RU2001122164A - Кристаллическая кальциевая соль бис[(е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]- пиримидин-5-ил]-(3r,5s)-3,5-дигидроксигепт-6-еновой кислоты] - Google Patents
Кристаллическая кальциевая соль бис[(е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]- пиримидин-5-ил]-(3r,5s)-3,5-дигидроксигепт-6-еновой кислоты]Info
- Publication number
- RU2001122164A RU2001122164A RU2001122164/04A RU2001122164A RU2001122164A RU 2001122164 A RU2001122164 A RU 2001122164A RU 2001122164/04 A RU2001122164/04 A RU 2001122164/04A RU 2001122164 A RU2001122164 A RU 2001122164A RU 2001122164 A RU2001122164 A RU 2001122164A
- Authority
- RU
- Russia
- Prior art keywords
- crystalline form
- form according
- methyl
- methylsulfonyl
- fluorophenyl
- Prior art date
Links
- 159000000007 calcium salts Chemical class 0.000 title claims 2
- 239000013078 crystal Substances 0.000 title claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 title 1
- 239000002253 acid Substances 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 title 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 title 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 title 1
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical group CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 2
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 claims 1
- 108090000895 Hydroxymethylglutaryl CoA Reductases Proteins 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- BPRHUIZQVSMCRT-VEUZHWNKSA-N rosuvastatin Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1\C=C\[C@@H](O)C[C@@H](O)CC(O)=O BPRHUIZQVSMCRT-VEUZHWNKSA-N 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Claims (8)
1. Кристаллическая форма кальциевой соли бис[(Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]-пиримидин-5-ил](3R, 5S)-3, 5-дигидроксигепт-6-еновой кислоты] формулы I
или ее гидрат, имеющая порошковую рентгенограмму с характерными пиками при значениях угла 2-тета (2θ)=4,92; 11,50; 6,93; 9,35; 23,12 и 18,76°.
2. Кристаллическая форма по п.1, которая является кристаллической гидратированной формой.
3. Фармацевтическая композиция, содержащая кристаллическую форму по п.1 или 2 вместе с фармацевтически приемлемым носителем.
4. Способ получения кристаллической формы для гидратированной формы по п.1, который включает формирование кристаллов из смеси соединения формулы 1, воды и одного или более органических растворителей.
5. Способ по п.4, в котором органический растворитель выбран из ацетонитрила, ацетона или смеси метанола и метил- третбутилового эфира.
6. Способ получения фармацевтической композиции по п.3, который включает смешивание кристаллической формы по п.1 с фармацевтически приемлемым носителем.
7. Применение кристаллической формы по п.1 для изготовления лекарственного препарата.
8. Способ лечения болезненного состояния, для которого полезно ингибирование ГМГ-СоА-редуктазы, который включает введение теплокровным млекопитающим эффективного количества кристаллической формы по п.1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9900339.4A GB9900339D0 (en) | 1999-01-09 | 1999-01-09 | Chemical compounds |
| GB9900339.4 | 1999-01-09 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2001122164A true RU2001122164A (ru) | 2003-05-20 |
| RU2236404C2 RU2236404C2 (ru) | 2004-09-20 |
Family
ID=10845719
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2001122164/04A RU2236404C2 (ru) | 1999-01-09 | 1999-12-23 | Кристаллическая гидратированная форма кальциевой соли бис[(е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]-пири мидин-5-ил]-(3r,5s)-3,5-дигидроксигепт-6-еновой кислоты], способ ее получения, фармацевтическая композиция, способ ее получения и способ лечения |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US6589959B1 (ru) |
| EP (1) | EP1144389B1 (ru) |
| JP (2) | JP4996786B2 (ru) |
| KR (1) | KR100645858B1 (ru) |
| CN (1) | CN1213033C (ru) |
| AT (1) | ATE282027T1 (ru) |
| AU (1) | AU762909B2 (ru) |
| BR (1) | BR9916786A (ru) |
| CA (1) | CA2356212C (ru) |
| CZ (1) | CZ299843B6 (ru) |
| DE (1) | DE69921855T2 (ru) |
| DK (1) | DK1144389T3 (ru) |
| EE (1) | EE05033B1 (ru) |
| ES (1) | ES2232194T3 (ru) |
| GB (1) | GB9900339D0 (ru) |
| HK (1) | HK1040989B (ru) |
| HU (1) | HU228116B1 (ru) |
| ID (1) | ID29432A (ru) |
| IL (1) | IL143977A0 (ru) |
| IN (2) | IN213326B (ru) |
| IS (1) | IS2410B (ru) |
| MX (1) | MX223771B (ru) |
| NO (1) | NO320189B1 (ru) |
| NZ (1) | NZ512560A (ru) |
| PL (1) | PL201800B1 (ru) |
| PT (1) | PT1144389E (ru) |
| RU (1) | RU2236404C2 (ru) |
| SI (1) | SI1144389T1 (ru) |
| SK (1) | SK285807B6 (ru) |
| TR (1) | TR200101894T2 (ru) |
| WO (1) | WO2000042024A1 (ru) |
| ZA (1) | ZA200105187B (ru) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9900339D0 (en) * | 1999-01-09 | 1999-02-24 | Zeneca Ltd | Chemical compounds |
| GB0001621D0 (en) * | 2000-01-26 | 2000-03-15 | Astrazeneca Ab | Pharmaceutical compositions |
| GB0003305D0 (en) * | 2000-02-15 | 2000-04-05 | Zeneca Ltd | Pyrimidine derivatives |
| DE10135493A1 (de) * | 2001-07-20 | 2003-01-30 | Jobst Krauskopf | Pharmazeutische Zusammensetzung zur Behandlung von Hypercholesterinämie |
| GB0218781D0 (en) | 2002-08-13 | 2002-09-18 | Astrazeneca Ab | Chemical process |
| US20060019269A1 (en) * | 2002-10-17 | 2006-01-26 | Decode Genetics, Inc. | Susceptibility gene for myocardial infarction, stroke, and PAOD, methods of treatment |
| US20080293750A1 (en) * | 2002-10-17 | 2008-11-27 | Anna Helgadottir | Susceptibility Gene for Myocardial Infarction, Stroke, Paod and Methods of Treatment |
| US7585988B2 (en) * | 2003-04-25 | 2009-09-08 | Nippon Chemiphar Co., Ltd. | Salt of (2S, 3S) -3- [[(1S) -1- isobutoxymethyl-3-methylbutyl] carbamoly] oxirane-2-carboxylic acid |
| GB0312896D0 (en) | 2003-06-05 | 2003-07-09 | Astrazeneca Ab | Chemical process |
| UY28501A1 (es) * | 2003-09-10 | 2005-04-29 | Astrazeneca Uk Ltd | Compuestos químicos |
| GB0322552D0 (en) | 2003-09-26 | 2003-10-29 | Astrazeneca Uk Ltd | Therapeutic treatment |
| GB0324791D0 (en) | 2003-10-24 | 2003-11-26 | Astrazeneca Ab | Chemical process |
| WO2005051921A1 (en) * | 2003-11-24 | 2005-06-09 | Teva Pharmaceutical Industries Ltd. | Crystalline ammonium salts of rosuvastatin |
| CZ200486A3 (cs) * | 2004-01-16 | 2005-08-17 | Zentiva, A.S. | Způsob výroby hemivápenaté soli (E)-7-[4-(4-fluorfenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxy-6-heptenové kyseliny |
| EP1709008A1 (en) * | 2004-01-19 | 2006-10-11 | Ranbaxy Laboratories Limited | Salts of hmg-coa reductase inhibitors and use thereof |
| EP1737828A1 (en) * | 2004-01-19 | 2007-01-03 | Ranbaxy Laboratories Limited | Amorphous magnesium salts of rosuvastatin |
| US20100216863A1 (en) * | 2004-01-30 | 2010-08-26 | Decode Genetics Ehf. | Susceptibility Gene for Myocardial Infarction, Stroke, and PAOD; Methods of Treatment |
| US8158362B2 (en) * | 2005-03-30 | 2012-04-17 | Decode Genetics Ehf. | Methods of diagnosing susceptibility to myocardial infarction and screening for an LTA4H haplotype |
| US7241800B2 (en) | 2004-03-17 | 2007-07-10 | Mai De Ltd. | Anhydrous amorphous form of fluvastatin sodium |
| WO2006035277A2 (en) * | 2004-09-27 | 2006-04-06 | Ranbaxy Laboratories Limited | Novel processes for preparing amorphous rosuvastatin calcium and a novel polymorphic form of rosuvastatin sodium |
| CA2594692A1 (en) * | 2005-01-31 | 2006-08-03 | Ciba Specialty Chemicals Holding Inc. | Crystalline forms of rosuvastatin calcium salt |
| JP5146965B2 (ja) | 2005-06-24 | 2013-02-20 | レツク・フアーマシユーテイカルズ・デー・デー | 不純物を含まない非晶質ロスバスタチンカルシウムの調製方法 |
| CZ299215B6 (cs) * | 2005-06-29 | 2008-05-21 | Zentiva, A. S. | Zpusob výroby hemivápenaté soli (E)-7-[4-(4-fluorofenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl] (3R,5S)-3,5-dihydroxy-6-heptenovékyseliny |
| US7868169B2 (en) * | 2005-08-16 | 2011-01-11 | Teva Pharmaceutical Industries, Ltd. | Crystalline rosuvastatin intermediate |
| HU227696B1 (en) * | 2006-04-13 | 2011-12-28 | Egyt Gyogyszervegyeszeti Gyar | Zinc salt of rosuvastatin, process for its preparation and pharmaceutical compositions containing it |
| EP2066644A2 (en) * | 2006-08-04 | 2009-06-10 | Glenmark Pharmaceuticals Limited | Salts of rosuvastatin and processes for their preparation |
| EP1948618A1 (en) * | 2006-09-18 | 2008-07-30 | Teva Pharmaceutical Industries Ltd. | Crystalline rosuvastatin calcium |
| US20080249141A1 (en) * | 2007-04-06 | 2008-10-09 | Palepu Nageswara R | Co-therapy with and combinations of statins and 1,4-dihydropyridine-3,5-dicarboxydiesters |
| US20080249156A1 (en) * | 2007-04-09 | 2008-10-09 | Palepu Nageswara R | Combinations of statins and anti-obesity agent and glitazones |
| JP2010523659A (ja) * | 2007-04-09 | 2010-07-15 | サイドース・エルエルシー | スタチン類と抗肥満症薬との組み合わせ |
| EP2298745B1 (en) | 2008-05-27 | 2014-09-03 | Changzhou Pharmaceutical Factory | Preparation method of rosuvastatin calcium and its intermediates |
| EP2336116A1 (en) * | 2009-12-16 | 2011-06-22 | LEK Pharmaceuticals d.d. | Process for the preparation of key intermediates for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof |
| WO2011074016A1 (en) | 2009-12-17 | 2011-06-23 | Matrix Laboratories Ltd | Novel polymorphic forms of rosuvastatin calcium and process for preparation of the same |
| US20130156720A1 (en) | 2010-08-27 | 2013-06-20 | Ironwood Pharmaceuticals, Inc. | Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders |
| CA2818007A1 (en) | 2010-11-22 | 2012-05-31 | Basf Se | Multicomponent system of rosuvastatin calcium salt and sorbitol |
| EP2699552A1 (en) | 2011-04-18 | 2014-02-26 | Basf Se | Multicomponent crystalline system of rosuvastatin calcium salt and vanillin |
| WO2014050874A1 (ja) * | 2012-09-27 | 2014-04-03 | 東和薬品株式会社 | ロスバスタチンカルシウムの新規結晶形態およびその製造方法 |
| RO129060B1 (ro) | 2013-04-25 | 2014-11-28 | Antibiotice S.A. | Compoziţie farmaceutică stabilă cu rosuvastatină calcică amorfă |
| CN103755643A (zh) * | 2013-12-31 | 2014-04-30 | 连云港金康医药科技有限公司 | 瑞苏伐他汀钙盐i晶型 |
| CN105153040B (zh) * | 2015-10-15 | 2018-04-13 | 江苏师范大学 | 瑞舒伐他汀钙新晶型及其制备方法 |
| WO2017183040A1 (en) | 2016-04-18 | 2017-10-26 | Morepen Laboratories Limited | New polymorphic form of crystalline rosuvastatin calcium & novel processes for crystalline as well as amorphous rosuvastatin calcium |
| CN105837516B (zh) * | 2016-05-16 | 2018-07-10 | 山东新时代药业有限公司 | 一种瑞舒伐他汀钙晶型及其制备方法 |
| CN114105885A (zh) * | 2020-08-28 | 2022-03-01 | 广东东阳光药业有限公司 | 一种瑞舒伐他汀钙晶型a的制备方法 |
| WO2022228551A1 (zh) * | 2021-04-30 | 2022-11-03 | 江苏恒瑞医药股份有限公司 | 一种血小板生成素受体激动剂的给药方案 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9027018D0 (en) * | 1990-12-12 | 1991-01-30 | Ici Plc | Heterocyclic compounds |
| JP2648897B2 (ja) * | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | ピリミジン誘導体 |
| GB9900339D0 (en) * | 1999-01-09 | 1999-02-24 | Zeneca Ltd | Chemical compounds |
-
1999
- 1999-01-09 GB GBGB9900339.4A patent/GB9900339D0/en not_active Ceased
- 1999-12-23 AU AU18826/00A patent/AU762909B2/en not_active Ceased
- 1999-12-23 CN CNB998155047A patent/CN1213033C/zh not_active Expired - Lifetime
- 1999-12-23 DK DK99962471T patent/DK1144389T3/da active
- 1999-12-23 SK SK963-2001A patent/SK285807B6/sk not_active IP Right Cessation
- 1999-12-23 SI SI9930731T patent/SI1144389T1/xx unknown
- 1999-12-23 IL IL14397799A patent/IL143977A0/xx not_active IP Right Cessation
- 1999-12-23 NZ NZ512560A patent/NZ512560A/en not_active IP Right Cessation
- 1999-12-23 TR TR2001/01894T patent/TR200101894T2/xx unknown
- 1999-12-23 DE DE69921855T patent/DE69921855T2/de not_active Expired - Lifetime
- 1999-12-23 EP EP99962471A patent/EP1144389B1/en not_active Expired - Lifetime
- 1999-12-23 BR BR9916786-7A patent/BR9916786A/pt not_active Application Discontinuation
- 1999-12-23 JP JP2000593592A patent/JP4996786B2/ja not_active Expired - Lifetime
- 1999-12-23 CA CA002356212A patent/CA2356212C/en not_active Expired - Fee Related
- 1999-12-23 WO PCT/GB1999/004439 patent/WO2000042024A1/en active IP Right Grant
- 1999-12-23 PL PL348775A patent/PL201800B1/pl unknown
- 1999-12-23 RU RU2001122164/04A patent/RU2236404C2/ru not_active IP Right Cessation
- 1999-12-23 US US09/869,462 patent/US6589959B1/en not_active Expired - Lifetime
- 1999-12-23 AT AT99962471T patent/ATE282027T1/de active
- 1999-12-23 HK HK02102104.7A patent/HK1040989B/en not_active IP Right Cessation
- 1999-12-23 KR KR1020017008546A patent/KR100645858B1/ko not_active Expired - Fee Related
- 1999-12-23 ID IDW00200101470A patent/ID29432A/id unknown
- 1999-12-23 PT PT99962471T patent/PT1144389E/pt unknown
- 1999-12-23 EE EEP200100359A patent/EE05033B1/xx not_active IP Right Cessation
- 1999-12-23 CZ CZ20012460A patent/CZ299843B6/cs not_active IP Right Cessation
- 1999-12-23 HU HU0104828A patent/HU228116B1/hu unknown
- 1999-12-23 ES ES99962471T patent/ES2232194T3/es not_active Expired - Lifetime
-
2001
- 2001-06-08 IN IN758MU2001 patent/IN213326B/en unknown
- 2001-06-22 IS IS5977A patent/IS2410B/is unknown
- 2001-06-22 ZA ZA200105187A patent/ZA200105187B/en unknown
- 2001-07-06 MX MXPA01006953 patent/MX223771B/es active IP Right Grant
- 2001-07-06 NO NO20013368A patent/NO320189B1/no not_active IP Right Cessation
-
2003
- 2003-02-14 IN IN223MU2003 patent/IN2003MU00223A/en unknown
- 2003-04-10 US US10/410,650 patent/US20040009997A1/en not_active Abandoned
-
2009
- 2009-11-16 JP JP2009260812A patent/JP2010090128A/ja active Pending
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