Abstract: The present invention relates to nucleic acids and polypeptides encoded thereby, whose expression is modulated in brain microvascular endothelial cells undergoing early dynamic inflammation-induced changes in blood-brain bather functionality. Such polypeptides are referred to as lipopolysaccharide-sensitive (LPSS) polypeptides. These nucleic acids and polypeptides may be useful in methods for controlling blood-brain bather properties in mammals in need of such biological effects. This includes the diagnosis and treatment of disturbances in the blood-brain/retina barrier, brain (including the eye) disorders, as well as peripheral vascular disorders. Additionally, the invention relates to the use of anti-LPSS polypeptide antibodies or ligands as diagnostic probes, as blood-brain barrier targeting agents or as therapeutic agents as well as the use of ligands or modulators of expression, activation or bioactivity of LPSS polypeptides as diagnostic probes, therapeutic agents or drug delivery enhancers.

Abstract: In one embodiment, the invention provides a method of suppressing, inhibiting, preventing, or treating conjunctivitis in a subject, comprising the step of administering an effective amount of a lipid or phospholipid moiety bound via an ester or amide bond to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof to a subject with conjunctivitis.

Abstract: A filter and a method of forming a suture structure. The filter includes layered structure(s) interior to the filter. Each layered structure includes a carbon structure comprising carbon and a coating on a surface of the carbon structure. Each layered structure may further include a heparin layer that includes heparin and is on the coating. The coating of the filter includes cellulose, PMMA, PEMA, or PHEMA. The carbon structure may include an activated charcoal layer or carbon nanotube(s). The layered structure is configured to remove a contaminant flowing through the filter. The method of forming the suture structure includes forming a film on a suture that has been previously formed on a mammal. The film includes both a coating on the suture and a heparin layer that includes heparin and is on the coating. The coating of the suture structure includes cellulose, PMMA, PEMA, or PHEMA.

Abstract: Preparations of low molecular weight heparins (LMWHs) having improved properties, e.g., properties that provide a clinical advantage, are provided herein. Methods of making and using such preparations as well as methods of analyzing starting materials, processing, intermediates and final products in the production of such LMWH preparations are provided.

Abstract: The present invention provides an agent which induces acceleration of hard tissue formation, acceleration of cell differentiation and increase in cellular alkaline phosphatase activity, by directly acting on the cell. Specifically, it provides a hard tissue formation promoter, a cell differentiation inducer and a cellular alkaline phosphatase activity reinforcing agent comprising, as an active ingredient, a glycosaminoglycan or a salt thereof that keeps sulfate group and has the characteristics of the following (1) and (2): (1) a basic structure is a disaccharide repeating structure consisting of a hexuronic acid residue and a glucosamine residue, (2) one or less of the position among a 2-position hydroxyl group of a hexuronic acid residue, a 6-position hydroxyl group of a glucosamine residue and a 2-position amino group of the glucosamine residue in the basic structure of the aforementioned (1) does not have the sulfate group.

Abstract: Methods are presented for attenuating myelosuppressive side effects of treatment regimens, promoting thrombopoiesis and neutrophil production, and increasing efficacy of treatment regimens, by administering PF4-interacting heparinoids.

Abstract: The disclosure features methods of analyzing preparations of heparin, and materials derived from heparin using strong anion exchange high performance liquid chromatography (SAX-HPLC).

Abstract: This invention provides for the use of compounds represented by the structure of the general formula (A): wherein L is a lipid or a phospholipid, Z is either nothing, ethanolamine, serine, inositol, choline, or glycerol, Y is either nothing or a spacer group ranging in length from 2 to 30 atoms, X is a physiologically acceptable monomer, dimer, oligomer, or polymer, wherein X is a glycosaminoglycan; and n is a number from 2 to 1000, wherein any bond between L, Z, Y and X is either an amide or an esteric bond in treating a subject suffering from a disease associated with elevated level of a Matrix Metalloprotease (MMP) such as a malignant cancer.

Abstract: Polysaccharide preparations lacking substantial anticoagulant activity are provided herein. Methods of making and using such preparations are provided.

Abstract: A stent is provided in combination with delivery of a tocopherol agent, and in particular a des-methyl tocopherol agent, and further beneficially a gamma-tocopherol agent, so as to reduce restenosis along the vessel or other lumenal wall where the stent is implanted. In particular applications, the stent is an endolumenal stent, and more specific beneficial applications is an endovascular stent, and the gamma-tocopherol elutes from a coating or carrier coupled with the stent. Certain combinations are provided with the des-methyl-tocopherol or phytyl substituted chromanol, e.g. gamma-tocopherol, combined with an additional agent such as an anti-restenosis agent, e.g. sirolimus, tacrolimus, everolimus, or paclitaxel, in order to provide synergistic benefit to tissues along the stented or recanalized regions. Other forms of tocopherol or tocotrienol, or other phytyl substituted chromanols, and other compounds such as palm oil, are ailso contemplated. for use to treat restenosis.

Abstract: Methods are presented for attenuating myelosuppressive side effects of treatment regimens, promoting thrombopoiesis and neutrophil production, and increasing efficacy of treatment regimens, by administering PF4-interacting heparinoids.

Abstract: The present invention provides methods and compositions for modulating certain metabolic processes and for treating a variety of disorders associated with metabolic syndrome, including insulin related disorders, ischemia, oxidative stress, atherosclerosis, hypertension, obesity, abnormal lipid metabolism, and stroke by administering an effective dose of a chloroquine compound. The invention also provides methods and compositions relating to administering an effective dose of a chloroquine compound in combination with at least a second pharmaceutically active ingredient or compound including an antihyperglycemic diabetes treatment, an antihypertensive agent, an antithrombotic agent, and/or an inhibitor of cholesterol synthesis or absorption.

Abstract: Polysaccharide preparations lacking substantial anticoagulant activity are provided herein. Methods of making and using such preparations are provided.

Abstract: The present invention is based on the discovery of genetic polymorphisms that are associated with venous thrombosis. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.

Abstract: The invention concerns novel biotinylated hexadecasaccharides of general formula (I) wherein: Biot is a biotin derivative; R, R1 and R2, represent independently of one another a C1-C6 alkoxy or and —OSO3; R3 represents a C1-C6 alkoxy or an —OSO3, or R3 constitutes a —O—CH2— bridge; Pe represents a saccharide concatenation; as well as their pharmaceutically acceptable salts, and their use as medicines.

Abstract: A pharmaceutical composition comprising a pharmaceutically effective amount of a pharmaceutically active substance and a pharmaceutically acceptable carrier including a cationic excipient, wherein said cationic excipient is a labile ester of betaine and a lipophilic alcohol having at least one primary hydroxyl group. Also, the use of a labile ester of betaine and a lipophilic alcohol having at least a primary hydroxyl group as a cationic excipient in a carrier for a pharmaceutical composition comprising a pharmaceutically active substance.

Abstract: The instant invention relates to decasaccharides of formula (I): wherein Ac represents an acetyl group and R represents a group of formula —OH or —OSO3?, in their acid form or in the form of any one of their pharmaceutically acceptable salts, and to their process of preparation. The oligosaccharides of formula (I) are useful as antithrombotic agents.

Abstract: The present invention relates to compounds and compositions useful for inhibiting and/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: The present invention discloses a magnetic nanodrug for treating thrombosis, which comprises a core formed of magnetic nanoparticles, a shell enveloping the core and made of carboxyl-functionalized polyaniline, and a thrombosis-treatment drug covalently bonded to the shell. The magnetic nanodrug of the present invention is non-toxic to vascular endothelial cells, has superior stability, features superparamagnetism, and can be uniformly dissolved in water. Therefore, the magnetic nanodrug for treating thrombosis can be guided by an external magnetic field to concentrate on a specified region and increase the effect of thrombosis treatment.

Abstract: A medicament for treating cystitis and a method of treatment are provided. An agent to repair the damaged glycosaminoglycan (“GAG”) layers lining the urothelium, noted in cystitis, such as pentosan polysulfate, hyaluronic acid, chondroitin, etc., is provided in a liposomal carrier. Cystitis is treated by intravesically administering to a patient a therapeutically effective dose of the medicament.

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: The present invention is related to compositions which can undergo targeted degradation under certain physiological reducing conditions. The compositions may, for example, be hydrogels in which maleimide-functionalized low molecular weight heparin is cross-linked with various thiol-functionalized polyethylene glycol multi-arm star polymers. Both the gelation and degradation of the hydrogels can be modified by careful selection of the thiol. For example, hydrogels prepared from aryl thiol-maleimide adducts can undergo a retro Michael addition-type reaction, leading to degradation of the composition and release of the bioactive molecule.

Abstract: The invention relates to compositions and methods for the modulation of the permeability of the epithelial cell barrier complex. In particular, the invention provides compositions and methods for using polysaccharides, preferably glycosaminoglycans, and agents that modify cell surface glycosaminoglycans, preferably glycosaminoglycan-degrading enzymes to modulate intercellular junctions. The compositions and methods provided can be used to facilitate the delivery of biologically active molecules.

Abstract: A method of treating protracted labor in a pregnant woman comprises administering to a pregnant woman an effective amount of a depolymerized low molecular weight heparin treated with periodate to eradicate antithrombin III binding affinities, thereby exhibiting an anticoagulant activity of 10 BP units/mg or less and an average molecular weight not higher than 10000 Da to prime or curatively treat the cervix and myometrium and for treatment of slow progress of labor. A method for prophylactic priming or curative treatment of the cervix and the myometrium for establishing effective labor in a pregnant woman comprises administering to a pregnant woman an effective amount of a depolymerized low molecular weight heparin as described to prophylactically prime or curatively treat the cervix and myometrium and for establishing effective labor in the pregnant woman.

Abstract: The instant invention relates to the heptasaccharide of formula (I): in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of formula (I) is useful as an antithrombotic agent.

Abstract: The invention relates to methods and products for characterizing and using polysaccharides. Low molecular weight heparin products and methods of use are described. Methods for characterizing purity and activity of polysaccharide preparations including glycosaminoglycans such as heparin are also described.

Abstract: Provided herein are methods of diagnosing and/or treating malignant or pre-malignant conditions in a subject. Overexpression of copy number variant-dependent genes, e.g., genes encoding a cell surface receptor, resulting from copy number changes compared to control is diagnostic of the condition, such as multiple myeloma or monoclonal gammopathy of undetermined significance. Also provided are methods for treating malignant conditions, such as multiple myeloma or a hyperdiploid subtype, with therapeutic agents, with or without other anti-cancer drugs, to downrregulate the overexpressed CNV genes and/or up-regulate the underexpressed genes. Furthermore, methods for lowering drug resistance in multiple myeloma cells via inhibition of platelet activation or thrombin release and for increasing survivability of a multiple myeloma subject via lithibition of PSMD4 gene to increase b-catenin protein expression are provided.

Abstract: The present invention provides non-anticoagulant sulfated or sulfonated polysaccharides (NASPs), which accelerate the blood clotting process. Also provided are pharmaceutical formulations comprising a NASP of the invention in conjunction with a pharmaceutically acceptable excipient and, in various embodiments, these formulations are unit dosage formulations. The invention provides a NASP formulation, which is orally bioavailable. Also provided are methods for utilizing the compounds and formulations of the invention to promote blood clotting in vivo as therapeutic and prophylactic agents and in vitro as an aid to studies of the blood clotting process.

Abstract: The present invention relates to compounds which are capable of exerting an inhibitory effect on the Na+ glucose cotransporter SGLT in order to hinder glucose and galactose absorption, as well as on lipase thus reducing dietary triglyceride metabolism, for use in the treatment of conditions which benefit therefrom (diabetes, Metabolic Syndrome, obesity, prevention of weight gain or aiding weight loss). These compounds comprise a non-absorbable, non-digestible polymer having a glucopyranosyl or galactopyranosyl or equivalent moiety stably and covalently linked thereto, said glucopyranosyl or galactopyranosyl moiety being able to occupy the glucose-binding pocket of a SGLT transporter.

Abstract: The disubstituted piperazine analogs (DPAs) derivative compound and DPAs amine complex compound disclosed in the present aspects have characterized by presented pharmaceutics having functions to improve lipolysis, such as inhibiting obesity hyperlipidemia, and atherosclerosis.

Abstract: The invention relates to methods of use for compounds in treating, reducing the incidence, reducing the severity or pathogenesis of an intestinal disease or condition in a subject, including, inter alia, inflammatory bowel disease, Crohn's disease, ulcerative colitis, or a combination thereof.

Abstract: The instant invention relates to the decasaccharide of formula (I), wherein Ac represents an acetyl group: in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of formula (I) is useful as an antithrombotic agent.

Abstract: There is described inter alia a medical device having a surface which comprises a coating layer, the coating layer being a biocompatible composition comprising an anti-coagulant entity capable of interacting with mammalian blood to prevent coagulation or thrombus formation, which anti-coagulant entity is covalently attached to the surface through a linker comprising a thioether.

Abstract: The present invention relates to a method of interfering with dengue infection comprising interfering with dengue virus binding to a syndecan present on a cell targeted by dengue virus. The present invention further relates to treating a patient for dengue virus infection comprising administering to a patient, either having a dengue infection or a patient exposed to dengue infection, an effective amount of an agent that interferes with dengue virus binding to a syndecan on a surface of a cell targeted by dengue virus. The present invention further relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier, and an effective amount of an agent that interferes with dengue virus binding to a syndecan on a surface of a cell targeted by dengue virus.

Abstract: Methods to reduce damage to organelles, cells, tissues, organs and organ systems or components thereof caused by strain due to mechanical stress, including stretch stress and shear stress, are provided. The methods involve treating the organelles, cells, tissues, organs, and organs systems or components thereof (such as veins used for grafts in bypass surgery) with PX-18 and related compounds. Treatment with PX-18 and related compounds reduces damage due to stress and improves the functioning of the cells, tissues, organs or organs systems or components thereof. For example, the methods prevent the buildup of atherosclerotic plaque in transplanted (grafted) veins after coronary bypass surgery.

Abstract: Methods and compositions related to promoting hair growth are described.

Abstract: Invented is a method of treating thrombocytopenia in a human, in need thereof which comprises the in vivo administration of a therapeutically effective amount of a peptide or a non-peptide TPO receptor agonist and an anti-clotting agent or agents, and optional further active ingredients, to such human.

Abstract: Compositions, methods, and systems are disclosed for the development and use of heparosan, a natural polymer related to heparin, as a new therapeutic modifying agent or vehicle which can modulate drug cargo pharmacokinetics and behavior within a mammalian patient.

Abstract: Methods and compositions related to targeting agents to tumor tissue are described.

Abstract: The embodiments provide a carbon nanocapsule conjugated with at least one of the anticoagulants on the surface and an antithrombotic drug containing the anticoagulant-conjugated carbon nanocapsule as an active ingredient. The anticoagulant-conjugated carbon nanocapsule has less cytotoxicity and good biocompatibility. A method for preparing the anticoagulant-conjugated carbon nanocapsule is also provided.

Abstract: The disclosure relates to edible and biodegradable eating utensils and edible and biodegradable containers. In one aspect a method of making and preserving an edible and biodegradable utensil or container is disclosed.

Abstract: An improved method of treating lower urinary dysfunctional epithelium (LUDE) or a disease, condition, or syndrome associated with LUDE, including interstitial cystitis, comprises the step of administering orally a pharmaceutically effective quantity of heparin to a patient in need of treatment for LUDE or a disease, condition, or syndrome associated with LUDE in order to treat LUDE or a disease, condition, or syndrome associated with LUDE. The heparin can be administered together with a quantity of a penetration enhancer that is sufficient to result in a tissue concentration of heparin that is sufficient to treat LUDE or a disease, condition, or syndrome associated with LUDE. A suitable penetration enhancer is sodium N-[8-(2-hydroxybenzoyl)amino]caprylate.

Abstract: The present invention relates to a method for inhibiting oxidative damage of islet beta cells in vivo in a subject by administering to the subject a therapeutically effective amount of heparan sulfate capable of protecting islet beta cells from reactive oxygen species or in vitro by exposing isolated islet beta cells, prior to transplantation, to a concentration of heparan sulfate that protects them from reactive oxygen species.

Abstract: The present invention provides methods for the production of N-deacetylate N-sulfate derivatives of non-sulfated N-acetyl heparosan (HS) polysaccharides, compounds thus obtained and compositions comprising same. This invention also provides applications of N-deacetylate N-sulfate derivatives of non-sulfated N-acetyl heparosan (HS) polysaccharides, and compositions comprising same, for use in controlling coagulation and treating thrombosis.

Abstract: The present invention provides compositions containing clopidogrel, present as a free base or a pharmaceutically acceptable salt thereof, and sulfoalkyl ether cyclodextrin (SAE-CD). The compositions can be liquid, suspension or solid compositions. They can be adapted for oral, peroral or parenteral administration. The SAE-CD serves to aid in dissolution and stabilization of the clopidogrel in aqueous media. The stability of clopidogrel against hydrolytic degradation, thermal degradation, and photolytic degradation are improved. SAE-CD provides improved results over other cyclodextrin derivatives. The SAE-CD-containing composition of clopidogrel can be provided in liquid form, solid form or as a reconstitutable powder. Both ready-to-use and concentrated liquid compositions can be prepared. The liquid composition is optionally available as a clear solution.

Abstract: The disclosure features methods of analyzing preparations of heparin, and materials derived from heparin using strong anion exchange high performance liquid chromatography (SAX-HPLC).

Abstract: Aspects of the invention include methods for enhancing blood coagulation in a subject. In practicing methods according to certain embodiments, an amount of a non-anticoagulant sulfated polysaccharide (NASP) is administered to a subject to enhance blood coagulation in the subject. Also provided are methods for preparing a NASP composition having blood coagulation enhancing activity. Compositions and kits for practicing methods of the invention are also described.

Abstract: A composition for placental exfoliation and a method for placental exfoliation. The composition for placental exfoliation contains an arachidonic acid derivative or the like, and the method for placental exfoliation comprises the step of administering an arachidonic acid derivative or the like to a mammal after the fetal delivery.

Abstract: The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof as an antithrombotic treatment in patients undergoing hip replacement surgery, wherein said use involves an improved safety in terms of clinically relevant bleedings and of major bleedings compared to a standard antithrombotic treatment.

Abstract: The present invention relates to a topical pharmaceutical composition comprising heparin and to the use thereof for preventing a functional complication of A-V fistulas and A-V grafts in chronic haemodialysis patients.