RU2219181C2 - Кристаллические макролиды, способы их получения и фармацевтическая композиция на их основе - Google Patents
Кристаллические макролиды, способы их получения и фармацевтическая композиция на их основе Download PDFInfo
- Publication number
- RU2219181C2 RU2219181C2 RU2000101826/04A RU2000101826A RU2219181C2 RU 2219181 C2 RU2219181 C2 RU 2219181C2 RU 2000101826/04 A RU2000101826/04 A RU 2000101826/04A RU 2000101826 A RU2000101826 A RU 2000101826A RU 2219181 C2 RU2219181 C2 RU 2219181C2
- Authority
- RU
- Russia
- Prior art keywords
- compound
- formula
- crystalline form
- temperature
- crystalline
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims abstract 7
- 239000003120 macrolide antibiotic agent Substances 0.000 title claims abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract 3
- 229940041033 macrolides Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 14
- 230000000947 anti-immunosuppressive effect Effects 0.000 claims abstract 4
- 230000003110 anti-inflammatory effect Effects 0.000 claims abstract 4
- 230000001028 anti-proliverative effect Effects 0.000 claims abstract 4
- 239000003795 chemical substances by application Substances 0.000 claims abstract 2
- 239000012453 solvate Substances 0.000 claims abstract 2
- 239000002904 solvent Substances 0.000 claims 5
- 239000007858 starting material Substances 0.000 claims 5
- 238000006243 chemical reaction Methods 0.000 claims 3
- 238000001816 cooling Methods 0.000 claims 3
- 238000002425 crystallisation Methods 0.000 claims 3
- 230000008025 crystallization Effects 0.000 claims 3
- 238000001914 filtration Methods 0.000 claims 3
- 230000001939 inductive effect Effects 0.000 claims 3
- 239000007788 liquid Substances 0.000 claims 3
- 239000013078 crystal Substances 0.000 claims 2
- 238000002329 infrared spectrum Methods 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 abstract 1
- 229940088710 antibiotic agent Drugs 0.000 abstract 1
- 230000004071 biological effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Images
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)
- 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)
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 |
|---|---|
| RU2000101826A RU2000101826A (ru) | 2001-09-27 |
| RU2219181C2 true RU2219181C2 (ru) | 2003-12-20 |
Family
ID=10815103
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2000101826/04A RU2219181C2 (ru) | 1997-06-30 | 1998-06-26 | Кристаллические макролиды, способы их получения и фармацевтическая композиция на их основе |
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)
| 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 (2)
| 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 |
Family Cites Families (14)
| 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 |
| CA2229718A1 (en) * | 1995-08-24 | 1997-03-06 | David J. Mathre | Process for the preparation of imidazolyl macrolide immunosuppressants |
| GB9713730D0 (en) * | 1997-06-30 | 1997-09-03 | Ciba Geigy Ag | Organic compounds |
-
1997
- 1997-06-30 GB GBGB9713730.1A patent/GB9713730D0/en active Pending
-
1998
- 1998-06-25 CO CO98036359A patent/CO4940463A1/es unknown
- 1998-06-26 RU RU2000101826/04A patent/RU2219181C2/ru active
- 1998-06-26 BR BR9810956-1A patent/BR9810956A/pt not_active Application Discontinuation
- 1998-06-26 WO PCT/EP1998/003929 patent/WO1999001458A1/en not_active Ceased
- 1998-06-26 PL PL336719A patent/PL192761B1/pl unknown
- 1998-06-26 AU AU85409/98A patent/AU739211B2/en not_active Expired
- 1998-06-26 CA CA002290412A patent/CA2290412C/en not_active Expired - Lifetime
- 1998-06-26 DK DK98936392T patent/DK0994880T3/da active
- 1998-06-26 AR ARP980103094A patent/AR017754A1/es active IP Right Grant
- 1998-06-26 PT PT98936392T patent/PT994880E/pt unknown
- 1998-06-26 IL IL13276198A patent/IL132761A0/xx not_active IP Right Cessation
- 1998-06-26 ID IDW991682A patent/ID24897A/id unknown
- 1998-06-26 CN CNB988064677A patent/CN1139595C/zh not_active Expired - Lifetime
- 1998-06-26 AT AT98936392T patent/ATE287410T1/de active
- 1998-06-26 CZ CZ0474099A patent/CZ297244B6/cs not_active IP Right Cessation
- 1998-06-26 NZ NZ500994A patent/NZ500994A/en not_active IP Right Cessation
- 1998-06-26 SK SK1866-99A patent/SK285665B6/sk not_active IP Right Cessation
- 1998-06-26 JP JP50628799A patent/JP3880634B2/ja not_active Expired - Lifetime
- 1998-06-26 KR KR10-1999-7010048A patent/KR100399765B1/ko not_active Expired - Lifetime
- 1998-06-26 DE DE69828692T patent/DE69828692T2/de not_active Expired - Lifetime
- 1998-06-26 PE PE1998000568A patent/PE97699A1/es not_active IP Right Cessation
- 1998-06-26 ES ES98936392T patent/ES2236922T3/es not_active Expired - Lifetime
- 1998-06-26 HU HU0003053A patent/HU227755B1/hu unknown
- 1998-06-26 TR TR1999/03189T patent/TR199903189T2/xx unknown
- 1998-06-26 EP EP98936392A patent/EP0994880B1/en not_active Expired - Lifetime
- 1998-06-29 MY MYPI98002955A patent/MY118718A/en unknown
- 1998-06-29 ZA ZA985655A patent/ZA985655B/xx unknown
- 1998-07-21 TW TW087111867A patent/TW552264B/zh not_active IP Right Cessation
-
1999
- 1999-12-02 NO NO19995909A patent/NO312765B1/no not_active IP Right Cessation
-
2000
- 2000-10-17 US US09/690,404 patent/US6423722B1/en not_active Expired - Lifetime
-
2006
- 2006-03-01 JP JP2006055107A patent/JP4504323B2/ja not_active Expired - Lifetime
Patent Citations (2)
| 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 |
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| Date | Code | Title | Description |
|---|---|---|---|
| PC41 | Official registration of the transfer of exclusive right |
Effective date: 20131029 |