CA2255625A1 - New amino acid derivatives and their use as thrombin inhibitors - Google Patents
New amino acid derivatives and their use as thrombin inhibitors Download PDFInfo
- Publication number
- CA2255625A1 CA2255625A1 CA002255625A CA2255625A CA2255625A1 CA 2255625 A1 CA2255625 A1 CA 2255625A1 CA 002255625 A CA002255625 A CA 002255625A CA 2255625 A CA2255625 A CA 2255625A CA 2255625 A1 CA2255625 A1 CA 2255625A1
- Authority
- CA
- Canada
- Prior art keywords
- pab
- ch2oh
- pro
- compound
- mmol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE9602263A SE9602263D0 (sv) | 1996-06-07 | 1996-06-07 | New amino acid derivatives |
| SE9602263-7 | 1996-06-07 | ||
| PCT/SE1997/000989 WO1997046577A1 (en) | 1996-06-07 | 1997-06-05 | New amino acid derivatives and their use as thrombin inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2255625A1 true CA2255625A1 (en) | 1997-12-11 |
Family
ID=20402928
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002255625A Abandoned CA2255625A1 (en) | 1996-06-07 | 1997-06-05 | New amino acid derivatives and their use as thrombin inhibitors |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US6255301B1 (enExample) |
| EP (1) | EP0910573B1 (enExample) |
| JP (1) | JP4237824B2 (enExample) |
| CN (1) | CN1129604C (enExample) |
| AR (1) | AR008046A1 (enExample) |
| AT (1) | ATE231883T1 (enExample) |
| AU (1) | AU723420B2 (enExample) |
| BR (1) | BR9709560A (enExample) |
| CA (1) | CA2255625A1 (enExample) |
| CZ (1) | CZ398698A3 (enExample) |
| DE (1) | DE69718791T2 (enExample) |
| DK (1) | DK0910573T3 (enExample) |
| EE (1) | EE9800425A (enExample) |
| ES (1) | ES2191840T3 (enExample) |
| HU (1) | HUP0002404A3 (enExample) |
| ID (1) | ID17016A (enExample) |
| IL (2) | IL127325A0 (enExample) |
| IS (1) | IS4906A (enExample) |
| NO (1) | NO317135B1 (enExample) |
| NZ (1) | NZ332964A (enExample) |
| PL (1) | PL330482A1 (enExample) |
| SE (1) | SE9602263D0 (enExample) |
| SK (1) | SK165398A3 (enExample) |
| TR (1) | TR199802536T2 (enExample) |
| WO (1) | WO1997046577A1 (enExample) |
| ZA (1) | ZA974542B (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SA96170106A (ar) * | 1995-07-06 | 2005-12-03 | أسترا أكتيبولاج | مشتقات حامض أميني جديدة |
| 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 |
| SE9704543D0 (sv) * | 1997-12-05 | 1997-12-05 | Astra Ab | New compounds |
| JP2003529528A (ja) | 1998-04-24 | 2003-10-07 | ３−ディメンショナル ファーマシューティカルズ， インコーポレイテッド | プロテアーゼインヒビターとしてのアミノ酸アミジノヒドラゾン、アルコキシグアニジン、およびアミノグアニジン |
| SE9804313D0 (sv) | 1998-12-14 | 1998-12-14 | Astra Ab | New compounds |
| WO2000042059A1 (en) * | 1999-01-13 | 2000-07-20 | Astrazeneca Ab | New amidinobenzylamine derivatives and their use as thrombin inhibitors |
| AR023510A1 (es) | 1999-04-21 | 2002-09-04 | Astrazeneca Ab | Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina. |
| SE9902270D0 (sv) * | 1999-06-16 | 1999-06-16 | Astra Ab | Pharmaceutically active compounds |
| 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 |
| SI1311480T1 (sl) * | 2000-08-16 | 2008-12-31 | Astrazeneca Ab | Novi amidino derivati in njihova uporaba kot trombinski inhibitorji |
| 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 |
| RU2300521C2 (ru) * | 2000-12-01 | 2007-06-10 | Астразенека Аб | Новые производные миндальной кислоты и их применение в качестве ингибиторов тромбина |
| US7129233B2 (en) * | 2000-12-01 | 2006-10-31 | Astrazeneca Ab | Mandelic acid derivatives and their use as thrombin inhibitors |
| 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 |
| TW200827336A (en) * | 2006-12-06 | 2008-07-01 | Astrazeneca Ab | New crystalline forms |
| US20090061000A1 (en) * | 2007-08-31 | 2009-03-05 | Astrazeneca Ab | Pharmaceutical formulation use 030 |
| PL2242759T3 (pl) | 2008-02-06 | 2013-06-28 | Astrazeneca Ab | Związki |
| GB0913342D0 (en) | 2009-07-31 | 2009-09-16 | Astrazeneca Ab | Compounds - 801 |
| KR101181918B1 (ko) * | 2010-11-09 | 2012-09-11 | 주식회사 세라젬 | 온열치료기용 상하운동 조절장치 |
| WO2015044951A1 (en) | 2013-09-30 | 2015-04-02 | Council Of Scientific & Industrial Research | 3,7-diazabicyclo[3.3.1 ]nonane carboxamides as antithrombotic agents |
| JP6382997B2 (ja) * | 2014-02-07 | 2018-08-29 | エクセセーラ ファーマシューティカルズ インコーポレイテッド | 治療用化合物および組成物 |
| CN108530297B (zh) * | 2017-03-03 | 2021-09-24 | 联化科技股份有限公司 | 2-氯-3-甲基苯甲酸及其中间体的制备方法 |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU178398B (en) | 1979-06-12 | 1982-04-28 | Gyogyszerkutato Intezet | Process for producing new agmatine derivatives of activity against haemagglutination |
| 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 |
| EP0362002B1 (en) | 1988-09-01 | 1995-07-26 | Merrell Dow Pharmaceuticals Inc. | HIV protease inhibitors |
| ZA897514B (en) | 1988-10-07 | 1990-06-27 | Merrell Dow Pharma | Novel peptidase inhibitors |
| TW201303B (enExample) | 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 |
| NZ245039A (en) | 1991-11-12 | 1994-12-22 | Lilly Co Eli | N-phenylalanyl and n-phenylglycyl derivatives of the dipeptide of l-azetidine-2-carboxylic acid and l-arginine aldehyde; anti-blood clotting compositions |
| SE9103612D0 (sv) | 1991-12-04 | 1991-12-04 | Astra Ab | New peptide derivatives |
| WO1993018060A1 (en) | 1992-03-04 | 1993-09-16 | Gyógyszerkutató Intézet Kft. | New anticoagulant peptide derivatives and pharmaceutical compositions containing the same as well as a process for the preparation thereof |
| TW223629B (enExample) | 1992-03-06 | 1994-05-11 | Hoffmann La Roche | |
| US5583146A (en) | 1992-12-02 | 1996-12-10 | Bristol-Myers Squibb Company | Heterocyclic thrombin inhibitors |
| AU675981B2 (en) | 1992-12-02 | 1997-02-27 | Bristol-Myers Squibb Company | Guanidinyl-substituted heterocyclic thrombin inhibitors |
| JPH06340619A (ja) | 1993-05-03 | 1994-12-13 | Bristol Myers Squibb Co | グアニジニルまたはアミジニル置換メチルアミノ複素環トロンビン抑制剤 |
| US5780631A (en) | 1993-06-03 | 1998-07-14 | Astra Aktiebolag | Starting materials in the synthesis of thrombin and kininogenase inhibitors |
| 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 |
| CA2140598C (en) | 1994-01-27 | 2010-03-09 | Masahiro Ohshima | Prolineamide derivatives |
| US5707966A (en) | 1994-03-04 | 1998-01-13 | Eli Lilly And Company | Antithrombotic agents |
| US5705487A (en) | 1994-03-04 | 1998-01-06 | Eli Lilly And Company | Antithrombotic agents |
| IL112795A (en) * | 1994-03-04 | 2001-01-28 | Astrazeneca Ab | Peptide derivatives as antithrombic agents their preparation and pharmaceutical compositions containing them |
| US5726159A (en) | 1994-03-04 | 1998-03-10 | 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 |
| US5510369A (en) | 1994-07-22 | 1996-04-23 | Merck & Co., Inc. | Pyrrolidine thrombin inhibitors |
| DE4443390A1 (de) | 1994-12-06 | 1996-06-13 | Basf Ag | Neue dipeptidische p-Amidinobenzylamide mit N-terminalen Sulfonyl- bzw. Aminosulfonylresten |
| HUP9800634A3 (en) | 1995-02-10 | 2000-04-28 | Abbott Gmbh & Co Kg | P-amidino-benzylamide derivatives as thrombin inhibitors, intermediates and use thereof |
| KR100388185B1 (ko) * | 1995-02-17 | 2003-11-28 | 애보트 게엠베하 운트 콤파니 카게 | 트롬빈 억제제로서의 신규 디펩티드 아미딘 |
| US5914319A (en) | 1995-02-27 | 1999-06-22 | Eli Lilly And Company | Antithrombotic agents |
| US5710130A (en) | 1995-02-27 | 1998-01-20 | Eli Lilly And Company | Antithrombotic agents |
| JPH11503161A (ja) | 1995-04-04 | 1999-03-23 | メルク エンド カンパニー インコーポレーテッド | トロンビン阻害剤 |
| 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 |
| TWI238827B (en) | 1995-12-21 | 2005-09-01 | Astrazeneca Ab | Prodrugs of thrombin inhibitors |
| JPH1095898A (ja) | 1996-09-25 | 1998-04-14 | Sumitomo Bakelite Co Ltd | 難燃性樹脂組成物およびこれを用いた積層板 |
| DE19632772A1 (de) | 1996-08-14 | 1998-02-19 | Basf Ag | Neue Benzamidine |
| DE19632773A1 (de) | 1996-08-14 | 1998-02-19 | Basf Ag | Neue Thrombininhibitoren |
| SE9704543D0 (sv) * | 1997-12-05 | 1997-12-05 | Astra Ab | New compounds |
-
1996
- 1996-06-07 SE SE9602263A patent/SE9602263D0/xx unknown
-
1997
- 1997-05-23 ZA ZA9704542A patent/ZA974542B/xx unknown
- 1997-06-03 ID IDP971884A patent/ID17016A/id unknown
- 1997-06-05 WO PCT/SE1997/000989 patent/WO1997046577A1/en not_active Ceased
- 1997-06-05 US US08/860,871 patent/US6255301B1/en not_active Expired - Fee Related
- 1997-06-05 BR BR9709560A patent/BR9709560A/pt active Search and Examination
- 1997-06-05 NZ NZ332964A patent/NZ332964A/xx not_active IP Right Cessation
- 1997-06-05 CN CN97196864A patent/CN1129604C/zh not_active Expired - Fee Related
- 1997-06-05 EE EE9800425A patent/EE9800425A/xx unknown
- 1997-06-05 EP EP97926356A patent/EP0910573B1/en not_active Expired - Lifetime
- 1997-06-05 CZ CZ983986A patent/CZ398698A3/cs unknown
- 1997-06-05 PL PL97330482A patent/PL330482A1/xx unknown
- 1997-06-05 CA CA002255625A patent/CA2255625A1/en not_active Abandoned
- 1997-06-05 IL IL12732597A patent/IL127325A0/xx active IP Right Grant
- 1997-06-05 SK SK1653-98A patent/SK165398A3/sk unknown
- 1997-06-05 AT AT97926356T patent/ATE231883T1/de not_active IP Right Cessation
- 1997-06-05 AU AU31140/97A patent/AU723420B2/en not_active Ceased
- 1997-06-05 HU HU0002404A patent/HUP0002404A3/hu unknown
- 1997-06-05 JP JP50050298A patent/JP4237824B2/ja not_active Expired - Fee Related
- 1997-06-05 ES ES97926356T patent/ES2191840T3/es not_active Expired - Lifetime
- 1997-06-05 TR TR1998/02536T patent/TR199802536T2/xx unknown
- 1997-06-05 DK DK97926356T patent/DK0910573T3/da active
- 1997-06-05 DE DE69718791T patent/DE69718791T2/de not_active Expired - Fee Related
- 1997-06-06 AR ARP970102484A patent/AR008046A1/es not_active Application Discontinuation
-
1998
- 1998-11-25 IS IS4906A patent/IS4906A/is unknown
- 1998-11-30 IL IL127325A patent/IL127325A/en not_active IP Right Cessation
- 1998-12-04 NO NO19985700A patent/NO317135B1/no not_active IP Right Cessation
-
2001
- 2001-04-30 US US09/844,427 patent/US6838478B2/en not_active Expired - Fee Related
Also Published As
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|---|---|---|
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Discontinued |