32 results about "Arg-Gly-Asp-Val" patented technology

The invention discloses RGD peptide-modified carbolino-hexahydropyrazine-1,4-diketones, which are three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD tetrapeptide and are shown in the general formula I. In the general formula I, R represents Arg-Gly-Asp-Val, Arg-Gly-Asp-Phe or Arg-Gly-Asp-Ser. The invention also discloses heterocyclic nucleuses of the novel conjugates, wherein R represents OH. The invention also discloses a preparation method and in-vitro anti-platelet aggregation effects of the novel conjugates, and also discloses an antithrombotic use of the novel conjugates in a rat thrombus formation model. A result shows that the three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD tetrapeptide (wherein R represents Arg-Gly-Asp-Val, Arg-Gly-Asp-Phe or Arg-Gly-Asp-Ser) and their heterocyclic nucleuses (wherein R represents OH) have good antithrombotic activity and clear application prospects in antithrombotic agent preparation.

The present invention discloses six pseudo-peptides of the general formula I, wherein R1 is H or CH3, and R2 is Lys or Lys (Pro-Ala-Lys)-Arg-Gly-Asp-Val or Lys (Pro-Ala-Lys)-Ala-Gly-Asp-Val. The present invention further discloses a preparation method and use thereof. The compounds of the present invention have excellent thrombolytic activity, antithrombotic activity, anti-inflammatory activity, and OH radical scavenging activity, and a nanostructure.

The present invention discloses three materials such as warfarin-4-O-acetyl-Arg-Gly-Asp-Val, warfarin-4-O-acetyl-Arg-Gly-Asp-Ser and warfarin-4-O-acetyl-Arg-Gly-Asp-Phe, preparation methods, anti-arterial thrombus activities, anti-venous thrombosis activities, in vivo vitamin K content lowering activities, in vivo blood coagulation factor II content lowering activities, platelet aggregation inhibition activities thereof, and in vivo platelet membrane glycoprotein IIb / IIIa (GPIIb / IIIa) content lowering activities thereof, and discloses the advantages of no warfarin-like bleeding risk in warfarin-4-O-acetyl-Arg-Gly-Asp-Val, warfarin-4-O-acetyl-Arg-Gly-Asp-Ser and warfarin-4-O-acetyl-Arg-Gly-Asp-Phe, such that the invention discloses applications of warfarin-4-O-acetyl-Arg-Gly-Asp-Val, warfarin-4-O-acetyl-Arg-Gly-Asp-Ser and warfarin-4-O-acetyl-Arg-Gly-Asp-Phe in preparation of anti-arterial thrombus drugs, anti-venous thrombosis drugs, platelet aggregation inhibition drugs, GPIIb / IIIa antagonists, vitamin K antagonists, and blood coagulation factor II antagonists.

The invention discloses KRGD peptide-modified carbolino-hexahydropyrazine-1,4-diketones, which are three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD peptide and are shown in the general formula I. In the general formula I, R represents Lys-Arg-Gly-Asp-Val, Lys-Arg-Gly-Asp-Phe or Lys-Arg-Gly-Asp-Ser. The invention also discloses heterocyclic nucleuses of the novel conjugates, wherein R represents OH. The invention also discloses a preparation method and in-vitro anti-platelet aggregation effects of the novel conjugates, and also discloses an antithrombotic use of the novel conjugates in a rat thrombus formation model. A result shows that the three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD peptide (wherein R represents Lys-Arg-Gly-Asp-Val, Lys-Arg-Gly-Asp-Phe or Lys-Arg-Gly-Asp-Ser) and their heterocyclic nucleuses (wherein R represents OH) have good antithrombotic activity and clear application prospects in antithrombotic agent preparation.

The invention discloses N-(3S-6,7-dihydroxy-1,1-dimethyl-1,2,3,4-tetrahydroisoquinoline-3-formyl)-Lys (Gly-Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val and a preparation method, antithrombus activity and thrombolytic activity thereof and also discloses the effect of the compound on treatment of rats suffering from cerebral ischemia. The invention discloses application of the compound in preparation of antithrombus medicines, thrombolytic medicines and medicines for treating ischemic stroke.

The invention discloses TRGD peptide-modified carbolino-hexahydropyrazine-1,4-diketones, which are three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and TRGD peptide and are shown in the general formula I. In the general formula I, R represents Thr-Arg-Gly-Asp-Val, Thr-Arg-Gly-Asp-Phe or Thr-Arg-Gly-Asp-Ser. The invention also discloses heterocyclic nucleuses of the novel conjugates, wherein R represents OH. The invention also discloses a preparation method and in-vitro anti-platelet aggregation effects of the novel conjugates, and also discloses an antithrombotic use of the novel conjugates in a rat thrombus formation model. A result shows that the three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and TRGD peptide (wherein R represents Thr-Arg-Gly-Asp-Val, Thr-Arg-Gly-Asp-Phe or Thr-Arg-Gly-Asp-Ser) and their heterocyclic nucleuses (wherein R represents OH) have good antithrombotic activity and clear application prospects in antithrombotic agent preparation.

The invention relates to an aspirin-Arg-Gly-Asp-Val conjugate, synthesis, a nano structure, and an application thereof as a drug carrying system. The invention discloses a novel aspirin-Arg-Gly-Asp-Val (A-RGDV) conjugate, and also discloses a preparation method and an application thereof as an antithrombotic agent. The A-RGDV is characterized in that in the blood the A-RGDV can be selectively transferred as nano particles, when the A-RGDV nano particles arrive at the thrombus forming parts, the A-RGDV reacts with the GPIIb / IIIa receptors on the platelet surfaces, and thus aspirin is released during the process. So the A-RGDV can be used as a target drug delivery system for aspirin. A-RGDV has a strong antithrombotic activity, and has a good clinical application prospect. The structural formula of A-RGDV is represented in the description.

The invention discloses 1R-methyl-1,2,3,4-tetrahydro-beta-carboline-3S-acyl-Lys(Gln-Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val, a preparation method, antithrombotic activity and thrombolytic activity thereof, and application of the compound in treating rats with a 24-hour stroke. Thus the invention discloses application of the compound in preparation of antithrombotic drugs, thrombolytic drugs and drugs fortreatment of ischemic strokes. The compound has a formula shown in the description.

The invention discloses The-Arg-Gly-Asp-Val-Gly-Arg-Pro-Ala-Lys decapeptide, discloses a preparation method of the The-Arg-Gly-Asp-Val-Gly-Arg-Pro-Ala-Lys decapeptide,and discloses an activity, an antithrombotic activity and a thrombus dissolving activity of the The-Arg-Gly-Asp-Val-Gly-Arg-Pro-Ala-Lys decapeptide in treating ischemic stroke. Therefore, the invention discloses application of the The-Arg-Gly-Asp-Val-Gly-Arg-Pro-Ala-Lys decapeptide to the preparation of antithrombotic and thrombolytic medicines for treating ischemic stroke.

The present invention discloses 1R-methyl-1,2,3,4-tetrahydro-beta-carboline-3S-acyl-Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val of a formula shown in the description, discloses a preparation method of the compound, discloses the antithrombotic activity of the compound, discloses the thrombolytic activity of the compound and discloses the effect of the compound in treating a rat with a stroke of 24 hours, andthus the present invention discloses application of the compound in preparation of an antithrombotic drug, a thrombolytic drug and drugs for treating ischemic stroke drugs.

The invention discloses 1R-methyl-1,2,3,4-tetrahydro-beta-carboline-3S-acyl-Lys(Ala-Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val, a preparation method, antithrombotic activity and thrombolytic activity thereof, and application of the compound in treating rats with a 24-hour stroke. Thus the invention discloses application of the compound in preparation of antithrombotic drugs, thrombolytic drugs and drugs fortreatment of ischemic strokes. The compound has a formula shown in the description.

The invention discloses The-Lys(Lys-Ala-Pro-Arg-Gly)-Arg-Gly-Asp-Val hendeca-peptide, and discloses a preparation method of the The-Lys(Lys-Ala-Pro-Arg-Gly)-Arg-Gly-Asp-Val hendeca-peptide, activity of treating ischemic stroke, antithrombus activity and thrombolytic activity. Therefore, the invention discloses application of the The-Lys(Lys-Ala-Pro-Arg-Gly)-Arg-Gly-Asp-Val hendeca-peptide in preparation of ischemic stroke treatment, antithrombus and thrombolytic medicines.

The invention discloses a pentamethoxytryptophanylcarbonylpropionyl-RPAK peptide, and a preparation method, activities and applications thereof, and concretely relates to a pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val with the formula shown in the description, a preparation method thereof, an antithrombotic activity and a thrombus dissolving activity of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val, and an application of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val in the treatment of stroke rats. The invention also discloses an application of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val in the preparation of antithrombotic medicines, thrombus dissolving medicines and ischemic stroke treatment medicines.

The invention discloses RGD peptide-modified carbolino-hexahydropyrazine-1,4-diketones, which are three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD tetrapeptide and are shown in the general formula I. In the general formula I, R represents Arg-Gly-Asp-Val, Arg-Gly-Asp-Phe or Arg-Gly-Asp-Ser. The invention also discloses heterocyclic nucleuses of the novel conjugates, wherein R represents OH. The invention also discloses a preparation method and in-vitro anti-platelet aggregation effects of the novel conjugates, and also discloses an antithrombotic use of the novel conjugates in a rat thrombus formation model. A result shows that the three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD tetrapeptide (wherein R represents Arg-Gly-Asp-Val, Arg-Gly-Asp-Phe or Arg-Gly-Asp-Ser) and their heterocyclic nucleuses (wherein R represents OH) have good antithrombotic activity and clear application prospects in antithrombotic agent preparation.

The invention discloses the following formula: 4, 5, 6, 7-tetralin-3H-imidazo [4, 5-c] pyridine-6-formyl-Lys-Arg-Gly-Asp-Val. The invention discloses a preparation method of the formula, the antithrombus activity of the formula, and application of the formula to antithrombus drugs.

The invention discloses 4'-oxyacetyl-Ala-Pro-Ala-Lys-7-oxyacetyl-Arg-Gly-Asp-Val-isoflavone, a preparation method thereof, antithrombotic activity thereof, thrombolytic activity thereof, cerebral-thrombus-treating activity thereof, and free-radical-removing activity thereof. The invention discloses an application of 4'-oxyacetyl-Ala-Pro-Ala-Lys-7-oxyacetyl-Arg-Gly-Asp-Val-isoflavone to prepare antithrombotic medicines, thrombolytic medicines, cerebral-thrombus-treating medicines, and free-radical-removing medicines.

The invention discloses 1S-methyl-1,2,3,4-tetrahydro-beta-carboline-3S-formyl-Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val as shown in the formula, its preparation method, its antithrombotic activity, its thrombolytic activity, and its effect of treating rats with stroke for 24 hours. Therefore, the invention discloses preparation of the 1S-methyl-1,2,3,4-tetrahydro-beta-carboline-3S-formyl-Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val in preparation of antithrombotic drugs, thrombolytic drugs and drugs for treating ischemic stroke.

The invention discloses a pentamethoxytryptophanylcarbonylpropionyl-RPAK peptide, and a preparation method, activities and applications thereof, and concretely relates to a pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val with the formula shown in the description, a preparation method thereof, an antithrombotic activity and a thrombus dissolving activity of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val, and an application of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val in the treatment of stroke rats. The invention also discloses an application of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val in the preparation of antithrombotic medicines, thrombus dissolving medicines and ischemic stroke treatment medicines.

The invention relates to cyclic peptides for inhibiting the proliferation of alpha v beta 3 positive cells in a target direction and the preparation and application thereof. The cyclic peptide has an amino acid sequence as follows: Cys Arg Gly Asp Val Cit Arg Leu Arg Trp Arg Lys Cys, wherein, Cys at the end of N and Cys at the end of C form a ring through a disulfide bond.

The invention discloses Gly-Arg-Pro-Ala-Lys-Arg-Gly-Asp-Val-The decapeptide, and a preparation method and ischemic stroke treatment activity, antithrombotic activity and thrombolytic activity thereof.Thus, the invention discloses an application of the Gly-Arg-Pro-Ala-Lys-Arg-Gly-Asp-Val-The decapeptide in preparation of ischemic stroke treatment, antithrombotic and hemolytic thrombolytic drugs.

The invention discloses a pentamethoxytryptophanylcarbonylpropionyl-Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val with the formula shown in the description, a preparation method thereof, an antithrombotic activity and a thrombus dissolving activity of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val, and an application of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val in the treatment of stroke rats. The invention also discloses an application of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val in the preparation of antithrombotic medicines, thrombus dissolving medicines and ischemic stroke treatment medicines.

The invention discloses 1S-methyl-1,2,3,4-tetrahydro-beta-carboline-3S-formyl-Lys(Ala-Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val as shown in the formula, its preparation method, its antithrombotic activity, itsthrombolytic activity, and its effect of treating rats with stroke for 24 hours. Therefore, the invention discloses application of the 1S-methyl-1,2,3,4-tetrahydro-beta-carboline-3S-formyl-Lys(Ala-Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val in preparation of antithrombotic drugs, thrombolytic drugs and ischemic stroke treatment drugs.

Aspirin‑Arg‑Gly‑Asp‑Val conjugate, its synthesis, nanostructure and application as a drug delivery system. The invention discloses a novel aspirin-Arg-Gly-Asp-Val (A-RGDV) conjugate, its preparation method and its application as an antithrombotic agent. A-RGDV is characterized in that it can be selectively transported in the blood as nanoparticles, and after reaching the site of thrombus formation, it interacts with the GPIIb / IIIa receptors on the surface of activated platelets to release aspirin. Therefore, A‑RGDV is a targeted drug delivery system for aspirin. A‑RGDV has strong antithrombotic activity and has good clinical application prospects. The following is the structural formula of A‑RGDV. .

The invention discloses an Arg-Gly-Asp-Val-The-Gly-Arg-Pro-Ala-Lys decapeptide and its preparation method and activity of ischemic stroke treatment, thrombus formation resistance and thrombus dissolution. The invention discloses a use of the Arg-Gly-Asp-Val-The-Gly-Arg-Pro-Ala-Lys decapeptide in preparation of drugs for treating ischemic stroke, resisting thrombus formation and dissolving thrombus.

The invention discloses a The-Gly-Arg-Pro-Ala-Lys-Arg-Gly-Asp-Val decapeptide, a preparation method thereof, and an ischemic apoplexy treatment activity, an antithrombotic activity and a thrombus dissolving activity of the decapeptide. The invention also discloses an application of the decapeptide in the preparation of ischemic apoplexy treatment, antithrombosis and thrombus dissolving medicines.

The invention discloses a conjugate of a peptide chain and two fatty alcohol chains, a preparation method thereof and medicinal application thereof. The conjugate is formed by conjugating one Arg-Gly-Asp-Val chain and two fatty alcohol chains by Asp and has a general formula of Arg-Gly-Asp-Val-Asp[OCH2(CH2)nCH3]2, wherein n may be 6, 8, 10 or 12. The conjugate of the invention has high oral antithrombotic activities, high self-assembling property and can be used as preparation materials for preparing medicament carries such as micro emulsion and liposome.

The invention discloses 4'-oxyacetyl-Ala-5-hydroxyl-7-oxyacetyl-Arg-Gly-Asp-Val-isoflavone, a preparation method thereof, antithrombotic activity thereof, thrombolytic activity thereof, cerebral-thrombus-treating activity thereof, and free-radical-removing activity thereof. The invention discloses an application of 4'-oxyacetyl-Ala-5-hydroxyl-7-oxyacetyl-Arg-Gly-Asp-Val-isoflavone to prepare antithrombotic medicines, thrombolytic medicines, cerebral-thrombus-treating medicines, and free-radical-removing medicines.

The invention discloses KRGD peptide-modified carbolino-hexahydropyrazine-1,4-diketones, which are three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD peptide and are shown in the general formula I. In the general formula I, R represents Lys-Arg-Gly-Asp-Val, Lys-Arg-Gly-Asp-Phe or Lys-Arg-Gly-Asp-Ser. The invention also discloses heterocyclic nucleuses of the novel conjugates, wherein R represents OH. The invention also discloses a preparation method and in-vitro anti-platelet aggregation effects of the novel conjugates, and also discloses an antithrombotic use of the novel conjugates in a rat thrombus formation model. A result shows that the three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD peptide (wherein R represents Lys-Arg-Gly-Asp-Val, Lys-Arg-Gly-Asp-Phe or Lys-Arg-Gly-Asp-Ser) and their heterocyclic nucleuses (wherein R represents OH) have good antithrombotic activity and clear application prospects in antithrombotic agent preparation.

The invention discloses an Arg-Gly-Asp-Val-The-Gly-Arg-Pro-Ala-Lys decapeptide and its preparation method and activity of ischemic stroke treatment, thrombus formation resistance and thrombus dissolution. The invention discloses a use of the Arg-Gly-Asp-Val-The-Gly-Arg-Pro-Ala-Lys decapeptide in preparation of drugs for treating ischemic stroke, resisting thrombus formation and dissolving thrombus.