Abstract: The present disclosure provides compounds and pharmaceutically acceptable salt thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.

Abstract: This disclosure relates to topical lithium agents including inhalable lithium agents for treating a viral infection characterized by a cytokine storm in the respiratory tract of a subject such as a human. Topical lithium formulations can be used to mitigate such viral infections, including coronavirus infections.

Abstract: Embodiments of a spray-drying process for producing low aspect ratio particles of poly[(methyl methacrylate)-co-(methacrylic acid)] (PMMAMA) are disclosed. In some examples, at least 95% of PMMAMA-containing particles made by the process have an aspect ratio <10. The particles may further include an active ingredient and/or an excipient.

Abstract: Crosslinkers of an amide or thiocarbamate of 7-nitroindoline were prepared with at least two attached reactive groups for crosslinking capability. The photo-cleavability of the invented crosslinkers is based on the known photolysis behavior of N-acyl-7-nitroindolines, and the photolysis behavior of amides and thiocarbamates of 7-nitroindolines. These crosslinkers enable crosslinking of biopolymers, which can be reversed by illumination with light.

Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described.

Abstract: The present invention features improved methods of identifying patients having cancer (e.g., melanoma, adenocarcinoma, lung, cervical, liver or breast cancer) using biomarkers (e.g., PDE3A, SLFN12) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention (e.g., DNMDP, zardaverine, and anagrelide).

Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.

Abstract: Provided an agent for suppressing an odor of a polysulfide compound. This agent for suppressing an odor of a polysulfide compound comprises, as an active ingredient, at least one selected from the group consisting, butyl 2-methylbutanoate, ?-terpinene, dipentene, cis-4-heptenal, 1,4-cineol, trimethylhexyl aldehyde, and (+)-limonene oxide, wherein the polysulfide compound is represented by the following formula (I): R1—[S]n—R2 (I) (in the formula, R1 and R2 are the same or different, and each denote a linear-chain or branched-chain alkyl or alkenyl group having 1 to 6 carbon atoms, and n denotes an integer of 2 to 5).

Abstract: Methods for preventing feedlot bovine respiratory diseases employing an anti-inflammatory drug rupatadine are disclosed. Compositions are further disclosed. Beneficially, the methods and compositions provide safe and cost-effective management of a costly disease.

Abstract: The present invention provides compositions and methods of using transposons. In one aspect, methods are disclosed that are useful for identifying negatively selected genes in an insertional mutagenesis screen. In another aspect, compositions for reducing proliferation of a tumor cell expressing an oncogenic RAS include an activator of a WNT pathway. Pharmaceutical compositions for reducing proliferation of tumor cells in a subject in need thereof by administering an effective amount of an activator of a WNT pathway to the tumor cells of the subject are also disclosed.

Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described.

Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.

Abstract: The administration of a compound advantageously efficacious as ROS1 inhibitor and its effect on subjects with cancer includes administering a compound having certain structural components such as a quinoline moiety in the backbone and at least one tertiary amine containing moiety in a side chain as well as heteroatoms, in particular oxygen atoms, present in the backbone and the side chain for treating a subject suffering from a disease such as cancer. The presence of such structural components allows for an advantageous interaction with the ROS1 kinase domain, in particular with the hinge region. The administered compounds represent a highly promising opportunity in particular for patients bearing ROS1-dependent cancer. A method for targeting tumor cells harboring an abnormality in ROS1 gene includes contacting a cell with compounds of the present invention as well as pharmaceutical compositions comprising such compounds.

Abstract: The present invention relates to a pharmaceutical composition comprising propiverine, trospium or glycopyrrolate; and a non-anticholinergic antiemetic agent. It is also related to a pharmaceutical composition comprising a high dose of solifenacin or a pharmaceutically acceptable salts thereof; and a non-anticholinergic antiemetic agent. Pharmaceutical compositions containing high dose of nsPAChA for use for increasing the AChEI blood concentrations and for combating neurodegeneration are also described. The invention also relates to a method for inducing neuroprotection and combating neurodegeneration in a patient suffering from Alzheimer type dementia as well as to a method for increasing the blood levels of an acetyl choline esterase inhibitor (AChEI) in a human subject treated with an AChEI dose.

Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.

Abstract: This invention provides a method of treating lung cancer including administering a therapeutically effective amount of a compound of 0089-0022 formula I to a subject in need thereof. The compound activates pyruvate kinase M2 isoform (PKM2) to treat the lung cancer. In one example, the lung cancer is Non-Small Cell Lung Cancer (NSCLC).

Abstract: Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5 is H, optionally substituted alkyl, optionally substituted heterocycle, —C(?O)—R6, —C(?O)—O—R7, or —C(?O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH?CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.

Abstract: The present invention provides novel, rationally designed human control antibodies for use in various in vivo and in vitro applications. The antibodies of the present invention have well characterized variable domains that have been designed to minimize or eliminate antigen binding without altering gross antibody structure. Using the antibodies of the present invention in various assays allows researchers to distinguish effects that result from specific antigen-antibody interactions from other, non-specific antibody effects.

Abstract: This disclosure is directed to the use of sequentially applied topical therapy with a lower dosage strength imiquimod composition and photodynamic therapy for treating actinic keratosis, wherein the photodynamic therapy is administered subsequent to the topical therapy with the imiquimod composition. In some embodiments, the imiquimod composition comprises from about 1% (w/w) to about 4.25% (w/w) imiquimod.

Abstract: Provided herein are combination therapies for the treatment of progeroid diseases and conditions, cellular aging, bone diseases, and cardiovascular diseases. The provided combination therapies target the aberrant farnesylation of the mutant lamin A protein progerin, and inhibit farnesyl biosynthesis, lamin A prenylation, and increase progerin clearance.

Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described.

Abstract: An improved, high yielding process is disclosed for making bisglycidyl ether derivatives of isosorbide, isomannide and/or isoidide, wherein up to quantitative yields overall are demonstrated. In another related aspect, a process is disclosed for making novel monoallyl, monoglycidyl ether derivatives or a combination of monoallyl, monoglycidyl ether derivatives and bisglycidyl ether derivatives via the same diallyl isohexide intermediate.

Abstract: Disclosed are pharmaceutical compositions having a portion of aspirin for intraoral release and another aspirin for gastrointestinal release. The compositions can further include niacin. Methods of using such compositions to treat diseases or conditions suitably treated by niacin are also provided which result in reduced flushing.

Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.

Abstract: The present invention relates in general to the field of modulators of the innate immune system, particularly to pharmaceutical compositions comprising imidazoquinolin(amines) and derivatives thereof, preferably suitable for local administration, such as, intravesical administration. In addition, the present invention concerns the use of imidazoquinolin(amines) and derivatives thereof for intravesical treatment of bladder diseases, such as, for example, bladder cancer and cystitis. The present invention furthermore comprises methods of treatment for these diseases as well as methods of administration of the inventive pharmaceutical compositions.

Abstract: The present invention is in the fields of medicine, pharmaceuticals, nutraceuticals, endocrinology and cardiology. The invention provides compositions comprising a statin, an inhibitor of the angiotensin converting enzyme, an antiplatelet compound and an anti-hyperglycemic compound for use in the treatment and/or prevention of cardiometabolic risk factors of Metabolic Syndrome and treatment and/or prevention of Metabolic Syndrome. The present invention provides for the use of such compositions in the manufacture of products for treatment and/or prevention of Metabolic Syndrome. The biguanide metformin of the composition could be present in extended release form allowing its use together with the other drugs in a single dosage form at low dose. This combination of drugs in a single daily dosage greatly improves compliance and adherence to treatment which is a critical factor for treating patients with Metabolic Syndrome.

Abstract: Compositions, methods of making, and methods of using nanoclusters in which the nanoclusters comprise a plurality of nanoparticles having a core of nanoparticles arranged such that the surfaces of the nanoparticles contact adjacent nanoparticles, the nanoparticles comprise an active ingredient, and the nanocluster has a mass median aerodynamic diameter of from about 0.25 ?m to about 20 ?m.

Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.

Abstract: The invention provides compositions for the prevention and treatment of the symptoms of alcoholic beverage-induced hangover syndrome, related kits and methods of using the compositions and kits.

Abstract: The use of a dopamine agonist in the manufacture of a medicament for the treatment or prevention of endometriosis.

Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.

Abstract: The present invention is directed to novel compounds that are able to inhibit the interaction of paxillin or its paralogues, including leupaxin or Hic-5, with alpha.4 integrin or its binding partners that regulate signaling events downstream of the paxillin-.alpha.4 interaction. The present invention further relates to methods for therapeutic use of such compounds and pharmaceutical compositions of such compounds for the treatment of a disease or condition.

Abstract: A biocompatible plasticizer useful for forming a coating composition with a biocompatible polymer is provided. The coating composition may also include a biobeneficial polymer and/or a bioactive agent. The coating composition can form a coating on an implantable device. The implantable device can be used to treat or prevent a disorder such as atherosclerosis, thrombosis, restenosis, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, tumor obstruction, or combinations thereof.

Abstract: The use of a dopamine agonist in the manufacture of a medicament for the treatment or prevention of endometriosis.

Abstract: Disclosed is a compound of formula (I) and salts thereof. Also disclosed are methods of making the compound of formula (I) and the use of the compound as an intermediate for making pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors.

Abstract: The invention discloses a pharmaceutical composition comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is for oral administration wherein the composition delivers phenylephrine or a pharmaceutically acceptable salt thereof via absorption in the colon. The pharmaceutical composition comprises a core comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is in a time-dependent, pH-dependent, or colon-specific enzyme-dependent erodible layer that degrades to expose the core to release phenylephrine in the colon. In one preferred embodiment, the erodible layer encases the core. The composition optionally further comprises phenylephrine in the erodible layer or other additional layer(s).

Abstract: The invention relates to the areas of therapeutics, pharmaceuticals, drug discovery, and immunotherapy. More specifically, the present invention relates to methods of stimulating the immune system through the administration of flavone acetic acid [FAA] analogs, and in particular, the flavone acetic acid analog, 5,6-dimethylxanthenone-4-acetic acid (DMXAA) so as to comprise an antimicrobial therapeutic agent for the treatment of viral infections of DNA and RNA viruses in humans and non-human animals. The invention is especially suitable for use in a process of treating and preventing infection by, for example, rhinoviruses, enteroviruses, and influenza viruses.

Abstract: The subject invention is directed to a pharmaceutical composition comprising an open matrix network carrying a pharmaceutically active ingredient, wherein the open matrix network comprises both the polysaccharides levan and inulin.

Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.

Abstract: The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

Abstract: The subject invention is directed to a pharmaceutical composition comprising an open matrix network carrying a pharmaceutically active ingredient, wherein the open matrix network comprises levan.

Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.

Abstract: The present invention provides therapeutic combinations that include an immune response modifier (IRM) component and an anti-inflammatory component. The inventions further provide methods of treating a condition by administering to one having the condition a therapeutic combination that includes an IRM component and an anti-inflammatory component.

Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.

Abstract: The present invention generally relates to compositions containing chemical compounds and compositions and pharmaceutical formulations of the compounds which increase the expression of total hemoglobin or globin protein such as embryonic or fetal globin, or the proliferation of hemoglobin expressing and other blood cells. These compositions can be used to treat or prevent the symptoms associated with anemia, sickle cell diseases, thalassemia, and other blood cell deficiencies and blood disorders. The invention also relates to methods for administering these compositions to subjects and for use as medical aids for the treatment and prevention of blood and other disorders.

Abstract: Although it can be farnesylated, the mutant lamin A protein expressed in Hutchinson Gilford Progeria Syndrome (HGPS) cannot be defarnesylated because the characteristic mutation causes deletion of a cleavage site necessary for binding the protease ZMPSTE24 and effecting defarnesylation. The result is an aberrant farnesylated protein (called “progerin”) that alters normal lamin A function as a dominant negative, as well as assuming its own aberrant function through its association with the nuclear membrane. The retention of farnesylation, and potentially other abnormal properties of progerin and other abnormal lamin gene protein products, produces disease. Farnesyltransferase inhibitors (FTIs) (both direct effectors and indirect inhibitors) will inhibit the formation of progerin, cause a decrease in lamin A protein, and/or an increase prelamin A protein. Decreasing the amount of aberrant protein improves cellular effects caused by and progerin expression.

Abstract: Disclosed is the use of rupatadine in the manufacture of pharmaceutical composition for preventing or treating chronic obstructive bronchitis, obstructive emphysema or chronic obstructive pulmonary disease. The new medicament, i.e. rupatadine, for treating chronic obstructive pulmonary disease is obvious in therapeutic effects, and low in toxic and side effects, and safe in use in the aspects of treating chronic obstructive bronchitis, obstructive emphysema or chronic obstructive pulmonary disease.

Abstract: A stable ternary solid dispersion composition with enhanced physical stability and/or bioavailability comprising: (a) about 1% wt. to about 50% wt. of one or more poorly soluble active pharmaceutical ingredient (API) which belongs to Biopharmaceutics Classification System (BCS) class II and/or IV; (b) about 11% wt. to about 50% wt. of at least one water-soluble polymer; and (c) about 20% wt. to about 99% wt. of crosslinked polyvinylpyrrolidone (crospovidone, a water-insoluble polymer). The solid dispersion is capable of inhibiting crystallization of API in solid state and/or aqueous gastrointestinal tract (GIT) medium. Also disclosed is a method of preparation of such solid dispersion composition by fusion or solvent or fusion-solvent method.

Abstract: The use of a dopamine agonist in the manufacture of a medicament for the treatment or prevention of endometriosis.

Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.