Abstract: This invention relates to a therapeutic composition comprising, as active ingredient, a combination of a pyridine derivative having an anti-blood-platelet-aggregation activity and of sulfinpyrazone.Said composition has outstanding anti-blood-platelet-aggregating and antithrombotic properties, both components of the active ingredient functioning according to a synergistic effect.

Abstract: Heparin derivatives containing hydrophobic groups and exhibiting improved permeability are disclosed. Said derivatives exhibit anticoagulant activity and improved solubility in organic solvents.

Abstract: The healing of wounds is promoted by contacting the wound surfaces with a suspension of collagen and a glycosaminoglycan that is chemotactic for fibroblasts and/or endothelial cells. Typical glycosaminoglycans that exhibit the desired chemotaxis are heparin, heparan sulfate, and alginate. Two or more glycosaminoglycans can be present in the suspensions. Collagen is present in the suspension in the order of 7-10 mg/ml; while the glycosaminoglycan is present in much lower concentrations, e.g., 250-350 .mu.g/ml. Application of the collagen/glycosaminoglycan suspension to open wounds greatly increases the rate of healing.

Abstract: Acetyl ester derivatives of heparin are disclosed. These derivatives exhibit improved Anti-Xa activity in relation to their global anticlotting activity.

Abstract: Low molecular weight heparin derivatives containing hydrophobic groups and exhibiting improved permeability are disclosed. Said derivatives exhibit anticoagulant activity and improved solubility in organic solvents.

Abstract: Ester derivatives of heparin are disclosed. These derivatives exhibit low anti-Xa activity in relation to global anticlotting activity.

Abstract: Disclosed are methods for purifying proteins including AHF by column chromatography in the presence of additives including sugars and polyhydric alcohols which serve to increase the electrostatic forces on the surface of said proteins while decreasing the hydrophobicity of said proteins resulting in preparations of such proteins of high purity and/or resolution and/or recovery.

Abstract: The present invention provides certain novel substituted naphthalenes, indoles, benzofurans, and benzothiophenes of Formula I which are useful as inhibitors of leukotriene biosynthesis and as inhibitors of lipoxygenase. They are thus employed wherever it is medically necessary or desirable to inhibit these systems.

Abstract: Novel depolymerized and supersulfated heparin having a molecular weight comprised between 2000 and 9000 and a sulfation degree of at least 2.5, in which all of the primary hydroxy groups are sulfated; a process for its preparation by reacting a heparin of natural origin, or a fraction thereof with a sulfuric acid/chlorosulfonic acid mixture; and pharmaceutical compositions containing it as active ingredient, having potential antithrombotic, hypolipemic and fibrinolytic activity and useful in the prevention of thrombosis and for the treatment of atherosclerosis.

Abstract: Microdroplets of water-insoluble drugs coated with a phospholipid are prepared by sonication. As an example, microdroplets of the general anesthetic methoxyfluorane coated by a unimolecular layer of dimysistoyl phosphatidylcholine are prepared by sonication. The microdroplets so prepared remain stable in physiologically-compatible solution, and are suitable for injection, typically intradermally or intraveneously, into a patient for inducing local anesthesia. These methoxyflurane-containing microdroplets have been demonstrated to cause long-term local anesthesia when injected intradermally, giving duration of anesthesia 28 times longer than with other anesthetics, such as lidocaine and 11 times longer than with bupivacaine. The latter is considered longest acting conventional local anesthetic.

Abstract: A method for inhibiting blood platelet aggregation in humans, and promoting vasodilation in humans, by administering to a human in need of the same an effective amount of 2-hydroxy-3-isopropyl-5,6-dimethylpyrazine or a hydrate or a pharmaceutically acceptable non-toxic salt thereof. Administration can be orally in an amount of about 0.02-12 mg/kg body weight per day, or parenterally in an amount of about 0.01-6 mg/kg of body weight per day.

Abstract: Plastic articles having enhanced antithrombogenic activity due to the presence of hydrophobic materials attached to amine compounds bonded on the surface of the plastic which repel bonded antithrom bogenic agents outwardly from the plastic surface, making them more readily available to the blood for subsequent thrombus inhibition.

Abstract: Pharmaceutical compositions are described which have antithrombotic activity suitable for the prevention and for the therapy of cardiac infarcts, cerebral infarcts and venous thrombosis. They contain as the active component a fraction of heparin which has been modified by nitrogen desulfatation and succinylation, which fraction contains less than 10% of the N-sulfate groups of the heparin starting material and more than 0.6 succinyl radicals per disaccharide unit. The method of treatment is described.

Abstract: The present invention relates to novel xylan sulfates of average molecular weight comprised between 2000 and 5000 Daltons.The invention also relates to their process of preparation by fractionation and their use in therapeutics as orally active antithrombotic and hypolipaemic agents.

Abstract: An antithrombogenic/antibiotic plastic material prepared using an organic solvent system containing a specific chlorofluorocarbon compound and petroleum ether.

Abstract: The invention provides novel orally active salts of the formula ##STR1## in which .circle. is the skeleton of a polyol, n is the number of OH's in the polyol (3 to 24); p is .gtoreq.3 and .ltoreq.n; r is the available valence of the heparin unit and .gtoreq.3 and .ltoreq.7; sr is equal to pv; and R.sup.+ is ##STR2## in which R.sup.iv is C.sub.1 -C.sub.3 alkyl; R' and R" are C.sub.1 -C.sub.7 alkyl, the same or different, or combined so that --NR'R" represents the residue of a saturated monocyclic secondary amine; R"' is identical to the corresponding portion of a natural amino acid; the alkylene groups contain 1 to 3 carbon atoms; and R.sup.v is H, --CONH.sub.2 or --COO(C.sub.1 -C.sub.7 alkyl). The salts are stable lipoidal "ion pairs" or complexes which can be absorbed through the gastrointestional wall and which slowly release heparinic acid to achieve long-lasting anticoagulant activity. Novel quaternary salts which are intermediates to the heparin salts of the invention are also disclosed.

Abstract: This invention relates to new xylane sulfates having an apparent molar weight comprised between 7000 and 12000.This invention relates also to a process for their preparation by fractionation, and to the therapeutic application thereof as anti-thrombosis and hypolipemic agents.

Abstract: There is disclosed a process for producing a convalently bound heparin--antithrombin-III complex useful for anticoagulant therapy, a covalently bound heparin--antithrombin-III complex produced by the process, a composition thereof in a pharmaceutically acceptable carrier, and a method for preventing and treating thromboembolisms by administering to a human patient a therapeutically effective amount of the complex or preparation.

Abstract: The invention relates to a method and composition for thrombolytic treatment. It comprises administering to thrombosis-afflicted patients a low molecular weight heparin in an amount effective to cause lysis of thrombi in vivo.

Abstract: Peptides of the general formulaH.sub.2 N-(Ch)-Arg-Gly-Asp-(Cx)-Hand the derivatives thereof described herein, wherein (Cx) and (Ch) each contains 1 to 20 amino acid residues and (Ch) contains at least one Lys or Arg residue, or at least one of each, inhibit platelet-fibrinogen binding and platelet-platelet aggregation and are thus useful inhibitors of cell adhesion.

Abstract: An antithrombogenic thermoplastic polyurethane product and process for preparing the same which comprises a substrate and at least one layer of a polyurethane alloy complex comprising a thermoplastic polyurethane and completely dispersed therein a preformed complex of an antithrombogenic material ionically bonded with a quaternary ammonium compound.

Abstract: Conjugates are provided which are covalently bonded conjugates of an anticoagulant and protein that are prepared in the presence of a coupling agent that forms amide linkages between the anticoagulant and the protein. Such amide linking coupling agents exclude highly toxic coupling agents such as CNBr. These conjugates are useful for enhancing the blood compatibility of certain surfaces of a prosthetic device, a surgical apparatus, or an extra-corporeal medical device.

Abstract: Described are lipid emulsions of marine oils comprising high concentrations of omega-3-fatty acid esters and low concentrations of free fatty acids for intraveneous administration for the treatment of thrombic disease states. More specifically, a lipid emulsion for parenternal use is provided comprising an emulsifier, water and a marine oil comprising an omega-3-fatty ester in which the concentration of the free fatty acid in the emulsion is below about 5 meq/l.

Abstract: An antithrombogenic thermoplastic polyurethane product and process for preparing the same which comprises a substrate and at least one layer of a polyurethane alloy complex comprising a thermoplastic polyurethane and completely dispersed therein a preformed complex of an antithrombogenic material ionically bonded with a quaternary ammonium compound.

Abstract: A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.

Abstract: Conjugates are provided which are covalently bonded conjugates of an anticoagulant and protein that are prepared in the presence of a coupling agent that forms amide linkages between the anticoagulant and the protein. Such amide linking coupling agents exclude highly toxic coupling agents such as CNBr. These conjugates are useful for enhancing the blood compatibility of certain surfaces of a prosthetic device, a surgical apparatus, or an extra-corporeal medical device.

Abstract: A pharmaceutical composition comprising an amount, effective for inhibiting platelet aggregation, of guanosine monophosphate represented by the following formula ##STR1## wherein one of X, Y and Z represents a H.sub.2 PO.sub.3 group and the remaining two of these represent a hydrogen atom,or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable diluent or carrier.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; alkyl of 1 to 7 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; monosubstituted alkyl of 1 to 3 carbon atoms, where the substituent is pyridyl, methylpyridyl, phenyl, mono-, di- or trisubstituted phenyl, where the substituents on the phenyl ring, which may be identical to or different from each other, are selected from the group consisting of one amino, one dimethylamino, one to two hydroxyls, one to three methoxys and one to three halogens; .omega.-monosubstituted alkyl of 2 to 4 carbon atoms, where the substituent is hydroxyl or di(alkyl of 1 to 3 carbon atoms)amino; phenyl; monohalo-phenyl; unsubstituted or monosubstituted straight or branched alkanoyl of 1 to 6 carbon atoms, where the substituent is phenyl, methoxyphenyl or cycloalkyl of 3 to 7 carbon atoms; or unsubstituted or monosubstituted phenylsulfonyl, where the substituent is methyl or methoxy; and,R.sub.

Abstract: Platelet aggregation inhibiting compositions and methods of use containing compounds of the formula ##STR1## where Z completes a bond or is a ##STR2## group; one of R.sub.1 and R.sub.2 is hydroxy and the other is hydrogen or alkyl, or R.sub.1 and R.sub.2, taken together, form an oxo group; and the remaining substituents are as defined in the specification.

Abstract: The invention discloses that the tissues of earthworms contain fibrinolytically or thrombolytically active ingredients which can be extracted and purified by a suitable sequence of extraction and purification procedures into the individual active ingredients including six novel proteases named F-O-HM-45, F-I-1-HM-54, F-I-2-HM-15, F-II-HM-64, F-III-1-HM-27 and F-III-2-HM-89. The chromatographic fractionation of the earthworm extract with an aqueous extractant gives five active fractions, the first four of which contain each one of the first mentioned four proteases and the last of which contains the last mentioned two proteases. The disclosure includes description of the suitable purification methods for the proteases as well as the physico-chemical identification data thereof. Various thrombolytic medicament forms prepared with the novel proteases as the effective ingredient are described together with the results of the clinical tests carried out by the oral administration of the novel proteases.

Abstract: A compound of the formula ##STR1## wherein X.sup.1 is a free or an esterified carboxyl group, or a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7 membered saturated heterocyclic group), Y is a group of the formula: ##STR3## (R.sup.6 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) or ##STR4## (R.sup.6 is as defined above), R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sup.1 and R.sup.2, when taken together, mean a single linkage to form a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.

Abstract: This invention relates to a therapeutic composition comprising, as active ingredient, a combination of a pyridine derivative having an anti-blood-platelet-aggregation activity and of sulfinpyrazone.Said composition has outstanding anti-blood-platelet-aggregating and antithrombotic properties, both components of the active ingredient functioning according to a synergistic effect.

Abstract: The object of the invention is to provide a new antithrombotic agent.Coagulation of blood acts through a cascade of stages, the mechanisms and interaction of which have not been fully clarified. The present invention provides a derivative of heparin which can be administered orally, topically, or parenterally to antagonize the effect of factor Xa to a greater extent than commercial porcine heparin. In addition, the derivative has insignificant USP anticoagulant and platelet aggregating activities.The heparin derivative according to the invention, has a molecular weight of from about 2,500 to about 4,000 daltons, gives a positive metachromatic test for sulfated polysaccharides. Preferably, when isolated as the sodium salt, the derivative contains by elemental analysis about 26.2% carbon, 4.33% hydrogen, 1.98% nitrogen, 7.1% sulfur, and 9.8% sodium, the molar ratio C:N:S:Na being about 10:1.5:2:4.

Abstract: Conjugates are provided which are covalently bonded conjugates of an anticoagulant and protein that are prepared in the presence of a coupling agent that forms amide linkages between the anticoagulant and the protein. Such amide linking coupling agents exclude highly toxic coupling agents such as CNBr. These conjugates are useful for enhancing the blood compatibility of certain surfaces of a prosthetic device, a surgical apparatus, or an extra-corporeal medical device.

Abstract: Compounds having blood-anticoagulant properties of the general molecular formula: ##STR1## in which Z represents a halogen atom, preferably a chlorine atom, and n is 0, 1 or 2 and R.sup.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is a substituted alkoxy group, or an optionally substituted mercapto or amino group,R.sub.2 is a cyclic imino group,R.sub.3 is hydrogen, phenyl, alkyl or acyl, andn is 2 or 3,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as antithrombotics.

Abstract: An orally administrable heparin comprising: a complex of heparin with (1) a protonated tertiary organic ammonium ion having the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently represent a branched or unbranched alkyl group of 1 to 12 carbon atoms, which may be unsubstituted or substituted with hydroxy or alkoxy groups, or R.sup.1 and R.sup.3 together with the N atom can form a pyrrolidine, imidazole or morpholine ring; or (2) an ester-containing quaternary ammonium ion having the formula: ##STR2## wherein R.sup.4, R.sup.5 and R.sup.6 each independently represent a branched or unbranched alkyl group of 1 to 12 carbon atoms, which may be unsubstituted or substituted with hydroxy or alkoxy groups, or R.sup.4 and R.sup.6 together with the N atom can form a pyrrolidine, imidazole or morpholine ring;R.sup.7 represents an alkyl group of 4 to 16 carbon atoms; andR.sup.8 represents a hydrogen atom or a methyl group.

Abstract: Compounds of the formula (I) ##STR1## wherein the symbol represents a single or a double bond; Z completes a single bond or is a --CH.sub.2 -- group; each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different is(a) hydrogen; hydroxy; halogen; cyano; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 alkoxy; a C.sub.2 -C.sub.4 acyl or C.sub.2 -C.sub.4 acylamino group; --SR', --N(R') (R"), --CH.sub.2 OR', --COR or --CH.sub.2 COR, wherein R is OR' or --N(R') (R") and each of R' and R", being the same or different, is hydrogen or C.sub.1 -C.sub.6 alkyl; or(b) one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is 5- tetrazolyl or a group selected from --COCH.sub.2 OR', --CH.dbd.C(R')-COR and --X-C(R') (R")-COR, wherein R, R' and R" are as defined above, and X is --O--, --S--, or --NH--, and the others are as defined above under (a);one of R.sub.5 and R.sub.6 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.

Abstract: Mucopolysaccharides biologically active and more specific than heparin, particularly with respect to the blood factor Xa. These mucopolysaccharides may be obtained by partial depolymerisation, under controlled conditions, of heparin, by the action of a chemical agent such as nitrous acid. The conditions implemented allow the preparation of mucopolysaccharides having a USP titer lower than that of the starting heparin and a Yin-Wessler titer at least equal to that of said heparin. These products may be used particularly as antithrombotic drugs.