Abstract: Methods are provided for the treatment of cancer by administering a combination of metabolic interventions to differentiate the cancer cells. The effect on the targeted cancer cell is enhanced relative to a regimen in which a single agent is used; and the effect may be synergistic relative to a regimen in which a single agent is used.

Abstract: Provided herein are enhanced systems for potentiating cell-mediated oncolytic viral therapy. Also provided are modified viruses for such systems, and methods of treatment of cancers by administering such systems.

Abstract: Disclosed herein are compositions and methods for treating cancer in a subject. In some embodiments, the methods involve generating an immune response in an individual by inducing the expression of neoantigens on the surface of abnormal (such as proliferative) cells. In one embodiment, a method of treating cancer in a subject includes administering amlexanox in combination with immune modulators, such as checkpoint inhibitors, immune co-stimulatory molecules, TLR agonists, and TNFR superfamily agonists. In one embodiment, the checkpoint inhibitors are selected from antibodies against PD-1, PD-L1, and CTLA-4.

Abstract: Provided herein are novel lipase inhibitors and methods for using the same to treat inflammation, multisystem organ failure, necrotic pancreatic acinar cell death, acute pancreatitis, sepsis (e.g., culture negative sepsis), burns, and acne. For example, provided herein are two novel lipase inhibitors useful in the methods described herein: or a pharmaceutically acceptable salt thereof.

Abstract: A method for non-invasive assessment of photoreceptor function in a mammalian subject comprises exposing a subject's eye to a visible light stimulus to initiate an intrinsic reflectance response in one or a population of photoreceptors and capturing multiple images of photoreceptor's intrinsic reflectance response to the stimulus. Patterns of variability in the intrinsic reflectance response of a single photoreceptor or population of photoreceptors are useful in diagnosis and treatment monitoring of an ocular condition, disease, disorder or a response to treatment for said ocular condition, disease or disorder.

Abstract: Provided herein are triazacyclododecansulfonamide (“TCD”)-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer.

Abstract: Disclosed are a novel therapeutic means effective and practical against cancer, and a novel substance useful as such a therapeutic means. Provided are novel peptides derived from a partial region of HMGN1, HMGN2, HMGN4 or HMGN5, and anti-cancer agents and anti-cancer effect enhancers containing the peptide as an active ingredient. The peptide of the present invention has an anti-tumor effect even independently, and exerts a remarkably excellent anti-tumor effect particularly when used in combination with an immune checkpoint regulator, or an anti-CD4 antibody or antigen-binding fragment thereof.

Abstract: A method and system is provided for determining a discrimination index in a subject that may be suffering from or at risk for a stress-induced psychiatric disorder. The discrimination index may be equal to a ratio of a subject's cued fear response and non-cued fear response measured during a fear-potentiated startle (FPS) paradigm. Such a value may allow a physician or researcher to quantify how well a subject discriminates between signaled (cued) fear and un-signaled (non-cued) fear, which may be a biomarker for psychiatric disorders like post-traumatic stress disorder, panic disorder, phobias, and/or generalized anxiety disorder. The determined discrimination index may provide a standardized way of diagnosing and evaluating mental illnesses, more uniform treatment of patients, and/or more precise monitoring and evaluation of treatment efficacy.

Abstract: The present disclosure provides, among other things, a way to amplify and sequence target sequences in a low-input sample. In some embodiments, the method comprises ligating a double-stranded adaptor onto a population of fragments to produce tagged fragments, and linearly amplifying the tagged fragments.

Abstract: The present invention provides a quinoline derivative for treating triple-negative breast cancer and use thereof in preparing a pharmaceutical composition for treating a tumor.

Abstract: The disclosure provides cryptophycin intermediates, cryptophycin analogs, and cryptophycin chimeric molecules useful in treating cancer, as well as methods of producing these compounds and methods of treating cancer.

Abstract: This disclosure features methods and compositions for treating diseases of the gastrointestinal tract with an immunosuppressant.

Abstract: Provided herein are carrier cells and virus combinations and methods for treatment of cancers. Also provided are modified carrier cells for such treatment, and methods of selecting carrier cells that are matched to subjects for such treatment.

Abstract: The current methods and compositions provide for therapeutic approaches to treating hepatocellular carcinoma (HCC) and other types of cancer including, for example, pancreatic and colon cancer. Accordingly, certain aspects of the disclosure relates to methods and compositions for treating HCC, pancreatic and colon cancer using one or more small molecule inhibitors disclosed herein. In certain embodiments, the small molecule inhibitor is a benzothiazine, a sulfonamide, a thiazolidinone or other chemical compound.

Abstract: In various embodiments, the present invention provides compositions and methods for treating and/or preventing cardiovascular-related diseases in subject in need thereof.

Abstract: In various embodiments, the present invention provides compositions and methods for treating and/or preventing cardiovascular-related diseases in subject in need thereof.

Abstract: The invention provides compounds of formula (I) and compositions comprising compounds of formula (I). The invention further provides uses of the compounds of formula (I) and compositions comprising compounds of formula (I), including the use of such compounds for the detection of tau deposits, and the use of such compounds and compositions as diagnostic agents in the diagnosis or monitoring of the progression of a disease or disorder such as Alzheimer's disease or corticobasal degeneration, or for the prevention or treatment of a disease or disorder such as Alzheimer's disease or corticobasal degeneration.

Abstract: The invention relates to a CXCR4 receptor-binding compound for use for increasing or restoring interferon (IFN) level in an individual, wherein the interferon is a type-I interferon (IFN-I).

Abstract: Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.

Abstract: The present invention relates to methods of using HEATR1 expression levels for guiding chemotherapy treatment of pancreatic cancer. In particular, measuring lower HEATR1 expression in pancreatic cancer is associated with resistance to the use of certain chemotherapy treatments such that by changing the treatment a better prognosis may be obtained for the patient. Further, lower HEATR1 expression is related to a poorer long-term prognosis of pancreatic cancer patients thus measuring an increase or maintenance/decrease during treatment may be useful for predicting treatment response.

Abstract: The present invention provides compounds (n-3 PUFA derivatives) of formula (I): that modulate conditions associated with cardiac damage, especially cardiac arrhythmias.

Abstract: Disclosed are processes for forming compositions comprising small domains of an active agent and a matrix material, and methods of using them. A suspension of an active agent, a matrix material, a first solvent, and a second solvent is formed at a temperature T1, heated to a temperature T2 and spray dried.

Abstract: Methods of treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing percutaneous coronary intervention (PCI), comprising administering to the patient a pharmaceutical composition comprising cangrelor. The method may further comprise administering an additional therapeutic agent to the patient, the additional therapeutic agent comprising a P2Y12 inhibitor. Pharmaceutical compositions useful for treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing PCI. The pharmaceutical compositions comprise cangrelor. Methods of preparing a pharmaceutical composition for treating, reducing the incidence of, and/or preventing an ischemic event in a patient undergoing PCI, comprising admixing cangrelor with one or more pharmaceutically acceptable excipients. An ischemic event may include stent thrombosis, myocardial infarction, ischemia-driven revascularization, and mortality.

Abstract: Provided herein are novel lipase inhibitors and methods for using the same to treat inflammation, multisystem organ failure, necrotic pancreatic acinar cell death, acute pancreatitis, sepsis (e.g., culture negative sepsis), burns, and acne. For example, provided herein are two novel lipase inhibitors useful in the methods described herein: or a pharmaceutically acceptable salt thereof.

Abstract: Provided herein are methods, devices, compositions, and kits for monitoring neuromodulation efficacy based on changes in the level or activity of one or more target biomarkers. One aspect includes a comparison of baseline and post-modulation levels of one or more biomarkers in bodily fluid that have each been collected from a human subject at a relevant time, and that may be used to assess the neuromodulation efficacy. The post-neuromodulation levels for the one or more biomarkers may be collected from the human subject within about 5 minutes to about 14 days post-neuromodulation.

Abstract: Provided herein are compounds that can bind GAS5 long non-coding RNA, compositions thereof, and uses thereof.

Abstract: The present invention relates to methods of treating a tumor or treating cancer in a subject having a p53 DNA contact mutation that involve administering, to the subject, a ROCK inhibitor. Also disclosed is a method of identifying a subject as a candidate for such treatment.

Abstract: A process for preparing the benzothiophen-2-yl boronate of formula (VI) which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of proliferative disorders, such as cancer and tumor diseases.

Abstract: The invention relates to novel heteroaryl compounds of Formula (I) and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cardiovascular diseases, and methods treating sepsis or septic shock, using the novel heterocyclic compounds disclosed herein.

Abstract: Methods of treating sleep disorders, particularly certain aspects of insomnia, in elderly patients (65 years and older) by administering initial daily dosages of doxepin of 1-3 mg. These ultra-low initial dosages are more effective in elderly versus non-elderly patients in decreasing wake time during sleep, latency to persistent sleep and wake time after sleep, and are particularly efficacious in treating those conditions in the last hour of an 8-hour sleep cycle. Also, the dosages described herein are safe for elderly individuals.

Abstract: Disclosed is a method for preparing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) of formula (II), comprising the following steps: carrying out an alkylation reaction on cyclen in formula (I) and XCH2COOR in the presence of an acid-binding agent in water; adjusting a pH value to separate out a crude product of DOTA; and recrystallizing. The preparation method of the present invention is applicable to large-scale industrial production of DOTA, the whole process does not need to adopt an ion-exchange resin or low-temperature refrigeration mode for purification, and the purity and yield of the product are higher.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula (I) where p; q; X1; X2; Y; R1; R2; R3; R4; R5 and R6 are as defined herein.

Abstract: The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intellectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder).

Abstract: The disclosure relates to compounds of formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.

Abstract: The 6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,2,4]triazepine derivatives or salts thereof of the present invention have BRD4 inhibitory activity, and thus, they are useful as medicaments, in particular, as prophylaxis and/or therapeutic agents for diseases associated with BRD4.

Abstract: Methods of the invention treat, reduce, or reverse fibrosis of a bodily tissue by administering to the local affected tissue a composition comprising an inhibitor of p38 MAP kinase, which treatment leads to a reduction or reversal of fibrosis.

Abstract: The present invention refers to new purified compositions of long chain polyunsaturated fatty acids, or their salts or esters, characterized by being essentially free from other usually present—but structurally different—components, such as furan fatty acids, phytanic and pristanic acids, squalene, and some oligomers, as well as several “persistent” environmental pollutants, such as polychlorinated dibenzo-dioxins and polychlorinated dibenzo-furans, polychlorinated biphenyls, polybrominated diphenyl-ethers, polycyclic aromatic hydrocarbons, and others, which are also usually present and extremely toxic. The invention also refers to the purification method to obtain said compositions and the use thereof as food, food for special medical use, food and diet supplement, and drug.

Abstract: The use of direct factor Xa inhibitors, administered in a dose sufficient to reduce the activity of factor Xa to about 25% less than normal or lower, has the effect of preventing the onset of atherosclerosis, and stabilizing atherosclerotic lesions, and preventing the occurrence or recurrence of atherosclerotic events.

Abstract: Provided herein are methods, devices and compositions for assessing neuromodulation efficacy based on changes in the level of one or more biomarkers in plasma or urine collected from a human subject following a renal neuromodulation procedure.

Abstract: Derivatives of N,N-diethyl-N?-phenyl-piperazine, a silent agonist of the mammalian ?7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.

Abstract: The present invention provides pharmaceutical composition of antineoplastic alkylating agent in oral suspension dosage form. The oral suspension composition comprises of alkylating agent with other pharmaceutical excipients such as vehicle, preservative, antioxidant, suspending agent, surfactant, sweetener and flavouring agent. The present invention is an oral suspension having improved stability and palatability. The present invention also provides oral solution with flavor that has masked bitter taste of the drug. Further, the present invention also provides a process for preparation thereof.

Abstract: The present invention relates to a coumarin (keto) oxime ester compound of formula (I), wherein n and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification. The compound has strong ultraviolet absorption in the range of 300 to 450 nm. After absorbing light energy, it can quickly transfer energy and continuously initiate polymerization. It has obvious advantages in terms of photosensitivity and pattern integrity, and is very suitable for radiation curing by UV-LED light source. In addition, the compound of formula (I) also has good thermal stability. The present invention also relates to a method for preparing the compound of formula (I) and use of the compound. The compound is suitable as a photoinitiator in a UV-LED light curing system and is suitable for the radiation wavelength of UV-LED light curing.

Abstract: 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.

Abstract: The present invention provides 4-anilino-3-quinolinecarbonitriles compounds useful for treating a subject having an BcrAbl positive leukemia that is resistant to imatinib.

Abstract: The invention provides an amorphous metal-organic framework for use in methods of treatment. The amorphous metal-organic framework may hold a component for delivery. The amorphous metal-organic framework is obtained or is obtainable by amorphization of a crystalline amorphous metal-organic framework holding the component. The amorphous metal-organic framework may be a zirconium-containing or a bismuth-containing metal-organic framework, such as a framework having arylcarboxylate ligands, such as benzenedicarboxylate ligands.

Abstract: The present invention relates to substituted methanopyrido [2,1-a]isoindolones of formula I, wherein, R1 is selected from phenylsulfonyl or p-toluenesulfonyl; and n=1, 2, 3; their derivatives, stereoisomers, pharmaceutically acceptable salts and pharmaceutically acceptable compositions having potential muscarinic acetylcholine receptor modulator activity.

Abstract: 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.

Abstract: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

Abstract: Disclosed are compounds of Formula 1, stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein L, r, s, R5, R6, R7, R9, R10, R11, R12, X1, X2, X3, X4, X13, and X14 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.

Abstract: Disclosed is a novel quinazoline compound. Specifically, disclosed are a compound represented by the formula (I) and a pharmacologically acceptable salt.