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 (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)
| 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 |
| ATE450535T1 (de) * | 2003-09-03 | 2009-12-15 | Glaxo Group Ltd | Neues verfahren zur herstellung von pleuromutilinderivaten |
| SI1734927T1 (sl) * | 2004-04-08 | 2012-09-28 | Meda Pharma S A R L | Pimekrolimusni penjen sestavek, ki vsebuje heksilenglikol, po izbiri oleil alkohol, dimetilizosorbid in/ali srednjeveriĹľne trigliceride |
| DE602005021684D1 (de) * | 2004-12-01 | 2010-07-15 | Teva Gyogyszergyar Zartkoeruen | Verfahren zur herstellung von pimecrolimus |
| 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 |
| 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 |
| EP3064230B1 (en) | 2009-07-10 | 2019-04-10 | Boston Scientific Scimed, Inc. | Use of nanocrystals for a drug delivery balloon |
| JP5933434B2 (ja) | 2009-07-17 | 2016-06-08 | ボストン サイエンティフィック サイムド,インコーポレイテッドBoston Scientific Scimed,Inc. | 薬剤送達バルーンの製造方法 |
| 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 |
| CN105102967B (zh) * | 2013-03-15 | 2018-10-12 | 生物传感器国际集团有限公司 | 雷帕霉素衍生物的纯化 |
| EP3178824A1 (en) | 2015-12-08 | 2017-06-14 | Medichem, S.A. | Process for preparing pimecrolimus |
| KR102592374B1 (ko) * | 2017-05-01 | 2023-10-25 | 메다 파마 게엠베하 운트 코. 카게 | 조질의 아스코마이신을 정제된 피메크롤리무스로 전환하는 방법 |
| 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 |
|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| WO1995022390A1 (en) * | 1994-02-22 | 1995-08-24 | Curators Of The University Of Missouri | Macrocyclic antibiotics as separation agents |
| EP0848717A1 (en) * | 1995-08-24 | 1998-06-24 | Merck & Co., Inc. | 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 EP EP98936392A patent/EP0994880B1/en not_active Expired - Lifetime
- 1998-06-26 RU RU2000101826/04A patent/RU2219181C2/ru active
- 1998-06-26 CN CNB988064677A patent/CN1139595C/zh not_active Expired - Lifetime
- 1998-06-26 DK DK98936392T patent/DK0994880T3/da active
- 1998-06-26 PE PE1998000568A patent/PE97699A1/es not_active IP Right Cessation
- 1998-06-26 SK SK1866-99A patent/SK285665B6/sk not_active IP Right Cessation
- 1998-06-26 CA CA002290412A patent/CA2290412C/en not_active Expired - Lifetime
- 1998-06-26 TR TR1999/03189T patent/TR199903189T2/xx unknown
- 1998-06-26 ID IDW991682A patent/ID24897A/id unknown
- 1998-06-26 CZ CZ0474099A patent/CZ297244B6/cs not_active IP Right Cessation
- 1998-06-26 PT PT98936392T patent/PT994880E/pt unknown
- 1998-06-26 NZ NZ500994A patent/NZ500994A/en not_active IP Right Cessation
- 1998-06-26 IL IL13276198A patent/IL132761A0/xx not_active IP Right Cessation
- 1998-06-26 JP JP50628799A patent/JP3880634B2/ja not_active Expired - Lifetime
- 1998-06-26 DE DE69828692T patent/DE69828692T2/de not_active Expired - Lifetime
- 1998-06-26 AR ARP980103094A patent/AR017754A1/es active IP Right Grant
- 1998-06-26 BR BR9810956-1A patent/BR9810956A/pt not_active Application Discontinuation
- 1998-06-26 AU AU85409/98A patent/AU739211B2/en not_active Expired
- 1998-06-26 HU HU0003053A patent/HU227755B1/hu unknown
- 1998-06-26 ES ES98936392T patent/ES2236922T3/es not_active Expired - Lifetime
- 1998-06-26 KR KR10-1999-7010048A patent/KR100399765B1/ko not_active Expired - Lifetime
- 1998-06-26 AT AT98936392T patent/ATE287410T1/de active
- 1998-06-26 PL PL336719A patent/PL192761B1/pl unknown
- 1998-06-26 WO PCT/EP1998/003929 patent/WO1999001458A1/en not_active Ceased
- 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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PC41 | Official registration of the transfer of exclusive right |
Effective date: 20131029 |