390 results about "Proliferative disease" patented technology

The present application discloses substituted polycyclic heterocycles compound of Formula (I), pharmaceutically acceptable salt and / or solvate and pharmaceutical compositions thereof useful in the treatment of proliferative disease or condition characterized by a dysregulation of the RAS-ERK pathway such as neoplasm disease or disorder, inflammatory disease or immune system disorder.

The present disclosure is related to dual payload immunostimulatory antibody drug conjugates comprising at least STING agonist and at least one cytotoxic agent, pharmaceutical compositions thereof, and the use of the dual payload immunostimulatory antibody drug conjugates and compositions thereof for the treatment of diseases and disorders, including proliferative diseases.

The present disclosure provides amino acid sequences (e.g., antibodies) capable of binding to glypican 3 protein (GPC3). The present disclosure relates to antigen binding fragments of GPC3 antibodies; conjugates of a GPC3 antibody, including an immunoconjugate; bispecific antibodies comprising a GPC3 antibody and related compositions and formulations. The disclosure also relates to methods of treating GPC3-related diseases, disorders and conditions, including cell proliferative diseases, such as cancer, more particularly liver cancer, using these sequences, such as GPC3 antibodies and antigen-binding fragments thereof.

The present invention is directed to the tartrate salt of a FAK inhibitor defined by formula I below, and the use of that inhibitor for treating a proliferative disease:

A method for treating proliferative diseases such as cancer in a subject by a combination therapy, which includes administering to the subject a pharmaceutical composition including a benzenesulfonamide derivative such as p-Toluenesulfonamide and at least one other therapeutic agents in a different classification of anticancer agents.

The present invention relates to MOFs for use in imaging and as radiolabeled tracers. More specifically, the present invention provides particles comprising MOFs, optionally at least one targeting moiety, and at least one short-lived radionuclide; compositions comprising the particles; the particles or compositions for use as imaging agents; the particles or compositions for use in methods for diagnosing proliferative diseases; the particles or compositions for use in methods for diagnosing chronic inflammatory diseases; and kits comprising particles comprising MOFs, optionally a targeting moiety, and a short-lived radionuclide cation.

The present disclosure provides a novel bifunctional compound that degrades EGFR, pharmaceutical compositions containing the compound, methods of preparation, and uses of the compounds of the disclosure to treat cell proliferative diseases, such as cancer.

The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of the PI3Kα enzyme using the compounds and compositions of the present disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3Kα signaling using the compounds and compositions of the present disclosure. Inhibitors of PI3Kα are considered to be particularly valuable in the treatment of proliferative diseases and other disorders. A plurality of inhibitors of PI3K (for example, taselisib, alpelisib, buparlisib, etc.) have been developed, but these molecules inhibit multiple class 1A PI3K isoforms.

The present invention relates to a benzo five-membered heterocyclic derivative and a use thereof. Specifically, disclosed is a compound having a structure as shown in formula (I) or formula (II), the definitions of the groups and substituents being as set forth in the description. Also disclosed is a use of the compound in treating or preventing diseases related to PARG activity, in particular proliferative diseases (such as cancer).

The present invention relates to compounds having cyclin-dependent kinase (CDK)-inhibitory functions and / or pharmaceutically acceptable salts thereof, the use of these compounds as pharmaceutically active agents, especially for the prophylaxis and / or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing such compounds.

The present invention relates to MOFs for radiotherapy. More specifically, the present invention provides: a particle comprising an MOF, optionally at least one targeting moiety, and at least one beta-emitting radionuclide; a composition comprising the particles; said particles or composition for use as a medicament; said particles or compositions for use in a method of treating a proliferative disease; and a kit comprising a particle comprising an MOF, optionally a targeting moiety, and a beta-emitting radionuclide.

The present invention is directed to the tartrate salt of a FAK inhibitor defined by formula (I) below, and the use of that inhibitor for treating a proliferative disease.

Provided are serum-resistant vaccinia extracellular enveloped viruses (EEV), methods of producing serum-resistant EEVs, and modified EEVs for systemic oncolytic viral therapy. Provided herein are methods to modify vaccinia viruses to produce serum resistant EEVs for systemic oncolytic viral therapy. Compositions containing serum resistant EEVs and methods of treating cancers and other proliferative diseases are provided.

A camptothecin compound and a conjugate thereof, or a tautomer thereof, an enantiomer thereof, a diastereomer thereof, or a mixture form thereof, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutical composition thereof, a preparation method therefor, and use thereof. The compound and the conjugate can be used for treating proliferative diseases related to abnormal cell activity.

The present disclosure provides compounds of Formula (I), (II), and (III). The provided compounds are able to bind protein kinases (e.g., SIK) and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase (e.g., SIK, (e.g., SIK1, SIK2, or SIK3)) in a subject or cell. The provided compounds may be useful in treating or preventing a disease (e.g., proliferative disease, musculoskeletal disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.

The present invention relates to compounds of formula (I): wherein R2, R3, R4, R5, Y1, Y2, A1, A2, A3 and A4 are each as defined herein, targeting a component MLH1 of a DNA mismatch repair (MMR) process. The invention also relates to processes for preparing these compounds, pharmaceutical compositions comprising them, and their use in the treatment of proliferative diseases, such as cancer, as well as other diseases or conditions involving MLH1 activity (e.g., triad repeat disorders). # imgabs0 #

Provided herein, inter alia, are novel compositions and solid forms of Compound 1 useful for the prevention and / or treatment of allergic diseases, inflammatory diseases, metabolic diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage renewal, congenital cartilage malformations, and / or intermediates associated with IFN [alpha], interferon ("interferon disease", etc. In particular type I or type III interferon disease), diseases associated with excessive secretion of IL-12 and / or IL-23. # imgabs0 #

Disclosed are compounds of Formula (I) or a salt thereof, wherein Ring A is a carbon-linked ring; and Ring A, R1, and n are defined herein. Also disclosed are methods of using such compounds to inhibit Helios protein, and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

The present disclosure is related to dual mechanism of action payload antibody drug conjugates comprising at least two payload residues, pharmaceutical compositions thereof, and the use of the antibody drug conjugates and compositions thereof for the treatment of diseases and disorders, including proliferative diseases.

The present disclosure is related to antibody conjugates, including antibody drug conjugates, comprising multiple payloads at high payload to antibody ratios, pharmaceutical compositions thereof, and the use of the antibody conjugates and compositions thereof for the treatment of diseases and disorders, including proliferative diseases.

The invention is based on the surprising finding that SIK3 is associated with resistance against anti-tumour immune responses. In particular, the invention provides methods for treating proliferative diseases using inhibitors of SIK3, especially nucleic acid or small molecule inhibitors of SIK3. Also provided are methods of sensitising cells involved with a proliferative disorder against the cytotoxic effect of certain pro-inflammatory signalling pathways, and / or to kill such cells and / or methods for treating proliferative diseases, using a SIK3 inhibitor together with ligands or agonists of such signalling pathways. Other methods provided by the invention include those involving SIK3 inhibitors to enhance or overcome certain side effects associated with treatments that utilise such signalling pathways, as well as diagnostic, prognostic and monitoring methods and kits based on the detection of SIK3 in a sample obtained from a subject, and screening methods useful for identifying or characterising inhibitors of SIK3.

Compounds, compositions and their use in the treatment of a proliferative disease or condition such as a said proliferative disease or disorder is associated with a RAF gene mutation and / or a RAS gene mutation. The compounds disclosed are of Formula I or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, X1, X2, X3 and X4 are as defined herein:

This document provides bifunctional compounds, one part of which (e.g., lenalidomide, thalidomide) is a binder of an E3 ubiquitin ligase (e.g., Cereblon) and the other part of which is a binder of a target protein (e.g., a kinase (e.g., CDK (e.g., CDK9 and / or CDK12))) to induce the degradation of the target protein CDK9 and / or CDK12. Pharmaceutical compositions comprising bifunctional compounds are also provided, as well as methods for treating and / or preventing diseases (e.g., proliferative diseases such as cancers (e.g., ovarian cancer, breast cancer, or prostate cancer)). Methods for inducing the degradation of target proteins (e.g., kinases (e.g., CDK (e.g., CDK9 and / or CDK12))) and methods for inducing apoptosis in biological samples or subjects by administering the bifunctional compounds or compositions described herein are also provided.

Provided herein are compounds that act as molecular glues, inducing degradation of CK1α or CK1α / GSPT1, and pharmaceutically acceptable derivatives thereof. Also provided are pharmaceutical compositions containing the compounds and methods of using the compounds for treating a subject with a proliferative disease.

This invention provides compounds for the treatment, prevention, or suppression of various pathological conditions (such as proliferative disorders like cancer, β-globin disorders, fibrosis, pain, neurodegenerative diseases, Prader-Willi syndrome, malaria, viral infections, myopathy, and autism) by inhibiting G9a. [Solution] The following general formula (I) TIFF2026062914000401.tif2449 A compound represented by or a pharmacoposly acceptable salt thereof is provided.

The present invention discloses compounds according to Formula I:wherein R1a, R1b, R1c, R2a, W1, W2, X1, X2, X3, Y, and Z are as defined herein.The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and / or treatment of inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of IL-6, diseases associated with hypersecretion of TNFα, interferons, IL-12 and / or IL-23, respiratory diseases, endocrine and / or metabolic diseases, cardiovascular diseases, dermatological diseases, and / or abnormal angiogenesis associated diseases by administering the compound of the invention.

The present disclosure provides a class of compounds useful for restoring the wild-type function of the mutant p53, pharmaceutical compositions containing the compounds, and methods of treating cell proliferative diseases, such as cancer, using the compounds of the disclosure. The compound has a structure as shown in a formula (I-C). # imgabs0 #

Disclosed are new anti-HER2 ADCs conjugated to camptothecin derivatives as toxins for therapeutic use. The antitumor effects of the ADCs of Formula (PL-A) (e.g., compounds MB-2a and MB-3a (trastuzumab meditecan)) render these compounds useful for treating cell proliferative diseases such as cancers.

Disclosed are compounds of Formula (1): Also disclosed are methods of using such compounds to decrease the levels of Ikaros protein, Helios protein, Aiolos protein, and Eos protein; and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.