122results about How to "Good antithrombotic activity" patented technology

The invention discloses a compound with general formula (I) of anti-thrombus activity. The invention also discloses a preparation method of the compound and the application as the anti-thrombus agent. The invention introduces the amino acid residues into the second N of (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid to prepare the compound with general formula (I) of the invention. The compound of the invention not only has the good anti-thrombus activity, but also has the simpler structure and the lower preparation cost by comparing with the anti-thrombus agent prepared by the L-amino acid modification of (3S)-1,2,3,4-tetrahydro-Beta-carboline-3-carboxylic acid. Moreover, whether in the polar solvent or the non-polar solvent, the compound with the general formula (I) of the invention has the good solubility and high bioavailability.

The invention relates to the field of thrombotic disease related drugs and particularly relates to a PAR (Protease Activated Receptor)-1 antagonist with a brand new structure as the specification, a preparation method of the PAR-1 antagonist, a pharmaceutical composition containing the PAR-1 antagonist and an application of the PAR-1 antagonist to preparation of drugs for treating thrombotic diseases.

The invention relates to the field of medicines related to thrombotic diseases, particularly to a para-position substituted PAR-1 (Protease Activated Acceptor-1) agonist containing a tetrazole acetophenone structure, a preparation method, a medicine composition containing the PAR-1 agonist, and application for preparing medicines for treating the thrombotic diseases. The definition of an R group is shown in the description.

The invention relates to the field of medicine related to thrombotic diseases, in particular to a meta-substituted PAR-1 agonist containing tetrazole acetophenone, a preparation method of the agonist, medicine composition containing the agonist, and application of the medicine composition in preparing medicine treating thrombotic diseases. The formula I is shown in the specification. The R group is defined in the specification.

The invention relates to the field of drugs associated with thrombotic diseases, in particular to a category of PAR-1 antagonists of an oxadiazole sulfoxide structure comprising halogeno benzene, a preparation method of the PAR-1 antagonists, and application of drug combinations comprising the halogeno benzene and the halogeno benzene in preparation of the drugs for treating the thrombotic diseases. Please see the formula in the specification, wherein R is selected from halogen substituent groups.

The invention relates to the field of drugs related to thrombotic diseases. Specifically, the invention belongs to a triazole schiff base compound with a novel skeleton and a derivative thereof and particularly relates to a PAR-1 antagonist adopting the structure of the phenyl triazole schiff base, a preparation method for the PAR-1 antagonist, a pharmaceutical composition containing the PAR-1 antagonist and the application of the pharmaceutical composition in preparing drugs for treating thrombotic diseases; in the formula (I) (as shown in the specification), each replaced definition is as described in the specification.

The invention relates to O-unsaturated fatty acid acylated chitosan oligosaccharides, which are characterized in that the O-unsaturated fatty acid acylated chitosan oligosaccharides are a mixed component and have a molecular weight of 800-25000 Da; the deacelation degree of the mixed component is 50-100%; the substitution degree of O-unsaturated fatty acid is 30-200%; and the components of the O-unsaturated fatty acid acylated chitosan oligosaccharides have a structure shown in the specification, wherein R1 is H or CH3CO-, R2 is C12-22 unsaturated fatty acid acyl or H, and n is 0-30. The O-unsaturated fatty acid acylated chitosan oligosaccharides have activities of resisting oxidation, delaying aging, inhibiting tumor, resisting inflammation, lowering blood pressure, preventing thrombosis, improving diabetes mellitus, lowering blood sugar, resisting atherosclerosis and the like, and can be used as important raw materials for medicines, health-care food and cosmetics.

The invention discloses applications of human derived antibacterial peptide LL-37 in the preparation of drugs for treating and / or preventing thrombotic diseases and functional food for preventing thrombus and coagulation and reducing blood density. The human derived antibacterial peptide LL-37 can inhibit the platelet aggregation, prominently prolongs the APTT and PT time, has an activity for preventing thrombosis, can be used to prepare drugs for preventing and / or treating thrombotic diseases, and can also be used to produce functional food for preventing thrombus and coagulation and reducing blood density.

The invention discloses a carboline carboxylic acid-tetrapeptide conjugate and a synthesis method as well as application thereof used as an antithrombotic agent. In the invention, tri-carboxyl of 3S-1,2,3,4-tetrahydro-Beta-carboline-3-carboxylic acid with antithrombotic activity is conjugated with the ammonia end of AA-Tyr-Ser-Val tetrapeptide to obtain a finished product after deprotection, wherein AA is selected from alanine, glycine, proline, glutamine, leucine, phenylalanine, isoleucine, valine, tyrosine, tryptophane, histidine, asparaginate, aspartate, glutamate, serine, threonine, methionine, lysine or arginine residue. The evaluation experiment on a thrombotic model of a rat shows that the compound of the invention has excellent antithrombotic activity and can be applied as the antithrombotic agent. In addition, the invention can overcome the defect of low bioavailability caused by low solubility of the 3S-1,2,3,4-tetrahydro-Beta-carboline-3-carboxylic acid in polar solvents and non-polar solvents.

The invention discloses a butyphthalide derivative as well as a preparation method and application thereof and belongs to the fields of medicinal chemistry and pharmacotherapeutics. The invention further discloses application of the butyphthalide derivative disclosed by the invention in medicines for preventing and treating ischemic cardiovascular and cerebral vascular diseases, anti-platelet aggregation drugs, antithrombotic drugs, anti-cerebral ischemia drugs, anti-dementia drugs and anti-atherosclerosis drugs. Pharmacological experiment results show that, the butyphthalide derivative disclosed by the invention has excellent anti-platelet aggregation and antithrombotic activity, and can be clinically used for preparing medicines for preventing or treating platelet aggregation related diseases.

The invention relates to the field of thrombotic disease related drugs and particularly relates to a PAR (Protease Activated Receptor)-1 antagonist with a brand new structure as the specification, wherein a benzene ring at one side of N-morpholinyl is substituted by ethyoxyl, and a benzene ring at the other side of N-morpholinyl is substituted by dimethoxyl. The invention also relates to an application of the PAR-1 antagonist to preparation of drugs for treating thrombotic diseases.

The invention relates to the field of medicines related to thrombotic diseases, particularly to a di-alkoxy substituted PAR-1 (Protease Activated Acceptor-1) agonist containing a tetrazole acetophenone structure, a preparation method of the di-alkoxy substituted PAR-1 agonist, a medicine composition containing the PAR-1 agonist, and application for preparing medicines for treating the thrombotic diseases. The definition of an R group is shown in the description.

The invention discloses polyasparagine-L-arginine and a preparation method and medical application thereof. In the invention, arginine serves as a pharmacophore, polyaspartic acid serves as a medicine loading system, and the arginine and the polyaspartic acid are bonded to form the polyasparagine-L-arginine with the chain length of 59. An in-vivo / in-vitro antithrombotic model experiment shows that: the polyasparagine-L-arginine compound has accurate antithrombotic activity.

The invention relates to the field of drugs relevant to thrombotic diseases, particularly to a halogen-substituted and four nitrogen azole acetophenone structure contained PAR-1 agonist, and a preparation method thereof, pharmaceutical compositions containing the halogen-substituted and four nitrogen azole acetophenone structure contained PAR -1 agonist and the application of the pharmaceutical compositions in preparing drugs treating thrombotic diseases. The R base is defined as in the specification.

The invention relates to the field of drugs relevant to thrombotic diseases, in particular to a PAR-1 antagonist with an aniline and diene fluoro adamantane structure, a preparation method of the PAR-1 antagonist and the application of the PAR-1 antagonist. The structural general formula of the PAR-1 antagonist is specified in the specification, wherein R1 and R2 are selected from alkyl groups of H and C1-C5 respectively.

The invention relates to the field of medicines related to thrombotic diseases, in particular to a disubstituted PAR-1 (Protease Activated Acceptor-1) agonist containing a tetrazole acetophenone structure, a preparation method thereof, a medicine composition containing the PAR-1 agonist and application of the PAR-1 agonist to preparation of medicines for treating thrombotic diseases. The formula (I) and the definition of R group are shown in the specification.

The invention provides a valve material with synergistic anticoagulation and anti-calcification functions and a preparation method of the valve material. The preparation method comprises the followingsteps: carrying out glutaraldehyde crosslinking treatment on an animal-derived biological valve material; immersing the treated valve material in confining liquid containing an amino compound to perform treatment for 0.5-6 h, and then confining aldehyde groups remaining after glutaraldehyde crosslinking; then putting the valve material into a reaction solution containing an anticoagulant and a cross-linking agent, and carrying out cross-linking treatment for 6-24 hours at 4-37 DEG C; and finally, cleaning the valve material to obtain the valve material, and storing the valve material in a glutaraldehyde or isopropanol / glycerol mixed solvent. The method can effectively solve the problems of easy calcification and thrombus formation caused by aldehyde group residue in the valve material prepared by an existing method, and the valve material prepared by the method disclosed by the invention can be used as a valve material required by aortic valve, pulmonary valve, venous valve, mitral valve and tricuspid valve replacement.

The invention relates to N-unsaturated fatty acid acylated chitosan oligosaccharide and preparation and application thereof, which is a mixing component with the molecular weight of 800-15000Da. Degree of deacetylation of the mixing component is 50%-100%, degree of substitution of the N-unsaturated fatty acid acylated is 30-100%, the structure of the composition is shown in the description, wherein R is the N-unsaturated fatty acid acylated acyl group, hydrogen or CH3CO- with the carbon chain length of 12-22, and n is an integral between 0 and 30. The first glass N-unsaturated fatty acid acylated chitosan oligosaccharide can resist oxidant, delay senility, restrain tumour, resist inflammatory, reduce blood press, avoid thrombopoiesis, improve diabetes mellitus, regulate blood sugar level, resist atherosclerosis, promote plant grow and induce activity such as plant antiviral, and the first glass N-unsaturated fatty acid acylated chitosan oligosaccharide can serve as important raw materials of medicaments, health foods, cosmetics and biopesticide.

The present invention relates to mixtures of polysaccharides derived from heparin having a mean molecular weight of 1500 to 3000 Daltons and an anti-Xa / anti-IIa ratio greater than 30, their method of preparation and pharmaceutical compositions containing them.

The invention relates to the field of thrombotic disease related drugs and particularly relates to a PAR (Protease Activated Receptor)-1 antagonist with a brand new structure as the specification, wherein the benzene ring at one side of N-morpholinyl is substituted by ethyoxyl. The invention also relates to an application of the PAR-1 antagonist to preparation of drugs for treating thrombotic diseases.

The invention relates to the field of thrombotic disease related drugs, belongs to triazole Schiff base compounds with brand new structures and derivatives of the triazole Schiff base compounds and particularly relates to PAR (Protease Activated Receptor)-1 antagonists with terminally-substituted phenyl triazole Schiff base structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. The substituent groups R1 and R2 are defined as the specification.

The invention relates to the field of biomedicine, and discloses a synthetic polypeptide BNC (basal nucleus complex) with antithrombotic activity, a preparation method thereof and an application of the synthetic polypeptide BNC as an antithrombotic agent. The BNC is synthesized by using a Fomc solid-phase chemical process, and contains 3 amino acid residues; the sequence of the BNC is Pyr-Asn-Cys; the molecular weight of the BNC is 346; and the structural formula is shown in the specification. The animal experiment indicates that the polypeptide has inhibiting effects on the formation of thrombus after electrically stimulating the common carotid artery intima of a rat and the formation of ADP-induced (adenosine diphosphate-induced) acute lung thrombus of a mouse, and can prolong the coagulation time of the mouse. The structure formula of the BNC is shown in the specification.

The invention relates to the field of medicines relevant to thrombotic diseases, in particular to a PAR (protease activated acceptor)-1 antagonist with an exocyclic imine structure containing benzo five-membered heterocycle, a preparation method of the PAR-1 antagonist, a medicine composition containing the PAR-1 antagonist and application of the PAR-1 antagonist to medicines for treating the thrombotic diseases. R1, R2 and R3 are independently selected from alkyl groups of C1, C2, C3, C4 and C5, and X is selected from O and C(CH3)2.

The invention relates to the field of thrombotic disease related drugs, belongs to triazole Schiff base compounds with brand new structures and derivatives of the triazole Schiff base compounds and particularly relates to PAR (Protease Activated Receptor)-1 antagonists with terminally-disubstituted triazole Schiff base structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. All the substituent groups are defined as the specification.

The invention relates to the field of thrombotic disease related drugs, belongs to triazole Schiff base compounds with brand new structures and derivatives of the triazole Schiff base compounds and particularly relates to PAR (Protease Activated Receptor)-1 antagonists with terminally-disubstituted methyl triazole Schiff base structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. All substituent groups are defined as the specification.

The invention relates to the field of drugs related to thrombotic diseases, belongs to the triazole schiff base compound of a kind of brand new skeleton, and a derivative thereof, and particularly relates to a kind of PAR-1 antagonist containing a phenyl substituted triazole schiff base structure, the preparation method thereof, drug compounds adopting the same, and the application thereof during the preparation of drugs for treating the thrombotic diseases. The structure of the component is shown in the Specification, and definitions of various substitutes are described in the Specification.

The invention relates to the field of medicines related to thrombotic diseases, in particular to an alkyl disubstituted PAR-1 (Protease Activated Acceptor-1) agonist containing a tetrazole acetophenone structure, a preparation method thereof, a medicine composition containing the PAR-1 agonist and application of the PAR-1 agonist to preparation of medicines for treating thrombotic diseases. The formula (I) and the definition of R group are shown in the specification.

The invention belongs to the technical field of biological medicines, and particularly relates to an isaridin cyclic ester peptide derivative as well as a preparation method and application thereof. Tests prove that the derivative shows good anti-inflammatory and antithrombotic activity, even the activity is higher than that of a positive control drug, in addition, a natural compound derived from marine microorganisms has the characteristics of difficulty in resistance generation, high safety and the like, and tests also prove that the cytotoxicity of the compound disclosed by the invention is low. Meanwhile, the isaridin cyclic depsipeptide derivative disclosed by the invention is extracted from sea squirt-associated epiphytic fungi, can be fermented on a large scale by utilizing microorganisms, has the characteristics of simple production process, short period, low product cost and the like, and has a wide application prospect.

The invention relates to a compound shown in a formula (I), a preparation method thereof, and application in preparing antithrombotic drugs or cardiovascular drugs. The formula is shown in the description.

The invention relates to the field of medicines related to thrombotic diseases, belongs to a triazole Schiff base compound of a brand new framework and derivatives of the triazole Schiff base compound, and particularly relates to a methyl-substituted PAR-1 antagonist of a triazole Schiff base structure, a preparation method of the PAR-1 antagonist, medicine combinations containing the PAR-1 antagonist and applications of the medicine combinations to preparation of medicines for treating thrombotic diseases. A general formula is shown in the specification, wherein definitions of substitutes are shown in the specification.