60 results about "Blood Platelet Aggregation Inhibitors" patented technology

A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically acceptable salt thereof useful as a platelet aggregation inhibitor.

The present invention relates to a novel process for the manufacture of blood-platelet aggregation inhibiting agent. In particular, the present invention is directed to a process for the manufacture of Methyl-(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno [3,2-c]pyridine-S-(4H)acetate bisulfate Form-I.

The present invention provides a composition comprising a platelet aggregation inhibitor, for example, cilostazol, or a salt or derivative thereof, useful in the treatment and prevention of ischemic symptoms. The invention provides a composition which comprises nanoparticulate particles comprising the platelet aggregation inhibitor and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. The invention provides also a composition that delivers a platelet aggregation inhibitor, or nanoparticles comprising the same, in a pulsatile or continuous manner.

[Problem] To provide a compound having excellent platelet aggregation inhibitory activity.[Means for Resolution] It was found that quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. In addition, it was confirmed that these quinolone derivatives also have excellent platelet aggregation inhibitory activity. Based on the above, these quinolone derivatives or pharmaceutically acceptable salts thereof are useful as platelet aggregation inhibitors.

[Problem]Provided is a compound, which exhibits a P2Y12 inhibitory action and is useful as a medical drug, particularly, as a platelet aggregation inhibitor.[Means for Solution]The inventors have eagerly investigated P2Y12 inhibitors. As a result, the inventors have found that a bicyclic heterocyclic compound such as quinazolinedione, isoquinolone, and the like having an amino group substituted with lower alkyl, cycloalkyl, or lower alkylene-cycloalkyl at the specific position exhibits an excellent platelet aggregation inhibitory action, thereby completing the present invention. Since the compound of the invention exhibits excellent P2Y12 inhibitory action and platelet aggregation inhibitory action, it is useful as a platelet aggregation inhibitor.

The present invention relates to a stable solid oral pharmaceutical multi-component composition comprising combination of blood pressure lowering drugs with lipid lowering agent / s and optionally a platelet aggregation inhibitor in a single dosage form. The blood pressure lowering agents are selected from β-adrenergic receptor blocking agent, ACE inhibitor and diuretic. The lipid lowering agent is selected from HMG Co-enzyme-A reductase inhibitor. The pharmaceutical composition made as per present invention a) overcomes any drug-drug interactions, b) exhibits pharmacokinetic and pharmacodynamic profile of individual therapeutic agent, c) has minimal side effects. The invention provides multi-component composition (MCC) to increase adherences to therapy. The MCC as per present invention provides compositions that maintain activity of all active ingredients without significant increase in adverse event profile. The present invention further relates to a method of preparing the said pharmaceutical composition.

Linking Magnesium ions to Nitric Oxide precursor L-Arginine, chemically 2-amino-5-guanidino valeric acid, with a platelet aggregation inhibitor compound such as, but not limited to acetylsalicylic acid or clopidogrel bisulfate, unexpectedly results in a pharmaceutically stabilized compositions with extended shelf life to be taken orally to provide gradual release vasodilatory and anti-platelet aggregation pharmacological activity with reduced potential for producing gastrointestinal lesions. L-Arginine releases ADNO (Arginine derived Nitric Oxide) in the coronary artery epithelium as EDRF (endothelium dependent relaxing factor) to dilate the arteries to promote blood flow to the myocardium, and the platelet aggregation inhibitor such acetylsalicylic acid or clopidogrel and others of this class of drugs inhibits or antagonizes the aggregation adhesion of platelets in the blood stream. Aggregated or clumped blood platelets contribute to arterial stenosis due to formation of atherosclerotic plaques that occlude coronary and other circulatory arteries. In addition to coronary arteries, atherosclerotic plaques can occlude and stenose carotid arteries and femoral arteries due to aggregated or clumped blood platelets, and the subject of this patent discovery will also be of cardiovascular health benefit respectively in preventing carotid cerebrovascular accidents and femoral artery leg circulation disease.

The present invention provides a composition comprising a platelet aggregation inhibitor, for example, cilostazol, or a salt or derivative thereof, useful in the treatment and prevention of ischemic symptoms. The invention provides a composition which comprises nanoparticulate particles comprising the platelet aggregation inhibitor and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. The invention provides also a composition that delivers a platelet aggregation inhibitor, or nanoparticles comprising the same, in a pulsatile or continuous manner.

The invention relates to a blood withdrawal device (10) having an active liquid (12) containing a platelet aggregation inhibitor, a microneedle patch (14) having a plurality of microneedles (20), wherein a plurality of microneedles (20) is configured for dispensing the active liquid (12) into the skin (34) of a patient, and comprising a negative pressure generating device (16) connected to a plurality of microneedles (20) such that blood (46) can be drawn from the skin (34) by means of the microneedles (20). According to the invention the active liquid (12) contains a pain killer, the active liquid (12) is arranged in the blood reservoir (18), and the negative pressure generating device (16) is connected to the blood reservoir (18) such that by generating an excess pressure in the blood reservoir (18), the active liquid (12) can be dispensed by way of microneedles (20), and by generating a negative pressure, blood (46) can be drawn into the blood reservoir (18).

The present invention relates to crystalline form I of Prasugrel hydrogensulfate. A process for the preparation of these salts, pharmaceutical compositions comprising the salts and the use of the salts as a pharmaceutical, in particular as a blood platelet aggregation inhibitor are also described. Seed crystals which can be employed in the above mentioned process as well as a process for their preparation are also disclosed.

The present invention relates to a fused heterocyclic compound having the Formula 1, which is useful as a platelet aggregation inhibitor, a method for preparing the same, and a pharmaceutical composition for inhibiting platelet aggregation comprising the same.

The present invention relates to a compound represented by Formula (I):wherein Ar1, Ar2, R1 and R2 each represent a substituent,a salt thereof, or a solvate of the compound or the salt, and to a medicine containing the same.According to the present invention, a potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.

The present invention relates to a novel process for the manufacture of blood-platelet aggregation inhibiting agent. In particular, the present invention is directed to a process for the manufacture of Methyl-(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-S-(4H)acetate bisulfate Form-I.

The invention pertains to the field of medical technology and relates to a furo [2, 3-h] chromene compound and an application thereof for inhibiting platelet aggregation; the furo [2, 3-h] chromene compound, pharmaceutically-acceptable salt, or stereo-isomers and pre-drugs of the furo [2, 3-h] chromene compound, as well as pharmaceutical compatibility acceptable carriers or diluents of the furo [2, 3-h] chromene compound can be used as platelet aggregation inhibitors. The structural formula of the furo [2, 3-h] chromene compound is as shown above, wherein, X can be chosen from CH2 or C=O, R1 can be independently chosen from H or a substituted or un-substituted aromatic base, R2 can be independently chosen from H or a substituted or un-substituted aromatic base, and R can be independently chosen from H, alkyl group with one to four carbon atoms, chlorine, bromine, fluorin, methoxyl, nitryl or hydroxyl. The furo [2, 3-h] chromene compound has simple synthetic method, adapts to industrialized production and is more stable compared with natural analogues. Shown by biological activity assay, the furo [2, 3-h] chromene compound has antithrombin activity and is a platelet aggregation inhibiting drug.

Novel compounds comprising a guanidine-rich head covalently coupled to one or more oligonucleotide antisense sequences which are useful to modulate blood coagulation by affecting the expression of integrin αIIb or β3 are described herein. This invention also includes pharmaceutical compositions containing these compounds, with or without other therapeutic agents, and to methods of using these compounds as inhibitor of platelet aggregation, as thrombolytics, and / or for the treatment of other thromboembolic disorders. Vivo-MOs, which include eight guanidine groups dendrimerically arranged in the guanidine-rich head and two synthetic antisense morpholino oligonucleotides, are representative compounds of the present invention.

The present invention relates to a novel process for the manufacture of blood-platelet aggregation inhibiting agent. In particular, the present invention is directed to a process for the manufacture of Methyl-(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-S-(4H)acetate bisulfate Form-I.

The present invention provides a conjugate wherein GP (glycoprotein) Ib and a lipid are bonded via polyalkylene oxide. The present invention also provides a complex (GPIb lipid complex) containing this conjugate and a free lipid. The GPIb lipid complex is expected to have a potential for practical application in a wide range, as a platelet substitute, a pharmaceutical agent for the prophylaxis or treatment of angiopathy, vascular damage and thrombosis, a diagnostic for vWF deficiency and the like, a biological or medical reagent, a reagent for screening platelet aggregation suppressant or antithrombosis, and the like. The GPIb lipid complex of the present invention is also useful as a diagnostic for finding the location of vascular lesion or thrombus formation, or a therapeutic agent thereof. Moreover, the GPIb lipid complex of the present invention is also superior in retention property in blood, which enables continuous expression of a pharmacological action. The conjugate of the present invention is highly utilizable as an active ingredient of the GPIb lipid complex of the present invention.

Disclosed are process steps and processes for producing chromane compounds, preferably 2-(6-amino-chroman-2yl) acetic acid esters which are intermediates for producing platelet aggregation inhibitors and / or are themselves potent platelet aggregation inhibitors.

A novel domain of Aggrus involved in the binding to CLEC-2 was searched for, and monoclonal antibodies recognizing the domain were obtained. The newly found PLAG4 domain is important for Aggrus binding to CLEC-2. Monoclonal antibodies recognizing this region were further developed. The present invention can provide novel Aggrus-CLEC-2 binding inhibitors, platelet aggregation inhibitors, cancer metastasis inhibitors, and tumor growth inhibitors using these antibodies.

The present invention relates to a novel compound having an effect of inhibiting platelet aggregation and a salt thereof and, more specifically, to: a novel platelet aggregation inhibitor specifically inhibiting shear stress-induced platelet aggregation; a pharmaceutical composition containing the same as an active ingredient; and a preparation method therefor.

The invention discloses a 12-quinoline substituted-andrographolide derivative and a preparation method and application thereof. The method comprises the following steps that (1) a compound (I) is taken as a starting material, and a compound (II) is prepared under oxidation of acidic potassium permanganate; (2) a target derivate (IV) is prepared under an alkaline condition by the compound (II) and a 2-methylquinoline compound (III). The preparation method has the advantages that the natural product andrographolide is subjected to structural modification, so that a novel platelet aggregation inhibitor is obtained; the synthetic route is simple and short, the operation is simple and easy to operate, the product structure is novel, and the anti-platelet aggregation effect is equivalent to clopidogrel, which is worthy of further study.

DPA-enriched pharmaceutical compositions of polyunsaturated fatty acids in free acid form, therapeutic methods for their use, and processes for refining the compositions from fish oil are presented. Also provided are methods of treating hypertriglyceridemia (200 mg / dL-500 mg / dL) by adjunctive administration of a statin and the pharmaceutical compositions described herein. Further treatment methods include, inter alia, treatments to increase plasma EPA:AA ratios, treatments to decrease ApoCIII levels, and treatments to reduce or prevent resistance to platelet aggregation inhibitors.