Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: A multivalent cationic lipid having a positively-charged head group including two quaternary amine groups and a hydrophobic portion including four hydrocarbon chains, which may be the same or different and which are optionally substituted alkyl and alkenyl groups, two alkyl chains attached to each of the two quaternary amine groups can be used for the introduction of polyanionic materials such a nucleic acid polymers into cells. Specific cationic lipids are N,N,N?,N?-tetraoleyl-N-N?-dimethyl-1,3-propanediammonium chloride and N,N,N?,N?-tetraoleyl-N-N?-dimethyl-1,6-hexanediammonium chloride.

Abstract: Fluorinated compounds and emulsions including the compounds. The compositions are useful as oxygen carriers and surfactants. In one embodiment, the fluorinated compound is pH sensitive. In one embodiment, the fluorinated compound is a vitamin E derivative. In one embodiment, the fluorinated compound is a vitamin K derivative.

Abstract: The present invention relates to a novel class of gelling agents or thickeners, to a process for preparing gelling agents or thickeners and to their use to prepare the gels. The present gelling agents or thickeners have the form of an N,N?-disubstituted aldaramide or N,N?-disubstituted pentaramide.

Abstract: The present invention relates to an improved synthesis of imidazo[1,2-a]pyridine-3-N,N-dialkylacetamides, including zolpidem tartrate.

Abstract: The invention relates to a process for racemising an enantiomer-enriched Schiff base of a primary amino acid amide with a strong base that is chemically reactive towards water. The reaction is conducted in an organic solvent. Preferably a metal alkoxide, a metal alkyl, a metal amide, or a metal hydride, in particular a metal alkoxide is applied as the strong base. As the Schiff base preferably N-benzylidene primary amino acid amide is used, with the primary amino acid amide preferably being derived from an aliphatic primary amino acid amide, for example tertiary-leucine amide. As organic solvent use is preferably made of an aromatic hydrocarbon, a cyclic, aliphatic hydrocarbon or a ether, in particular an aromatic hydrocarbon is applied. The invention may also be applied for the racemisation of an enantiomer-enriched primary amino acid amide.

Abstract: The present invention relates to a novel class of gelling agents or thickeners, to a process for preparing gelling agents or thickeners and to their use to prepare the gels. The present gelling agents or thickeners have the form of an N,N′-disubstituted aldaramide or N,N′-disubstituted pentaramide.

Abstract: Compounds, in particular those based on polyisobutyleneamines, are suitable as emulsifiers for water-in-oil emulsions and are used in particular as additives for fuels and lubricants.

Abstract: This invention relates to peptide-containing &agr;-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.

Abstract: A composition is provided comprising a novel cationic lipid compound having hydrophobic tails and two quaternary ammonium headgroups bridged by a linker. The composition is useful as a cytofectin for facilitating delivery and transfection of biologically active agents, particularly anionic bioactive agents such as DNA, into cells. The composition is useful also as an adjuvant for enhancing the humoral immune response of a vertebrate to an immunogen, especially an immunogen encoded by a polynucleotide-based vaccine. In certain preferred embodiments, the cationic lipid compound is a dimer containing quaternary ammonium headgroups bridged by a linker having DNA and/or cell receptor binding affinity, such as a polypeptide or polyamine. Also disclosed is an immunogenic composition comprising an immunogen and the composition of the present invention.

Abstract: The present invention discloses the identification of the inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.

Abstract: A lock unimolecular micelle includes at least one engineered acceptor specifically binding a ligand (or specifically a “key” unimolecular micelle) thereto. A key unimolecular micelle comprises a core molecule and a plurality of branches extending therefrom, at least one of the branches including a shank portion extending therefrom having a terminal moiety at an end thereof for binding to a complimentary acceptor of a lock unimolecular micelle. Together, the lock and key micelles form a unit, either irreversibly or reversibly bound wherein the lock micelles is a soluble receptor engineered to specifically bind to the specifically engineered key micelle.

Abstract: The invention relates to novel amino- and amido-diphenyl ethers, processes for their preparation and their use in pharmaceuticals, in particular for the indications of arteriosclerosis and hypercholesterolaemia.

Abstract: A novel tandem acyl-Claisen rearrangement reaction is provided. An allylic reactant such as an allylic amine or an allylic thioether, having at least two functional groups that enable the reactant to undergo at least two successive Claisen rearrangement reactions, is reacted with an acid chloride in the presence of a Lewis acid catalyst composition composed of a Lewis acid and a second catalyst component selected from the group consisting of tertiary amines and non-nitrogenous bases. The stereochemistry of the reaction product is readily controlled by the positioning and size of substituents on the allylic reactant. The reaction may be carried out on a solid support, i.e., on the surface of a substrate suitable for conducting solid phase chemical reactions.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis.

Abstract: A method is described for producing saturated dicarboxylic acids with a chain length of C6 to C21 or the corresponding diamidic dicarboxylic acids from fatty acid cleavage of unsaturated fatty acids or the bis-fatty acid diamides of these unsaturated fatty acids by oxidative ozonolysis and subsequent separation and purification of the dicarboxylic acids, whereby after oxidative ozonolysis, the reaction products are dissolved at a high temperature in a carboxylic acid or a mixture of several carboxylic acids with a medium chain length of C6 to C12 or esters of short-chain alcohols of these carboxylic acids as the recrystallization solvent.

Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Abstract: A new composition of matter for a diamidodiol and a method for preparing the diamidodiol. The exemplary diamidodiol has the formula C15H30N2O4 and is prepared by reacting a first quantity of 2-amino-2-methyl-1-propanol with a second quantity of a di-substituted malonyl dichloride (i.e., diethylmalonyl dichloride), preferably in ethyl acetate as solvent. A tetraamido macrocycle is prepared from the diamidodiol in two steps by oxidizing the diamidodiol to form a diacid followed by coupling using a known procedure of the diacid with an aryl diamine (e.g., 1,2-diaminobenzene) to yield the tetraamido macrocycle.

Abstract: A new composition of matter for a diamidodiol and a method for preparing the diamidodiol. The exemplary diamidodiol has the formula C15H30N2O4 and is prepared by reacting a first quantity of 2-amino-2-methyl-1-propanol with a second quantity of a di-substituted malonyl dichloride (i.e., diethylmalonyl dichloride), preferably in ethyl acetate as solvent. A tetraamido macrocycle is prepared from the diamidodiol in two steps by oxidizing the diamidodiol to form a diacid followed by coupling using a known procedure of the diacid with an aryl diamine (e.g., 1 ,2-diaminobenzene)to yield the tetraamido macrocycle.

Abstract: A urethanized &bgr;-hydroxyalkylamide compound, a process for its preparation, and powder coating materials containing them.

Abstract: A process for preparing polymers of allylic amine compounds comprising: a) preparing a reaction mixture comprising: i) a polar reaction solvent; ii) at least one salt of an allylic amine compound; and iii) a free radical initiator comprising a water soluble non-ionic diazo compound represented by: wherein: R1, R2, R3 and R4 are the same or different lower alkyl groups; R5 and R6 are each independently selected from the group consisting of hydroxyalkyl amide or hydroxyalkyl ester; and b) polymerizing the reaction mixture.

Abstract: A new composition of matter for a diamidodiol and a method for preparing the diamidodiol. The exemplary diamidodiol has the formula C15H30N2O4 and is prepared by reacting a first quantity of 2-amino-2-methyl-1-propanol with a second quantity of a di-substituted malonyl dichloride (i.e., diethylmalonyl dichloride), preferably in ethyl acetate as solvent. A tetraamido macrocycle is prepared from the diamidodiol in two steps by oxidizing the diamidodiol to form a diacid followed by coupling using a known procedure of the diacid with an aryl diamine (e.g., 1,2-diaminobenzene)to yield the tetraamido macrocycle.

Abstract: A new class of useful gasoline additives is prepared via two consecutive reactions including: (1) amidation of water-soluble hydrophilic, low molecular weight triamine with alkyl acetate at an elevated temperature under N2 pressure to prepare a symmetrical triamide; and (2) alkoxylation of the triamides with 1,2-epoxyalkane to prepare poly(oxyalkylene)triamide alkoxylate of three telechelic hydroxy groups, having the general formula: wherein x, y and z are from 1 to 20, R is poly(oxyalkylene) of a molecular weight from 72 to 1000, and R′ is an alkyl having a carbon number from 2 to 18.

Abstract: Process for the continuous preparation of hydroxyalkylamides Process for the continuous preparation of hydroxyalkylamides from carboxylic esters and alkanolamines, wherein the reaction of the starting materials is carried out in an extruder or intensive mixer by intensive mixing and brief reaction with supply of heat and simultaneous removal of the alcohol formed and the final product is then isolated.

Abstract: A multi-branched compound which can give a compound having a relatively high molecular weight but a low viscosity and having excellent coating performances, and can give a solvent-less composition having sufficient coating performances and having a low viscosity sufficient for forming a coating, and which can serve to decrease the amount of a low-molecular-weight compound having performance problems and the multi-branched compound is obtained by reacting a core compound obtained by subjecting (a) a polyamino compound having a molecule containing a primary or secondary amino group and (b-1) an active-hydrogen-containing (meth)acrylic compound in Michael addition reaction with (c) a vinyl-group-containing compound having a functional group reactive with the active hydrogen.

Abstract: The object of the present invention is to provide a novel bioactive substance of value as a therapeutic agent for mycosis, and the like.This invention relates to the bioactive substance TKR1785 of the following general formula (A): ##STR1## (wherein R represents --CH(CH.sub.3).sub.2 or --CH(CH.sub.3)C.sub.2 H.sub.5).

Abstract: Novel chiral boron and aluminum hydride complexes, compositions comprising the chiral hydride complexes, and methods for their synthesis and use are described. The novel chiral hydride complexes are of the formulas:MBH.sub.4-n-a (R*).sub.n (R').sub.a ;MBH.sub.2-b (R**) (R').sub.b ;MBH(R***);MBH(R*) (R");MAlH.sub.4-n-a (R*).sub.n (R').sub.a ;MAlH.sub.2-b (R**)(R').sub.b ;MAlH(R***); andMAlH(R*) (R"),whereinM is Na.sup.+, Li.sup.+ or K.sup.+ ;each R* is independently a monodentate chiral ligand;R** is a bidentate chiral ligand;R*** is a tridentate chiral ligand;R' is a monodentate achiral ligand;R" is a bidentate achiral ligand;n is 1-3;a is 0-2; andb is 0-1,with the proviso that n+a.ltoreq.3, and with the further proviso that when R** is S-BINOL, M is not Li.sup.+.

Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2)a-(X.sub.1).sub.b -Q.sub.1 -Q.sub.2 -C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radical or one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 -R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2, their preparation process and their use as pesticides.

Abstract: Methods and compositions for treating CF by mobilizing mutant forms of CFTR, which retain at least some functional activity, to the plasma membrane where they can mediate chloride ion transport are disclosed.

Abstract: A lock unimolecular micelle includes at least one engineered acceptor specifically binding a ligand (or specifically a "key" unimolecular micelle) thereto. A key unimolecular micelle comprises a core molecule and a plurality of branches extending therefrom, at least one of the branches including a shank portion extending therefrom having a terminal moiety at an end thereof for binding to a complimentary acceptor of a lock unimolecular micelle. Together, the lock and key micelles form a unit, either irreversibly or reversibly bound wherein the lock micelles is a soluble receptor engineered to specifically bind to the specifically engineered key micelle.

Abstract: This invention describes an integrated process for making ethylidene bisformamide in high yield wherein water, which is formed as a reaction by-product, is readily removed from the reaction product mixture without adversely affecting the efficiency of the overall process. The process contemplates isolating the reaction zone from the separation zone and comprises circulating a stream of formamide through a reaction zone containing a solid acidic catalyst and a separation zone; introducing acetaldehyde into the circulating stream of formamide to form a reaction mixture and contacting the reaction mixture with the solid acidic catalyst under reaction conditions sufficient to form a product mixture comprising ethylidene bisformamide and water; and separating water from the product mixture in the separation zone to form a water-depleted product mixture containing ethylidene bisformamide.

Abstract: Methods and compositions for treating CF by mobilizing mutant forms of CFTR, which retain at least some functional activity, to the plasma membrane where they can mediate chloride ion transport are disclosed.

Abstract: An improved process for preparing 1,1'-?1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine, and subsequent dimerization and hydrolyzation/tosylation to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a first step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a second step, and the detosylation of said cyclam dimer in a third step followed by basification to obtain the desired 1,1'-?1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane.

Abstract: A curing agent having less odor and providing a cured resin which is excellent in appearance, mechanical properties, water resistance and chemical resistance, and a one-component type humidity-curing resin composition having excellent storage stability and providing a cured matter which is excellent in appearance and physical properties. Specifically, provided are polyaminoamide or ketimine obtained by dehydration of 2,5- and/or 2,6-bis(aminomethyl)-bicyclo?2.2.1!heptane with carboxylic acids or ketones, a curing agent for epoxy resins using the same and a one-component type humidity-curing epoxy resin or urethane prepolymer composition containing the curing agent.

Abstract: The invention relates to compounds having at least one vinyl ether group which also contain in the molecule at least one further functional group selected from acrylate, methacrylate, epoxy, alkenyl, cycloalkenyl and vinylaryl groups, to compositions, especially for stereolithography, comprising those vinyl ether compounds, and to a method of producing three-dimensional objects using those compositions.

Abstract: Novel complexes of paramagnetic ions and compounds bearing long acyl chains have been synthesized as magnetic resonance imaging contrast agents. These novel liposoluble contrast agents may be administered alone, or with lipids, suspending agents or other additives. The lipids may be in the form of liposomes, micelles or lipid emulsions. The contrast agents of the invention have particular use in magnetic resonance imaging of the liver, blood pool and reticuloendothelial system.

Abstract: An amide derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a C.sub.1-40 hydrocarbon; R.sup.2 represents a C.sub.1-6 alkylene; R.sup.3 represents H, OH or alkoxyl; R.sup.4 represents a C.sub.1-39 hydrocarbon; R.sup.5 represents ##STR2## with the proviso that when R.sup.5 represents ##STR3## R.sup.3 does not represent OH; and a composition of the amide derivative for topical application to human skin. The composition improves the barrier function of the stratum corneum, providing improvement and prevention of dermatitis, skin roughness, or similar disorders.

Abstract: 1,2-di-substituted indan expressed by general formula (I) wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, Y is a halogen atom, and X and Y can be in either cis- or trans-configuration forming either a racemic body or an optically active substance; or 1,2-di-substituted indan expressed by general formula (I') wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, and X and OH group can be in either cis- or trans-configuration forming either a racemic body or an optically-active substance; or cis-1,2-epoxyindan expressed by general formula (VI) wherein R is phenyl or a lower alkyl group, oxazoline ring is in cis-configuration forming either a racemic body or an optically active substance is reacted, under an acidic condition, with a nitrile expressed by general formula (II) wherein R is phenyl or a lower alkyl group to produce cis-1-aminoindan-2-ol

Abstract: The invention relates to novel compositions comprising ene and free radical adducts of unsaturated and saturated hydrocarbons, and acyclic and cyclic vicinal polycarbonyl compounds such as diethyl ketomalonate and indantrione. The adducts are reacted with nucleophiles such as amines, electrophiles such as anhydrides and esters, and metal ions. Post-products are obtained via reaction of said products with capping reagents such as boric acid. Compositions containing said adducts, products and post-products include oleaginous substances such as fuels and lube oils.

Abstract: The present invention relates, by way of novel industrial products, to compounds which are structurally related to 15-deoxyspergualin and which have the formula ##STR1## in which: A is a single bond, a group --CH.sub.2 --, a group --CH.sub.2 O--, a group --CH.sub.2 NH--, a group --CH(OH)--, a group --CHF-- or a group --CH(OCH.sub.3)--, andn is equal to 6 or 8,and their addition salts.These novel compounds are useful especially as immunosuppressants. The invention further relates to the method of preparing said compounds.

Abstract: The invention provides compounds, several of which belong to a class having two or more nonpolar components connected by a polar group and having polar groups on the termini of the compound.The invention also concents a method of selectively inducing termini differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable condition with an amount of the compound effect to selectively induce terminal differentiation.Moreover, the invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells, thereby inhibiting their proliferation and suppressing oncogenicity.

Abstract: Chlorine-substituted olefins I ##STR1## (R.sup.1 =organic radical; R.sup.2 =--CN, --CO--R.sup.3, --CO--S--R.sup.3, --CO--O--R.sup.3 --CO--N(R.sup.4,R.sup.5); R.sup.3 =organic radical; R.sup.4, R.sup.5 =H, organic radical)are prepared by reacting oxiranes II ##STR2## in the presence of a carboxamide (IIIa) or of a lactam (IIIb) in liquid phase with a chlorinating agent (IV). The products I are important intermediates for dyes, drugs and crop protection agents.

Abstract: Disclosed herein are compounds of the formula:A--N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A is various oxygen-bearing radicals; for example, HO--CH(R.sup.3)CH.sub.2 wherein R.sup.3 is, inter alia, hydrogen, lower alkyl, lower cycloalkyl or phenyl; or HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein each of R.sup.5 and R.sup.6 is lower alkyl, or R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, cyclo-alkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.

Abstract: This invention pertains to perfluoropolyethers and perhalogenated chlorofluoropolyethers that can be prepared by fluorinating addition polymers made by polymerizing epoxides.

Abstract: A synergistic mixture of a carbonate and/or bicarbonate with a phosphonate, especially an organoamino methylene phosphonate or an N-oxide thereof, inhibits or reduces nitrosamine contamination during preparation, storage and/or heating of products which are susceptible to contamination with nitrosamine.

Abstract: A continuous process for the production of oxamide is based on the catalytic oxidation of hydrogen cyanide with oxygen or air in a strong excess in a solution of copper nitrate in water-acetic acid.The process is carried out in a vertical tubular reactor, with continuous recycling of part of the suspension of oxamides from the bottom to the top of the reactor.

Abstract: The present invention relates, by way of novel industrial products, to compounds which are structurally related to 15-deoxyspergualin. These novel compounds have the formula ##STR1## in which: n is equal to 6 or 8 andA is a single bond, CH.sub.2, CHF, CH(OH), CH(OCH.sub.3), CH.sub.2 NH or CH.sub.2 O,and their addition salts.

Abstract: Novel complexes of paramagnetic ions and compounds bearing long acyl chains have been synthesized as magnetic resonance imaging contrast agents. These novel liposoluble contrast agents may be administered alone, or with lipids, suspending agents or other additives. The lipids may be in the form of liposomes, micelles or lipid emulsions. The contrast agents of the invention have particular use in magnetic resonance imaging of the liver, blood pool and reticuloendothelial system.

Abstract: A synergistic mixture of a carbonate and/or bicarbonate with a phosphonate, especially an organoamino methylene phosphonate or an N-oxide thereof, inhibits or reduces nitrosamine contamination during preparation, storage and/or heating of products which are susceptible to contamination with nitrosamine.

Abstract: The present invention provides the compound having the structure: wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R1 and R2 are different, R1=R3—N—R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells.