Abstract: The present invention is intended to provide a novel antitumor agent that shows marked antitumor effects with reduced side effects. The present invention relates to an antitumor agent characterized by coadministration of an acyl thiourea compound represented by general formula (I) or a salt thereof, and an immune checkpoint molecule regulator.

Abstract: This disclosure provides methods for treating a hepatocellular carcinoma (e.g., unresectable HCC) with lenvatinib or a pharmaceutically acceptable salt thereof. Also encompassed by the disclosure are dosage regimens described herein of lenvatinib or a pharmaceutically acceptable salt thereof for use in treating hepatocellular carcinoma (e.g., unresectable hepatocellular carcinoma) according to any of the methods described herein. Particularly useful dosages and dose modifications upon the occurrence of an adverse event or events are also disclosed.

Abstract: The invention relates to novel crystalline solid forms of salts of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly renal cell carcinoma (RCC) and medullary thyroid cancer (MTC).

Abstract: A novel tumor therapeutic agent for a combination therapy is disclosed. More specifically, a tumor therapeutic agent used for a combination therapy of lenvatinib, ifosfamide, and etoposide is disclosed.

Abstract: The present invention relates to compounds for treatment of a disease or disorder associated with excessive vascularisation of the eye, such as for instance corneal neovascularisation, neovascularisation of the iris, neovascularisation of the ciliary body, corneal pannus, choroidal neovascularisation, retinal neovascularisation, wet age-related macular degeneration, proliferative diabetic retinopathy, retinopathy of prematurity, and ischemic retinopathy.

Abstract: Disclosed herein are compounds of Structural Formula I. Compounds of Structural Formula I inhibit aldehyde dehydrogenase isoform Ia3 (ALDHIa3) and are useful for treating cancer, for example, metastatic or chemoresistant cancer, such as metastatic cancer resistant to chemotherapy. Also disclosed herein are compositions comprising compounds of Structural Formula I and uses of compounds of Structural Formula I for treating cancer, for example, metastatic or chemoresistant cancer.

Abstract: The present invention relates to quinoline derivatives which are inhibitors for Axl/Mer RTK (receptor tyrosine kinase) and CSF1R (colony stimulating factor 1 receptor). These compounds are suitable for the treatment of disorders associated with, accompanied by, caused by or induced by Axl/Mer RTK and CSF1R, in particular a hyperfunction thereof. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly immune-suppressive cancer (such as those cancers with an immunosuppression of innate immunity in a tumor microenvironment (TME), refractory cancer and cancer metastases. They are also useful in the treatment of inflammatory diseases and/or neurodegenerative diseases.

Abstract: Pharmaceutical compositions are provided, which comprise cabozantinib or pharmaceutically acceptable salts thereof, and at least one pharmaceutically acceptable excipient, wherein the inventive compositions exhibit enhanced bioavailability compared to the currently marketed or commercially available formulations. The present invention also provides manufacturing processes thereof and use of the said inventive compositions for the prevention, treatment or prophylaxis of disorders in human patients in need thereof. The present invention relates to oral pharmaceutical compositions of cabozantinib, methods for their administration, processes for their production, and use of these compositions for treatment of diseases treatable by cabozantinib.

Abstract: The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.

Abstract: The present invention relates to pharmaceutical formulations comprising metolazone, a lipid, and an emulsifier that provide a lipid formulation of metolazone that can be administered intravenously to patients, thereby enhancing the therapeutic delivery and improving patient care for acute heart failure and resistant edmitious states.

Abstract: The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.

Abstract: The disclosure provides processes for synthesizing compounds for use as CFTR modulators.

Abstract: This invention relates to a liquid pharmaceutical composition comprising cabozantinib to treat locally advanced or metastatic solid tumors, particularly advanced urothelial cancer or renal cell carcinoma in patients in need thereof.

Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.

Abstract: Patients diagnosed with a cancer harboring an IDH-1 mutation can be treated by the administration of a therapeutically effective amount of a pharmaceutical composition comprising Compound 1, a selective inhibitor of 2-HG production from mIDH-1 enzymes including the R132 mutations R132C, R132H, R132L, R132G, and R132S.

Abstract: The present disclosure relates to methods of treating a malignancy in a subject in need thereof. The method involves administering to the subject a combination therapy comprising: (i) an inhibitor of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) having the structure of Formula (I) or a pharmaceutically acceptable salt, hydrate, polymorph, or solvates thereof, and (ii) an inhibitor of an anti-apoptotic Bcl-2 family protein, where the combination therapy is administered in an amount effective to treat the malignancy in the subject. Also disclosed are methods of reducing levels of regulatory T cells in a patient suffering from a malignancy, as well as combination therapeutics comprising an inhibitor of mucosa-associated lymphoid tissue lymphoma translocation protein (MALT1) having the structure of Formula (I) or a pharmaceutically acceptable salt, hydrate, polymorph, or solvates thereof, and an inhibitor of an anti-apoptotic Bcl-2 family protein.

Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.

Abstract: Disclosed are pharmaceutical compositions comprising Compound I, having the formula: and an effective amount of sofosbuvir wherein the sofosbuvir is substantially crystalline. Also disclosed are methods of use for the pharmaceutical composition.

Abstract: This disclosure relates to compounds according to Formula (I), salts, prodrugs and pharmaceutical formulation comprising the compound are provided herein for the treatment of CXCR4 and CCR5 related conditions. The conditions may include viral infections, abnormal cellular proliferation, retinal degeneration and inflammatory diseases, or the compounds may be used as immunostimulants or immunosuppressants. Furthermore, the compounds may be used in combination with another active ingredient selected from an antiviral agent or chemotherapeutic agent.

Abstract: Compounds of Formula (I) and methods for treating, delaying, and/or preventing the adverse effects of proliferative diseases, such as cancers including, for example, lung cancer, breast cancer, ovarian cancer, prostate cancer, head cancer, neck cancer, head and neck cancer, or leukemia (e.g., cancer resistant to treatment by one or more microtubule-targeting agents, e.g., cancer resistant to multiple drugs associated with P-glycoprotein (P-gp) overexpression). Methods of inhibiting polymerization of a cancer cell microtubule in a subject in need thereof or a cell, tissue, or biological sample, binding ?-tubulin, inhibiting microtubule assembly and, inducing apoptosis in a cancer cell resistant to multiple drugs in a tissue, biological sample, or subject. Pharmaceutical compositions, kits, and methods of using the compounds for treating any of the target diseases described herein.

Abstract: Provided are a prediction device and the like capable of more accurately simulating an analysis target. The prediction device generates function information for a gene sequence of a living body to be an analysis target based on first model information representing a relevance between sequence information and the function information, the sequence information representing the gene sequence of the analysis target, the function information representing a function potentially expressed by the gene sequence; and generates prediction information representing observation information predicted for the analysis target based on second model information and the function information, the second model information representing a relevance among the function information of the living body, environment information representing an environment around the living body, and the observation information observed for the living body, the function information being generated for the gene sequence of the analysis target.

Abstract: Provided herein are compounds, compositions and methods of using the compounds and compositions for the treatment of diseases modulated, as least in part, by AhR. The compounds are represented by formulae Formula (I), (II), (III), (iv): wherein the letters and symbols a, b, c, d, e, f, g, Z, R1b, R2a and R2b have the meanings provided in the specification.

Abstract: The present invention relates to the field of cancer therapy. Specifically, provided are methods of treating cancer, for example, peripheral T-cell lymphoma (“PTCL”), with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on gene expression characteristics.

Abstract: The present invention relates to use of an aminomethylenecyclohexane-1,3-dione compound, more particularly to use of a compound shown in the following formula (I) or a pharmaceutically acceptable salt thereof alone or in combination with other drug in preparing a drug for regulating or treating a disease related to autophagy, especially mammalian ATG8 homologous proteins.

Abstract: The present invention concerns Thymosin alpha 1 (T?1) for use in treatment of cystic fibrosis as a CFTR corrector, CFTR potentiator and anti-inflammatory agent.

Abstract: This invention is directed to the treatment of cancer, particularly lung cancer, breast cancer, melanoma, renal cell carcinoma, thyroid cancer that has metastasized to the bone. The invention is also directed to a method for treating bone cancer pain in an individual in need of such treatment comprising administering to the individual an effective amount of a compound of Formula I.

Abstract: This invention relates to a liquid pharmaceutical composition comprising cabozantinib to treat locally advanced or metastatic solid tumors, particularly advanced urothelial cancer or renal cell carcinoma in patients in need thereof.

Abstract: The present invention relates to an improved process for the preparation of N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide compound of formula-1 which is represented by the following structural formula:

Abstract: Methods of treating patients diagnosed with AML or MDS harboring mutant IDH-1 include detecting an IDH1 mutation and the therapeutic administration of an inhibitor of a mutant IDH-1 as a single agent, or in combination with azacitidine (AZA) or cytarabine.

Abstract: A bilayer composition for amelioriation of, or prophylaxis against, SARS-CoV-2 infection comprising a: (i) a first layer consisting of 250 mg to 1600 mg of 5-aminolevulinic acid (ALA), or salt thereof, and pharmaceutically acceptable excipients that allow for immediate release of the 5-aminolevulinic acid; (ii) a second layer consisting of hydroxychloroquine (HCQ), and/or a salt thereof, in a dose of 100 mg-1500 mg, or salt thereof, and at least one pharmaceutically acceptable excipient comprising a release modifier for sustained release of the hydroxychloroquine or chloroquine.

Abstract: The present invention relates to compounds for treatment of a disease or disorder associated with excessive vascularisation of the eye, such as for instance corneal neovascularisation, neovascularisation of the iris, neovascularisation of the ciliary body, corneal pannus, choroidal neovascularisation, retinal neovascularisation, wet age-related macular degeneration, proliferative diabetic retinopathy, retinopathy of prematurity, and ischemic retinopathy.

Abstract: Provided are compounds and compositions for prevention and/or elimination of Zika virus infection. Also provided are methods for preventing and treating a subject in need of prevention or treatment of Zika virus.

Abstract: The present invention provides a quinoline derivative for the treatment of nasopharyngeal carcinoma and use thereof in preparation of a pharmaceutical composition for tumor treatment.

Abstract: The present invention relates to methods for treating a disease associated with insulin resistance selected from a nonalcoholic fatty liver disease (NAFLD) and its sequelae, a lipodystrophic syndrome or a combination thereof with the selective PPAR? agonist, INT131 and optionally vitamin E or compositions thereof. NAFLDs that may be treated with methods and compositions of the present invention include, but are not limited to, simple nonalcoholic fatty liver and nonalcoholic steatohepatitis (NASH). Lipodystrophic syndromes that may be treated with the methods and compositions of the present invention include, but are not limited to, generalized lipodystrophy including congenital generalized lipodystrophy and acquired generalized lipodystrophy and/or partial lipodystrophy, including congenital partial lipodystrophy and acquired partial lipodystrophy, all of which may or may not include hyperlipidemia and/or hyperglycemia and may or may not include NAFLD.

Abstract: The present invention provides compounds useful for treating, ameliorating or preventing a disease or disorder that is caused, induced or characterized by abnormal reduction in glutamate transporter activity or abnormal increase in extracellular CNS glutamate concentration in a subject. In certain embodiments, the compound stimulates a glutamate transporter.

Abstract: The invention relates to compounds of formula I inhibiting Rho Kinase that are tyrosine analogues derivatives, processes of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

Abstract: It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators.

Abstract: Patients diagnosed with a cancer harboring an IDH-1 mutation can be treated by the administration of a therapeutically effective amount of a pharmaceutical composition comprising Compound 1, a selective inhibitor of 2-HG production from mIDH-1 enzymes including the R132 mutations R132C, R132H, R132L, R132G, and R132S.

Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

Abstract: Method and compounds for treating cancer by, for example, modulating immune system activity, are provided.

Abstract: A novel quinolone derivative and methods of its preparation are described in which the novel derivative comprises a diphenyl ether substituent on the nitrogen atom at the 1-position of the main quinolone ring. The novel derivative is shown to have antibacterial and anti-tumor cell activity.

Abstract: The present invention relates to a pharmaceutical composition comprising a DUSP1 inhibitor. The pharmaceutical composition comprising the DUSP1 inhibitor according to the present invention can solve the problems of inhibitors that target the active site because it inhibits DUSP1 by an allosteric inhibitory mechanism, and is effective for preventing or treating diseases involving DUSP1 enzymes, for example, a cancer such as a liver cancer, a breast cancer and a pancreatic cancer, a hepatitis C, and a depression. In particular, the DUSP1 inhibitor according to the present invention is very effective in treating a depression because it directly acts on neuronal growth.

Abstract: The present disclosure relates to a method of treating advanced renal cell carcinoma (RCC) in human patients who have received prior anti-angiogenic therapy using CABOMETYX, a kinase inhibitor.

Abstract: Aminoquinoline compounds useful for treating chronic pain, addiction, and other conditions are provided. The aminoquinoline compound is represented by Formula (I): in which the substituents thereof are defined as set forth in the specification.

Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.

Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide.

Abstract: The present invention relates to a method of treating and/or preventing cancer comprising administering a combination of an effective amount of a DNA hypomethylating agent and an effective amount of at least one immunomodulatory agent and/or optionally an effective amount of at least one targeted therapy agent.

Abstract: Described herein are compounds that are LOXL2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.

Abstract: The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.

Abstract: The present invention describes methods of identifying drugs for the treatment or prevention of diabetes by measuring the activity of the human zinc transporter ZnT8 and pharmaceutical compositions.