BR9810956A - "macrolidas cristalinas e processo para sua preparação" - Google Patents

"macrolidas cristalinas e processo para sua preparação"

Info

Publication number
BR9810956A
BR9810956A BR9810956-1A BR9810956A BR9810956A BR 9810956 A BR9810956 A BR 9810956A BR 9810956 A BR9810956 A BR 9810956A BR 9810956 A BR9810956 A BR 9810956A
Authority
BR
Brazil
Prior art keywords
compound
preparation
formula
crystalline
macrolides
Prior art date
Application number
BR9810956-1A
Other languages
English (en)
Inventor
Cornelia Dosenbach
Maximilian Grassberger
Otto Hartmann
Amarylla Horvath
Jean-Paul Mutz
Gerhard Penn
Sabine Pfeffer
Dierk Wiechhusen
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=BR9810956(A) "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 BR9810956A publication Critical patent/BR9810956A/pt

Links

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)
  • 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)

Abstract

Patente de Invenção: <B>"MACROLIDAS CRISTALINAS E PROCESSO PARA SUA PREPARAçãO"<D>. Esta invenção refere-se a 33-epicloro-33-desoxiascomicina de fórmula I e a várias formas tautoméricas ou solvatadas da mesma, em forma cristalina, tais como Forma A e Forma B. Sua preparação envolve converter apropriadamente composto amorfo de fórmula I, ou composto de fórmula I em apenas Forma A, ou composto de fórmula I em apenas Forma B, respectivamente, a partir de uma solução do composto, sob condições indutoras de cristalização ou condições que induzem cristalização preferencial de Forma A ou B, respectivamente. Tais cristais são particularmente indicados para uso na preparação de formas galênicas tópicas do composto para uso farmacêutico, por exemplo cremes, emulsões e ung³entos.
BR9810956-1A 1997-06-30 1998-06-26 "macrolidas cristalinas e processo para sua preparação" BR9810956A (pt)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
BR9810956A true BR9810956A (pt) 2000-09-26

Family

ID=10815103

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9810956-1A BR9810956A (pt) 1997-06-30 1998-06-26 "macrolidas cristalinas e processo para sua preparação"

Country Status (32)

Country Link
US (1) US6423722B1 (pt)
EP (1) EP0994880B1 (pt)
JP (2) JP3880634B2 (pt)
KR (1) KR100399765B1 (pt)
CN (1) CN1139595C (pt)
AR (1) AR017754A1 (pt)
AT (1) ATE287410T1 (pt)
AU (1) AU739211B2 (pt)
BR (1) BR9810956A (pt)
CA (1) CA2290412C (pt)
CO (1) CO4940463A1 (pt)
CZ (1) CZ297244B6 (pt)
DE (1) DE69828692T2 (pt)
DK (1) DK0994880T3 (pt)
ES (1) ES2236922T3 (pt)
GB (1) GB9713730D0 (pt)
HK (1) HK1028597A1 (pt)
HU (1) HU227755B1 (pt)
ID (1) ID24897A (pt)
IL (1) IL132761A0 (pt)
MY (1) MY118718A (pt)
NO (1) NO312765B1 (pt)
NZ (1) NZ500994A (pt)
PE (1) PE97699A1 (pt)
PL (1) PL192761B1 (pt)
PT (1) PT994880E (pt)
RU (1) RU2219181C2 (pt)
SK (1) SK285665B6 (pt)
TR (1) TR199903189T2 (pt)
TW (1) TW552264B (pt)
WO (1) WO1999001458A1 (pt)
ZA (1) ZA985655B (pt)

Families Citing this family (18)

* 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
EP1817314A1 (en) * 2004-12-01 2007-08-15 Teva Gyógyszergyár Zártköruen Muködo Részvenytarsaság Non-hygroscopic and powdery amorphous pimecrolimus
WO2008057511A2 (en) * 2006-11-06 2008-05-15 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
WO2008073757A1 (en) * 2006-12-07 2008-06-19 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
ES2550634T3 (es) 2009-07-10 2015-11-11 Boston Scientific Scimed, Inc. Uso de nanocristales para un balón de suministro de fármaco
US10080821B2 (en) 2009-07-17 2018-09-25 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
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
CA3060330A1 (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
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
WO1991000865A1 (en) 1989-07-10 1991-01-24 Gema S.A. A novel stable form of cephradine, process for its production and intermediates used therein
NZ235991A (en) * 1989-11-09 1993-05-26 Sandoz Ltd Macrolide compounds and pharmaceutical compositions thereof
JPH05505798A (ja) * 1990-03-13 1993-08-26 フアイソンズ・ピーエルシー 免疫抑制マクロ環状化合物
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
US5626757A (en) * 1994-02-22 1997-05-06 Advanced Separation Technologies Inc. Macrocyclic antibiotics as separation agents
AU6900596A (en) * 1995-08-24 1997-03-19 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
SK285665B6 (sk) 2007-05-03
US6423722B1 (en) 2002-07-23
DK0994880T3 (da) 2005-05-30
GB9713730D0 (en) 1997-09-03
IL132761A0 (en) 2001-03-19
HUP0003053A2 (hu) 2001-02-28
CZ474099A3 (cs) 2000-04-12
CZ297244B6 (cs) 2006-10-11
JP4504323B2 (ja) 2010-07-14
PT994880E (pt) 2005-06-30
JP3880634B2 (ja) 2007-02-14
DE69828692T2 (de) 2006-01-12
TR199903189T2 (xx) 2000-06-21
AR017754A1 (es) 2001-10-24
ZA985655B (en) 1998-12-30
NO995909D0 (no) 1999-12-02
JP2006151999A (ja) 2006-06-15
KR20010020423A (ko) 2001-03-15
CA2290412A1 (en) 1999-01-14
PE97699A1 (es) 1999-10-29
TW552264B (en) 2003-09-11
AU8540998A (en) 1999-01-25
ID24897A (id) 2000-08-31
PL336719A1 (en) 2000-07-03
WO1999001458A1 (en) 1999-01-14
RU2219181C2 (ru) 2003-12-20
HK1028597A1 (en) 2001-02-23
NZ500994A (en) 2001-08-31
MY118718A (en) 2005-01-31
EP0994880B1 (en) 2005-01-19
JP2001506279A (ja) 2001-05-15
AU739211B2 (en) 2001-10-04
ATE287410T1 (de) 2005-02-15
HU227755B1 (en) 2012-02-28
NO995909L (no) 1999-12-02
PL192761B1 (pl) 2006-12-29
SK186699A3 (en) 2000-05-16
DE69828692D1 (de) 2005-02-24
CN1261365A (zh) 2000-07-26
KR100399765B1 (ko) 2003-09-29
CO4940463A1 (es) 2000-07-24
CA2290412C (en) 2009-11-10
NO312765B1 (no) 2002-07-01
ES2236922T3 (es) 2005-07-16
EP0994880A1 (en) 2000-04-26
HUP0003053A3 (en) 2003-03-28
CN1139595C (zh) 2004-02-25

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Legal Events

Date Code Title Description
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: ALTERADA DE INT.CL: C07D 498/18, A61K 31/36, A61K 31/4353, A61K 31/695, A61P 29/00, A61P 37/00

Ipc: C07D 498/18 (2008.04), A61K 31/36 (2008.04), A61K

B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: INDEFERIMENTO DO PRESENTE PEDIDO DE PATENTE, POR NAO ESTA DE ACORDO COM OS ARTIGOS 8O, 11,13, 24 E25 DA LPI

B12B Appeal against refusal [chapter 12.2 patent gazette]