CA2290412C - Crystalline macrolides and process for their preparation - Google Patents

Crystalline macrolides and process for their preparation Download PDF

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Publication number
CA2290412C
CA2290412C CA002290412A CA2290412A CA2290412C CA 2290412 C CA2290412 C CA 2290412C CA 002290412 A CA002290412 A CA 002290412A CA 2290412 A CA2290412 A CA 2290412A CA 2290412 C CA2290412 C CA 2290412C
Authority
CA
Canada
Prior art keywords
compound
solution
formula
crystalline
crystallization
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
CA002290412A
Other languages
English (en)
French (fr)
Other versions
CA2290412A1 (en
Inventor
Cornelia Dosenbach
Maximilian 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
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=CA2290412(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 CA2290412A1 publication Critical patent/CA2290412A1/en
Application granted granted Critical
Publication of CA2290412C publication Critical patent/CA2290412C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

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)
  • 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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA002290412A 1997-06-30 1998-06-26 Crystalline macrolides and process for their preparation Expired - Lifetime CA2290412C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9713730.1A GB9713730D0 (en) 1997-06-30 1997-06-30 Organic compounds
GB9713730.1 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
CA2290412A1 CA2290412A1 (en) 1999-01-14
CA2290412C true CA2290412C (en) 2009-11-10

Family

ID=10815103

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002290412A Expired - Lifetime CA2290412C (en) 1997-06-30 1998-06-26 Crystalline macrolides and process for their preparation

Country Status (31)

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

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
US7875630B2 (en) * 2003-09-03 2011-01-25 Glaxo Group Limited Process salts compositions and use
AU2005230401B2 (en) * 2004-04-08 2008-11-27 Meda Pharma S.A.R.L. Pimecrolimus foam composition containing hexylene glycol, optionally oleyl alcohol, dimethylisosorbide and/or medium chain triglycerides
TW200628483A (en) 2004-12-01 2006-08-16 Teva Gyogyszergyar Zartkoruen Mukodo Reszvenytarsasag Processes for producing crystalline macrolides
EP1960406A2 (en) * 2006-11-06 2008-08-27 TEVA Gyógyszergyár Zártkörüen Müködö Részvénytársaság Ascomycin and pimecrolimus having reduced levels of desmethylascomycin and 32-deoxy-32-epichloro-desmethylascomycin respectively, and methods for preparation thereof
EP2099298A4 (en) * 2006-12-07 2010-01-06 Helsinn Healthcare Sa CRYSTALLINE AND AMORPHOUS FORMS OF PALONOSETRON HYDROCHLORIDE
US9192697B2 (en) 2007-07-03 2015-11-24 Hemoteq Ag Balloon catheter for treating stenosis of body passages and for preventing threatening restenosis
EP2451496B1 (en) 2009-07-10 2015-07-22 Boston Scientific Scimed, Inc. Use of nanocrystals for a drug delivery balloon
WO2011008393A2 (en) 2009-07-17 2011-01-20 Boston Scientific Scimed, Inc. Nucleation of drug delivery balloons to provide improved crystal size and density
WO2012031236A1 (en) 2010-09-02 2012-03-08 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
US9056152B2 (en) 2011-08-25 2015-06-16 Boston Scientific Scimed, Inc. Medical device with crystalline drug coating
SG10202112135VA (en) 2013-03-15 2021-12-30 Biosensors International Group Ltd Purification of rapamycin derivatives
EP3178824A1 (en) 2015-12-08 2017-06-14 Medichem, S.A. Process for preparing pimecrolimus
WO2018202733A1 (en) * 2017-05-01 2018-11-08 Meda Pharma Gmbh & Co. Kg Process to convert crude ascomycin into purified 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
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
IE910847A1 (en) * 1990-03-13 1991-09-25 Fisons Plc Immunosuppressive macrocyclic compounds
US5143918A (en) * 1990-10-11 1992-09-01 Merck & Co., Inc. Halomacrolides and derivatives having immunosuppressive activity
EP0480623A1 (en) * 1990-10-11 1992-04-15 Merck & Co. Inc. New 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
WO1997008182A1 (en) * 1995-08-24 1997-03-06 Merck & Co., Inc. 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
EP0994880A1 (en) 2000-04-26
HUP0003053A3 (en) 2003-03-28
US6423722B1 (en) 2002-07-23
JP2006151999A (ja) 2006-06-15
CZ297244B6 (cs) 2006-10-11
AR017754A1 (es) 2001-10-24
GB9713730D0 (en) 1997-09-03
PE97699A1 (es) 1999-10-29
PL192761B1 (pl) 2006-12-29
RU2219181C2 (ru) 2003-12-20
ATE287410T1 (de) 2005-02-15
IL132761A0 (en) 2001-03-19
EP0994880B1 (en) 2005-01-19
ID24897A (id) 2000-08-31
PT994880E (pt) 2005-06-30
CN1261365A (zh) 2000-07-26
KR20010020423A (ko) 2001-03-15
AU739211B2 (en) 2001-10-04
CO4940463A1 (es) 2000-07-24
CA2290412A1 (en) 1999-01-14
ZA985655B (en) 1998-12-30
SK285665B6 (sk) 2007-05-03
HK1028597A1 (en) 2001-02-23
DE69828692D1 (de) 2005-02-24
CN1139595C (zh) 2004-02-25
BR9810956A (pt) 2000-09-26
JP3880634B2 (ja) 2007-02-14
JP2001506279A (ja) 2001-05-15
DK0994880T3 (da) 2005-05-30
SK186699A3 (en) 2000-05-16
CZ474099A3 (cs) 2000-04-12
JP4504323B2 (ja) 2010-07-14
TR199903189T2 (xx) 2000-06-21
NO312765B1 (no) 2002-07-01
AU8540998A (en) 1999-01-25
NZ500994A (en) 2001-08-31
PL336719A1 (en) 2000-07-03
WO1999001458A1 (en) 1999-01-14
KR100399765B1 (ko) 2003-09-29
NO995909D0 (no) 1999-12-02
ES2236922T3 (es) 2005-07-16
HU227755B1 (en) 2012-02-28
HUP0003053A2 (hu) 2001-02-28
TW552264B (en) 2003-09-11
MY118718A (en) 2005-01-31
DE69828692T2 (de) 2006-01-12
NO995909L (no) 1999-12-02

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EEER Examination request
MKEX Expiry

Effective date: 20180626