Abstract: The present invention is directed towards a process for the preparation of Cariprazine (Ia) or a pharmaceutically acceptable salt thereof, wherein, N,N-dimethyl-1H-imidazole-1-carboxamide alkyl halide (VII) is reacted with trans-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexanamine or a salt thereof (IIa) to produce Cariprazine (Ia) or a pharmaceutically acceptable salt thereof. The present invention is also directed towards amorphous form of Cariprazine hydrochloride (I) and solid dispersion of Cariprazine hydrochloride (I), and its preparation thereof.

Abstract: Disclosed herein are diketopiperazine microparticles having a specific surface area of less than about 67 m2/g. The diketopiperazine microparticle can be fumaryl diketopiperazine and can comprise a drug such as insulin.

Abstract: The present invention concerns methods for treating a proliferation disorder, such as prostate cancer, basal cell carcinoma, lung cancer, and other cancers, using an inhibitor of the Hedgehog pathway (HhP); and methods for monitoring subjects undergoing such treatments based on biomarkers and other criteria predictive of efficacy.

Abstract: The invention relates to prolyl endopeptidase (PREP) inhibitors which contain a condensed 2,4-dihydro-3H-1,2,4-triazol-3-one ring system, methods for producing same, the use thereof alone or in combinations for treating and/or preventing diseases, and the use thereof for producing drugs for treating and/or preventing diseases, in particular for treating and/or preventing inflammatory lung diseases (COPD).

Abstract: The present invention relates to metallo-?-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein RA, R1, and Z are as defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.

Abstract: The disclosure provides new transmucosal and subcutaneous pharmaceutical compositions comprising 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or 1-(4-fluoro-phenyl)-4-((6bR,10aS)-2,2-d2-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or comprising -(4-fluoro-phenyl)-4-((6bR,10aS)-1,1,2,2-d4-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, in free base, co-crystal or salt form, together with methods of making and using them.

Abstract: Provided herein are methods for treating cholestasis in a subject having a liver disease. The method includes administering to the subject an Apical Sodium-dependent Bile Acid Transporter (ASBTI). More specifically, the present invention relates to methods for treating cholestasis in a subject where the method includes administering an ASBTI to a subject at a dose of at least 10 ?g/kg/day.

Abstract: Described herein are certain dosing schedules and amounts that effectively prevent and manage side effects associated with histone deacetylase inhibitor (HDACi) treatment. Optionally, these schedules and dosing regimens include treatment with an antiviral agent.

Abstract: The compositions and methods of the invention provide compositions and methods for preferential targeting of tissues to delivery therapeutic or diagnostic agents. For example, such compounds are useful in the treatment of joint disorders those affecting articulating joints, e.g., injury-induced osteoarthritis as well as autoimmune diseases affecting joint tissue such as rheumatoid arthritis.

Abstract: The invention provides a pharmaceutical composition for treating disease in a patient and inhibition of PI3K activity. The pharmaceutical composition includes an effective amount of Palbociclib and a pharmaceutically acceptable carrier. The invention further provides a pharmaceutical composition for use in the treatment of a disease in a patient. The application of the pharmaceutical composition of the present invention and use thereof are advantageous for inhibiting of PI3K activity and thus treating a disease.

Abstract: The present invention relates to 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one for use in the treatment of spinal muscular atrophy (SMA), its pharmaceutical composition to be used in the treatment of SMA, its methods of treatment thereof.

Abstract: The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.

Abstract: The present invention relates to an oral liquid suspension that includes lamotrigine and methods of medical treatment that include administering the oral liquid suspension. The oral liquid suspension has desirable physicochemical properties and technical attributes. The oral liquid suspension is useful in patients having difficulties in swallowing tablets and provide medical practitioners with additional options for dose titration.

Abstract: A method for treating neurodegenerative disease in a subject in need thereof by administering to the subject an effective amount of a Nedd4 activator as described herein.

Abstract: The present invention covers an ATR kinase inhibitor, particularly 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(H-pyrazol-5-yl)-1,7-naphthyridine (“Compound A”), for use in the treatment of a hyper-proliferative disease in a subject, wherein the hyper-proliferative disease or the subject is or has been characterized by one or more biomarker(s), wherein the biomarker(s) comprise(s) a) one or more functional mutations in one or more gene(s)/protein(s) selected from RBBP8, APOBEC3A, APOBEC3B, CLSPN, ERCC, HUS1, MAD2L2, PGBD5, POLD1, RAD1, TIMELESS and/or TIPIN; and/or b) the expression of a fusion gene encoding a fusion protein selected from EWSR-ERG, EWSR1-FLI1, SS18-SSX and/or SS18-SSX2 gene/protein.

Abstract: The present invention provides a preparation that is minimally colored through irradiation with light by coating a preparation containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a crystal thereof with a light stabilizing substance and a polymer, particularly with one or more of titanium oxide and talc used as the light stabilizing substance and hypromellose used as the polymer.

Abstract: The application relates to a pharmaceutical combination of an allosteric EGFR inhibitor of Formula Ia or Ib: (Ia) or (Ib), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and an ATP-competitive EGFR inhibitor of Formula I?: (I?), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the combination, and a method of treating or preventing a disease in which EGFR plays a role.

Abstract: The present invention relates to methods of treating hypogonadism in a male subject through administering intranasally to the male subject an intranasal testosterone bio-adhesive gel formulation to deliver a therapeutically effective amount of testosterone. In particular, the testosterone therapy of the invention remains effective if an allergic rhinitis event occurs in the male during the treatment or when the male subject uses a topical nasal vasoconstrictor or a topical intranasal decongestant during the hypogonadism treatment. Further, the present invention relates to a method of preventing the occurrence of an allergic rhinitis event in a male, who is undergoing a hypogonadism treatment with an intranasal testosterone bio-adhesive gel. In certain embodiments, the intranasal testosterone bio-adhesive gel formulation according to the invention comprises 4.0% and 4.5% testosterone.

Abstract: By initially lowering the SHBG with a synthetic androgen and, thereafter, raising the testosterone level in a person's body, an effective method for treating gastrointestinal disorders such as irritable bowel syndrome, inflammatory bowel diseases, including Crohn's Disease and ulcerative colitis, is achieved by first using a synthetic anabolic steroid and, thereafter, a natural androgen.

Abstract: Hormone Injectable Formulations for controlling the estrous cycle in mammals, triggering puberty and improving pregnancy in mammals, including a hormone, a Sucrose polymer, organic solvents, vegetable oils, oxyethylene polymers and excipients, where the formulation forms porous microspheres when in contact with a water-based liquid medium, and where the formulation is a single-phase clear liquid. The hormone can be Progesterone or its derivatives, alone or in combination with Estradiol.

Abstract: The present invention relates to a gallstone solubilizing agent, comprising ursodeoxycholic acid (UDCA) or a pharmaceutically acceptable salt thereof; omega-3 fatty acid; and an excipient, the gallstone solubilizing agent resulting in a process which prevents cholesterol gallstones from being formed or causes cholesterol gallstones to be dissolved, a pharmaceutical composition comprising the same, and a health functional food composition comprising the same. A pharmaceutical composition prepared to have UDCA and omega-3 fatty acid at an optimal content ratio allows cholesterol to remain in a dissolved state without forming crystals, and thus results in a process which prevents cholesterol gallstones from being formed or causes cholesterol gallstones to be dissolved, thereby exhibiting increased effects of preventing or treating cholesterol gallstones.

Abstract: Amorphous forms of onapristone and methods of making such amorphous forms are provided. Amorphous forms can be characterized by their X-ray powder diffraction patterns and other properties.

Abstract: The present invention relates to the use of SHIP1 inhibitors and pan-SHIP1/2 inhibitors in various methods, including, without limitation: (i) a method to treat obesity or reduce body fat of an obese subject; (ii) a method to limit bone development in a subject suffering from an osteopetrotic or sclerotic disease; (iii) a method to treat or prevent diabetes; (iv) a method to reduce glucose intolerance or insulin resistance; and (v) a method to lower cholesterol.

Abstract: Provided is a method of forming a copper-containing complex, including contacting a sample containing copper with a compound of Formula I: wherein R is —OH or —O—CH3. Also provided is a method of inhibiting enzymatic activity of a kinase in a sample, including contacting the sample with a compound of Formula I. Further provided is a method of administering to a subject a pharmaceutical composition including a compound of Formula I optionally complexed with copper. Also provided is a pharmaceutical composition including copper complexed with a compound of Formula I.

Abstract: The invention provides a compound of formula (I): or a salt thereof, wherein R1, R2, R3, R4 and R6 have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are agonists of the TGR5 receptor.

Abstract: Tri-phenyl-phosphonium (TPP) is a non-toxic chemical moiety that functionally behaves as a mitochondrial targeting signaling in living cells. TPP-related compounds may be utilized to target mitochondria in cancer stem cells (CSCs), and may be used for treating and/or preventing tumor recurrence, metastasis, drug resistance, and/or radiotherapy resistance, as well as for anti-cancer therapies. Various TPP-related compounds validated for oxygen consumption inhibition (OCR), were non-toxic, and had little or no effect on ATP production in normal human fibroblasts. Yet these compounds selectively target adherent “bulk” cancer cells. These compounds also inhibit the propagation of CSCs in suspension. TPP-related compounds provide a novel chemical strategy for effectively targeting both i) “bulk” cancer cells and ii) CSCs, while specifically minimizing or avoiding off-target side-effects in normal cells, among other useful therapies.

Abstract: The present invention provides pharmaceutical compounds for the treatment of high-grade superficial bladder cancer in patent in need thereof. Further described are compositions of azolium salts for use in such treatment.

Abstract: A nutraceutical and/or pharmaceutical composition designed to stimulate the production of type 2 beta-defensins. The composition includes as a sole active ingredient a gluco-oligosaccharide presenting the following basic oligomeric structure: for the treatment of intestinal inflammations in the quantity of 0.5 to 10 g. Application to the treatment of functional colopathy.

Abstract: Disclosed are an anticancer composition comprising an alginate oligosaccharide as an active ingredient and, more specifically, an anticancer composition and an anticancer adjuvant each comprising, as an active ingredient, a mannuronate and guluronate mixed alginate oligosaccharide (AOS) having a higher proportion of mannuronate among alginate oligosaccharides, and a method for preventing or treating cancer by using the composition.

Abstract: The present invention relates to a use of an agarobiose or agarooligosaccharides having anticariogenic activity. More specifically, a lower concentration of agarobiose or agarooligosaccharides than the concentration of xylitol suppresses the growth of Streptococcus mutans and suppresses acid production, and thus can be used for anti-cariogenic purposes.

Abstract: Described herein are methods and compositions for intracellular delivery of therapeutic molecules. Disclosed herein are selective delivery conjugate comprising a targeting ligand conjugated to a selective delivery molecule (a) an acidic sequence (portion of A) which is effective to inhibit or prevent the uptake into cells or tissue retention, (b) a molecular transport or retention sequence (portion of B), and (c) a linker between portion of A and portion of B, and (d) at least one cargo moiety. Also, described are selective delivery molecules comprising a second linker comprising an intracellular cleavage site and optionally a self-immolative cleavage site.

Abstract: Provided are methods of treating feline Coronavirus infections comprising administering a therapeutically effective amount of a compound of Compound 1 to Compound 9, or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to methods for modulation of the gut flora and/or for supporting immune system function in animals comprising administration of one or more sophorolipids to an animal in need thereof. Animal feed compositions comprising sophorolipids are also provided.

Abstract: The present invention discloses a pharmaceutical use of argininyl fructosy glucose (AFG), and belongs to the field of research and development of pharmaceutical products. The pharmaceutical use refers to application of the AFG as an active ingredient in preparation of a drug for treating or preventing an acute hepatic failure disease (AHFD). The AHFD is an oxidative stress injury caused by use of a combination of lipopolysaccharide (LPS) and D-galactosamine (D-GalN), and the drug is used for protecting liver cells from injuries, and reducing apoptosis caused by LPS/D-GalN. The purity of the AFG is 80%-99.99%. The present invention proposes the use of the AFG in prevention or treatment of the acute hepatic failure for the first time, which provides a new raw material for the preparation of the drug for the acute hepatic failure, and also provides a new method for the prevention and treatment of the acute liver failure.

Abstract: An amorphous form of ertugliflozin and process for its preparation is described. A solid form of ertugliflozin and process for preparation thereof is also described.

Abstract: Disclosed herein are compounds, compositions and methods for modulating splicing of SMN2 mRNA in a subject. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders, including spinal muscular atrophy.

Abstract: Provided herein are double-stranded, chemically-modified oligonucleotide mimetics of miR-29 for use in treating ocular diseases or disorders associated with ocular fibrosis, and ocular fibrotic conditions.

Abstract: The invention relates to saRNA targeting a C/EBP? transcript and therapeutic compositions comprising said saRNA. Methods of using the therapeutic compositions are also provided.

Abstract: Provided herein are an isolated Imperata cylindrica polysaccharide and use thereof in the manufacture of a medicament for treating hyperlipoidemia. The Imperata cylindrica polysaccharide comprises L-arabinose, D-xylose, D-mannose, D-glucose and D-galactose, wherein the molar ratio of the L-arabinose:D-xylose:D-mannose:D-glucose:D-galactose is 1-20:1-15:1-15:15-40:25-60.

Abstract: Methods and compositions are provided for oligonucleotides that bind targets of interest. The targets include circulating biomarkers such as micro vesicles, including those derived from various diseases.

Abstract: A decolonization drug, a preparation method thereof and an application thereof. The decolonization drug is non-antibiotic, simple and convenient to use, and can be used systemically, and has more types of sterilization; The decolonization drug involved in the invention contains added special components, which can improve the bactericidal performance of the drug through the activator effect; The decolonization drug is suitable for use in adults and sensitive populations, including the elderly, pregnant women, infants, children, etc.; especially as a mucosal drug for nasal mucosa, oral mucosa, ocular mucosa, abdominal mucosa, genital mucosa, etc., and can also be used as a bactericidal drug in other medical fields, including diabetic foot, burns, surgical site infections (SSIs), etc.

Abstract: An object is to provide an external composition for skin capable of easily enhancing body balance ability even for ordinary people such as housewives, students, middle-aged and mature-aged males and females, and elderly persons who do not aggressively exercise on a routine basis other than athletes. The object has been solved by an external composition for skin including a rhodochrosite extract extracted from rhodochrosite with water, a hematite extract extracted from hematite with water, a smithsonite extract extracted from smithsonite with water, and an olivine extract extracted from olivine with water, and the like.

Abstract: Novel dinuclear silver(I) pyrazolido complexes and methods of synthesizing them are provided. Advantageously, the novel silver(I) pyrazolido complexes have excellent antimicrobial activity and methods of using said complexes to treat bacterial, fungal, and viral infections are also provided.

Abstract: The present invention provides methods of improve efficiency, growth, and performance in an animal by orally administering to the animal an effective amount of a therapeutic clay. The methods can reduce embryonic loss, increase litter size, increase the number of live births, improve the immune status of the maternal animal, reduce the concentration of maternal fecal amino acids, reduce the concentration of maternal fecal short-chained amino acid, increasing litter birth weight in the maternal animal, increase the amount of young animal colostrum intake, reduce young animal pre-weaning mortality, reduce the number of young animals lost due to low viability, reduce the number of weaned young animals, improve the immune status of young animals at weaning, reduce the number of lightweight young animals from nursery to market, increase the number of young animals marketed per sow, and increase calculated litter weight gain.

Abstract: Methods for the reversal of hemorrhagic shock or hemorrhagic trauma.

Abstract: The disclosure provides for compounds, compositions, and methods of use thereof for treating diabetes (e.g., type 2 diabetes). In another aspect, one or more proteins described herein or compositions containing one or more proteins described herein are provided for. In yet another aspect, compounds, compositions, and methods containing one or more proteins described herein are used for treating a disorder in a patient in need thereof, such as type 2 diabetes.

Abstract: A medicament for cancer treatment includes as an active ingredient T cells having a chimeric antigen receptor that binds to glypican 1 (GPC1). The medicament is administered concomitantly with an immune checkpoint inhibitor according to regimens (a) and (b) to maintain the anti-tumor activity of the T cells: The regimens include (a) administering an effective amount of the T cells to a cancer patient and (b) continuously administering 0.01 mg/kg body weight to 100 mg/kg body weight of the immune checkpoint inhibitor per dose to the cancer patient every 1 to 5 weeks.

Abstract: The invention provides a chimeric antigen receptor (CAR) which can specifically bind to a BCMA protein comprising a BCMA binding structural domain, a transmembrane domain, a co-stimulatory domain, and an intracellular signaling domain. The invention also provides uses of the CAR in treating diseases or conditions linked to the expression of BCMA.

Abstract: A vector containing a first nucleotide sequence S1 encoding a protein Z1, a second nucleotide sequence S2 encoding a protein Z2, a third nucleotide sequence S3 encoding a protein Y1, and a fourth nucleotide sequence S4 encoding a protein Y2, in which Z1 and Z2 form a first dimer and Y1 and Y2 form a second dimer, in which the first dimer Z1Z2 is different from the second dimer Y1Y2.

Abstract: The disclosure relates generally to ligand-based chimeric antigen receptor (CAR) cells. More specifically, the CAR cells express B-cell activating factor (BAFF) protein for recognition by a receptor of BAFF on the surface of a cell. CAR cells can include cytotoxic T lymphocytes, natural killer (NK) cells or natural killer T (NKT) cells that express a chimeric receptor that recognizes a receptor of BAFF. The disclosure further relates to methods of treating a variety of conditions, such as cancers and autoimmune diseases, using the disclosed CAR cells.