AU739211B2 - Crystalline macrolides and process for their preparation - Google Patents

Crystalline macrolides and process for their preparation Download PDF

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Publication number
AU739211B2
AU739211B2 AU85409/98A AU8540998A AU739211B2 AU 739211 B2 AU739211 B2 AU 739211B2 AU 85409/98 A AU85409/98 A AU 85409/98A AU 8540998 A AU8540998 A AU 8540998A AU 739211 B2 AU739211 B2 AU 739211B2
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AU
Australia
Prior art keywords
compound
crystalline
compound according
formula
solution
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
Application number
AU85409/98A
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English (en)
Other versions
AU8540998A (en
Inventor
Cornelia Dosenbach
Maximillian Grassberger
Otto Hartmann
Amarylla Horvath
Jean-Paul Mutz
Gerhard Penn
Sabine Pfeffer
Dierk Wieckhusen
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.)
Meda Pharma SARL
Original Assignee
Novartis AG
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Filing date
Publication date
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Application filed by Novartis AG filed Critical Novartis AG
Publication of AU8540998A publication Critical patent/AU8540998A/en
Application granted granted Critical
Publication of AU739211B2 publication Critical patent/AU739211B2/en
Assigned to MEDA Pharma S.a.r.l reassignment MEDA Pharma S.a.r.l Alteration of Name(s) in Register under S187 Assignors: NOVARTIS AG
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

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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

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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)
AU85409/98A 1997-06-30 1998-06-26 Crystalline macrolides and process for their preparation Expired AU739211B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9713730.1A GB9713730D0 (en) 1997-06-30 1997-06-30 Organic compounds
GB9713730 1997-06-30
PCT/EP1998/003929 WO1999001458A1 (en) 1997-06-30 1998-06-26 Crystalline macrolides and process for their preparation

Publications (2)

Publication Number Publication Date
AU8540998A AU8540998A (en) 1999-01-25
AU739211B2 true AU739211B2 (en) 2001-10-04

Family

ID=10815103

Family Applications (1)

Application Number Title Priority Date Filing Date
AU85409/98A Expired AU739211B2 (en) 1997-06-30 1998-06-26 Crystalline macrolides and process for their preparation

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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0427680A1 (en) * 1989-11-09 1991-05-15 Sandoz Ltd. Heteroatoms-containing tricyclic compounds
EP0480623A1 (en) * 1990-10-11 1992-04-15 Merck & Co. Inc. New halomacrolides and derivatives having immunosuppressive activity
WO1997008182A1 (en) * 1995-08-24 1997-03-06 Merck & Co., Inc. Process for the preparation of imidazolyl macrolide immunosuppressants

Family Cites Families (13)

* 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.
EP0594600A1 (en) * 1990-03-13 1994-05-04 FISONS plc Immunosuppressive macrocyclic compounds
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
GB9713730D0 (en) * 1997-06-30 1997-09-03 Ciba Geigy Ag Organic compounds

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0427680A1 (en) * 1989-11-09 1991-05-15 Sandoz Ltd. Heteroatoms-containing tricyclic compounds
EP0480623A1 (en) * 1990-10-11 1992-04-15 Merck & Co. Inc. New halomacrolides and derivatives having immunosuppressive activity
WO1997008182A1 (en) * 1995-08-24 1997-03-06 Merck & Co., Inc. Process for the preparation of imidazolyl macrolide immunosuppressants

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
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
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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FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired