Abstract: In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.

Abstract: A compound with anti-drug resistant bacteria activity having the following formula (I): is disclosed. A method of preparing the compound of formula (I) is also disclosed.

Abstract: In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.

Abstract: A catalyst-containing particle including a core and an acidic coating layer thereon, wherein the core includes a nitrogen-containing catalyst for a thermoset polymeric system, and the acidic coating layer comprises a binder; and a method of making such particles. A curable, one-part epoxy/thiol resin composition that includes: an epoxy/thiol resin mixture including: an epoxy resin component that includes an epoxy resin having at least two epoxide groups per molecule; a thiol component that includes a polythiol compound having at least two primary thiol groups; and catalyst-containing particles dispersed in the epoxy/thiol resin mixture; wherein each particle includes a core and an acidic coating layer thereon, wherein the core includes a nitrogen-containing catalyst for the epoxy resin; and a method of curing such curable composition.

Abstract: Methods of treating developmental encephalopathies by administering compositions including ketamine, norketamine, or other derivatives of ketamine, or a pharmaceutically acceptable salt of any of the foregoing, are provided. The methods and compositions may be used to treat conditions such as Dravet syndrome.

Abstract: Described herein are compositions and methods for the treatment of meibomian gland dysfunction. Said compositions and methods comprise keratolytic agents, such as salicylic acid, selenium disulfide, or the like. Topical administration of said compositions to the eyelid margin or surrounding areas provides therapeutic benefit to patients suffering from meibomian gland dysfunction.

Abstract: In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.

Abstract: In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.

Abstract: A method for treating pancreatic cancer is provided. The method comprises administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical formulation, wherein the pharmaceutical formulation comprises (Z)-butylidenephthalide and is substantially free of (E)-butylidenephthalide.

Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

Abstract: Apoptosis is generally believed to be a process that requires several hours, in contrast to non-programmed forms of cell death that can occur in minutes. Our findings challenge the time-consuming nature of apoptosis. We describe herein the discovery and characterization of a small molecule, named Raptinal, which initiates intrinsic pathway caspase-dependent apoptosis within minutes, in multiple different cell lines. Comparison to a mechanistically diverse panel of apoptotic stimuli reveals Raptinal-induced apoptosis proceeds with unparalleled speed. The rapid phenotype enabled identification of the critical roles of mitochondrial voltage-dependent anion channel function, mitochondrial membrane potential/coupled respiration, and mitochondrial complex I, III and IV function for apoptosis induction. Use of Raptinal in whole organisms demonstrates its utility to study apoptosis in vivo for a variety of applications.

Abstract: The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of inflammatory disease and/or central nervous system disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like. The present invention relates to a compound represented by formula (I) and a salt thereof: (wherein, each symbol is explained in greater detail in the specification).

Abstract: The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.

Abstract: The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of inflammatory disease and/or central nervous system disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like. The present invention relates to a compound represented by formula (I) and a salt thereof: (wherein, each symbol is explained in greater detail in the specification).

Abstract: The present invention relates to a process for the preparation of a solid, orally administrable pharmaceutical composition, comprising 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide in hydrophilized form, and its use for the prophylaxis and/or treatment of diseases.

Abstract: In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.

Abstract: The present invention relates to a process for the preparation of a solid, orally administrable pharmaceutical composition, comprising 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide in hydrophilized form, and its use for the prophylaxis and/or treatment of diseases.

Abstract: The present invention relates to novel phenylalkyl sulfamate compounds, a method for preventing or treating a disease associated with muscle spasm. The present invention ensures the enhancement of muscle relaxation activity essential for alleviation of muscle spasm, such that it is promising for preventing or treating various diseases associated with muscle spasm.

Abstract: Embodiments of the present disclosure provide compositions including ketamine analogs, salts, and disalts, pharmaceutical compositions including ketamine analogs, salts, or disalts, methods of treatment of a condition or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.

Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.

Abstract: The present invention provides a method of treatment of Scedosporium spp.

Abstract: Compositions including a highly branched alpha-D-glucan or modified forms thereof and a solute compound are described herein. The compositions can provide increased water solubility and/or increased rate of dissolution for the solute compound. The compositions can also provide increased stability for the solute compound. Methods for preparing and using compositions including a solute compound and a highly branched alpha-D-glucan are also described.

Abstract: Disclosed are substituted 2-oxaspiro[5.5]undec-8-ene derivatives of formula (I) and their use as odorants. This disclosure relates furthermore to a method of their production and flavor and fragrance compositions comprising them.

Abstract: The invention relates to a novel compound of the formula or pharmaceutically acceptable salts thereof as well as pharmaceutical, nutraceutical, and botanical drug compositions and therapeutic methods related thereto. In certain embodiments, the compounds are used for the treatment of abnormal cell growth, hyperproliferative disorders, and inflammatory diseases in mammals. In other embodiments, the invention encompasses methods to isolate and synthesize the compounds.

Abstract: A liquid composition comprises an organic diluent and at least one cellulose ether having anhydroglucose units joined by 1-4 linkages and having methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl as substituents such that hydroxyl groups of anhydroglucose units are substituted with methyl groups such that s23/s26 is 0.29 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 3-positions of the anhydroglucose unit are substituted with a methyl group and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 6-positions of the anhydroglucose unit are substituted with a methyl group. The liquid composition can be used for preparing a solid dispersion of an active ingredient in a cellulose ether.

Abstract: An esterified cellulose ether comprises (i) aliphatic monovalent acyl groups or (ii) groups of the formula —C(O)—R—COOA wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation or (iii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein the cellulose ether has anhydroglucose units joined by 1-4 linkages and has methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl as substituents such that the esterified cellulose ether has an MS (hydroxyalkyl) of 0.05 to 1.00, and hydroxyl groups of anhydroglucose units are substituted with methyl groups such that [s23/s26?0.2*MS(hydroxyalkyl)] is 0.

Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.

Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the biphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular biphenyl-substituted cyclic ketoenols through the addition of ammonium or phosphium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or nematicides and/or acaricides and/or fungicides and/or for preventing unwanted plant growth.

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: Methods for treating an individual to improve cognitive function are provided. In the subject methods, an effective amount of a noncompetitive GABAA ionophore blocker is administered to the individual, resulting in an improvement in cognitive function of the host. The subject methods find use in a variety of different applications.

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 the class of the tetronic or tetramic acids, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids.

Abstract: The invention relates to insecticidal and acaricidal mixtures comprising certain cyclic ketoenols and agonists or antagonists of nicotinic acetylcholine receptors for protecting plants against attack by pests.

Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides processes for making the compounds described herein. Furthermore, the present invention provides a composition comprising the compounds described herein, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The present invention also provides methods of treating or preventing bacteria infection in a subject, comprising administering to the subject an effective amount of the compound or the composition described herein.

Abstract: A combination of sheets can be combined into an ingestible unit. The individual sheets can be prepared to have one or more functionalities, such as providing a biologically active agent, disintegrating and opening the unit, controlling release of an agent, facilitating absorption from the GI tract, as well as many others. The individual sheets can be selectively identified for combining into a multifunctional ingestible unit with a random or predetermined arrangement or stacking pattern. The individual sheets can be loose in a capsule or laminated together into a stacked layered structure. The combination of sheets can be pressed, laminated, tableted, or otherwise prepared into an ingestible unit. The ingestible unit can be predetermined to be useful for administering a drug, drug combination, multi-drug regimen as well as tailored to subject-specific multi-drug therapeutic regimens. The sheets can be loaded with any type of agent ranging from drugs to anti-counterfeit agents.

Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:

Abstract: The present invention involves new and original sigma receptors ligands: (Mono-or dialkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl ?-[(adamantyl-1)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or diastereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Asteinizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, antimetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotective and cytoregenerative activity against the cytodegenerative diseases.

Abstract: Embodiments of the present disclosure provide compositions including ketamine analogues, salts, and disalts, pharmaceutical compositions including ketamine analogues, salts, or disalts, methods of treatment of a condition or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

Abstract: The invention relates to novel insecticidal active compound combinations comprising, firstly, cyclic ketoenols or other acaricidally active compounds and, secondly, further insecticidally active compounds from the group of the anthranilamides, which combinations are highly suitable for controlling animal pests, such as insects and unwanted acarids.

Abstract: This invention relates to diterpenes of general formula (1) belonging to labdane class, isolated from Leucas stelligera, being useful for prevention, treatment, inhibition or controlling growth and proliferation of mycobacterial activity in mammals. The invention further discloses process for isolation of the fractions containing the same.

Abstract: The present invention relates to active ingredient combinations which are composed of a known dihydrofuranone derivative on the one hand and of other known active pesticidal ingredients on the other hand, and are suitable for controlling animal pests from the families of the Aleyrodidae, Thripidae, Psyllidae and Agromyzidae, and also, more particularly, from the order of the Acari. The invention also relates to combinations which consist of the abovementioned active ingredient combinations on the one hand and of beneficial species on the other hand and which are suitable for controlling animal pests.

Abstract: The invention relates to a novel compound of the formula or pharmaceutically acceptable salts thereof as well as pharmaceutical, nutraceutical, and botanical drug compositions and therapeutic methods related thereto. In certain embodiments, the compounds are used for the treatment of abnormal cell growth, hyperproliferative disorders, and inflammatory diseases in mammals. In other embodiments, the invention encompasses methods to isolate and synthesize the compounds.

Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

Abstract: The present invention relates to the use of active substance combinations which consist firstly of known cyclic ketoenols and secondly of further known insecticidal active substances, for controlling animal pests from the stink bug family (Pentatomidae).

Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: The present invention relates to the use of active substance combinations for controlling animal pests, for example, from the chinch bug family (Lygaeidae), as well as animal pests that has shown resistance to pyrethroids.

Abstract: Described herein are compounds which exhibit progesterone antagonistic effects and methods of treating cancer using such compounds.

Abstract: The field of the invention relates to stable dosage forms comprising spiro or dispiro 1,2,4-trioxolane antimalarials, or their pharmaceutically acceptable salts, prodrugs and analogues, and processes for their preparation. The water content of the dosage form is not more than 6.5% w/w.

Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the tetronic acid derivatives group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.

Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selective herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, halogen-substituted spirocyclic ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as pesticides and/or fungicides and/or for preventing unwanted plant growth. The invention also relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.