RU2016137943A - Аморфная форма производного тиоколхицина - Google Patents
Аморфная форма производного тиоколхицина Download PDFInfo
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- RU2016137943A RU2016137943A RU2016137943A RU2016137943A RU2016137943A RU 2016137943 A RU2016137943 A RU 2016137943A RU 2016137943 A RU2016137943 A RU 2016137943A RU 2016137943 A RU2016137943 A RU 2016137943A RU 2016137943 A RU2016137943 A RU 2016137943A
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- RU
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- Prior art keywords
- amorphous compound
- formula
- pharmaceutical composition
- amorphous
- paragraphs
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
- C07C323/31—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
- C07C323/38—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton with the sulfur atom of the thio group bound to a carbon atom of a six-membered aromatic ring being part of a condensed ring system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
- C07C319/26—Separation; Purification; Stabilisation; Use of additives
- C07C319/28—Separation; Purification
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
- C07C319/26—Separation; Purification; Stabilisation; Use of additives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
- C07C323/39—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
- C07C323/43—Y being a hetero atom
- C07C323/44—X or Y being nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
- C07C2603/30—Ortho- or ortho- and peri-condensed systems containing three rings containing seven-membered rings
- C07C2603/34—Benzoheptalenes; Hydrogenated benzoheptalenes
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Dermatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Claims (13)
1. Аморфное соединение Формулы (I):
имеющее картину XRPD (порошковой рентгеновской дифракции), показанную на Фиг. 1.
2. Аморфное соединение по п. 1, имеющее профиль DSC (дифференциальная сканирующая калориметрия), отличающееся переходом в стеклообразное состояние с началом при 186,9°С и окончанием при 194,5°С, зарегистрированным при линейной скорости нагрева 10°С/мин.
3. Аморфное соединение по п. 1, имеющее профиль TG/DTA (термогравиметрия/дифференциальный термический анализ), отличающееся эндотермическим сигналом от 185,4°С до 195,4°С, зарегистрированным при линейной скорости нагрева в 10°С/мин.
4. Способ получения аморфного соединения формулы (I), как определено по п. 1, включающий стадии:
а) растворения неочищенного соединения формулы (I) в DMSO;
б) удаления возможных остаточных растворителей, происходящих из синтетического процесса, путем нагревания раствора при 65°С в вакууме;
в) осаждения аморфного соединения формулы (I) путем добавления по каплям раствора, полученного на стадии б), к воде при 20-25°С.
5. Фармацевтическая композиция, содержащая аморфное соединение формулы (I) по любому из пп. 1-3 и фармацевтически приемлемый носитель и разбавитель.
6. Фармацевтическая композиция по п. 5 для парентерального или перорального введения.
7. Фармацевтическая композиция по п. 6 в форме инъекционного препарата.
8. Аморфное соединение формулы (I) по любому из пп. 1-3 для применения в лечении солидных опухолей.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14161945.2A EP2924022A1 (en) | 2014-03-27 | 2014-03-27 | Amorphous form of a thiocolchicine derivative |
| EP14161945.2 | 2014-03-27 | ||
| PCT/EP2015/056658 WO2015144857A1 (en) | 2014-03-27 | 2015-03-26 | Amorphous form of a thiocolchicine derivative |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2016137943A true RU2016137943A (ru) | 2018-04-27 |
| RU2016137943A3 RU2016137943A3 (ru) | 2018-10-10 |
| RU2684925C2 RU2684925C2 (ru) | 2019-04-16 |
Family
ID=50389871
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2016137943A RU2684925C2 (ru) | 2014-03-27 | 2015-03-26 | Аморфная форма производного тиоколхицина |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9688625B2 (ru) |
| EP (2) | EP2924022A1 (ru) |
| JP (1) | JP6538711B2 (ru) |
| KR (1) | KR102302055B1 (ru) |
| CN (1) | CN106132927B (ru) |
| AU (1) | AU2015238266B2 (ru) |
| CA (1) | CA2943699C (ru) |
| DK (1) | DK3122722T3 (ru) |
| ES (1) | ES2686882T3 (ru) |
| HU (1) | HUE040059T2 (ru) |
| IL (1) | IL247968B (ru) |
| PL (1) | PL3122722T3 (ru) |
| PT (1) | PT3122722T (ru) |
| RU (1) | RU2684925C2 (ru) |
| SG (1) | SG11201607947XA (ru) |
| SI (1) | SI3122722T1 (ru) |
| WO (1) | WO2015144857A1 (ru) |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1291550B1 (it) * | 1997-04-11 | 1999-01-11 | Indena Spa | Derivati della colchicina e della tiocolchicina ad attivita' antinfiammatoria e miorilassante |
| IT1318401B1 (it) * | 2000-03-17 | 2003-08-25 | Indena Spa | Derivati di n-desacetiltiocolchicina e composizioni farmaceutiche cheli contengono. |
| KR100603974B1 (ko) * | 2003-12-05 | 2006-07-25 | 김갑식 | 고체상 지질을 용매로 이용한 나노수준의 또는 비결정질입자의 제조 방법 |
| KR20070067175A (ko) * | 2004-10-28 | 2007-06-27 | 워너-램버트 캄파니 엘엘씨 | 무정형 아토르바스타틴 형성 방법 |
| CA2598213C (en) * | 2005-02-18 | 2011-04-19 | Abraxis Bioscience, Inc. | Drugs with improved hydrophobicity for incorporation in medical devices |
| US20070166388A1 (en) * | 2005-02-18 | 2007-07-19 | Desai Neil P | Combinations and modes of administration of therapeutic agents and combination therapy |
| SI3248600T1 (sl) * | 2005-02-18 | 2020-09-30 | Abraxis Bioscience, Llc | Kombinacije in načini dajanja terapevtskih sredstev in kombinacijska terapija |
| EP2013138B1 (en) * | 2006-05-04 | 2014-04-09 | Bio-Synectics Inc. | Method for preparing nano-scale particle of active material |
| EP2056812A1 (en) * | 2006-08-31 | 2009-05-13 | Abraxis BioScience, LLC | Methods of inhibiting angiogenesis and treating angiogenesis-associated diseases |
| US20080280987A1 (en) * | 2006-08-31 | 2008-11-13 | Desai Neil P | Methods of inhibiting angiogenesis and treating angiogenesis-associated diseases |
| CN101730526A (zh) * | 2007-03-07 | 2010-06-09 | 阿布拉科斯生物科学有限公司 | 作为抗癌剂的包含雷帕霉素和白蛋白的纳米颗粒 |
| BRPI1008955A2 (pt) * | 2009-03-13 | 2015-09-01 | Abraxis Bioscience Llc | Terapia de combinação com derivados de tiocolchicina. |
-
2014
- 2014-03-27 EP EP14161945.2A patent/EP2924022A1/en not_active Withdrawn
-
2015
- 2015-03-26 PT PT15713860T patent/PT3122722T/pt unknown
- 2015-03-26 SI SI201530398T patent/SI3122722T1/sl unknown
- 2015-03-26 EP EP15713860.3A patent/EP3122722B1/en active Active
- 2015-03-26 SG SG11201607947XA patent/SG11201607947XA/en unknown
- 2015-03-26 PL PL15713860T patent/PL3122722T3/pl unknown
- 2015-03-26 US US15/124,679 patent/US9688625B2/en active Active
- 2015-03-26 HU HUE15713860A patent/HUE040059T2/hu unknown
- 2015-03-26 ES ES15713860.3T patent/ES2686882T3/es active Active
- 2015-03-26 WO PCT/EP2015/056658 patent/WO2015144857A1/en active Application Filing
- 2015-03-26 CN CN201580015791.8A patent/CN106132927B/zh active Active
- 2015-03-26 RU RU2016137943A patent/RU2684925C2/ru active
- 2015-03-26 DK DK15713860.3T patent/DK3122722T3/en active
- 2015-03-26 AU AU2015238266A patent/AU2015238266B2/en active Active
- 2015-03-26 CA CA2943699A patent/CA2943699C/en active Active
- 2015-03-26 KR KR1020167026456A patent/KR102302055B1/ko active IP Right Grant
- 2015-03-26 JP JP2016558744A patent/JP6538711B2/ja active Active
-
2016
- 2016-09-22 IL IL247968A patent/IL247968B/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| RU2016137943A3 (ru) | 2018-10-10 |
| HUE040059T2 (hu) | 2019-02-28 |
| DK3122722T3 (en) | 2018-08-13 |
| SI3122722T1 (sl) | 2018-10-30 |
| AU2015238266A1 (en) | 2016-10-13 |
| CN106132927B (zh) | 2018-07-27 |
| WO2015144857A1 (en) | 2015-10-01 |
| KR20160138423A (ko) | 2016-12-05 |
| JP2017510584A (ja) | 2017-04-13 |
| JP6538711B2 (ja) | 2019-07-03 |
| ES2686882T3 (es) | 2018-10-22 |
| AU2015238266B2 (en) | 2019-03-07 |
| PL3122722T3 (pl) | 2018-11-30 |
| CA2943699C (en) | 2022-07-12 |
| EP3122722B1 (en) | 2018-07-04 |
| PT3122722T (pt) | 2018-10-18 |
| EP3122722A1 (en) | 2017-02-01 |
| EP2924022A1 (en) | 2015-09-30 |
| RU2684925C2 (ru) | 2019-04-16 |
| KR102302055B1 (ko) | 2021-09-15 |
| IL247968B (en) | 2019-03-31 |
| SG11201607947XA (en) | 2016-10-28 |
| CA2943699A1 (en) | 2015-10-01 |
| US20170022155A1 (en) | 2017-01-26 |
| US9688625B2 (en) | 2017-06-27 |
| CN106132927A (zh) | 2016-11-16 |
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