AR039937A1 - Derivados de azetidina como inhibidores de tripsina proteasas - Google Patents
Derivados de azetidina como inhibidores de tripsina proteasasInfo
- Publication number
- AR039937A1 AR039937A1 ARP030101935A ARP030101935A AR039937A1 AR 039937 A1 AR039937 A1 AR 039937A1 AR P030101935 A ARP030101935 A AR P030101935A AR P030101935 A ARP030101935 A AR P030101935A AR 039937 A1 AR039937 A1 AR 039937A1
- Authority
- AR
- Argentina
- Prior art keywords
- inhibitors
- tripsine
- azetidine
- proteases
- derivatives
- 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
Abstract
Sales de adición ácida aceptables para uso farmacéutico de compuestos de fórmula (1), donde R1 representa C1-2 alquilo sustituido por uno o más sustituyentes fluoro; R2 representa C1-2 alquilo; y n representa 0, 1 o 2, donde las sales son útiles como prodrogas de inhibidores competitivos de tripsina proteasas tales como la trombina, y por consiguiente, en particular, en el tratamiento de trastornos en la que requiere de la inhibición de la trombina (por ejemplo, trombosis), o como anticoagulantes.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE0201661A SE0201661D0 (sv) | 2002-05-31 | 2002-05-31 | New salts |
Publications (1)
Publication Number | Publication Date |
---|---|
AR039937A1 true AR039937A1 (es) | 2005-03-09 |
Family
ID=20288039
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030101935A AR039937A1 (es) | 2002-05-31 | 2003-05-30 | Derivados de azetidina como inhibidores de tripsina proteasas |
Country Status (31)
Country | Link |
---|---|
US (2) | US7273858B2 (es) |
EP (2) | EP1513806B1 (es) |
JP (1) | JP4541140B2 (es) |
KR (1) | KR20050009726A (es) |
CN (2) | CN1656067A (es) |
AR (1) | AR039937A1 (es) |
AT (1) | ATE425963T1 (es) |
AU (1) | AU2003232871B2 (es) |
BR (1) | BR0311365A (es) |
CA (1) | CA2487509A1 (es) |
CY (1) | CY1109085T1 (es) |
DE (1) | DE60326720D1 (es) |
DK (1) | DK1513806T3 (es) |
ES (1) | ES2322048T3 (es) |
HK (1) | HK1073102A1 (es) |
IL (1) | IL165295A0 (es) |
IS (1) | IS7598A (es) |
MX (1) | MXPA04011912A (es) |
MY (1) | MY133333A (es) |
NO (1) | NO329064B1 (es) |
NZ (2) | NZ536738A (es) |
PL (1) | PL373794A1 (es) |
PT (1) | PT1513806E (es) |
RU (2) | RU2345064C2 (es) |
SA (1) | SA03240440B1 (es) |
SE (1) | SE0201661D0 (es) |
SI (1) | SI1513806T1 (es) |
TW (2) | TWI313173B (es) |
UA (1) | UA81246C2 (es) |
WO (1) | WO2003101957A1 (es) |
ZA (1) | ZA200409228B (es) |
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 |
Family Cites Families (74)
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HU178398B (en) | 1979-06-12 | 1982-04-28 | Gyogyszerkutato Intezet | Process for producing new agmatine derivatives of activity against haemagglutination |
JPS57149217A (en) | 1981-03-11 | 1982-09-14 | Kaken Pharmaceut Co Ltd | Slow-releasing pharmaceutical preparation |
HU192646B (en) | 1984-12-21 | 1987-06-29 | Gyogyszerkutato Intezet | Process for preparing new n-alkyl-peptide aldehydes |
CA1341029C (en) | 1985-02-04 | 2000-06-20 | Michael Kolb | Peptidase inhibitors |
US5187157A (en) | 1987-06-05 | 1993-02-16 | Du Pont Merck Pharmaceutical Company | Peptide boronic acid inhibitors of trypsin-like proteases |
US4792452A (en) | 1987-07-28 | 1988-12-20 | E. R. Squibb & Sons, Inc. | Controlled release formulation |
EP0362002B1 (en) | 1988-09-01 | 1995-07-26 | Merrell Dow Pharmaceuticals Inc. | HIV protease inhibitors |
ZA897515B (en) | 1988-10-07 | 1990-06-27 | Merrell Dow Pharma | Novel peptidase inhibitors |
IT1229491B (it) * | 1988-12-28 | 1991-09-03 | Roussel Maestretti S P A Ora R | Derivati della 1,2,5,6-tetraidropiridina, loro procedimento di preparazione e loro impiego come sostanze medicinali |
TW201303B (es) * | 1990-07-05 | 1993-03-01 | Hoffmann La Roche | |
CA2075154A1 (en) | 1991-08-06 | 1993-02-07 | Neelakantan Balasubramanian | Peptide aldehydes as antithrombotic agents |
SE9102462D0 (sv) | 1991-08-28 | 1991-08-28 | Astra Ab | New isosteric peptides |
US5169638A (en) | 1991-10-23 | 1992-12-08 | E. R. Squibb & Sons, Inc. | Buoyant controlled release powder formulation |
ZA928581B (en) | 1991-11-12 | 1994-05-06 | Lilly Co Eli | Antithrombotic agents |
SE9103612D0 (sv) | 1991-12-04 | 1991-12-04 | Astra Ab | New peptide derivatives |
JPH08501057A (ja) | 1992-03-04 | 1996-02-06 | ヂョヂセルクタトー インテーゼット カーエフテー | 新規な抗凝結因子ペプチド誘導体及びそれを含有する製薬学的組成物及びその製造方法 |
TW223629B (es) | 1992-03-06 | 1994-05-11 | Hoffmann La Roche | |
US6984627B1 (en) | 1993-06-03 | 2006-01-10 | Astrazeneca Ab | Peptide derivatives |
US5783563A (en) | 1993-06-03 | 1998-07-21 | Astra Aktiebolag | Method for treatment or prophylaxis of venous thrombosis |
SE9301912D0 (sv) | 1993-06-03 | 1993-06-03 | Ab Astra | Process for the production of aminoalkylguandines |
SE9301916D0 (sv) | 1993-06-03 | 1993-06-03 | Ab Astra | New peptides derivatives |
EP0648780A1 (en) | 1993-08-26 | 1995-04-19 | Bristol-Myers Squibb Company | Heterocyclic thrombin inhibitors |
TW394760B (en) | 1993-09-07 | 2000-06-21 | Hoffmann La Roche | Novel Carboxamides, process for their preparation and pharmaceutical composition containing the same |
AU1025795A (en) | 1994-01-27 | 1995-08-03 | Mitsubishi Chemical Corporation | Prolineamide derivatives |
US5705487A (en) | 1994-03-04 | 1998-01-06 | Eli Lilly And Company | Antithrombotic agents |
IL112795A (en) | 1994-03-04 | 2001-01-28 | Astrazeneca Ab | Derivatives of peptides as antithrombotic drugs, their preparation, and pharmaceutical preparations containing them |
US5707966A (en) | 1994-03-04 | 1998-01-13 | Eli Lilly And Company | Antithrombotic agents |
US5561146A (en) | 1994-06-10 | 1996-10-01 | Bristol-Myers Squibb Company | Modified guanidino and amidino thrombin inhibitors |
DE4421052A1 (de) * | 1994-06-17 | 1995-12-21 | Basf Ag | Neue Thrombininhibitoren, ihre Herstellung und Verwendung |
US5498724A (en) | 1994-06-28 | 1996-03-12 | Aktiebolaget Astra | Pyrazoleamidine compounds |
US5510369A (en) | 1994-07-22 | 1996-04-23 | Merck & Co., Inc. | Pyrrolidine thrombin inhibitors |
NZ302649A (en) | 1995-02-17 | 2000-01-28 | Basf Ag | Dipeptide amidine derivatives, preparation and pharmaceutical compositions thereof |
US5710130A (en) | 1995-02-27 | 1998-01-20 | Eli Lilly And Company | Antithrombotic agents |
US6083532A (en) * | 1995-03-01 | 2000-07-04 | Duramed Pharmaceuticals, Inc. | Sustained release formulation containing three different types of polymers and tablet formed therefrom |
US5695781A (en) | 1995-03-01 | 1997-12-09 | Hallmark Pharmaceuticals, Inc. | Sustained release formulation containing three different types of polymers |
EP0820453A4 (en) | 1995-04-04 | 2001-08-29 | Merck & Co Inc | THROMBIN INHIBITORS |
US5629324A (en) | 1995-04-10 | 1997-05-13 | Merck & Co., Inc. | Thrombin inhibitors |
SA96170106A (ar) | 1995-07-06 | 2005-12-03 | أسترا أكتيبولاج | مشتقات حامض أميني جديدة |
TW541316B (en) | 1995-12-21 | 2003-07-11 | Astrazeneca Ab | Prodrugs of thrombin inhibitors |
SE9601556D0 (sv) | 1996-04-24 | 1996-04-24 | Astra Ab | New pharmaceutical formulation of a thrombin inhibitor for parenteral use |
SE9602263D0 (sv) | 1996-06-07 | 1996-06-07 | Astra Ab | New amino acid derivatives |
CA2258915A1 (en) * | 1996-06-25 | 1997-12-31 | Michael Robert Wiley | Anticoagulant agents |
SE9602646D0 (sv) | 1996-07-04 | 1996-07-04 | Astra Ab | Pharmaceutically-useful compounds |
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 |
US6251430B1 (en) | 1998-02-04 | 2001-06-26 | Guohua Zhang | Water insoluble polymer based sustained release formulation |
US6174913B1 (en) | 1998-06-05 | 2001-01-16 | The University Of North Carolina At Chapel Hill | Naphtho- and dihydrobenzo-thiophene derivatives as cytotoxic antitumor agents |
SE9802938D0 (sv) | 1998-09-01 | 1998-09-01 | Astra Ab | Improved stability for injection solutions |
SE9802973D0 (sv) | 1998-09-03 | 1998-09-03 | Astra Ab | Immediate release tablet |
SE9802974D0 (sv) | 1998-09-03 | 1998-09-03 | Astra Ab | New crystalline forms |
ATE363292T1 (de) | 1998-09-04 | 2007-06-15 | Scios Inc | Hydrogelzusammensetzungen mit kontrollierter freigabe von wachstumsfaktoren |
SE9804313D0 (sv) | 1998-12-14 | 1998-12-14 | Astra Ab | New compounds |
EP1150996B1 (en) | 1999-01-13 | 2007-11-21 | AstraZeneca AB | New amidinobenzylamine derivatives and their use as thrombin inhibitors |
SE9902550D0 (sv) | 1999-07-02 | 1999-07-02 | Astra Ab | New crystalline forms |
SE0001803D0 (sv) | 2000-05-16 | 2000-05-16 | Astrazeneca Ab | New compounds i |
US6433186B1 (en) | 2000-08-16 | 2002-08-13 | Astrazeneca Ab | Amidino derivatives and their use as thormbin inhibitors |
WO2002014270A1 (en) | 2000-08-16 | 2002-02-21 | Astrazeneca Ab | New amidino derivatives and their use as thrombin inhibitors |
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 |
SE0102921D0 (sv) | 2001-08-30 | 2001-08-30 | Astrazeneca Ab | Pharmaceutically useful compounds |
US7129233B2 (en) * | 2000-12-01 | 2006-10-31 | Astrazeneca Ab | Mandelic acid derivatives and their use as thrombin inhibitors |
US6287599B1 (en) * | 2000-12-20 | 2001-09-11 | Shire Laboratories, Inc. | Sustained release pharmaceutical dosage forms with minimized pH dependent dissolution profiles |
AR034517A1 (es) * | 2001-06-21 | 2004-02-25 | Astrazeneca Ab | Formulacion farmaceutica |
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
- 2003-05-27 EP EP03728206A patent/EP1513806B1/en not_active Expired - Lifetime
- 2003-05-27 CN CNA038124912A patent/CN1656067A/zh active Pending
- 2003-05-27 AU AU2003232871A patent/AU2003232871B2/en not_active Ceased
- 2003-05-27 MX MXPA04011912A patent/MXPA04011912A/es active IP Right Grant
- 2003-05-27 CA CA002487509A patent/CA2487509A1/en not_active Abandoned
- 2003-05-27 BR BR0311365-5A patent/BR0311365A/pt not_active IP Right Cessation
- 2003-05-27 CN CN200910260483A patent/CN101735131A/zh active Pending
- 2003-05-27 US US10/516,422 patent/US7273858B2/en not_active Expired - Fee Related
- 2003-05-27 KR KR10-2004-7019439A patent/KR20050009726A/ko not_active Application Discontinuation
- 2003-05-27 ES ES03728206T patent/ES2322048T3/es not_active Expired - Lifetime
- 2003-05-27 EP EP09151657A patent/EP2055696A1/en not_active Withdrawn
- 2003-05-27 UA UA20041109441A patent/UA81246C2/uk unknown
- 2003-05-27 PL PL03373794A patent/PL373794A1/xx not_active Application Discontinuation
- 2003-05-29 MY MYPI20031981A patent/MY133333A/en unknown
- 2003-05-30 AR ARP030101935A patent/AR039937A1/es unknown
- 2003-05-30 TW TW092114807A patent/TWI313173B/zh active
- 2003-05-30 TW TW097151265A patent/TWI367754B/zh not_active IP Right Cessation
- 2003-12-10 SA SA3240440A patent/SA03240440B1/ar unknown
-
2004
- 2004-11-09 NO NO20044867A patent/NO329064B1/no not_active IP Right Cessation
- 2004-11-17 ZA ZA200409228A patent/ZA200409228B/en unknown
- 2004-12-15 IS IS7598A patent/IS7598A/is unknown
-
2005
- 2005-06-20 HK HK05105118.1A patent/HK1073102A1/xx not_active IP Right Cessation
-
2007
- 2007-08-16 US US11/839,842 patent/US7763597B2/en not_active Expired - Fee Related
-
2008
- 2008-07-09 RU RU2008127541/04A patent/RU2008127541A/ru not_active Application Discontinuation
-
2009
- 2009-05-20 CY CY20091100535T patent/CY1109085T1/el unknown
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Legal Events
Date | Code | Title | Description |
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