Abstract: A process for the separation of streptokinase from contaminating proteins in a streptokinase-containing mixture, which comprises treating the mixture with a reducing agent to reduce disulphide bridges in the contaminating proteins to free thiol groups, contacting the mixture with a reagent R-X wherein R is a group capable of reacting with a free thiol group and X is a group R.sup.1 capable of reacting with a free thiol group or is a thiol-containing matrix, and thereafter separating the resulting chemically modified contaminating proteins from the mixture to provide streptokinase in a form substantially free of contaminating proteins.

Abstract: The combination of a fibrinolytic and a prostacyclin analogue is very useful for thrombosis treatment, especially to avoid subsequent rethrombosis.

Abstract: A pharmaceutical composition is prepared wherein a biologically active conjugated protein is selectively conjugated to at least one heparin fragment having a terminal 2,5-anhydro-D-mannose residue which has an aldehyde not involved in intramolecular hemiacetal formation. The resulting conjugate has a prolonged half-life as compared to native protein and is able to deliver heparin to the site of clots or to prevent reocclusion within the blood stream. Typical proteins include enzymes such as plasminogen activators, and in particular tissue plasminogen activators, and erythropoietin, hormones, antibodies and the like.

Abstract: There is disclosed a pharmaceutical preparation based on Lys-plasminogen and available in the lyophilized form. This preparation contains a serine-protease inhibitor and optionally an inhibitor co-factor, preferably in an amount of 0.5 to 30 nmol per mg Lys-plasminogen. This preparation is free of side-effects and may be used for the treatment and prophylaxis of plasminogen deficiency syndromes and thromboses as well as for the production of thromboresistant artificial organs.

Abstract: Purified DNA comprising a sequence encoding chrysoptin.Chrysoptin can be used to alter the hemodynamic or hemostatic properties of an animal's blood by administering to the animal an effective amount of chrysoptin.

Abstract: The present invention is directed to a new class of piperidinyl medicinal agents which are useful as antithrombotic agents and as serotonin 5HT.sub.2 antagonists.

Abstract: Processes for stabilizing active PAI-1 protein comprising combining active PAI-1 protein with an aqueous buffer having an ionic strength of at least about 5 millisiemens and a sugar selected from the group consisting of monosaccharides and disaccharides, and/or subjecting the active PAI-1 protein to lyophilization, are disclosed. Also described are compositions, including pharmaceutical compositions and kits, which include the stabilized active PAI-1 protein, and therapeutic processes employing the same in the treatment of fibrinolysis.

Abstract: Medicinal agents are claimed exhibiting sustained release of active compound, containing a solid active ingredient, poorly soluble in water, and auxiliary agents, characterized in that the active compound, in a microcrystalline form or in form of a molecular dispersion, is distributed in or on pellets, and that the pellets are covered by a membrane having retarded permeability with respect to the active compound.

Abstract: Disclosed is an anticoagulant material comprising a polymer obtained from an ionically bonded composite synthesized from i) a basic compound having a copolymerizable functional group and ii) a heparin salt. Disclosed is also a process for preparing the anticoagulant material. The anticoagulant material of the present invention can maintain excellent anticoagulant properties or antithrombotic properties over a long period of time and is capable of being applied as a component material for various medical articles such as artificial internal organs and artificial blood vessels, and a process for preparing it.

Abstract: A hemolysis depressant and a plasticizer each comprising a triglyceride compound. Resin compositions for medical appliances, medical implements and blood preserving liquid using the triglyceride compound as a hemolysis depressant are capable of preventing the blood held in contact therewith from the phenomenon of hemolysis by the activity of the compound in protecting erythrocytes. Vinyl chloride type resin compositions for medical appliances and medical implement using the compound as a plasticizer are substantially deviced of toxicity and offers extremely high safety.

Abstract: This invention provides a peptide fragment of human von Willebrand Factor (vWF) and sub-fragment thereof isolated as enzymtic digestion products from naturally occurring human vWF, or isolated from synthetic peptide mixtures or isolated from lysates of organisms capable of producing recombinant human vWF. The fragments and sub-fragments are useful in the prevention and treatment of cardiovascular disorders by virtue of their ability to inhibit the binding of vWF to platelets, heparin and/or collagen.

Abstract: This invention relates to cyclic peptide derivatives which are useful anticoagulant agents.

Abstract: Lipids obtained from blackcurrant seed are used for reducing thrombogenicity of blood vessels in humans.

Abstract: This invention relates to peptide derivatives which are useful anticoagulant agents.

Abstract: The use of 1-phenoxycarbonyl-2-pyrrolidinone derivatives as an anti-platelet aggregating agent. The derivatives are of the formula ##STR1## wherein R is a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a nitro group or a halogen atom and n is 0, 1 or 2.

Abstract: The present invention relates to polypeptide inhibitors of platelet activation and derivatives thereof, purified from the venom of the North American Water Moccasin and to methods for their purification. This invention also relates to DNA sequences and recombinant DNA molecules which code for these polypeptide inhibitors of platelet activation. And this invention relates to recombinant DNA molecules which code for fusion proteins comprising both a polypeptide inhibitor of platelet activation and a conventional anti-thrombin polypeptide. This invention also relates to pharmaceutically acceptable compositions and methods characterized by at least one of these natural or recombinant inhibitors of platelet activation, alone or in combination with conventional anti-thrombin compounds. The compositions, combinations and methods of this invention are particularly useful in the treatment of thrombotic diseases.

Abstract: This invention relates to cyclic peptide derivatives which are useful anticoagulant agents.

Abstract: A cleavage-resistant plasminogen molecule is provided that is conveniently produced in recombinant cells by expression of a nucleic acid sequence encoding the plasminogen molecule. Preferably the plasminogen is a sequence variant with a modification in its two-chain cleavage site. The plasminogen molecule may be purified, acylated, complexed with acylated or non-acylated fibrinolytic enzymes, and formulated into pharmaceutical compositions for use in thrombolytic therapy.

Abstract: A protein having a molecular weight of about 6,000 daltons which is biologically active in the inhibition of Factor Xa during the blood coagulation cascade, a method for producing the protein, methods for inhibiting blood coagulation using the protein, and suitable pharmaceutical compositions.

Abstract: Meizothrombin- and thrombin-inhibiting inhibitors which do not bind bivalent cations and which are used for the anticoagulant pretreatment of blood samples to be used in the determination of the functions and/or changes of state of blood cells and blood corpuscles, and for treating devices and receptacles used for taking and/or receiving blood samples.

Abstract: An intraocular anticoagulant including antithrombin III is applicable as an injection into the ocular chamber of the eye at the time of cataract surgery, intraocular lens implant surgery, and other ocular surgeries. The anticoagulant prevents fibrin deposits from forming on the intraocular lens surface after surgery and avoids postoperative viscoelastic material inducing transient elevation in intraocular pressure.

Abstract: Plasminogen activators of the tissue-type and plasminogen activators of the urokinase-type appear to have a synergistic action in vivo when administered together as thrombolytic agents. Use in pharmaceutical compositions and in methods for the preparation and use thereof are set forth.

Abstract: The present invention provides sulphonamides of the general formula: ##STR1## wherein R is a hydrogen or halogen atom, a cyano group or a C.sub.1 -C.sub.6 -alkyl or trifluoromethyl radical, n is 1, 2 or 3, m is 0 or 1 to 5, X is a valency bond, an oxygen atom, a carbonyl group or a --CHOH-- group, A is a valency bond or a carbonyl group and B is a valency bond or an --NH-- group; the physiologically acceptable salts thereof with inorganic and organic acids, as well as the optical isomers thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

Abstract: Peptides comprising the tripeptide sequence of arginine-tyrosine-aspartic acid, linked from amino- to carboxy-terminus, are inhibitors of fibrinogen binding, platelet aggregation, glycoprotein IIb-IIIa binding and related aberrant and normal physiological conditions.

Abstract: A composition comprising a polymer having dispersed therethrough a prostacyclin derivative selected from the group consisting of compounds of formula (I): ##STR1## (in which R.sup.1 represents hydrogen or lower alkyl, R.sup.2 represents a C.sub.3 -C.sub.12 alkyl group or a C.sub.3 -C.sub.12 alkenyl group; and n is an integer from 1 to 5; and pharmaceutically acceptable salts thereof) can be used to make a medical appliance from which the prostaglandin, having antithrombotic properties, will be released gradually and in a controlled way.

Abstract: This invention refer to chelerythrine, a considerably effective drug in the prevention and therapy of the thrombosis, which is a quaternary amine derivative and a major component of the organic solvent soluble extract of Zanthoxylum simulans. The effects of chelerythrine on the thromboembolism and the constriction of the blood vessel are also examined.

Abstract: Pharmaceutical compositions for inhibiting the aggregation of erthyrocytes or thrombocytes which include phenylamides which conform to the formula: ##STR1## with R.sub.1-6, X, A and B being as defined. Processes for the preparation of novel phenylamides coming within the above formula are also discussed.

Abstract: Substituted propanamines having anticoagulant or antifungal activity are disclosed. Also disclosed are methods of use involving the substituted propanamines as well as pharmaceutical compositions containing them.

Abstract: Pharmaecutical composition for topical use containing Defibrotide have been found effective in the therapy of local pathologies characterized by a reduced resistance of the blood capillary vessels.

Abstract: An aqueous parenteral solution of tissue-plasminogen activator, in which the pH is from 2 to 5.

Abstract: The present invention relates, by way of novel industrial products, to the sulfonylphenyl-.beta.-D-thioxyloside compounds of the formula ##STR1## in which: X is a sulfur atom or an oxygen atom;R is a C.sub.1 -C.sub.4 alkyl group, a substituted amino group NR.sub.1 R.sub.2 (where R.sub.1 and R.sub.2, which are identical or different, are each a C.sub.1 -C.sub.4 alkyl group, it being possible for R.sub.1 and R.sub.2, taken together, to form a piperidinyl or morpholinyl group with the nitrogen atom to which they are bonded) or a phenyl group which is unsubstituted or substituted in the para position by a cyano group or by a halogen atom; andY is the hydrogen atom or an aliphatic acyl group.These compounds are useful in therapeutics, especially as venous antithrombotics.

Abstract: A material and method are described to reduce the non-specific binding of a labelled material, wherein the labelled material comprises a fluorochrome and a specific binding pair member. The invention is particularlly suited to the lysis of peripheral blood wherein a labelled material is used to identify and detect cell populations within a sample of blood.

Abstract: Improved articles having reduced thrombogenicity when in contact with blood products containing albumin and methods of their preparation and use are provided. The articles comprise at the surface of blood contact a water insoluble polymeric substrate material having covalently attached thereon aliphatic extension of 12 to 22 carbon atoms. When exposed to blood, the aliphatic chain extensions provide a hydrophobic binding site for albumin. The articles when implemented with whole blood or blood products selectively enhance albumin affinity binding to the exclusion of other blood components, and subsequently minimize thrombus formation as well as other biocompatibility parameters, such as foreign body immune responses.

Abstract: Compositions useful for thrombolytic therapy comprising a plasminogen activator such as tPA or streptokinase together with an imidazolium salt having the formula ##STR1## in a pharmaceutically acceptable carrier and methods for inhibiting hard clot formation or supplementing fibrinolytic therapy are described. The imidazolium salt also may be used with a platelet aggregation inhibitor or anticoagulant.

Abstract: A pharmaceutical composition for preventing and treating thrombosis containing, as an active component, a saccharoascorbic acid derivative such as 2,3-di-O-benzyl-D-glucosaccharoascorbic acid n-octadecanethiol ester is disclosed.

Abstract: The invention relates to a combination preparation for thrombosis treatment consisting of acetylsalicylic acid and carbacyclin derivatives.

Abstract: Taurolin compounds are used as blood coagulation-inhibiting agents and as abacterial inflammation-inhibiting agents. The outstanding coagulation-inhibiting action of taurolin is especially suitable for use in medical conditions requiring dialysis and for vascular protheses. These compounds can also be used together with other anti-coagulants such as coumarin or heparin.

Abstract: Arylthioalkylphenylcarboxylic acids are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## wherein R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic diseases.

Abstract: Trigramin, a 72-amino acid polypeptide, has the following amino acid sequence: EAGEDCDCGSPANPCCDAATCKLIPGAQCGEGLCCDQCSFIEEGTVCRIARGDDLDDYCNGRSAGCPRNPFH. The molecule is a potent inhibitor of fibrinogen binding to receptors expressed on the glycoprotein IIb/IIIa complex in the membrane of platelets. Trigramin is thus a potent inhibitor of fibrinogen-induced human platelet aggregation. It is useful in inhibiting the formation of hemostatic platelet plugs.

Abstract: In accordance with the present invention, a method is provided for treating sickle cell anemia. The method comprises injecting an effective concentration of a surface active copolymer into the patient with sickle cell anemia.The surface active copolymer can be an ethylene oxide-propylene oxide condensation product with the following general formula:HO(C.sub.2 H.sub.4 O).sub.b (C.sub.3 H.sub.6 O).sub.a (C.sub.2 H.sub.4 O).sub.b Hwherein a is an integer such that the hydrophobe represented by (C.sub.3 H.sub.6 O) has a molecular weight of approximately 950 to 4000, preferably approximately 1200 to 3500, and b is an integer such that the hydrophile portion represented by (C.sub.2 H.sub.4 O) constitutes approximately 50% to 90% by weight of the compound.

Abstract: A substrate for medical devices and a process for making the substrate is provided, the substrate having on at least part of its surface a blood-compatible surface produced by coupling a physiologically active substance to the surface. The physiologically active substance is one having an inhibitory effect on the formation of blood clots and/or is capable of breaking down blood clots formed. The physiologically active substance is bonded to a polyacid, and the polyacid is attached to the surface by a covalent bond.

Abstract: A leach resistant composition includes a quaternary ammonium complex of heparin and a silicone. A method for applying a coating of the composition to a surface of a medical article is within the purview of the present invention. Medical articles having surfaces which are both lubricious and antithrombogenic, are produced in accordance with the method hereof.

Abstract: The present invention relates to new 3-guanidinoalkyl-2-azetidinones of the formula ##STR1## wherein: U and W can be the same or different and are selected from the group consisting of hydrogen and an amino protecting group;n is 1 to 3;X is a member selected from the group consisting of hydrogen, trialkylsilyl, arylsulfonyl, amino substituted arylsulfonyl, alkylsulfonyl, arylaminocarbonyl, alkylcarbonyl and arylcarbonyl; andY is a member selected from the group consisting of hydrogen, arylalkenyl, arylalkyl, formyl, carboxy, alkoxycarbonyl, acyloxy, arylthio, arylsulfinyl, arylsulfonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, arylaminocarbonyl, the radical ##STR2## in which R is hydrogen, alkyl or arylalkyl, and the radical ##STR3## in which m is 1 to 3 and R' is hydrogen or --CO.sub.2 R" wherein R" is hydrogen, alkyl or arylalkyl.The novel azetidinones of the present invention exhibit anti-thrombin and anti-trypsin activities and are thus useful in controlling blood coagulation and treating pancreatitis.

Abstract: Heterocyclic acids and esters useful as inhibitors of mammalian blood platelet aggregation characterized by Formula I are disclosed.HET.sub.1 --(CH.sub.2).sub.n CO.sub.2 R (I)Formula I compounds are those wherein n is 6-9, R is hydrogen, lower alkyl or an alkali metal ion, and HET.sub.1 is the heterocyclic radical 3,4-diphenyl-1H-pyrrol-1-yl.

Abstract: The present invention provides a method of preventing blood from clotting in a filter during continuous arteriovenous or venovenous hemodialysis on a patient comprising administering to the blood an amount of citrate sufficient to prevent clotting in the filter. The invention preferably utilizes a dialysate having a sodium and calcium concentration below that of normal blood and an alkali concentration sufficiently low to reduce or prevent alkalosis.

Abstract: In accordance with the present invention, a method is provided for efficiently delivering drugs to damaged tissue. The method comprises administering an admixture of an effective concentration of a surface-active copolymer and an effective concentration of a drug into the patient requiring the drug. Drugs that can be used in the present invention include, but are not limited to, antibiotics, antifungal drugs, chemotherapeutic drugs, free radical scavenger drugs, antinflammatory drugs, membrane stabilizing drugs, anticoagulants, ionotropic drugs and autonomic nervous system modulators.The surface-active copolymer can be an ethylene oxide-propylene oxide condensation product with the following general formula:HO(C.sub.2 H.sub.4 O).sub.b (C.sub.3 H.sub.6 O).sub.a (C.sub.2 H.sub.4 O).sub.b Hwherein a is an integer such that the hydrophobe represented by (C.sub.3 H.sub.

Abstract: A pharmaceutical composition is prepared wherein a biologically active conjugated plasminogen activator is selectively conjugated to at least one heparin fragment having a terminal 2,5-anhydro-D-mannose residue which has an aldehyde not involved in intramolecular hemiacetal formation. The resulting conjugate has a prolonged half-life as compared to native tissue plasminogen activator and is able to deliver heparin to the site of clot dissolution to prevent reocclusion.

Abstract: Improved articles having reduced thrombogenicity when in contact with blood products containing albumin and methods of their preparation and use are provided. The articles comprise at the surface of blood contact a water insoluble polymeric substrate material having covalently attached thereon aliphatic extension of 12 to 22 carbon atoms. When exposed to blood, the aliphatic chain extensions provide a hydrophobic binding site for albumin. The articles when implemented with whole blood or blood products selectively enhance albumin affinity binding to the exclusion of other blood components, and subsequently minimize thrombus formation as well as other biocompatibility parameters, such as foreign body immune responses.

Abstract: A leach resistant composition includes a quaternary ammonium complex of heparin and a silicone. A method for applying a coating of the composition to a surface of a medical article is within the purview of the present invention. Medical articles having surfaces which are both lubricious and antithrombogenic, are produced in accordance with the method hereof.

Abstract: The present invention relates to modified heparins having antithrombotic activity.The invention also relates to a process of preparing such modified heparins starting from water insoluble heparin ammonium quaternary complexes.Finally, the invention relates to pharmaceutical compositions containing the above modified heparins.