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BR9911100A - Inibidores de pirazinona protease - Google Patents

Inibidores de pirazinona protease

Info

Publication number
BR9911100A
BR9911100A BR9911100-4A BR9911100A BR9911100A BR 9911100 A BR9911100 A BR 9911100A BR 9911100 A BR9911100 A BR 9911100A BR 9911100 A BR9911100 A BR 9911100A
Authority
BR
Brazil
Prior art keywords
blood
compounds
inhibiting
formation
thrombi
Prior art date
Application number
BR9911100-4A
Other languages
English (en)
Inventor
Tiabao Lu
Bruce E Tomczuk
Thomas P Markotan
Original Assignee
Dimensional Pharm Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Dimensional Pharm Inc filed Critical Dimensional Pharm Inc
Publication of BR9911100A publication Critical patent/BR9911100A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

''INIBIDORES DE PIRAZINONA PROTEASE'' São descritos compostos de pirazinona, incluindo compostos da fórmula (I), em que X é 0, NR^ 11^ ou CH=N, R^ 3^-R^ 11^, R^ a^, R^ b^, R^ c^, W, m e n são apresentados na especificação, assim como hidratos, solvatos ou sais seus aceitáveis do ponto de vista farmacêutico. Os compostos da invenção são inibidores potentes de proteases, especialmente das proteases de serina semelhante a tripsina, tais como quimotripsina, tripsina, trombina, plasmina e fator Xa. Determinados compostos apresentam atividade antitrombótica através da inibição direta e seletiva de trombina. São descritas as composições para a inibição de perda de plaquetas sang³íneas, inibição de formação de agregados de plaquetas sang³íneas, inibição de formação de fibrina, inibição de formação de trombos, e inibição de formação de êmbolos. Outros empregos dos compostos da invenção são como anti-coagulantes quer embutidos nos materiais empregados na fabricação de dispositivos empregados na coleta de sangue, circulação de sangue e armazenagem de sangue, tais como cateteres, máquinas de diálise sang³íneas, seringas e tubos para a coleta de sangue, tubulações para sangue e stents quer fisicamente ligados a tais materiais. Além disso os compostos podem ser rotulados de modo a serem detectáveis e empregados para a visualização dos trombos in vivo.
BR9911100-4A 1998-06-11 1999-06-11 Inibidores de pirazinona protease BR9911100A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US8898998P 1998-06-11 1998-06-11
PCT/US1999/013228 WO1999064446A1 (en) 1998-06-11 1999-06-11 Pyrazinone protease inhibitors

Publications (1)

Publication Number Publication Date
BR9911100A true BR9911100A (pt) 2001-02-13

Family

ID=22214697

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9911100-4A BR9911100A (pt) 1998-06-11 1999-06-11 Inibidores de pirazinona protease

Country Status (21)

Country Link
US (2) US6204263B1 (pt)
EP (2) EP1086122B1 (pt)
JP (1) JP4554077B2 (pt)
KR (1) KR100669953B1 (pt)
CN (2) CN1769274A (pt)
AT (2) ATE461210T1 (pt)
AU (1) AU759427B2 (pt)
BR (1) BR9911100A (pt)
CA (1) CA2334679C (pt)
DE (2) DE69942159D1 (pt)
DK (1) DK1086122T3 (pt)
EA (1) EA004884B1 (pt)
ES (2) ES2249012T3 (pt)
HU (1) HUP0103283A3 (pt)
IL (1) IL139867A0 (pt)
NO (1) NO20006300L (pt)
NZ (1) NZ508669A (pt)
PL (1) PL344749A1 (pt)
SI (1) SI1086122T1 (pt)
WO (1) WO1999064446A1 (pt)
ZA (1) ZA200007306B (pt)

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Also Published As

Publication number Publication date
PL344749A1 (en) 2001-11-19
SI1086122T1 (sl) 2006-02-28
ZA200007306B (en) 2001-06-13
DE69926884T2 (de) 2006-06-14
HUP0103283A2 (hu) 2002-04-29
NO20006300L (no) 2001-02-12
HUP0103283A3 (en) 2002-05-28
ES2343120T3 (es) 2010-07-23
KR100669953B1 (ko) 2007-01-18
WO1999064446A1 (en) 1999-12-16
AU759427B2 (en) 2003-04-17
DE69926884D1 (de) 2005-09-29
ATE461210T1 (de) 2010-04-15
EP1589029A3 (en) 2006-01-18
ES2249012T3 (es) 2006-03-16
JP2002517512A (ja) 2002-06-18
AU4561899A (en) 1999-12-30
DE69942159D1 (de) 2010-04-29
EP1589029B1 (en) 2010-03-17
CN1224629C (zh) 2005-10-26
EP1086122A1 (en) 2001-03-28
EA200100025A1 (ru) 2001-06-25
US20010021713A1 (en) 2001-09-13
ATE302794T1 (de) 2005-09-15
KR20010052772A (ko) 2001-06-25
DK1086122T3 (da) 2006-01-09
NZ508669A (en) 2003-06-30
NO20006300D0 (no) 2000-12-11
CA2334679A1 (en) 1999-12-16
IL139867A0 (en) 2002-02-10
EP1086122B1 (en) 2005-08-24
EP1589029A2 (en) 2005-10-26
JP4554077B2 (ja) 2010-09-29
US6514978B2 (en) 2003-02-04
CA2334679C (en) 2012-10-23
CN1305492A (zh) 2001-07-25
CN1769274A (zh) 2006-05-10
US6204263B1 (en) 2001-03-20
EA004884B1 (ru) 2004-08-26

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Legal Events

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B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: INDEFIRO O PEDIDO DE ACORDO COM O(S) ARTIGO(S) 8O, 13 E 24 DA LPI.

B09B Patent application refused [chapter 9.2 patent gazette]

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