Abstract:
The present invention relates generally to alkyne containing pharmaceutical agents, and in particular, to phenylethynyl-thiophene based metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of MMP inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP inhibitors for the treatment of pain and other diseases such as cancer. Additionally, the present invention relates to methods for treating pain in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
Abstract:
The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
Abstract:
The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds having the following formulas: wherein R1, R2, R3, and R4 are as defined in the specification. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds amide containing heterobicyclic compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.
Abstract:
The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.
Abstract:
An immunoscintillating composition and method of radioimmunoassay is disclosed whereby polymer coated paramagnetic particles and binding agent such as an antibody are associated by chemical or physical means to provide solid scintillating immunoadsorbent particles which are paramagnetic. These particles are capable of selectively binding or retaining radioactive or labeled antigens or ligands and transmitting radioactive energy to a phosphor or photon emitting substance that is bound by chemical or physical means to the particles. Upon binding of the antigens or ligands to the surface of the particles the particles are separated from the unbound components in solution by application of a magnetic field. The luminescence emitted by the phosphor which is attached to the magnetically separated particles is measured by a scintillator counter and is directly proportional to the radioactive energy released by the labeled antigen bound to the antibody. Upon completion of the measurement the paramagnetic particles can be magnetically separated and the labeled antigens or ligands removed for further analysis and the particles recycled for use in other assays.
Abstract:
The present invention relates generally to bis-amide containing MMP inhibiting compounds, and more particularly to selectively deuterated bis-amide MMP-13 inhibiting compounds that exhibit increased stability or potency in relation to currently known MMP-13 inhibitors. Additionally, the present invention relates to methods for treating pain and inflammation in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
Abstract:
The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.
Abstract:
The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.
Abstract:
The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.
Abstract:
The present invention relates to amide containing aromatic MMP inhibiting compounds with a mono-amide heteroaromatic group, of formulas I and II: