75 results about "Brain cancers" patented technology

Disclosed herein are methods of producing organoids. In some aspects, the methods involve producing organoids by implanting primary cancer cells such as glioblastoma cells into brain organoids, thereby producing brain cancer organoids. The method can comprise an incubation step in which the brain organoid is incubated with primary cancer cells in a hanging liquid droplet to produce the brain cancer organoid. In some aspects, the brain cancer organoids provide tools for understanding and treating cancers of the nervous system, such as glioblastoma.

Disclosed herein are antibodies and compositions used for binding to Gal3. Some embodiments allow for disrupting interactions between Galectin-3 (Gal3) and cell surface markers and / or proteins associated with neurological diseases and / or proteopathies, such as Alzheimer's disease. Additionally, disclosed herein are methods of treatment and uses of the antibodies or binding fragments thereof for the treatment of fibrosis, liver fibrosis, kidney fibrosis, cardiac fibrosis, pulmonary fibrosis, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, sepsis, atopic dermatitis, psoriasis, cancer, brain cancer, breast cancer, colorectal cancer, kidney cancer, liver cancer, lung cancer, pancreatic cancer, bladder cancer, stomach cancer, hematological malignancy, neurological diseases and / or proteopathies. Furthermore, some embodiments provided herein can cross the blood-brain barrier and can be conjugated or otherwise associated with one or more payloads for the treatment of a neurological disease.

A quinazoline derivative (represented by the formula (I)) salt's crystal form, a preparation method and application are provided; specifically, the hydrochloride crystal form A, B, C, D, F, H, I, Sulphate crystal form A, Maleate crystal form A, Succinate crystal form A, Adipate crystal form A, Glycolate crystal form A, Malate crystal form A, Fumarate Salt crystal form A, besylate crystal form A, B, C, benzoate crystal form A, hippurate crystal form A and oxalate crystal form A of the quinazoline derivative represented by formula (I). The salt crystal form provided by the present invention has good stability, which can be used in the treatment of non-small cell lung cancer brain metastasis, meningeal metastasis, primary brain cancer or glioma, etc., and has good bioavailability, which is of great significance for further research on the efficacy of such solid drugs.

Provided are methods and compositions for enhancing radiotherapy in various cancers by administering dopamine receptor (DRD2)‐binding phenylpiperazine derivatives such as brexpiprazole, cariprazine, pipamperone, and perospirone. In vitro studies show that combining these agents with ionizing radiation (e.g., 5 Gy) significantly reduces cancer cell survival, suppresses metastatic and stemness markers (e.g., CD44, MMP‑2, Snail, Nanog), and promotes apoptosis. Fractionated or single‐fraction radiation regimens can be paired with DRD2 antagonists to lower treatment‐resistant phenotypes, decrease the likelihood of recurrence, and potentially reduce necessary radiation dosages. The approach applies to breast, prostate, lung, pancreatic, and brain cancers, among others. Depending on tumor characteristics, additional chemotherapeutic or immunotherapeutic agents may further improve outcomes.

The present application relates to the field of polymer chemistry and biomedical technology, and particularly relates to a macrocyclic lactone polymer shown in formula (I) which is used for preventing or treating hyperproliferative diseases, including liver cancer, leukemia, breast cancer, colon adenocarcinoma, gastric cancer, lung cancer, Barrett's esophageal cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymphoma, kidney cancer, brain cancer, nerve cancer, nasopharyngeal cancer, oral cancer, bladder cancer, colorectal cancer and melanoma, and has the potential to be developed into a new type of antitumor drug.

The present disclosure is concerned with compounds and compositions for use in the prevention and treatment of cancer associated with FBOX21 mediated p85a ubiquitination such as, for example, cancer (e.g., sarcoma, a carcinoma, a hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, melanoma, a glioma, leukemia, lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, non-small cell lung carcinoma, renal cancer, lung cancer, colon cancer, cervical cancer, and plasma cell neoplasm (myeloma)). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The present disclosure is concerned with compounds and compositions for use in the prevention and treatment of cancer such as, for example, a primary or secondary tumor within a subject's brain, breast, kidney, pancreas, lung, colon, prostate, lymphatic system, liver, ovary, or cervix. Additional examples of cancers for which the disclosed compounds and compositions can be useful include, but are not limited to, sarcomas, carcinomas, hematological cancers, solid tumors, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, melanomas, gliomas, leukemia, lymphoma, chronic myeloproliferative disorders, myelodysplastic syndrome, myeloproliferative neoplasm, non-small cell lung carcinomas, and plasma cell neoplasms (myelomas). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The present disclosure relates to linezolid derivatives, in particular of Formula (I), the definition of p, A, A1 and R1 are as defined in the specification; the process of preparing the same and uses thereof in treatment of brain cancers, in particular glioblastoma.

The present invention relates to a local targeting photodynamic therapy device for treating cancer. In more detail, an endoscope is disposed at the center of the end of a probe for photodynamic therapy, and a plurality of optical fibers are disposed along the edge to irradiate a plurality of lights to a lesion site, wherein the plurality of optical fibers of the probe receive light from independent light sources to independently perform light irradiation. The present invention is a device for minimizing damage to unnecessary normal tissue by adjusting the light irradiation area, i.e., each independent light source determines a light irradiation area including a lesion site in a real-time image provided by an endoscope disposed at the end of the probe, and only causes the independent light source that irradiates the determined light irradiation area to emit light, thereby achieving local light irradiation, etc. The local targeting photodynamic therapy device of the present invention can treat a variety of cancers or tumors, including cervical cancer, female cancers (endometrial cancer, ovarian cancer, breast cancer), skin cancer, brain cancer, etc., which are small and can be treated locally.

A compound derivative is provided, where R in the compound of formula A is piperidine, and the compound derivative can be used in the treatment of cancer and other diseases through the development of small molecules as eukaryotic elongation factor 2 kinase (eEF2K) enzyme inhibitors that are active in breast, pancreatic, brain, ovarian, lung, skin and blood cancers.

Disclosed are purine derivatives of formulae (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods involving the inventive compounds or compositions for treating and / or preventing cell proliferative diseases including certain cancers of breast, brain, ovarian, lung, colorectal cancer, leukemias, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma and inflammatory and myotonic dystrophy type 1 diseases in a mammal. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of kinases, such as a cyclin-dependent kinases (CDK) (e.g., CDK12 / 13), and therefore, induce potent antiproliferative and apoptotic effects and / or inhibit transcription in the subject.

The present disclosure relates to RNAi agents useful in methods of treating KRAS-related diseases such as a proliferative disease, including without limitation a solid or liquid cancer, adenocarcinoma, colorectal cancer, advanced and / or metastatic colorectal cancer, colon cancer, lung, non-small cell lung cancer and lung adenocarcinoma, acute myelogenous lung, bladder, brain, breast, cervical, endometrial, gastric, head and neck, kidney, leukemia, myelodysplastic syndrome, myeloid leukemia, liver, melanoma, ovarian, pancreatic, prostate, testicular, thyroid cancers, and cardio-facio-cutaneous (CFC) syndrome and Noonan syndrome, and similar and related diseases, using a therapeutically effective amount of a RNAi agent to KRAS.

Osmotic blood-tissue barrier opening offers a promising approach to surmounting challenges posed by the blood-brain barrier in the treatment of brain cancer and neurological diseases. By enhancing permeability of any blood-organ barrier, enabling precise targeting, reducing toxicity, being less invasive, and potentially accommodating larger therapeutic molecules, osmotic blood-organ barrier opening represents a valuable strategy in the fight against diseases such as brain cancer and neurological diseases.

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

To provide anti-Gal3 antibodies and methods of use.SOLUTION: Disclosed herein are antibodies and compositions used for binding to Gal3. Some embodiments allow for disrupting interactions between Gal3 and cell surface markers and / or proteins associated with neurological diseases and / or proteopathies, such as Alzheimer's disease. Additionally, disclosed herein are methods of treatment and uses of antibodies or binding fragments thereof for treatment of fibrosis, liver fibrosis, kidney fibrosis, cardiac fibrosis, pulmonary fibrosis, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, sepsis, atopic dermatitis, psoriasis, cancer, brain cancer, breast cancer, colorectal cancer, kidney cancer, liver cancer, lung cancer, pancreatic cancer, bladder cancer, stomach cancer, hematological malignancy, neurological diseases and / or proteopathies. Furthermore, some embodiments provided herein can cross the blood-brain barrier and can be conjugated or otherwise associated with one or more payloads for the treatment of a neurological disease.SELECTED DRAWING: Figure 1

The invention relates to compounds, compositions, and methods for derepressing RE1 silencing transcription factor (REST) target genes are provided. In particular, a peptide having the sequence TEDLEPPEPPLPKEN (SEQ. ID NO: 1) and EDLEPPEPPLPK (SEQ. ID NO: 15), or the reversed sequences made of D-amino acids (retro inverted, RI) nekplppeppeldet (SEQ ID NO: 16) and kplppeppelde (SEQ ID NO: 17), are disclosed for inhibiting REST activity. The peptides are useful to treat, prevent, or ameliorate conditions such as traumatic brain injury, epilepsy, dementia, Huntington's Disease (HD), chronic pain, brain cancer (including glioblastoma multiforme), pancreatic cancer; diabetes, and peripheral nerve injury

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of carbothioamide (and structurally related) small-molecule compounds which function as inhibitors of SIRT5, and their use as therapeutics for the treatment of diseases associated with posttranslational modification functions (e.g., diseases associated with SIRT5 activity) (e.g., cancer (e.g., melanoma, non-small cell lung cancer (NSCLC), hepatocellular carcinoma (HCC), ovarian cancer, colorectal cancer (CRC), acute myeloid leukemia (AML), Ewing's sarcoma, brain cancer, pancreatic cancer, renal cancer, breast cancer, prostate cancer, lung cancer, leukemia and lymphoma), diabetes, autoimmune diseases, inflammatory diseases, fibrotic diseases, cardiovascular diseases, and neurodegenerative diseases).

Combination therapies for use in the treatment of brain tumours, particularly glioma and embryonal brain tumours. Disclosed herein are pharmaceutical compositions comprising a complex of Panobinostat and a cyclodextrin, a second pharmaceutical agent, and a pharmaceutically acceptable excipient, diluent or carrier, in which the second pharmaceutical agent is Niclosamide, Dasatinib or Duvelisib. Associated methods of treatment and use are further disclosed.

Disclosed herein are novel compounds that are Mpsl / TTK inhibitors. Also disclosed are compositions comprising the compounds and methods of using the compounds in treating various diseases. In some embodiments, some such compounds, compositions, and their uses may be useful for the treatment of cancer. In some implementations, the cancer is brain cancer, glioblastoma multiforme, head and neck cancers, colorectal cancer, stomach or gastric cancer, pancreatic cancer, melanoma, bladder cancer, kidney cancer, renal cell carcinoma, breast cancer, ovarian cancer, lymphoma, thyroid cancer, mesothelioma, sarcoma, lung cancer, non-small cell lung cancer, small cell lung cancer, or endometrial cancer.

A compound derivative is provided, where R in the compound of formula A is (2-(2-(piperidin-1-yl)ethane-1-amine), and the compound derivative can be used in the treatment of cancer and other diseases through the development of small molecules as eukaryotic elongation factor 2 kinase (eEF2K) enzyme inhibitors that are active in breast, pancreatic, brain, ovarian, lung, skin and blood cancers.

The present invention relates to a 2-amino-substituted derivative (Formula I) or an ethylenediamine-substituted derivative (Formulas II and III) of hypocrellin as a photodynamic drug for treating the following tumors: esophageal cancer, gastric cancer, lung cancer, liver cancer, cholangiocarcinoma, colon cancer cells related to digestive tract tumors; brain cancer, head and neck cancer, tongue cancer, nasal cancer, oral cancer, glioblastoma cells related to head, neck and facial tumors; basal cell carcinoma, squamous cell carcinoma, cutaneous T-cell lymphoma, melanoma cells related to skin tumors; prostate cancer, bladder cancer cells related to genitourinary tumors. At the same time, such derivatives can localize the location of tumor tissues through their own fluorescence and are used for fluorescence-guided surgical resection of tumors.

Photodynamic therapy (PDT) is a minimally invasive treatment that involves the administration of a light-activatable drug followed by light activation of the lesion to produce reactive oxygen species that kill cancer cells. VISUDYNE®, a liposomal formulation of benzoporphyrin derivative (BPD) photosensitizer, is clinically approved for PDT of ocular diseases and is now being tested for PDT and imaging of pancreatic, brain, and other cancers. While VISUDYNE® improves the pharmacokinetics of BPD, it lacks treatment selectivity. This present disclosure is directed to dBPD, dBPD nanoparticles, and preparation and use thereof that provide cancer treatment selectivity for cancers characterized by overexpression of folate receptor (FR).

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecule compounds having a 6,6-heterocyclic structure (e.g., compounds having a naphthyridine, pyrido-pyridazine, pyrido-pyrazine, quinoline, pyrazino-pyridazine, pyrimido-pyrimidine, quinazoline, quinoxaline or cinnoline ring system) which function as inhibitors of DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK3, CLK4, CDK7, CDK8 / 19, PI3K, PDGFrA / B, mTOR, WNT, homeodomain-interacting kinases (HIPKs), and / or CMGC kinases leading to inhibition of WNT signaling, and their use as therapeutics for the treatment of Alzheimer's disease, down syndrome, Parkinson's disease, Huntington's disease, diabetes, autoimmune diseases, inflammatory disorders (e.g., airway inflammation, osteoarthritis (e.g., knee related osteoarthritis)), cancer (e.g., glioblastoma, prostate cancer, metastatic breast cancer, metastatic lung cancer, multiple myeloma, secondary metastatic tumors of the brain, colorectal cancer and metastatic colorectal cancer (e.g., metastatic colorectal cancer in the liver)), and other diseases.

The presently disclosed subject matter relates to antibodies and antigen-binding fragments that bind specifically to phosphorylated PDGFRA, and methods of treating cancer expressing MAN2A1-FER which ectopically phosphorylates PDGFRA. MAN2A1-FER can be expressed in liver cancer, prostate cancer, brain cancer, glioblastoma multiforme, breast cancer, lung cancer, non-small cell lung cancer, colon cancer, and renal cell carcinoma.

Methods for identifying tumor tissue and determining a margin of a tumor to be resected in a subject are disclosed within. The methods utilize guanidinoacetic acid (GAA) as a tissue biomarker of malignant brain tumors. The presently disclosed subject matter further relates to methods for providing a diagnosis or prognosis about a cancer in a subject.

The present application relates to sequences that enhance penetration of immunotherapeutics across the blood brain barrier (BBB), compositions comprising the same, and methods thereof for treating brain cancers such as glioblastoma (GBM). Further disclosed are a number of potential targeting peptide sequences identified as enhancing penetration across the BBB when inserted into the capsid of an adeno-associated virus (AAV).

The present invention relates to a compound of formula (I) wherein R1 represents a halogen atom, a (C1-C6) alkyl group, a (C3-C6) cycloalkyl group, a (C2-C6) alkenyl group, a (C1-C6) alkoxy group or a (C3-C6) cycloalkyloxy group, X and Y independently represent a-CH = group,-CR3 = group or-N = group, Z1 and Z2 independently represent a-CH2-group, an = CH-group or an = N-group, and R3 and R4 independently represent a hydrogen atom or a halogen atom, or any pharmaceutically acceptable salt thereof. The invention also relates to the use of the compounds as a medicament, in particular for the treatment and / or prevention of cancers, in particular cancers exhibiting recruitment of MDM2 to chromatin, the present invention relates to a cancer, more particularly a cancer selected from the group consisting of bone cancer, brain cancer, ovarian cancer, breast cancer, lung cancer, colorectal cancer, osteosarcoma, skin cancer, leukemia (including acute myelogenous leukemia), pancreatic cancer, prostate cancer and liposarcoma, even more particularly a cancer selected from the group consisting of skin cancer, liposarcoma and leukemia, such as but not limited to liposarcoma, melanoma and acute myelogenous leukemia.

The present disclosure relates to compounds, pharmaceutical compositions, and methods of using the compounds and compositions to restore activity of von Hippel Lindau tumor suppressor protein (pVHL). Such compounds and compositions can be useful in, for example, the treatment of cancer (e.g.. a sarcoma, a carcinoma, a head-and-neck cancer, hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, melanoma, a glioma, leukemia, lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, non-small cell lung carcinoma, small cell lung carcinoma, renal cancer, lung cancer, colon cancer, cervical cancer, and plasma cell neoplasm (myeloma)) and von Hippel-Lindau disease (VHLD). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The present disclosure relates to a combination of a tubulin polymerization inhibitor and a cholesterol homeostasis disrupting agent that can be used to treat proliferative diseases, such as cancer. Preferred combinations are shown to be effective against a variety of cancer cell types, including brain cancers, such as glioblastoma.

Nanoparticle compositions including one or more active agents, and strategies for enhanced delivery of the active agents, are provided. In preferred embodiments, the nanoparticles are composed of block copolymers of one or more hydrophobic polymers that form the core, and a hyperbranched polymer that forms a shell or corona. In some embodiments, the particles include an acid-sensitive, poly(amine-co-ester) (PACE) that can increase release of the active agent in acidic environments, for example within endosomes. The compositions can include one or more targeting moieties. Preferred targeting moieties include adenosine agonists and pHLIP which can enhance delivery to tumor cells. Methods of using the compositions to treat diseases and disorders of the central nervous system, for example, brain cancers such as glioma, are also provided.