104 results about "Factor inhibitors xa" patented technology

The present invention relates to compounds of formula (I) possessing an indole moiety linked to an indazole moiety, to compounds having similar core structures, and to associated salts, solvates, prodrugs and pharmaceutical compositions. The present invention further relates to methods of synthesising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by Factor B inhibition.

The present invention relates to compounds (I) possessing an indole moiety linked to an isoindoline moiety, to compounds having similar core structures, and to associated salts, solvates, prodrugs and pharmaceutical compositions. The present invention further relates to methods of synthesising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by Factor B inhibition.

The invention provides a complement factor B inhibitor compound, pharmaceutically acceptable salts thereof, a medicinal composition thereof and application of the complement factor B inhibitor compound in preparation of medicines related to complement factor B. The compound has a structural formula shown in a formula (I), and experimental results show that the compound has good complement factor B inhibitory activity, good in-vivo C3a level inhibition rate, bioavailability and safety. Particularly, the polypeptide has more remarkable binding capacity with target protein. # imgabs0 #

Disclosed in the present invention are a preparation method for a complement factor D inhibitor, an intermediate thereof, and a preparation method for an intermediate. The present invention provides a preparation method for a new complement factor D inhibitor, a new intermediate, and a preparation method for an intermediate. The selectivity of a reaction is improved by means of the new intermediate, the material conversion rate of each step of a route is high, a reaction type is common, the length of the route is moderate, and the obtained products can all be purified by means of a conventional method to obtain a target product, thereby reducing the production costs, and facilitating industrial production.

The present invention belongs to the field of biotechnology. Disclosed is a dosage composition of a complement factor B inhibitor. Specifically, the present invention provides a pharmaceutical composition comprising a compound represented by formula I, an isomer thereof, or a pharmaceutically acceptable salt thereof in a unit dosage form, wherein the mass of the compound or the pharmaceutically acceptable salt thereof is 5-1500 mg based on the free base.

Described herein are methods of treating gMG (generalized Myasthenia gravis) with the Factor B inhibitor iptacopan or a pharmaceutically acceptable salt or hydrate thereof.

The present invention belongs to the technical field of biology. Disclosed are a crystal form of a complement factor B inhibitor, a preparation method therefor and the use thereof. Specifically, the present invention provides a crystal form of a compound represented by formula I, a preparation method therefor and the use thereof. The crystal form prepared by the present invention has good stability, for example, crystal form stability and thermal stability.

Provided herein are compounds of formula (I) and pharmaceutical compositions thereof that are useful for treating diseases or disorders mediated by complement factor B. [Formula 1] TIFF2025511100000139.tif32170

Devices, systems, and methods are provided including a structure having one or more surfaces configured for internal use within a patient's body and one or more therapeutic compositions comprising one or more active substances including at least one of a chelating agent, a direct factor Xa inhibitor, a direct factor IIa inhibitor, and a factor XI / XIa inhibitor disposed in or on the structure. The structure is configured to be positioned adjacent a target site in the patient's body. The therapeutic composition is formulated to release the one or more active substances to the target site to provide one or more of inhibit clot formation, promote clot dissolution, inhibit or dissolute inflammation, inhibit vessel injury, increase time before clotting, and / or inhibit cell proliferation. Delayed or other controlled release of the therapeutic composition from the structure may be provided.

Described herein are methods of treating ANCA-associated vasculitis (AAV) with the Factor B inhibitor iptacopan or a pharmaceutically acceptable salt thereof, e.g., iptacopan hydrochloride, or hydrate thereof.

To provide proteins for enhancing proliferation and / or healing and / or inhibiting apoptosis of non-transformed tissue or non-transformed cells.SOLUTION: The present invention provides proteins comprising amino acid sequences encoded by nucleic acids derived from a human chromosomal region C19Orf10 termed Factor 1 and / or C19Orf63 termed Factor 2, or inhibitors thereof. Further provided is use of inhibitors of Factor 1 and Factor 2 for medical use, preferably for use in treating or preventing a disease in which angiogenesis contributes to disease development or progression.SELECTED DRAWING: None

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

Disclosed herein is a method for treating immune complex-mediated membranoproliferative glomerulonephritis (IC-MPGN) with the factor B inhibitor iptacopan or a pharmaceutically acceptable salt thereof (e.g., iptacopan hydrochloride).

The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.

Disclosed are direct-binding dual hypoxia-inducible factor (HIF) inhibitors and their use for treating cancer, including, but not limited to, breast, colorectal, lung, melanoma, pancreatic, and prostate cancer as a monotherapy and in combination with anti-CTLA-4 or anti-PD-1 immunotherapies. The dual HIF inhibitors also can be used for treating diseases, disorders, or conditions associated with ocular neovascularization, including, but not limited to, diabetic macular edema, diabetic retinopathy, and other ischemic retinopathies (including, but not limited to retinal vein occlusion, sickle cell retinopathy, retinopathy of prematurity, Norrie's disease, and Coat's disease), corneal neovascularization, and the treatment or prevention of neurovascular (wet-type) age-related macular degeneration.

Described herein are methods of treating immune complex mediated membrane proliferative glomerulonephritis (IC-MPGN) with a factor B inhibitor ipropam or a pharmaceutically acceptable salt thereof, e.g., ipropam hydrochloride.

The present invention relates to the technical field of biology. Disclosed are a salt of a complement factor B inhibitor, a preparation method therefor and a use thereof. Specifically, the present invention provides a salt of a compound as shown in formula (A), a preparation method therefor and a use thereof.

The present invention provides novel antigen-binding peptides, such as antibodies or antibody fragments, that specifically bind to selective FXIa inhibitors and / or dual inhibitors of FXIa and plasma kallikrein.The present invention further relates to a method of reducing the antithrombotic effect of FXIa inhibitors by administering to a subject a pharma- ceutical effective amount of the antigen-binding peptides disclosed herein.In addition, the present invention provides detection reagents and methods for detecting FXIa inhibitor levels in biological samples. TIFF2024505390000129.tif113125

The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more compounds of Formula I compounds, and methods for using the compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

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 complement factor B inhibitor, and a method for treating various specific diseases or symptoms by using the complement factor B inhibitor. # imgabs0 #

The present invention provides compounds of Formula (I):or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and / or inflammatory disorders using the same.

The invention provides an application of a transcription factor PU.1 inhibitor or a pharmaceutically acceptable salt thereof in preparation of a medicine for treating ulcerative colitis, and belongs to the technical field of biological medicines. According to the invention, intervention is carried out from the upstream of an inflammation network through a small-molecule inhibitor specifically targeting a core transcription factor PU.1, and the multi-dimensional and synergistic treatment effect on ulcerative colitis is realized by regulating and controlling the functions of intestinal immune cells and maintaining the integrity of an intestinal barrier and the steady state of intestinal flora.

The present invention relates unit dose formulations of antidotes to anticoagulants targeting factor Xa. Disclosed herein are methods of stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.

Provided herein are methods for treating a subject with PNH comprising administering to a subject a therapeutically effective amount of complement component C5 (C5) inhibitor, complement component C3 (C3) inhibitor, or complement factor B (CFB) inhibitor in combination with a therapeutically effective amount of small molecule complement factor D (CFD) inhibitor of Formula I or Formula II, or a pharmaceutically acceptable salt thereof.

Described herein are methods of treating paroxysmal nocturnal hemoglobinuria (PNH) with the Factor B inhibitor LNP023 or a pharmaceutically acceptable salt thereof, e.g. LNP023 hydrochloride.

The present invention relates to binding molecules capable of reversing the anti-coagulant activity of direct oral anticoagulants in-vivo and in-vitro. The present invention, more particularly concerns binding molecules for reversing the factor Xa inhibition activity of a factor Xa inhibitor such as in a patient to whom a factor Xa inhibitor is administered. The present invention is further related to binding molecules capable of reversing the anti-coagulant activity of direct oral anticoagulants, for use in medicine and diagnostics. More particularly, the present invention concerns binding molecules for use in the treatment or prevention of bleeding, and for use in the detection and quantification of such molecules, e.g. in human plasma. The present invention further provides a method for detecting a factor Xa inhibitor in a sample.

The present invention provides a method for preventing, treating or alleviating bleeding caused by an anticoagulant using an anticoagulant reversal agent. The anticoagulant reversal agent has a structure as shown in formula I, can well inhibit bleeding complications caused by anticoagulants, for example, bleeding complications caused by anticoagulants such as an Xa factor inhibitor, and has the characteristics of broad spectrum and high efficiency.

The present application relates to a kind of 7-difluoromethyl-5-aryl pyrazolopyrimidine compound and preparation and application, the structural general formula of the compound is as shown in formula a, it is a kind of compound with inhibiting HIF-2 alpha activity, can block HIF-2 alpha / ARNT dimerization and play the role of HIF-2 transcription inhibition.The present application is proved by multiple experiments, the synthesized compound all has excellent HIF-2 transcription inhibition effect, in human renal clear cell carcinoma cell strain 786-O, show good VEGF protein inhibitory activity.The compound described in the present application can be applied in the preparation of hypoxia-inducible factor-2 alpha (HIF-2 alpha) inhibitor for treating VHL deletion or / and HIF-2 alpha abnormal expression disease.This kind of compound can inhibit the overexpression and activation of HIF-2 alpha, to achieve the treatment and prevention of target disease, such as VHL deletion or / and HIF-2 alpha abnormal expression disease.

Described herein are methods of treating paroxysmal nocturnal hemoglobinuria (PNH) with the Factor B inhibitor LNP023 or a pharmaceutically acceptable salt thereof, e.g. LNP023 hydrochloride.