Abstract: Disclosed herein are substituted amino alcohol anti-mycobacterial agents and/or chelation therapy agents of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A method of transalkoxylation of nucleophilic compounds in which an alkoxylated and a nucleophilic compound are combined in a suitable vessel and reacted in the presence of a heterogeneous catalyst under conditions capable of transferring at least one hydroxyalkyl group from the alkoxylated compound to the nucleophilic compound. The method is especially useful in the transalkoxylation of alkanolamines to transfer a hydroxyalkyl group from an alkanolamine having a greater number of hydroxyalkyl groups to an alkanolamine having a lesser number of hydroxyalkyl groups.

Abstract: A compound of formula (I): wherein k is 1 or 2; Y is —CH2CH(CF3)2 or —(CH2)nCF; X is hydrogen, —(CH2)nRf, or —C(O)[CF(A)]p-B—Rf, wherein B is a covalent bond, —O— or —(CH2)m—; A is —F or —CF3; and each Rf is independently C1 to C6 perfluorinated alkyl, optionally interrupted by one or more oxygens; Ro is Ro1 or is an alkyl having from about 10 to about 100 carbon atoms, interrupted or substituted by one or more hydrophilic groups; R is hydrogen or a C1 to C4 alkyl; and Ro1 is an aliphatic group of from about 10 to about 100 carbon atoms, interrupted by about from about 5 to about 50 ether oxygens; provided that 1) when Y is —(CH2)nRf, Ro is Ro1; 2) when X is hydrogen, Y is —CH2CH(CF3)2; and 3) when X is —(CH2)nRf and Y is —(CH2)nRf, Ro is Ro1.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: The present inventor discovered stabilizing agents/stabilizing conditions for suppressing isomerization reactions of sc(Fv)2. It was also discovered that the above-mentioned isomerization reactions can be suppressed through use of freeze-dried formulations. As disclosed herein, by applying the discovered stabilizing agents/stabilizing conditions or the freeze-dried formulation, the isomerization reaction of an sc(Fv)2-type molecule from the bivalent scFv type to the single chain diabody type, and/or the isomerization reaction from a single chain diabody type to a bivalent scFv type can be suppressed in both directions or one direction.

Abstract: The invention relates to the use, as agent for depigmenting and/or whitening the skin, in particular for eliminating pigmentary spots and/or senescence spots, and/or as anti-browning agents, of a compound of formula (I): R1—CHOH—CH(NH—COR2)(CH2OH)??(I) in which R1 denotes a C11 to C21 alkyl radical, and R2 denotes a linear, optionally hydroxylated C11-C19 hydrocarbon-based radical, with the hydroxyl group being in the alpha-position with respect to the carbonyl, which may comprise one or more ethylenic unsaturations, in particular one or two ethylenic unsaturations. The invention also relates to a cosmetic process for depigmenting and/or lightening skin exhibiting pigmentation spots, comprising the application to the skin of a composition comprising, in a physiologically acceptable medium, a compound of formula (I).

Abstract: Cationic lipid compositions are provided that are useful for efficient delivery of macromolecules, such as nucleic acids, into a wide variety of eukaryotic cell types. Methods for using the compositions also are provided.

Abstract: It comprises a preparation process of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by submitting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6)-alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6)-cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4)-alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process.

Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)I, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and w

Abstract: The present invention relates to a method (assay) for determining the activity of an enzyme selected from the group consisting of a sphingosine kinase and a phosphatase involved in the sphingolipid pathway by use of a labeled sphingosine.

Abstract: Synthetic methods provide for the simple, efficient preparation of amino polyols and derivatives. The methods include a three-component reaction of a carbohydrates with organoboron compounds and primary or secondary amine derivatives. The resulting amino polyols can be transformed into amino sugars. In one implementation, the amine moiety is protected, and an alkenyl, aryl or heteroaryl moiety is cleaved to form the amino sugar. Amino polyols and amino sugars prepared according to the methods are also described.

Abstract: The use of bis-amines to enhance the antimicrobial activity of pharmaceutical compositions is described. The bis-amines are particularly useful for enhancing the antimicrobial activity of aqueous ophthalmic compositions, such as artificial tears or ocular lubricants, and solutions for disinfecting contact lenses.

Abstract: Severely sterically hindered secondary aminoether alcohols are prepared by reacting an organic carboxylic acid or alkali metal salt of an organic carboxylic acid with a sulfonyl halide, a sulfuryl halide, a mixed sulfuryl ester halide or a mixed sulfuryl amide halide to yield a sulfonic-carboxylic anhydride compound which is then reacted with a dioxane to cleave the ring of the dioxane, yielding a cleavage product which cleavage product is then aminated with an alkylamine and hydrolyzed with base to yield the severely sterically hindered secondary aminoether alcohol.

Abstract: A method of making an amino-alkylenediol and intermediate compounds useful in the method is disclosed. The method includes preparing a first intermediate compound comprising an aminoalkylene diol wherein a protecting group is linked to the amino functionality, and optionally, preparing a second intermediate compound comprising a salt of the first intermediate compound. The first intermediate compound has the structure wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, and Z is a protecting group. The second intermediate compound has the structure wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, TsO? is toluene sulfonate, and Z is a protecting group.

Abstract: The present invention is in the field of prevention and treatment of atherosclerosis and atherosclerosis-related clinical conditions. In particular, the present invention relates to the use of sphingolipids, more preferably phytosphingosine, sphingosine, sphinganine, ceramide, cerebroside lyso-sphingomyelin and/or sphingomyelin for prevention and treatment of inflammatory processes associated with atherosclerosis, psoriasis, colitis or auto-immune diseases in a subject.

Abstract: Severely sterically hindered secondary aminoether alcohols are prepared by reacting acid anhydrides or organic carboxylic acid halides with SO3 to yield a sulfonic carboxylic anhydride compound which is then reacted with a dioxane to cleave the ring of the dioxane yielding a cleavage product which is then aminated with an alkylamine and hydrolyzed with a base to yield the severely sterically hindered secondary aminoether alcohol.

Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2-Z or -Z; R1–R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and

Abstract: The present invention provides (i) a novel composition which is the polyol reaction product polyol made by mixing together a polyhydroxyl-tertiary amine, at least two of the hydroxyl groups of said amine being indirectly bonded to a nitrogen atom of said amine through a chain containing at least two carbon atoms, with an organic polyisocyanate, essentially all the isocyanate groups of said polyisocyanate being reacted with hydroxyl groups of said amine, and (ii) a coating composition containing a film forming binder and a volatile organic liquid carrier, said binder containing (I) hydroxyl-containing acrylic polymer and (II) the novel composition (i).

Abstract: This application relates to the use of certain amines of formula (I) for combatting and preventing systemic and local complement activation, and in particular to the use of meglumine and derivatives and optionally salts thereof in combatting and preventing said activation. The amines are also of use in combatting activation of the kinin/kallikrein system or blood coagulation system.

Abstract: The present invention relates to a continuous process for the manufacture of triethanolamine (TEA) comprising, in succession: (i) a step of synthesizing the TEA by continuously bringing ammonia into contact with ethylene oxide under conditions allowing the formation of a reaction mixture comprising mono-, di- and triethanolamines, (ii) a step of continuously separating the ammonia that has not reacted from the reaction mixture and (iii) a step of continuously separating the TEA from the mixture resulting from step (ii). The process is characterized in that a specific mixture of alkanolamines, comprising TEA and from 0.5 to 50% by weight of at least one secondary dialkanolamine, is prepared or isolated from the mixture resulting from step (ii), and in that the TEA is separated and isolated with a degree of purity equal to or greater than 99.2% by weight, by a continuous distillation of the specific mixture of alkanolamines.

Abstract: Methods and compositions for treating disease caused by microorganisms, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: Intermediate compounds which can be used in the preparation of phytone and Vitamin E, a process for the preparation thereof, and a process for the preparation of phytone and Vitamin E from these intermediate compounds.

Abstract: Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to, porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.

Abstract: A process for producing a high purity trialkanolamine excelling in hue and having an APHA of not more than 40, characterizing by including producing a mixed alkanolamine by the reaction of an alkylene oxide with ammonia; removing low-boiling substances from the mixed alkanolamine; removing high-boiling substances by subjecting the product deprived of the low-boiling substance to vacuum distillation, and redistilling the distillate obtained by the vacuum distillation.

Abstract: Perfluoroalkyl-substituted amines, acids, amino acids and thioether acid compounds containing a perfluoroalkyl-iodoalkyl or perfluoroalkyl-alkene group as well as derivatives thereof, are described. They are useful as surfactants in a variety of applications where low surface tensions are required, including coating formulations for glass, wood, metal, cement, paper, textiles, as foam control agents in polyurethane foams and especially in aqueous fire-fighting formulations.

Abstract: Cationic lipids are provided which are useful in the preparation of liposomes and other lipid vesicle carriers. The lipids of the invention are particularly useful as carriers of nucleic acids and other negatively charged substances, for delivery to cells.

Abstract: Disclosed is a method for preparing tertiary amine compounds from primary amines and nitrites in the presence of hydrogen gas and a metal catalyst, or metal-containing catalyst composition, at a temperature from about 50° C. to about 200° C. and at a pressure from about 100 psig to 1500 psig. The primary amines and the nitriles used in the process may be diamines and/or dinitriles, or may be combinations of primary amines and/or nitrites. Also disclosed are novel tertiary amine compounds made by the described method.

Abstract: This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy.

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

Abstract: The present invention provides novel cationic amphiphiles containing novel N-hydroxyalkyl group and therapeutic formulations containing the said amphiphiles that are capable of facilitating transport of biologically active molecules into cells.

Abstract: Provided herein are catalyst systems useful for providing polyurethane foam products which exhibit low fogging characteristics while possessing favorable overall physical properties when used as interior components of automobiles and other motorized vehicles.

Abstract: The present invention relates to a novel sphingolipid ceramide N-deacylase (SCDase) having a wide substrate specificity; a method for enzymatically producing a lysosphingolipid or a sphingolipid derivative using the SCDase which is useful in the fields of medicine, carbohydrate engineering, cell engineering, and the like; the lysosphingolipid or sphingolipid derivative obtained by this production method; a gene which encodes a polypeptide having an SCDase activity useful in sphingolipid technology; a method for industrially producing a polypeptide having an SCDase deacylase activity and a recombinant polypeptide thereof using a transformant to which the gene is introduced; a probe or primer which hybridizes to the gene; and an antibody or a fragment thereof which specifically binds to the polypeptide.

Abstract: The invention relates to &agr;-galactosidase and to polynucleotides encoding the &agr;-galactosidase. In addition methods of designing new &agr;-galactosidases and method of use thereof are also provided. The &agr;-galactosidases have increased activity and stability at increased pH and temperature.

Abstract: An aqueous phase inhibitor for quenching free radical polymerization comprising a free radical quenching agent having a hydrophilic tail is disclosed, as well as a coating and related methods. In one embodiment, the free radical quenching agent can either be an N-hydroxylamine or an N-nitrosonamine, the hydrophilic tail can be a polyhydric alcohol tail and the inhibitor can be a concentrate in a liquid medium such as water, alcohol and mixture thereof.

Abstract: The present invention provides novel cationic amphiphiles containing novel N-hydroxyalkyl group and therapeutic formulations containing the said amphiphiles that are capable of facilitating transport of biologically active molecules into cells.

Abstract: The invention relates to compositions and methods for gelling liquid hydrocarbons by the introduction of certain phosphate esters, a crosslinking agent, and an enhancer. The enhancer of the present invention is preferably an oxyalkylated amine or a blend of an oxyalkylated amine with another amine or a non-nitrogen-containing component. Mixed phosphate esters containing an oxyalkylene group are useful in the practice of the invention. Gel-forming compositions for addition to liquid hydrocarbons, as well as methods for forming fracturing fluids, are encompassed. The present compositions and methods are an improvement in the field of hydrocarbon gelling, e.g., in fracturing formations, by providing more rapid gellation and greater viscosities.

Abstract: Preparation of alkanolamines having improved color quality by treating the alkanolamine with hydrogen in the presence of a hydrogenation catalyst at elevated temperature, by using, as hydrogenation catalyst, a heterogeneous catalyst comprising Re, Ru, Rh, Pd, Os, Ir, Pt and/or Ag and a support material chosen from the group consisting of activated carbon, alpha-aluminum oxide, zirconium dioxide and titanium dioxide, where the catalyst, in the case of activated carbon as support material, has a cutting hardness of at least 10 N, a side crushing strength of at least 30 N or a compressive strength of at least 25 N.

Abstract: The present invention relates to derivatives of polyalkenyl amine substituted with numerous hydroxy groups of the following formula (I) useful as a novel fuel detergent. ##STR1## wherein polyalkenyl denotes a branched alkyl derived from polyolefin which has a molecular weight of 400.about.5,000 and is prepared with olefin having 2 to 6 carbon atoms; m is an integer ranging from 2 to 10, R.sup.1, R.sup.2 and R.sup.3 may be identical or different, and represent a hydrogen atom or a linear or branched alkyl having 1 to 4 carbon atoms: R.sup.4 and R.sup.5 may be identical or different, and denote a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a hydroxyalkyl, a phenyl, naphthyl, an aminoalkyl of formula (II) or a polyaminoalkylene of formula (III) ##STR2## wherein R.sup.6 denotes a C.sub.2 -C.sub.10 alkylene group: R.sup.7 and R.sup.8 may be identical or different, and denote a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a phenyl, a naphthyl or a C.sub.1 -C.sub.

Abstract: The present invention relates to a catalyst based on titanosilicalites having a content by weight of alkali metal or metals of between 0.05 and 2%. The subject of the invention is more particularly a process for producing N,N-disubstituted hydroxylamine from hydrogen peroxide and the corresponding disubstituted amine.

Abstract: The subject of the invention is a process for the preparation of 2-aminoalkane-1,3,4-triols, in a single stage, preferably a single reduction state, from alkyl 2-hydroxyimino-3-oxo-4-acyloxyalkanoates. The invention makes possible a significant reduction in the number of stages and a marked improvement in the synthesis yields.

Abstract: Disclosed are polyamines having the formula: ##STR1## or salts or stereoisomers thereof wherein R.sub.1 -R.sub.4 and ALK.sub.1 -ALK.sub.3 are as defined in the specification. Pharmaceutical compositions and therapeutic methods of treatment utilizing the compounds are also disclosed.

Abstract: The present invention relates to an amine derivative represented by the following general formula (1): ##STR1## wherein R.sup.2 and R.sup.3 mean individually an alkyl or alkenyl group which may have --OH and has 1-24 carbon atoms, A denotes an alkylene or alkenylene group which may have at least one --OH, --COOH or --SO.sub.3 H and has 1-6 carbon atoms, y.sup.1 is --COOH, --SO.sub.3 H or --OSO.sub.3 H, y.sup.2 means --OH, --OSO.sub.3 H or --OCO--A--COOH, n stands for a number of 0 or 1, and p is an integer of 1-8, or a salt or quaternized product thereof, and a detergent composition containing such a compound. This compound is low in irritativeness to the skin and hair and excellent in foamability, and can give a pleasant feeling to the user's skin and the like.

Abstract: Hydroxyalkyl-substituted aminoalkynes of the general formula I ##STR1## where at least one of the substituents R.sup.1, R.sup.4 or R.sup.5 is hydroxyalkyl are prepared in a reaction with heterogeneous catalysis.

Abstract: The present invention relates to an amine derivative represented by the following general formula (I) or (II): ##STR1## wherein R.sup.1 means a heteroatom-containing C.sub.1 -C.sub.40 hydrocarbon group which may have a ring structure, or the like; R.sup.2 -R.sup.5 each denote a C.sub.1 -C.sub.20 hydrocarbon group, hydrogen or the like; A.sup.1 represents ##STR2## or R.sup.15 --Z--.sup.16 --(CH.sub.2).sub.n --; B.sup.1 stands for hydrogen, a C.sub.1 -C.sub.10 hydrocarbon group, nitrogen or the like; C.sup.1 denotes hydrogen, a C.sub.1 -C.sub.10 hydrocarbon group, nitrogen, alcohol residue, phosphoric acid residue or the like; a dermatologic preparation containing the same; and a process for producing the amine derivative. This amine derivative has excellent effects of smoothing or removing wrinkles and improving keratinization.

Abstract: A process for producing mixtures of mono-, di- and triethanol-amine by reacting ammonia and ethylene oxide in a cooled tubular reactor at temperatures from 110.degree. to 160.degree. C. and pressures from 50 to 120 bar comprises using ammonia and ethylene oxide in a molar ratio from 1:1 to 100:1 and ammonia in the form of a from 60 to 99.99% strength aqueous solution and adding from 1 to 80% of the ethylene oxide in from one to ten aliquots over from 10 to 70% of the total length of the tubular reactor.

Abstract: A process is disclosed for producing a substituted ethylenediamine, the process comprising reacting an oxazolidinone with a secondary amine or an alkanolamine. The process includes, in one aspect, reacting precursors of the oxazolidinone in situ.

Abstract: A tertiary amino alcohol, being useful as an emulsifier, is defined by the formula (1) or (2): ##STR1## where R is a C.sub.2 to C.sub.24 straight-chain or branched alkylene group, an alicyclic alkylene group, an aralkylene group or --CH.sub.2 CH.sub.2 O).sub.p (CH.sub.2 CH.sub.2).sub.q (where p is 0 or a positive integer and q is a positive integer), R' is a C.sub.1 to C.sub.24 straight-chain or branched alkyl group or an aralkyl group and n is a positive integer of 2 to 50.

Abstract: Ionic monomeric diallylammonium compounds having a targeted combination of diallylammonium cations with selected anions have particularly high and constant charge control properties and very good heat stabilities and dispersibilities.The compounds according to the invention are outstandingly suitable for use as colorless charge control agents in toners and developers for electrophotographic recording processes and for use as charge-improving agents in powders and paints for surface coating, in particular in triboelectrically or electrokinetically sprayed powder paints.

Abstract: Therapeutic compounds have the formula:(X)j-(non-cyclic core moiety),j being an integer from one to three, the core moiety is non-cyclic and X is a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.2 form a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. R.sub.