Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

Abstract: The present invention relates to novel fatty acid analogues of the general formula (I): CH3—[CH2]m—[xi—CH2]n—COOR, as defined in the specification, which can be used for the treatment and/or prevention of diabetes. Further, the invention relates to a nutritional composition comprising such fatty acid analogues.

Abstract: Sulfur heteroatom substitution at the C4 position of 18F-labeled fatty acids yields a tracer that is retained in proportion to the beta-oxidation rates in mammalian tissue, particularly hypoxic myocardium. Most preferably, the invention is embodied in an [18F]fluoro-4-thia-fatty acid having a chain length of between 8 to 20 carbon atoms. The 18F-labeled 4-thia fatty acids of this invention find particular utility the radiolabelling of tissue sites (e.g., myocardium) for purposes of positron emission tomography.

Abstract: The present invention provides compositions and methods for protecting cells from injury due to intrinsic membrane lysis, oxidation and/or invasion by destructive agents. Even more particularly, the present invention provides compositions and methods for treating or prophylactically inhibiting phospholipase mediated injury, injury due to oxidation, and inflammation. In a very specific sense, this invention provides compositions and methods of making these compositions that are inhibitors of phospholipase.

Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

Abstract: A fusogenic liposome composition for delivering a liposome-entrapped compound into the cytoplasm of a target cell is described. The liposomes have an outer surface coating of chemically releasable hydrophilic polymer chains which shield hydrophobic polymers on the liposome outer surface. Release of the hydrophilic polymer chains exposes the hydrophobic polymers for interaction with outer cell membranes of the target cells to promote fusion of the liposome with the target cells. Also disclosed is a polymer-lipid conjugate for use in promoting fusion between target membranes. The conjugate is composed of a first segment composed of a hydrophilic polymer and a second hydrophobic polymer segment. The second segment is joined to the first segment by a bond effective to release the first segment in response to an existing or an induced physiologic condition. Attached to the second segment is a vesicle-forming lipid member.

Abstract: A pharmaceutical formulation for stimulating growth of Gram-positive Bacilli and increasing the acidity in vagina comprises sucrose and/or maltose, optionally with other sugars, viscous base, and anti-fungal and/or anti-bacterial agents.

Abstract: The invention relates to the production and purification of salts of 6,8-bis (amidiniumthio)octanoic acid, its enantiomers (+)-6,8-bis(amidiniumthio)octanoic acid and (-)-6,8-bis (amidiniumthio)octanoic acid and of the esters of these compounds as well as to their use to produce dihydrolipoic acid and .alpha.-lipoic acid.

Abstract: A method of inhibiting parasitic activity is disclosed in which the biosynthesis, structure and/or function of the glycosyl phosphatidylinositol (GPI) anchor of said parasite may be affected by incorporating into said GPI anchor selected analogs of myristic acid containing various heteroatoms, substituents and unsaturated bonds, including ester-containing analogs, ketocarbonyl-containing analogs, sulfur-containing analogs, double bond- and triple bond-containing analogs, aromatic moiety-containing analogs, nitrated analogs and halogenated analogs.

Abstract: Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.

Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

Abstract: A process for the production of a solid esterquat free from solvents comprising the steps ofA) forming a mixture comprising(i) at least one fatty acid triethanolamine ester corresponding to formula (I) ##STR1## in which R.sup.1 CO is a saturated and/or unsaturated acyl radical containing 6 to 22 carbon atoms, R.sup.2 and R.sup.3 independently of one another represent hydrogen or have the same meaning as R.sup.1 CO, and n, m and p together stand for O or for a number of from 1 to 10;(ii) at least one fatty alcohol polyglycol ether, and(iii) at least one fatty acid partial glyceride; andB) adding an alkylating agent to the above mixture to form said solid esterquat.

Abstract: There is disclosed a lubricant additive ingredient that imparts extreme pressure anti-wear properties to lubricant additive compositions. Specifically, there is disclosed a derivative of a vegetable oil triglyceride, a wax ester or a telomerized oil reacted with phosphorous pentasulfide to produce a phosphorous-sulfur (PS) extreme pressure additive.

Abstract: The synthesis of pure enantiomers of 8-chloro-6-sulfonyloxy-octanoic acids and their alkyl esters and of pure enantiomers of 6,8-dichloro-octanoic acid and its alkyl esters as intermediates for the synthesis of the enantiomers of .alpha.-liponic acid as well as a method for converting the two enantiomers of 8-chloro-6-hydroxy-octanoic acid into an enantiomer of .alpha.-liponic acid.

Abstract: Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.

Abstract: A method for the topical or systemic treatment of disorders mediated by proteases which result in skin or mucosal lesions, and in particular, pemphigus, cicatricial pemphigoid, bullous pemphigoid, lichen planus, and canker sores, is disclosed wherein the host is treated with an effective amount of N-acetyl ysteine or a derivative thereof, or its pharmaceutically acceptable salt, optionally in a pharmaceutically acceptable diluent or carrier for systemic or topical delivery.

Abstract: A method of imparting low fogging characteristics to tanned leather, which includes the step of treating the leather in an aqueous emulsion including an effective quantity of an oil having less than 3 percent of fatty acid components of less than C-16, the oil having been first distilled to remove low molecular weight trace elements. The oil may be by way of example soybean oil, lard oil, safflower oil, or sunflower oil.

Abstract: These compounds are denoted by the following formula (I): ##STR1## in which: Z denotes H or a linear or branched alkyl radical,X denotes O or S,each of A and B independently denotes an alkylene radical, it being possible for this radical to be substituted,R denotes H or an alkali metal, or else a linear or branched alkyl radical,x has the value of 0 or 1, andy has the value of 0, 1 or 2,the radical A not existing if x and y are both equal to 0, X being incapable of denoting O when R=alkyl and when R=H with x=y=0, and B being incapable of denoting optionally substituted methylene when X=S, x=y=0 and R=alkyl.According to the invention, different simple and efficient processes are proposed for preparing these new compounds, which can be applied to the preparation of new polymers and copolymers.

Abstract: A compound of the invention is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different, an acyl group; R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are the same or different, hydrogen or an alkyl group; R.sup.5 is hydrogen, an alkyl group or a hydroxyl group which may optionally be protected, or R.sup.4 and R.sup.5 are combined to form a chemical bond; X is a carbonyl group or a sulfonyl group; Y is an amino acid sequence consisting of 1 to 7 amino acid residues which may optionally be protected and having optionally an intervening --SO.sub.2 NH--; n is an integer of 0 to 2, or a salt thereof.

Abstract: Ammonium fatty acid hydroxyalkanesulfonates are made by a process in which (a) ammonium hydroxyalkanesulfonate corresponding to general formula (I):HO--(C.sub.n H.sub.2n)--SO.sub.3 NH.sub.4 (I)wherein n=2 to 4, is subjected to the esterification reaction with a fatty acid corresponding to the formula (II)R--COOH (II)wherein RCO is an aliphatic, linear or branched acyl radical containing 6 to 18 carbon atoms, in the presence of an esterification catalyst, characterized in that (a) before the esterification reaction, the starting compounds corresponding to formulae (I) and (II) are dried at a temperature of 120.degree. C. to 160.degree. C. and under a pressure of 100 to 700 mbar; (b) the esterification reaction is carried out at a temperature above 160.degree. C. to 195.degree. C. and under a pressure of 250 mbar to atmospheric pressure; (c) water of solution and water of reaction formed are directly removed from the reaction mixture; (d) the catalyst is neutralized with a base on completion of the reaction.

Abstract: Disclosed are methods for dispersing sulfur in aqueous systems comprising adding an alkylcarboxylic acid compound to the system. This prevents fouling of the aqueous system by the precipitated sulfur.

Abstract: The present invention relates to derivatives of natural fats and oils that are liquid or flowable, respectively, and to a process for the production of said derivatives, in which oxalkylation is carried out at elevated temperatures in the presence of basic catalysts with at least one compound containing an epoxide group, and sulfation is carried out in a manner known per se, in which a starting material containingA) at least one C.sub.8 -C.sub.24 -fatty acid ester of an aliphatic C.sub.1 -C.sub.5 -monoalcoholThe present invention furthermore relates to the use of said derivatives, optionally in combination with other greasing substances and anionic and/or non-ionic emulsifiers, for the fatliquoring and greasing of leather.

Abstract: In the production of highly concentrated pastes of .alpha.-sulfofatty acid alkyl ester alkali metal salts by reaction of fatty acid alkyl esters with gaseous SO.sub.3, subsequent after-reaction in liquid phase and neutralization with aqueous alkali hydroxide solutions, the sulfonation product and aqueous alkali metal hydroxide solution are introduced during neutralization into an aqueous phase initially containing 0 to 55% by weight washing-active substance at a pH value in the range from 2 to 8 and washing-active substance contents of 60 to 70% by weight are established.

Abstract: In the production of light-colored pastes of .alpha.-sulfofatty acid alkyl ester alkali metal salts by reaction of fatty acid alkyl esters with gaseous SO.sub.3, subsequent after-reaction in liquid phase, neutralization with aqueous alkali metal hydroxide solutions and bleaching, effective bleaching can be obtained without any reduction in the washing-active substance content by addition of the hydrogen peroxide during neutralization of the .alpha.-sulfofatty acid alkyl ester and subjecting the neutralization product obtained to a temperature-controlled after-reaction.

Abstract: In the production of highly concentrated pastes of .alpha.-sulfofatty acid alkyl ester alkali metal salts by reaction of fatty acid alkyl esters with gaseous SO.sub.3, subsequent after-reaction in liquid phase and neutralization with aqueous alkali hydroxide solutions, the sulfonation product and aqueous alkali metal hydroxide solution are introduced during neutralization into an aqueous phase initially containing at least 55% by weight washing-active substance at a pH value in the range from 2 to 8 and washing-active substance contents of 60 to 70% by weight are established.

Abstract: The invention relates to fatty acid monoglyceride polyglycol ether sulfosuccinates of the general formula ##STR1## where R represents a straight-chain or branched alkyl or alkylene group having from 7 to 21 carbon atoms;R.sup.1 represents H or CO--R;R.sup.2 may represent, independently of each other, H or the group --CO--CH(SO.sub.3.sup.- M.sup.+)--CH.sub.2 --COO.sup.- M.sup.+ ;A represents the same or different and each is an alkylene group having from 2 to 3 carbon atoms;a,b,c,d may be the same or different, from 0 to 5,e being from 1 to 3,f is a multiplication product of c times e, and a+b+f+d is from 2 to 25; andM.sup.+ represents an alkali-metal ion or an ammonium ion, and to their preparation and use.

Abstract: Salts of aminosulfonic acid derivatives of formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each independently of the others an aliphatic hydrocarbon radical having from 7 to 21 carbon atoms,n is 0 or 1,As is the amidically bonded residue of a (D)- or (L)-amino acid or of a (D)- or (L)-amino acid derivative from the group consisting of Gly, Ala, Ser, Thr, Asp, Asp(R.sup.5), Glu, Glu(R.sup.5), Gla, Gla(R.sup.5) and Gla(R.sup.5).sub.2, andR.sup.4 and R.sup.5 are each independently of the other the amidically bonded radical of an unsubstituted or carboxy-substituted .omega.-amino-C.sub.2 -C.sub.3 alkanesulfonic acid, are described.Those salts have an immunostimulating action and can be used as medicaments.

Abstract: The invention relates to compounds containing carbonate groups and carbonyl groups and having the general formula ##STR1## in which R stands for a C.sub.1 -C.sub.4 -alkyl radical, an aryl radical, or a radical R.sup.1, whereR.sup.1 has the following formula ##STR2## in which R.sup.2 to R.sup.6 stand for H, alkyl, OH, O-alkyl, SH, S-alkyl, halogen, N(alkyl).sub.2, or N(alkyl)(aryl) and at least one but not more than three of the radicals R.sup.2 to R.sup.6 stand for a radical of the formula ##STR3## in which A, B and C stand for alkylene, cycloalkylene, oxaalkylene, polyoxaalkylene or arylene, k and l both stand for an integer from 1 to 80, and the end group Z stands for alkyl, aryl, alkoxycarbonyl, alkoxycarbonyloxy, or aryl.These compounds are suitable for use as emulsifiers for dispersions.

Abstract: Aryl alkenoic acid derivatives, and physiologically acceptable salts thereof, are provided which are potent leukotriene antagonists and may be used for the treatment of circulatory diseases and preferably for respiratory diseases such as asthma. The derivatives have a general formula I ##STR1## in which X is --S--,W is CH.dbd.CH;o is 1 to 4;n is 2 to 6;m is 0 to 2;T and Z, same or different, represent oxygen or a direct bond;R.sup.2 and R.sup.3, represent hydrogen, or fluorine;A represents carboxyl, CO.sub.2 R.sub.4.sup.4, wherein R.sup.4 is lower alkylR is ##STR2## wherein Y represents carboxyl, CO.sub.2 R.sup.4, wherein R.sup.4 is lower alkylR.sup.7 and R.sup.8, same or different, represent H or lower alkyl;R.sup.9 represents --OH, --O-alkyl, NH.sub.2 or a NHCH.sub.2 CO.sub.2 H group; andR.sup.10 R3 is H.

Abstract: A process for producing desulfurized fats and oils or fatty acid esters is disclosed, which comprises treating fats and oils or fatty acid esters under hydrogen or a mixture of hydrogen and an inert gas atmosphere at a pressure of from 0.1 to 500 kg/cm.sup.2 in the absolute pressure at a temperature of from 100.degree. to 350.degree. C. in the presence of a catalyst of the following formula (I):Cu.multidot.X.sub.x .multidot.Y.sub.y .multidot.O.sub.z (I)wherein all symbols are defined in the disclosure. A process for producing an alcohols using desulfurized fats and oils or fatty acid esters is also disclosed. According to the process for producing an alcohol of the present invention, an alcohol of a high purity and good qualities can efficiently and effectively be produced.

Abstract: A product formed by heating (A) a mixture of a carboxylic acid ester and a fatty acid oxyalkylated amine derivative selected from fatty acid amides, fatty acid esters, fatty acid ester-amides of such oxyalkylated amine, and mixtures thereof with (B) sulfur or a sulfur source at an elevated temperature at which sulfurization occurs. Such products are effective as oil additives in inhibiting excessive wear and sludge formation. And they possess excellent compatibility with oils of lubricating viscosity, such as mineral oils used as crankcase lubricating oil base stocks.