Abstract: The present invention relates to immobilized biologically active entities that retain significant biological activity following sterilization of the immobilized biologically active entities.

Abstract: An integrated patient monitoring and control system is provided which includes a closed-loop control system for monitoring and adjusting the heparin infusion rate for a patient. The system includes a processor which uses a dynamic patient model that is continuously adjusted based on the patient's aPTT measurements to calculate an optimal heparin infusion rate to achieve an operator-input aPTT target range. The processor also includes a forecasting model to calculate the optimum sample time interval for measuring the patient's aPTT to calculate a new infusion rate. An automated sampling system, which includes a storage device for storing a series of assay devices, an advancement mechanism for moving the assay devices to a sample area, and a measurement device for analyzing a sample dispensed on the assay, is provided. The sampling system is used to repeatedly measure the patient's aPTT according to the sample time interval determined by the processor.

Abstract: A pharmaceutical composition comprising a drug and a permeation enhancer that comprises a multi-carbon backbone having a functional group and also one or more side chains which have one or more carbon atoms and, optionally, one or more functional groups.

Abstract: A method for lubricating an implant or graft prior to implantation into a target implant site which enhances the lubricity of the implant or graft and promotes bone growth. The method comprises the steps of lubricating the implant or graft with the composition comprising hyaluronic acid and optionally a growth factor and/or an antiseptic and/or antibiotic, and subsequently implanting the lubricated implant or graft into a target implant site.

Abstract: Novel serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.

Abstract: Alkali and alkali-earth metal salts of polysaccharides derived from heparin, their method of preparation and the pharmaceutical compositions containing them.

Abstract: The present invention relates to the use of glycosaminoglycan fractions having an average molecular weight of 2400 (±200) D for the preparation of pharmaceutical compositions suitable for the treatment of emotional dysfunctions, especially depressive disorders, anxiety disorders, anxiety neurosis, agitation, confusion.

Abstract: This invention provides a method of treating a subject suffering from an obstructive respiratory disease, including the step of administering to a subject a compound comprising a lipid or phospholipid moiety bound to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof, in an amount effective to treat the subject suffering from an obstructive respiratory disease.

Abstract: Novel depolymerized-LMWepiK5-N,O-sulfates obtainable starting from a LMW-epiK5-N-sulfate prepared by nitrous depolymerization of an epiK5-N-sulfate or by C5-epimerization of a LMW-K5-N-sulfate obtained by nitrous depolymerization of a K5-N-sulfate. A process consists of submitting the starting depolymerized-LMW-epiK5-N-sulfate to four steps: a O-oversulfation, a partila O-desulfation, a 6-O-sulfation and a N-sulfation. The new depolymerized-LMWepiK5-N,O-sulfates present a di- or trisulfated 2,5-anhydromannitol unit at the reducing end of the majority of its chains, have a content of iduronic acid of 40-60%, a sulfation degree of from 2.3 to 2.9 and a mean molecular weight of from about 1,500 to about 12,000. They exhibit a good antithrombotic activity with a low pro-hemorrhagic risk.

Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

Abstract: The invention relates to oligosaccharides, the preparation method and use thereof, and pharmaceutical compositions containing same. More specifically, the invention relates to oligosaccharides which can be used for the treatment of cancer and, in particular, to prevent and inhibit the formation of metastases. The inventive oligosaccharides can be used, for example, during early breast, lung, prostate, colon or pancreatic cancer. The oligosaccharides can be administered subcutaneously, orally or intravenously. Moreover, said oligosaccharides can be used alone or together with other anticancer agents, e.g. cytotoxics such as docetaxel or paclitaxel.

Abstract: Compositions and methods of employing compositions in flushing and coating medical devices are disclosed. The compositions include combinations of a chelating agent, anticoagulant, or antithrombotic agent, with a C4-C9 carboxylate antimicrobial agent, such as octanoic acid. Methods of using these compositions for coating a medical device and for inhibiting catheter infection are also disclosed. Particular combinations of the claimed combinations include, for example, octanoic acid or other C4-C9 carboxylate antimicrobial agent together with EDTA, EGTA, DTPA, heparin and/or hirudin in a pharmaceutically acceptable diluent.

Abstract: The invention provides blood compatible nanomaterials, biomaterials prepared therewith and blood compatible medical devices fabricated using the biomaterials of the invention. The invention further provides methods of making and using the nanomaterials, biomaterials and medical devices of the invention for the diagnosis, prevention and treatment of medical conditions. The invention further provides methods of using room temperature ionic liquids to make blood compatible nanomaterials.

Abstract: Plaster for topical use having an analgesic activity and at the same time being able to re-absorb haematomas, comprising: a substrate layer; an adhesive layer in the form of a hydrogel matrix containing a pharmaceutically acceptable diclofenac salt, heparin or a heparinoid; a protective film which can be removed at the moment of use.

Abstract: The invention concerns a method and a system for producing a signal, in particular an electric signal, or a substance having a coagulating or anticoagulant effect. The method is characterised in that it is based on a source substance with coagulating effect, in particular, Ca++ ions, or an anticoagulant affect, in particular heparin. The method consists in: transforming the electromagnetic field derived from said source substance located in the chamber, into a signal, in particular an electric signal, using a transducer-receiver sensing the electromagnetic field; applying to a receiving substance located in the chamber, in particular water or a water-ethanol mixture or homeopathic granules, said signal derived from said transducer-receiver, using a transducer-transmitter. After said treatment, the receiving substance, initially inactive, has a coagulating or anticoagulant effect.

Abstract: According to an aspect of the present invention, implantable or insertable medical devices are provided which contain (a) one or more depressions that contain at least one therapeutic agent, and (b) a nanoporous coating, disposed over the therapeutic-agent-containing depressions, which regulate transport of species between the therapeutic-agent-containing depressions and the exterior of the device. The implantable or insertable devices are configured to preform a role beyond mere drug delivery, for example, providing mechanical and/or electrical functions within the body, among other functions. An advantage of the present invention is that medical devices may be provided, which release therapeutic agents in quantities far exceeding the void volume within the nanoporous coating, while at the same time providing functionality that extends beyond drug delivery. Such release may further approach or achieve a zero order kinetic drug release profile.

Abstract: A method of treatment for treating, preventing, inhibiting or reducing extracellular matrix build-up in a body tissue or a bodily fluid transport vessel, in a subject, includes administering to a subject in need of such treatment an effective amount of a composition including a peptide agent including amino acid sequence LKKTET, a conservative variant thereof, or a peptide agent that stimulates production of an LKKTET peptide, or a conservative variant thereof, in the tissue.

Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: Partially desulfated glycosaminoglycan derivatives are described, particularly heparin, and more particularly formula (I) compounds where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives exhibit antiangiogenic activity and are devoid of anticoagulant activity.

Abstract: The present invention includes compositions and methods for treating and delivering medicinal formulations using an inhaler. The composition includes a space filled flocculated suspension having one or more flocculated particles of one or more active agents and a hydrofluoroalkane propellant. A portion of the one or more flocculated particles is templated by the formation of hydrofluoroalkane droplets upon atomization and the templated floc compacts upon the evaporation of the hydrofluoroalkane propellant to form a porous particle for deep lung delivery.

Abstract: Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly a compound of formula (I) where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives have antiangiogenic and heparanase-inhibiting activity and are devoid of anticoagulant activity.

Abstract: The invention relates to a solid oral dosage form comprising a pharmaceutically active ingredient in combination with an enhancer which enhances the bioavailability and/or the absorption of the active ingredient. Accordingly, a solid oral dosage form comprises a drug and an enhancer wherein the enhancer is a medium chain fatty acid ester, ether or salt or a derivative of a medium chain fatty acid, which is, preferably, solid at room temperature and which has a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is controlled release dosage form such as a delayed release dosage form.

Abstract: The present invention provides for methods of treating and preventing cardiac hypertrophy. Class I HDACs, which are known to participate in regulation of chromatin structure and gene expression, have generally been considered as pro-hypertrophic in their action. However, the present invention demonstrates that inhibition of certain Class I HDACs should be avoided in the treatment of cardiac hypertrophy, thereby pointing toward selective, and not global, inhibition of Class I HDACs. In particular, the present invention provides for selective inhibition of HDACs 1 and/or 2, and the avoidance of inhibition of HDAC3.

Abstract: A mixed micellar pharmaceutical formulation includes a micellar pharmaceutical agent, an alkali metal C8 to C22 alkyl sulfate, alkali metal salicylate, a pharmaceutically acceptable edetate and at least one absorption enhancing compound. The absorption enhancing compounds are selected from the group consisting of lecithin, hyaluronic acid, pharmaceutically acceptable salts of hyaluronic acid, octylphenoxypolyethoxyethanol, glycolic acid, lactic acid, chamomile extract, cucumber extract, oleic acid, linolenic acid, borage oil, evening primrose oil, trihydroxy oxo cholanyiglycine, glycerin, polyglycerin, lysine, polylysine, triolein and mixtures thereof. Each absorption enhancing compound is present in a concentration of from 1 to 10 wt:/wt. % of the total formulation, and the total concentration of absorption enhancing compounds are less than 50 wt./wt. % of the formulation. Methods for administering insulin and heparin to the buccal region are also disclosed.

Abstract: This invention provides a method of treating a subject suffering from a dermatologic condition, including, inter alia, psoriasis, contact dermatitis, and seboreic dermatitis, the method includes the step of administering to a subject a compound comprising a lipid or phospholipid moiety bound to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof, in an amount effective to treat the subject suffering from a dermatologic condition.

Abstract: In the present invention there are disclosed new derivatives of dianhydrohexite mononitrate corresponding to formula (I), tautomers, pharmaceutically acceptable salts, prodrugs and solvates thereof: as well as pharmaceutical compositions comprising these compounds and uses thereof.

Abstract: The present invention relates to the field of nutraceuticals, and in particular to nutraceuticals comprising sulfated polysaccharides, Astragalus polysaccharides, resveratrol, and combinations thereof. These compositions find use in inducing physiological responses such, decreasing body fat, increasing lean body mass, alleviating the symptoms of colds, preventing the onset of colds, increasing energy, increasing the feeling of well-being in subjects, and improving skin tone and appearance.

Abstract: Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising: a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties; and a physiologically active substance.

Abstract: The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention also relates to methods for screening compounds and compositions useful for inhibiting or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.

Abstract: Oral insulin formulations and processes for preparing oral insulin formulations are provided.

Abstract: Methods for treating ST-segment elevation myocardial infarction in a human patient 75 years of age or older. The methods comprise administering a dose of less than 1 mg per kg body weight, about 0.75 mg per kg of body weight, or 0.75 mg per kg of body weight of enoxaparin sodium by subcutaneous injection approximately every twelve hours for a therapeutic dosing period. The methods may include fibrinolytic therapy. The treatment methods may be used to prevent one or more of, mortality, myocardial re-infarction, myocardial ischemia, stroke, or severe congestive heart failure. Articles of manufacture for use in connection with treating ST-segment elevation myocardial infarction in a human patient 75 years of age or older are also disclosed. The articles of manufacture comprise enoxaparin sodium, and instructions designed to achieve administration to a patient of a dose of less than 1 mg per kg body weight, about 0.75 mg per kg of body weight, or 0.

Abstract: The present invention relates to a biologically active functionalized electrospun matrix to permit immobilization and long-term delivery of biologically active agents. In particular the invention relates to a functionalized polymer matrix comprising a matrix polymer, a compatibilizing polymer and a biomolecule or other small functioning molecule. In certain aspects the electrospun polymer fibers comprise at least one biologically active molecule functionalized with low molecular weight heparin. Examples of active molecules that may be used with the multicomponent polymer of the invention include, for example, a drug, a biopolymer, for example a growth factor, a protein, a peptide, a nucleotide, a polysaccharide, a biological macromolecule or the like. The invention is further directed to the formation of functionalized crosslinked matrices, such as hydrogels, that include at least one functionalized compatibilizing polymer capable of assembly.

Abstract: The present invention describes new pharmaceutical compositions in treatment of skin and/or mucous injuries, new therapeutic use of compounds and use of compositions and compounds in treatment of injuries that involve skin and/or mucous, and/or therapies where regeneration or modelling of tissues growth is necessary. Particularly these pharmaceutical compositions are indicated for treatment of injuries caused by burns.

Abstract: The present invention relates to a biologically active functionalized electrospun matrix to permit immobilization and long-term delivery of biologically active agents. In particular the invention relates to a functionalized polymer matrix comprising a matrix polymer, a compatibilizing polymer and a biomolecule or other small functioning molecule. In certain aspects the electrospun polymer fibers comprise at least one biologically active molecule functionalized with low molecular weight heparin. Examples of active molecules that may be used with the multicomponent polymer of the invention include, for example, a drug, a biopolymer, for example a growth factor, a protein, a peptide, a nucleotide, a polysaccharide, a biological macromolecule or the like. The invention is further directed to the formation of functionalized crosslinked matrices, such as hydrogels, that include at least one functionalized compatibilizing polymer capable of assembly.

Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: The present invention relates to new amide inhibitors of renin, pharmaceutical compositions thereof, and methods of use thereof

Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric form of thyroid hormone, or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Compositions of the polymeric forms of thyroid hormone, or thyroid hormone analogs, are also disclosed.

Abstract: The invention relates to methods for delivering polysaccharides by a pulmonary route to achieve local and systemic therapeutic effects. The polysaccharides may be formulated or unformulated and in some instances have an extremely fast absorption rate.

Abstract: The present invention relates to pharmaceutical compounds for delivering active agents, such as biologically or chemically active agents, to a target. The invention also relates to pharmaceutical compositions comprising at least one delivery agent compound of the present invention and at least one active agent, and unit dosage forms comprising such compositions. Methods for the preparation and administration of the pharmaceutical compositions are also disclosed.

Abstract: The invention relates to the use of TGF-beta stimulating agents, and in particular members of the triphenylethylene class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of cardiovascular disease, autoimmune diseases or neurodegeneration. In particular, improved compositions consisting of triphenylethylene agents combined with one or more additional active pharmaceutical agents in order to mitigate against side-effects of the triphenylethylene are described and claimed.

Abstract: The invention provides synthetic heparin-binding growth factor analogs having at least one peptide chain, and preferably two peptide chains branched from a dipeptide branch moiety composed of two trifunctional amino acid residues, which peptide chain or chains bind a heparin-binding growth factor receptor and are covalently bound to a non-signaling peptide that includes a heparin-binding domain, preferably by a linker, which may be a hydrophobic linker. The synthetic heparin-binding growth factor analogs are useful as pharmaceutical agents, soluble biologics or as surface coatings for medical devices.

Abstract: The present invention is directed to a combination of therapeutic compounds and treatment methods and kits using the combination. In particular, one of the combination affects the NCca-ATP channel of neural tissue, including neurons, glia and blood vessels within the nervous system. Exemplary SUR1 and/or TRPM4 antagonists that inhibit the NCca-ATP channel may be employed in the combination. The combination therapy also employs one or more of a non-selective cation channel blocker and/or an antagonist of VEFG, NOS, MMP, or thrombin. Exemplary indications for the combination therapy includes the prevention, diminution, and/or treatment of injured or diseased neural tissue, including astrocytes, neurons and capillary endothelial cells, that is due to ischemia, tissue trauma, brain swelling and increased tissue pressure, or other forms of brain or spinal cord disease or injury, for example.

Abstract: The present invention relates to inhibiting or preventing infection and protecting against patency complications after a blood catheter has been inserted in a patient comprising administering to the device a pharmaceutically effective amount of a composition comprising: (A) at least one taurinamide derivative, (B) at least one compound selected from the group consisting of biologically acceptable acids and biologically acceptable salts thereof; and (C) heparin at a low concentration.

Abstract: Methods for increasing plasmin activity in a patient in need thereof are provided, comprising administering to the patient a therapeutic amount of an agent which binds to ?2-antiplasmin at a binding site to increase conversion of cc2-antiplasmin from an inhibitor to a plasmin substrate, thereby increasing plasmin activity in the patient. Also provided are methods for the identification of compounds or molecules that increase plasmin activity, comprising determining whether the compound or molecule binds to a binding site on ?2-antiplasmin which increases the conversion of ?2-antiplasmin from an inhibitor to a plasmin substrate, wherein the compound or molecule is not an antibody, thereby identifying a compound or molecule which increases plasmin activity. Further provided are pharmaceutical compositions and methods of use thereof for the treatment of myocardial infarction, thrombosis, ischemic stroke, and pulmonary embolism.

Abstract: The composition and method for healing tissues is a medicinal composition for facilitating the growth, protection and healing of tissues and cells in animals and humans. The composition is formulated as a either a powder, gel, paste, film, fluid injectable, rehydratable freeze-dried paste or sponge, sprayable solution, topically applied patch with adhesive and reservoir system, an intermediate for coatables such as films and bandages, a matrix for membranes, or as a matrix of flexible polymer(s), or delivered as either an orally ingestible liquid, tablet or capsule. The main ingredient of the formulated compositions is hydrolyzed collagen, which can be combined with polysulfated glycosaminoglycans, hyaluronic acid or salts thereof, or a glucosamine salt, and mixtures thereof. The composition may be formulated as an aqueous eye drop solution.

Abstract: The invention relates to biotinylated low molecular weight heparins comprising constituent polysaccharides having at their reducing ends at least one covalent bond with biotin or a biotin derivative, and also to the process for preparing them, to pharmaceutical compositions containing them and to their therapeutic use.

Abstract: The disclosure provides in vitro and in vivo methods for identifying Heparins and Heparinoids that modulate the activity of selectins. The disclosure also provides Heparins and Heparinoids that modulate the activity of selectins. The identification and isolation of these heparin formulations has the potential to mediate a wide variety of pathologies mediated by P- and/or L-selectin, including hematogenous metastasis, diseases associated with inflammation (e.g., asthma, arthritis, allergic dermatitis), ischemia-reperfusion injury, or other pathologies such as sickle cell anemia. Selectin inhibition can be achieved at plasma concentrations lower than those that cause excessive anticoagulation or unwanted bleeding in a human subject.

Abstract: The present invention relates to a process for the preparation of sulphated glycosaminoglycans derived from N— acetylheparosan which comprises: a) N-deacetylation and N-sulphation of the N-acetylheparosan polysaccharide prepared from natural or recombinant bacterial strain, preferably K5 E. coli, b) enzymatic epimerization with the glucuronyl C5-epimerase enzyme, c) partial O-sulphation followed by a partial O-desulphation, d) partial 6-O-sulphation, e) N-sulphation and an intermediate step of controlled depolimerization characterised by the fact that both O-sulphations (O-sulphation and 6O-sulphation) are partial. Furthermore the invention relates to the products obtained according to the process which show a ratio between the anti-Xa activity and anti-IIa activity equal to or higher than 1 and to compositions comprising said products in combination with suitable and pharmaceutically acceptable excipients and/or diluent.

Abstract: The invention relates, in part, to methods and products related to producing low molecular weight heparin.