Abstract: Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

Abstract: The present invention relates to methods for reducing the heterogeneity of a population of recombinant proteins produced in cell culture, said methods comprising growing host cells producing a recombinant protein in a cell culture medium wherein the cell culture medium comprises one or more cysteine/cystine analogs.

Abstract: The present disclosure describes methods of treating a central nervous system condition associated with oxidative stress using a 5-lipoxigenase activating protein (FLAP) inhibitor, for example, N-acetylcysteine or nordihydroguaiaretic acid. The present disclosure also describes methods of treating a central nervous system condition with N-acetylcysteine and a second therapeutic agent such as prostaglandin E2.

Abstract: Liquid parenteral formulations are provided that include tigecycline and at least one or more pharmaceutically acceptable excipient or adjuvant, where the formulation is ready to use without additional steps for reconstitution at the time of administration.

Abstract: The invention belongs to the field of microbes and specifically relates to a myroides odoratimimus biocontrol strain for efficiently degrading aflatoxin and an application thereof. A myroides odoratimimus biocontrol strain 3J2MO is preserved at the China Center for Type Culture Collection (referred to as CCTCC) on Jun. 13, 2017 with preservation number CCTCC No. M 2017329. The myroides odoratimimus biocontrol strain of the invention can effectively degrade aflatoxin and may be configured to degrade aflatoxin and treat aflatoxin pollution of food crops.

Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating deseases, such as cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating deseases, such as cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

Abstract: The present invention relates to compounds of formula (I) having insecticidal activity to processes and interediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests claim 1: or salts thereof.

Abstract: Compounds suitable for use in providing male contraception, an assay method for identifying such compounds, and methods of providing contraception using the compounds, are provided. In one embodiment, the compounds described herein mimic the binding of anti-EPPIN antibodies to EPPIN, and thus inhibit the forward motility of sperm in humans and other primates. In another embodiment, the compounds described herein inhibit or enhance EPPIN-semenogelin binding, and inhibit forward motility of sperm. The assays described herein identify compounds which inhibit sperm motility, and can be carried out in a high throughput manner, using labeled recombinant EPPIN and semenogelin. The compounds can be used in oral or transdermal compositions to temporarily and reversibly inhibit male fertility. They can also be used in addition to, or in place of, spermicides in spermicidal compositions, such as those used in conjunction with condoms, diaphragms, and spermicidal jellies.

Abstract: The present invention relates to an improved process for the synthesis of (R)-Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.

Abstract: The present invention relates to a disaccharide intermediate and a synthesis method thereof, relates to the chemical pharmaceutical field, and more specifically relates to a method for preparing a disaccharide segment of a key intermediate for chemically synthesizing heparin and heparinoid compounds. Disclosed are a new disaccharide intermediate and three methods for synthesizing the disaccharide intermediate, that is, compounds of a formula (4) and glucopyranose protected by different anomeric carbon are made to react in the presence of an active agent, to obtain the disaccharide intermediate. According to the technical solutions of the present invention, synthetic raw materials are easy to obtain, have a mild reaction condition, and are suitable for industrialized production.

Abstract: The disclosure provides methods for determining the self-renewal potential of a cancer stem cell (CSC), or for predicting the drugability (susceptibility to a drug) of a CSC, and/or for predicting the progression of a cancer that corresponds to the CSC. In alternative embodiments, the disclosure provides methods for determining whether a CSC in a niche is more pro-apoptotic or more anti-apoptotic in relation to a normal stem cell or a CSC from another niche. In alternative embodiments, the disclosure provides methods for determining the prognosis or malignant potential of a cancer. In alternative embodiments, the disclosure provides methods determining the anti-apoptotic versus a pro-apoptotic potential of a cancer stem cell (CSC).

Abstract: Disclosed are compounds of formulae: (I) and pharmaceutically acceptable salts thereof, wherein the variables, R1, R2, Y, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.

Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.

Abstract: The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein X1, X2, X3, X4, X5, W1, W2, W3, and W4 are as described. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. In one aspect, the invention relates to selective HDAC3 inhibitors useful for protecting ?-cells and improving insulin resistance. The selective HDAC3 inhibitors are also useful for promoting cognitive function and enhancing learning and memory formation.

Abstract: The present invention provides a novel method for preparing lacosamide with high chiral purity from D-serine. The method of the present invention can obtain lacosamide with high chiral purity in a high yield through a simple and environmentally-friendly process and thus can be easily applied to mass production.

Abstract: Provided herein is a method for treating pain in a subject without risking hepatotoxicity by administering a pharmaceutical composition containing an acetaminophen dimer compound wherein the phenolic hydroxyl groups of two acetaminophen molecules are linked via an ethylene spacer.

Abstract: Embodiments of the invention relate to methods and compositions for treating symptoms related to inflammatory conditions and to methods and compositions for treating inflammatory components of a common cold, utilizing various methods of administration od X-ray contrast media (CM).

Abstract: The present invention comprises homeopathic preparations of compounds, methods for using such preparations and delivery systems for the treatment of disease symptoms through the administration of these homeopathic compositions.

Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.

Abstract: The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S31-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis.

Abstract: New improved formulations comprising a first composition and a second composition, the first composition being a streptogramin, the second composition being an inhibitor of lipid A deacetylase resulting in permeabilization of an outer membrane of a microorganism to which it is provided to. Said composition, alone or in combination may be used to treat bacterial infections, providing better efficacy, bioavailability and or pharmacokinetics as compared with other antimicrobial agents. The combination may be provided independently or together, and via any route(s) and in any formulation or form.

Abstract: Provided herein are methods for treating pain such as acute or chronic pain or fever in subject without risking hepatotoxicity. The subject may be at risk of hepatotoxicity if administrated an acetaminophen monomer. The method includes administering a pharmaceutical composition containing an acetaminophen dimer compound, wherein the phenolic hydroxyl groups of two acetaminophen compounds are linked via an ethylene spacer.

Abstract: Provided are a Tigecycline crystalline hydrate, and a preparation method therefor and use thereof. The crystalline hydrate has high stability for storage, and is used for the manufacture of a medicament for treating or preventing the infection of respiratory system, hepatobiliary system, facial features, urogenital system, bone and joint, skin and soft tissue and endocarditis, septicemia, meningitis caused by susceptible strains of Gram-positive or Gram-negative bacteria, anaerobic bacteria, chlamydia, and mycoplasma in human or animal.

Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumor-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.

Abstract: Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.

Abstract: Provided is a novel plant growth regulator. The disclosed plant growth regulator comprises flubendiamide as an active ingredient.

Abstract: A therapy for renal diseases, in particular renal diseases, which develop in diabetic patients or patients who have been subjected to a treatment with an antitumor chemotherapy such as a platinum derivative and more generally cytotoxic drugs at renal level for treating of neoplastic diseases. More particularly, palmitoylethanolamide and diethanolamide of fumaric acid are used in the treatment of renal diseases, in particular those caused by dysmetabolic diseases or by toxic or chemotherapy agents, such as platinum derivatives. Palmitoylethanolamide is used preferably in micronized or ultra-micronized form. Diethanolamide of fumaric acid is used preferably in aqueous solution.

Abstract: Salts of kukoamine B, their preparation method and their pharmaceutical use in preparation of drugs for preventing and treating sepsis. Experiments indicate that salts of kukoamine B have a good effect on antagonizing the key factors inducing sepsis, and can be used in the preparation of drugs for preventing and treating sepsis. Under the current circumstances of the lack of effective measures for the treatment of sepsis in clinical practice, the medicinal formulations, which comprise the salts of kukoamine B, pharmaceutically acceptable carrier and/or diluent, provide a new approach for the prevention and treatment of sepsis.

Abstract: Pharmaceutically active homo-dimers of opioid and other pharmaceutically active agents characterized by a single phenolic hydroxyl group wherein the respective monomers are ether-linked through such groups by an ethylene residue. The dimers share the receptor pharmacology of the corresponding monomer, in particular cases are non-absorbed, and the ether link of the dimers is particularly resistant to metabolism when administered to a subject, all conferring divers advantages relative to the corresponding monomers. Exemplary of the dimers are those of buprenorphine, naloxone, naltrexone, des-venlafaxine, albuterol and acetaminophen.

Abstract: Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Form B, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline tacedinaline Form B, the novel crystalline tacedinaline TFA salt, and/or amorphous tacedinaline, and methods of treating various conditions by administering those novel solid forms, are also disclosed.

Abstract: Zn2+-chelating motif-tethered fatty acids as histone deacetylase (HDAC) inhibitors. Compounds performed well in in vitro and in vivo tests.

Abstract: A scleral lens is provided with a sodium channel blocker or a sodium channel modulator disposed in the pre-corneal tear film between the scleral lens and the cornea. This system can be used to deliver sodium channel blockers or a sodium channel modulators not currently used because of poor bioavailability. Methods of using this sodium channel blocker delivery system or a sodium channel modulator delivery system are also disclosed.

Abstract: This disclosure describes methods of use for N-acetylcysteine amide for the treatment of various disorders

Abstract: A method of identifying a subject having cancer who is likely to benefit from treatment with a combination therapy with a MAPK pathway inhibitor, such as a RAF inhibitor, MEK inhibitor, or ERK inhibitor, and a GEF or HDAC inhibitor is provided. A method of treating cancer in a subject in need thereof is also provided and includes administering to the subject an effective amount of a MAPK inhibitor, such as a RAF inhibitor, MEK inhibitor, or ERK inhibitor, and an effective amount of a GEF or HDAC inhibitor. A method of identifying targets that confers resistance to a MAPK pathway inhibitor is also provided.

Abstract: This disclosure describes methods of use for N-acetylcysteine amide for the treatment of penetrating head injury.

Abstract: The invention provides compounds of formula (I): wherein R1-R3, n, and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.

Abstract: The present invention relates to the use of compounds of formula wherein the variables are as defined in the description, in the free form or in salt form, for controlling sea lice on fish.

Abstract: The invention relates to a combination comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to a combination comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.

Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of local pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of moderate to severe pain, neuropathic pain, post herpetic neuralgia and rheumatic pains.

Abstract: A modified release formulation of lacosamide.

Abstract: The present disclosure provides compounds, specifically pyrimidin-4,6-dicarboxylic acid amide derivatives, or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds. Also provided are methods for treating a mammal having malaria, or killing or inhibiting the growth of a Plasmodium species, comprising administering to said mammal or contacting said Plasmodium species with, an effective amount of a pyrimidin-4,6-dicarboxylic acid amide derivative.

Abstract: The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors.

Abstract: Various embodiments of the present invention relate to, among other things, compounds that are inhibitors of Memapsin 1 and, as a result, are effective in the treatment of Alzheimer's disease or diabetes (e.g., Type 2 diabetes).

Abstract: The invention relates to compounds of formula (I), and the use thereof as a drug, particularly for the treatment of tumors associated with hyperactivation of the hedgehog protein signaling pathway, treatment of neurodegenerative diseases, treatment of diseases related to cerebral development (holoprosencephaly), for stem cell monitoring treatment of cerebrovascular accidents and cardiovascular accidents, treatment of diseases involving oligodendrocytes and diseases involving neurolemmocytes, for application thereof in vitro for modulating human or animal stem cell renewal, and for the treatment of diabetes. The invention also relates to pharmaceutical compositions having a compound of formula (I).

Abstract: A therapy for renal diseases, in particular renal diseases, which develop in diabetic patients or patients who have been subjected to a treatment with an antitumor chemotherapy such as a platinum derivative and more generally cytotoxic drugs at renal level for treating of neoplastic diseases. More particularly, palmitoylethanolamide and diethanolamide of fumaric acid are used in the treatment of renal diseases, in particular those caused by dysmetabolic diseases or by toxic or chemotherapy agents, such as platinum derivatives. Palmitoylethanolamide is used preferably in micronized or ultra-micronized form. Diethanolamide of fumaric acid is used preferably in aqueous solution.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.