Abstract: The invention provides a compound of formula I and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the formula I compounds, as well as methods of using such as therapeutic agents for the treatment of pain-related disorders and diseases and in combination with other therapeutic agents.

Abstract: The invention provides methods for producing analgesia in an animal comprising administering to the animal a compound of the formula Ia?, Ib?, Ic?, and Id?: and pharmaceutically acceptable salts thereof, wherein the variables A, R6, R7, R8, R9, Rx, L, X, Y, and Z have the meaning as described herein.

Abstract: Novel compositions that promote hair growth or hair restoration, and compositions that prevent hair loss. Compositions including an iNOS inhibitor as an active ingredient are provided. Advantageous affects for hair growth or hair restoration are obtained when a composition including an iNOS inhibitor as an active ingredient is administered to a mammal. For the iNOS inhibitor, a low-molecular compound, an antibody, or a nucleic acid drug such as an antisense oligonucleotide or siRNA may be used. A method of screening for effective substances for promotion of hair growth or hair restoration or prevention of hair loss is also provided.

Abstract: Disclosed are methods of treating obesity or an obesity-related condition comprising administering an effective amount of soluble (pro)renin receptor (sPRR) to a subject that is obese or having an obesity-related condition. In some instances, obesity-related conditions can be, but are not limited to, steatosis, hyperglycemia, insulin resistance, chronic renal disease. Disclosed are methods of reducing body weight comprising administering an effective amount of sPRR to a subject in need thereof. Disclosed are methods of treating fatty liver in a subject comprising administering an effective amount of sPRR to a subject in need thereof. Disclosed are methods of treating a fluid and electrolyte disorder comprising administering an effective amount of sPRR to a subject diagnosed with a fluid and electrolyte disorder.

Abstract: The present invention disclosed herein provides synergistic nutritional neuroprotective compositions for ameliorating neural dysfunction. Particularly, the invention relates to synergistic, efficient, nutritional composition for comprising specific combination of decarboxylated L-arginine called agmatine sulphate and nicotinamide riboside chloride, wherein agmatine sulphate and nicotinamide riboside chloride are present in the weight ratio of 1:0.05 to 1:2 along with pharmaceutically acceptable excipients. More particularly, the present invention offers synergistic effect for ameliorating neural dysfunction encompasses cerebrovascular diseases, neurodevelopmental disorders, mood disorders, mental health disorders and like thereof.

Abstract: The invention concerns a medicine and a prophylactic medicine for COVID-19 disease. The inventive medicine targets the endosomic, non-endosomic and/or intracellular viral pathways and inhibits them. The best mode of the invention is considered to be the medicine that blocks all three viral pathways. In the best mode the individual dose of a constituent component of the medicine is arranged to a dosage size sufficient to inhibit its designated SARS-CoV-2 viral pathway. This allows the dose of a particular pharmacological agent to be smaller than in a drug with just one kind of pharmacological agent. The best mode of the invention shuts the two cell membrane viral pathways and the one intracellular viral pathway with the minimum efficient dose, thereby preventing drug overdose, and enabling prophylactic or preventive use.

Abstract: The present invention discloses novel agents and methods for diagnosis and treatment of colon cancer. Also disclosed are related arrays, kits, and screening methods.

Abstract: The present invention provides specific alkoxylation products, a process for preparing them, compositions which comprise these alkoxylation products, and the use thereof.

Abstract: A method for the treatment and/or prophylaxis of a neurological and/or neuropsychiatric disorder associated with altered dopamine function comprising administering to the eye of a patient in need thereof an effective amount of an agent that modulates neurotransmitter production or function.

Abstract: Agents and methods are provided for breaking down and/or assisting in the removal of clots, in embodiments chronic clots, from the vasculature. In embodiments, the agents and methods may be used in the vasculature, in particular the peripheral venous vasculature, in order to prevent clot formation and/or lyse clots in patients suffering from complications, such as thrombosis, or from conditions, such as deep vein thrombosis (DVT).

Abstract: Compositions and methods for treating disordered tissues, such as caused by pathogens and/or by toxins. The treatment compositions include an anti-infective active agent, a liquid carrier, and benzocaine in an amount so that the treatment composition penetrates more quickly into disordered tissue compared to the treatment composition in the absence of the benzocaine. In addition, the benzocaine can increase residence time of the anti-infective active in the treatment area. The preferred anti-infective active agent can be an organohalide, such as a quaternary ammonium halide compound, an example of which is benzalkonium chloride. The treatment compositions and methods may employ the use of an applicator adapted for use in promoting penetration of the treatment composition and/or agitation of the disordered tissue to further enhance penetration.

Abstract: The present invention provides a method for the synthesis of 18F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimized.

Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.

Abstract: The invention is dietary supplements, nutraceutical compositions, medical foods, and animal feeds that have cytoprotective (cell and tissue protection) and health promoting effects. The compositions contain a high dose range of agmatine and nutraceutical acceptable salts thereof as dietary fortification for providing effective long-term cytoprotection and affording for soft stool. The compositions may contain agmatine alone or in combination with other dietary ingredients having health promoting effects. The compositions can be prepared with dietary accepted excipients and compatible forms of carriers, including but not limited to, powders, tablets, capsules, controlled release carriers, lozenges and chewable preparations, liquid suspensions, suspensions in an edible supporting matrix or foodstuff and oral rehydration solutions, to enable consumption of said compositions.

Abstract: Provided are dithiol mucolytic agents. These agents increase the liquefaction of mucus in a patient with excessive mucus or mucus with increased viscoelastic, cohesive, or adhesive properties. Also provided are a variety of methods of treatment using these inventive mucolytic agents.

Abstract: The present invention provides compositions and methods for detecting carboxymethyl-lysine (CML) and circulating receptor for advanced glycation end (RAGE) products, and methods for correlating CML and RAGE levels with age-related disease. In particular, serum CML and/or circulating receptor for advanced glycation end (RAGE) products can be used as a clinical biomarker in diagnostics to identify people who are at a higher risk of developing adverse ageing-related outcomes.

Abstract: A composition and method of treating stroke by administration of a novel sigma agonist is presented. Twenty-four hours after MCAO, systemic administration of several novel sigma agonists including: Bromo-DTG; Chloro-DTG; N,N?-di-1-Naphthylguanidine hydrochloride (NAGH); N,N?-di-p-Nitrophenylguanidine HCL (NAD) or vehicle were injected subcutaneously daily for 3 days. Rats treated with Bromo-DTG and Chloro-DTG had no significant improvements in any of the motor or cognitive tests while NAGH treated rats showed improved vertical movement and had significantly less motor asymmetry and bias than vehicle treated rats. Sigma receptor agonist NAGH also was found to exert its long-term neuroprotective effects by preserving both gray matter and white matter tracts.

Abstract: A product comprising a calixarene for its use in the treatment of pathologies involving at least one bacterial strain having a resistance to at least one defined antibiotic, on patients undergoing simultaneous or sequential treatment with a given antibiotic to which said bacterial strain optionally has a resistance.

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Abstract: The present invention provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.

Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said composition dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.

Abstract: Cationic surfactants derived from the condensation of fatty acids and esterified dibasic amino acids, such as from lauric acid and arginine, in particular the ethyl ester of the lauramide of the arginine monohydrochloride (LAE), may be used for the treatment of objects which are infected with spores. The spores may originate from bacteria or fungi.

Abstract: The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a compound of formula I: wherein A, B, and X have any of the meanings defined in the specification; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to novel compositions including a mixture of cadaverine, putrescine, spermine and spermidine at a concentration ranging from 0.31 to 0.63 nmol per gram of composition, the composition also including agmatine at a concentration ranging from 120 to 17100 nmol per gram of composition, and uses thereof in the treatment, in a patient, of pathologies associated with cellular hyperproliferation.

Abstract: The invention relates to insecticide mixtures comprising thiodicarb and at least one other known active ingredient from the category of chloronicotinyls, as well as the use of these mixtures to control animal pests.

Abstract: The invention is dietary supplements, nutraceutical compositions, medical foods, and animal feeds that have cytoprotective (cell and tissue protection) and health promoting effects. The compositions contain a high dose range of agmatine and nutraceutical acceptable salts thereof as dietary fortification for providing effective long-term cytoprotection and affording for soft stool. The compositions may contain agmatine alone or in combination with other dietary ingredients having health promoting effects. The compositions can be prepared with dietary accepted excipients and compatible forms of carriers, including but not limited to, powders, tablets, capsules, controlled release carriers, lozenges and chewable preparations, liquid suspensions, suspensions in an edible supporting matrix or foodstuff and oral rehydration solutions, to enable consumption of said compositions.

Abstract: Processes for making and using compounds of formula (I): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. These compounds are disclosed as being useful in treating inflammatory conditions or diseases.

Abstract: Agents and methods are provided for breaking down and/or assisting in the removal of clots, in embodiments chronic clots, from the vasculature. In embodiments, the agents and methods may be used in the vasculature, in particular the peripheral venous vasculature, in order to prevent clot formation and/or lyse clots in patients suffering from complications, such as thrombosis, or from conditions, such as deep vein thrombosis (DVT).

Abstract: Facially amphiphilic polyphenylene and heteroarylene polymers and articles made therform having biocidal surfaces are disclosed. The polymers can inhibit the growth of microorganisms in contact with the surface or in areas adjacent to said biocidal surface. There is also disclosed a methods to attach facially amphiphilic polmers to a solid support. Utility as a contact disinfectant is disclosed.

Abstract: Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.

Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.

Abstract: Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.

Abstract: This invention pertains to dental care compositions with antimicrobial benefits. In particular, the invention provides for compositions of oral tissue-adherent salts that release biocidal ions on a controlled release basis and thereby provide and maintain an essentially uniform concentration of biocidal ions above the MBC or MIC of the target bacteria at the site of application in the mouth for an extended period of time. The compositions are useful for treating or preventing oral diseases resulting from bacteria, fungal or yeast infections, such as caries, gingivitis, periodontal disease and candidiasis.

Abstract: An antimicrobial composition comprising: a complex of an anionic polyester with an antimicrobial cationic surfactant, wherein the anionic polyester has at least one carboxylic group. A medical device having an antimicrobial composition comprising: a complex of an anionic polyester with an antimicrobial cationic surfactant wherein the anionic polyester has at least one carboxylic group.

Abstract: Provided herein are phenyl-guanidine derivatives for the inhibition of Rac1 which blocks its interaction with guanosine exchange factors (GEFs) belonging to the DBL family as agents for the treatment of aggressive and/or resistant tumours, as well as pharmaceutical compositions comprising them, their use in therapy and processes for their preparation.

Abstract: Embodiments of the present invention relate to insecticidal Bacillus thuringiensis Cry1 and Cry2 polypeptides. Methods for using the polypeptides and nucleic acids of embodiments of the invention to synergistically enhance resistance of plants to insect predation are encompassed in embodiments of the present invention.

Abstract: The invention relates to inhibition of SDF-1? expression in subacromial bursa cells by CXCR-4 inhibitors. Bursal cell migration in response to SDF-? stimulation is also decreased in the presence of CXCR4 inhibitors. Accordingly, provided are methods for treating or ameliorating a musculoskeletal disorder.

Abstract: The invention concerns a suspension concentrate comprising, expressed by weight based on the total weight of the composition: a) 40 to 80% particles of dodecylguanidine or an acid salt of dodecylguanidine of the structure (1), wherein X represents an acid residue of a monocarboxylic, dicarboxylic or a mineral acid, b) 0 to 10% of an anti-freeze compound, c) 1 to 10% of a wetting agent and/or d) a dispersing agent, e) 0 to 5% of an antifoaming agent, f) remainder water characterized in that, the median diameter of the particles (d50) is at least 7 ?m and below 40 ?m; and its use for the treatment of a fungicidal disease on crops or ornamental plants.

Abstract: Methods and devices for treating excess mucus accumulation in mammals by administering gaseous inhaled nitric oxide or nitric oxide releasing compounds as a mucolytic agent or expectorant are provided. Delivery of gaseous nitric oxide can be made nasally or orally and is preferably substantially coincident with inhalation of the mammal or based on a synchronous parameter of the mammal's respiratory cycle. Varying therapeutic profiles may be used for the delivery of gaseous nitric oxide depending on the severity of the excess mucus accumulation. Parameters for the therapeutic profiles may include flow rate of nitric oxide containing gas, duration of administration of nitric oxide containing gas, number of breaths for which nitric oxide containing gas is to be administered, and concentrations of therapeutic NO delivered to the airways.

Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.

Abstract: The invention provides methods for treating or ameliorating cognitive dysfunction, fatigue, energy, concentration, mood, and pain associated with fibromyalgia using compositions containing methylphenidate or pharmaceutically equivalents thereof.

Abstract: Systems, techniques and methods for estimating the metabolic state or flux, e.g., the body energy state (“BES”) of a patient, are disclosed. The BES provides deep insight into the nutritional needs of the patient, thus allowing for a sort of exquisite glycemic control with regard to the patient. The invention discloses systems and methods for estimating fractional gluconeogenesis, which is the % of glucose production that comes from gluconeogenesis (“GNG”), as opposed to glycogenolysis (“GLY”), the other form of glucose production. Nutritional formulations, materials, cocktails and methods for feeding patients by parenteral and other means are disclosed. The amount, type and rate of such nutritional feeding are typically based upon the above estimating. The invention discloses formulations that contain labels, such as deuterium, for medical diagnostics, such as for estimating BES and fractional gluconeogenesis.

Abstract: Novel compounds of the following formula (I): in which: n represents an integer from 1 to 12, in particular from 1 to 8, m and m? represent, independently of one another, integers from 0 to 8, q and q? represent, independently of one another, integers from 0 to 2, p and p? represent, independently of one another, integers from 0 to 4, A and A? represent, independently of one another, a CH2 group, (particular case of amidines) an NH group or an NR? group, in which R? is a linear or branched alkyl group with 1 to 3 carbon atoms, B and B? represent, independently of one another, an oxygen atom or a CH2 group, R and R? are, independently of one another, a halogen, such as chlorine, bromine, iodine or fluorine atoms, or a linear or branched alkyl group with 1 to 3 carbon atoms, use thereof as medicaments and the method of preparation thereof.

Abstract: Agrochemical compositions are described which contain a carboxylic acid salt of dodecylguanidine and a compatibility agent for slowing down the dissociation reaction of the carboxylic acid salt of dodecylguanidine in an aqueous medium. Also, the formation of anionic dodecylguanidine is suppressed or prevented. The ratio of the dodecylguanidine acetate to that of the compatibility agent in the agricultural compositions is below 5.0, preferably between 3.0 and 0.5, more preferably equals 1.4.

Abstract: A product comprising a calixarene for its use in the treatment of pathologies involving at least one bacterial strain having a resistance to at least one defined antibiotic, on patients undergoing simultaneous or sequential treatment with a given antibiotic to which said bacterial strain optionally has a resistance.

Abstract: The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.

Abstract: The invention relates to ether guanidines of the general formulae (I) and/or salts or hydrates thereof, in which R1=—CH2—CH2—CH2—O—R3 where R3 is, independently of the others, hydrocarbon radicals having greater than or equal to 10 carbon atoms, where part of the ether guanidines has radicals R3 which are branched and part of the ether guanidines has radicals R3 which are unbranched, and R2=independently of the others H or an optionally branched, optionally double-bond-containing hydrocarbon radical having 1 to 30 carbon atoms, and use thereof in hair treatment compositions and hair aftertreatment compositions, in particular for preventing damage by chemical treatment compositions and for repairing hair which is already damaged.

Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

Abstract: A method for determining the levels of biomarkers, specifically, advanced glycation end products (AGEs) and oxidation products (Ops) in a biological sample such as a plasma ultrafiltrate, is used to determine a patient's risk and/or rate of developing diabetes related nephropathy. The preferred biomarkers to measure include N?-(1-carboxyethyl-lysine (CEL), methylglyoxyl-derived hydroimidazolone (MGHI) and N?-carboxymethyllysine (CML). Also provided herein is a method of diabetic care which includes determining a diabetic patient's risk of developing diabetes related kidney disease and adjusting the patient's treatment regimen to include in addition to glucose lowering agents, additional treatments such as medications that modify the renin-angiotensin system, or specialized diets with low levels of AGEs or oxidative products.

Abstract: The present invention provides a rapid-acting, blood arginine level-increasing oral preparation containing citrulline or a salt thereof and arginine or a salt thereof as active ingredients. The rapid-acting, blood arginine level-increasing oral preparation of the present invention can rapidly and effectively increase blood arginine level after ingestion, and can rapidly provide an arginine ingestion effect.