40 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.

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 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 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 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.

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 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 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.

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.

The present invention relates to benzopyrazole compounds and analogs thereof. Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of Formula (I), and methods relating to the use of the compounds and compositions to treat and prevent diseases and conditions characterized by aberrant complement system activity.

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 invention relates to a pyrazol[3,4 c] pyridine derivative, preparation method and use in medicine thereof. Specifically, the present invention relates to a novel pyrazol[3,4 c] pyridine derivative, preparation method thereof and a pharmaceutical composition comprising the derivative and use thereof as a therapeutic agent, especially their use as Xa factor inhibitors and in the preparation of drugs for treating diseases like thromboembolism.

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

The invention discloses application of a transcription factor regulatory factor X1 (RFX1) inhibitor in preparation of a medicine for treating cardiac hypertrophy, and belongs to the field of gene application. A myocardial cell specific Rfx1 gene knockout mouse and a same-nest wild type Rfx1fl / fl mouse are taken as experimental subjects, a myocardial hypertrophy animal model is induced through aortic arch constriction, and the result shows that in the mouse myocardial hypertrophy model, the expression of RFX1 is remarkably up-regulated compared with that of a normal group; compared with a same-nest wild type Rfx1fl / fl model mouse, the heart weight / body weight, myocardial cell cross section area and fibrosis of the myocardial cell specific Rfx1 gene knockout mouse are all obviously reduced, the cardiac systolic function is obviously improved, and the results show that the Rfx1 gene knockout relieves the disease progress of pathological myocardial hypertrophy. Aiming at the effects of the RFX1, the inhibitor of the RFX1 can be used for preparing medicines for preventing, relieving and / or treating cardiac hypertrophy and heart failure.

The application discloses a model for predicting the risk of rivaroxaban anticoagulation bleeding and application thereof, and belongs to the technical field of biological detection. The model comprises a data input unit of two independent risk factors of a CYP3A4 genotype and clinical bleeding history of a subject, an assignment unit, an efficacy prediction unit and a report output unit, a C&B scoring system is formed according to the units, the total score is 3 points, if the C&B score is less than or equal to 1 point, rivaroxaban can be used as a coagulation factor X inhibitor for anticoagulant therapy, and if the C&B score is greater than or equal to 2 points, warfarin can be selected for anticoagulant therapy. The model can be used for guiding a clinician to accurately select a coagulation factor X inhibitor, the result of predicting the risk of rivaroxaban bleeding is accurate and reliable, and balance between anticoagulation benefits and bleeding risks can be achieved.

This invention discloses an isolated anti-FXI and / or anti-FXIa antibody or its antigen-binding fragment, which specifically binds to human FXI or FXIa, and provides a drug targeting FXI that effectively prevents or treats thrombosis with minimal side effects to meet medical needs. Because currently approved anticoagulants interfere with hemostasis, leading to an increased risk of bleeding, there is a significant unmet medical need for safer anticoagulants. Although thrombosis can be treated or prevented with anticoagulants (e.g., heparin, warfarin, aspirin, or factor Xa inhibitors), these treatments have significant adverse effects. Genetic and pharmacological evidence in humans and animals suggests that lowering coagulation factor XI (FXI) can successfully prevent and manage thrombosis with minimal bleeding.

The present invention relates to a therapeutic agent for use in treating diseases associated with gain of function of the androgen receptor (AR) and / or overexpression of an AR-activating cofactor, such as Kennedy's disease or cancer. The therapeutic agent of the present invention comprises at least one inhibitor of an androgen receptor (AR)-activating cofactor, selected from a protein arginine methyltransferase 6 (PRMT6) inhibitor, a lysine-specific demethylase 1 (LSD1) inhibitor, or a combination thereof.

The invention provides a transcription factor PfAP2-O5 inhibitor for Plasmodium falciparum, a pharmaceutical composition, and a drug for treating malaria resistant to artemisinin and an analog thereof. Disclosed in the present invention is new use of a triazoloquinoline derivative or a pharmaceutically acceptable salt or hydrate thereof. The triazoloquinoline derivative can inhibit the expression of an invasion gene pfap2-o5, block the invasion of Plasmodium falciparum into red blood cells, affect its growth and development, and achieve the effect of killing Plasmodium falciparum. Therefore, the triazoloquinoline derivative can be used as an inhibitor for pfap2-o5, a drug for inhibiting Plasmodium falciparum, or a drug for preventing or treating malaria.

The present disclosure provides a culture medium for cell culturing, the culture medium containing a combination of specific components. The present disclosure provides a culture medium which contains a combination of components selected from the group consisting of: (1) a halcinonide component; (2) an ALK4 / 7 inhibitor or a TGFβ receptor type-1 kinase inhibitor; (3) a BRD7 / 9 double degradation factor or a BRD7 / 9 binding molecule (degradation factor); (4) an LATS1 / 2 inhibitor, a PKA inhibitor, or an AKT1 inhibitor; (5) a CK1 / 2 inhibitor, an insulin receptor inhibitor, a Tyr kinase inhibitor, a PKA inhibitor or a PKC inhibitor, or an adenosine kinase inhibitor; (6) an E-selectin inhibitor, a VCAM1 inhibitor, or an ICAM1 inhibitor; and (7) an LATS1 inhibitor + an LATS2 inhibitor.

Disclosed are compounds of formula (I), 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.