34 results about "Integrelin" patented technology

Novel compounds that act as inhibitors of alpha4beta7 integrin are disclosed. Pharmaceutical compositions and methods of use of inhibitors of [alpha] 4 [beta] 7 integrin are disclosed. In particular, methods of using the [alpha] 4 [beta] 7 inhibitors in the treatment of diseases or conditions associated with inflammatory bowel diseases, including ulcerative colitis and Crohn's disease.

The application provides a combined drug, a liposome, a biomimetic liposome, a preparation method of the combined drug, the liposome and the biomimetic liposome, and application of the combined drug, the liposome and the biomimetic liposome in preparation of an anti-breast cancer lung metastasis drug, and belongs to the technical field of biological medicines. The combined drug comprises panatinib and ginsenoside Rg3. The application further provides a liposome PNT-Rg3-Lipo for simultaneously loading the two, and a biomimetic liposome MM / PNT-Rg3-Lipo coated with a macrophage membrane. Experiments show that the combination of the two can synergistically regulate chemokines CXCL1 , CXCL2 and CXCL11 , and the effect is better than the sum of the single use. The MM / PNT-Rg3-Lipo has uniform particle size, retains integrin alpha 4 / beta 1 functional proteins, can target lung metastases, significantly reduces metastatic nodules, and has good biocompatibility. The application provides an effective new strategy for resisting breast cancer lung metastasis.

Provided herein are variant α4β7 integrin antibodies and methods of use.

Provided are alpha V beta6 and alpha V beta 1 integrin inhibitors, methods of making such alpha V beta6 and alpha V beta 1 integrin inhibitors, pharmaceutical compositions of alpha V beta6 and alpha V beta 1 integrin inhibitors and methods of treating and / or preventing various medical disorders in subjects in need of treatment by administration of alpha V beta6 and alpha V beta 1 integrin inhibitors.

Provided herein are variant α4β7 integrin antibodies and methods of use.

The invention relates to the technical field of medicines, in particular to application of an integrin beta3 inhibitor RGDfK in preparation of a medicine for treating metabolic dysfunction related fatty liver diseases. The RGDfK provided by the invention can inhibit palmitoylation and membrane localization of CD36 in liver tissues of mice with fatty liver diseases related to metabolic dysfunction induced by high fat diet feeding, so that lipid uptake of the liver is inhibited. Experimental results show that RGDfK can improve obesity and insulin resistance of mice with metabolic dysfunction-related fatty liver diseases, can improve fat accumulation, fibrosis and inflammatory infiltration of liver tissues of the mice with fatty liver diseases, and is expected to become a new medicine for treating the metabolic dysfunction-related fatty liver diseases.

Methods for inhibiting or preventing activation of a macrophage, by a receptor antagonist of α9β1 integrin are provided. Further provided are methods for treating or preventing an inflammatory disease or a metabolic disorder, including a metabolic syndrome, in a subject in need thereof, and a pharmaceutical composition comprising a peptide comprising the amino acid sequence: EDDMMEVPY, for use in treatment or prevention of an inflammatory disease or a disorder, in a subject in need thereof.

Provided herein are integrin inhibitors, compositions thereof, and methods of their uses. Crystalline forms of salts of the inhibitors are also described, along with methods of preparing the crystalline forms. X-ray powder diffraction data, thermogravimetric analysis, and differential scanning calorimetry data are provided for the crystalline forms. The integrin inhibitors are useful for treatment of, inter alia, fibrotic diseases.

The invention belongs to the technical field of biological medicine, and particularly relates to an engineered cell exosome for specifically targeting liver, construction and application. The exosome is derived from mesenchymal stromal cells of an overexpressed integrin subunit beta 5, and the mesenchymal stromal cells of the overexpressed integrin subunit beta 5 are prepared by lentivirus infection. The liver targeting engineered umbilical cord mesenchymal stromal cell exosome can be remarkably enriched in liver tissue after intravenous infusion, the in-vivo anti-fibrosis curative effect is improved, the cell source of the engineered exosome is easy to obtain, the problem of exosome yield is solved, and good application prospects are shown.

Provided herein are variant α4β7 integrin antibodies and methods of use.

To provide a method for treating disease.SOLUTION: The present disclosure provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease. The present disclosure relates generally to novel compounds that have α4β7 integrin inhibitory action, prodrugs of compounds having α4β7 integrin inhibitory action, and methods of use and manufacture thereof.SELECTED DRAWING: None

Anti-alpha4beta7 integrin antibody liquid formulations are described that have a high concentration of antibody, e.g., 90 mg / ml or more, have a viscosity suitable for injection for subcutaneous delivery, including by self-administration by the patient. In certain embodiments, formulations can be used in combination with an autoinjector having a suitable force of delivery given the viscosity of the formulation.

The present invention relates to compounds that are α4β7 integrin inhibitors. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with α4β7.

Linker-payload compounds comprise a JAK inhibitor and a cleavable linker, and antibody-drug conjugates (ADCs) comprise the same. ADCs targeting antigens associated with autoimmune or inflammatory diseases include but are not limited to integrin α4β7, MAdCAM-1, IL-17, IL-23, or TNF-α. The conjugates provided herein may comprise a variety of payloads, such as JAK inhibitors. Pharmaceutical compositions comprising the compounds or ADCs, and methods of producing them are also provided herein. Medical uses of these compounds and ADCs, including for the treatment of autoimmune diseases, inflammatory diseases, and fibrotic diseases, are also disclosed.

This invention relates to the field of biomimetic nanozymes and their preparation technology, disclosing a biomimetic nanozyme, its preparation method, and its applications. A peptide-functionalized biomimetic nanozyme (HRPL) is obtained by loading rapamycin onto HMPB nanozymes, coating the surface with a platelet membrane, and functionalizing it with the integrin-binding peptide LXW7. The binding of the platelet membrane to the LXW7 peptide enables targeted delivery to the site of endothelial injury, promoting endothelial repair and re-epithelialization. In an acidic inflammatory microenvironment, HRPL releases rapamycin, inhibiting smooth muscle cell proliferation and migration, and preventing restenosis. HRPL also scavenges reactive oxygen species, reducing oxidative stress and local inflammation, thereby improving the vascular microenvironment. The therapeutic effect was evaluated using a typical rat carotid balloon injury model. This dual-targeting mechanism not only promotes endothelial repair but also reduces restenosis and inflammation, showing significant clinical therapeutic potential. Especially after stent implantation, HRPL helps improve prognosis, reduce complications, and restore vascular homeostasis.

The present invention aims to provide an arthritis treatment agent containing synovial membrane-derived mesenchymal stem cells having molecules essential for joint treatment, and a method for producing the arthritis treatment agent. [Solution] According to the present invention, an arthritis treatment agent is provided which comprises synovial mesenchymal stem cells having one or more surface antigens, either integrin β1 or platelet-derived growth factor receptor β.

The present invention relates to a pharmaceutical composition to be used in the prevention or treatment of diseases involving vascular fibrosis. Specifically, the pharmaceutical composition according to the present invention contains a peptide that reduces fibrosis of perivascular tissue or the extracellular matrix constituting the vascular wall, and is useful for preventing or treating diseases involving vascular fibrosis, particularly pulmonary arterial hypertension.

The invention belongs to the technical field of cosmetics, and particularly relates to cyclic peptide for promoting expression of human skin full-configuration protein and application of the cyclic peptide in cosmetics. The structure of the cyclic peptide is shown as a formula (I) or (II). The cyclopeptide provided by the invention can significantly up-regulate the expression levels of COL1A1, COL3A1, ELN and ITGB1 in human dermal fibroblasts and promote the synthesis of collagen, elastin and integrin, so that the skin elasticity and compactness can be improved, and the cyclopeptide has excellent stability and biological safety. The cyclic peptide disclosed by the invention can be widely applied to cosmetics for resisting aging, improving skin elasticity, tightening and repairing. (I) (II)

The invention relates to the field of molecular biology and biological medicine, and particularly discloses an antithrombotic effect of Meteorin protein or gene. Experiments prove that after Meteorin protein is incubated, the platelet aggregation reaction can be remarkably inhibited, the platelet spreading area can be reduced, blood clot contraction can be delayed, and meanwhile ATP release and alpha particle release of platelets and activation of surface integrin alpha IIb beta 3 can be inhibited. In a whole thrombus experiment, the Meteorin protein can effectively inhibit the formation of arterial thrombosis. The Meteorin protein is a human endogenous protein, so that the Meteorin protein has relatively small side effects, has relatively high safety as a potential drug, and has a good industrialization prospect.

Provided herein are formulations of α4β7 integrin antibodies and methods of use.

Novel compounds that act as inhibitors of alpha4beta7 integrin are disclosed. Pharmaceutical compositions and methods of use of inhibitors of [alpha] 4 [beta] 7 integrin are disclosed. In particular, methods of using the [alpha] 4 [beta] 7 inhibitors in the treatment of diseases or conditions associated with inflammatory bowel diseases, including ulcerative colitis and Crohn's disease.

The present invention provides cross-species anti-latent TGF-beta 1 antibodies. The present inventors have conducted diligent studies and consequently created cross-species anti-latent TGF-beta 1 antibodies which inhibit a protease mediated activation of TGF-beta 1 but do not inhibit integrin mediated activation of latent TGF-beta 1. It has been reported that latent TGF-beta is cleaved to release active TGF-beta by proteases. However, surprisingly, the present inventors have found that the anti-TGF-beta 1 antibodies inhibit a protease mediated activation of latent TGF-beta 1 without inhibiting protease mediated cleavage of the LAP region of latent TGF-beta 1, and have in vivo anti-fibrotic effects as well. Further, antibodies of the invention are useful for the diagnosis or treatment of cancer, and can also be used in combination with immune check point inhibitors.

The invention belongs to the field of biological medicine, and discloses a radioactive diagnosis and treatment drug targeting integrin alpha5beta1, and a labeled precursor, a preparation method and application thereof. Experimental verification shows that the prepared radioactive diagnosis and treatment medicine has good binding specificity with the integrin alpha5beta1, is mainly metabolized through a renal pathway, has low hepatotoxicity, and has important clinical application value in diagnosis and treatment integration of diseases such as tumors with high expression of the integrin alpha5beta1, hepatic fibrosis, central ischemic diseases, atherosclerosis and the like.

The present invention relates to compounds that are α4β7 integrin inhibitors, which have structural formula I, as defined herein. The present invention also relates to processes for the preparation of these compounds, pharmaceutical compositions containing them, and their use in the treatment of α4β7-related diseases or disorders.

The present disclosure provides peptides that inhibit a binding interaction between a β integrin and a G protein subunit, as well as compositions, e.g., pharmaceutical compositions, particularly nanoparticle compositions, comprising the same and to methods of using the peptides to treat atherosclerosis, thrombosis, stroke, heart attack, inflammation, acute respiratory distress syndrome (ARDS), autoimmune diseases, AV Fistula for hemodialysis or organ transplantation.

The present invention relates to compounds that are α4β7 integrin inhibitors. The compounds have the structural formula I defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with α4β7.

Provided herein are antibodies to active integrin beta-2 and compositions comprising such antibodies for the treatment of a cancer, e.g., acute myeloid leukemia.

This invention discloses the application of GLPG0187 in combination with propranolol in the preparation of drugs for the treatment or inhibition of hemangiomas. GLPG0187 is an integrin β1 inhibitor, and propranolol is a β-receptor blocker. This invention was validated through CCK8 assays, scratch assays, and tube formation assays. The results showed that, compared with propranolol monotherapy, GLPG0187 (4 nM) combined with propranolol (20-30 μM) could further inhibit the proliferation, migration, and tube formation ability of human hemangioma endothelial cells, demonstrating superior efficacy compared to propranolol monotherapy. This invention addresses the issue that approximately 2.1% of patients treated with propranolol monotherapy for infantile hemangiomas experience side effects such as sleep disturbances, bronchospasm, and hypoglycemia, providing a new combination therapy regimen and offering a new drug option for reducing the clinical dosage of propranolol and minimizing the risk of side effects. This invention identifies a new target for the treatment of hemangiomas, providing new possibilities for hemangioma treatment.

Biochemical markers that can be measured to determine the level of mechanical activation of a population of platelets are provided, and their use to prepare molecular signatures thereof are provided. The markers include phosphatidylserine, thrombin, integrin GPIIb / IIIa activation, glycoprotein GP Ib, P-selectin; platelet size; microparticle generation, or lipidomic profile of the membrane. The disclosed markers, measurement thereof, and signatures composed therefrom can be used in a variety of methods of patient selection, treatment monitoring, treatment selection, including both devices and active agents, and methods of treating subjects in need thereof, particularly humans. Examples of such methods include, but are not limited to, reducing shear-activated platelets; selecting a blood-contacting medical device; selecting between two or more medical devices; identifying a subject at a risk of developing a thrombogenic event; monitoring the prophylactic treatment of a subject; selecting a mechanoceutical agent; and delivering an agent to a subject.