KR100695834B1 - 마크로리드의 안정화 방법 - Google Patents

마크로리드의 안정화 방법 Download PDF

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Publication number
KR100695834B1
KR100695834B1 KR1020017007009A KR20017007009A KR100695834B1 KR 100695834 B1 KR100695834 B1 KR 100695834B1 KR 1020017007009 A KR1020017007009 A KR 1020017007009A KR 20017007009 A KR20017007009 A KR 20017007009A KR 100695834 B1 KR100695834 B1 KR 100695834B1
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KR
South Korea
Prior art keywords
rapamycin
ascomycin
derivative
antioxidant
mixture
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 - Lifetime
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KR1020017007009A
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English (en)
Korean (ko)
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KR20010101128A (ko
Inventor
프랑쏘와 나바로
사무엘 쁘띠
가이 스톤
Original Assignee
노파르티스 아게
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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=KR100695834(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 노파르티스 아게 filed Critical 노파르티스 아게
Publication of KR20010101128A publication Critical patent/KR20010101128A/ko
Application granted granted Critical
Publication of KR100695834B1 publication Critical patent/KR100695834B1/ko
Anticipated expiration legal-status Critical
Expired - Lifetime 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
    • A61K31/435—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

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  • 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)
KR1020017007009A 1998-12-07 1999-12-06 마크로리드의 안정화 방법 Expired - Lifetime KR100695834B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB9826882.4 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
GB9904934.8 1999-03-04

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020067017352A Division KR20060096477A (ko) 1998-12-07 1999-12-06 마크로리드의 안정화 방법

Publications (2)

Publication Number Publication Date
KR20010101128A KR20010101128A (ko) 2001-11-14
KR100695834B1 true KR100695834B1 (ko) 2007-03-19

Family

ID=26314797

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020067017352A Ceased KR20060096477A (ko) 1998-12-07 1999-12-06 마크로리드의 안정화 방법
KR1020017007009A Expired - Lifetime KR100695834B1 (ko) 1998-12-07 1999-12-06 마크로리드의 안정화 방법

Family Applications Before (1)

Application Number Title Priority Date Filing Date
KR1020067017352A Ceased KR20060096477A (ko) 1998-12-07 1999-12-06 마크로리드의 안정화 방법

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)

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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
ES2300622T3 (es) 2002-07-30 2008-06-16 Wyeth Formulaciones parenterales que contienen un hidroxiester de rapamicina.
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
EP1962819A1 (en) * 2005-12-20 2008-09-03 Wyeth Control of cci-779 dosage form stability through control of drug substance impurities
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

Citations (1)

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EP0663916A1 (en) * 1992-10-09 1995-07-26 SANDOZ-ERFINDUNGEN Verwaltungsgesellschaft m.b.H. O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants

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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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RU2158267C2 (ru) * 1995-06-09 2000-10-27 Новартис Аг Производные рапамицина и фармацевтическая композиция на их основе
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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

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
EP0663916A1 (en) * 1992-10-09 1995-07-26 SANDOZ-ERFINDUNGEN Verwaltungsgesellschaft m.b.H. O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants

Also Published As

Publication number Publication date
NZ527781A (en) 2004-11-26
TR200201428T2 (tr) 2002-12-23
AU759219B2 (en) 2003-04-10
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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