148 results about "Urokinase Plasminogen Activator" patented technology

Treating or preventing the early stages of degeneration of articular cartilage or subchondral bone in the affected joint of a mammal is accomplished by administering a chondroprotective compound of Formula (I):where A is hydroxy, (C1-C4)alkoxy, amino, hydroxy-amino, mono-(C1-C2)alkylamino, di-(C1-C2)alkylamino; X and Y are independently H or (C1-C2)alkyl; and n is 1 or 2; R6 is halogen, (C1-C3)alkyl, trifluoromethyl, or nitro; R9 is H; (C1-C2)alkyl; phenyl or phenyl-(C1-C2)alkyl, where phenyl is optionally mono-substituted by fluoro or chloro; -C(=O)-R, where R is (C1-C2)alkyl or phenyl, optionally mono-substituted by fluoro or chloro; or -C(=O)-O-R', where R1 is (C1-C2)alkyl.This treatment ameliorates, diminishes, actively treats, reverses or prevents any injury, damage or loss of articular cartilage or subchondral bone subsequent to said early stage of said degeneration. Whether or not a mammal needs such treatment is determined by whether or not it exhibits a statistically significant deviation from normal standard values in synovial fluid or membrane from the affected joint, with respect to at least five of the following substances: increased interleukin-1 beta (IL-1beta); increased tumor necrosis factor alpha (TNFalpha); increased ratio of IL-1beta to IL-1 receptor antagonist protein (IRAP); increased expression of p55 TNF receptors (p55 TNF-R); increased interleukin-6 (IL-6); increased leukemia inhibitory factor (LIF); decreased insulin-like growth factor-1 (IGF-1); decreased transforming growth factor beta (TGFbeta); decreased platelet-derived growth factor (PDGF); decreased basic fibroblast growth factor (b-FGF); increased keratan sulfate; increased stromelysin; increased ratio of stromelysin to tissue inhibitor of metalloproteases (TIMP); increased osteocalcin; increased alkaline phosphatase; increased cAMP responsive to hormone challenge; increased urokinase plasminogen activator (uPA); increased cartilage oligomeric matrix protein; and increased collagenase.

A method is provided for preparing a biologically active molecule having an increased serum half-life. The method involves conjugating a polymer such as polyethylene glycol to the biologically active molecule. Also provided are polypeptide drugs having an increased serum half-life, e.g., human urokinase plasminogen activator (human “uPA” or “hUPA”) or a fragment or derivative thereof. Pharmaceutical compositions containing such molecules and methods of using them to treat uPA-mediated and uPA receptor-mediated disorders are also provided.

Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have Pi a group having an amidino or guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.

Methods are disclosed for sterilizing preparations of urokinase to reduce the level therein of one or more active biological contaminants or pathogens, such as viruses, bacteria (including inter- and intracellular bacteria, such as mycoplasmas, ureaplasmas, nanobacteria, chlamydia and rickettsias), yeasts, molds, fungi, single or multicellular parasites, and prions or similar agents responsible, alone or in combination, for TSEs. These methods involve sterilizing preparations of urokinase with irradiation.

The present invention relates to the use of molecules capable of specifically binding a urokinase plasminogen activator receptor (uPAR) as diagnostic reagents for the detection of metastases in vivo. Such metastases can include, but are not limited to, micrometastases.

The present invention relates to a method of identifying urokinase plasminogen activator (uPA) antibodies. The invention also relates to antibodies that are capable of binding uPA and which are capable of reducing or inhibiting uPA activity. Furthermore, the invention relates to uses for such antibodies, such as therapeutic and pharmaceutical uses.

The present invention relates to the cross-linked scuPA / suPAR complex and / or tcuPA / suPAR cross-linked complex, the process of preparation of the covalently bound single compound having fibrinolytic activity and use of the cross-linked scuPA / suPAR or tcuPA / suPAR complex in the prevention and / or treatment of thrombolytic disorders. The invention further relates to combination compositions and / or therapy regimens, comprising the cross-linked scuPA / suPAR complex or tcuPA / suPAR and one or more currently used plasminogen activators to achieve improved therapeutic efficacy and / or reduce side effects.

The presence of the ancient anti-inflammatory peptide α-melanocyte stimulating hormone (α-MSH [1-13], SYSMEHFRWGKPV) in barrier organs such as gut and skin suggests a role in the nonspecific (innate) host defense system. α-MSH and other amino acid sequences derived from α-MSH were determined to have antimicrobial influences, including against two major and representative cutaneous and mucosal pathogens: Staphylococcus aureus and Candida albicans. C-MSH peptides had antimicrobial effects against S. aureus and significantly reversed the enhancing effect of urokinase on S. aureus colony formation. α-MSH and other amino acid sequences reduced C. albicans viability and germination. α-MSH peptides also enhanced C. albicans killing by human neutrophils. The antimicrobial agent is selected from the group consisting of one or more peptides including the amino acid sequence KPV, one or more peptides including the amino acid sequence MEHFRWG, or a biologically functional equivalent of any of the foregoing. The most effective of the peptides were those bearing the C-terminal amino acid sequence of α-MSH, i.e., α-MSH (1-13), (6-13), and (11-13). The α-MSH “core” sequence (4-10), important for melanotropic effects, was also effective but significantly less potent. Antimicrobial influences of α-MSH peptides could be mediated by their well-known capacity to increase cellular cAMP; this messenger was significantly augmented in peptide-treated yeast. α-MSH has potent anti-inflammatory effects and is expected to be useful for treatment of inflammation in human and veterinary disorders. Reduced killing of pathogens is a detrimental consequence of therapy with corticosteroids and nonsteroidal anti-inflammatory drugs during infection. Therefore, anti-inflammatory agents based on α-MSH peptides that do not reduce microbial killing, but rather enhance it, would be very useful. The antimicrobial effects of these α-MSH peptides occurred over a broad range of concentrations including the physiological (picomolar) range.

The invention discloses an effect vector of uPA expression regulated by a Tet-on system. The nucleotide sequence of the effect vector comprises a bacteria tetracycline drug-resistant operon sequence, an immediate early promoter sequence of macrophages, a mice pro-urokinase activator expression cassette sequence and a sequence behind the last exon of the mice pro-urokinase activator expression cassette, the four sequences are serially connected in turn. The invention establishes a transgenic mice model of uPA expression regulated by the Tet-on system or tetracycline derivative inducible expression system, and lays solid foundation for further establishing a transgenic animal model of tissue specificity regulatable expression uPA for uPA function research in specific tissues.

The method for producing antithrombotic medicine by using silkworm utilizes the Bombyx noriNuclear polyhedrosis virus expression system to recombine fusion protein gene with human Annexin V and low molecular weight urokinase to obtain recombinant virus. Said recombinant virus is inoculated in bombyx mori larva and chrysalis to make expression, through separation, purification and freeze-drying, the invented antithrombotic oral liquor and injection can be made up. The animal tests show that it possesses obvious antithrombotic action, and is a new type thrombolytic medicine.

The present invention provides a rapid urokinase absorption bag, which comprises a mutton gauze layer, a modified cellulose layer, and a modified resin layer or a modified silica gel layer, wherein the mutton gauze layer, the modified cellulose layer, and the modified resin layer or the modified silica gel layer are sequentially arranged from the outside to the inside. The rapid urokinase absorption bag has the following characteristics that: a structure is simple; use is convenient; combination of the modified cellulose layer and the modified resin layer or the modified silica gel layer is adopted, such that the prepared absorption bag can timely and rapidly absorb urokinase in a toilet urinal so as to reduce steps of initial urine collection, transportation and the like in the traditional method, substantially simplify steps and workload of urokinase crude product extraction, provide characteristics of convenience and rapidness, and substantially save cost. In addition, large-scale industrial production of the rapid urokinase absorption bag is easily achieved.