RU2002124621A - Кристаллические соли 7-[4-(4-фторфенил)-6-изопропил-2-[метил (метилсульфонил) амино]пиримидин-5-ил]-(3r,5s)-3, 5-дигидроксигепт-6-еновой кислоты - Google Patents
Кристаллические соли 7-[4-(4-фторфенил)-6-изопропил-2-[метил (метилсульфонил) амино]пиримидин-5-ил]-(3r,5s)-3, 5-дигидроксигепт-6-еновой кислотыInfo
- Publication number
- RU2002124621A RU2002124621A RU2002124621/04A RU2002124621A RU2002124621A RU 2002124621 A RU2002124621 A RU 2002124621A RU 2002124621/04 A RU2002124621/04 A RU 2002124621/04A RU 2002124621 A RU2002124621 A RU 2002124621A RU 2002124621 A RU2002124621 A RU 2002124621A
- Authority
- RU
- Russia
- Prior art keywords
- crystalline
- methylsulfonyl
- fluorophenyl
- isopropyl
- amino
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (15)
1. Кристаллическая соль соединения (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты, где соль представляет собой соль аммония, метиламмония, этиламмония, диэтаноламмония, трис(гидроксиметил)метиламмония, бензил-аммония, 4-метоксибензиламмония, лития или магния.
2. Кристаллическая соль по п.1, которая представляет собой кристаллическую аммониевую соль (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты, в порошковой рентгенограмме которой присутствуют характеристические пики при 2-тета = 12,9, 15,2, 18,0, 18,2, 18,5, 20,2, 22,4, 23,0, 24,0 и 27,2°.
3. Кристаллическая соль по п.1, которая представляет собой кристаллическую метиламмониевую соль (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты, в порошковой рентгенограмме которой присутствуют характеристические пики при 2-тета = 8,2, 12,3, 15,7, 16,5, 17,6, 18,7, 19,9, 21,0, 24,3 и 25,9°.
4. Кристаллическая соль по п.1, которая представляет собой кристаллическую этиламмониевую соль (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты, в порошковой рентгенограмме которой присутствуют характеристические пики при 2-тета = 8,6, 15,9, 16,9, 18,4, 18,7, 19,7, 20,8, 23,3, 23,8 и 25,8°.
5. Кристаллическая соль по п.1, которая представляет собой кристаллическую диэтаноламмониевую соль (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,53)-3,5-дигидроксигепт-6-еновой кислоты, в порошковой рентгенограмме которой присутствуют характеристические пики при 2-тета = 9,9, 11,4, 16,1, 18,0, 18,7, 19,0, 20,6, 22,9, 24,3 и 25,0°.
6. Кристаллическая соль по п.1, которая представляет собой кристаллическую трис(гидроксиметил)метиламмониевую соль (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]-пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты, в порошковой рентгенограмме которой присутствуют характеристические пики при 2-тета = 7,9, 8,5, 10,2, 16,7, 18,4, 19,3, 19,8, 20,2, 21,5 и 24,9°.
7. Кристаллическая соль по п.1, которая представляет собой кристаллическую бензиламмониевую соль (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты, в порошковой рентгенограмме которой присутствуют характеристические пики при 2-тета = 6,1, 6,7, 16,8, 17,6, 18,1, 19,3, 21,1, 21,9, 23,0 и 26,8°.
8. Кристаллическая соль по п.1, которая представляет собой кристаллическую 4-метоксибензиламмониевую соль (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты, в порошковой рентгенограмме которой присутствуют характеристические пики при 2-тета = 14,2, 15,1, 17,5, 18,8, 19,7, 20,1, 20,7, 21,5, 23,7 и 24,5°.
9. Кристаллическая соль по п.1, которая представляет собой кристаллическую литиевую соль (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты, в порошковой рентгенограмме которой присутствуют характеристические пики при 2-тета=10,2, 11,0, 16,4, 17,0, 19,3, 19,8, 20,4, 20,9, 21,5 и 28,0°.
10. Кристаллическая соль по п.1, которая представляет собой кристаллическую магниевую соль (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты, в порошковой рентгенограмме которой присутствуют характеристические пики при 2-тета = 11,5, 14,5, 16,3, 16,8, 18,0, 19,1, 19,8, 21,8, 22,6 и 23,0°.
11. Фармацевтическая композиция, содержащая кристаллическую соль по любому из пп.1-10 в смеси с фармацевтически приемлемым разбавителем или носителем.
12. Способ получения кристаллической соли по любому из пп.2-9, включающий добавление соответствующего амина или основания к раствору (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты в ацетонитриле или этилацетате.
13. Применение кристаллической соли по любому из пп.1-10 для получения аморфной кальциевой соли (Е)-7-[4-(4-фторфенил)-6-изопропил-2-[метил(метилсульфонил)амино]пиримидин-5-ил]-(3R,5S)-3,5-дигидроксигепт-6-еновой кислоты.
14. Применение кристаллической соли по п.13, где используемая кристаллическая соль представляет собой соль метиламмония по п.3.
15. Применение кристаллической соли по любому из пп.1-10 для получения лекарственного средства.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0003305.0 | 2000-02-15 | ||
| GBGB0003305.0A GB0003305D0 (en) | 2000-02-15 | 2000-02-15 | Pyrimidine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2002124621A true RU2002124621A (ru) | 2004-01-10 |
| RU2265599C2 RU2265599C2 (ru) | 2005-12-10 |
Family
ID=9885517
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2002124621/04A RU2265599C2 (ru) | 2000-02-15 | 2001-02-12 | Кристаллические соли 7-[4-(4-фторфенил)-6-изопропил-2-[метил (метилсульфонил) амино]пиримидин-5-ил]-(3r,5s)-3,5-дигидроксигепт-6-еновой кислоты, способ их получения и фармацевтическая композиция |
Country Status (36)
| Country | Link |
|---|---|
| US (2) | US6841554B2 (ru) |
| EP (2) | EP1263739B9 (ru) |
| JP (1) | JP4099333B2 (ru) |
| KR (1) | KR100708262B1 (ru) |
| CN (1) | CN1210266C (ru) |
| AR (1) | AR029228A1 (ru) |
| AT (2) | ATE449079T1 (ru) |
| AU (1) | AU775569B2 (ru) |
| BG (1) | BG65562B1 (ru) |
| BR (1) | BR0108378A (ru) |
| CA (1) | CA2397450C (ru) |
| CO (1) | CO5280213A1 (ru) |
| CY (2) | CY1107225T1 (ru) |
| CZ (1) | CZ302136B6 (ru) |
| DE (2) | DE60140581D1 (ru) |
| DK (2) | DK1873148T3 (ru) |
| EE (1) | EE05288B1 (ru) |
| ES (2) | ES2335542T3 (ru) |
| GB (1) | GB0003305D0 (ru) |
| HK (2) | HK1051532A1 (ru) |
| HU (1) | HU228422B1 (ru) |
| IL (2) | IL150807A0 (ru) |
| IS (1) | IS2592B (ru) |
| MX (1) | MXPA02007819A (ru) |
| MY (1) | MY129018A (ru) |
| NO (1) | NO323770B1 (ru) |
| NZ (1) | NZ520032A (ru) |
| PL (1) | PL206729B1 (ru) |
| PT (2) | PT1263739E (ru) |
| RU (1) | RU2265599C2 (ru) |
| SA (1) | SA01220166B1 (ru) |
| SI (2) | SI1263739T1 (ru) |
| SK (1) | SK287144B6 (ru) |
| UA (1) | UA74567C2 (ru) |
| WO (1) | WO2001060804A1 (ru) |
| ZA (1) | ZA200205331B (ru) |
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