Abstract:
Novel compounds of formula in which A is a substituted or unsubstituted phenyl, naphthyl or monocyclic heterocyclic ring, D is a substituted or unsubstituted phenyl or aromatic six-membered heterocyclic ring, K is a substituted or unsubstituted phenyl, naphthyl or bicyclic heterocyclic ring, and the other variables are as defined in the claims, their salts and other derivatives and compositions related thereto having activity against mammalian Factor Xa are disclosed. The coumpounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
Abstract:
The present invention discloses that phosphorylation of cytoplasmic tyrosine residues in the beta -subunit of integrins is needed for signal protein association. The invention provides methods of identifying signaling partners involved in integrin mediated signaling, methods of identifying agents which block integrin mediated signaling, methods of using agents which block intergrin mediated signaling to modulate biological and pathological processes, and agents which block integrin mediated signaling.
Abstract:
This invention relates to certain spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
Abstract:
This invention relates to the glycoprotein v gene. Specifically, this invention discloses the sequence and structure of the glycoprotein v gene and the amino acid sequence of the glycoprotein v polypeptide. In addition, the evolutionary relationship of the glycoprotein v gene with other glycoproteins is described and several uses of the isolated glycoprotein v gene are shown.
Abstract:
The present invention is directed towards immunoglobulin polypeptides that specifically bind to the extracellular domain of the human type beta PDGF receptor. The binding of the immunoglobulin polypeptides to the receptor inhibits PDGF-induced (or stimulated) receptor activation as indicated by inhibition of receptor phosphorylation and dimerisation, and by inhibition of PDGF-mediated mitogenesis, chemotaxis and migration of cells displaying the human PDGF type beta receptor on the cell surface. Nucleic acids encoding the immunoglobulin polypeptides are also included in the invention. The immunoglobulin polypeptides have diagnostic and therapeutic uses.
Abstract:
Analogs of Factor Xa (Factor Xai) which are inactive as proteases in the prothrombinase reaction are useful in treatment of diseases characterized by thrombosis. These antithrombotic agents can be conveniently prepared using recombinant techniques. In addition, modified forms of Factor Xa that generate Factor Xa in serum but have extended half-lives are useful in treating hemophilic conditions. These modified forms of Factor Xa are typically acylated forms of the serine residue in the active site which are slowly deacylated in vivo.
Abstract:
The present invention relates to therapeutics and diagnostics that take advantage of a novel signal transduction pathway in platelets. In addition, the present invention provides methods for identifying agents that modulate activities mediated by the novel transduction pathway including platelet activation and thrombosis.
Abstract:
Disclosed are processes for producing chromane compounds, preferably chroman-2-yl acetic acid compounds and 6-amino-chroman-2-yl acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.
Abstract:
Disclosed are process steps and novel processes for producing chromane compositions enriched in at least one (2R or 2S) enantiomer, preferably chroman-2-yl carboxylic acid compounds and chroman-2-yl carboxylic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are enzymatic processes for resolving chiral intermediates or final products to provide desired enantiomers.
Abstract:
Disclosed are processes for producing chromane compounds, preferably 2-(6-aminochroman-2-yl) acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.