72 results about "Factor inhibitors xa" patented technology

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.

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.

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).

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 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.

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 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 gMG (systemic myasthenia gravis) with the factor B inhibitor ipropam, or a pharmaceutically acceptable salt or hydrate thereof.

The present invention provides compounds useful for the treatment or prevention of diseases or conditions involving (a) thromboembolic disorders, (b) inflammatory disorders, or (c) plasma kallikrein activity. [Solution] A compound of formula (I), or its tautomers, stereoisomers, isotope substitutions, or pharmaceutically acceptable salts or solvates is provided. TIFF2026062690000101.tif47128

The invention provides a complement factor B inhibitor, the structure of the complement factor B inhibitor is basically shown in a general formula (I), and the definition of each substituent group in the formula is shown in the specification. The compound provided by the invention has obvious complement factor B inhibition activity, and can be used for preventing and / or treating complement factor B inhibitor mediated diseases or disease states. # imgabs0 #

The present disclosure is in the field of coagulation diagnostics and relates to a method for excluding anticoagulants from the group of factor XIa inhibitors in a patient sample.

Provided is use of a complement factor B inhibitor in the preparation of a drug for treating or preventing IgA nephropathy or a disease or condition related thereto. Specifically, provided is use of a compound represented by formula I or a pharmaceutically acceptable salt thereof or a hydrate thereof in the preparation of a drug for treating or preventing IgA nephropathy or a disease or condition related thereto. The drug can effectively reduce creatinine and urea nitrogen levels in patients with IgA nephropathy, reduce renal inflammation and / or fibrosis in patients with IgA nephropathy, and provide a novel, effective and safe option for the treatment of IgA nephropathy.

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

The present invention provides compounds of Formula (I):or stereoisomers, tautomers, or pharmaceutically acceptable salts 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 present invention relates to compounds of formula (I) having an indole moiety attached to an indazole moiety, compounds having core-like structures and related salts, solvates, prodrugs and pharmaceutical compositions. The invention also relates to methods of synthesizing such compounds and to the use of such compounds in the treatment and prophylaxis of medical conditions and diseases, most particularly by Factor B inhibition.

The present invention relates to compounds (I) having an indole moiety attached to an isoindoline moiety, compounds having core-like structures and related salts, solvates, prodrugs and pharmaceutical compositions. The invention also relates to methods of synthesizing such compounds and to the use of such compounds in the treatment and prophylaxis of medical conditions and diseases, most particularly by Factor B inhibition.

The present invention is directed to 3-(1H-imidazol-2-yl)-2,3,8,8a-tetrahydroindolizin-5(1H)-one derivatives, stereoisomers, isotopologues, and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and / or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.