Abstract: Compounds particularly for use in an autoimmune inflammatory disease and especially the treatment of inflammatory bowel disease have the absolute stereochemistry and formula: In some cases R1 is leucine and R is selected from: OH, OCH3, OCH2CH3, OCH2CH2CH3, NH2, NHCH2CH2OH, NHCH3, N(CH3)2, NH(4-OH-3-benzoic acid).

Abstract: An acid diffusion control agent includes a compound represented by a formula (1), a compound represented by a formula (2) or both thereof. R1 represents a hydrocarbon group comprising a monovalent alicyclic structure, or the like. R2 and R3 each independently represent a monovalent hydrocarbon group, or the like. R4 and R5 each independently represent a monovalent hydrocarbon group, or the like. R6 and R7 each independently represent a monovalent hydrocarbon group, or the like. R8 represents a monocyclic heterocyclic group together with the ester group and with the carbon atom. n is an integer of 1 to 6. R9 represents a monovalent hydrocarbon group, or the like. R10 represents a monovalent hydrocarbon group having 1 to 10 carbon atoms. R11 and R12 each independently represent a monovalent hydrocarbon group, or the like. R13 and R14 each independently represent a monovalent hydrocarbon group, or the like.

Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

Abstract: One subject of the present invention is the use, as solvents, of compounds of esteramide type. Another subject of the invention are particularly practical processes for preparing esteramides. Another subject of the invention are novel esteramides, which may in particular be used as solvents, for example in phytosanitary formulations.

Abstract: The invention relates to a method for improving bioavailability of pharmaceutical substances and for allowing the pharmaceutical substances to permeate the blood-brain barrier, the pharmaceutical substances having at least one or more amidine, guanidine, N-hydroxyamidine (amidoxime) or N-hydroxyguanidine functions. The invention also relates to medicaments containing the correspondingly modified pharmaceutical substances.

Abstract: A lipid particle can include a cationic lipid. The cationic lipid can include one or more hydrophobic tails, which can include one or more sites of unsaturation. The sites of unsaturation can include cycloalkyl groups, e.g., cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl groups. The lipid particle is suitable for delivering an active agent.

Abstract: An esteramide compound of the following formula (I): R1OOC-A-CONR2R3??(I) is described, wherein: A is a covalent bond or a methylene group —CH2—; R1 is an optionally substituted, saturated or unsaturated aliphatic or cycloaliphatic hydrocarbon group including from 5 to 36 carbon atoms, R2 and R3, either identical or different, are groups selected from a hydrogen atom, and optionally substituted hydrocarbon groups, preferably including from 1 to 36 carbon atoms, and R2 and R3 not being simultaneously hydrogen atoms. Also described, are applications for using the esteramide compound, notably as a solvent.

Abstract: The use of an esteramide compound, alone or as a mixture of the following formula (I): R1OOC-A-CONR2R3??(I) is described, wherein: A is a covalent bond or a methylene group —CH2—, R1 is an optionally substituted hydrocarbon group having from 1 to 36 carbon atoms, R2 and R3, either identical or different, are groups selected from a hydrogen atom and optionally substituted hydrocarbon groups comprising from 1 to 36 carbon atoms, R2 and R3 may form together a ring having the nitrogen atom to which they are bound, said ring being, if need be, substituted and/or having an additional heteroatom and R2 and R3 not being simultaneously hydrogens. Also described, are applications for using the esteramide compound as a solvent, a co-solvent, a coalescence agent, a crystallization inhibitor, a plasticizer or an agent for increasing biological activity.

Abstract: The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

Abstract: The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

Abstract: A method is provided for producing optically active ?-amino acid benzyl esters. The method includes reacting an optically active ?-amino acid and benzyl alcohols in the presence of an acid, wherein the reaction is carried out under reduced pressure without substantially using a solvent, while distilling off water generated by the progress of the reaction.

Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.

Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.

Abstract: The presently disclosed subject matter provides compounds of the formula, formula (Ia): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, and n are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting acid ceramidase and ceramidase-related activity, and their use as drugs and prodrugs in the treatment and/or prevention of diseases associated with undesirable ceramidase or sphingosine kinase activity, including, but not limited to, cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, asthma, and atopic dermatitis.

Abstract: This invention provides compound having a structure of Formula I or Formula II. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.

Abstract: An object of the present invention is to provide dermatological agents such as whitening agents and hair growth accelerators that contain a compound having high water solubility and a specific structure capable of releasing 2,3-dimethoxy-5-methyl-1,4-dihydroxybenzene (reduced form). A dermatological agent according to the present invention contains a 2,3-dimethoxy-5-methyl-1,4-dihydroxybenzenecarboxylic acid ester derivative represented by the following general Formula (I) or a salt thereof: wherein in the Formula (I), R1, R2 and R3 are specific groups.

Abstract: The invention relates to compouns derived from betulin, and to the use thereof as antibacterial agents in pharmaceutical and cosmetic applications.

Abstract: Particular compounds having a fluorene skeleton are superior in broad utility and stability, as a protecting reagent for liquid phase synthesis of amino acids and/or peptides.

Abstract: The invention relates to compounds of the formula I where the substituents AA1, AA2, o and R have a meaning indicated in claim 1, and to the salts and solvates and mixtures thereof, to a process for the preparation thereof, preparations and the use thereof.

Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.

Abstract: The present invention relates to compositions and uses of novel high penetration compositions or high penetration prodrugs (HPP), in particular HPPs for 4-aminophenol derivatives, which are capable of crossing biological barriers with high penetration efficiency. The HPPs herein are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, due to the ability of penetrating biological barriers, the HPPs herein are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs herein can be administered to a subject through various administration routes.

Abstract: The present invention discloses certain novel prodrugs of florfenicol and/or of florfenicol analogs, including prodrugs of salts pharmaceutically acceptable salts of florfenicol and its analogs, including nitrogen-containing esters of the secondary alcohol group of florfenicol and of its analogs, and pharmaceutically acceptable salts thereof, compositions containing them, and methods of administering them to subjects. In particular embodiments the prodrugs are sufficiently water-soluble to serve the functions needed of a water-soluble prodrug of florfenicol or of a water-soluble prodrug of a florfenicol analog. A certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing florfenicol or the florfenicol analog in question.

Abstract: A probucol or a probucol derivative can be efficiently converted to a monoester or monoether of probucol by reacting the free hydroxyl-containing probucol or a derivative thereof (by which is meant a probucol compound with at least one substituent that is different from that on the parent probucol molecule but which maintains the two free hydroxyl groups) with a Grignard reagent or a lithium reagent that produces a magnesium bromide or lithium salt of probucol or the probucol derivative. The probucol compound anion anion is then reacted with an ester or ether forming compound.

Abstract: Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.

Abstract: The invention relates generally to a novel type of arginine mimetics which are inhibitors of factor Xa; to pharmaceutical compositions which comprise these mimetics; and to the use of these arginine mimetics for producing compositions for antithrombotic therapy.

Abstract: The present invention relates to novel covalent derivatives of alkanolamides of monocarboxylic and dicarboxylic acids with aminoalcohols of general formula (I) which can usefully be used as agonists of the CB2 cannabinoid receptor and hence as drugs active in pathological conditions which can be controlled by stimulation and/or costimulation of this receptor

Abstract: The invention relates to stabilized amido acid compositions. More particularly, the invention relates to compositions of amido acids, such as 6-nonanoylamidohexanoic acid, stabilized with antioxidants. The stabilized amido acid compositions are useful in the manufacture of bleach activators such as sodium nonanamidohexanoyloxybenzenesulfonate. Bleach activators made from the stabilized amido acids of the invention are capable of possessing improved coloration.

Abstract: Aminobutylic acid derivatives of the formula (I) wherein the symbols are as defined in specification; and non-toxic salts thereof. Because of inhibiting matrix metalloproteinase, the compounds of the formula (I) are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, osteoarthritis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, cornea ulcer, metastasis, invasion or growth of tumor cells, autoimmune disease, disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, arota aneurysm, endometriosis, restenosis after PTCA, unstable angina, acute myocardial infarction, transient ischemic attack.

Abstract: The present invention related to an oligocycloalkanoid compound comprising formula (I) wherein m, n, and o are independently an integer from 0 to 2; A1 through A10 are independently a direct link, alkylene, alkylene-O—, carbonyl, oxygen, or sulfur; X and Y are independently hydrogen, hydroxy, alkyl, or in combination an electrophilic group; and R1 through R10 are independently hydrogen, hydroxy, alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, N-, S-, or O-heterocycles, fused or multi-ring aryl with or without hetero ring members, arylalkyl, arylalkenyl, arylalkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, alkoxy, alkenyloxy, alkynyloxy, substituted or unsubstituted aryloxy, substituted or unsubstituted arylalkoxy, alkylacyl, alkenylacyl, alkynylacyl, arylacyl, aroyl, alkylaroyl, aminoaroyl, aminoalkylacyl, aminoalkyl, aminoalkenyl, aminoalkynyl, amino, alkylamino, alkenylamino, alkynylamino, arylamino, dialkylamino, dialkenylamino, dialkynylamino, arylalkylamino, arylalk

Abstract: Compounds of formula I, ##STR1## and the physiologically tolerable salts thereof, wherein the substituents R.sub.1 -R.sub.4 have the meanings given in the specifications and show an activity against inflammatory conditions.

Abstract: The present invention is relative to a chemical method of producing compounds of the general formula (I) ##STR1## starting from compounds of the general formula (II) and (III) ##STR2## under radical conditions. Products I are used as intermediates in the synthesis of bioactive substances.

Abstract: The novel compounds of the formula I ##STR1## in which n is an integer from the range from 4 to 8 and m is an integer from the range from 1 to 4,A is the aliphatic, aromatic, araliphatic or heterocyclic radical of a monobasic to tetrabasic carboxylic acid, andR.sup.1 and R.sup.1', independently of one another, are C.sub.1 -C.sub.24 alkyl or C.sub.5 -C.sub.8 cycloalkyl, are suitable for stabilizing organic material against thermal, oxidative or actinic degradation.

Abstract: The present invention provides alkyl and alkylbenzyl ethers of substituted hydroquinones and pharmaceutical compositions containing them. The present invention further provides methods of using these compounds and compositions to inhibit monoamine oxidase, particularly monoamine oxidase B. The present invention further provides methods for the treatment of diseases involving monoamine oxidase.

Abstract: Disclosed is a substantially optically pure hapten, useful in an immunoassay for dextropropoxyphene and/or nordextropropoxyphene. The hapten corresponds to a specified structural formula (IX).Also disclosed is an immunogen derived from the hapten as well as an antibody raised in response to an immunogen derived from the hapten.Also disclosed is a fluorescent tracer derived from a substantially optically pure compound corresponding to the hapten, the tracer being useful in an immunoassay for dextropropoxyphene and/or nordextropropoxyphene.Also disclosed is an improved immunoassay for determining dextropropoxyphene and/or nordextropropoxyphene in a biological sample involving a step of contacting the sample with antibodies raised in response to the immunogen.

Abstract: Carboxylic acid esters and formamide are efficiently obtained by reacting carboxylic acid amides and formic acid esters, or by reacting carboxylic acid amides, alcohols and carbon monoxide in the presence of a dehydrated condensate of carboxylic acid amide with an alkali metal hydroxide or an alkaline earth metal hydroxide catalyst.

Abstract: An emulsifying agent for emulsion polymerization comprising at least one compound selected from the group consisting of (i) betaine esters of polyoxyalkylene alkyl ethers, (ii) betaine esters of polyoxyalkylene alkylphenyl ethers, (iii) betaine esters of polyoxyalkylene dialkylphenyl ethers, (iv) betaine esters of polyoxyalkylene phenyl ethers having two or more benzene nuclei, and (v) betaine esters of polyoxyalkylene polyol ethers. This emulsifying agent is suitable for use in the emulsion polymerization of polymer emulsions capable of forming a film having an excellent water resistance, transparency, and smoothness.

Abstract: A process for the preparation of the optically active compound [IR-(1.alpha., 2.beta., 3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-6H-purin-6-one, represented by the formula: ##STR1## and novel intermediates are described.

Abstract: A process for preparing N-substituted amino acid esters having the formula (I): ##STR1## wherein R.sub.1 and R.sub.4, the same or different, are an alkyl, aralkyl, cycloalkyl or aryl group; and R.sub.2 and R.sub.3, the same or different,are an alkyl, aralkyl, aryl, heterocycle-alkyl, aminoalkyl or guanidylalkyl, by the reaction of .alpha.-amino acid esters with .alpha.-substituted carboxylic acid esters, under the condition of substantially free from solvent, which can afford their optical isomers in a good yield.

Abstract: This invention provides novel insecticidally and acaricidally active pyrimidine derivatives of formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is selected from alkyl; alkenyl; alkynyl; haloalkyl; haloalkenyl; and cycloalkyl optionally substituted by alkyl or halogen;R.sup.2 is selected from alkyl; haloalkyl; alkoxy; alkylamino; dialkylamino; halogen; cycloalkyl optionally substituted by halogen or alkyl; and phenyl optionally substituted by alkyl, haloalkyl, halogen or alkoxy;R.sup.3 is selected from hydrogen and halogen;R.sup.4 is the residue of an alcohol of formula R.sup.4 -OH which forms an insecticidal ester when combined with chrysanthemic acid, permethrin acid or cyhalothrin acid; andX is selected from oxygen and sulphur.

Abstract: Compounds of Formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.

Abstract: Carboxylic acid esters, industrially important compounds, are obtained by reacting carboxylic acid amides and formic acid esters, or carboxylic acid amides, alcohols and carbon monoxide in the presence of metal alcoholate.

Abstract: The present invention provides a purified compound of the structure; ##STR1## wherein R may be palmitoyl or steroyl. The invention also provides compositions comprising an admixture of the foregoing palmitate and stearate esters.The invention also provides a compound of the structure: ##STR2## The invention further provides pharmaceutical compositions including the aforementioned compounds and compositions and methods of inhibiting the acyl CoA: cholesterol acyltransferase catalyzed conversion of cholesterol to cholesteryl esters.

Abstract: Carboxylic acid esters, industrially important compounds, are efficiently obtained by reacting carboxylic acid amides with formic acid esters in the presence of an inorganic solid acid catalyst.

Abstract: Differentiation of the two enantiotopic groups in prochiral glycerol derivatives gives chiral molecules directly, which in turn are easily converted either into the S-series or into the R-series by selective manipulation of the functional groups.

Abstract: Aphidicolane derivatives of the formula: ##STR1## wherein R.sup.1 stands for hydrogen or a hydroxy radical, R.sup.2 stands for a hydroxy or methyl radical, or the group CR.sup.1 R.sup.2 stands for a keto group; R.sup.3 stands for a formyl or hydroxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.6, wherein R.sup.6 stands for a defined radical or R.sup.2 and R.sup.3 are joined together to form the group --O.CO.OCH.sub.2 --; R.sup.4 stands for a hydroxy radical; R.sup.5 stands for a formyl radical, a hydroxyalkyl radical --(CH.sub.2).sub.1-3 OH, a radical --CHR.sup.7 OH, wherein R.sup.7 stands for a defined radical, or R.sup.5 stands for an azidomethyl or pyrrolidinylcarbonyloxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.8, wherein R.sup.8 stands for a defined radical, or R.sup.5 stands for the group --CH.sub.2 O.CO.(CH.sub.2).sub.m.CR.sup.11 R.sup.12.(CH.sub.2).sub.n.NR.sup.9 R.sup.10, wherein m, n, R.sup.9, R.sup.10, R.sup.11 and R.sup.12 have defined values, or R.sup.

Abstract: Mono- or bis-complex esters or ethers of a phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined mono- or bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus; whereinA is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, whereinR.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, whereinR.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; whereinR.sup.12 is hydrogen or alkyl, and whereinR.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.

Abstract: The present invention provides certain novel substituted naphthalenes, indoles, benzofurans, and benzothiophenes of Formula I which are useful as inhibitors of leukotriene biosynthesis and as inhibitors of lipoxygenase. They are thus employed wherever it is medically necessary or desirable to inhibit these systems.

Abstract: Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## and pharmaceutically acceptable salts thereof are disclosed.

Abstract: The subject invention relates to novel cyclopropanone hydrate derivatives of the structural formula ##STR1## whereinR.sub.1 and R.sub.2 are selected from the group consisting of --H, --(CH.sub.2).sub.n -- where n is an integer between 1 and 20, preferably 2 and 10, --COCH.sub.2 NH.sub.2, and ##STR2## and R.sub.3 and R.sub.4 selected from the group consisting of --H, --OH, 13 NH.sub.2, --CN, --COOR.sub.5, --COOH, --SH, --(CH.sub.2).sub.n OH, --(CH.sub.2).sub.n NH.sub.2, --(CH.sub.2).sub.n COOH, --(CH.sub.2).sub.n COOR.sub.5, --CCH.sub.3 OH (CH.sub.2).sub.n COOH, halogen and C.sub.7 -C.sub.10 arakyls, where n is an integer between 1 and 20, preferably 1 and 10, and R.sub.5 is an alkyl radical having between 1 and 20, preferably 1 and 10, carbon atoms;and to a process for the synthesis thereof.