Plasminogen activator inhibitor-1 inhibitor

Details Plasminogen activator inhibitor-1 inhibitor Plasminogen activator inhibitor-1 inhibitor

2011-05-31

2011-05-31

Shameem, Golam M (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C544S358000, C544S359000, C544S379000, C514S252120, C514S438000

Reexamination Certificate

active

07951806

ABSTRACT:
The present invention relates to an inhibitor of plasminogen activator inhibitor-1. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. Furthermore, the present invention relates to a novel compound having PAI-1 inhibitory activity represented by the following general formula (I), and a salt thereof.Each symbol is defined as those in the specification.

REFERENCES:
patent: 56-007716 (1981-01-01), None
patent: WO 2006/107719 (2006-10-01), None
patent: WO 2007/083689 (2007-07-01), None
Aya et al, Tissue-Type Plasminogen Activator and its Inhibitor in Human Glomerulonephritis,Journal of Pathology, vol. 166: 289-295 (1992).
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Huang et al, A Mutant, Noninhibitory Plasminogen Activator Inhibitor Type 1 Decreases Matrix Accumulation in Experimental Glomerulonephritis,The Journal of Clinical Investigation112(3):379-388 (2003).
Haraguchi et al, t-PA Promotes Glomerular Plasmin Generation and Matrix Degradation in Experimental Glomerulonephritis,Kidney International59:2146-2155 (2001).
Egelund et al, A Regulatory Hydrophobic Area in the Flexible Joint Region of Plasminogen Activator Inhibitor-1, Defined with Fluorescent Activity-Neutralizing Ligands,The Journal of Biological Chemistry, 276 (16):13077-13086 (2001).
Matsuo et al, Plasminogen Activator in Bronchoalveolar Fluid,Haemostasis16:43-50 (1986).
Kivirikko et al, Modifications of a Specific Assay for Hydroxyproline in Urine,Analytical Biochemistry19:249-255 (1967).
Ashcroft et al, Simple Method of Estimating Severity of Pulmonary Fibrosis on a Numerical Scale,Journal of Clinical Pathology41:467-470 (1988).
Eitzman et al, Bleomycin-Induced Pulmonary Fibrosis in Transgenic Mice That Either Lack or Overexpress the Murine Plasminogen Activator Inhibitor-1 Gene,The Journal of Clinical Investigation97(1):232-237 (1996).
Milton et al, Biaryl Acids: Novel Non-Nucleoside Inhibitors of HIV Reverse Transcriptase Types 1 and 2,Bioorganic & Medicinal Chemistry Letters8:2623-2628 (1998).

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