-28 2020-12-02 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
US20190038605A1 (en) * 2015-09-18 2019-02-07 Nippon Kayaku Kabushiki Kaisha Pharmaceutical composition comprising rapamycin or derivative thereof
WO2017129772A1 (en) 2016-01-29 2017-08-03 Xellia Phamaceuticals Aps Stable pharmaceutical compositions of temsirolimus
WO2017204215A1 (ja) 2016-05-27 2017-11-30 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
KR102051806B1 (ko) * 2018-01-12 2019-12-04 주식회사 종근당 에베로리무스를 포함하는 안정화된 약제학적 제제
EP4126882A1 (en) * 2020-03-27 2023-02-08 Boston Scientific Scimed Inc. Methods for crystallization of drugs
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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SG47580A1 (en) 1992-10-13 1998-04-17 American Home Prod Carbamates of rapamycin
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
US5985890A (en) 1995-06-09 1999-11-16 Novartis Ag Rapamycin derivatives
FR2736550B1 (fr) * 1995-07-14 1998-07-24 Sandoz Sa Composition pharmaceutique sous la forme d'une dispersion solide comprenant un macrolide et un vehicule
PT956034E (pt) * 1996-07-30 2002-12-31 Novartis Ag Composicoes farmaceuticas para o tratamento da rejeicao de transplantes estados inflamatorios ou auto-imunes compreendendo ciclosporina a e 40-o-(2-hidroxietil)-rapamicina
US6362264B1 (en) * 1996-12-20 2002-03-26 Ck Witco Corporation Stabilizer for food contact and medical grade PVC
CA2279259A1 (en) 1997-02-04 1998-08-06 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
SK7662001A3 (en) 2001-12-03
KR100695834B1 (ko) 2007-03-19
GB9826882D0 (en) 1999-01-27
PL348333A1 (en) 2002-05-20
EP1137439A2 (en) 2001-10-04
US20080161334A1 (en) 2008-07-03
NZ511936A (en) 2003-10-31
BE1012869A3 (fr) 2001-04-03
SK287325B6 (sk) 2010-07-07
ES2288033T3 (es) 2007-12-16
PT1137439E (pt) 2007-09-25
CA2732620A1 (en) 2000-06-15
MY127579A (en) 2006-12-29
ITMI992520A1 (it) 2001-06-02
ZA200104360B (en) 2002-01-16
DE69936352T3 (de) 2012-05-03
CY1106870T1 (el) 2012-09-26
US7297703B2 (en) 2007-11-20
US7572804B2 (en) 2009-08-11
HK1038889B (en) 2008-01-25
MY120594A (en) 2005-11-30
RU2243769C2 (ru) 2005-01-10
JP2005200429A (ja) 2005-07-28
US20090270441A1 (en) 2009-10-29
SI1137439T2 (sl) 2012-05-31
SK286688B6 (sk) 2009-03-05
NO20012424D0 (no) 2001-05-16
US7741338B2 (en) 2010-06-22
CA2732620C (en) 2013-08-06
EP2279751A3 (en) 2011-02-16
HUP0104489A3 (en) 2004-05-28
IL143092A0 (en) 2002-04-21
EP1137439B2 (en) 2011-11-23
FR2786771B1 (fr) 2002-12-27
JP5043308B2 (ja) 2012-10-10
SI1137439T1 (sl) 2008-06-30
KR20060096477A (ko) 2006-09-11
CA2351580C (en) 2012-03-20
EP1743657A3 (en) 2007-03-28
JP3805625B2 (ja) 2006-08-02
CA2651609A1 (en) 2000-06-15
NO20012424L (no) 2001-05-16
ID29250A (id) 2001-08-16
CN1261163C (zh) 2006-06-28
CN1876657B (zh) 2013-01-09
AR048073A2 (es) 2006-03-29
TR200101416T2 (tr) 2002-01-21
EP1137439B1 (en) 2007-06-20
US6605613B2 (en) 2003-08-12
CA2351580A1 (en) 2000-06-15
TR200201428T2 (tr) 2002-12-23
AU1657300A (en) 2000-06-26
CN1876657A (zh) 2006-12-13
US20050107418A1 (en) 2005-05-19
DK1137439T4 (da) 2012-03-19
JP2006111637A (ja) 2006-04-27
BR9915986A (pt) 2001-09-04
JP5165199B2 (ja) 2013-03-21
JP2002531527A (ja) 2002-09-24
WO2000033878A2 (en) 2000-06-15
HU228939B1 (en) 2013-07-29
ITMI992520A0 (it) 1999-12-02
HUP0104489A2 (hu) 2002-03-28
DE69936352D1 (de) 2007-08-02
PL196627B1 (pl) 2008-01-31
US6852729B2 (en) 2005-02-08
GB9904934D0 (en) 1999-04-28
DK1137439T3 (da) 2007-09-10
CZ303006B6 (cs) 2012-02-22
SG151072A1 (en) 2009-06-29
EP1743657A2 (en) 2007-01-17
EP2269651A3 (en) 2011-03-09
FR2786771A1 (fr) 2000-06-09
AR026102A1 (es) 2003-01-29
CZ302210B6 (cs) 2010-12-22
CN1374872A (zh) 2002-10-16
KR20010101128A (ko) 2001-11-14
NO334612B1 (no) 2014-04-22
IT1319701B1 (it) 2003-10-27
US20030191148A1 (en) 2003-10-09
NZ527781A (en) 2004-11-26
TW200540179A (en) 2005-12-16
PE20001333A1 (es) 2000-12-12
ES2288033T5 (es) 2012-04-10
NO332698B1 (no) 2012-12-10
HU230174B1 (hu) 2015-09-28
US20020032213A1 (en) 2002-03-14
TWI270550B (en) 2007-01-11
EP2269651A2 (en) 2011-01-05
EP2279751A2 (en) 2011-02-02
TWI248938B (en) 2006-02-11
CZ20012001A3 (cs) 2001-09-12
ATE365051T1 (de) 2007-07-15
WO2000033878A3 (en) 2000-11-02
DE69936352T2 (de) 2008-02-14
PL208854B1 (pl) 2011-06-30
HK1038889A1 (en) 2002-04-04
NO20121113L (no) 2001-05-16
CO4980847A1 (es) 2000-11-27
AR054444A2 (es) 2007-06-27

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