KR100399765B1 - 결정형 마크로리드 및 이들의 제조방법 - Google Patents

결정형 마크로리드 및 이들의 제조방법 Download PDF

Info

Publication number
KR100399765B1
KR100399765B1 KR10-1999-7010048A KR19997010048A KR100399765B1 KR 100399765 B1 KR100399765 B1 KR 100399765B1 KR 19997010048 A KR19997010048 A KR 19997010048A KR 100399765 B1 KR100399765 B1 KR 100399765B1
Authority
KR
South Korea
Prior art keywords
compound
formula
crystalline
ethanol
solubility
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
KR10-1999-7010048A
Other languages
English (en)
Korean (ko)
Other versions
KR20010020423A (ko
Inventor
코넬리아 도젠바흐
맥시밀리안 그라스베르거
오토 하르트만
아마릴라 호르바쓰
쟝-뽈 무츠
게르하르트 펜
사빈 페퍼
디르크 비크후젠
Original Assignee
노파르티스 아게
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=KR100399765(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 노파르티스 아게 filed Critical 노파르티스 아게
Publication of KR20010020423A publication Critical patent/KR20010020423A/ko
Application granted granted Critical
Publication of KR100399765B1 publication Critical patent/KR100399765B1/ko
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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)
  • 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)
KR10-1999-7010048A 1997-06-30 1998-06-26 결정형 마크로리드 및 이들의 제조방법 Expired - Lifetime KR100399765B1 (ko)

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
KR20010020423A KR20010020423A (ko) 2001-03-15
KR100399765B1 true KR100399765B1 (ko) 2003-09-29

Family

ID=10815103

Family Applications (1)

Application Number Title Priority Date Filing Date
KR10-1999-7010048A Expired - Lifetime KR100399765B1 (ko) 1997-06-30 1998-06-26 결정형 마크로리드 및 이들의 제조방법

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
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

Similar Documents

Publication Publication Date Title
KR100399765B1 (ko) 결정형 마크로리드 및 이들의 제조방법
KR100353783B1 (ko) 마그네슘오메프라졸
CN104059072B (zh) 短效苯并二氮杂*盐及其多晶型
JP2025169363A (ja) ７ｈ－ベンゾ［７］アヌレン－２－カルボン酸誘導体の結晶形態
US20230357322A1 (en) Method of manufacturing a pharmaceutical composition
JP4655930B2 (ja) キノリンカルボン酸誘導体溶媒和物の結晶
RU2830121C2 (ru) Способ получения фармацевтической композиции
HK1028597B (en) Crystalline macrolides and process for their preparation
MXPA99011294A (es) Macrolidos cristalinos y proceso para su preparacion
BR122025018455A2 (pt) Formas sólidas de um composto inibidor de cyp11a1 estruturado com 4h-piran-4-ona, métodos para preparar as mesmas, forma de dosagem farmacêutica e uso das referidas formas sólidas para o tratamento de cânceres hormonalmente regulados
WO2025040026A1 (zh) 一种alk抑制剂的结晶形态
US20080249035A1 (en) Polymorph of Clarithromycin (Form V)
PL195879B1 (pl) Sposób wytwarzania krystalicznego dihydratu azytromycyny

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 19991029

Patent event code: PA01051R01D

Comment text: International Patent Application

A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20000925

Comment text: Request for Examination of Application

PG1501 Laying open of application
E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20021031

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20030619

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20030917

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20030918

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
PR1001 Payment of annual fee

Payment date: 20060908

Start annual number: 4

End annual number: 4

PR1001 Payment of annual fee

Payment date: 20070906

Start annual number: 5

End annual number: 5

PR1001 Payment of annual fee

Payment date: 20080911

Start annual number: 6

End annual number: 6

PR1001 Payment of annual fee

Payment date: 20090910

Start annual number: 7

End annual number: 7

PR1001 Payment of annual fee

Payment date: 20100910

Start annual number: 8

End annual number: 8

PR1001 Payment of annual fee

Payment date: 20110811

Start annual number: 9

End annual number: 9

FPAY Annual fee payment

Payment date: 20120910

Year of fee payment: 10

PR1001 Payment of annual fee

Payment date: 20120910

Start annual number: 10

End annual number: 10

FPAY Annual fee payment

Payment date: 20130905

Year of fee payment: 11

PR1001 Payment of annual fee

Payment date: 20130905

Start annual number: 11

End annual number: 11

FPAY Annual fee payment

Payment date: 20140904

Year of fee payment: 12

PR1001 Payment of annual fee

Payment date: 20140904

Start annual number: 12

End annual number: 12

FPAY Annual fee payment

Payment date: 20150903

Year of fee payment: 13

PR1001 Payment of annual fee

Payment date: 20150903

Start annual number: 13

End annual number: 13

FPAY Annual fee payment

Payment date: 20160908

Year of fee payment: 14

PR1001 Payment of annual fee

Payment date: 20160908

Start annual number: 14

End annual number: 14

FPAY Annual fee payment

Payment date: 20170807

Year of fee payment: 15

PR1001 Payment of annual fee

Payment date: 20170807

Start annual number: 15

End annual number: 15

EXPY Expiration of term
PC1801 Expiration of term

Termination date: 20181226

Termination category: Expiration of duration