27 results about "Complement inhibitor" patented technology

To provide further complement inhibitors with therapeutic potential in the treatment of many disorders.SOLUTION: Disclosed are compounds of formula (I)-(IV), and pharmaceutically acceptable salts thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.SELECTED DRAWING: None

The present disclosure provides methods of treating inflammatory indications with complement inhibitor compounds and compositions. Included are compounds and methods of treating neuromuscular inflammatory indications, such as Immune-Mediated Necrotizing Myopathy.

The invention relates to saxifraga stolonifera polysaccharide and application thereof in preparation of complement inhibitors or anti-inflammatory drugs. Based on activity guidance, it is found that a water extraction part of saxifraga stolonifera has good anti-complement activity when experimental screening is conducted on the anti-complement active part of saxifraga stolonifera, graded alcohol precipitation is conducted on the water extraction part, the activity of crude polysaccharide precipitated by 90 alcohol (90% ethyl alcohol) is higher than that of crude polysaccharide precipitated by 75 alcohol (75% ethyl alcohol), and the anti-complement activity of the crude polysaccharide precipitated by 90 alcohol is higher than that of a positive drug (heparin). On the basis, five neutral heteropolysaccharides with anticomplement activity, namely SSP-90-1, SSP-90-2, SSP-90-3, SSP-90-4 or SSP-90-5, are separated from the 90 alcohol precipitation crude polysaccharide. Compared with the prior art, the structural characteristics of the saxifraga stolonifera polysaccharide are represented, and the preparation method of the saxifraga stolonifera polysaccharide and the application of the saxifraga stolonifera polysaccharide in preparation of complement inhibitors and anti-inflammatory drugs are provided. The invention verifies the anti-complement activity of the saxifraga stolonifera polysaccharide and the therapeutic effect of the saxifraga stolonifera polysaccharide on lipopolysaccharide (LPS)-induced acute lung injury and systemic inflammatory response.

The present invention relates to the use of an s100a8 / a9 and complement 3 inhibitor in the preparation of a drug for treating or preventing cachexia. The treatment or prevention of cachexia comprises increasing the body weight, lean body mass and fat mass, and increasing food intake in a cachectic subject, or preventing fat mass consumption, slowing the rate of body weight loss, the rate of fat mass loss and the rate of lean body mass loss, counteracting anorexia, muscle strength loss, fatigue and body weight loss, or improving abnormal biochemical results. Provided is a new understanding for the mechanism of energy balance regulation in cancer cachexia, with an emphasis on the effects of S100a8 / a9 and C3 in cancer cachexia. The inhibition of S100a8 / a9 and complement 3 can promote fat recovery and increase food intake. Particularly, it is verified that an S100a8 / a9 inhibitor can prevent body weight loss, especially adipose tissue loss, in a cachectic subject, and significantly increases food intake in the subject.

This invention relates to the use of S100a8 / a9 and complement 3 inhibitors in the preparation of medicaments for the treatment or prevention of cachexia, wherein the treatment or prevention of cachexia involves increasing the body weight, lean body mass, fat mass, and food intake of cachectic subjects, or preventing fat loss, slowing the rate of weight loss, slowing the rate of fat mass loss, slowing the rate of lean body mass loss, resisting anorexia, resisting muscle weakness, resisting fatigue, resisting weight loss, and improving abnormal biochemical results. This invention provides a new understanding of the mechanism of energy balance regulation in cancer cachexia, focusing on the roles of S100a8 / a9 and C3 in cancer cachexia. This invention finds that inhibiting S100a8 / a9 and complement 3 can promote fat recovery and increase food intake. In particular, it demonstrates that S100a8 / a9 inhibitors can prevent the loss of body weight, especially adipose tissue, in cachectic subjects and significantly increase their food intake.

The present invention relates to the medical device and ophthalmological industry, as well as related fields such as dermatology and cosmetics, since the formulation includes natural neuroprotective components. The invention describes an iontophoretic delivery of cannabinoid-based formulations designed for ophthalmic conditions, that comprise pharmaceutically acceptable charged vehicles, including but not limited to cationic surfactants, cyclodextrins, nanoparticles and microspheres, emulsions or liposomes, with control the size distribution, potential, osmolality and pH. In a further embodiment of the invention, the intraocular composition proposed further comprises one or more synergistic agents, including but not limited to neuropeptides, exosomes, mitochondrial-derived peptides, complement inhibitors, senolytics, autophagy enhancers, antioxidants, saffron, and non-steroidal anti-inflammatory pharmaceutical drugs with pharmaceutically acceptable charged vehicle.

The present invention provides compounds and compositions for inhibiting complement-mediated damage to cells, tissues, or organs. [Solution] The present invention provides cell-reactive compstatin analogs and compositions comprising cell-reactive compstatin analogs. Furthermore, it provides methods for using cell-reactive compstatin analogs, for example, to inhibit complement-mediated damage to cells, tissues, or organs, for example, to treat complement-mediated disorders. Furthermore, it provides long-acting compstatin analogs and compositions comprising long-acting compstatin analogs. Furthermore, it provides methods for using long-acting compstatin analogs, for example, to inhibit complement-mediated damage to cells, tissues, or organs, for example, to treat complement-mediated disorders. Furthermore, it provides targeted compstatin analogs and compositions comprising targeted compstatin analogs.

A method of treating a patient with a complement-associated disorder with a complement inhibitor and then monitoring the patient during administration of the complement inhibitor and thereafter. The method includes certifying a prescriber and a dispenser and then monitoring the patient during and after administration of the complement inhibitor for an adverse event, including a meningococcal or pneumococcal event.

In some aspects, the present invention provides cell-reactive compstatin analogs and compositions comprising cell-reactive compstatin analogs. In some aspects, the invention further provides methods of using cell-reactive compstatin analogs, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides long-acting compstatin analogs and compositions comprising long-acting compstatin analogs. In some aspects, the invention further provides methods of using long-acting compstatin analogs, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides targeted compstatin analogs and compositions comprising targeted compstatin analogs. In some aspects, the invention further provides methods of using targeted compstatin analogs, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ.

Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.

The present disclosure relates to the development and application of a complement inhibitor, which is an antibody or antigen-binding portion thereof that binds to MASP-2. The disclosed antibody binds to MASP-2 with high affinity and specifically recognizes the enzymatically active domains CCP1-CCP2-SP of human, monkey, mouse, and rat MASP-2. It effectively inhibits the production of complement components C4b and C3 convertase C4b2b at low concentrations, with blocking activity 50-200 times higher than that of known antibodies. Furthermore, the MASP-2 antibody is well tolerated, exhibits no toxicity, and exhibits superior efficacy and safety compared to similar antibodies.

A composition for the use in peritoneal dialysis (PD) is hereby provided, the composition comprising a biologically compatible solvent, an osmotic agent and a complement inhibitor. Methods of manufacturing and of use of the composition are also provided.

The present application relates to the preparation method and application of the polysaccharide of Herba Siegesbeckiae, which includes total polysaccharide SOP and two uniform polysaccharides SOPC2-3 and SOPC3. The experiments prove that the polysaccharide of Herba Siegesbeckiae has a significant inhibitory effect on complement activation, and can be further used as an active ingredient to prepare a new complement inhibitor. The cell model experiments prove that the polysaccharide of Herba Siegesbeckiae can significantly inhibit the inflammatory response of LPS-induced RAW264.7 cells, and has anti-inflammatory activity, and can be further used as an active ingredient to prepare an anti-inflammatory drug. The animal experiments prove that the polysaccharide of Herba Siegesbeckiae (SOP and SOPC3) can effectively relieve LPS-induced acute lung injury in mice, and can be further used as an active ingredient to prepare a drug for preventing and treating acute lung injury.

This application provides antibody-drug synergistic compounds, compositions, and methods for treating ocular diseases such as dry AMD, GA secondary to AMD, and exudative AMD. The antibody-drug synergistic compounds may include antibodies such as anti-angiogenic antibodies or anti-VEGF antibodies conjugated to small molecule complement inhibitors by a linker, or anti-complement antibodies conjugated to small molecule inhibitors of VEGF, VEGFR, PDGF, PDGFR, FGF, or FGFR by a linker. The linker conjugating the antibody and drug is hydrolyzable over time within the target eye, thereby allowing both the antibody and drug to exert their functions within the target eye. The compounds and compositions can confer superior efficacy compared to either the antibody or the drug alone due to the synergistic effect of the ADS compounds. Methods for treating age-related macular degeneration using ADS compounds and compositions are also provided.

The present disclosure provides methods of treating inflammatory indications with complement inhibitor compounds and compositions. Included are compounds and methods of treating neuromuscular inflammatory indications, such as Immune-Mediated Necrotizing Myopathy.

The invention relates to development and application of a complement inhibitor. The complement inhibitor is an antibody which binds to MASP-2 or an antigen binding part thereof. The antibody disclosed by the invention can be combined with MASP-2 with high affinity, can specifically recognize enzyme activity domains CCP1-CCP2-SP of human, monkey, mouse and rat MASP-2, can effectively inhibit generation of complement components C4b and C3 invertase C4b2b under a low-concentration condition, has blocking activity 50-200 times higher than that of a known antibody, has good tolerance, does not have any toxic reaction, and can be used for preparing the MASP-2 antibody. The curative effect and the safety are better than those of similar antibodies.

The present application provides antibody-drug synergistic compounds, compositions, and methods for treating ocular diseases, such as dry AMD, GA secondary to AMD, and exudative AMD. The antibody-drug synergistic compound may comprise an antibody such as an anti-angiogenic antibody or an anti-VEGF antibody linked to a small molecule complement inhibitor through a linking group; or an anti-complement antibody linked to a small molecule inhibitor of VEGF, VEGFR, PDGF, PDGFR, FGF or FGFR via a linking group. A linking group linking the antibody and the drug may hydrolyze in the eye of the subject over time such that both the antibody and the drug function in the eye of the subject. Due to the synergy of the ADS compounds, the compounds and compositions can confer better efficacy than the antibody or drug alone. Methods of treating age-related macular degeneration using the ADS compounds and compositions are also provided.

The invention relates to a herba siegesbeckiae polysaccharide as well as a preparation method and application thereof. The herba siegesbeckiae polysaccharide comprises a herba siegesbeckiae total polysaccharide SOP and two homogeneous polysaccharides SOPC2-3 and SOPC3. Experiments prove that the herba siegesbeckiae polysaccharide has a remarkable inhibition effect on complement activation and can be further used as an active ingredient for preparing a novel complement inhibitor; a cell model experiment proves that the herba siegesbeckiae polysaccharide can remarkably inhibit inflammatory response of RAW264.7 cells induced by LPS, has anti-inflammatory activity and can be further used as an active component for preparing anti-inflammatory drugs; animal experiments prove that the herba siegesbeckiae polysaccharide (SOP and SOPC3) can effectively relieve LPS-induced acute lung injury of mice, and can be further used as an active component to prepare the medicine for preventing and treating the acute lung injury.

The present disclosure relates, inter alia, to compositions comprising a human complement inhibitor and use of the compositions in methods of treating or preventing complement-related disorders. In some embodiments, the inhibitor is administered chronically to patients. In some embodiments, the inhibitor is administered to a patient in an amount and frequency such that systemic complement inhibition is maintained and escape is prevented. In some embodiments, the composition comprises an antibody, or antigen-binding fragment thereof, which binds to the protein constituting the C5 component of human complement or to a fragment of the protein, such as C5a or C5b.

Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.

The present disclosure relates to the use of a Factor B inhibitor in the treatment of paroxysmal nocturnal hemoglobinuria. Specifically, the present disclosure relates to the use of the Factor B inhibitor or a pharmaceutically acceptable salt thereof in the preparation of a formulation for treating paroxysmal nocturnal hemoglobinuria (PNH) previously using a C5 complement inhibitor, wherein the Factor B inhibitor is represented by formula (I), (II) or (III).

To provide an inhibitor of complement system.SOLUTION: Compounds of Formula (I), and pharmaceutically acceptable salts thereof, are disclosed. Also provided are pharmaceutical compositions comprising such compounds, and methods of using the compounds and compositions in the treatment or prevention of diseases or conditions characterized by aberrant complement system activity.SELECTED DRAWING: None

The invention discloses a complement inhibitor as well as a preparation method and application thereof, and particularly discloses a compound as shown in a formula (I) or pharmaceutically acceptable salt thereof. The compound shown in the formula (I) has better in-vitro complement pathway hemolysis inhibition activity or better in-vivo half-life period, and lays a foundation for developing medicines for treating complement-related diseases. And R1-R2-R3-R4 (I) (In the formula, R1, R2, R3 and

The use of urine C5b-9 (uC5b-9) as a highly accurate and superior biomarker that is well correlated to complement activity in local tissue affected by complement-mediated diseases (e.g., diseases with renal lesion components) is provided. The biomarkers may be used, for example, in the absence of systemic complement inhibition, to treat and / or monitor diseases mediated by such complements using complement inhibitors targeted to local tissue affected by such complements.

The present application provides Antibody-Drug Synergism compounds, compositions, and methods for treating ocular diseases such as dry AMD, GA secondary to AMD, and exudative AMD. The Antibody-Drug Synergism compounds can comprise an antibody, such as an anti-angiogenesis or anti-VEGF antibody connected by a linker to a small molecule complement inhibitor; or an anti-complement antibody connected by a linker to a small molecule inhibitor of VEGF, VEGFR, PDGF, PDGFR, FGF, or FGFR. The linker connecting the antibody and the drug is hydrolysable over time in the eye pf a subject, so that both the antibody and the drug exert their functions in the subject's eye. The compounds and compositions can confer better efficacy than either the antibody or the drug alone due to a synergism of the ADS compound. Methods of treating age-related macular degeneration using the ADS compounds and compositions are also provided.

The present disclosure relates to the development and application of a complement inhibitor, which is an antibody or antigen-binding portion thereof that binds to MASP-2. The disclosed antibody binds to MASP-2 with high affinity and specifically recognizes the enzymatically active domains CCP1-CCP2-SP of human, monkey, mouse, and rat MASP-2. It effectively inhibits the production of complement components C4b and C3 convertase C4b2b at low concentrations, with blocking activity 50-200 times higher than that of known antibodies. Furthermore, the MASP-2 antibody is well tolerated, exhibits no toxicity, and exhibits superior efficacy and safety compared to similar antibodies.

The present invention relates generally to the field of disorders of complement activation. More specifically, the present invention provides methods and compositions useful for diagnosing and treating complementopathies and monitoring therapy in disease where complement inhibitors are used. In one aspect, the present invention provides a method for detecting dysregulation of the alternative pathway of complement in a patient. In one embodiment, the method comprises the steps of (a) contacting serum obtained from a patient with a composition comprising double CD46 / PIGA knockout (DKO) cells suspended in MgEGTA buffer; and (b) measuring luminescence continuously or serially over a period of time, wherein a lower luminescence related to a healthy control indicates dysregulation of the alternative pathway of complement in the patient.