Abstract: The present invention relates to fatty acid alkanolamides or polyolamides containing at least one group Y, where Y stands for CF3—(CH2)a—O—, SF5—, CF3—(CH2)a—S—, CF3CF2S—, [CF3—(CH2)a]2N— or [CF3—(CH2)a]NH—, where a stands for an integer selected from the range from 0 to 5, or formula (I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)r— or [CF3—(CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, to processes for the preparation of these compounds, and to uses of these surface-active compounds.

Abstract: Novel retro-anandamides are presented which have high affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy, as well as suppression of the immune system, enhancement of appetite and in treatment of certain mental disorders.

Abstract: Novel analogs of arachidonylethanolamide are presented which have higher affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications for relief of pain caused by cancer and nausea caused by chemotherapy, as well as for peripheral pain. The compounds may also be useful as oral and topical contraceptives, in suppression of the immune system, enhancement of appetite and in treatment of psychomotor disorders, multiple sclerosis and hypertension.

Abstract: Amino acid derivative as carrier compounds and compositions which are useful in the delivery of active agents are provided. The active agents can be a peptide, mucopolysaccharide, carbohydrate, or lipid. Methods of administration, including oral administration, and preparation are provided as well.

Abstract: There are described compounds of formula 1

Abstract: The compound of the formula (I) 1

Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide (hereinafter referred to as a “protected/activated salicylamide”). The method comprises the steps of (a) alkylating the protected/activated salicylamide with an alkylating agent to form a protected/activated alkylated salicylamide, and (b) deprotecting and deactivating the protected/activated alkylated salicylamide, simultaneously or in any order, to form the alkylated salicylamide. The alkylated salicylamides prepared by this method are suitable for use in compositions for delivering active agents via oral or other routes of administration to animals.

Abstract: Selected quaternary ammonium salts containing fluoroalkyl, preferably perfluoroalkyl, groups that are stable to bases are described. They are useful as phase transfer reaction catalysts, especially in basic media.

Abstract: Inhibitors of oleamide hydrolase, responsible for the hydrolysis of an endogenous sleep-inducing lipid (1, cis-9-octadecenamide) were designed and synthesized. The most potent inhibitors possess an electrophilic carbonyl group capable of reversibly forming a (thio) hemiacetal or (thio) hemiketal to mimic the transition state of a serine or cysteine protease catalyzed reaction. In particular, the tight binding .alpha.-keto ethyl ester 8 (1.4 nM) and the trifluoromethyl ketone inhibitor 12 (1.2 nM) were found to have exceptional inhibitory activity. In addition to the inhibitory activity, some of the inhibitors displayed agonist activity which resulted in the induction of sleep in laboratory animals.

Abstract: An aniline derivative of the formula (1) ##STR1## wherein R.sup.1 is an eicosapentaenoyl or docosahexaenoyl; R.sup.2 and R.sup.3 are each independently an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; R.sup.4 is a hydrogen atom, an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; and A is a single bond, --C(.dbd.O)NH--(CH.sub.2).sub.n --NH-- wherein n is 2 or 3, or a bivalent group of the following formula ##STR2## wherein m and p are each independently 0 or 1. The aniline derivative of the present invention has high inhibitory activity against and high selectivity for ACAT derived from macrophage and is useful as an agent for the prophylaxis and treatment of arteriosclerosis.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.8 cycloalkyl, halo-C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, halo-C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, --Si(R.sub.3).sub.3, --S--R.sub.4, --SO.sub.2 --R.sub.6 or --CO--R.sub.9 ;R.sub.2 is halogen, C.sub.1 -C.sub.4 alkyl or CF.sub.3, the substituents R.sub.2 being identical or different when n is 2;R.sub.3 each independently of the others is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or phenyl;R.sub.4 is aryl or heteroaryl each of which is unsubstituted or substituted;R.sub.6 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.20 -alkoxy, C.sub.2 -C.sub.6 alkenyloxy, C.sub.2 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, aryl, aryloxy or arylthio, or is optionally substituted amino;R.sub.9 is hydroxy, unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.

Abstract: Aromatic acid-derived lipophilic polyhalogenated compounds are provided for use as contrast agents in diagnostic imaging or as therapeutic agents. These compounds are particularly useful when incorporated into an oil-in-water emulsion for tissue-specific delivery to the liver. For hepatocyte-selective delivery, the emulsion is chylomicron remnant-like by being in a size range of 50 to 200 nm and having a composition simulating naturally-occuring chylomicron remnants.

Abstract: This invention relates to novel processes for synthesizing intermediates in the preparation of N-aryl and N-heteroarylamide inhibitors of the enzyme acyl coenzyme A: cholesterol acyltransferase (ACAT), and to novel intermediates used in such processes.

Abstract: Compound of the formula (I):Q.sup.1 Q(CR.sup.2 .dbd.CR.sup.3).sub.a (CR.sup.4 .dbd.CF)(CR.sup.5 .dbd.CR.sup.6).sub.b C(.dbd.O)NHR.sup.1 (1)or a salt thereof, wherein Q.sup.1 is a phenyl ring or a fused bicyclic ring system containing 9 or 10 ring carbon atoms at least one ring being aromatic, or Q.sup.1 is a dihalovinyl group; Q is an alkyl chain containing 1 to 12 carbon atoms and optionally containing one or two oxygen atoms and/or an unsaturated group --CR.sup.7 .dbd.CR.sup.8 --, or --C.dbd.C--, wherein R.sup.7 and R.sup.8 are selected from hydrogen or halo; a is 0 or 1; b is 0 or 1; the sum of a and b is 0 or 1; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and are independently selected from hydrogen, halo and C.sub.1-4 alkyl; R.sup.1 is selected from hydrogen and C.sub.1-6 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy are disclosed which have pesticidal activity.