Abstract: The disclosure provides a method for synthesizing free base forms of (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine. In an embodiment synthesis of (2R,6R)-hydroxynorketamine (HNK) includes preparation of (R)-norketamine via chiral resolution from racemic norketamine via a chiral resolution with L-pyroglutamic acid. The disclosure also provided crystal forms of the corresponding (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine hydrochloride salts.

Abstract: Methods and systems are described for producing non-invasive and targeted neuronal lesions using magnetic resonance and acoustic energy. Imaging data corresponding to a region of interest is obtained, the region of interest within an imaging subject. Information indicative of a target region within the region of interest is received from the obtained imaging data. Focused acoustic energy directed to the target region within the region of interest is generated to disrupt a barrier between a therapeutic agent and parenchymal tissue in response to insonification by the focused acoustic energy, the therapeutic agent comprising a neurotoxin and microbubbles.

Abstract: The present invention relates to balloon catheters with or without crimped stent, whose surface is coated with at least one antirestenotic agent and at least one transport promoting molecular dispersant, as well as a method for the preparation of these medical devices.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.

Abstract: A compounded topical solution may include approximately 85% to approximately 95% (v/v) diclofenac sodium topical solution, 1.5% (w/w), and approximately 5% to approximately 15% (v/v) lidocaine hydrochloride topical solution, 4% USP.

Abstract: Long term storage stable bendamustine-containing compositions are disclosed. The compositions can include bendamustine or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable fluid which can include in some embodiments PEG, PG or mixtures thereof and an antioxidant or chloride ion source. The bendamustine-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 223 nm, after at least about 15 months of storage at a temperature of from about 5° C. to about 25° C.

Abstract: The present invention provides a composition for controlling harmful arthropods having an excellent control efficacy on harmful arthropods. A composition for controlling harmful arthropods comprising a carboxylic acid compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of neonicotinoid compounds selected from the group (A) consisting of imidacloprid, clothianidin, thiamethoxam, dinotefuran, acetamiprid, thiacloprid and nitenpyram, shows an excellent controlling efficacy on harmful arthropods.

Abstract: The present invention relates to a method for diagnosing and/or treating sodium-iodide symporter (NIS)-expressing primary carcinomas and metastases, preferably glandular carcinomas, in particular carcinomas of the thyroid, of the salivary gland, of the uterus and carcinomas of the breast, and to a pharmacological composition comprising substances which induce and/or increase the expression or function of the NIS symporter and, as a consequence, increase iodide uptake into the cells, and to corresponding uses. This can be used for an efficient tumor-specific radioiodide uptake in diagnosis and therapy of said carcinomas and metastases.

Abstract: An agrichemical composition comprising a compound represented by the formula (1) and at least one fungicidally active compound selected from Group (A). Group (A): metalaxyl, metalaxyl-M, benalaxyl, benalaxyl-M, pyraclostrobin, trifloxystrobin, azoxystrobin, dimoxystrobin, fluoxastrobin, kresoxim methyl, picoxystrobin, metconazole, ipconazole, tebuconazole, difenoconazole, epoxiconazole, fluquinconazole, triticonazole, triadimenol, prothioconazole, propioconazole, prochloraz, penconazole, flusilazole, diniconazole, bromuconazole, cyproconazole, triflumizole, tetraconazole, myclobutanil, bitertanol, imazalil and the like.

Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, and in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. Antiviral activity of enzyme inhibitors is demonstrated.

Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.

Abstract: Provided is a sensitizing detection agent of an oral or intravenous administration type which enables the detection of bladder cancer with a higher sensitivity without causing pain to the patient. A sensitizing detection agent for bladder cancer comprising 5-aminolevulinic acid (ALA), a derivative thereof, or a salt of these is orally or intravenously administered, and a video camera system is inserted via the urethra and a blue light at 380-440 nm is irradiated to observe the red fluorescent part. Further, VLD-M1 is inserted and a blue light at 405 nm is irradiated to observe fluorescence intensity (relative intensity) of the red light part. For oral administration, 20 mg/kg (maximum of 1 g) of ALA is dissolved in 50 mL of a 5% glucose solution prior to the administration.

Abstract: The invention generally relates to methods of treating an overweight or obese subject, and treating overweight- or obesity-related conditions using non-daily administration of e.g, a MetAP-2 inhibitor.

Abstract: A parenteral formulation of esmolol hydrochloride for use in the treatment of a patient suffering from tachycardia comprising a lyophilized powder consisting of pure esmolol hydrochloride, wherein said powder is reconstituted to obtain a ready-to-use i.v. solution of esmolol hydrochloride at a concentration of 20-100 mg/mL, and said i.v. solution is directly administered to the patient, and further a method of producing a ready-to-use i.v. solution of esmolol hydrochloride by reconstituting a lyophilized powder consisting of pure esmolol hydrochloride with a solvent, characterized in that said solvent is an i.v. solvent devoid of alcohol or a buffer excipient, in an amount necessary to obtain a ready-to-use i.v. solution at a concentration of 20-100 mg/mL, and the ready-to-use i.v.

Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.

Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.

Abstract: The invention generally relates to methods of treating an overweight or obese subject, and treating overweight- or obesity-related conditions using non-daily administration of e.g., a MetAP-2 inhibitor.

Abstract: The present invention relates to new dihydroxyphenyl modulators of neurotransmitter levels, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A concentrate esmolol formulation is provided that is safer than current concentrate (e.g., 250 mg/ml) esmolol compositions. The concentrate esmolol formulation can include from about 40-60 mg/ml of esmolol hydrochloride. The concentrate esmolol composition allows a practitioner the flexibility of choosing a bolus volume for direct injection to a patient or, optionally, to use the composition to make a customized, diluted composition of esmolol. Methods of the present invention provide for the reduction of potential adverse health consequences resulting in the improper dosing of prior art concentrate compositions of esmolol. Also, a medical product is provided that includes a concentrate esmolol housed in a container, and a package housing the container and instructions.

Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.

Abstract: Combinations, compositions and methods of use for modulating plant pathogen infection using plant extracts containing anthraquinone derivatives which induce resistance to plant phytopathogens and an antimicrobial agent, a biological control agent and/or a surfactant having fungicidal activity.

Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II) and pyribencarb: shows an excellent controlling efficacy on plant diseases.

Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II) and pyribencarb: shows an excellent controlling efficacy on plant diseases.

Abstract: A ready-to-use injectable, co-solvents (ternary mixture) pharmaceutical composition for the treatment of cardiac conditions and diagnosis applications, comprising methyl-3-[4-(2-hydroxy-3-isopropylamino) propoxy]phenylpropionate hydrochloride (Esmolol hydrochloride), a buffering agent, ethanol and propylene glycol which capable of been stored in modified flexible plastic container, heat-sterilized without deformation and/or integrity of the closure system been compromised, as well as method for its manufacture, is disclosed.

Abstract: A composition comprising racecadotril, at least one surfactant and a lipid.

Abstract: A ready-to-use injectable, co-solvents (ternary mixture) pharmaceutical composition for the treatment of cardiac conditions and diagnosis applications, comprising methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride (Esmolol hydrochloride), a buffering agent, ethanol and propylene glycol. The ready-to-use injectable, co-solvents (ternary mixture) pharmaceutical composition is capable of being stored in a modified flexible plastic container that may be heat-sterilized without deformation and/or without having the integrity of the closure system being compromised. A method for the manufacture of the ready-to-use injectable, co-solvents (ternary mixture) pharmaceutical composition is also disclosed.

Abstract: PROBLEM There are provided a composition for controlling plant diseases and a method for controlling plant diseases having excellent control effect for plant diseases. SOLUTION A composition for controlling plant diseases comprising, as active ingredients, a compound represented by formula (1) wherein X1 represents a methyl group, a difluoromethyl group or an ethyl group; X2 represents a methoxy group or a methylamino group; and X3 represents a phenyl group, a 2-methylphenyl group or a 2,5-dimethylphenyl group, and at least one compound selected from the group consisting of tolclofos-methyl, metalaxyl and mefenoxam, and a method for controlling plant diseases using the composition.

Abstract: Coating composition for an oilseed plant seed from which roots and shoots are capable of growing, wherein the coating composition comprises an organic carrier material and one or more biological agents that possess an activity against at least one or more pathogens of the oilseed plant.

Abstract: A pharmaceutical composition comprising (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate in a concentration between about 75 mM and about 150 mM, which is substantially free of the R-isomer or pharmaceutically acceptable salt thereof, is provided. A method of treating a cardiac disorder is also provided and includes administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride, wherein the (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride is present at a concentration between about 75 mM and about 150 mM and wherein the pharmaceutical composition is substantially free of (R)-methyl-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate or pharmaceutically acceptable salt thereof.

Abstract: Benzonatate resinates of weak acid ion exchange resins having the same distribution of butyl 4-aminobenzoate homologs as exist in the benzonatate listed in the F.D.A. Orange Book as Application No. N011210. These resinates, in simulated gastrointestinal dissolution, release essentially the same distribution of butyl-4 aminobenzoate homologs as exist in the benzonatate listed in the F.D.A. Orange Book as Application No. N011210.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: This disclosure relates to methods of managing brain injury such as inflammation due to trauma induced brain injury and ischemic stroke by administering resatorvid or derivative there of a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating cerebral ischemia comprising administering an effective amount of resatorvid to a subject in need thereof. In certain embodiments, the effective amount is 3 mg/kg. In certain embodiments, resatorvid is administered by injection.

Abstract: The present invention provides a composition for controlling harmful arthropods having an excellent control efficacy on harmful arthropods. A composition for controlling harmful arthropods comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of neonicotinoid compounds selected from the group (A) consisting of imidacloprid, clothianidin, thiamethoxiam, dinotefuran, acetamiprid, thiacloprid and nitenpyram, shows an excellent controlling efficacy on harmful arthropods.

Abstract: The present invention provides a composition for controlling harmful arthropods having an excellent control efficacy on harmful arthropods. A composition for controlling harmful arthropods comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof, and at least one kind of neonicotinoid compounds selected from the group (A) consisting of imidacloprid, clothianidin, thiamethoxiam, dinotefuran, acetamiprid, thiacloprid and nitenpyram, shows an excellent controlling efficacy on harmful arthropods.

Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.

Abstract: A compound having an ability to bind to an SIP receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.

Abstract: A compound of formula (I) as defined herein is useful in the treatment and prevention of a disorder such as cachexia, stroke, atherosclerosis, coronary artery disease, and diabetes and pharmaceutical compositions of the same. Also, a method of screening for lipase inhibitors using a compound of formula (I) and determining its lipase inhibitory activity. The method includes in vitro assays of compounds using ATGL and/or HSL, and cellular assays wherein inhibition is followed by observing indicators of efficacy. Also, methods for treatment or prevention of a condition involving cachexia, stroke, artherosclerosis, coronary artery disease, diabetes, preferably diabetes type II by administering a pharmaceutical composition comprising an agent which is able to inhibit ATGL. Also contemplated herein, are compositions comprising one or more ATGL-inhibiting agents optionally in combination with one or more lipase inhibitors or inhibitors of inflammatory cytokines.

Abstract: The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications.

Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.

Abstract: This invention relates to a new topical gel formulation of the drug Esmolol hydrochloride for treatment of chronic wounds such as diabetic wounds, burn wounds, venous ulcers and pressure ulcers.

Abstract: Disclosed are concentrate esmolol injection essentially free from other related esters of esmolol and diluted esmolol compositions. The concentrate esmolol formulation includes from about 25-1000 mg/ml of esmolol and about 1-25% w/v of benzyl alcohol and the combination thereof. The compositions can also be used as multi-dose compositions. The present invention also discloses diluted, ready-to-use compositions of esmolol prepared by dilution of the present invention concentrates. Also disclosed are methods of making and using the ready-to-use compositions of the present invention.

Abstract: A conjugate comprising L-DOPA covalently linked to at least one ?-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.

Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).

Abstract: Disclosed herein are thiol mediated/activated prodrugs of SO2, particularly 2,4-dinitrophenylsulfonamide analogues, having Formula-I or pharmaceutically acceptable salts thereof exhibiting tunable release profiles of SO2 with significant therapeutic efficacy against bacterial infections. Further, the present invention provides pharmaceutical compositions comprising compound of Formula I or pharmaceutically acceptable salts thereof, along with pharmaceutically acceptable carriers/excipients.

Abstract: The present invention relates to formulation comprising at least (i) two pesticidal compounds A and B dissolved in a lactic acid ester and wherein a) both A and B have melting points below 900 C b) both A and B are selected from the following list: pyraclos-trobin, metalaxyl, mefenoxam, trifloxystrobin, imazalil, pro-chloraz and ipconazole with the proviso that A is different from B (ii) at least one pesticidal compound C present in solid particles, and having a melting point of 900 C and above, and to their use as seed treatment formulation as well as their use for plant protection, including seed and crop protection.

Abstract: The present invention provides novel compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of a compound of the invention to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.

Abstract: A method of treating tachycardia while minimizing and/or controlling hypotension associated with such treatment includes administering a therapeutically effective amount of a pharmaceutical composition comprising the S-isomer of esmolol to a subject in need thereof.

Abstract: The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases