CN1129604C - 新的氨基酸衍生物及其作为凝血酶抑制剂的用途 - Google Patents

新的氨基酸衍生物及其作为凝血酶抑制剂的用途 Download PDF

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Publication number
CN1129604C
CN1129604C CN97196864A CN97196864A CN1129604C CN 1129604 C CN1129604 C CN 1129604C CN 97196864 A CN97196864 A CN 97196864A CN 97196864 A CN97196864 A CN 97196864A CN 1129604 C CN1129604 C CN 1129604C
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China
Prior art keywords
pab
pro
compound
mmol
formula
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Expired - Fee Related
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CN97196864A
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English (en)
Chinese (zh)
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CN1226895A (zh
Inventor
D·古斯塔夫松
J·－E·奈斯特勒姆
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AstraZeneca AB
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Astra AB
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Publication of CN1226895A publication Critical patent/CN1226895A/zh
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    • 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

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  • 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)
CN97196864A 1996-06-07 1997-06-05 新的氨基酸衍生物及其作为凝血酶抑制剂的用途 Expired - Fee Related CN1129604C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE9602263A SE9602263D0 (sv) 1996-06-07 1996-06-07 New amino acid derivatives
SE96022637 1996-06-07

Publications (2)

Publication Number Publication Date
CN1226895A CN1226895A (zh) 1999-08-25
CN1129604C true CN1129604C (zh) 2003-12-03

Family

ID=20402928

Family Applications (1)

Application Number Title Priority Date Filing Date
CN97196864A Expired - Fee Related CN1129604C (zh) 1996-06-07 1997-06-05 新的氨基酸衍生物及其作为凝血酶抑制剂的用途

Country Status (26)

Country Link
US (2) US6255301B1 (en:Method)
EP (1) EP0910573B1 (en:Method)
JP (1) JP4237824B2 (en:Method)
CN (1) CN1129604C (en:Method)
AR (1) AR008046A1 (en:Method)
AT (1) ATE231883T1 (en:Method)
AU (1) AU723420B2 (en:Method)
BR (1) BR9709560A (en:Method)
CA (1) CA2255625A1 (en:Method)
CZ (1) CZ398698A3 (en:Method)
DE (1) DE69718791T2 (en:Method)
DK (1) DK0910573T3 (en:Method)
EE (1) EE9800425A (en:Method)
ES (1) ES2191840T3 (en:Method)
HU (1) HUP0002404A3 (en:Method)
ID (1) ID17016A (en:Method)
IL (2) IL127325A0 (en:Method)
IS (1) IS4906A (en:Method)
NO (1) NO317135B1 (en:Method)
NZ (1) NZ332964A (en:Method)
PL (1) PL330482A1 (en:Method)
SE (1) SE9602263D0 (en:Method)
SK (1) SK165398A3 (en:Method)
TR (1) TR199802536T2 (en:Method)
WO (1) WO1997046577A1 (en:Method)
ZA (1) ZA974542B (en:Method)

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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
US6417161B1 (en) 1998-04-24 2002-07-09 3-Dimensional Pharmaceuticals, Inc. Amino acid amidinohydrazones, alkoxyguanidines and aminoguanidines as protease inhibitors
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
PT1150996E (pt) * 1999-01-13 2008-01-15 Astrazeneca Ab Novos derivados de amidinobenzilamina e sua utilização como inibidores da trombina
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
AU2001280395B2 (en) * 2000-08-16 2005-11-24 Astrazeneca Ab New amidino derivatives and their use as thrombin inhibitors
US6433186B1 (en) 2000-08-16 2002-08-13 Astrazeneca Ab Amidino derivatives and their use as thormbin 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
US7129233B2 (en) * 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
RU2300521C2 (ru) * 2000-12-01 2007-06-10 Астразенека Аб Новые производные миндальной кислоты и их применение в качестве ингибиторов тромбина
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
CN102083839B (zh) 2008-02-06 2014-03-26 阿斯利康(瑞典)有限公司 化合物
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
EP3052498A1 (en) 2013-09-30 2016-08-10 Council of Scientific & Industrial Research 3,7-diazabicyclo[3.3.1]nonane carboxamides as antithrombotic agents
RU2733405C2 (ru) * 2014-02-07 2020-10-01 Экзитера Фармасьютикалз Инк. Терапевтические соединения и композиции
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

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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
ZA86746B (en) 1985-02-04 1986-09-24 Merrell Dow Pharma Novel 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
ZA897515B (en) 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
TW201303B (en:Method) 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
ZA928581B (en) 1991-11-12 1994-05-06 Lilly Co Eli Antithrombotic agents
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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
WO1996024609A1 (de) 1995-02-10 1996-08-15 Basf Aktiengesellschaft Thrombininhibitoren
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
US5914319A (en) 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
WO1996031504A1 (en) 1995-04-04 1996-10-10 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
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
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Also Published As

Publication number Publication date
JP2000512631A (ja) 2000-09-26
EP0910573B1 (en) 2003-01-29
JP4237824B2 (ja) 2009-03-11
AU3114097A (en) 1998-01-05
DK0910573T3 (da) 2003-06-23
SK165398A3 (en) 1999-08-06
NO985700D0 (no) 1998-12-04
SE9602263D0 (sv) 1996-06-07
US20020019371A1 (en) 2002-02-14
NO985700L (no) 1999-02-05
ES2191840T3 (es) 2003-09-16
EE9800425A (et) 1999-06-15
IS4906A (is) 1998-11-25
US6838478B2 (en) 2005-01-04
AU723420B2 (en) 2000-08-24
CA2255625A1 (en) 1997-12-11
DE69718791D1 (de) 2003-03-06
WO1997046577A1 (en) 1997-12-11
EP0910573A1 (en) 1999-04-28
US6255301B1 (en) 2001-07-03
NO317135B1 (no) 2004-08-23
TR199802536T2 (xx) 1999-03-22
CN1226895A (zh) 1999-08-25
CZ398698A3 (cs) 1999-07-14
HUP0002404A3 (en) 2001-02-28
ATE231883T1 (de) 2003-02-15
PL330482A1 (en) 1999-05-24
NZ332964A (en) 2000-08-25
HUP0002404A2 (hu) 2000-10-28
AR008046A1 (es) 1999-12-09
DE69718791T2 (de) 2003-10-23
ID17016A (id) 1997-12-04
IL127325A (en) 2006-10-31
BR9709560A (pt) 1999-08-10
ZA974542B (en) 1997-12-08
IL127325A0 (en) 1999-09-22

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C06 Publication
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C10 Entry into substantive examination
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GR01 Patent grant
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CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20031203

Termination date: 20100605