Abstract: A sulfonic acid salt composition includes compounds of formula (I), wherein n is 1 or 2, R1 is H or C1-C6 alkyl, R2 is COOM, SO3M or CH(OH)SO2—OM, each M is an equivalent of a multivalent metal, preferably magnesium, calcium, aluminum, zinc and combinations thereof. The molar ratio of a compound wherein n is 1 to a compound wherein n is 2 is below 0.1. The sulfonic acid salt composition is useful for color stabilization of non-living organic matter such as from lacquers, paints, powder-coatings, and polymers in particular water-absorbent polymers.

Abstract: The present invention in one embodiment provides a process of generating chlorine dioxide by reacting formamidinesulfinic acid (FSA) and sodium chlorite in an aqueous solution.

Abstract: Cell culture media comprising antioxidants are provided herein as are methods of using the media for cell culturing and polypeptide production from cells. Compositions comprising polypeptides, such as therapeutic polypeptides, produced by the methods herein are also provided.

Abstract: A method of inhibiting enzymatic browning in food involves the contacting of hypotaurine, a salt of hypotaurine or an equivalent of hypotaurine with the food. The hypotaurine can be provided from solution, an extract, or in solid form to a food that can loose its appeal to a consumer due to browning, such as cut fruits and vegetables, seafood, or a beverage. The antibrowning agent can be applied to the food by spraying, dusting, dipping, or dissolving, depending upon the form of the food to which the agent is added.

Abstract: A chemically amplified positive resist composition comprises an acid-decomposable keto ester compound of steroid skeleton which is insoluble in alkaline developer, but turns soluble in alkaline developer under the action of acid. The composition is exposed to EB, deep-UV or EUV and developed to form a pattern with a high resolution and improved LER.

Abstract: A drug delivery system (DDS) for administration of a water soluble, cationic, and amphiphilic pharmaceutically active substance (API) which DDS comprises amorphous particles of <100 nm of a poorly water soluble complex of the API with a Na-salt of N-all-trans-retinoyl cysteic acid methyl ester and/or a Na-salt of N-13-cis-retinoyl cysteic acid methyl ester, which particles are entrapped in nanoparticles formed a Na-salt of N-all-trans-retinoyl cysteic acid methyl ester and/or a Na-salt of N-13-cis-retinoyl cysteic acid methyl ester, the w/w-ratio of Na-salt of N-alltrans-retinoyl cysteic acid methyl ester and/or a Na-salt of N-13-cis-retinoyl cysteic acid methyl ester to the complex is about 0.5:1 to about 20:1. A pharmaceutical composition comprising such a DDS. Methods for preparation of such a DDS and such a pharmaceutical composition. Use of such a DDS and pharmaceutical composition for treatment of cancer.

Abstract: This invention relates to sulfur based compounds useful in methods of carbon dioxide or sulfur dioxide removal.

Abstract: A method of inhibiting enzymatic browning in food involves the contacting of hypotaurine, a salt of hypotaurine or an equivalent of hypotaurine with the food. The hypotaurine can be provided from solution, an extract, or in solid form to a food that can loose its appeal to a consumer due to browning, such as cut fruits and vegetables, seafood, or a beverage. The antibrowning agent can be applied to the food by spraying, dusting, dipping, or dissolving, depending upon the form of the food to which the agent is added.

Abstract: Superabsorbents comprising a compound of the formula (I) in which M is a hydrogen atom, an ammonium ion, a monovalent metal ion or one equivalent of a divalent metal ion of groups 1, 2, 8, 9, 10, 12 or 14 of the periodic table of the elements; R1 is OH or NR4R5 where R4 and R5 are each independently H or C1-C6-alkyl; R2 is H or an alkyl, alkenyl, cycloalkyl or aryl group, where this group optionally has 1, 2 or 3 substituents which are each independently selected from C1-C6-alkyl, OH, O—C1-C6-alkyl, halogen and CF3; and R3 is COOM, SO3M, COR4, CONR4R5 or COOR4, where M, R4 and R5 are each as defined above or, when R2 is aryl which is optionally substituted as specified above, are also H, salts thereof or mixtures of such compounds and/or salts thereof, exhibit improved stability to discoloration in the course of storage under elevated temperatures and/or elevated air humidity.

Abstract: Compositions are provided that include an electron donor and a sensitizing compound. More specifically, the electron donor is an arylsulfinate salt. Methods of polymerization are also provided that can be used to prepare polymeric material from a photopolymerizable composition that includes ethylenically unsaturated monomers and a photoinitiator system. The photoinitiator system includes an electron donor and a sensitizing compound.

Abstract: Intermediates useful in the preparation of the antiviral agent entecavir are disclosed. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various processes useful in the preparation of entecavir are also disclosed.

Abstract: The present invention relates to processes for the preparation of a compound of the formula wherein W is nitrogen or —CR3; R1 is halogen, haloalkyl, haloalkoxy, R4S(O)n— or —SF5; R2 is hydrogen or halogen; R3 is halogen; R4 is alkyl or haloalkyl; and n is 0, 1 or 2; and processes for using a compound of the formula (I) in the synthesis of compounds of the formula

Abstract: Processes are disclosed for preparing the antiviral agent entecavir. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various intermediates useful in the preparation of entecavir are also disclosed.

Abstract: A group of new compounds, N-(all-trans-Retinoyl)-L-cysteic acid, N-(13-cis-Retinoyl)-L-cysteic acid, N-(all-trans-Retinoyl)-L-cysteinesulfinic acid, N-(13-cis-Retinoyl)-L-cysteinesulfinic acid, N-(all-trans-Retinoyl)-L-homocysteic acid, N-(13-cis-Retinoyl)-L-homocysteic acid, and sodium salts of these compounds, including sodium salts of their esters and amides, is shown to exhibit therapeutic effects per se, and which compounds in combination with cytotoxic compounds, such as docetaxel, paclitaxel, doxorubicin and mitoxantrone, exhibit a synergistic effect. These compounds make it possible to manufacture new formulations of poorly soluble pharmaceutical compounds, and the present invention discloses a process of manufacturing water-soluble formulations of such compounds, exemplified by docetaxel, and paclitaxel, exhibiting enhanced pharmacological activity, and formulations of water-soluble pharmaceuticals exemplified by doxorubicin and mitoxantrone, exhibiting improved therapeutic efficacy.

Abstract: Novel compounds of formula (I) wherein R1 represents hydrogen; R2 represents hydroxy, fluoro, or an oxo group; R3 represents hydrogen; R4 represents hydrogen; and pharmaceutically acceptable salts, solvates, and the stereoisomers thereof, with the exception of the racemate of (3-amino-2-hydroxypropyl)sulphinic acid. The compounds are useful in therapy, especially for the treatment of reflux disease.

Abstract: The invention relates to the compounds of general formula (I), that are present with respect to R1 as racemates as well as L- or D-configured compounds and as E/Z mixtures as well as E or Z isomers and in which the various symbols are defined as in the description and the claims, as well as to the salts thereof, for use as therapeutic agents and for diagnostic purposes. The inventive compounds can be processed to medicaments or to diagnostic agents that are used for the diagnosis, therapy and prevention of urokinase- or urokinase-receptor associated diseases, for example for the treatment of tumors. The compounds are highly efficient in inhibiting growth and/or spread of malign tumors, for example tumor spread of pancreatic cancer, tumor growth of breast cancer and the formation of tumor metastases. The compounds of formula (I) and the salts thereof can be produced by conventional methods.

Abstract: This invention pertains to nitrogen mustard compounds (Formula (II)) and prodrugs therefor (Formula (I)), methods for their preparation, pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in therapy and treatment, for example, of cancer, wherein: R1 and R2 are independently —Cl, —Br, —I, —OSO2CH3, or —OSO2Ph; R1a, R2a, R1b, and R2b are independently —H, a C1-4alkyl group, or a C1-4haloalkyl group; R3 is —F, —Cl, —Br, —I, —OCHF2, —C?CH, —OCF3, —CH3, —CF3, —SF5, —SCF3, or —CF2CF3; R4 is —H or as defined for R3?, R5 is —H or —F; R7 is —H, —C(CH3)3, or —CH2—CH—CH2; Z is —CH2—T—W; T is —CH2—, —O—, —S—, —(S?O)—, or —(SO2)—; W is one of: (1) —COOH; (2)—(C?O)OR8; (3) —(C?O)NR9R9; (4) —SO2NHR10?, (5) SO2OR11; (6)—PO3R11R11; (7) a tetrazol-5-yl group; (8) —CONH—SO2R12; and, (9)-M-Het.

Abstract: In producing optically-active amino acid benzyl esters by reacting optically-active amino acids with benzyl alcohols, hydrazines are present in the reaction system, or the compounds are reacted in the absence of oxygen, or the compounds are reacted in the absence of oxygen while hydrazines are present in the reaction system. The processes are simple and give optically-active amino acid benzyl esters of high optical purity.

Abstract: Phosphinoamidite carboxylates and analogs are provided that have the structure of formula (I) wherein R1, R2, R3, R4, X, Y, Z and n are as defined herein. The compounds are useful as phosphitylating agents, e.g., in the phosphitylation of 3′ and 5′ hydroxyl groups of nucleosides and oligonucleotides. Also provided are phosphonocarboxylate and H-phosphonite carboxylate analogs of the compounds of formula (I). The compounds enable synthesis of phosphinocarboxylate and phosphonocarboxylate oligonucleotides having reduced internucleotide charge and enhanced nuclease resistance.

Abstract: This invention relates to novel compounds, capable of potentiating the efficacy of therapeutically active compounds, for example cytotoxic compounds used in the treatment of cancer. The novel compounds have been shown to increase the pharmacological activity of a conventional paclitaxel formulation and to make it possible to manufacture a new formulation of paclitaxel, exhibiting improved solubility, improved storage properties, and increased therapeutic efficacy as shown in the enclosed examples.

Abstract: The present invention relates to sulfinic acid compounds of the formula (I) where the substituents are as defined in the description. The novel sulfinic acid compounds can be used as reducing agents which do not eliminate formaldehyde.

Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.

Abstract: The present invention relates to sulfinic acid compounds of the formula (I) 1

Abstract: Sulfinic derivatives such as zinc dithionite, sodium dithionite, zinc or sodium hydroxymethyl sulfinate or zinc or sodium hydroxy-ethyl sulfinate, their condensation products with ammonia, and aminoiminomethanesulfinic acid are stabilized to degradation by admixture of potassium carbonate.

Abstract: A process for producing a thiourea dioxide fluid by mixing thiourea and a peroxide, or thiourea, a peroxide and a reaction catalyst, or thiourea, a peroxide, a reaction catalyst and a chelating agent, in the absence or presence of pulp and a process for bleaching pulp by the use of the thiourea dioxide fluid produced by the above process economically advantageously with a small chemicals loss and by small consumption of energy.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: The present invention relates to a process for producing amino/guanidinothiosulfonic acid, which comprises treating a styrenedivinylbenzene copolymer sulfonate of amino/guanidinoethyl disulfoxide into contact with an alkali, selectively eluting amino/guanidinosulfinic acid, then reacting this product in a non-aqueous solvent in the presence of a base, and passing the reaction product through a weakly acidic cation exchange resin column; in accordance with the present invention, hypotaurine, thiotaurine and the like having a high purity can industrially be produced.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: The present invention relates to a process for producing amino/guanidinothiosulfonic acid, which comprises treating a styrenedivinylbenzene copolymer sulfonate of amino/guanidinoethyl disulfoxide into contact with an alkali, selectively eluting amino/guanidinosulfinic acid, then reacting this product in a non-aqueous solvent in the presence of a base, and passing the reaction product through a weakly acidic cation exchange resin column; in accordance with the present invention, hypotaurine, thiotaurine and the like having a high purity can industrially be produced.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, and inhibition of cholesterol biosynthesis, are effected by compounds of the formula ##STR1## their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein:x is --ONR.sup.1 C(O)--, --N(OR.sup.1)C(O)--, --NR.sup.1 C(O)--, --C(O)NR.sup.1 --, --NR.sup.1 S(O.sub.2)--, --C(O)O--, --OC(O)--, --C(O)--, --O--, --NR.sup.1 -- or --(S).sub.q --;Y is --CO.sub.2 R.sup.2, --SO.sub.3 R.sup.2 or --P(O) (OR.sup.2) (R.sup.3);R is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkenylene or aryl;R.sup.3 is --(O).sub.t R.sup.4 ;R.sup.1, R.sup.2 and R.sup.4 are each independently hydrogen, alkyl, aryl or aralkyl;m and n are each independently 0 or an integer from 1 to 5;p and t are each independently 0 or 1; andq is an integer from 1 to 2.

Abstract: Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products.A process for the introduction of a fluoro substituent into a substantially adjacent position to an electron-donating group into an aromatic compound in high yield is disclosed.The fluoroaromatic compounds are useful as synthetic intermediates for example in the manufacture of agrochemicals, pharmaceuticals and dyestuffs.

Abstract: A compound selected from the group consisting of all possible isomeric forms and mixtures thereof of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms and cycloalkyl and cycloalkylalkyl of 3 to 8 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, cycloalkyl of 3 to 8 carbon atoms and acyl of 1 to 9 carbon atoms, X.sub.1 and X.sub.2 are individually selected from the group consisting of fluorine, chlorine, bromine, iodine, --CF.sub.3, --CN, --COOR and ##STR2## R is alkyl of 1 to 8 carbon atoms, Hal is chlorine, bromine or fluorine and R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and residue of an alcohol used in pyrethrinoid synthesis having excellent pesticidal properties.