Abstract: The present invention includes novel methods of treating a disease or disorder characterized by hyperactivity of Vps34, and compound as Vps34 inhibitors; particularly compounds of Formula I or a pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Vps34 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.

Abstract: An object is to provide a method for producing a high theobromine-containing composition effectively in a simple way. The method for producing a theobromine-containing composition comprises: (a) performing an extraction of a theobromine-containing plant or a processed product thereof with a solvent, to obtain a crude theobromine extract; (b) applying the crude theobromine extract to a cation exchange resin subjected in advance to hydrogen ion substitution, to allow an adsorption of theobromine onto the cation exchange resin; and (c) passing a solvent containing no ionic substance through the cation exchange resin subsequently to the step (b), to obtain a theobromine eluate.

Abstract: Embodiments of the present invention are directed to porous resins for solid phase extractions. The resins feature at least one hydrophobic component, at least one hydrophilic component and at least one ion exchange functional group. The resins exhibit superior wetting and ion exchange performance.

Abstract: The present invention relates to an N-phenyl-2-pyrimidine-amine derivative showing a superior effect on lung cancer, gastric cancer, colon cancer, pancreatic cancer, hepatoma, prostatic cancer, breast cancer, chronic or acute leukemia, hematologic malignancy, encephalophyma, bladder cancer, rectal cancer, or cervical cancer, etc. of warm-blooded animals and its salt. The present invention also relates to a process for preparing the compound, and to a pharmaceutical composition for the treatment of the above various diseases, which comprises an effective amount of the compound as an active ingredient together with pharmaceutically acceptable inert carriers.

Abstract: The present invention relates to a thermolabile caffeine fraction useful for an efficient Agrobacterium-mediated genetic transformation in plant systems to develop desired traits in plant, and a method of preparing said fraction from tea leaves and also, an efficient and cost-effective method of introducing said Agrobacterium-mediated genetic transformation into plant systems using said caffeine fraction of tea leaves.

Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

Abstract: The invention relates to the use of theobromine and/or its salts and/or its complexes optionally in admixture with other known active ingredients and inert solid or liquid carriers, additives and auxiliary agents for the manufacture of a pharmaceutical composition suitable for relieving cough syndrome. Further subject of the invention is a method of treatment of a human or animal subject being in condition where relieving of cough is desirable which comprise steps of administering in an effective amount theobromine and/or salts and/or its complexes optionally in admixture with other known active ingredients and suitable inert, solid or liquid carriers, additives and auxiliary agents.

Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pylidinedicarboxylic acids.

Abstract: The invention relates to a process for recovering caffeine from caffeine-loaded activated carbon and which is characterized in that the caffeine destroying activity of the activated carbon is reduced before or after loading with caffeine. The activated carbon can to that end be treated with acids, buffers, complexing agents, redox substances, caffeine and other xanthine derivatives. The caffeine recovery yield can be considerably increased by this means.

Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pyridinedicarboxylic acids.

Abstract: The invention relates to a process for recovering caffeine from caffeine-loaded activated carbon using a circulated inert gas sweeping stream held at a temperature of 250.degree. to 460.degree. C., in which process the activated carbon is preheated prior to the desorption of the caffeine with heat sources other than the sweeping gas and held during the desorption step at a uniform temperature or at a temperature increasing from the inlet to the outlet of the inert gas sweeping stream within the range of 250.degree. to 460.degree. C. and the caffeine is subsequently separated from the inert gas sweeping stream by conventional means.

Abstract: Ipoxantine derivatives of general formula (I): ##STR1## both as racemate and chiral forms and the salts thereof with pharmacologically acceptable cations, wherein n is an integer comprised between 2 and 6, and A is the residue of a dipeptide, tripeptide, tetrapeptide and pentapeptide selected, respectively, from the groups consisting of:(a) glycyl-aspartate, alanyl-glycine, glycyl-glycine, aspartyl-arginine, leucyl-arginine;(b) arginyl-lysyl-aspartate, aspartyl-lysyl-arginine, lysyl-prolyl-arginine, prolyl-prolyl-arginine, lysyl-histidyl-glycinamide, prolyl-phenilalanyl-arginine, phenylalanyl-prolyl-arginine;(c) arginyl-lysyl-aspartyl-valine (SEQ ID NO: 1), valyl-aspartyl-lysyl-arginine (SEQ ID NO: 2), threonylvalyl-leucyl-histidyne (SEQ ID NO: 3); and(d) arginyl-lysyl-aspartyl-valyl-tyrosine (SEQ ID NO: 4);are endowed with immunomodulating activity and can be formulated in orally or parenterally administrable pharmaceutical compositions.

Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pyridinedicarboxylic acids.

Abstract: Tea trimmings and wastes are dried and then burned either directly or indirectly to liberate caffeine which is recovery by water scrubbing or electrostatic precipitation. The crude caffeine is then concentrated and purified by crystallization for use in foods and pharmaceuticals.

Abstract: Methods and compositions are provided for treating drug-dependent individuals so as to effect withdrawal from the drug of abuse, e.g., natural and synthetic narcotics, or stimulant-type drugs such as cocaine, amphetamines, nicotine, or the like. The method involves substitution therapy wherein a serotonin antagonist such as ergotamine or a derivative thereof and a CNS stimulant such as caffeine are substituted for the drug of abuse.

Abstract: Disclosed are a compound of the formula (I) or an acid addition salt thereof: ##STR1## wherein Q represents R.sup.1 , R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, n and z are defined as in the specification, preparation method thereof and fungicides containing the same.

Abstract: Substituted cyclohexanols are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.

Abstract: A process for recovering from caffeine-loaded activated carbon by treatment f the loaded carbon with an acid. According to the present invention, activated carbon is treated with a compound having the formula ##STR1## wherein R.sub.1 is methyl, H or Cl, and R.sub.2 is Cl, OH or phenyl.

Abstract: This invention relates to a process for recovering caffeine from laden acated carbon by treating the laden activated carbon with an organic acid. In order to achieve good extraction efficiencies, on the one hand, and to avoid problems with the flash point, such as with acetic acid, on the other hand, the process according to the invention is characterized by treating the activated carbon with a mixture comprising at least 65% by weight of acetic acid and at least 2% by weight of citric acid.

Abstract: A process for the purification of caffeine which comprises carrying out the following steps in any order;(a) recrystallization of caffeine from an aqueous alkaline solution of caffeine containing a reducing agent and(b) extraction of the caffeine from an aqueous alkaline solution of caffeine with a substantially water-immiscible solvent which is liquid under the conditions of the process.

Abstract: The invention relates to a process for separating caffeine from caffeine-loaded active carbon in which a circulated inert gas sweeping stream is passed rectangularly through the stream of active carbon at a temperature of 350.degree. to 450.degree. C., and the caffeine desorbed from the active carbon is precipitated in the form of solid particles by quenching the inert gas sweeping stream, and separated.

Abstract: The invention relates to a process for recovering caffeine adsorbed to activated carbon by treating the loaded activated carbon with formic acid.

Abstract: A process for the purification of caffeine which comprises carrying out the following steps in any order;(a) recrystallization of caffeine from an aqueous alkaline solution of caffeine containing a reducing agent and(b) extraction of the caffeine from an aqueous alkaline solution of caffeine with a substantially water-immiscible solvent which is liquid under the conditions of the process.

Abstract: The recovery of caffeine from activated carbon is accomplished according to the present invention by employing an aqueous acetic acid solution, preferably having a concentration of between about 50 and 80%, by weight, and which is capable of competing for the active sites on the carbon occupied by the caffeine to displace at least a portion of the caffeine which is then dissolved in the solvent. After the desired period of contact, preferably at a temperature above 100.degree. C., the caffeine is separated from the solution.

Abstract: The invention relates to a process for recovering caffeine adsorbed to activated carbon with simultaneous regeneration of the activated carbon in which the caffeine-loaded activated carbon is treated with water at a pressure of at least 86 bar and at a temperature of at least 300.degree. C.

Abstract: The process disclosed herein is capable of decaffeinating green coffee beans at a moisture content near that employed for shipping and storage. The green coffee beans are contacted with dimethyl sulfoxide, an aprotic solvent, to remove at least a portion of the caffeine. The caffeine is preferably removed from the solvent by use of a solid adsorbent such as activated carbon.

Abstract: The process described herein improves the decaffeination of both wet and dry green coffee beans with a liquid or supercritical carbon dioxide extractant by dissolving dimethyl sulfoxide in the extractant prior to contact with the beans. Rates of extraction are greatly improved, especially in the preferred mode where the dimethyl sulfoxide is employed at near saturation levels.

Abstract: A process for producing a decaffeinated vegetable material, such as coffee or tea in aqueous extract or solid form, for use in preparation of beverages, which comprises:(a) contacting a caffeine-containing composition with a liquid, water-immiscible fatty material which is capable of removing caffeine therefrom;(b) maintaining said vegetable material and said fatty material in contact for a time sufficient to transfer caffeine from said vegetable material to said fatty material; and(c) separating the decaffeinated vegetable material from the caffeine-laden fatty material.Other features of the invention are described in the specification.

Abstract: Provided is a method of increasing the purity of amphoteric compound compositions. The method is: (a) providing an amount of a crude amphoteric compound composition, (b) using a portion of the crude composition to prepare in solution a cationic salt of the amphoteric compound, (c) using another portion of the crude composition to prepare in solution an anionic salt of the amphoteric compound, (d) mixing together the solutions wherein a precipitate is formed, and (e) collecting the precipitate which is an amphoteric compound composition of higher purity than the crude composition.

Abstract: Caffeine adsorbed on caffeine adsorbents is recovered by contacting the carbon with a solvent, preferably an aqueous solution of ethylene carbonate or propylene carbonate. The caffeine adsorbent is contacted with the solvent for a period time sufficient to remove at least a portion of the caffeine adsorbed thereon and then separated from caffeine-containing solvent. The caffeine may be recovered from the solvent by precipitation.

Abstract: Caffeine is prepared from theophylline, carbon monoxide and methanol.

Abstract: Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, phenyl, or substituted phenyl having one or more substituents each of which is selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, chloro and dialkylamino wherein the alkyl portions, which can be the same or different, each have 1 to 5 carbon atoms, with the proviso that when R.sub.1 is alkoxy or alkylthio, then R.sub.2 cannot be alkoxy or alkylthio; X and X', which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl, halo, C.sub.1 -C.sub.

Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.

Abstract: Novel 5-aroyl-6-chloro- or 6-bromo-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-7-carboxylic acids represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein Y is chloro or bromo and Ar is an optionally substituted phenyl, 2-furyl, or 2-thienyl ring or a 3-furyl, 3-thienyl, 2-pyrrolyl or 1-alkyl-2-pyrrolyl ring. These compounds are useful as anti-inflammatory, analgesic and antipyretic agents and as smooth muscle relaxants.

Abstract: The object of the invention is to provide an improved process for recovering caffeine adsorbed on activated carbon.Caffeine removed from the commercial decaffeination of vegetable materials and extracts can be effectively removed from the extraction solvent, or can be purified, by the use of activated carbon. Unfortunately, the caffeine is tenaciously held by the carbon and none of the techniques currently available for removing the caffeine is wholly satisfactory.The recovery of caffeine from activated carbon is accomplished according to the present invention by employing a liquid, food-grade caffeine solvent which comprises an organic acid or alcohol, and which is capable of competing for the active sites on the carbon occupied by the caffeine to displace at least a portion of the caffeine which is then dissolved in the solvent. After the desired period of contact, the caffeine is separated from the solvent.

Abstract: A process is disclosed wherein the decaffeination of solutions of caffeine in fatty media is effected with hydrophilic, phenol/formaldehyde polymeric resins having phenolic functional groups. In particular, the solutions are contacted with resin to effect decaffeination and the solvent medium is recovered, whereas the exhausted resin containing adherent caffeine and any non-caffeine solids may be regenerated for re-use. Other features of the invention are described in the specification.

Abstract: Aqueous vegetable extracts such as extracts of tea or green or roasted coffee are decaffeinated by permitting caffeine to diffuse through at least one porous, hydrophilic membrane and a water-immiscible solvent phase and into a water phase. The solvent may be either internal to a single membrane or positioned between two spaced-apart membranes.