31 results about "Factor XIa" patented technology

Novel binding molecules comprising humanized antibodies, fragments, variants, and derivatives thereof, as well as compositions, methods, and kits comprising the same, are described, wherein the binding molecules specifically bind to FX1 and FX1a. The binding molecules are capable of binding to the factor X1A2 domain and forming immune complexes, thereby disrupting the contact activation molecule complex without affecting the activity or activation of hemostatic factor XI. The binding molecules disclosed herein are suitable for safely inhibiting thrombosis and inflammation without impairing hemostasis. Thus, the binding molecules, compositions, methods, and kits provided herein are intended for treating diseases and conditions, particularly those associated with thrombosis and inflammation. In addition, polynucleotides encoding the binding molecules disclosed herein, vectors comprising the polynucleotides, and host cells for producing the polynucleotides are also provided.

The present disclosure describes cyclic peptide inhibitors of Factor XI (FXI), preferably FXIa. Also described are pharmaceutical compositions comprising the cyclic peptides and their use in treating conditions, diseases and / or disorders responsive to FXI, preferably FXIa inhibition, including thrombosis or thrombo-inflammatory conditions.

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 disclosure provides methods for using antibodies that bind to Factor XI (FXI) for the purpose of preventing or treating clot formation or thrombogenesis after a surgical procedure. According to certain embodiments, the antibodies are antagonist antibodies that inhibit blood clot formation via the intrinsic pathway without affecting hemostasis, as shown by their effect on prolonging aPTT without affecting PT. As such, these antagonist antibodies may be used to treat or prevent clot formation in a subject requiring such treatment, such as, but not limited to, post-surgery.

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 present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XI activation inhibitors.

RNA interference (RNAi) agents for inhibiting the expression of Factor XI (FXI) are provided, as are pharmaceutical compositions comprising one or more FXI RNAi agents together with one or more excipients capable of delivering the RNAi agent(s) to a liver cell in vivo. Delivery of the FXI RNAi agent(s) to liver cells in vivo provides for inhibition of FXI gene expression and can provide for treatment of myocardial infarction, atrial fibrillation (AFib), deep vein thrombosis, pulmonary embolism, ischemic stroke, transient ischemic attack, retinal artery occlusion, mesenteric ischemia, renal vein thrombosis, cerebral venous sinus thrombosis, venous thromboembolism due to deep vein thrombosis, and peripheral artery disease, as well as diseases and disorders associated with angioedema, thrombosis, and / or coagulation.

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 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.

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 provides a heparin-insensitive assay for measuring the quantity of Factor XIa in a sample. The present invention provides a method for measuring the concentration of Factor XIa in a plasma sample by using enzymatic heparin degradation as sample pretreatment step.

This disclosure relates to dosage regimens for combination therapies comprising anti-Factor XI and / or activated Factor XI (Factor XIa) antibodies, or antigen-binding fragments thereof, e.g., for use in the treatment of thromboembolic disorders or related conditions.

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.

RNA interference (RNAi) agents for inhibiting the expression of Factor XI (FXI) are provided, as are pharmaceutical compositions comprising one or more FXI RNAi agents together with one or more excipients capable of delivering the RNAi agent(s) to a liver cell in vivo. Delivery of the FXI RNAi agent(s) to liver cells in vivo provides for inhibition of FXI gene expression and can provide for treatment of myocardial infarction, atrial fibrillation (AFib), deep vein thrombosis, pulmonary embolism, ischemic stroke, transient ischemic attack, retinal artery occlusion, mesenteric ischemia, renal vein thrombosis, cerebral venous sinus thrombosis, venous thromboembolism due to deep vein thrombosis, and peripheral artery disease, as well as diseases and disorders associated with angioedema, thrombosis, and / or coagulation.

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XI activation inhibitors.

The present invention is directed to Factor XIa inhibitors, tautomers, stereoisomers, isotopologues, and pharmaceutically acceptable salts and solvates 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.

A Factor XIa inhibitor having therapeutic properties useful in methods for treating or preventing ischemic stroke.

The present disclosure belongs to the field of biomedicines, and specifically relates to a nucleic acid capable of inhibiting the expression of a coagulation factor XI (factor XI), a pharmaceutical composition containing the nucleic acid, and an siRNA conjugate. Specifically, provided in the present disclosure is a double-stranded oligonucleotide capable of inhibiting the expression of FXI. The double-stranded oligonucleotide comprises a sense strand and an antisense strand, wherein the sense strand and the antisense strand are at least partially reverse-complementary to form a double-stranded region, the antisense strand is at least partially complementary to a segment of nucleotides within FXI-transcribed mRNA, the length of the sense strand does not exceed 21 nucleotides, the length of the antisense strand does not exceed 23 nucleotides, and the antisense strand comprises a sequence of at least 17 contiguous nucleotides that differs from any one of the nucleotide sequences as set forth in SEQ ID NOs: 175-347 and 706-714 by no more than 4, 3, 2, or 1 nucleotides. The oligonucleotide prepared in the present disclosure has a good inhibitory effect on the expression of the coagulation factor XI both in vitro and in vivo.

Methods for treating cancer using combination therapy with an anti-coagulant and a B-Raf inhibitor and / or a mitogen-activated protein kinase (MEK) inhibitor are disclosed. The anti-coagulant may be a direct inhibitor of thrombin or an indirect inhibitor of thrombin, such as an inhibitor of factor Xa, factor XIa, or other coagulation factors.

This invention relates to the field of pharmaceutical biology and discloses a single-domain antibody against coagulation factor XI (FXI) and its derived protein. Specifically, this invention discloses a coagulation factor XI (FXI) binding protein derived from a single-domain antibody against coagulation factor XI (FXI) and its uses.

The present disclosure describes cyclic peptide modulators of Factor XI (FXI). Also described are pharmaceutical compositions comprising the cyclic peptides and their use in treating conditions, diseases and / or disorders responsive to FXI modulation, including thrombosis or thrombo-inflammatory conditions.

The present disclosure provides antibodies that bind to the catalytic domain of factor XI (FXI) and methods of use thereof. According to certain embodiments, the antibodies are antagonistic antibodies that inhibit clot formation via the intrinsic pathway without affecting hemostasis, as demonstrated by their ability to prolong aPTT without affecting PT. Thus, these antagonistic antibodies can be used in the treatment or therapeutic regimen of blood clotting diseases or disorders that have clot formation as a risk factor, such as, but not limited to, atrial fibrillation. In certain embodiments, the present disclosure includes antibodies that bind to FXI and mediate clot or thrombus formation. The antibodies of the present disclosure can be fully human, non-naturally occurring antibodies.

The present invention relates to monoclonal antibodies and antigen-binding fragments thereof that bind to human Factor XI and activated Factor XI ("Factor XIa"), as well as to pharmaceutical compositions and treatment methods comprising them.

The present invention provides a factor XIa inhibitor having therapeutic properties useful in a method of preventing a thrombotic condition in a human patient suffering from cardiovascular or cerebrovascular disease.

The present invention is in the field of coagulation diagnostics and concerns a method for excluding Factor XIa inhibitors in a patient sample.

The invention relates to the field of medical biology, and discloses a single-domain antibody aiming at a blood coagulation factor XI (FXI) and a derived protein thereof. Specifically, the invention discloses a blood coagulation factor XI (FXI) binding protein derived from a single domain antibody aiming at the blood coagulation factor XI (FXI) and application of the blood coagulation factor XI (FXI) binding protein.

The invention relates to an anti-FXI and / or FXIa antibody or an antigen-binding fragment thereof, a nucleic acid molecule encoding the antibody or the antigen-binding fragment thereof, a pharmaceutical composition containing the antibody and application of the composition in preparation of drugs for preventing and / or treating diseases or symptoms related to blood coagulation or thromboembolism. Experiments show that after being subjected to humanized modification, the anti-FXI and / or FXIa antibody or the antigen binding fragment thereof has higher affinity to FXI and / or FXIa than MAA868, and can effectively inhibit the activity of FXI and / or FXIa.