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

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Metallurgy (AREA)
  • Materials Engineering (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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 (2)
EP (1) EP0994880B1 (2)
JP (2) JP3880634B2 (2)
KR (1) KR100399765B1 (2)
CN (1) CN1139595C (2)
AR (1) AR017754A1 (2)
AT (1) ATE287410T1 (2)
AU (1) AU739211B2 (2)
BR (1) BR9810956A (2)
CA (1) CA2290412C (2)
CO (1) CO4940463A1 (2)
CZ (1) CZ297244B6 (2)
DE (1) DE69828692T2 (2)
DK (1) DK0994880T3 (2)
ES (1) ES2236922T3 (2)
GB (1) GB9713730D0 (2)
HU (1) HU227755B1 (2)
ID (1) ID24897A (2)
IL (1) IL132761A0 (2)
MY (1) MY118718A (2)
NO (1) NO312765B1 (2)
NZ (1) NZ500994A (2)
PE (1) PE97699A1 (2)
PL (1) PL192761B1 (2)
PT (1) PT994880E (2)
RU (1) RU2219181C2 (2)
SK (1) SK285665B6 (2)
TR (1) TR199903189T2 (2)
TW (1) TW552264B (2)
WO (1) WO1999001458A1 (2)
ZA (1) ZA985655B (2)

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
EP1663220B1 (en) * 2003-09-03 2009-12-02 Glaxo Group Limited Novel process for the preparation of pleuromutilin derivatives
PT1734927E (pt) * 2004-04-08 2012-09-05 Meda Pharma S A R L Composição em espuma de pimecrolimus contendo hexilenoglicol, opcionalmente álcool oleílico, dimetilisossorbida e/ou triglicéridos de cadeia média
CA2584430A1 (en) * 2004-12-01 2006-06-08 Teva Gyogyszergyar Zartkoruen Mukodo Reszvenytarsasag Methods for preparing pimecrolimus
TW200837067A (en) * 2006-11-06 2008-09-16 Teva Gyogyszergyar Zartkoruen Mukodo Reszvenytarsasag Ascomycin and pimecrolimus having reduced levels of desmethylascomycin 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
EP2944332B1 (en) 2009-07-10 2016-08-17 Boston Scientific Scimed, Inc. Use of nanocrystals for a drug delivery balloon
EP2453938B1 (en) 2009-07-17 2015-08-19 Boston Scientific Scimed, Inc. Nucleation of drug delivery balloons to provide improved crystal size and density
EP2611476B1 (en) 2010-09-02 2016-08-10 Boston Scientific Scimed, Inc. Coating process for drug delivery balloons using heat-induced rewrap memory
US8669360B2 (en) * 2011-08-05 2014-03-11 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
WO2014145780A1 (en) 2013-03-15 2014-09-18 Biosensors International Group, Ltd. Purification of rapamycin derivatives
EP3178824A1 (en) 2015-12-08 2017-06-14 Medichem, S.A. Process for preparing pimecrolimus
ES2906158T3 (es) * 2017-05-01 2022-04-13 Meda Pharma Gmbh & Co Kg Proceso para convertir ascomicina bruta en pimecrolimus purificado
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
JPS51118816A (en) * 1975-04-08 1976-10-19 Meiji Seika Kaisha Ltd A process for stabilizing non-crystalloidal solid
US4127647A (en) * 1975-04-08 1978-11-28 Meiji Seika Kaisha, Ltd. Process for preparation of stable amorphous macrolide antibiotic solids
CY1306A (en) 1980-10-01 1985-12-06 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
JPH089630B2 (ja) 1989-07-10 1996-01-31 ヘマ・ソシエダード・アノニマ 有機化合物の、または関連する改善
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
ES2100291T3 (es) 1991-07-30 1997-06-16 Ajinomoto Kk Cristales de n-(trans-4-isopropilciclohexilcarbonil)-d-fenilalanina y metodos para prepararlos.
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
SK186699A3 (en) 2000-05-16
CA2290412A1 (en) 1999-01-14
HU227755B1 (en) 2012-02-28
AR017754A1 (es) 2001-10-24
EP0994880B1 (en) 2005-01-19
US6423722B1 (en) 2002-07-23
IL132761A0 (en) 2001-03-19
PT994880E (pt) 2005-06-30
HK1028597A1 (en) 2001-02-23
CN1261365A (zh) 2000-07-26
CO4940463A1 (es) 2000-07-24
CZ297244B6 (cs) 2006-10-11
HUP0003053A2 (hu) 2001-02-28
JP3880634B2 (ja) 2007-02-14
CN1139595C (zh) 2004-02-25
JP2001506279A (ja) 2001-05-15
ID24897A (id) 2000-08-31
WO1999001458A1 (en) 1999-01-14
MY118718A (en) 2005-01-31
KR20010020423A (ko) 2001-03-15
NO995909L (no) 1999-12-02
PE97699A1 (es) 1999-10-29
ZA985655B (en) 1998-12-30
ATE287410T1 (de) 2005-02-15
AU739211B2 (en) 2001-10-04
TR199903189T2 (xx) 2000-06-21
PL192761B1 (pl) 2006-12-29
JP2006151999A (ja) 2006-06-15
SK285665B6 (sk) 2007-05-03
NO995909D0 (no) 1999-12-02
KR100399765B1 (ko) 2003-09-29
NZ500994A (en) 2001-08-31
DE69828692T2 (de) 2006-01-12
GB9713730D0 (en) 1997-09-03
DK0994880T3 (da) 2005-05-30
JP4504323B2 (ja) 2010-07-14
PL336719A1 (en) 2000-07-03
NO312765B1 (no) 2002-07-01
DE69828692D1 (de) 2005-02-24
EP0994880A1 (en) 2000-04-26
HUP0003053A3 (en) 2003-03-28
ES2236922T3 (es) 2005-07-16
CZ474099A3 (cs) 2000-04-12
AU8540998A (en) 1999-01-25
RU2219181C2 (ru) 2003-12-20
CA2290412C (en) 2009-11-10
BR9810956A (pt) 2000-09-26

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