RU2004133388A - Новые соли - Google Patents
Новые соли Download PDFInfo
- Publication number
- RU2004133388A RU2004133388A RU2004133388/04A RU2004133388A RU2004133388A RU 2004133388 A RU2004133388 A RU 2004133388A RU 2004133388/04 A RU2004133388/04 A RU 2004133388/04A RU 2004133388 A RU2004133388 A RU 2004133388A RU 2004133388 A RU2004133388 A RU 2004133388A
- Authority
- RU
- Russia
- Prior art keywords
- addition salt
- acid addition
- acid
- ochf
- salt according
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
Claims (19)
1. Фармацевтически приемлемая соль присоединения кислоты соединения формулы I
где R1 представляет собой С1-2алкил, замещенный одним или более чем одним заместителем фторо;
R2 представляет собой С1-2алкил; и
n равно 0, 1 или 2.
2. Соль присоединения кислоты по п.1, где кислота представляет собой сульфоновую кислоту.
3. Соль присоединения кислоты по п.1, где кислота представляет собой этансульфоновую кислоту, н-пропансульфоновую кислоту, бензолсульфоновую кислоту, 1,5-нафталиндисульфоновую кислоту или н-бутансульфоновую кислоту.
4. Соль присоединения кислоты по п.1, где R1 представляет собой -OCHF2 или -OCH2CH2F.
5. Соль присоединения кислоты по п.1, где R2 представляет собой метил.
6. Соль присоединения кислоты по п.1, где n равно 0 или 2.
7. Соль присоединения кислоты по п.1, где соединение формулы I представляет собой
Ph(3-Cl)(5-OCHF2)-(R)СН(ОН)С(O)-(S)Aze-Pab(ОМе) или
Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-(S)Aze-Pab(2,6-диF)(OMe).
8. Соль присоединения кислоты по п.1 в по существу кристаллической форме.
9. Соль присоединения кислоты по п.1 в частично кристаллической форме.
10. Соль присоединения кислоты по пп.1-8, где n равно 0, в по существу кристаллической форме.
11. Соль присоединения кислоты по пп.1-7 или 9, где n равно 2, в частично кристаллической форме.
12. Соль присоединения кислоты по пп.1-8, которая представляет собой соль бензолсульфоновой кислоты Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-(S)Aze-Pab(OMe), характеризующаяся картиной дифракции рентгеновских лучей на порошке, характеризующейся пиками со значениями d равными 5,9, 4,73, 4,09 и 4,08 A.
13. Соль присоединения кислоты по пп.1-7 или 9, которая представляет собой соль геми-1,5-нафталиндисульфоновой кислоты Ph(3-Cl)(5-OCHF2)-(R)СН(ОН)С(O)-(5)Aze-Pab(2,6-диF)(ОМе), характеризующаяся картиной дифракции рентгеновских лучей на порошке, характеризующейся пиками со значениями d равными 18,3, 9,1, 5,6, 5,5, 4,13, 4,02, 3,86, 3,69 и 3,63 A.
14. Способ получения соли присоединения кислоты по любому из пп.1-13, который включает добавление кислоты к соединению формулы I, как оно определено в п.1.
15. Способ получения соли присоединения кислоты по п.14, который включает кристаллизацию соли присоединения кислоты, как она определена в любом из пп.1-13.
16. Фармацевтический препарат, включающий соль присоединения кислоты по любому из пп.1-13 в смеси с фармацевтически приемлемым адъювантом, разбавителем или носителем.
17. Соль присоединения кислоты по любому из пп.1-9 для применения в лечении состояния, при котором требуется ингибирование тромбина.
18. Применение соли присоединения кислоты по любому из пп.1-13 в качестве ингредиента для изготовления лекарственного средства для лечения состояния, при котором требуется ингибирование тромбина.
19. Способ лечения состояния, при котором требуется ингибирование тромбина, включающий введение терапевтически эффективного количества соли присоединения кислоты по любому из пп.1-13 субъекту, страдающему от такого состояния или подверженному ему.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0201661A SE0201661D0 (sv) | 2002-05-31 | 2002-05-31 | New salts |
| SE0201661-6 | 2002-05-31 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008127541/04A Division RU2008127541A (ru) | 2002-05-31 | 2008-07-09 | Новые соли |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2004133388A true RU2004133388A (ru) | 2005-07-10 |
| RU2345064C2 RU2345064C2 (ru) | 2009-01-27 |
Family
ID=20288039
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2004133388/04A RU2345064C2 (ru) | 2002-05-31 | 2003-05-27 | Фармацевтически приемлемые соли присоединения сульфоновой кислоты метоксиамидинового соединения и способ их получения |
| RU2008127541/04A RU2008127541A (ru) | 2002-05-31 | 2008-07-09 | Новые соли |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008127541/04A RU2008127541A (ru) | 2002-05-31 | 2008-07-09 | Новые соли |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US7273858B2 (ru) |
| EP (2) | EP1513806B1 (ru) |
| JP (1) | JP4541140B2 (ru) |
| KR (1) | KR20050009726A (ru) |
| CN (2) | CN1656067A (ru) |
| AR (1) | AR039937A1 (ru) |
| AT (1) | ATE425963T1 (ru) |
| AU (1) | AU2003232871B2 (ru) |
| BR (1) | BR0311365A (ru) |
| CA (1) | CA2487509A1 (ru) |
| CY (1) | CY1109085T1 (ru) |
| DE (1) | DE60326720D1 (ru) |
| DK (1) | DK1513806T3 (ru) |
| ES (1) | ES2322048T3 (ru) |
| HK (1) | HK1073102A1 (ru) |
| IL (1) | IL165295A0 (ru) |
| IS (1) | IS7598A (ru) |
| MX (1) | MXPA04011912A (ru) |
| MY (1) | MY133333A (ru) |
| NO (1) | NO329064B1 (ru) |
| NZ (2) | NZ536738A (ru) |
| PL (1) | PL373794A1 (ru) |
| PT (1) | PT1513806E (ru) |
| RU (2) | RU2345064C2 (ru) |
| SA (1) | SA03240440B1 (ru) |
| SE (1) | SE0201661D0 (ru) |
| SI (1) | SI1513806T1 (ru) |
| TW (2) | TWI313173B (ru) |
| UA (1) | UA81246C2 (ru) |
| WO (1) | WO2003101957A1 (ru) |
| ZA (1) | ZA200409228B (ru) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR035216A1 (es) | 2000-12-01 | 2004-05-05 | Astrazeneca Ab | Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios |
| AR034517A1 (es) | 2001-06-21 | 2004-02-25 | Astrazeneca Ab | Formulacion farmaceutica |
| SE0201659D0 (sv) | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | Modified release pharmaceutical formulation |
| SE0201661D0 (sv) * | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | New salts |
| US7781424B2 (en) * | 2003-05-27 | 2010-08-24 | Astrazeneca Ab | Modified release pharmaceutical formulation |
| JP4550884B2 (ja) * | 2004-04-09 | 2010-09-22 | ハンミ ファーム． シーオー．， エルティーディー． | 結晶性クロピドグレルナフタレンスルホン酸塩又はその水和物、その製造方法及びそれを含む医薬組成物 |
| BRPI0510008A (pt) * | 2004-04-20 | 2007-09-18 | Sanofi Aventis | sal de clopidogrel e formas polimórficas deste |
| TW200827336A (en) * | 2006-12-06 | 2008-07-01 | Astrazeneca Ab | New crystalline forms |
| TW200900033A (en) * | 2007-06-21 | 2009-01-01 | Wen-Qing Li | Automatic brewing machine |
| US20090061000A1 (en) * | 2007-08-31 | 2009-03-05 | Astrazeneca Ab | Pharmaceutical formulation use 030 |
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| DE19632772A1 (de) | 1996-08-14 | 1998-02-19 | Basf Ag | Neue Benzamidine |
| SE9603724D0 (sv) | 1996-10-11 | 1996-10-11 | Astra Ab | New pharmaceutical parenteral formulation of a thrombin inhibitor |
| AR013084A1 (es) | 1997-06-19 | 2000-12-13 | Astrazeneca Ab | Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados |
| IT1297461B1 (it) | 1997-10-29 | 1999-12-17 | Ciocca Maurizio | Preparazione di compresse a rilascio controllato a base di complessi tra carragenano e farmaci basici solubili |
| SE9704543D0 (sv) | 1997-12-05 | 1997-12-05 | Astra Ab | New compounds |
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| SE9802973D0 (sv) | 1998-09-03 | 1998-09-03 | Astra Ab | Immediate release tablet |
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| US6811794B2 (en) * | 2001-12-20 | 2004-11-02 | Shire Laboratories, Inc. | Sustained release pharmaceutical dosage forms with minimized pH dependent dissolution profiles |
| SE0201659D0 (sv) * | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | Modified release pharmaceutical formulation |
| SE0201661D0 (sv) * | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | New salts |
| SE0201658D0 (sv) * | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | Immediate release pharmaceutical formulation |
| US7781424B2 (en) * | 2003-05-27 | 2010-08-24 | Astrazeneca Ab | Modified release pharmaceutical formulation |
| SE0303220D0 (sv) * | 2003-11-28 | 2003-11-28 | Astrazeneca Ab | New process |
| GB0503672D0 (en) * | 2005-02-23 | 2005-03-30 | Astrazeneca Ab | New process |
| GB0510546D0 (en) * | 2005-05-24 | 2005-06-29 | Astrazeneca Ab | New process |
| TW200827336A (en) * | 2006-12-06 | 2008-07-01 | Astrazeneca Ab | New crystalline forms |
-
2002
- 2002-05-31 SE SE0201661A patent/SE0201661D0/xx unknown
-
2003
- 2003-05-27 NZ NZ536738A patent/NZ536738A/en not_active IP Right Cessation
- 2003-05-27 SI SI200331578T patent/SI1513806T1/sl unknown
- 2003-05-27 IL IL16529503A patent/IL165295A0/xx unknown
- 2003-05-27 DE DE60326720T patent/DE60326720D1/de not_active Expired - Lifetime
- 2003-05-27 PT PT03728206T patent/PT1513806E/pt unknown
- 2003-05-27 AT AT03728206T patent/ATE425963T1/de not_active IP Right Cessation
- 2003-05-27 WO PCT/SE2003/000859 patent/WO2003101957A1/en active Application Filing
- 2003-05-27 NZ NZ554323A patent/NZ554323A/en not_active IP Right Cessation
- 2003-05-27 JP JP2004509651A patent/JP4541140B2/ja not_active Expired - Fee Related
- 2003-05-27 DK DK03728206T patent/DK1513806T3/da active
- 2003-05-27 RU RU2004133388/04A patent/RU2345064C2/ru not_active IP Right Cessation
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