CN1139595C - 结晶性大环内酯及其制备方法 - Google Patents

结晶性大环内酯及其制备方法 Download PDF

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Publication number
CN1139595C
CN1139595C CNB988064677A CN98806467A CN1139595C CN 1139595 C CN1139595 C CN 1139595C CN B988064677 A CNB988064677 A CN B988064677A CN 98806467 A CN98806467 A CN 98806467A CN 1139595 C CN1139595 C CN 1139595C
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CN
China
Prior art keywords
compound
crystalline
formula
solution
preparation
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Expired - Lifetime
Application number
CNB988064677A
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English (en)
Chinese (zh)
Other versions
CN1261365A (zh
Inventor
C�������ɭ
C·多森巴克
M·格拉斯伯格
O·哈特曼
A·霍瓦斯
J·－P·穆兹
���˹���Ѷ���
G·彭
�������ɭ
S·普费夫
D·维克胡森
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.)
Ahmed Luxemburg Pharmaceutical Co Ltd
Original Assignee
Novartis AG
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Application filed by Novartis AG filed Critical Novartis AG
Publication of CN1261365A publication Critical patent/CN1261365A/zh
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    • 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
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C30—CRYSTAL GROWTH
    • C30B—SINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B7/00—Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Materials Engineering (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Metallurgy (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CNB988064677A 1997-06-30 1998-06-26 结晶性大环内酯及其制备方法 Expired - Lifetime CN1139595C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9713730.1A GB9713730D0 (en) 1997-06-30 1997-06-30 Organic compounds
GB9713730.1 1997-06-30

Publications (2)

Publication Number Publication Date
CN1261365A CN1261365A (zh) 2000-07-26
CN1139595C true CN1139595C (zh) 2004-02-25

Family

ID=10815103

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB988064677A Expired - Lifetime CN1139595C (zh) 1997-06-30 1998-06-26 结晶性大环内酯及其制备方法

Country Status (31)

Country Link
US (1) US6423722B1 (https=)
EP (1) EP0994880B1 (https=)
JP (2) JP3880634B2 (https=)
KR (1) KR100399765B1 (https=)
CN (1) CN1139595C (https=)
AR (1) AR017754A1 (https=)
AT (1) ATE287410T1 (https=)
AU (1) AU739211B2 (https=)
BR (1) BR9810956A (https=)
CA (1) CA2290412C (https=)
CO (1) CO4940463A1 (https=)
CZ (1) CZ297244B6 (https=)
DE (1) DE69828692T2 (https=)
DK (1) DK0994880T3 (https=)
ES (1) ES2236922T3 (https=)
GB (1) GB9713730D0 (https=)
HU (1) HU227755B1 (https=)
ID (1) ID24897A (https=)
IL (1) IL132761A0 (https=)
MY (1) MY118718A (https=)
NO (1) NO312765B1 (https=)
NZ (1) NZ500994A (https=)
PE (1) PE97699A1 (https=)
PL (1) PL192761B1 (https=)
PT (1) PT994880E (https=)
RU (1) RU2219181C2 (https=)
SK (1) SK285665B6 (https=)
TR (1) TR199903189T2 (https=)
TW (1) TW552264B (https=)
WO (1) WO1999001458A1 (https=)
ZA (1) ZA985655B (https=)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9713730D0 (en) * 1997-06-30 1997-09-03 Ciba Geigy Ag Organic compounds
GB9826656D0 (en) 1998-12-03 1999-01-27 Novartis Ag Organic compounds
GB0125443D0 (en) * 2001-10-23 2001-12-12 Novartis Ag Organic Compounds
US7645876B2 (en) * 2004-12-01 2010-01-12 TEVA Gyógyszergyár Zártkörúen Müködö Részvénytársaság Processes for producing crystalline macrolides
JP5460947B2 (ja) * 2003-09-03 2014-04-02 グラクソ グループ リミテッド 新規調製方法、塩、組成物及び使用
ES2389443T3 (es) * 2004-04-08 2012-10-26 Meda Pharma S.À.R.L. Composición de espuma de pimecrolimus que contiene hexilenglicol, opcionalmente alcohol de oleílo, dimetilisosorbida y/o triglicéridos de cadena media
CA2668134A1 (en) * 2006-11-06 2008-05-15 Teva Gyogyszergyar Zartkoerueen Muekoedoe Reszvenytarsasag Ascomycin and pimecrolimus having reduced levels of des-methylascomycin and 32-deoxy-32-epichloro-desmethylascomycin respectively, and methods for preparation thereof
JP2010512333A (ja) * 2006-12-07 2010-04-22 ヘルシン ヘルスケア ソシエテ アノニム 塩酸パロノセトロンの結晶及び非晶質形
US9192697B2 (en) 2007-07-03 2015-11-24 Hemoteq Ag Balloon catheter for treating stenosis of body passages and for preventing threatening restenosis
ES2550634T3 (es) 2009-07-10 2015-11-11 Boston Scientific Scimed, Inc. Uso de nanocristales para un balón de suministro de fármaco
EP2453938B1 (en) 2009-07-17 2015-08-19 Boston Scientific Scimed, Inc. Nucleation of drug delivery balloons to provide improved crystal size and density
US8889211B2 (en) 2010-09-02 2014-11-18 Boston Scientific Scimed, Inc. Coating process for drug delivery balloons using heat-induced rewrap memory
WO2013022458A1 (en) * 2011-08-05 2013-02-14 Boston Scientific Scimed, Inc. Methods of converting amorphous drug substance into crystalline form
WO2013028208A1 (en) 2011-08-25 2013-02-28 Boston Scientific Scimed, Inc. Medical device with crystalline drug coating
ES2897473T3 (es) 2013-03-15 2022-03-01 Biosensors Int Group Ltd Purificación de derivados de la rapamicina
EP3178824A1 (en) 2015-12-08 2017-06-14 Medichem, S.A. Process for preparing pimecrolimus
PL3619215T3 (pl) * 2017-05-01 2022-03-21 Meda Pharma Gmbh & Co. Kg Sposób przekształcania surowej askomycyny w oczyszczony pimecrolimus
EP3741367A1 (en) 2019-05-21 2020-11-25 Premark Pharma GmbH Treatment of ocular disease
WO2024209038A1 (en) 2023-04-06 2024-10-10 Premark Pharma Gmbh Use of pimecrolimus for the treatment of dry eye in patients characterized by a corneal staining score of 4 or 5 on the oxford grading scale

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4127647A (en) * 1975-04-08 1978-11-28 Meiji Seika Kaisha, Ltd. Process for preparation of stable amorphous macrolide antibiotic solids
JPS51118816A (en) * 1975-04-08 1976-10-19 Meiji Seika Kaisha Ltd A process for stabilizing non-crystalloidal solid
GB2084580B (en) 1980-10-01 1984-07-04 Glaxo Group Ltd Aminoalkyl furan derivative
JP2728482B2 (ja) * 1989-01-26 1998-03-18 協和醗酵工業株式会社 マクロライド系抗生物質の精製法
ES2023560A6 (es) 1989-07-10 1992-01-16 Gema Sa Procedimiento para la produccion de hidrato de cefradina y solvato de cefradina y dimetilformamida.
DK0427680T3 (da) * 1989-11-09 1995-12-18 Sandoz Ltd Heteroatom-holdige cykliske forbindelser
EP0594600A1 (en) * 1990-03-13 1994-05-04 FISONS plc Immunosuppressive macrocyclic compounds
EP0480623A1 (en) * 1990-10-11 1992-04-15 Merck & Co. Inc. New halomacrolides and derivatives having immunosuppressive activity
US5143918A (en) * 1990-10-11 1992-09-01 Merck & Co., Inc. Halomacrolides and derivatives having immunosuppressive activity
DE10199058I2 (de) 1991-07-30 2006-04-27 Alcm Co Kristalle von N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanin und Verfahren zu ihrer Herstellung
US5247076A (en) 1991-09-09 1993-09-21 Merck & Co., Inc. Imidazolidyl macrolides having immunosuppressive activity
US5221740A (en) 1992-01-16 1993-06-22 American Home Products Corporation Oxepane isomers of rapamycin useful as immunosuppressive agents
UA41884C2 (uk) * 1993-11-05 2001-10-15 Амерікан Хоум Продактс Корпорейшн Спосіб відокремлення рапаміцину від кислотних, основних та неполярних нейтральних домішок, присутніх в концентраті екстрактів ферментаційного бульйону або маточних розчинів
JP3808500B2 (ja) * 1994-02-22 2006-08-09 キューレータズ オブ ディ ユニバーシティ オブ ミズーリ 分離剤としての大環状抗生物質
CA2229718A1 (en) * 1995-08-24 1997-03-06 David J. Mathre Process for the preparation of imidazolyl macrolide immunosuppressants
GB9713730D0 (en) * 1997-06-30 1997-09-03 Ciba Geigy Ag Organic compounds

Also Published As

Publication number Publication date
CA2290412C (en) 2009-11-10
JP2001506279A (ja) 2001-05-15
KR100399765B1 (ko) 2003-09-29
HK1028597A1 (en) 2001-02-23
IL132761A0 (en) 2001-03-19
EP0994880B1 (en) 2005-01-19
JP2006151999A (ja) 2006-06-15
CZ297244B6 (cs) 2006-10-11
KR20010020423A (ko) 2001-03-15
CA2290412A1 (en) 1999-01-14
AU739211B2 (en) 2001-10-04
CN1261365A (zh) 2000-07-26
DE69828692D1 (de) 2005-02-24
DK0994880T3 (da) 2005-05-30
PL192761B1 (pl) 2006-12-29
GB9713730D0 (en) 1997-09-03
ATE287410T1 (de) 2005-02-15
ZA985655B (en) 1998-12-30
AR017754A1 (es) 2001-10-24
EP0994880A1 (en) 2000-04-26
HUP0003053A3 (en) 2003-03-28
HU227755B1 (en) 2012-02-28
US6423722B1 (en) 2002-07-23
CZ474099A3 (cs) 2000-04-12
CO4940463A1 (es) 2000-07-24
JP3880634B2 (ja) 2007-02-14
DE69828692T2 (de) 2006-01-12
NO995909L (no) 1999-12-02
NZ500994A (en) 2001-08-31
PL336719A1 (en) 2000-07-03
RU2219181C2 (ru) 2003-12-20
NO312765B1 (no) 2002-07-01
ID24897A (id) 2000-08-31
HUP0003053A2 (hu) 2001-02-28
BR9810956A (pt) 2000-09-26
SK186699A3 (en) 2000-05-16
TR199903189T2 (xx) 2000-06-21
TW552264B (en) 2003-09-11
MY118718A (en) 2005-01-31
NO995909D0 (no) 1999-12-02
AU8540998A (en) 1999-01-25
ES2236922T3 (es) 2005-07-16
SK285665B6 (sk) 2007-05-03
WO1999001458A1 (en) 1999-01-14
PE97699A1 (es) 1999-10-29
PT994880E (pt) 2005-06-30
JP4504323B2 (ja) 2010-07-14

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Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
ASS Succession or assignment of patent right

Owner name: MED PHARMACEUTICAL LUXEMBOURG CO., LTD.

Free format text: FORMER OWNER: NOVARTIS AG

Effective date: 20130814

C41 Transfer of patent application or patent right or utility model
TR01 Transfer of patent right

Effective date of registration: 20130814

Address after: Luxemburg Luxemburg

Patentee after: Ahmed Luxemburg Pharmaceutical Co. Ltd.

Address before: Basel

Patentee before: Novartis AG

CX01 Expiry of patent term
CX01 Expiry of patent term

Granted publication date: 20040225