Abstract: The present invention relates to a stable ready to use and powder for oral suspension dosage forms of Lamotrigine and its pharmaceutically acceptable salts and process of preparing such compositions. The liquid and powder for oral suspension dosage forms of Lamotrigine have been previously known only as extemporaneous preparations. Present invention relates to manufacture of liquid and powder for oral suspension dosage forms of Lamotrigine having improved physico-chemical properties with desired technical attributes. The prepared dosage forms are useful in patients having difficulties in swallowing tablets and provide physician with more options for dose titration.

Abstract: The present invention provides methods for reducing loss of muscle strength, muscle mass, or Type I muscle fibers in an immobilized limb by administering (E)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

Abstract: The invention provides a compound of formula 1 or a pharmaceutically-acceptable salt thereof, that is useful as a JAK inhibitor. The invention also provides crystalline forms of the compound, pharmaceutical compositions comprising the compound, methods of using the compound to treat diseases amenable to a JAK inhibitor, and processes and intermediates useful for preparing the compound.

Abstract: Described herein, to overcome the limitations of conventional antibiotics, antibiotics have been encapsulated in biocompatible particles manufactured using Particle Replication In Non-wetting Templates (PRINT). These PRINT antibiotic particles were assessed as a topical agent to prevent E. coli infection using in vitro and in vivo models relevant to UTI and neurogenic bladder. The results show a prolonged efficacy and wide distribution in the bladder, resulting in a prophylactic environment in the bladder. The subject matter described herein is directed to molded particles containing an antibiotic active agent and methods of treating diseases and conditions with the particles, and methods of preparing the particles and compositions comprising the particles.

Abstract: Disclosed herein are methods of treating cancers by administration of a PAR-4 agonist.

Abstract: Method and composition for treating eating disorders in humans and veterinary animals by administering a composition including: (i) mirtazapine, (ii) a cannabis compound and (iii) a fat-soluble vitamin.

Abstract: A compound of formula (I) as defined herein, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Abstract: ?-Lactamase inhibiting compounds, therapeutic methods of using the f-lactamase inhibiting compounds, particularly in combination with ?-lactam antibiotics and pharmaceutical compositions thereof are disclosed. The ?-lactamase inhibiting compounds are suitable for oral administration.

Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I): wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R1, R1a, R2, R2a, R3, R3a, X, X1, X2, X3 have the meaning as indicated in the description and the claims and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer, and Z is a carrier group. The invention also relates to A-L, wherein A is a leaving group, pharmaceutical composition comprising said prodrugs and their use as medicaments.

Abstract: Provided are methods for the combined use of cyclin-dependent kinase 9 (CDK9) inhibitors and bromodomain containing 4 (BRD4) inhibitors to reduce, inhibit and/or prevent cartilage degradation and systemic traumatic inflammation. A combination of CDK9 inhibitors and BRD4 inhibitors can be used to reduce, inhibit and/or prevent cartilage degradation and loss of cartilage viability during allograft storage. A combination of CDK9 inhibitors and BRD4 inhibitors can be used as a post-injury intervention treatment to reduce, inhibit and/or prevent the acute cellular responses that lead to future cartilage degradation and osteoarthritis.

Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent the presence or absence of a double bond which can be in the cis or trans configuration and A, B, Z, X, R1 and R2 are as defined in the specification and a penetration enhancer. Such compositions are used in stimulating hair growth of human or non-human animals.

Abstract: The present invention relates to a composition for preventing, improving or treating drug-induced nephrotoxicity, the composition comprising oleanolic acid acetate as an active ingredient. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating drug-induced nephrotoxicity comprising oleanolic acid acetate or a pharmaceutically acceptable salt thereof as an active ingredient, a health functional food for preventing or improving drug-induced nephrotoxicity comprising the active ingredients, and an anticancer adjuvant comprising the active ingredients. The oleanolic acid acetate of the present invention is derived from a natural product and has no side effects and no cytotoxicity and has excellent effects of preventing, improving and treating nephrotoxicity caused by a drug, particularly a platinum-based anticancer drug, so that it can be utilized as a pharmaceutical composition, a health functional food, and a cancer adjuvant thereof.

Abstract: Described are combined oral contraceptive compositions with reduced cardiovascular effects and methods using them. In some embodiments, the methods relate to contraceptive methods or methods for treating dysmenorrhea with reduced cardiovascular effects, such as reduced venous thromboembolism (VTE) risk. The methods comprise administering to a female subject an effective amount of an estetrol component and a progestogenic component. The methods enjoy a favourable profile for thromboembolism compared to currently available methods which employs contraceptives from the so-called second, third or fourth generation.

Abstract: Methods for treating high risk HPV infection by inhibiting one or more phases of HPV replication cycle with antiviral compounds are disclosed. Moreover, a mechanism for the inhibition is suggested and targets for further antiviral compounds are disclosed.

Abstract: Disclosed are bioavailable solid state (17-?)-Hydroxy-4-Androsten-3-one esters suitable for pharmaceutical uses and administration to mammals in need of (17-?)-Hydroxy-4-Androsten-3-one.

Abstract: A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.

Abstract: A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.

Abstract: The present disclosure is directed to generally methods and/or compositions for treating mammographic breast density and/or breast stiffness in a patient in need thereof, such as a pre-menopausal, a peri-menopausal or a post-memopausal patient, comprising the administration of an effective amount of androgenic agent and an effective amount of an aromatase inhibitor. The present disclosure is also directed to methods and/or compositions for reducing breast pain. The present disclosure is also directed to method and/or compositions for reduing elasticity and/or decreasing mechano-transduction on the genome of breast cells. The present disclosure is also directed to methods and/or compositions for stabilizing and/or increasing the levels of androgen receptor expression in breast tissue.

Abstract: The disclosure relates to obeticholic acid formulations with improved stability, dissolution, and/or solubility, methods of preparing the same for use and methods of treating various diseases and conditions.

Abstract: The disclosure relates to obeticholic acid formulations with improved stability, dissolution, and/or solubility, methods of preparing the same for use and methods of treating various diseases and conditions.

Abstract: Provided herein are methods for treating proliferative diseases, such as cancer, via novel priming-eligible targets; and compositions therefor.

Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.

Abstract: Provided herein is a topical composition and related methods for making and using the composition. In a first aspect, the topical composition comprises minocycline, a magnesium salt, and a sulfite compound in a non-aqueous solvent. In yet another aspect, the topical composition comprises a tetracycline-class drug, a source of magnesium, a monohydric aliphatic alcohol, and a polyol, wherein (i) the ratio between the monohydric aliphatic alcohol and the propylene glycol is in the range of 1:1 to 99:1 by weight and (ii) the tetracycline-class drug is dissolved in the topical composition.

Abstract: The present disclosure relates to inhibitors of mitochondrial function. Methods of treating hypoxic cancer cells using anti-angiogenic agents and mitochondrial biogenesis inhibitors are disclosed. Tetracyclines, such as doxycycline, may serve as mitochondrial biogenesis inhibitors. Also described are methods of sensitizing hypoxic cancer cells to one or more chemotherapies by administering a mitochondrial biogenesis inhibitor with the chemotherapy.

Abstract: The invention provides methods and compositions for inhibiting CD38 activity, and methods of treating or preventing various disorders associated with CD38 activity.

Abstract: The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Abstract: This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

Abstract: Compositions involving a modified egg yolk extract for use as an effective anti-cancer agent are described. The modified egg yolk extract involves specific fractions of phosphatidylcholines and sphingomyelins modified and produced from a chemical synthesis applied to the extract that produce a beneficial effect on the inhibition of cancerous cell growth. Methods of administering these compositions are also described.

Abstract: Methods of treating anti-inflammatory conditions through the use of boron-containing small molecules are disclosed.

Abstract: The invention generally relates to anti-aging compositions and methods for using the anti-aging compositions. In one aspect, the invention provides a method for preventing cellular aging in a cell of a subject, the method comprising the step of providing to the cell an effective amount of at least one lithium compound or a pharmaceutically acceptable salt thereof, and an effective amount of at least one glycyrrhizie triterpenoid compound or a pharmaceutically acceptable salt thereof, thereby preventing the cell from aging. 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.

Abstract: Methods are disclosed for treating a subject with a vascular or cardiac disorder associated with oxidative stress. Methods are disclosed for treating a subject with GNE myopathy that has impaired cardiac function. These methods include administering to the subject a therapeutically effective amount of a sialic acid precursor, sialic acid, or one or more sialylated compounds, mannosamine, N-acetyl mannosamine or a derivative thereof. In other embodiments, methods are disclosed for detecting a disorder associated with oxidative stress.

Abstract: Use of albiflorin or a pharmaceutically acceptable salt thereof in the preparation of a product for regulating and improving the balance of human intestinal flora. Albiflorin or a pharmaceutically acceptable salt thereof, as a regulator for improving the function of intestinal flora system, can be used in the preparation of a medicament, a health care product, a food, a food additive, or a nutritional supplement that ameliorates and treats a sub-health status and/or a disease caused by intestinal flora disturbance; the sub-health status is selected from intestinal system dysfunction and/or affective disorder; and the disease is selected from one or more of irritable bowel syndrome, depression, anxiety, colitis, and colon cancer.

Abstract: This application describes compounds, compositions, and combinations thereof that can be used to treat cancer, such as cancers with and without BRAF and/or RAS mutations.

Abstract: When using a pharmaceutical composition for preventing or treating malignant hyperthermia, containing NAADP antagonists, of the present invention, malignant hyperthermia can be effectively prevented or treated through the inhibition of an oxygen consumption rate abnormal increase, which is associated with a ryanodine receptor (RYR) of skeletal muscles. In addition, the present invention can be used even after the onset of malignant hyperthermia and can inhibit an oxygen consumption rate abnormal increase even at concentrations lower than those of conventional agents for treating malignant hyperthermia, thereby enabling conventional agents for treating malignant hyperthermia to be replaced, and can be stably used, thereby being effectively usable in relevant industries.

Abstract: The present invention relates to compounds and methods of use thereof for treatment of certain disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries.

Abstract: Materials, formulations, production methods, and methods for delivery of CFTR mRNA for induction of CFTR expression, including in the mammalian lung are provided. The present invention is particularly useful for treating cystic fibrosis.

Abstract: The present invention relates to a composition for nucleus-independent, sustained inhibition of gene expression, comprising an mRNA fragment of T7 RNA polymerase, plasmid DNA for self-amplification of the T7 RNA polymerase, and a DNA fragment encoding a gene expression inhibitor; a transporter of the gene expression inhibitor comprising the composition; and a method of preparing the transporter. The composition of the present invention and the liposome transporter of the present invention comprising the composition can improve the expression of shRNA in the cytoplasm through self-amplification of nucleus-independent, sustained self-amplification of T7 RNA polymerase, and deliver them in a cancer tissue-specific manner. Therefore, the composition and the liposome transporter of the present invention can be utilized for use in treating chronic diseases that require reduced frequency of administration and long-term inhibition of gene expression.

Abstract: This disclosure relates to compositions including formulated sucralfate or other aluminum-crosslinked sulfated agents for delivery of agents to biological surfaces and/or the modulation of nutrient absorption through the intestinal lining as well as methods for the manufacture of and the use of these compositions for treating disorders including diabetes type II and clinical obesity that require a modulation of certain nutrients to the body.

Abstract: The invention relates to a method for the preparation of a polymer hydrogel, comprising cross-linking a precursor comprising a hydrophilic polymer optionally in combination with a second hydrophilic polymer, using a polycarboxylic acid as the cross-linking agent. The invention further concerns the polymer hydrogel obtainable by the method of the invention and the use thereof in a number of different applications.

Abstract: Disclosed herein are fully synthetic polymer-based lung surfactant materials, for the first time, as next generation SRT. In vitro studies on these polymer lung surfactants show that the candidate materials effectively mimic the surface tension controlling properties of currently marketed natural lung surfactants. Further, the polymer lung surfactants have strong protein resistance, which makes this class of materials promising also for potential use in Acute Respiratory Distress Syndrome (ARDS) treatment.

Abstract: The invention relates to a population of pellets, each pellet comprising cholestyramine and at least about 5% w/w of an acrylate copolymer. The invention also relates to an oral formulation for targeted delivery of cholestyramine to the colon, comprising a plurality of cholestyramine pellets and wherein said pellets are coated with a colon release coating. The invention also relates to the use of this formulation in the treatment of bile acid malabsorption.

Abstract: The invention relates to an oral formulation for targeted delivery of cholestyramine to the colon, comprising a plurality of cholestyramine pellets that are coated with a diffusion-controlled inner coating and an enteric outer coating. The invention also relates to the use of this formulation in the treatment of bile acid malabsorption.

Abstract: In exemplary embodiments, the disclosure provides a Colesevelam Colon Specific Drug Delivery System for use in treatment of, for example, cholestasis and/or cholestatic pruritus.

Abstract: Disclosed herein are polymers containing repeating units of formula (I) or copolymers containing the repeating units of formula (I) and (II), where R1 to R12, m, n, p, q, x and y are as defined herein. The polymers and copolymers have an antimicrobial effect and may be used therapeutically or in formulations intended for use as detergents.

Abstract: The disclosure relates to compositions and methods for delivery of magnesium. In one embodiment, the disclosure relates to a composition comprising a first plant based source of magnesium and a second plant based source of magnesium.

Abstract: The present invention relates to a suspension comprising smectite, and the suspension of the present invention comprises both a polymeric suspending agent and a low molecular suspending agent, and thus exhibits high dispersibility and sinking rate, ease of administration due to not high viscosity of a formulation, enhanced drug compliance while taking the formulation, and high preference. In addition, the suspension of the present invention enables uniform dispersion in preparation thereof, thus exhibiting ease of preparation and excellent efficiency, and accordingly, has an excellent effect on reducing a defect rate in the production of a suspension preparation.

Abstract: An application of a GSK3 inhibitor in preparation of a drug for treating Niemann-Pick disease type C. The GSK3 inhibitor can significantly improve the self-renewal and differentiation capacities of NPC1 KD or NPC1 KO hematopoietic and neural stem cells.

Abstract: Preparation of high-performance antimicrobial agent based on ZnO/GQD-PEI nanocomposites. Nano ZnO is regarded as the effective antibacterial agents because of its distinctive photocatalytic properties. However, the fast recombination of photo-generated electrons and holes on the surface of ZnO seriously affects antibacterial activities. Therefore, numerous methods such as controlling the size and morphology of ZnO, doping metal and nonmetal ions, coupling semiconductor, constructing heterojunction and surface modification have been used to increase the activity of ZnO. The application aims to synthesize a stable low-dimensional ZnO/GQD aqueous with excellent dispersity and enhanced absorption to further improve its antibacterial activities. Hence, amphiphilic polyethylenimine-functionalized graphene quantum dots (GQD-PEI) was prepared firstly, which was then used to transfer ZnO NPs to water to obtain water-soluble ZnO/GQD-PEI nanocomposites.

Abstract: There are disclosed topical silver(II) antibiotic formulations. Other embodiments are also disclosed.