35 results about "Proteinase-Activated Receptors" patented technology

Compositions and methods comprising proteinase activated receptor antagonists are provided. More particularly, the present invention relates to the use of proteins, peptides and molecules that bind to proteinase activated receptor 2, and inhibit the processes associated with the activation of that receptor. More specifically, the present invention provides novel compositions and methods for the treatment of disorders and diseases such as those associated with abnormal cellular proliferation, angiogenesis, inflammation and cancer.

The present invention provides methods for diagnosing and treating an immune-mediated disease, e.g., an autoimmune disease, an allergy or an inflammatory disease. Diagnosis is made by detecting a heterozygous or homozygous genotype of haptoglobin 2 or by detecting and quantifying pre-haptoglobin 2 mRNA or protein. After diagnosis, the disease may be treated by decreasing cell permeability leading to increased transepithelial electrical resistance, for example, by administering an antibody directed against single chain zonulin thereby inhibiting epidermal growth factor receptor and inhibiting proteinase-activated receptor 2 (PAR2).

The present invention provides methods for diagnosing an immune-mediated disease, e.g., an autoimmune disease, an allergy or an inflammatory disease. Diagnosis is made by detecting a heterozygous or homozygous genotype of haptoglobin 2 or by detecting and quantifying pre-haptoglobin 2 mRNA or protein. After diagnosis, the disease may be treated by decreasing cell permeability leading to increased transepithelial electrical resistance, for example, by administering an antibody directed against single chain zonulin thereby inhibiting epidermal growth factor receptor and inhibiting proteinase-activated receptor 2 (PAR2). Also provided is a single step method for determining severity of an immune-mediated disease in a subject by identifying a genotype for haptoglobin 2 in a biological sample from the subject. A homozygous genotype correlates to 2 copies of zonulin and a more severe disease than a heterozygous genotype correlating to 1 copy of zonulin.

The invention relates to the field of thrombotic disease related drugs, belongs to triazole Schiff base compounds with brand new structures and derivatives of the triazole Schiff base compounds and particularly relates to PAR (Protease Activated Receptor)-1 antagonists with terminally-disubstituted methyl triazole Schiff base structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. All substituent groups are defined as the specification.

The invention belongs to the technical field of medicines and relates to PAR (Protease Activated Receptor)-1 antagonists with structures as shown in the formula I, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases.

The invention relates to the field of thrombotic disease related drugs and particularly relates to novel PAR (Protease Activated Receptor)-1 antagonists with halogenated tetrazole acetophenone structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. The group R is defined as the specification.

The invention belongs to the technical field of medicines and relates to PAR (Protease Activated Receptor)-1 antagonists with structures as shown in the formula I, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases.

This invention relates to nucleic acid encoding guinea pig PAR 4 and to the protein encoded thereby. The guinea pig DNA and protein are useful for the development of models of human platelet aggregation. The invention further relates to an animal model to assess the role of PAR antagonists in thrombosis.

The present invention relates to a health food or pharmaceutical composition for alleviating or suppressing pruritus, comprising chestnut shell extract as an active ingredient. In one example of the present invention, the chestnut shell extract comprised in the health food or pharmaceutical composition of the present invention can suitably be used as the active ingredient of a health food or pharmaceutical composition for alleviating or suppressing pruritus as it has been confirmed that it can exhibit an outstanding effect in alleviating or suppressing pruritus by suppressing the activity of -2(proteinase-activated receptor-2:PAR-2) which is a source of stimulation in pruritus.

The invention relates to the field of thrombotic disease related drugs and particularly relates to novel PAR (Protease Activated Receptor)-1 antagonists with halogenated tetrazole acetophenone structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. The group R is defined as the specification.

The present invention provides novel compounds of the Formula (I), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for therapies such as metabolic syndrome, obesity, type II diabetes, fibrosis and cardiovascular diseases, whether they are used alone or in combination with other treatment modalities.

The present invention provides novel PAR lderived cytoprotective oligopeptides or polypeptides which typically contain at least the first 4 N-terminal residues that are substantially identical to the corresponding N-terminal residues of Met1-Arg46 deleted human PAR 1 sequence. These cytoprotective oligopeptides or polypeptides are capable of activating PAR 1 and promoting PAR 1 cytoprotective signaling activities. The invention also provides engineered cells or transgenic non-human animals which harbor in their genome an altered PAR 1 gene that is resistant to cleavage at Arg41 and / or Arg46 residues. Additionally provided in the invention are methods of screening candidate compounds to identity additional cytoprotective compounds or cytoprotective proteases. The invention further provides therapeutic use or methods of employing a PAR 1 derived cytoprotective oligopeptide or polypeptide to treat conditions associated with tissue injuries or undesired apoptosis.

The invention relates to the field of thrombotic disease related drugs, belongs to triazole Schiff base compounds with brand new structures and derivatives of the triazole Schiff base compounds and particularly relates to PAR (Protease Activated Receptor)-1 antagonists with terminally-disubstituted triazole Schiff base structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. All the substituent groups are defined as the specification.

The invention belongs to the technical field of medicines and relates to PAR (Protease Activated Receptor)-1 antagonists with structures as shown in the formula I, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases.

This invention is in the field of medicinal pharmacology. In particular, the invention relates to protease activated receptor type 2 (PAR2) modulating compounds (e.g., mimetic peptides), compositions comprising such modulating compounds, and their use as therapeutics for the treatment of conditions involving PAR2 activity.

The present invention provides novel PAR 1 derived cytoprotective oligopeptides or polypeptides which typically contain at least the first 4 N-terminal residues that are substantially identical to the corresponding N-terminal residues of Met1-Arg46 deleted human PAR 1 sequence. These cytoprotective oligopeptides or polypeptides are capable of activating PAR 1 and promoting PAR 1 cytoprotective signaling activities. The invention also provides engineered cells or transgenic non-human animals which harbor in their genome an altered PAR 1 gene that is resistant to cleavage at Arg41 and / or Arg46 residues. Additionally provided in the invention are methods of screening candidate compounds to identity additional cytoprotective compounds or cytoprotective proteases. The invention further provides therapeutic use or methods of employing a PAR 1 derived cytoprotective oligopeptide or polypeptide to treat conditions associated with tissue injuries or undesired apoptosis.