Abstract: The present disclosure provides a novel sweetener composition of improved taste of the sweetener (e.g., reduced bitterness and/or astringency, and improved overall sweet quality of the composition); food and beverage products containing the same; and methods of making the same.

Abstract: The invention disclosed herein relates to methods and means for allocating, allotting, apportioning, dispensing, distributing, preparing, portioning, meting out and/or otherwise providing, controlling and/or regulating access to quantities of foods, beverages, and/or other substances. Various embodiments of the methods and means of the invention may be performed by and/or implemented in hardware, in software, by one or more entities, and/or by some combination of hardware, software and/or one or more entities.

Abstract: The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.

Abstract: The invention relates to novel cells and cell lines, and methods for making and using them.

Abstract: A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1?6-benzo[d]isothiazol-3-one, preferably in the presence of an organic base.

Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.

Abstract: Provided are processes for the preparation of N-(2-acetyl-4,6-dimethylphenyl)-3-{[(3,4 dimethyl-5-isoxazolyl)amino]sulfonyl}-2-thiophenecarboxamide, a compound useful for the treatment of endothelin-mediated disorders.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: A process for the synthesis of an oligonucleotide is provided in which an oligonucleotide is assembled on a swellable solid support using the phosphoramidite approach in the presence of an activator, wherein the activator is not tetrazole or a substituted tetrazole. Preferred activators are pyridinium, imidazolinium and benzimidazolinium salts; benzotriazole and derivatives thereof; and saccharin or a saccharin derivative. Preferred swellable solid supports comprise functionalised polystyrene, partially hydrolysed polyvinylacetate or poly(acrylamide).

Abstract: A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1?6-benzo[d]isothiazol-3-one, preferably in the presence of an organic base.

Abstract: Multifunctional compounds having acylsulfonamide amine-reactive groups are described that can be used for the capture of amine containing materials.

Abstract: The invention relates to a method for isolating and purifying (1RS,2RS)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol as a saccharinate from a mixture of the diastereomers (1SR,2)RS-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol and (1SR-2RS)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol and optionally impurities.

Abstract: Disclosed are a compound of tramadol and a sugar substitute, pharmaceutical compositions and sustained-release formulations comprising the compound, and methods of treatment using the compound. The tramadol compound according to the present invention has reduced bitter taste of tramadol and is more acceptable to the patient.

Abstract: A positive resist composition comprising (A) a compound generating a specific sulfonimide compound by irradiation with an actinic ray or a radiation and (B) a resin having a group, which is decomposed by the action of an acid to increase the solubility of the composition in an alkali developer. The resist composition has an improved resolving power and an improved process allowance such as exposure margin and the depth of focus in a lithographic technique using a light source of short wavelengths capable of super fine working and a positive chemically amplified resist.

Abstract: Novel amides and imides are inhibitors of tumor necrosis factor&agr; and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions.

Abstract: The present application relates to saccharin-5-carbonyl derivatives of the formula I in which the substituents have the following meanings: L is C1-C6-alkyl, C1-C6-alkoxy; Z is C1-C6-alkyl, C3-C8-cycloalkyl, C3-C6-alkenyl, C3-C5-alkynyl, phenyl-C1-C6-alkyl or phenyl, where the phenyl rings are in each case optionally mono- or polysubstituted by C1-C6-alkyl, C1-C6-alkoxy or halogen; M is hydrogen, C1-C6-alkyl, C1-C6-alkoxy, halogen, cyano, nitro or halo-C1-C6-alkyl; R1, R2, R3, R4, R5, R6, R7, R8 are hydrogen, C1-C6-alkyl; and agriculturally utilizable salts of the compound I.

Abstract: Cyclic amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 3-phenyl-3-(1-oxoisoindolin-2-yl)propionamide.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: This invention provides sweetener blends comprising N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine 1-methyl ester and another sweetener. The sweetener blends of this invention exhibit isobole synergy.

Abstract: A process for preparing saccharincarbonyl halides of the formula 1 ##STR1## where: X is halogen,R.sup.1, R.sup.2 are each hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy, optionally C.sub.1 -C.sub.4 -alkyl-, fluorine- or C.sub.1 -C.sub.4 -alkoxy-substituted benzyl or phenyl,R.sup.3 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl or phenyl or benzyl which is optionally mono- or polysubstituted by C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -haloalkyl or C.sub.1 -C.sub.4 -alkoxy,by reaction of an isophthalylsulfonamide 2 with an inorganic acid halide to give the saccharincarbonyl halide 1 ##STR2## is described.

Abstract: "Esters" are synthesized by reacting a nucleophile with a propargyl xanthate advantageously having the formula (I):R.sub.3 --C.tbd.C--CR.sub.1 R.sub.2 --S--CS--Y--R (I)in the presence of at least one acid, Bronsted or otherwise, and at a temperature ranging from 0.degree. to 300.degree. C.; the subject reaction is particularly applicable to a wide variety of chiral organic syntheses.

Abstract: A general-purpose organic rust initiator which can effectively prevent corrosion of metals comprising a compound of formula (1): ##STR1## wherein R.sub.1 is a perfluoroalkyl group having 1 to 6 carbon atoms; R.sub.2 is a hydrogen atom or a group defined for R.sub.1 ; R.sub.4 is an acid group selected from --OH, --COOH, --SH, --SO.sub.2 OH, --PO(OH).sub.2, --SCH.sub.2 COOH, --SO.sub.2 NHCH.sub.2 COOH or a salt thereof; R.sub.3 is a hydrogen atom or a group defined for R.sub.4 ; or R.sub.3 and R.sub.4 together form an acid group selected from --N.dbd.N--NH--, --CH.dbd.N--N--, --SO.sub.2 --NH--CO--, --S--C(SH).dbd.N-- or a salt thereof.

Abstract: 4-R.sup.4 --R.sup.5 -2-Saccharinylmethyl aryl and aryloxy acetates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 --R.sup.5 -2-halomethylsaccharin with an aryl or aryloxyacetic acid in the presence of an acid-acceptor.

Abstract: Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2;L-R.sup.1 is a leaving group, H-L-R.sup.1 is the conjugate acid thereof and, when L is N, H-L-R.sup.1 has a pK.sub.a value less than or equal to 6, when L is O, H-L-R.sup.1 has a pK.sub.a value less than or equal to to 8, and when L is SO.sub.n, H-L-R.sup.1 has a pK.sub.a value less than or equal to 5;R.sup.2 is primary or secondary alkyl of two to four carbon atoms, primary alkylamino of one to three carbon atoms, primary alkylmethylamino of two to four carbon atoms, diethylamino or primary alkoxy of one to three carbon atoms; andR.sup.

Abstract: The incorporation of the heterocyclic saccharin functionality into the alkenylsuccinimide dispersant structures via the Mannich alkylaminoalkylation procedure provides a class of ashless non-phosphorus dispersants with multifunctional antiwear, antioxidant and corrosion inhibiting properties in lubricant compositions.

Abstract: 4-R.sub.1 -R.sub.2 -R.sub.3 -2-Saccharinylmethyl and 4,7-C-4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.

Abstract: Pigment preparation essentially comprisinga) at least one pigment from the class of azo, anthrapyrimidine, anthanthrone, quinacridone, perinone, diketopyrrolopyrrole, dioxazine, flavanthrone, indanthrone, isoindolinone, isoviolanthrone, perylene, phthalocyanine, pyranthrone or thioindigo pigments or a mixture of pigments belonging to various classes, andb) at least one dispersant of the formula (I) ##STR1## in which P, independently of the pigments mentioned in a), is a radical of an anthanthrone azo, quinacridone, perinone, diketopyrrolopyrrole, dioxazine, indanthrone, perylene, phthalocyanine or thioindigo pigment,R.sup.1 and R.sup.2, independently of one another, are hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.

Abstract: This invention concerns a new process for the catalytic carbonylation of certain aryl halides or aryl tosylates to amides by use of a complex of palladium and at least one ligand. More specifically, the invention concerns carbonylation of halogenoaromaticsulfonamides or tosylatoaromaticsulfonamides to saccharin, saccharin analogues or their salts.

Abstract: Fungicidal bisazolyl-hydroxyalkyl derivatives of the formula ##STR1## in which Ar stands for optionally substituted aryl,X stands for a grouping --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --SCH.sub.2 -- or --SH.dbd.CH--,Y stands for a nitrogen atom or the grouping CR.sup.3,R.sup.1, R.sup.2 and R.sup.3 stand for hydrogen, halogen or methyl, andn stands for the numbers 0, 1 or 2,and acid addition salts and metal salt complexes thereof. Intermediates of the formulas ##STR2## are also new.

Abstract: The aluminum salt of saccharin and a method for its preparation are disclosed. Chewing gum compositions comprising the novel salt are prepared.

Abstract: 1,2-benzoisothiazol-3(2H)-one, 1,1-dioxide, ion(1-),2-hydroxy-N,N,N-trimethyl-ethanaminium represented by the following formula (I): ##STR1## is found to have great utility as an effective component in plant protection agents for control of fungi and bacteria. By the use of the compound, diseases or blights of plants can be effectively prevented.

Abstract: Fungicidal saccharine salts of substituted hydroxypropylamines of the formula ##STR1## in which R.sup.1 is optionally substituted phenyl, phenoxy, phenylthio, phenylalkyl, phenoxyalkyl, or phenylthioalkyl, or optionally substituted cyclohexyl, cylohexyloxy, cyclohexylalkyl, cyclohexyloxyalkyl or cyclohexylthioalkyl,R.sup.2 is hydrogen or methyl,R.sup.3 is methyl or ethyl, andR.sup.4 and R.sup.5 each independently is alkyl or alkenyl, orR.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, are an optionally substituted saturated heterocyclic radical which can optionally contain further hetero atoms.

Abstract: Fungicidally active novel saccharine salts of substituted amines of the formula ##STR1## in which A represents in each case optionally substituted 2-decahydronaphthyl or .beta.-naphthyl andR.sup.1 and R.sup.2 independently of one another in each case represent alkyl or alkenyl or, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can contain further heteroatoms.

Abstract: Fungicidally active novel saccharine salts of aminomethyl heterocyclic compounds of the formula ##STR1## in which R represents optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted thienyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents alkyl,R.sup.3 represents alkyl andR.sup.4 represents alkyl, alkenyl or alkinyl, orR.sup.3 and R.sup.4, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical which can contain further hetero atoms,X represents oxygen or sulphur,Y represents oxygen, sulphur or the methylene group,m represents 0 or 1 andn represents 0 or 1.

Abstract: Fungicidally active saccharine salts of substituted amines of the formula ##STR1## in which A represents in each case optionally substituted cyclohexyl, cyclohexenyl or phenyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl,R.sup.3 and R.sup.4 independently of one another represent alkyl or, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical which can contain further hetero atoms andn represents the number 0 or 1.

Abstract: Fungicidally active aminomethyltetrahydrofurans of the formula ##STR1## in which A represents a divalent alkylene or alkenylene chain which is in each case optionally substituted andR.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, dialkoxyalkyl, hydroxyalkyl, hydroxyalkoxyalkyl, dioxolanylalkyl, oxolanylalkyl, or dioxanylalkyl, or represent in each case optionally substituted cycloalkylalkyl, cycloalkyl, aralkyl, aralkenyl or aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can optionally contain further heteroatoms,or an acid addition salts thereof. Some intermediates therefor wherein NR.sup.1 R.sup.2 is replaced by halogen or sulphonyloxy are also new.

Abstract: The invention is a process for the preparation of a N- or S-1,2-ethylenically unsaturated organic compound which comprises(a) contacting a N- or S-silylated organic compound with an aldehyde, wherein the aldehyde has a hydrogen atom bonded to the carbon adjacent to the carbonyl moiety, at elevated temperatures under conditions such that a N- or S-1-siloxyalkyl-substituted organic compound is prepared; and(b) pyrolyzing the N- or S-1-siloxyalkyl-substituted organic compound under conditions such that the siloxy moiety is elminated to prepare a N- or S-1,2-ethylenically unsaturated compound.

Abstract: Denatonium saccharide, which has a vile, bitter taste, is applied to protect an article against gnawing, biting, licking, and feeding by various animals.

Abstract: The specification describes a process for preparing 4-hydroxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide, a sweetener, from 1,2-benzisothiazol-3(2H)-one-1,1-dioxide by anodic oxidation in the presence of trifluoroacetic acid or trifluoromethanesulfonic acid and, optionally, in the presence of salts which increase the conductivity. The oxidation is effected in an anhydrous medium and the 4-trifluoroacetoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide formed as an intermediate when, for example, trifluoroacetic acid is used is decomposed with water to obtain the desired end product.

Abstract: A process for the preparation of saccharin by reacting an aqueous hydrochloric acid solution of o-methoxycarbonylbenzenediazonium chloride with sulfur dioxide, wherein(a) the aqueous diazonium salt solution is reacted with sulfur dioxide at from 0.degree. to 100.degree. C. in the presence of a water-immiscible or only partially water-miscible inert organic solvent,(b) in order to decompose the diazonium salt, the reaction mixture is treated simultaneously or subsequently with a diazonium salt decomposition catalyst,(c) the aqueous organic reaction mixture, or the organic phase obtained after removing the aqueous phase, is treated with an oxidizing agent at from 0.degree. to 100.degree. C. and(d) the organic phase is reacted with aqueous ammonia at from 0.degree. to 50.degree. C. and the saccharin is isolated from the aqueous phase in a conventional manner by acidifying with a strong acid.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxyl, and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as sweetening agents.

Abstract: The invention relates to a process for the preparation of carbamic acid phenyl esters of the formula (I) ##STR1## by acylating phenol derivatives of the formula (II) ##STR2## wherein R is alkyl having 1 to 8 carbon atoms, aryl, cycloalkyl having 5 or 6 carbon atoms, aralkyl having 7 to 16 carbon atoms which groups can be substituted by one or more alkyl groups,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms or acylamino,R.sup.2 is hydrogen, halogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, or ifR.sup.1 and R.sup.2 represent alkyl and/or alkoxy, they can form together a carbocyclic ring.According to the invention the phenol derivatives of the general formula (II), wherein R.sup.1 and R.sup.2 are as defined above, are reacted with N-carbamoyl-saccharin derivatives of the formula (IV) ##STR3## wherein R has the same meaning as defined above, in the presence of a base.

Abstract: A process is disclosed for preparing a carbamic acid phenyl ester of the formula (I) ##STR1## wherein R is alkyl having 1 to 8 carbon atoms, aryl, cycloalkyl having 5 or 6 carbon atoms, or aralkyl having 7 to 16 carbon atoms, wherein the aryl, cycloalkyl or aralkyl is unsubstituted or substituted by at least one alkyl group having 1 to 8 carbon atoms;R.sub.1 is hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, cyanomethyl, 1,3-dioxolan-2-yl, or carboalkoxyamino wherein the alkoxy group contains 1 to 4 carbon atoms;R.sub.2 is hydrogen, halogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms; orR.sub.1 and R.sub.2 form together a carbocyclic ring or a heterocyclic ring fused to the phenyl ring wherein the carbocyclic ring of the heterocyclic ring is unsubstituted or substituted by at least one alkyl having 1 to 8 carbon atoms, which comprises acylating a phenol of the formula (II) ##STR2## with a compound of the formula (IV) ##STR3## in the presence of a base.

Abstract: Members of the urea cycle, i.e. urea, ornithine, arginine and citrulline have been found to reduce the toxicity of saccharin.

Abstract: 1,4-Bis(2'-haloethyl)-1,4-diazabicyclo[2.2.1]-heptane derivatives, such as diperchlorate, dichloride, diacetate, dibenzoate, diascorbate, disalicylate, ditartrate, disaccharin, dihydrogen dimaleate, together with ethyl sulfonate and periodate.

Abstract: A method of preparing 2-sulfochloride benzoates which comprises diazotizing any anthranilate to form a 2-diazonium chloride benzoate and thereafter reacting said 2-diazonium chloride benzoate with sulfur dioxide to form a 2-sulfochloride benzoate. The invention also provides for the total synthesis of saccharin which comprises pyrolyzing a 2-sulfochloride benzoate to form an o-sulfobenzoic anhydride and then ammonolyzing the o-sulfobenzoic anhydride to saccharin which is free of bitter tasting contaminants from such reactants.