Abstract: The present invention provides a pharmaceutical composition comprising a binary conjugate, DC009, which is a conjugate of a thrombolytic peptide (Pro-Ala-Lys) and a tetrahydroisoquinoline compound having two C1-4 alkyl groups via a lysine linking arm, and a pharmaceutical acceptable carrier. The composition has a pH less than 6.5, preferably has a pH about pH 2-5.5 The composition may comprise a pharmaceutical acceptable excipient such as mannitol, sorbitol, sucrose, lactose, or trehalose.

Abstract: Provided herein are integrin antagonists and methods of using the same. For example, one or more of the compounds or polypeptides provided herein can be used in the treatment of disorders such as heart attacks, stroke, and cancer metastasis.

Abstract: Medium chain fatty acids or a composition comprising medium chain fatty acids for use in the prevention or treatment of cardiac enlargement, valvular heart disease and/or a condition associated with either of the foregoing in a human.

Abstract: Capsules contain in their interior a water-based substance, and are coated with a film of alginate of an alkaline earth metal selected from calcium and magnesium. The capsules are of a larger size than previous capsules, while maintaining their sphericality. The capsules of water-based substances are obtained by incubating the capsules in suspension.

Abstract: The object of the present invention relates to a novel family of peptide conjugates of formula (I): A-X1-X2-Pro-Ala-X—B??(I) wherein: A represents a hydrogen atom, a C6 to C20 acyl group or a cholesterol residue; X1 represents a covalent bond, an alanine or a proline; X2 represents an arginine, a lysine, or an alanine; X represents a lysine, an alanine, or a phenylalanine; and B represents a hydroxyl or an amine; or one of its preferentially pharmaceutically, dermatologically or cosmetically acceptable salts, as well as their synthesis processes and their uses for reducing hair loss and stimulating hair growth.

Abstract: Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH2—SO3H)COOH or Arg-Gly-NH—CH(CH2—SO3H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, stereoisomers, multimers, cyclic forms, linear forms, drug-conjugates, pro-drugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibiting cellular adhesion to RGD binding sites or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.

Abstract: The invention provides, inter alia, fatty acyl hydroxy fatty acid (FAHFA; a novel class of estolide-related molecules) and diagnostic and treatment methods for a variety of disorders—including diabetes-related disorders, Metabolic Syndrome, polycystic ovarian syndrome, cancer, and inflammatory disorders—using them; as well as methods of screening for additional compounds that are useful in treating these disorders and/or that modulate FAHFA levels, FAHFA-mediated signaling, and FAHFA-mediated biological effects.

Abstract: Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH2—SO3H)COOH or Arg-Gly-NH—CH(CH2—SO3H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, stereoisomers, multimers, cyclic forms, linear forms, drug-conjugates, pro-drugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibiting integrins including but not necessarily limited to ?5?1-Integrin, ?v?3-Integrin and ?v?5-Integrin, inhibiting cellular adhesion to RGD binding sites, preventing or treating viral or other microbial infections, inhibiting angiogenesis in tumors, retinal tissue or other tissues or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.

Abstract: Factor V peptides and methods of use thereof are disclosed.

Abstract: The present invention relates to the preparation of a compound library comprising the following steps: i. Having available at least two different compounds each comprising at least a dioxaborolane or dioxaborinane ring. In said compounds: the boron of the dioxaborolane or dioxaborinane ring is directly linked to a carbon atom of a hydrocarbon radical; at least one carbon atom of the dioxaborolane or dioxaborinane ring is monosubstituted, the other carbon atoms of the dioxaborolane or dioxaborinane ring being non-substituted or monosubstituted; in at least two compounds, the hydrocarbon radicals linked to the boron are different; in at least two compounds, the substituents carried by at least one of the carbon atoms of the dioxaborolane or dioxaborinane rings are different and/or the size of the boronic ester ring is different; ii. Reacting the compounds of step (i.) and forming, by a boronic ester metathesis reaction, the library comprising at least four different compounds.

Abstract: Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH2—SO3H)COOH or Arg-Gly-NH—CH(CH2—SO3H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, stereoisomers, multimers, cyclic forms, linear forms, drug-conjugates, pro-drugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibiting integrins including but not necessarily limited to ?5?1-Integrin, ?v?3-Integrin and ?v?5-Integrin, inhibiting cellular adhesion to RGD binding sites, preventing or treating viral or other microbial infections, inhibiting angiogenesis in tumors, retinal tissue or other tissues or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.

Abstract: The present invention relates to an injectable preparation comprising particles or fibrils with length less than 10 ?m and at least one pharmaceutically acceptable vehicle or excipient. The particles or fibrils comprise proteins or peptides inducing adhesion and activation of the platelets, or even aggregation thereof. The preparation is useful for treating hemorrhages.

Abstract: Embodiments herein report methods and compositions for treating cardiac conditions. In certain embodiments, compositions and methods relate to reducing, inhibiting or treating a subject having or suspected of undergoing cardiac remodeling after a cardiac event. Other embodiments herein relate to compounds including naturally occurring and synthetic compositions of alpha-1 antitrypsin and fragments thereof.

Abstract: Embodiments of the present invention relate to compositions and methods for treatment of subjects in need of or having a bone marrow transplant. Certain embodiments describe compositions and methods for treatment of conditions associated with bone marrow transplantations in a subject, for example, Graft versus Host Disease (GvHD) or bone marrow transplantation rejection. Some embodiments concern early or immediate bone marrow transplantation rejection. Certain embodiments relate to compositions and uses of alpha1-antitrypsin (?1-antitrypsin, AAT) and carboxyterminal peptide derivatives thereof and/or compositions and uses of serine protease inhibitors, immunomodulators or anti-inflammatory agent activity similar to that of AAT.

Abstract: The conversion of a peptide aldehyde to a hydrosulfite adduct can be used to increase the aqueous solubility in the purification of the peptide aldehydes. Advantageously, this hydrosulfite adduct is itself effective as a subtilisin inhibitor and stabilizer and it can also stabilize a second enzyme if present. The hydrosulfite adduct is effective as a subtilisin inhibitor, and it maintains its inhibitory and stabilizing effect in a liquid detergent during storage. Thus, use of the hydrosulfite adduct can avoid the cost and time of converting it back to the peptide aldehyde and subsequent drying of the peptide aldehyde can be saved, and this can avoid the inconvenience of handling the peptide aldehyde in powder form or as a highly diluted aqueous solution.

Abstract: An extract for preventing or treating thrombotic diseases, particularly, an extract of at least one of leeches and earthworms having a molecular weight of no more than 5,800 daltons is provided, wherein the extract includes 15% to 38% amino acid, 40% to 60% saccharide and 0.3% to 1% hypoxanthine. Processes for preparation, pharmaceutical compositions and uses thereof are also provided. Compared to conventional arts, the extract has safety greatly improved and drug actions maintained and even improved.

Abstract: The embodiments relate generally to medical devices and to methods of their manufacture. One aspect provides devices including chitosan fibers that are a free of chemical cross linking. Another aspect provides a method of manufacturing such devices.

Abstract: Methods for the expression and purification of non-N-glycosylated human Annexin A2 in yeast, e.g., in Pichia pastoris, purified Annexin A2 produced by those methods, and methods of using the Annexin A2.

Abstract: Matrix metalloproteases (MMPs) play many important roles in normal and pathological remodeling processes including atherothrombotic disease, inflammation, angiogenesis and cancer. This invention relates to the activation of protease-activated receptor-1 (PAR-1) by endogenous platelet MMP-1 collagenase on the surface of platelets. Exposure of platelets to fibrillar collagen converts the surface-bound pro-MMP-1 zymogen to active MMP-1, which promotes aggregation through PAR-1. MMP-1 is shown to cleave the PAR-1 extracellular domain at a novel site, which then strongly activates Rho-GTP signaling pathways, cell shape change and motility, and MAPK signaling. Blockade of MMP-PAR1 suppresses thrombogenesis under arterial flow conditions and inhibited thrombosis in animals. These studies provide a link between matrix-dependent activation of metalloproteases and platelet-G protein signaling and identify MMP-1/PAR-1 as a new target for the treatment and prevention of arterial thrombosis and other thrombotic diseases.

Abstract: The present invention relates to the use of thrombomodulin analogues for the manufacture of a medicament for the treatment of coagulopathy with hyperfibrinolysis, such as haemophilia disorders. These thrombomodulin analogues exhibit at therapeutically effective dosages an antifibrinolytic effect. Novel protein modifications together with methods for their identification are disclosed.

Abstract: The invention relates to a peptide compound and its pharmaceutical composition for inhibiting platelet aggregation and preventing/treating thrombogenic diseases. The invention develops pentapeptides and hexapeptides derived from snake venom C-type lectin-like proteins (CLPs) fragments, which can inhibit platelet aggregation and have antithrombotic activity without hemorrhagic tendency. Accordingly, they can be used as potential agents for the prevention and therapy of thrombogenic diseases.

Abstract: The present invention provides stimulus responsive nanocomplexes comprising a masking moiety, e.g., a peptide, and a therapeutic moiety, e.g., an anti-coagulant. The invention also provides methods for treating or preventing a condition, such as a hypercoagulable state, e.g., blood clotting disorders or a cardiovascular disease, in a subject.

Abstract: The present invention relates to chemically modified heparin for use in the treatment of sickle cell disease, with an antifactor II activity of less than 10 IU/mg, an antifactor Xa activity of less than 10 IU/mg and an average molecular weight (Mw) between about 6.5 and 9.5 kDa.

Abstract: The present invention relates to antibody molecules against anticoagulants, in particular dabigatran, and their use as antidotes of such anticoagulants.

Abstract: Provided herein are compounds that inhibit a binding interaction between a ? integrin and a G protein subunit, as well as compositions, e.g., pharmaceutical compositions, comprising the same, and related kits. In some embodiments, the compound is an antibody or antibody analog, and, in other embodiments, the compound is a peptide or peptide analog. Also provided are methods of using the compounds, including methods of treating or preventing a medical condition, such as stroke, heart attack, cancer, or inflammation.

Abstract: Factor V peptides and methods of use thereof are disclosed.

Abstract: The present invention relates to compositions and methods for preventing, treating or delaying various cardiovascular diseases or disorders in mammals, particularly in humans. More particularly, the present invention provides for compositions and methods for preventing, treating or delaying various cardiovascular diseases or disorders using, inter alia, a neuregulin protein, or a functional fragment thereof, or a nucleic acid encoding a neuregulin protein, or a functional fragment thereof, or an agent that enhances production and/or function of said neuregulin.

Abstract: The present invention relates to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, and more particularly, to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, including a first step of dissolving a biodegradable polymer in a non-volatile polar organic solvent, a second step of adding poorly soluble drugs to water and the biodegradable polymer solution to produce a dispersion, and a third step of adding the dispersion to emulsifier solutions in a batch under the condition of low mechanical energy level stirring.

Abstract: The present invention is directed to a therapeutic agent comprising a GPIIIa(49-66) specific targeting agent and a thrombi-specific homing agent. Also disclosed is the use of the therapeutic agent in carrying out a method of treating thromboembolic disorders and a method of inducing platelet fragmentation.

Abstract: The present disclosure provides combinations of salicylamide compounds, or pharmaceutically acceptable salts thereof, and histamine blocking agents, or pharmaceutically acceptable salts thereof, for antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.

Abstract: ClotBlock is a lyophilized fibrin hemostatic designed for use an adjunct or primary treatment in moderate to severe hemorrhage. It can be applied directly to the wound in a laparotomy procedure or as non-invasive sealant. Its crosslinking technology generates a strong and safe adhesive fibrin sealant required for high volume hemostasis. The attachment properties of the cake as well as the rapid formation of and stability of the fibrin clot ensures that a strong stable fibrin clot is formed within 1 to 5 minutes depending on the grade of the wound. The agent is safe, biocompatible, biodegradable and can be stored at room temperature for one year.

Abstract: The present invention relates to the use of at least one antibody and/or one inhibitor for inhibiting factor XII and for preventing the formation and/or the stabilization of three dimensional thrombi. It also relates to a pharmaceutical formulation and the use of factor XII as an anti-thrombotic target.

Abstract: Methods of treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing percutaneous coronary intervention (PCI), comprising administering to the patient a pharmaceutical composition comprising cangrelor. The method may further comprise administering an additional therapeutic agent to the patient, the additional therapeutic agent comprising a P2Y12 inhibitor. Pharmaceutical compositions useful for treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing PCI. The pharmaceutical compositions comprise cangrelor. Methods of preparing a pharmaceutical composition for treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing PCI, comprising admixing cangrelor with one or more pharmaceutically acceptable excipients. An ischemic event may include stent thrombosis, myocardial infarction, ischemia-driven revascularization, and mortality.

Abstract: Peptides useful as angiotensin converting enzyme inhibitors are provided. Also provided are compositions comprising one or more of the peptides and methods for preventing, treating and/or diminishing one or more syndromes associated with angiotensin converting enzyme by using the peptides.

Abstract: A pharmaceutical combined preparation containing a therapeutic protein having SH-groups which are nitrosated and a compound containing thiol groups and having an average molecular weight of at most 10,000.

Abstract: The present invention relates to the novel use of prostacyclin analogs for prevention and/or treatment of capillary leakage during surgery. The treatment of the present invention mediates discrete or minimal effects on haemostasis and vasodilation. Thus the present invention provides prostacyclin and analogs thereof for treatment which prevents capillary leakage while minimizing the risk of bleeding. The present invention further provides pharmaceutical compositions and kits of parts comprising prostacyclin or analogs thereof, and methods for treatment.

Abstract: The present invention relates to chimeric Factor VII polypeptides and methods of using the same.

Abstract: The present invention provides a method for the prevention and/or reduction of peri- or postoperative complications following surgical intervention, such as complications following vascular surgery, especially peripheral vascular surgery, comprising administering a therapeutically effective amount of Annexin (A5) or a functional analogue or variant thereof to a patient in need of such treatment, Also provided is a pharmaceutical composition comprising a therapeutically effective amount of Annexin (A5) or a functional analogue or variant thereof for use in the prevention and/or reduction of peri- or postoperative complications following surgical intervention, such as complications following vascular surgery, especially peripheral vascular surgery.

Abstract: Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise particular glycomimetics alone or linked to a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids) or a member of a class of compounds termed BACAs (Benzyl Amino Carboxylic Acids).

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, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb), and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

Abstract: Methods of using an ETB receptor agonist, such as IRL-1620, for the treatment of stroke or cerebrovascular accidents are disclosed. The ETB receptor agonist is used alone or in combination with a second agent useful in the treatment of stroke or other cerebrovascular accident.

Abstract: The embodiments provide methods of administering a high dose or a loading dose of a TPO modulator to a subject. The embodiments further provide methods of treating thrombocytopenia and/or neutropenia in a subject. Additionally, the embodiments further provide methods of increasing platelet production and/or enhancing the number of peripheral blood stem cells in a subject.

Abstract: The present invention relates to methods and compositions for modulating platelet activity by inhibiting or activating glutamate receptors. The invention further relates to preventing or treating thrombotic diseases.

Abstract: The present application provides compositions and methods for modulating the activity and quantity of platelets and preventing and treating disorders or diseases associated with abnormal activity and quantity of platelets.

Abstract: The present invention is directed to methods of using combination therapies containing [2-({4-[(dimethylamino)iminomethyl]phenyl}carbonylamino)-5-methoxyphenyl]-N-(5-chloro(2-pyridyl))carboxamide for the treatment of thrombotic disease(s) and pharmaceutical compositions thereof.

Abstract: The present invention relates to: a composition for dissolving thrombi comprising a peptide comprising the Arg-Gly-Asp motif; a pharmaceutical composition for treating stenotic or occlusive vascular diseases which comprises the same; and a thrombus dissolving method and a method for treating stenotic or occlusive vascular diseases, comprising the step of administering the same. The compositions and methods of the present invention have the advantage that they effectively break down already formed thrombi by adopting the principle of targeting integrin within the thrombus such as platelet surface GPIIb-IIIa, which is not the same as the existing principle of plasminogen activation. Also, the compositions and methods of the present invention have a nerve-protecting function as they effectively open as far as the microvasculature, without the occurrence of restenosis after penetration.

Abstract: Conjugates of a Factor IX moiety and one or more water-soluble polymers are provided. Typically, the water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided (among other things) are compositions comprising the conjugates, methods of making the conjugates, and methods of administering to a patient compositions comprising the conjugates.

Abstract: The present invention relates to a chimeric hirudin protein comprising a carrier attached to the N-terminus of hirudin, with an intervening plasmin cleavage site. The chimeric hirudin protein contains a relatively inactive form of hirudin. However, when such chimeric hirudin protein being cleaved by plasmin in the vicinity of a clot and, ultimately causing the release of active hirudin and the reduction of the size of the clot. The chimeric hirudin protein exhibited much slower clearance in mice than unfused wild-type hirudin.

Abstract: The present invention relates to binding molecules such as antibodies that specifically bind plasma coagulation factor XI and that inhibit factor XI activation and/or activity. The factor XI-binding molecules of the invention may used in methods for preventing or treating diseases, disorders and/or conditions that are mediated by factor XI activation and/or wherein inhibition of factor XI has a beneficial effect.

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.