Abstract: The invention relates to methods of therapy using compounds of formula (I) and formula (II): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (II) and pharmaceutical compositions thereof are integrin inhibitors that are useful in therapy for a condition, for example, caused by or associated with an infectious agent, shock, pancreatitis, or trauma. The condition can include one or more of pulmonary fibrosis associated with rheumatoid arthritis or progressive familial intrahepatic cholestasis (PFIC).

Abstract: The present invention relates to a composition effective in treating diabetes and dyslipidemia prepared according to the solid lipid nanotechnology from two natural phytochemical active ingredients: cinnamonaldehyde extracted from the Vietnamese cinnamon and berberine as a bioactive compound extracted from several plants, including a group of shrubs called Berberis. Via testing, all of the composition of the present invention has shown to have low toxicity and great bioavailability, reduced insulin resistance that allows the sugar level in blood to more effectively induce reduction of insulin, hyperglycolysis that aids the body in cellular sugar decomposition, reduced sugar production in the liver, carbohydrate decomposition slowed down in the intestines, and an increasing in the number of beneficial microbes in the intestines. The composition is effective in reducing the total cholesterol level (TC), and non-HDL-cholesterol, and has a tendency to reduce TG level.

Abstract: This invention provides a method of maintaining functional capacity, improving functional capacity, or lessening the decline of functional capacity in a human patient comprising periodically orally administering to the patient a pharmaceutical composition comprising pridopidine such that a dose of 90 mg of pridopidine is administered to the patient per day, so as to thereby maintain functional capacity, improve functional capacity, or lessen the decline of functional capacity in the human patient.

Abstract: The disclosure provides methods of treating, identifying and/or selecting for treatment a subject having a cancer in which an immune checkpoint protein is upregulated. In certain embodiments, the methods for treating cancer in a subject in need thereof comprise administering to the subject: (a) a therapeutically effective amount of an EZH2 inhibitor and (b) a therapeutically effective amount of an immune checkpoint inhibitor. In certain embodiments of the methods of the disclosure, the EZH2 inhibitor is tazemetostat.

Abstract: The present invention relates to the use of a pharmaceutical composition in the form of extended-release tablets containing Pirfenidone for treating NAFLD/NASH and advanced liver fibrosis by decreased serum cholesterol and triglycerides as well as reducing the content of hepatic fat accumulation, both in the form of macrosteatosis and microsteatosis. Additionally, its use as an agonist for PPARgamma (peroxisome proliferation receptor activated gamma), PPARalpha (peroxisome proliferation receptor activated alpha), LXR and CPT1, key molecules in the metabolism of fatty degradation and inflammation of the liver. In addition, another use is the induction of decreased expression of NFkB master gene, transcriptional inducer of hepatic inflammatory process factor. All of these events results in the reversal of NAFLD/NASH and advanced liver fibrosis.

Abstract: There is a dosage regimen for amlodipine for use in the treatment of hypertension.

Abstract: Disclosed are an external preparation of imidacloprid, a preparation method and use thereof, which relates to the technical field of veterinary drugs. The present disclosure uses alcohol solvent as the dispersion medium of imidacloprid technical, which can ensure the stability of imidacloprid technical; The present disclosure uses one or more of dibutyl hydroxytoluene, hydroxymethyl, propyl hydroxybenzoate and butylated hydroxyanisole as the antioxidant, which can effectively prevent the oxidation of imidacloprid technical and prolong the preservation time of external preparations of imidacloprid; The present disclosure uses one or more of propylene carbonate, povidone and copovidone as the stabilizer, which can reduce the volatility of the solvent and maintain the stability of the dispersion system. At the same time, the adjuvants used in the present disclosure have the advantages of safety, no skin irritation, low cost, and are suitable for market promotion and application.

Abstract: A compound may improve and/or ameliorate hair volume or quality, and such compounds may be contained in a composition. Specifically, a composition may contain pioglitazone for use in improving hair volume or quality. Such compositions may be configured for use in improving hair volume or quality, and increasing anagen-stage hairs. Such compositions may be as oral administration compositions or topical skin administration compositions. Such compositions may be configured for use in inducing a juvenile adipocyte, or inducing histogenesis of a skin accompanying induction of a juvenile adipocyte. The juvenile adipocyte may include a CD34-positive and PPARy-positive adipocyte.

Abstract: New uses of an FF-MAS metabolism inhibitor for protecting and/or regenerating a neuromuscular junction or for treating and/or preventing a disorder of a neuromuscular junction are disclosed. In one aspect, a method for protecting and/or regenerating a neuromuscular junction or a method for treating and/or preventing a disorder of a neuromuscular junction, the method including administering an effective amount of an FF-MAS metabolism inhibitor to a mammal is disclosed. In one aspect, an FF-MAS metabolism inhibitor for use in protecting and/or regenerating a neuromuscular junction or for use in treating and/or preventing a disorder of a neuromuscular junction is disclosed. In one aspect, uses of an FF-MAS metabolism inhibitor for manufacturing an agent for protecting and/or regenerating a neuromuscular junction or for manufacturing an agent for treating and/or preventing a disorder of a neuromuscular junction are disclosed.

Abstract: The invention relates to an aqueous pharmaceutical composition comprising: a) bilastine, or a pharmaceutically acceptable salt or solvate thereof, b) benzalkonium chloride, in combination with at least one further preservative selected from the group comprising phenylethyl alcohol, benzyl alcohol, sodium benzoate, chlorbutanol, phenoxyethanol, cetrimide and 2-(ethylmercuriomercapto)benzoic acid sodium salt, c) a suspending agent, and d) 2-hydroxypropyl-?-cyclodextrin; wherein the pH of the aqueous pharmaceutical composition is between 3.5 and 5.5. The invention also relates to said compositions for use in the treatment and/or prevention of a disorder or disease susceptible to amelioration by antagonism of H1 histamine receptor and/or of a corticosteroid-responsive disease through nasal administration. The invention also relates to a process for preparing the aqueous pharmaceutical composition above mentioned.

Abstract: The coronavirus SARS-Cov-2 which started in Wuhan, China, in December 2019 induced a threat to global health. Patients with mental disorders were thought to be at increased risk of becoming infected for several reasons but very much to the inventors' surprise, these psychiatric units remained nearly empty during the lock-down period as if psychiatric patients were protected from SARS-Cov-2 infection. Thus the inventors mined the literature to identify approved drugs with in vitro antiviral activities with a special emphasis on psychotropic drugs and compared these molecules using chemoinformatics strategies to the drugs most commonly used in their psychiatric department. A large number of compounds were found to be cationic amphiphilic drugs (CADs) and as such tend to also be phospholipidosis inducers in vitro (PLD). Several molecules most commonly used in their department were also found to have in vitro antiviral activity and/or can be clustered with compounds with known in vitro antiviral activity.

Abstract: Methods and compositions for reducing symptoms of mental concentration dysfunction, mood dysfunction, and/or stress-related dysfunction. In various examples, the methods include selecting a subject experiencing a symptom of mental concentration dysfunction, mood dysfunction, and/or stress-related dysfunction and providing for consumption by the subject, a nicotinamide composition formulated to reduce a frequency and/or severity of the symptom. The nicotinamide composition includes a first component and a second component. In some examples, the first component includes nicotinamide (NAM), nicotinamide riboside, or nicotinamide mononucleotide and the second component includes one or more compounds that provide a choline cation and a succinate anion (2?). In certain examples, the molar ratio of the choline cation:succinate anion (2?):first component is between 2:1:0.01 and 2:1:1.

Abstract: Compositions for use in the oral or nasal cavity are disclosed. The compositions include a biologically active agent, a matrix forming agent comprising ?-glucan and a filling agent. The compositions can further include additional excipients such as antioxidants, preservatives, taste or flavour enhancers, pH adjusters, plasticizers and sweeteners. Methods of producing the compositions are also disclosed.

Abstract: Methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R1 is halo; R2 is halo; and Q is CH or N.

Abstract: The present invention relates to the use of the compound of formula (I) or its pharmaceutically acceptable salts, in the prophylaxis and/or treatment of a viral infection. It also relates to an antiviral composition comprising or consisting of at least the compound of formula (I) or one of its pharmaceutically acceptable salts, and at least one other antiviral agent; and to products comprising or consisting of at least the compound of formula (I) or one of its pharmaceutically acceptable salts, and at least one antiviral agent, as a combined preparation for simultaneous, separate or sequential use in antiviral therapy; or for simultaneous, separate or sequential use for the prophylaxis and/or treatment of a viral infection.

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

Abstract: Use of an isoquinoline multifunctional ligand, amino-7 triethoxy-4,5,6 oxo-1 dihydro-1,3 isobenzofurannyl-3)-1methoxy-8 methyl-2 methylenedioxy 6,7tetrahydro-,2,3,4isoquinoline, or tritoqualine for the treatment of dry eyes, meibomian gland dysfunctions and lacrimal gland dysfunctions.

Abstract: Compositions and methods of modulating Akt3 are disclosed herein. Also disclosed are methods of their use to treat or prevent various diseases. Activators and inhibitors of Akt3 are disclosed for use in treating and preventing various diseases.

Abstract: This disclosure relates to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating apicomplexan parasite infections. More particularly, this disclosure relates to tetrahydroquinolinone compounds and pharmaceutical compositions thereof, methods of selectively inhibiting cytochrome b with these compounds, and methods of treating diseases that benefit from selective cytochrome b inhibition, such as a T. gondii infection.

Abstract: The present invention includes methods for treating a proliferative disorder by blocking both PDGFR and VEGFR signaling comprising a therapeutically effective amount of crenolanib or salt in combination with a VEGF/VEGFR inhibitor that is not axitinib wherein the crenolanib, VEGF/VEGFR inhibitor that is not axitinib are provided at least one of sequentially or concomitantly, in a subject for use in the treatment of the proliferative disorder, wherein the subject is a human subject.

Abstract: The application pertains to pharmaceutical combinations of orally administered paclitaxel and a P-gp inhibitor. The pharmaceutical combinations are suitable for the treatment of an angiosarcoma in a subject and for reducing or preventing toxicity, hypersensitivity-type infusion reactions, and other negative outcomes resulting from or associated with intravenously administered paclitaxel (e.g., Taxol® or paclitaxel formulated with Cremophor®) therapy in a subject suffering from an angiosarcoma.

Abstract: The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

Abstract: This invention discloses methods of preparation and usage of novel pharmaceutical compositions for the emergency treatment of life-threatening opioid overdose. The compositions targets the opiate receptors with two different opioid antagonists. A quick onset, short acting opioid antagonist and a slower onset, longer acting opioid antagonist.

Abstract: This invention is directed to compositions and methods of treating polycystic kidney disease by administering a kappa opioid receptor agonist (KOA).

Abstract: The present invention aims to provide a transdermal formulation in which apomorphine or a salt thereof is dissolved at a high concentration, so that a sufficient amount of apomorphine for treatment can be absorbed in a short time, and can be administered continuously. The present invention can include, for example, a transdermal formulation, comprising apomorphine or a salt thereof, a polyhydric alcohol with a carbon number of 6 or less and/or a low molecular weight polyethylene glycol, and propylene carbonate. According to the present invention, it is possible to prepare a solution containing apomorphine in a high concentration, and to allow a sufficient amount of apomorphine to be absorbed into the body through the skin in a short time and administered continuously.

Abstract: Presented herein are methods for preventing or treating tumor growth, tumor metastasis and/or abnormal proliferation of tumor cells in a subject, wherein the methods involve administration of a pharmaceutical composition comprising methylnaltrexone. Also presented herein are methods for inhibiting or slowing the growth of a tumor in a subject, wherein the methods include selecting a subject who is a suitable candidate for treatment with methylnaltrexone, and administering a composition comprising methylnaltrexone to the subject.

Abstract: The present invention relates to trans-N-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-N?,N?-dimethylurea (cariprazine), its salts, close analogs, derivatives, pharmaceutical compositions, metabolites and combinations for use in the treatment of symptoms of autism spectrum disorder in general, and preferably the object of the present invention is to treat one or more symptoms of autism. Furthermore, it was also found that cariprazine, its salts, close analogs, derivatives, pharmaceutical compositions, metabolites and combinations are suitable for treatment of conditions such as Asperger's syndrome, atypical autism (otherwise known as pervasive developmental disorder not otherwise specified; PDD-NOS), Rett syndrome, childhood disintegrative disorder, attention deficit hyperactivity disorder (ADHD) and sensory integration dysfunction.

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: Disclosed is an inhibitor of the acyl-protein thioesterase APT1, ML-348, of formula A: for use in the treatment and/or prevention of a disease or disorder in a subject in need thereof. In particular the inhibitor is for use in the treatment and/or prevention of a neurodegenerative disease or disorder, particularly Huntington's disease. Also disclosed is a pharmaceutical composition including at least the APT1 inhibitor and at least one pharmaceutically acceptable excipient. The inhibitor or composition is intended for use as a medicament. Furthermore, the inhibitor or composition is intended for use in the treatment and/or prevention of a disease or disorder related to impaired intracellular trafficking between the endoplasmic reticulum and the Golgi apparatus and between the latter and the plasma membrane.

Abstract: Provided herein is are methods of using 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, a mixture of enantiomers, a tautomer, or a pharmaceutically acceptable salt thereof and a bispecific antibody specifically binding to human B cell maturation antigen (BCMA) and to human CD3? (CD3) provided herein, in treating, preventing or managing multiple myeloma.

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the ?-opioid receptor.

Abstract: The present invention relates to a pharmaceutical composition comprising Varenicline or its pharmaceutically acceptable salt with reduced amount of nitrosamine impurity and a process for preparing the same.

Abstract: The invention is based on a method of modulating the activation or inhibition of Mixed lineage kinase domain-like (MLKL) protein, or a MLKL variant protein, via modulating the intramolecular interaction between the C-terminal helix (Hc) of the psK domain and a hydrophobic groove in the MLKL protein. The invention provides methods and compounds for to selectively target the herein firstly disclosed intramolecular interaction of MLKL protein. Based on the herein disclosed essential intramolecular rearrangement of MLKL, the invention provides small molecules capable of specifically inhibiting mouse or human MLKL. The invention provides uses, including medical applications such as treatments, of MLKL driven conditions including necroptosis, cell trafficking, pathological immune responses and/or inflammation.

Abstract: The invention concerns compositions and a method for treating or delaying the onset, progression, or relapse of a cancer in a subject, the method comprising administering, optionally with radiation therapy, two or more of: a DNA-dependent protein kinase catalytic subunit (DNA-PKcs) inhibitor, a poly-ADP ribose polymerase (PARP) inhibitor, an isocitrate dehydrogenase (IDH) inhibitor, a histone acetyltransferase (HAT) inhibitor, a histone deacetylase (HDAC), inhibitor, and a DNA polymerase theta (POLO) inhibitor. The inhibitors can be administered to the subject simultaneously, or sequentially in any order or combination.

Abstract: A class of thiazole-pyrimidine compounds is disclosed for use in the treatment of proliferative cell diseases and conditions in the CNS including glioblastoma. The compounds are considered to be capable of blocking tumour cell proliferation by inhibiting the activity of CDK4 and/or CDK6 and are capable of crossing the blood brain barrier.

Abstract: Methods for treating B cell lymphomas are provided. B cell lymphomas patients suitable for treatments can be identified based on the baseline B cell subset frequencies. For instance, increased frequency of transitional (CD10+) B cells within total nave B cells or within total B cells predicts poor response to kinase inhibitors. By contrast, having an increased nave B cells to total B cells frequency without an increased transitional (CD10+) B cell frequency predicts good response to the kinase inhibitors. Having a decreased frequency of nave B cells of the total B cell population with a corresponding increase in frequency of memory switched and double negative B cells of the total B cell population also predicts good response to the kinase inhibitors. Once the patients are identified, the patients can be suitably treated with the kinase inhibitors such as cerdulatinib.

Abstract: The present invention provides methods and compositions for treating and preventing lung injuries due to or associated with viral infections, such as those due to coronaviruses that cause Severe Acute Respiratory Syndrome, including COVID-19. More specifically the present invention provides methods for treating or preventing the lung injuries often associated with these infections, such as acute lung injury (ALI), lung fibrosis, and acute respiratory distress syndrome (ARDS). The methods comprise administering a therapeutically effective amount of a pharmaceutical composition comprising a protein kinase inhibitor compound having MAP3K2/AP3K3 inhibition activity, such as pazopanib or nintedanib, or a pharmaceutically acceptable salt, solvate, or prodrug thereof, to a patient in need thereof, The present invention also provides devices for administering the compositions.

Abstract: Provided herein are methods for treating liver disorders, including non-alcoholic steatohepatitis (NASH), and symptoms and manifestations thereof, in a patient comprising administration of the SSAO inhibitor: or a pharmaceutically acceptable salt thereof.

Abstract: The present specification provides methods for treating cancers characterized in having an activated hedgehog pathway.

Abstract: Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor nilotinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer. In some embodiments, the pharmaceutical compositions can be administered without regard to food consumption. In other embodiments, the pharmaceutical compositions can be administered at a significantly lower dose as compared to a commercially available immediate-release nilotinib formulation, while providing a comparable therapeutic effect.

Abstract: The present disclosure provides pharmaceutical compositions comprising a compound having activity as an ACVR1 (ALK2) or ALK5 inhibitor.

Abstract: This invention relates to an antidepressant/anxiolytic drug comprising a compound represented by the following formula (I) or (II), wherein R1 is a hydrogen atom, a C1-6-alkyl group, a C1-6-alkoxy group, a C2-6-alkenyloxy group, a halogen atom, a C1-6-haloalkyl group, a C1-6-haloalkoxy group, or a substituted or unsubstituted phenyl group; R2 is a hydrogen atom, a C1-6-alkyl group, a C1-6-alkoxy group, a C2-6-alkenyloxy group, a halogen atom, a C1-6-haloalkyl group, a C1-6-haloalkoxy group, or a substituted or unsubstituted phenyl group; and R is an indazolyl group substituted with a halogen atom; a substituted or unsubstituted phenyl group; a pyrazolyl group; or a substituted or unsubstituted aralkyl group; or a salt thereof, or a solvate thereof.

Abstract: The present invention provides compounds and methods for treating MKP-5 modulated disease. In certain embodiments, the MKP-5 modulated disease is a fibrotic disease.

Abstract: Methods and compositions to prevent or reduce the effects of neovascular eye disease in a subject are provided, wherein the subject is administered a pharmaceutical composition comprising an inhibitor of protein arginine methyltransferase 5 (PRMT5).

Abstract: The invention concerns an oral pharmaceutical composition consisting essentially of the PDE4B-inhibitor of formula III in the dose of 18 mg or 9 mg and optionally of one or more pharmaceutically acceptable carriers or excipients for use in the treatment of a patient suffering from one or more progressive fibrosing interstitial lung diseases (PF-ILD), wherein this oral pharmaceutical composition is to be administered to the patient twice daily. The invention further concerns oral pharmaceutical compositions comprising the PDE4B-inhibitor of formula III in the dose of 18 mg or 9 mg and a therapeutically effective dose of a second active ingredient selected from nintedanib or pirfenidone, wherein these oral pharmaceutical compositions are administered to the patient twice daily.

Abstract: The disclosure relates to stable topical pharmaceutical compositions of SHR0302 (also known as ARQ-250). In certain embodiments, pharmaceutical compositions of SHR0302 having a pH of less than about 4.6 have improved stability and do not exhibit crystal formation of the API. In certain embodiments, pharmaceutical compositions of SHR0302 comprising about 20% to about 30% dimethyl sulfoxide (DMSO) have improved stability and do not exhibit crystal formation of the API. The improved formulations of SHR0302 can exhibit acceptable commercial product shelf life and do not exhibit loss of potency of the API after prolonged storage.

Abstract: A compound of formula (I), for use in the treatment of non-traumatic acquired brain injury, in which M represents a NR1R2 group, an OR1 group or a SR1 group, A represents a NR4R5 group, an OR10 group or a hydrogen atom, R3 is a (C1-C6)alkyl group, a (C1-C6)cycloalkyl group, an aryl group, a —CH2-aryl group, a CH2-(C1-C6)cycloalkyl group or a —CH2-heteroaryl group, and its addition salts with pharmaceutically acceptable acids. A compound of formula (I) wherein R5 is a (C1-C8)alkyl group or a (C1-C6)cycloalkyl group, said alkyl and cycloalkyl group being substituted with one, two or three —OCORa group(s).

Abstract: The present disclosure relates to methods and compositions for the treatment of cancer (e.g., breast cancer).

Abstract: Compositions, kits and methods for the treatment or prevention of ocular allergies and inflammation and the symptoms thereof comprising alcaftadine or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are stable extended release formulations and pharmaceutical compositions of Clozapine that exhibit improved stability under a variety of conditions, as well as processes for the preparation of such formulations and compositions.