Abstract: The present invention relates to methods of treating p53 wild type (WT) tumors. In particular, the invention provides novel therapies for p53 WT tumors based on the combination of Mouse Double Minute 2 (MDM2) inhibitors, e.g. HDM201, together with Casein Kinase 1 alpha (CK1?) degrading agents and/or an MDM4 inhibitors, e.g. lenalidomide. The combination may be used in the treatment of solid as well as hematologic p53 WT tumors, e.g. Merkel cell carcinoma (MCC) or myelodysplastic syndrome (MDS).

Abstract: Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific irreversible inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL irreversible inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL interaction.

Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.

Abstract: Described herein is N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(R)-[(1-oxo-2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide (I) including crystalline forms, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include compound (I), as well as methods of using compound (I), alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: Compounds, compositions, and methods useful for inducing cancer cell death via methuosis, autophagy, or a combination thereof, are described. The compounds have a 4-pyridyl group linked by a heterocyclic group to an aryl, heteroaryl, aralkyl, or heteroaryl alkyl.

Abstract: The present disclosure relates to compounds of Formula (Ia) and (Ib): or a pharmaceutically acceptable salt thereof, which are useful in the treatment of an HIV infection in heavily treatment-experienced patients with multidrug resistant HIV infection.

Abstract: A compound 1,3-benzothiazol-2-yl-N?-[(pyridine-3-carbonyl)oxy]ethanimidamide, its synthesis, and its use as an anticancer and/or antimicrobial agent.

Abstract: Provided are a benzimidazole compound represented by the general formula (1) {wherein R1 represents a hydrogen atom or a cyano group, R2 represents a (C1-C6) alkyl group, a (C1-C6) alkoxy (C1-C6) alkyl group, or a halo (C1-C6) alkyl group, R represents a (C1-C3) alkylene group or a halo (C1-C3) alkylene group, and m represents 0, 1, or 2}, or a salt thereof, an agricultural and horticultural insecticide comprising the compound or the salt as an active ingredient; an animal ectoparasite or endoparasite control agent comprising the compound or the salt as an active ingredient; and a method for using the insecticide or the agent.

Abstract: The present invention relates to a stable pharmaceutical formulation comprising omeprazole, its enantiomer, or its pharmaceutically acceptable salt, and sodium bicarbonate, and a method for preparing the same. Specifically, the present invention provides a stable formulation by preventing omeprazole, its enantiomer, or its pharmaceutically acceptable salt, from coming in direct contact with sodium bicarbonate, to reduce the production of impurities.

Abstract: The present invention generally relates to liquid compositions and methods for treating oral inflammation by administering a liquid composition to the oral cavity. The liquid composition is prepared from a powder containing calcium glycerophosphate, one or more sodium phosphate salts, sodium chloride, and optionally sodium bicarbonate and silica. The powder is mixed with a quality of water to form a liquid that is supersaturated with calcium ions and phosphate ions and is essentially free of visible particles and precipitate.

Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.

Abstract: Provided are formulations and methods for treating one or more genitourinary conditions. The formulations may include a therapeutic agent that includes a calcium channel blocker, a rho kinase inhibitor, or a combination thereof. The methods may include locally administering a therapeutic agent into a ureter. Systems for delivering a therapeutic agent also are provided.

Abstract: The invention concerns a pharmaceutical combination of an inhibitor of the androgen receptor signaling pathway and of a p38 inhibitor for use in the treatment of prostate cancer in individuals wherein the prostate tumor cells express the AR-V7 variant androgen receptor protein or for preventing the occurrence of resistance in patients suffering from prostate cancer treated by an inhibitor of the androgen receptor signaling pathway. The invention further concerns a pharmaceutical composition comprising enzalutamide, abiraterone or apalutamide and a p38 inhibitor selected from LY2228820 and ARRY-614, and at least one pharmaceutically acceptable excipient.

Abstract: A pellet contains a core, which contains one or more biologically active ingredients, and a coating layer on the core. The coating layer contains a mixture of a first polymer and a second polymer. The first polymer is a core-shell polymer, containing 50 to 90% by weight of a core, containing polymerized units of 60 to 85% by weight of ethyl acrylate and 20 to 40% by weight of methyl methacrylate; and 10 to 50% by weight of a shell, containing polymerized units of 40 to 60% by weight ethyl acrylate and 40 to 60% by weight methacrylic acid. The second polymer contains polymerized units of 40 to 60% by weight of methacrylic acid and 60 to 40% by weight of ethyl acrylate or methyl methacrylate. A Multi-Unit Pellet System (MUPS), preferably a compressed tablet, contains a multitude of the pellets.

Abstract: The present invention relates to a pharmaceutical combination comprising (a) an MDM2 inhibitor and (b) an ERK inhibitor, for use in the treatment of a cancer. This invention relates to uses of such combination for preparation of a medicament for the treatment of a cancer; methods of treating a cancer in a subject in need thereof comprising administering to said subject a jointly therapeutically effective amount of said combination; pharmaceutical compositions comprising such combination; and kits and/or packages containing such combinations.

Abstract: Compounds, compositions, and methods useful for inducing cancer cell death via methuosis, autophagy, or a combination thereof, are described. The compounds have a 4-pyridyl group linked by a heterocyclic group to an aryl, heteroaryl, aralkyl, or heteroaryl alkyl.

Abstract: Embodiments can provide a wearable device for nicotine cessation behavioral support, comprising a top surface; a first surface; a second surface; an underside surface; a communication device; one or more buttons; an internal storage medium; and a power supply; wherein the one or more buttons are configured to log a NRT use event to the internal storage medium when depressed and subsequently released within a predetermined timeframe; wherein the one or more buttons are configured to log a tobacco use event to the internal storage medium when depressed and released at a time longer than the predetermined timeframe; wherein the one or more buttons, when depressed, are configured to log a craving event to the internal storage medium, wherein an intensity of the craving event is determined by a time duration between depression and release of the one or more buttons.

Abstract: Alkoxybenzeno five- or six-member heterocyclic amines compounds, their pharmaceutically acceptable salts, and pharmaceutical compositions are used as the active ingredients, and their application in drugs which can prevent and cure diseases caused by abnormal increasing of SM. These diseases caused by abnormal increasing of SM include atherosclerosis, type II diabetes, fatty liver, obesity, metabolic syndromes, enteritis and other inflammatory diseases.

Abstract: This disclosure relates to treatments for reducing the side effects associated with treatment of a medication or drug, such as a chemotherapy medication, being experienced by a patient. This may be accomplished by administering to a patient taking the medication, a buffered aqueous liquid having a pH of about 10 to about 11.5, wherein the buffered aqueous liquid comprises sodium bicarbonate, sodium carbonate, and trisodium phosphate.

Abstract: Methods for reducing platinum drug-induced toxicity in a cell expressing Organic Cation Transporter 2 (OCT2), methods for reducing platinum drug-induced toxicity in a subject, methods for treating cancer, methods for increasing efficacy of platinum drug treatment in a subject, and pharmaceutical compositions are described. The described methods and compositions include an OCT2 inhibitor where the OCT2 inhibitor is buflomedil or a salt thereof, dolutegravir or a salt thereof contains an imidazole, or is miconazole or a salt thereof.

Abstract: Provided herein are methods for treating and/or preventing hepatocellular carcinoma (HCC) characterized by hepatitis B virus (HBV) infection in a patient, comprising administering an effective amount of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one or a pharmaceutically acceptable salt or tautomer thereof (collectively referred to herein as “Compound 1”) to the patient having HCC characterized by HBV infection.

Abstract: The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.

Abstract: The present disclosure provides a benzene fused heterocyclic derivative of Formula (I): is a single or double bond; n is an integer of 0 or 1; A is —CH2—, —CH(OH)—, or —C(O)—; G is C or N; X is —CH2—, O, or —C(O)—; Y is alkyl, aryl, or heterocyclic alkyl optionally substituted with at least one substituent independently selected from a group consisting of: H, halogen, alkyl, alkyl substituted with at least one halogen, aryl, aryl substituted with at least one halogen, —NRy1Ry2, —ORy1, —Ry1C(O)Ry3, —C(O)Ry1, —C(O)ORy2, —C(O)ORy2Ry3, —NRy1C(O)Ry2, —NRy1C(O)NRy2Ry3, —NRy1C(O)ORy2Ry3, —NRy1C(O)Ry2ORy3, C(O)NRy1(Ry2Ry3), —C(O)NRy1(Ry2ORy1), —ORy2Ry3, and —ORy2ORy3, wherein each of Ry1 and Ry2 is independently selected from a group consisting of H, oxygen, alkyl, and aryl, and Ry3 is aryl optionally substituted with at least one halogen; Z is —NRz1Rz2, —NRz1Rz3, —ORz1, —ORz1Rz3, —C(O)Rz1Rz3, —C(O)ORz1Rz3, —NRz1C(O)Rz2Rz3, —NRz1C(O)ORz2Rz3, —C(O)NRz1Rz3, or ORz2ORz3, wherein each of Rz1 and Rz2 is independently sel

Abstract: Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders associated with mast cells. Also provided are pharmaceutical compositions comprising the novel compounds of Formula I and methods for their use in treating one or more diseases and disorders associated with mast cells.

Abstract: Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific irreversible inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL irreversible inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL inter-action; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides an oral pharmaceutical composition and a usage thereof, comprising a pharmaceutically acceptable acidic medicinal auxiliary material whose surface is modified and dabigatran etexilate or pharmaceutically acceptable salts or aquo-complexes thereof. The present invention further provides a surface modification method for a medicinal auxiliary material.

Abstract: Described herein are pharmaceutical compositions including a proton pump inhibitor and an antiparasitic drug. In some embodiments, the compositions can be formulated as a non-solid for oral administration. The compositions can be used to treat gastrointestinal conditions. Methods of treatment using the compositions are also described.

Abstract: Compositions comprising a mixture of at least two types of particles wherein a) the first type of particles comprise dabigatran etexilate in the form of the free base or in the form of pharmaceutically acceptable salts, polymorphs, solvates or hydrates thereof; and b) the second type of particles comprise at least one pharmaceutically acceptable organic acid, use of said compositions in the reduction of the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation and/or in the prevention of venous thromboembolic events in adult patients who have undergone elective total hip replacement surgery or total knee replacement surgery and processes for the preparation of said compositions.

Abstract: The disclosure provides chemical compounds useful as activators of PKR. PKR activating compounds are useful in the treatment of disease and disorders associated with modulation of PKR and/or PKM2, such as pyruvate kinase deficiency (PKD).

Abstract: This disclosure relates to treatments for reducing the side effects associated with treatment of a medication or drug, such as a chemotherapy medication, being experienced by a patient. This may be accomplished by administering to a patient taking the medication, a buffered aqueous liquid having a pH of about 10 to about 11.5.

Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma-2 receptor activity.

Abstract: A pharmaceutical composition comprising dabigatran etexilate, and preparation method and use thereof, and solid preparation comprising the pharmaceutical composition; the pharmaceutical composition comprises a vitamin C layer and a dabigatran etexilate layer separated by a semipermeable film layer, and the semipermeable film layer comprises a water-soluble compound, a water-insoluble compound and an optional anti-sticking agent and/or plasticizer.

Abstract: In one aspect, the present disclosure provides epothilone analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.

Abstract: The present invention provides an oral pharmaceutical composition and a usage thereof, comprising a pharmaceutically acceptable acidic medicinal auxiliary material whose surface is modified and dabigatran etexilate or pharmaceutically acceptable salts or aquo-complexes thereof. The present invention further provides a surface modification method for a medicinal auxiliary material.

Abstract: The present invention provides a novel crystalline form of Lumacaftor, specifically Lumacaftor Form APO-I, a co-crystal of Lumacaftor and nicotinamide, compositions including this crystalline form, and processes for the preparation of this crystalline form.

Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving elevated levels of aldosterone or abnormal or excessive fibrosis, such as kidney disease and hypertension.

Abstract: The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.

Abstract: Disclosed herein is a compound of formula (I) and/or a pharmaceutically acceptable salt thereof that can serve as Erk inhibitors. They are potentially useful in the treatment of diseases treatable by inhibition of Erk, such as cancers. Also disclosed herein is a pharmaceutical composition, comprising a compound of formula I and/or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Abstract: An object of the invention is to provide a novel method for producing an indazole compound, by which an indazole compound can be produced without using a reaction reagent that exhibits strong toxicity, and a novel indazole compound. According to the invention, a method for producing an indazole compound, including obtaining an indazole compound or a salt thereof from a diazonium salt prepared from an aniline compound in the presence of a compound represented by the following General Formula (1), is provided. In the formula, R1 represents a hydrogen atom or an alkali metal; R2 represents a hydrogen atom, a hydroxyl group, or the like; and R3 represents a hydrogen atom, a C1-30 alkylcarbonyl group which may have a substituent, or a C6-20 arylcarbonyl group which may have a substituent.

Abstract: Provided are a compound represented by the following Formula I, or a solvate, stereoisomer, or pharmaceutically acceptable salt thereof, and a composition for preventing or treating hair loss, the compound including the compound as an active ingredient:

Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methypyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.

Abstract: Methods of measuring the activity of Factor D, the key driver in the activation of the alternative complement pathway, methods of determining the potency of Factor D inhibitors, and methods of screening for Factor D inhibitors are provided.

Abstract: Derivatives of 1,2,4-Triazolo-[3,4-b]-1,3,4-thiadiazoles according to formula (I), as set forth below: processes for production thereof, pharmaceutical compositions containing the same and the use thereof in treatment of cancer.

Abstract: The present disclosure provides amorphous lumacaftor, amorphous solid dispersions of lumacaftor, crystalline lumacaftor acetic acid solvate, crystalline lumacaftor ethyl acetate solvate, and processes for the preparation thereof. The lumacaftor forms disclosed herein may be useful for the preparation of oral dosage forms for treating cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases.

Abstract: Described herein are pharmaceutical compositions including a proton pump inhibitor and an antiparasitic drug. In some embodiments, the compositions can be formulated as a non-solid for oral administration. The compositions can be used to treat gastrointestinal conditions. Methods of treatment using the compositions are also described.

Abstract: Liquid antacid compositions containing citrus extract are disclosed. The liquid antacid compositions possess superior resistance to microbial attack.

Abstract: The present invention relates to tackifier compounds and methods of using the same. In various embodiments, the present invention provides a tackifier compound including independently substituted or unsubstituted fused rings A and B each independently chosen from (C5-C10)cycloalkyl and (C2-C10)heterocyclyl. Fused ring A is substituted with (R1)1-8 and fused ring B is substituted with —(OC(O)R?C(O)R2)1-8. At each occurrence R? is independently chosen from (C2-C10)alkanylene, (C2-C10)alkenylene, (C2-C10)alkynylene, C5-C20(arylene), and (C1-C20)heteroarylene, wherein R? is unsubstituted or substituted. At each occurrence R1 is independently selected from —OH, —OR3, and —OC(O)R?C(O)R2. At each occurrence R2 is independently chosen from —OH, —OR3, —NH2, —NHR3, and —NR32. At each occurrence R3 is independently chosen from (C1-C10)alkanyl, (C2-C10)alkenyl, (C2-C10)alkynyl, C5-C20(aryl), and (C1-C20)heteroaryl, wherein R3 is unsubstituted or substituted.

Abstract: Provided herein are compounds of formula (I) which are, inter alia, useful allosteric inhibitors of Hsp70. The compounds and methods provided are useful for the treatment of cancer, infectious and neurodegenerative diseases.

Abstract: The present invention relates to a crystal form of a substituted aminopyran compound, and a pharmaceutical composition, a preparation method and a use thereof in the preparation of a drug for treating type II diabetes. In particular, the present invention relates to a crystal form IV of a compound as shown by formula (I) and a pharmaceutical composition, a preparation method and a use thereof in the preparation of a drug for treating type II diabetes.

Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.