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
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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)
  • 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)
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 (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
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
CA2290412C (en) 2009-11-10

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Legal Events

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