73 results about "Integrelin" patented technology

The invention belongs to the technical field of chemical drugs, and relates to a compound as shown in a general formula (I), or a racemate thereof, or an isomer thereof, or a pharmaceutically acceptable salt thereof, as a small molecule antagonist of alpha4beta7 integrin, and a method for treating various specific diseases or symptoms by using the compound. # imgabs0 #

The invention discloses a composition with sensitive skin repairing and anti-aging functions as well as an emulsion and application of the composition, and belongs to the technical field of cosmetics. The composition specifically comprises a pseudoalteromonas fermentation product extract, collagen, palmitoyl tripeptide-5, acetylchitosamine, sodium hyaluronate, silanetriol, caffeine and acetyl hexapeptide-8, and can promote the generation of laminin-5 and integrin beta1, promote the vitality of keratinocytes and fibroblasts, inhibit the growth of the keratinocytes and the fibroblasts, inhibit the growth of the keratinocytes and the fibroblasts, inhibit the growth of the keratinocytes and the fibroblasts, and promote the growth of the keratinocytes and the fibroblasts. The generation of inflammatory factors (IL-6) is inhibited; the generation of collagen IV and collagen VII is promoted; the invention further provides an emulsion prepared from the composition, and the optimal formula of the emulsion is obtained through optimization. The active composition disclosed by the invention has a wide application prospect in the field of cosmetics, and particularly has important significance in sensitive skin repair and anti-aging directions.

The invention relates to dosage forms for daily administration of compounds of formula (A) and formula (I):or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).

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

This invention discloses the application of integrin αv inhibitors combined with γ-secretase inhibitors in the preparation of drugs for treating tumors. The study found that the combined use of integrin αv inhibitors and γ-secretase inhibitors in tumor treatment exhibits a synergistic effect, not only inhibiting in situ tumor growth but also significantly suppressing tumor invasion, distant metastasis, and other malignant progression, thus helping to slow tumor progression, improve treatment efficacy, and enhance patient prognosis. Furthermore, the study found that the combined use of integrin αv inhibitors and γ-secretase inhibitors can reduce the production of the intracellular free domain of integrin αv and inhibit the activation of the classical downstream pathway of integrin αv. The combined use of integrin αv inhibitors and γ-secretase inhibitors shows broad application prospects in tumor treatment.

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.

In some embodiments, the invention provides a method for identifying an agent beneficial to treat a patient with inflammatory bowel disease comprising: a) determining a status of an intestinal barrier in the patient; and b) categorizing the status as severe dysfunction or moderate dysfunction, wherein a patient categorized as having severe dysfunction is identified as a patient who will benefit from treatment with an agent selected from the group consisting of an anti-TNF agent and / or an anti-IL-12 / 23 agent, and a patient categorized as having moderate dysfunction is identified as a patient who will benefit from treatment with an anti-integrin agent, an anti-janus kinase agent, and / or and a sphingosine-1-phosphate receptor agonist agent.

The invention relates to the technical field of medicines, and provides application of pulsatilla saponin B4 in preparation of a medicine for treating osteoarthritis. The pulsatilla saponin B4 can obviously promote the expression of SOX9, which is an important cartilage specific transcription factor, and inhibit the expression of matrix metalloproteinase 13 and disintegrin and metalloproteinase 5 with platelet reaction protein motifs at the same time, thereby finally relieving the degradation of extracellular cartilage matrixes such as II-type collagen and aggregation proteoglycan. Therefore, the pulsatilla saponin B4 can inhibit cartilage degeneration and improve cartilage extracellular matrix metabolic disorder. After the pulsatilla saponin B4 is injected into the abdominal cavity of a mouse with osteoarthritis, the progress of the osteoarthritis is effectively relieved, the side effect is relatively small, and no obvious injury is caused to main organs. The pulsatilla saponin B4 is applied to treatment of osteoarthritis, new application of the pulsatilla saponin B4 is developed, and a new choice is provided for preparation of the medicine for treating osteoarthritis.

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.

The invention relates to compounds of formula (I): formula (I) or a salt thereof wherein R1, R5, R7, R8, X, m, n, p and q are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating tissue specific fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).

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.

To provide a method of treating cardiac fibrosis in a patient.SOLUTION: The present invention relates to a method of treating cardiac fibrosis in a patient, comprising administering to the patient a therapeutically effective amount of an αV-integrin inhibitor. Pharmacological blockade of αV-containing integrins improved cardiac function and survival after MI by reducing infarct size and attenuating expansion of reactive cardiac fibrosis. Notably, after pharmacological blockade of αV-containing integrins, a total myocardial fibrogenesis area as well as interstitial fibrosis in the remote myocardial area are significantly reduced. These data identify a novel mechanism regulating cardiac fibrosis in response to an ischemic injury and suggest that pharmacological targeting of αV-integrins may provide clinical benefit in the treatment of cardiac fibrosis.SELECTED DRAWING: None

The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Described herein are methods of improving atrial function and reducing atrial arrhythmias in a subject in need thereof. In one embodiment, the method comprises administering to the subject a therapeutically effective amount of a cardiac bridging integrator 1 (cBIN1) gene therapy. In some aspects, the subject exhibits one or more improved atrial properties following administration of the cBIN1 gene therapy relative to before administration of the cBIN1 gene therapy. These improved atrial properties may comprise shortened P-wave duration, reduced atrial fibrosis, reduced left atrial dyssynchrony, increased intracellular T-tubule area, reduced atrial arrhythmia, or combinations thereof.

Methods of treating idiopathic nephrotic syndrome in a subject involve reducing urinary and / or blood levels of CD93, reducing or inhibiting CD93-mediated podocyte activation. or reducing or inhibiting CD93 release from glomerular endothelial cells. The methods may include administration of a composition including at least one of an anti-CD93 antibody and an inhibitor of pi integrin.

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.

Provided herein are crystalline forms of integrin inhibitors, compositions thereof, and methods of their uses. Crystalline forms of tartrate cocrystals 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.

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 present invention relates to using c-Src SH3 RT-loop as a target for anti-thrombosis. Specifically, the present invention provides the use of a c-Src SH3 RT-loop antagonist for preparing a composition or preparation, and the composition or preparation is used for: (a) interfering with the interaction between integrin β3 and c-Src; (b) inhibiting platelet spreading on solid-phase fibrinogen; (c) inhibiting platelet aggregation and / or adhesion; and / or (d) preventing and / or treating thrombosis. The present invention discovers for the first time that a drug combination or preparation targeting the RT-loop region of the c-Src SH3 domain can effectively treat thrombotic diseases without increasing the risk of bleeding.

The invention belongs to the technical field of medicines, and particularly relates to a quinoline compound with an integrin alpha5beta1 inhibition function and application of the quinoline compound in fibrosis and fibrosis-related diseases. Specifically, the invention provides a compound, and the compound has a structural general formula as shown in the specification or a pharmaceutically acceptable salt, solvate or hydrate thereof: # imgabs0 #. The compound has obvious inhibitory activity on integrin alpha5beta1, so that the compound can be used for obstacles, diseases or symptoms mediated by the integrin alpha5beta1, and tests prove that the compound has an obvious treatment effect on various fibrosis diseases, so that the compound has a good practical application value.

The present invention relates to the use of ADAMTS12 protein, a disintegrin and metalloproteinase 12 protein having a platelet-reactive protein motif, in the development of chronic kidney diseases, in particular progressive chronic kidney diseases and renal fibrosis. In particular, the present invention relates to a method for identifying compounds that bind to ADAMTS12 protein and the use of ADAMTS12 protein for screening and identifying ADAMTS12 interacting compounds and ADAMTS12 inhibiting compounds. The present invention also relates to pharmaceutical compositions for the treatment of kidney diseases, in particular pharmaceutical compositions comprising active agents that bind to and / or inhibit ADAMTS12 protein (Fig. 5).

The disclosure relates to fixed dose combinations of the integrin inhibitor bexotegrast ((S)-4-((2-methoxyethyl)(4-(5,6,7,8-tetrahydro-l,8-naphthyridin-2-yl)butyl)amino)-2- (quinazolin-4-ylamino)butanoic acid) with peroxisome proliferator-activated receptor agonists (PPAR agonists), and methods of treating a subject for a liver fibrotic disease, such as primary sclerosing cholangitis or primary biliary cholangitis, by administration of the fixed dose combinations.

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

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.

The invention discloses a pharmaceutical composition and application of the pharmaceutical composition in preparation of medicines for treating bladder cancer or colorectal cancer. The pharmaceutical composition comprises at least one of an integrin alpha5beta1 inhibitor, an immune checkpoint inhibitor combination and a biocompatible hydrogel. The pharmaceutical composition can form a hydrogel microenvironment at the local part of a tumor in a local administration mode, continuously release effective components, cooperatively inhibit angiogenesis, improve an immunosuppressive microenvironment and reduce dry-like tumor cells, so that the immunotherapy effect is remarkably enhanced, and the toxic and side effects of the whole body are reduced. Single cell transcriptomics verification and animal experiments prove the feasibility of the pharmaceutical composition in inhibiting angiogenesis and tumor dryness and improving ICI curative effect.

Blocking antibodies against αMβ2 (CBP-α-αMβ2), αM (CBP-α-αM), α3 (CBP-α-α3), and anti-TGFβ as well as inhibitors of Talin2 reverse fibrosis in a mouse fibrosis model. Accordingly, aspects of the disclosure relate to inhibitors of Talin2 and inhibitors of the integrins αMβ2, αM, and α3. Aspects relate to a method for treating and / or reversing fibrosis in a subject comprising administering a composition comprising an inhibitor of Talin2 or a composition comprising a nucleic acid of the disclosure. Further aspects relate to a method for treating and / or reversing fibrosis in a subject comprising administering a composition comprising an antibody conjugate of the disclosure or a composition comprising an inhibitor or blocking agent of integrin α3, αM, αMβ2, or combinations thereof to the subject. Methods also include treating kidney fibrosis in a subject comprising administering a composition comprising an anti-TGFβ antibody operatively linked to an ECM-affinity peptide. The methods may be for reducing or decreasing the amount of existing fibrosis. The methods differ from traditional methods for treating fibrosis, since the current methods do not delay or inhibit the progression of fibrosis, but instead have shown to reverse, reduce, and / or decrease existing fibrosis. Accordingly, methods of the disclosure may be used in a manner that provides treatment to existing fibrosis rather than a prophylactic to prevent more fibrosis.

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