TW552264B - Macrolide crystallines, process for preparation thereof and pharmaceutical composition comprising same - Google Patents

Macrolide crystallines, process for preparation thereof and pharmaceutical composition comprising same Download PDF

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Publication number
TW552264B
TW552264B TW087111867A TW87111867A TW552264B TW 552264 B TW552264 B TW 552264B TW 087111867 A TW087111867 A TW 087111867A TW 87111867 A TW87111867 A TW 87111867A TW 552264 B TW552264 B TW 552264B
Authority
TW
Taiwan
Prior art keywords
compound
formula
amorphous
crystallization
crystalline
Prior art date
Application number
TW087111867A
Other languages
English (en)
Chinese (zh)
Inventor
Cornelia Dosenbach
Maximilian Grassberger
Otto Hartmann
Amarylia Horvath
Jean-Paul Mutz
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=10815103&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TW552264(B) "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
Application granted granted Critical
Publication of TW552264B publication Critical patent/TW552264B/zh

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C30CRYSTAL GROWTH
    • C30BSINGLE-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
    • C30B7/00Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions

Landscapes

  • 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)
TW087111867A 1997-06-30 1998-07-21 Macrolide crystallines, process for preparation thereof and pharmaceutical composition comprising same TW552264B (en)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
TW552264B true TW552264B (en) 2003-09-11

Family

ID=10815103

Family Applications (1)

Application Number Title Priority Date Filing Date
TW087111867A TW552264B (en) 1997-06-30 1998-07-21 Macrolide crystallines, process for preparation thereof and pharmaceutical composition comprising same

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
CN1139595C (zh) 2004-02-25
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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