CN1261163C - 大环内酯的稳定化 - Google Patents

大环内酯的稳定化 Download PDF

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Publication number
CN1261163C
CN1261163C CNB998141240A CN99814124A CN1261163C CN 1261163 C CN1261163 C CN 1261163C CN B998141240 A CNB998141240 A CN B998141240A CN 99814124 A CN99814124 A CN 99814124A CN 1261163 C CN1261163 C CN 1261163C
Authority
CN
China
Prior art keywords
rapamycin
ethyl
mixture
derivative
macrolides
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
Application number
CNB998141240A
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English (en)
Chinese (zh)
Other versions
CN1374872A (zh
Inventor
F·纳瓦罗
S·派提特
G·斯通
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=CN1261163(C) "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 CN1374872A publication Critical patent/CN1374872A/zh
Application granted granted Critical
Publication of CN1261163C publication Critical patent/CN1261163C/zh
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
    • 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
    • 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

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)
CNB998141240A 1998-12-07 1999-12-06 大环内酯的稳定化 Expired - Lifetime CN1261163C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GBGB9826882.4A GB9826882D0 (en) 1998-12-07 1998-12-07 Organic compounds
GB9904934.8 1999-03-04
GBGB9904934.8A GB9904934D0 (en) 1998-12-07 1999-03-04 Organic compounds
GB9826882.4 1999-03-04

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN2006100798040A Division CN1876657B (zh) 1998-12-07 1999-12-06 大环内酯的稳定化

Publications (2)

Publication Number Publication Date
CN1374872A CN1374872A (zh) 2002-10-16
CN1261163C true CN1261163C (zh) 2006-06-28

Family

ID=26314797

Family Applications (2)

Application Number Title Priority Date Filing Date
CNB998141240A Expired - Lifetime CN1261163C (zh) 1998-12-07 1999-12-06 大环内酯的稳定化
CN2006100798040A Expired - Lifetime CN1876657B (zh) 1998-12-07 1999-12-06 大环内酯的稳定化

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN2006100798040A Expired - Lifetime CN1876657B (zh) 1998-12-07 1999-12-06 大环内酯的稳定化

Country Status (38)

Country Link
US (5) US6605613B2 (enExample)
EP (4) EP1743657A3 (enExample)
JP (3) JP3805625B2 (enExample)
KR (2) KR20060096477A (enExample)
CN (2) CN1261163C (enExample)
AR (3) AR026102A1 (enExample)
AT (1) ATE365051T1 (enExample)
AU (1) AU759219B2 (enExample)
BE (1) BE1012869A3 (enExample)
BR (1) BR9915986A (enExample)
CA (3) CA2651609A1 (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) HU228939B1 (enExample)
ID (1) ID29250A (enExample)
IL (1) IL143092A0 (enExample)
IT (1) IT1319701B1 (enExample)
MY (2) MY120594A (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) TWI270550B (enExample)
WO (1) WO2000033878A2 (enExample)
ZA (1) ZA200104360B (enExample)

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CA2475383C (en) 2002-02-13 2009-12-22 Biogal Gyogyszergyar Rt. Method for extracting a macrolide from biomatter
KR101131794B1 (ko) 2002-07-30 2012-03-30 와이어쓰 엘엘씨 Ｃｃｉ-779 공용매 농축액, 비경구 ｃｃｉ-779 제형 및 비경구 ｃｃｉ-779 제형의 제조방법
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
WO2005010015A1 (en) 2003-07-24 2005-02-03 Teva Gyogyszergyar Reszvenytarsasag Method of purifying macrolides
CA2539324A1 (en) 2003-09-18 2005-03-31 Macusight, Inc. Transscleral delivery
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US8551512B2 (en) * 2004-03-22 2013-10-08 Advanced Cardiovascular Systems, Inc. Polyethylene glycol/poly(butylene terephthalate) copolymer coated devices including EVEROLIMUS
WO2006039237A1 (en) * 2004-09-29 2006-04-13 Cordis Corporation Pharmaceutical dosage forms of stable amorphous rapamycin like compounds
BRPI0607606B1 (pt) 2005-02-09 2021-06-22 Santen Pharmaceutical, Co., Ltd. Formulação líquida
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
JP2009520818A (ja) * 2005-12-20 2009-05-28 ワイス 薬物物質不純物の制御によるｃｃｉ−７７９製剤安定性の制御
CN101605529B (zh) * 2006-02-09 2013-03-13 参天制药株式会社 稳定制剂及它们的制备和使用方法
BRPI0709016A2 (pt) 2006-03-23 2011-06-21 Macusight Inc formulações e métodos para doenças ou condições relacionadas com a permeabilidade vascular
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
WO2012066502A1 (en) 2010-11-19 2012-05-24 Biocon Limited Processes for preparation of everolimus and intermediates thereof
WO2012170384A1 (en) 2011-06-06 2012-12-13 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
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
US20190015513A1 (en) * 2015-08-28 2019-01-17 Nippon Kayaku Kabushiki Kaisha Pharmaceutical composition comprising rapamycin or derivative thereof
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
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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US3996355A (en) 1975-01-02 1976-12-07 American Home Products Corporation Permanent suspension pharmaceutical dosage form
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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
EP1266900A1 (en) 1992-10-13 2002-12-18 Wyeth Carbamates of rapamycin
RU2181054C2 (ru) * 1994-11-02 2002-04-10 Новартис Аг Микроэмульсионный предконцентрат
ATE228135T1 (de) * 1995-06-09 2002-12-15 Novartis Erfind Verwalt Gmbh Rapamycinderivate
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
EP1208847B8 (en) * 1996-07-30 2007-02-14 Novartis AG Pharmaceutical compositions for the treatment of transplant rejection, as well as autoimmune or inflammatory conditions
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Publication number Publication date
US6852729B2 (en) 2005-02-08
TWI270550B (en) 2007-01-11
WO2000033878A3 (en) 2000-11-02
ES2288033T3 (es) 2007-12-16
KR20010101128A (ko) 2001-11-14
HK1038889B (en) 2008-01-25
CN1374872A (zh) 2002-10-16
US7741338B2 (en) 2010-06-22
DE69936352D1 (de) 2007-08-02
CA2651609A1 (en) 2000-06-15
US7572804B2 (en) 2009-08-11
US7297703B2 (en) 2007-11-20
SK287325B6 (sk) 2010-07-07
TWI248938B (en) 2006-02-11
JP5165199B2 (ja) 2013-03-21
EP1743657A2 (en) 2007-01-17
EP1137439B1 (en) 2007-06-20
SI1137439T2 (sl) 2012-05-31
PT1137439E (pt) 2007-09-25
KR20060096477A (ko) 2006-09-11
AR048073A2 (es) 2006-03-29
HU230174B1 (hu) 2015-09-28
EP1137439B2 (en) 2011-11-23
JP3805625B2 (ja) 2006-08-02
AR026102A1 (es) 2003-01-29
CA2351580C (en) 2012-03-20
JP2006111637A (ja) 2006-04-27
WO2000033878A2 (en) 2000-06-15
EP2269651A2 (en) 2011-01-05
JP2005200429A (ja) 2005-07-28
MY120594A (en) 2005-11-30
EP1743657A3 (en) 2007-03-28
US20050107418A1 (en) 2005-05-19
HUP0104489A2 (hu) 2002-03-28
US20020032213A1 (en) 2002-03-14
NZ527781A (en) 2004-11-26
FR2786771B1 (fr) 2002-12-27
NO20012424D0 (no) 2001-05-16
IT1319701B1 (it) 2003-10-27
ATE365051T1 (de) 2007-07-15
SK286688B6 (sk) 2009-03-05
CA2732620A1 (en) 2000-06-15
AU1657300A (en) 2000-06-26
DE69936352T2 (de) 2008-02-14
US20090270441A1 (en) 2009-10-29
ID29250A (id) 2001-08-16
GB9826882D0 (en) 1999-01-27
HUP0104489A3 (en) 2004-05-28
IL143092A0 (en) 2002-04-21
CN1876657B (zh) 2013-01-09
DE69936352T3 (de) 2012-05-03
HK1038889A1 (en) 2002-04-04
DK1137439T4 (da) 2012-03-19
PL208854B1 (pl) 2011-06-30
NO20121113L (no) 2001-05-16
PE20001333A1 (es) 2000-12-12
ITMI992520A1 (it) 2001-06-02
AR054444A2 (es) 2007-06-27
CY1106870T1 (el) 2012-09-26
DK1137439T3 (da) 2007-09-10
HU228939B1 (en) 2013-07-29
EP1137439A2 (en) 2001-10-04
JP5043308B2 (ja) 2012-10-10
CZ20012001A3 (cs) 2001-09-12
NO332698B1 (no) 2012-12-10
US6605613B2 (en) 2003-08-12
NO334612B1 (no) 2014-04-22
CZ302210B6 (cs) 2010-12-22
PL348333A1 (en) 2002-05-20
PL196627B1 (pl) 2008-01-31
FR2786771A1 (fr) 2000-06-09
EP2279751A2 (en) 2011-02-02
ES2288033T5 (es) 2012-04-10
EP2269651A3 (en) 2011-03-09
US20080161334A1 (en) 2008-07-03
BR9915986A (pt) 2001-09-04
SI1137439T1 (sl) 2008-06-30
NZ511936A (en) 2003-10-31
TR200101416T2 (tr) 2002-01-21
SG151072A1 (en) 2009-06-29
KR100695834B1 (ko) 2007-03-19
MY127579A (en) 2006-12-29
CZ303006B6 (cs) 2012-02-22
SK7662001A3 (en) 2001-12-03
US20030191148A1 (en) 2003-10-09
CN1876657A (zh) 2006-12-13
GB9904934D0 (en) 1999-04-28
RU2243769C2 (ru) 2005-01-10
CA2732620C (en) 2013-08-06
BE1012869A3 (fr) 2001-04-03
NO20012424L (no) 2001-05-16
CO4980847A1 (es) 2000-11-27
ITMI992520A0 (it) 1999-12-02
TR200201428T2 (tr) 2002-12-23
CA2351580A1 (en) 2000-06-15
JP2002531527A (ja) 2002-09-24
TW200540179A (en) 2005-12-16
AU759219B2 (en) 2003-04-10
EP2279751A3 (en) 2011-02-16
ZA200104360B (en) 2002-01-16

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