Abstract: The present invention includes systems, methods and compositions for the generation of water-soluble cannabinoids in yeast, and other plant cell suspension cultures as well as novel water-soluble cannabinoid compounds. The present invention also includes compositions of matter that may contain one or more water-soluble cannabinoids.

Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.

Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.

Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction. Provided herein are methods for the synthesis of cephalosporin compounds of formula (I) employing a palladium-catalyzed alkylation reaction, as well as compositions related to the same. In an aspect, provided herein is a method for preparing a compound of formula (II), or a salt thereof, comprising the step of admixing, e.g., reacting, a compound of formula (III), or a salt thereof, with a nucleophile (Nuc) in the presence of reagents comprising: (a) a palladium source; and (b) a palladium-binding ligand, to form a compound of formula (II), or a salt thereof.

Abstract: The present invention provides an acid addition salt or a sodium salt of a compound represented by the formula (IA): or their hydrate or a stable crystalline solid thereof. The salt or the crystalline solid is extremely useful as an active ingredient for the production of a pharmaceutical product.

Abstract: The present invention relates to a stable pharmaceutical composition comprising a compound represented by formula (I), its pharmaceutically acceptable salt or a solvate thereof. The stable pharmaceutical composition can be prepared by comprising 1) a compound represented by formula (I), its pharmaceutically acceptable salt, or a solvate thereof, 2) one or more selected from the group consisting of alkali metal chlorides, alkaline earth metal chlorides, transition metal chlorides and magnesium chloride; and 3) sugar and/or a sugar alcohol.

Abstract: The invention relates to processes for the production of intermediates for preparing 2-alkyl cephem compounds useful as antimicrobial drugs. The invention provides a process which comprises oxidating a compound of the formula (I) or a salt thereof to give a compound of the formula (II) or a salt thereof wherein each symbol is as defined in the specification.

Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil via intermediates of Formulae (1), (3) or (4) of this process.

Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: Novel solid forms of ceftolozane are described, as well as methods for the preparation and use of these solid forms.

Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil as well as to a intermediates of this process.

Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.

Abstract: The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.

Abstract: A diluted solution of ceftiofur sodium is intrathecally or ventricularly delivered to effectively treat bacterial meningitis while maintaining the patient's threshold and reducing the likelihood of seizure.

Abstract: A novel process for purifying Cefmenoxime hydrochloride comprises: 1) adding a solvent wherein Cefmenoxime hydrochloride is insoluble at the temperature less than 30° C., filtering after vigorous stirring, washing the filter cake with a solvent wherein Cefmenoxime hydrochloride is insoluble at a temperature less 20° C., and drying; 2) placing the filter cake into ammonium hydroxide, controlling the pH value less than 9 with a gentle agitation to obtain Cefmenoxime acid solution in ammonium hydroxide, and then filtering out the precipitate; 3) adding hydrochloric acid at a concentration of 0.5-4 mol/L to Cefmenoxime acid solution in ammonium hydroxide slowly and controlling the temperature between 30-60° C. and the final pH between 0.5-3.0, and then cooling down to a minimum of 10° C. and standing still to allow crystallization, filtrating and vacuum drying.

Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.

Abstract: A novel process for refining Ceftizoxime sodium compound, comprises the steps of: 1) dissolving crude Ceftizoxime sodium in water, and extracting with cyclohexane or ethyl acetate, followed by separating the organic phase containing impurities, producing an aqueous phase containing Ceftizoxime sodium; 2) adding ammonia or ammonium hydroxide into the above aqueous phase while stirring, followed by filtrating the precipitate, producing an aqueous filtrate containing Ceftizoxime sodium; 3) adding an alcoholic solvent in the aqueous solution and recrystallizing under controlled temperature, followed by centrifuging and washing the resultant crystals, producing the refined Ceftizoxime sodium after drying; and 4) optionally returning the mother liquid of the recrystallization process to step 3).

Abstract: A method for increasing ozone concentration in a liquid can include: providing a gas having ozone; introducing the ozone-containing gas into a liquid, wherein the liquid and ozone combination has a temperature between about 0.8 and about 1.5 times the critical temperature of ozone; and increasing isothermally, the pressure of the ozone-containing gas above the liquid to about 0.3 to about 5 times the critical pressure of ozone so as to increase the ozone concentration in the liquid. The temperature is expressed in absolute units (Kelvin or Rankin). The method can be used for removing ozone from a gas or for purifying ozone. The liquid having a high ozone concentration can be used for ozonolysis of a substrate.

Abstract: Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.

Abstract: A novel process for refining Ceftizoxime sodium compound, comprises the steps of: 1) dissolving crude Ceftizoxime sodium in water, and extracting with cyclohexane or ethyl acetate, followed by separating the organic phase containing impurities, producing an aqueous phase containing Ceftizoxime sodium; 2) adding ammonia or ammonium hydroxide into the above aqueous phase while stirring, followed by filtrating the precipitate, producing an aqueous filtrate containing Ceftizoxime sodium; 3) adding an alcoholic solvent in the aqueous solution and recrystallizing under controlled temperature, followed by centrifuging and washing the resultant crystals, producing the refined Ceftizoxime sodium after drying; and 4) optionally returning the mother liquid of the recrystallization process to step 3).

Abstract: A novel process for purifying Cefmenoxime hydrochloride comprises: 1) adding a solvent wherein Cefmenoxime hydrochloride is insoluble at the temperature less than 30° C. filtering after vigorous stirring, washing the filter cake with a solvent wherein Cefmenoxime hydrochloride is insoluble at a temperature less 20° C., and drying; 2) placing the filter cake into ammonium hydroxide, controlling the pH value less than 9 with a gentle agitation to obtain Cefmenoxime acid solution in ammonium hydroxide, and then filtering out the precipitate; 3) adding hydrochloric acid at a concentration of 0.5-4 mol/L to Cefmenoxime acid solution in ammonium hydroxide slowly and controlling the temperature between 30-60° C. and the final pH between 0.5-3.0, and then cooling down to a minimum of 10° C. and standing still to allow crystallization, filtrating and vacuum drying.

Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.

Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein A1, A2, L1 and B are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

Abstract: The present invention provides a compound the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: A method for increasing ozone concentration in a liquid can include: providing a gas having ozone; introducing the ozone-containing gas into a liquid, wherein the liquid and ozone combination has a temperature between about 0.8 and about 1.5 times the critical temperature of ozone; and increasing isothermally, the pressure of the ozone-containing gas above the liquid to about 0.3 to about 5 times the critical pressure of ozone so as to increase the ozone concentration in the liquid. The temperature is expressed in absolute units (Kelvin or Rankin). The method can be used for removing ozone from a gas or for purifying ozone. The liquid having a high ozone concentration can be used for ozonolysis of a substrate.

Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders.

Abstract: The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R3, R6, R7, R8, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.

Abstract: The present invention provides BACE inhibitors of Formula I: methods for their use, intermediates, and methods for their preparation.

Abstract: The present invention provides a cyclic amine compound represented by formula (I) (in formula (I), Cy1 and Cy2 independently represent a C6-10 aryl group or a heterocyclyl group; R1a to R5a independently represent a hydrogen atom or an unsubstituted or substituted C1-6 alkyl group; R10, R11, R20 and R21 independently represent an unsubstituted or substituted C1-6 alkyl group, an unsubstituted or substituted C1-6 alkoxy group, a halogen atom or the like; m, n, p, and r each represent an integer of 0 to 5; and Y represents an oxygen atom or the like) or salt thereof, and an acaricide including the same.

Abstract: The present invention provides novel cephalosporin derivatives of formula I, their analogues, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.

Abstract: The present invention relates to an agent for treating or preventing disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound of formula (I), wherein, R1, R2a, R2b R3, R4a, R4b, ring A, and dashed line are described in this specification, its pharmaceutically acceptable salt or a solvate thereof.

Abstract: Antibacterial compounds including 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives are provided, and methods of treatment or prevention of bacterial infection with such compounds are provided.

Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.

Abstract: The present invention provides nitrogen and sulfur-containing heterocycle compounds to be used as scaffolds and, in particular, nitrogen and sulfur-containing heterocycle compounds having a thiomorpholine core. The compounds herein described may be useful in treating diseases such as diabetes, obesity, cancer, cardiovascular, Alzheimer's, inflammatory, antidepressant, rheumatoid arthritis, multiple sclerosis, allergic rhinitis, asthma as well as viral and bacterial infections. The compounds herein described may also be useful in treating CNS disorders such as but not limited to Schizophrenia, Alzheimer's disease (AD).

Abstract: Polymorphs of Ceftiofur sodium as a crystalline product and a process for the preparation of polymorphs of crystalline Ceftiofur sodium of formula (I).

Abstract: Disclosed is a compound represented by General formula (I), a pharmaceutically acceptable salt thereof, or a solvate of the compound or the pharmaceutically acceptable salt, which has an inhibitory activity of the production of A? or a BACE1-inhibiting activity, and is therefore useful as a prophylactic or therapeutic agent for A?-induced neurodegenerative diseases typified by Alzheimer-type dementia. Wherein the ring A represents a C6-14 aryl group or the like; L represents —NReCO— [wherein Re represents a hydrogen atom or the like] or the like; the ring B represents a C6-14 aryl group or the like; X represents a C1-3 alkylene group or the like; Y represents a single bond or the like; Z represents a C1-3 alkylene group or the like; R1 and R2 independently represent a hydrogen atom or the like; and R3, R4, R5 and R6 independently represent a hydrogen atom, a halogen atom or the like.

Abstract: Disclosed is a method of dyeing keratin-containing fibers comprising treating the fiber with at least one compound of formula (1), wherein R1, R2, R3, R4 independently from each other are hydrogen; hydroxy; —S—H; —S—C1-C12alkyl; halogen; C1-C12alkyl or C1-C12alkoxy, which may be substituted by one or more C1-C5alkyl, C1-C5-alkoxy, hydroxy, —(CO)—H or —(CO)—C1-C5alkyl; —NR5R6; —NO2; —(CO)H or (CO)—C1-C5alkyl; C6-C12aryl, C6-C12aryl-C1-C4alkyl or C6-C12aryl-C1-C4alkoxy, wherein the aryl moiety may be substituted by one or more C1-C5alkyl, C1-C5alkoxy, —(CO)—H or —(CO)—C1-C5alkyl; R5 and R6 independently from each other are hydrogen; hydroxy; C1-C12alkyl; hydroxy-C1-C12alkyl; —(CO)—H; —(CO)—C1-C5alkyl; phenyl or phenyl-C1-C5alkyl, wherein the phenyl moiety may be substituted by one or more C1-C5alkyl, C1-C5alkoxy, halogen, —NH2, mono-C1-C5alkylamino, di-C1-C5alkylamino, —NO2, carboxy or hydroxy; and An is an anion.

Abstract: The invention relates to novel N-heterocyclylphenyl-substituted cyclic ketoenols of the formula (I) in which CKE, W, X, Y and Z are as defined in the disclosure, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides. The invention further relates to selective herbicidal compositions comprising firstly the N-heterocyclylphenyl-substituted cyclic ketoenols and secondly a compound which improves crop plant tolerance.

Abstract: Non-peptidic renin inhibitors nitroderivatives of general formula (I): A1-(Xa—ONO2)j ??(I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndrome.

Abstract: Cobalt (II) complexes of porphyrins are effective catalysts for intramolecular nitrene insertion of C—H bonds with arylsulfonyl azides. The cobalt-catalyzed process can proceed efficiently under mild and neutral conditions in low catalyst loading without the need of other reagents or additives, generating nitrogen gas as the only byproduct.

Abstract: Provided herein are imaging methods for detecting, diagnosing and imaging pathogenic bacteria or a pathophysiological condition associated therewith using fluorescent, luminescent or colorimetric detection agents, e.g., fluorogenic substrates for bacterial enzymes, caged luciferins and fluorescent proteins, luciferases and enzymes expressed by recombinant bacteria. Signals emitted by the fluorescent, luminescent or colorimetric detection agents in the presence of the bacteria are compared to controls to detect and locate the pathogenic bacteria. Also provided is a method for screening therapeutic agents to treat the pathophysiological conditions by measuring fluorescence or luminescence emitted from the detection agents in the presence and absence of the potential therapeutic agent. In addition, a method for detecting a pathogenic bacteria via PET or SPECT imaging using a positron-emitting or gamma-emitting substrate for a beta-lactamase or other enzyme or protein of the pathogenic bacteria.

Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Abstract: This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.

Abstract: Disclosed is a method of dyeing keratin-containing fibers comprising treating the fiber with at least one compound of formula (1), wherein R1, R2, R3, R4 independently from each other are hydrogen; hydroxy; —S—H; —S—C1-C12alkyl; halogen; C1-C12alkyl or C1-C12alkoxy, which may be substituted by one or more C1-C5alkyl, C1-C5-alkoxy, hydroxy, —(CO)—H or —(CO)—C1-C5alkyl; —NR5R6; —NO2; —(CO)H or (CO)—C1-C5alkyl; C6-C12aryl, C6-C12aryl-C1-C4alkyl or C6-C12aryl-C1-C4alkoxy, wherein the aryl moiety may be substituted by one or more C1-C5alkyl, C1-C5alkoxy, —(CO)—H or —(CO)—C1-C5alkyl; R5 and R6 independently from each other are hydrogen; hydroxy; C1-C12alkyl; hydroxy-C1-C12alkyl; —(CO)—H; —(CO)—C1-C5alkyl; phenyl or phenyl-C1-C5alkyl, wherein the phenyl moiety may be substituted by one or more C1-C5alkyl, C1-C5alkoxy, halogen, —NH2, mono-C1-C5alkylamino, di-C1-C5alkylamino, —NO2, carboxy or hydroxy; and An is an anion.

Abstract: 1H-Pyrrolo-1,4-thiazines and a process for the preparation thereof are described. These compounds are useful as enzyme inhibitors in cells, particularly for medical uses.

Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.

Abstract: Disclosed are thiol dyes of formula (1), wherein R1 is hydrogen; C1-C12alkyl; or phenyl-C1-C4alkyl; X is C1-C12alkylene; C2-C12alkenylene; C5-C10cycloalkylene; C5-C10arylene; or C5-C10arylene-C1-C10alkylene; Y is the residue of an organic dye which corresponds to the formula (1a), wherein R2 is hydrogen; or C1-C5alkyl; R3 is a radical of formula (1a1): (1a2); or (1a3); or R2 and R3 together with the linking carbon atom 1C form a 6 to 10 membered carbocyclic ring which may optionally be a condensated aromatic system and may contain one or more than one hetero atom; and R4, R5 and R6 independently form each other are hydrogen, or C1-C5alkyl; Z is H; or a thio ester group of formula (1b), wherein A is O; S; or N—R9; B is —OR7; —NR7R8, or —SR7; and A is O; S; or N—R9; B is —OR7; —NR7R8, or —SR7; and R7, R8 and R9, independently from each other are hydrogen; C1-C12alkyl C6-C12aryl; or C6-C12aryl-C1-C12alkyl.

Abstract: A method for increasing ozone concentration in a liquid can include: providing a gas having ozone; introducing the ozone-containing gas into a liquid, wherein the liquid and ozone combination has a temperature between about 0.8 and about 1.5 times the critical temperature of ozone; and increasing isothermally, the pressure of the ozone-containing gas above the liquid to about 0.3 to about 5 times the critical pressure of ozone so as to increase the ozone concentration in the liquid. The temperature is expressed in absolute units (Kelvin or Rankin). The method can be used for removing ozone from a gas or for purifying ozone. The liquid having a high ozone concentration can be used for ozonolysis of a substrate.

Abstract: Tricyclic nitrogen containing compounds of formula (I) and their use as antibacterials.