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
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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
GBGB9826882.4A GB9826882D0 (en) 1998-12-07 1998-12-07 Organic compounds
GB9826882.4 1998-12-07
GB9904934.8 1999-03-04
GBGB9904934.8A GB9904934D0 (en) 1998-12-07 1999-03-04 Organic compounds

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
KR1020017007009A Expired - Lifetime KR100695834B1 (ko) 1998-12-07 1999-12-06 마크로리드의 안정화 방법
KR1020067017352A Ceased KR20060096477A (ko) 1998-12-07 1999-12-06 마크로리드의 안정화 방법

Family Applications After (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 (https=)
EP (4) EP2279751A3 (https=)
JP (3) JP3805625B2 (https=)
KR (2) KR100695834B1 (https=)
CN (2) CN1261163C (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) CZ303006B6 (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) HU228939B1 (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) PL208854B1 (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) TWI270550B (https=)
WO (1) WO2000033878A2 (https=)
ZA (1) ZA200104360B (https=)

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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
MXPA04007847A (es) 2002-02-13 2005-02-24 Biogal Gyogyszergyar Metodo para extraer un macrolido de biomateria.
NZ537829A (en) 2002-07-30 2006-09-29 Wyeth Corp Parenteral formulations containing a rapamycin hydroxyester
TR200500302T3 (tr) * 2003-03-31 2005-04-21 Biogal Gyogyszergyar Rt. Makrolidlerin kristalizasyonu ve saflaştırılması.
US20050118344A1 (en) 2003-12-01 2005-06-02 Pacetti Stephen D. Temperature controlled crimping
TW200523266A (en) 2003-07-24 2005-07-16 Biogal Gyogyszergyar Method of purifying macrolides
CA2539324A1 (en) 2003-09-18 2005-03-31 Macusight, Inc. Transscleral delivery
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
CN1889994A (zh) * 2003-12-10 2007-01-03 艾克若克斯Dds有限公司 伴随透皮或局部药物输送的不希望的效果的治疗方法
US8551512B2 (en) 2004-03-22 2013-10-08 Advanced Cardiovascular Systems, Inc. Polyethylene glycol/poly(butylene terephthalate) copolymer coated devices including EVEROLIMUS
US20060094744A1 (en) * 2004-09-29 2006-05-04 Maryanoff Cynthia A Pharmaceutical dosage forms of stable amorphous rapamycin like compounds
JP4974903B2 (ja) 2005-02-09 2012-07-11 参天製薬株式会社 疾患または状態を処置するための液体処方物
BRPI0619592A2 (pt) * 2005-12-07 2016-09-06 Wyeth Corp métodos para medir a qualidade da partícula de um composto de rapamicina, para determinar o tamanho de partícula médio de uma amostra e a cristalinidade de um composto de rapamicina, e para a purificação de rapamicina
US7700614B2 (en) * 2005-12-14 2010-04-20 Abbott Laboratories One pot synthesis of tetrazole derivatives of rapamycin
RU2008121713A (ru) * 2005-12-20 2010-01-27 Вайет (Us) Контроль стабильности лекарственной формы cci-779 посредством контроля примесей лекарственныхого вещества
WO2007092620A2 (en) * 2006-02-09 2007-08-16 Macusight, Inc. Stable formulations, and methods of their preparation and use
PL2001466T3 (pl) 2006-03-23 2016-06-30 Santen Pharmaceutical Co Ltd Rapamycyna w małej dawce do leczenia chorób związanych z przepuszczalnością naczyń
WO2011151704A2 (en) 2010-06-02 2011-12-08 Fresenius Kabi Oncology Ltd. Stable pharmaceutical compositions of rapamycin esters
WO2011156025A1 (en) * 2010-06-07 2011-12-15 Telik, Inc. Crystalline Ezatiostat Hydrochloride Ansolvate
EP2601201B1 (en) * 2010-08-04 2014-09-24 Meril Life Sciences Pvt. Ltd. Process for preparation of novel 42-0-(heteroalkoxyalkyl) rapamycin compounds with anti-proliferative properties"
WO2012066502A1 (en) 2010-11-19 2012-05-24 Biocon Limited Processes for preparation of everolimus and intermediates thereof
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
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
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
WO2017047618A1 (ja) * 2015-09-18 2017-03-23 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
JP6855470B2 (ja) 2016-05-27 2021-04-07 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
CN119431400A (zh) * 2020-03-27 2025-02-14 波士顿科学国际有限公司 用于使药物结晶的方法
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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KR0159766B1 (ko) * 1989-10-16 1998-12-01 후지사와 토모키치로 양모제 조성물
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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RU2181054C2 (ru) * 1994-11-02 2002-04-10 Новартис Аг Микроэмульсионный предконцентрат
EP0833828B1 (en) 1995-06-09 2002-11-20 Novartis AG Rapamycin derivatives
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.
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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
ITMI992520A1 (it) 2001-06-02
BE1012869A3 (fr) 2001-04-03
ES2288033T3 (es) 2007-12-16
US7572804B2 (en) 2009-08-11
SI1137439T2 (sl) 2012-05-31
GB9904934D0 (en) 1999-04-28
ITMI992520A0 (it) 1999-12-02
AU1657300A (en) 2000-06-26
JP2006111637A (ja) 2006-04-27
HUP0104489A3 (en) 2004-05-28
FR2786771A1 (fr) 2000-06-09
PE20001333A1 (es) 2000-12-12
PT1137439E (pt) 2007-09-25
CZ303006B6 (cs) 2012-02-22
NO20012424D0 (no) 2001-05-16
WO2000033878A3 (en) 2000-11-02
WO2000033878A2 (en) 2000-06-15
CA2732620A1 (en) 2000-06-15
IL143092A0 (en) 2002-04-21
US7741338B2 (en) 2010-06-22
FR2786771B1 (fr) 2002-12-27
AR048073A2 (es) 2006-03-29
EP2269651A2 (en) 2011-01-05
RU2243769C2 (ru) 2005-01-10
TR200101416T2 (tr) 2002-01-21
JP2002531527A (ja) 2002-09-24
NO20012424L (no) 2001-05-16
CZ20012001A3 (cs) 2001-09-12
ID29250A (id) 2001-08-16
NO20121113L (no) 2001-05-16
US20050107418A1 (en) 2005-05-19
CY1106870T1 (el) 2012-09-26
DK1137439T3 (da) 2007-09-10
US20030191148A1 (en) 2003-10-09
PL348333A1 (en) 2002-05-20
CN1876657B (zh) 2013-01-09
EP2279751A3 (en) 2011-02-16
US6605613B2 (en) 2003-08-12
CA2351580C (en) 2012-03-20
TWI270550B (en) 2007-01-11
US20090270441A1 (en) 2009-10-29
EP1743657A3 (en) 2007-03-28
US6852729B2 (en) 2005-02-08
GB9826882D0 (en) 1999-01-27
TW200540179A (en) 2005-12-16
JP3805625B2 (ja) 2006-08-02
SI1137439T1 (sl) 2008-06-30
US20080161334A1 (en) 2008-07-03
EP2279751A2 (en) 2011-02-02
BR9915986A (pt) 2001-09-04
EP1137439A2 (en) 2001-10-04
MY120594A (en) 2005-11-30
DE69936352T2 (de) 2008-02-14
ES2288033T5 (es) 2012-04-10
CO4980847A1 (es) 2000-11-27
PL196627B1 (pl) 2008-01-31
HK1038889A1 (en) 2002-04-04
US7297703B2 (en) 2007-11-20
ZA200104360B (en) 2002-01-16
CZ302210B6 (cs) 2010-12-22
EP1743657A2 (en) 2007-01-17
TWI248938B (en) 2006-02-11
HU228939B1 (en) 2013-07-29
EP1137439B1 (en) 2007-06-20
ATE365051T1 (de) 2007-07-15
TR200201428T2 (tr) 2002-12-23
AR026102A1 (es) 2003-01-29
NO334612B1 (no) 2014-04-22
HU230174B1 (hu) 2015-09-28
NZ527781A (en) 2004-11-26
KR20010101128A (ko) 2001-11-14
CA2351580A1 (en) 2000-06-15
JP5043308B2 (ja) 2012-10-10
HUP0104489A2 (hu) 2002-03-28
CN1876657A (zh) 2006-12-13
JP2005200429A (ja) 2005-07-28
CN1374872A (zh) 2002-10-16
SK286688B6 (sk) 2009-03-05
JP5165199B2 (ja) 2013-03-21
EP1137439B2 (en) 2011-11-23
CA2651609A1 (en) 2000-06-15
AR054444A2 (es) 2007-06-27
SK287325B6 (sk) 2010-07-07
DK1137439T4 (da) 2012-03-19
SK7662001A3 (en) 2001-12-03
PL208854B1 (pl) 2011-06-30
MY127579A (en) 2006-12-29
DE69936352D1 (de) 2007-08-02
AU759219B2 (en) 2003-04-10
CN1261163C (zh) 2006-06-28
US20020032213A1 (en) 2002-03-14
NZ511936A (en) 2003-10-31
KR20060096477A (ko) 2006-09-11
SG151072A1 (en) 2009-06-29
CA2732620C (en) 2013-08-06
EP2269651A3 (en) 2011-03-09
DE69936352T3 (de) 2012-05-03
IT1319701B1 (it) 2003-10-27
HK1038889B (en) 2008-01-25
NO332698B1 (no) 2012-12-10

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