RU2010150799A - НОВАЯ КРИСТАЛЛИЧЕСКАЯ И АМОРФНАЯ ФОРМА ТРИАЗОЛО(4,5-d)ПИРИМИДИНА - Google Patents
НОВАЯ КРИСТАЛЛИЧЕСКАЯ И АМОРФНАЯ ФОРМА ТРИАЗОЛО(4,5-d)ПИРИМИДИНА Download PDFInfo
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Abstract
1. Смесь соединения формулы (I): ! ! которое характеризуется порошковой рентгенограммой, содержащей характерные пики высокой интенсивности при 5,5° (±0,1°), 13,5° (±0,1), 18,3° (±0,1°), 22,7° (±0,1°) и 24,3° (±0,1°) 2θ, или ! характеризуется порошковой рентгенограммой, содержащей характерные пики при 5,5° (±0,1°), 6,8° (±0,1°), 10,6° (±0,1°), 13,5° (±0,1°), 14,9° (±0,1°), 18,3° (±0,1°), 19,2° (±0,1°), 22,7° (±0,1°), 24,3° (±0,1°) и 27,1° (±0,1°) 2θ, или ! характеризуется кривой дифференциальной сканирующей калориметрии, имеющей точку начала плавления, находящуюся в интервале 136-139°С, ! и соединения указанной формулы (I), ! которое характеризуется порошковой рентгенограммой, содержащей характерные пики высокой интенсивности при 14,0° (±0,1°), 17,4° (±0,1), 18,4° (±0,1°), 21,4° (±0,1°) и 24,1° (±0,1°) 2θ, или ! характеризуется порошковой рентгенограммой, содержащей характерные пики при 5,6° (±0,1°), 12,5° (±0,1°), 14,0° (±0,1°), 17,4° (±0,1°), 18,4° (±0,1°), 21,4° (±0,1°), 22,2° (±0,1°), 22,9° (±0,1°), 24,1° (±0,1°) и 24,5° (±0,1°) 2θ, или ! характеризуется кривой дифференциальной сканирующей калориметрии, имеющей точку начала плавления, находящуюся в пределах 127-132°С. ! 2. Смесь по п.1 для применения в качестве лекарственного препарата. ! 3. Фармацевтическая композиция, содержащая смесь по п.1 в смеси с фармацевтически приемлемым адъювантом, разбавителем или носителем. ! 4. Фармацевтическая композиция, содержащая смесь по п.1, для применения в целях профилактики артериальных тромботических осложнений у пациентов при заболеваниях коронарной артерии, цереброваскулярным и периферическим сосудистым заболеванием. ! 5. Фармацевтическая композиция, содержащая смесь по п.1, для производстве лекарственного препарата для применения в целях профилактики артериальны
Claims (5)
1. Смесь соединения формулы (I):
которое характеризуется порошковой рентгенограммой, содержащей характерные пики высокой интенсивности при 5,5° (±0,1°), 13,5° (±0,1), 18,3° (±0,1°), 22,7° (±0,1°) и 24,3° (±0,1°) 2θ, или
характеризуется порошковой рентгенограммой, содержащей характерные пики при 5,5° (±0,1°), 6,8° (±0,1°), 10,6° (±0,1°), 13,5° (±0,1°), 14,9° (±0,1°), 18,3° (±0,1°), 19,2° (±0,1°), 22,7° (±0,1°), 24,3° (±0,1°) и 27,1° (±0,1°) 2θ, или
характеризуется кривой дифференциальной сканирующей калориметрии, имеющей точку начала плавления, находящуюся в интервале 136-139°С,
и соединения указанной формулы (I),
которое характеризуется порошковой рентгенограммой, содержащей характерные пики высокой интенсивности при 14,0° (±0,1°), 17,4° (±0,1), 18,4° (±0,1°), 21,4° (±0,1°) и 24,1° (±0,1°) 2θ, или
характеризуется порошковой рентгенограммой, содержащей характерные пики при 5,6° (±0,1°), 12,5° (±0,1°), 14,0° (±0,1°), 17,4° (±0,1°), 18,4° (±0,1°), 21,4° (±0,1°), 22,2° (±0,1°), 22,9° (±0,1°), 24,1° (±0,1°) и 24,5° (±0,1°) 2θ, или
характеризуется кривой дифференциальной сканирующей калориметрии, имеющей точку начала плавления, находящуюся в пределах 127-132°С.
2. Смесь по п.1 для применения в качестве лекарственного препарата.
3. Фармацевтическая композиция, содержащая смесь по п.1 в смеси с фармацевтически приемлемым адъювантом, разбавителем или носителем.
4. Фармацевтическая композиция, содержащая смесь по п.1, для применения в целях профилактики артериальных тромботических осложнений у пациентов при заболеваниях коронарной артерии, цереброваскулярным и периферическим сосудистым заболеванием.
5. Фармацевтическая композиция, содержащая смесь по п.1, для производстве лекарственного препарата для применения в целях профилактики артериальных тромботических осложнений у пациентов при заболеваниях коронарной артерии, цереброваскулярным и периферическим сосудистым заболеванием.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0013407.2A GB0013407D0 (en) | 2000-06-02 | 2000-06-02 | Forms of a chemical compound |
| GB0013407.2 | 2000-06-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2010150799A true RU2010150799A (ru) | 2012-06-20 |
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Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2002135589/04A RU2325391C2 (ru) | 2000-06-02 | 2001-05-31 | НОВАЯ КРИСТАЛЛИЧЕСКАЯ И АМОРФНАЯ ФОРМА ТРИАЗОЛО[4,5-d]ПИРИМИДИНА |
| RU2005127356/04A RU2418802C2 (ru) | 2000-06-02 | 2005-08-30 | НОВАЯ КРИСТАЛЛИЧЕСКАЯ ФОРМА ТРИАЗОЛО (4,5-d) ПИРИМИДИНА |
| RU2010150799/04A RU2010150799A (ru) | 2000-06-02 | 2010-12-10 | НОВАЯ КРИСТАЛЛИЧЕСКАЯ И АМОРФНАЯ ФОРМА ТРИАЗОЛО(4,5-d)ПИРИМИДИНА |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2002135589/04A RU2325391C2 (ru) | 2000-06-02 | 2001-05-31 | НОВАЯ КРИСТАЛЛИЧЕСКАЯ И АМОРФНАЯ ФОРМА ТРИАЗОЛО[4,5-d]ПИРИМИДИНА |
| RU2005127356/04A RU2418802C2 (ru) | 2000-06-02 | 2005-08-30 | НОВАЯ КРИСТАЛЛИЧЕСКАЯ ФОРМА ТРИАЗОЛО (4,5-d) ПИРИМИДИНА |
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| Country | Link |
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| US (3) | US20030181469A1 (ru) |
| EP (3) | EP1289992B1 (ru) |
| JP (3) | JP5036947B2 (ru) |
| KR (1) | KR100781864B1 (ru) |
| CN (2) | CN1247583C (ru) |
| AR (2) | AR032335A1 (ru) |
| AT (2) | ATE320430T1 (ru) |
| AU (4) | AU2001262874B2 (ru) |
| BG (3) | BG65837B1 (ru) |
| BR (1) | BR0111328A (ru) |
| CA (1) | CA2408596C (ru) |
| CY (1) | CY1113047T1 (ru) |
| CZ (2) | CZ307468B6 (ru) |
| DE (1) | DE60117972T2 (ru) |
| DK (2) | DK1493745T3 (ru) |
| EE (1) | EE05222B1 (ru) |
| ES (2) | ES2259031T3 (ru) |
| GB (1) | GB0013407D0 (ru) |
| HK (1) | HK1052347B (ru) |
| HU (2) | HU230471B1 (ru) |
| IL (4) | IL152777A0 (ru) |
| IS (2) | IS2609B (ru) |
| MX (1) | MXPA02011795A (ru) |
| MY (2) | MY148652A (ru) |
| NO (3) | NO323780B1 (ru) |
| NZ (1) | NZ522638A (ru) |
| PH (1) | PH12011000127A1 (ru) |
| PL (2) | PL392882A1 (ru) |
| PT (2) | PT1289992E (ru) |
| RU (3) | RU2325391C2 (ru) |
| SG (1) | SG135965A1 (ru) |
| SI (2) | SI1289992T1 (ru) |
| SK (1) | SK287817B6 (ru) |
| UA (1) | UA73181C2 (ru) |
| WO (1) | WO2001092262A1 (ru) |
| ZA (1) | ZA200209324B (ru) |
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|---|---|---|---|---|
| TWI229674B (en) | 1998-12-04 | 2005-03-21 | Astra Pharma Prod | Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses |
| GB0013407D0 (en) * | 2000-06-02 | 2000-07-26 | Astrazeneca Ab | Forms of a chemical compound |
| GB0013488D0 (en) * | 2000-06-02 | 2000-07-26 | Astrazeneca Ab | Chemical compound |
| JP4298212B2 (ja) * | 2002-03-29 | 2009-07-15 | 大日本印刷株式会社 | 塩酸エピナスチン高融点型結晶の製造法 |
| US20080045548A1 (en) * | 2006-08-21 | 2008-02-21 | Astrazeneca Ab | Pharmaceutical Compositions |
| TWI482772B (zh) * | 2006-08-21 | 2015-05-01 | Astrazeneca Ab | 適合口服且包含三唑并[4,5-d]嘧啶衍生物之組合物 |
| WO2008054795A2 (en) * | 2006-10-31 | 2008-05-08 | Janssen Pharmaceutica, N.V. | Triazolopyrimidine derivatives as adp p2y12 receptor antagonists |
| WO2008127682A2 (en) * | 2007-04-13 | 2008-10-23 | Millennium Pharmaceuticals, Inc. | Combination anticoagulant therapy with a compound that acts as a factor xa inhibitor |
| TWI496776B (zh) * | 2007-11-15 | 2015-08-21 | Astrazeneca Ab | 製備(3aR,4S,6R,6aS)-6-胺基-2,2-二甲基四氫-3aH-環戊并[d][1,3]二氧雜環戊烯-4-醇之純非對映異構性之二苯甲醯-L-酒石酸鹽之方法 |
| UA100864C2 (ru) * | 2007-12-03 | 2013-02-11 | Астразенека Аб | Способ лечения или предотвращения аневризмы брюшной аорты |
| ES2558843T3 (es) | 2008-09-09 | 2016-02-09 | Astrazeneca Ab | Procedimiento para preparar [1S-[1-alfa,2-alfa,3-beta(1S*,2R*),5-beta]]-3-[7-[2-(3,4-difluorofenil)-ciclopropilamino]-5-(propiltio)-3H-1,2,3-triazolo[4,5-d]pirimidin-3-il]-5-(2-hidroxietoxi)ciclopentano-1,2-diol y a sus productos intermedios |
| ES2605625T3 (es) | 2009-07-27 | 2017-03-15 | Auspex Pharmaceuticals, Inc. | Moduladores de ciclopropilo del receptor P2Y12 |
| RU2012126029A (ru) * | 2009-12-03 | 2014-01-10 | Астразенека Аб | Сокристаллы триазоло[4,5 d]пиримидинового ингибитора агрегации тромбоцитов |
| ES2550033T3 (es) | 2009-12-23 | 2015-11-04 | Ratiopharm Gmbh | Forma de dosificación farmacéutica sólida de ticagrelor |
| CZ2011229A3 (cs) * | 2011-04-19 | 2012-08-15 | Zentiva, K.S. | Opticky aktivní soli (3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyklopenta-[d][1,3]dioxol-4-olu a zpusob jejich prípravy |
| US9101642B2 (en) | 2011-06-01 | 2015-08-11 | Astrazeneca Ab | Ticagrelor co-crystal |
| BR112014013085A2 (pt) * | 2011-11-30 | 2017-06-13 | Actavis Group Ptc Ehf | forma cristalina do ticagrelor, processo para a preparação da forma cristalina do ticagrelor, composição farmacêutica e processo para preparar uma composição farmacêutica |
| EP2834247A4 (en) | 2012-04-05 | 2016-03-30 | Reddys Lab Ltd Dr | PREPARATION OF TICAGRELOR |
| EP2867235A1 (en) | 2012-06-29 | 2015-05-06 | Zentiva K.S. | Novel pharmaceutical solid forms of (1s,2s,3r,5s)-3-[7-[(1r,2s)-2-(3,4difluorophenyl)cyclopropylamino]-5-(propylthio)-3h-[1,2,3]triazolo[4,5-d]pyrimidin-3yl]-5-(2-hydroxyethoxy)cyclopentane-l,2-diol |
| CN104640864B (zh) | 2012-07-04 | 2016-11-16 | 力奇制药公司 | 替格瑞洛与二价金属盐的加合物 |
| CZ2012705A3 (cs) * | 2012-10-16 | 2014-04-23 | Zentiva, K.S. | Pevná orální farmaceutická formulace obsahující ticagrelor |
| CN103772393B (zh) * | 2012-10-18 | 2017-08-04 | 博瑞生物医药（苏州）股份有限公司 | 替卡格雷的晶型及其制备方法 |
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| CN103848836B (zh) * | 2012-12-07 | 2016-08-03 | 天津市汉康医药生物技术有限公司 | 替卡格雷倍半水合物及其制备方法 |
| WO2014118808A2 (en) * | 2013-02-04 | 2014-08-07 | Hetero Research Foundation | Ticagrelor solid dispersion |
| CZ307217B6 (cs) | 2013-03-14 | 2018-04-04 | Zentiva, K.S. | Zlepšený způsob výroby a nové intermediáty syntézy ticagreloru |
| IN2013MU01111A (ru) * | 2013-03-25 | 2015-05-01 | Glenmark Generics Ltd | |
| CN104098570A (zh) * | 2013-04-07 | 2014-10-15 | 杭州领业医药科技有限公司 | 替卡格雷晶型及其制备方法和用途 |
| CN104098572A (zh) * | 2013-04-08 | 2014-10-15 | 博瑞生物医药技术(苏州)有限公司 | 替卡格雷共晶型 |
| CN104098553B (zh) * | 2013-04-10 | 2017-11-28 | 江苏恒瑞医药股份有限公司 | 替格瑞洛的中间体及其制备方法和替格瑞洛的制备方法 |
| EP2813216A1 (en) | 2013-06-10 | 2014-12-17 | Zentiva, a.s. | Stabilized amorphous ticagrelor |
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| US5561134A (en) * | 1990-09-25 | 1996-10-01 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties |
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| JP4125790B2 (ja) * | 1996-12-20 | 2008-07-30 | アストラゼネカ・アクチエボラーグ | トリアゾロ［４，５−ｄ］ピリミジニル誘導体および医薬としてのその使用 |
| TW530058B (en) * | 1997-07-22 | 2003-05-01 | Astra Pharma Prod | Triazolo [4,5-d]pyrimidine compounos and their use and process for preparation |
| KR100617608B1 (ko) * | 1997-07-25 | 2006-09-01 | 길리애드 사이언시즈, 인코포레이티드 | (ｒ)-ｐｍｐａ의 키랄 농축을 위한 조성물 및 그의 제조방법 |
| TWI229674B (en) * | 1998-12-04 | 2005-03-21 | Astra Pharma Prod | Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses |
| SE9904129D0 (sv) * | 1999-11-15 | 1999-11-15 | Astra Pharma Prod | Novel compounds |
| GB0013407D0 (en) * | 2000-06-02 | 2000-07-26 | Astrazeneca Ab | Forms of a chemical compound |
| GB0013488D0 (en) * | 2000-06-02 | 2000-07-26 | Astrazeneca Ab | Chemical compound |
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