Abstract: The present invention relates to compounds with a dioxane nucleus derived from carbohydrates and C-glucosides, process for obtaining same, to the use of such compounds as cytotoxic and antiproliferative agents and to the use thereof for producing a cancer treatment drug.

Abstract: The present invention involves a new synthesis route for the formation of lactylates. The method comprises reacting a dilactide with a compound comprising a hydroxy group. This reaction is preferably carried out in the presence of a cation or other source of alkalinity. Preferred compounds comprising a hydroxy group include any fatty acid and fatty acid alcohol (particularly C1-C26 fatty acid chains). Preferred cations include cations of Group I and II metals, with sodium, calcium, and potassium cations being particularly preferred. The inventive reactions proceed much more rapidly than prior art lactylate synthesis reactions, and can be used to form 1-, 2-, 3-, 4-, and 5-lactylates.

Abstract: The present invention relates to a method for the hydrothermolysis of a mono- and/or oligosaccharide-comprising composition which in addition comprises at least one monoalkyl and/or dialkyl ether of a polyalkylene glycol, and also relates to a hydrothermolysis device.

Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.

Abstract: The present invention relates to compounds with a dioxane nucleus derived from carbohydrates and C-glucosides, process for obtaining same, to the use of such compounds as cytotoxic and antiproliferative agents and to the use thereof for producing a cancer treatment drug.

Abstract: Compounds derived from acetone are provided. Particularly, the compounds are derivatives of hydroxyacetone, including dimers of both 1-hydroxyacetone and 1,3-dihydroxyacetone. The hydroxy moieties on the core hydroxyacetone molecule serves as an attachment point for a variety of moieties (e.g., ethers, esters, phosphorous containing, or nitrogen containing) that are selected to provide the compound with a particular property. Applications of the compounds include plasticizers, supersurfactants, and additives for health care products, such as shampoo and perfume.

Abstract: The present invention relates to a process for preparing tetramethylglycolide by heating a composition which comprises at least 50% by weight of 2-hydroxy-isobutyric acid and/or tetramethylglycolide to a temperature of at least 100° C.

Abstract: A PEPCK inhibitor can include identifying a molecule that has a size capable of fitting into and interacting with the PEPCK binding site and at least one of the following: (a) a first terminal substituent having co-planar atoms acting as metal ligands to the active site metal ion PEPCK; (b) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent includes a neutral carbon center or include an oxygen, sulfur, selenium, or other atom with similar physiochemical properties; (c) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent is devoid of an electropositive atom or substituents; or (d) a second terminal substituent opposite of the first terminal substituent, said second terminal substituent having an atom that is a hydrogen boding acceptor and/or is negatively charged.

Abstract: The present disclosure discloses a catalyst for directly producing a lactide which is a cyclic ester used as a monomer for polylactides, and a method for directly producing a lactide using the catalyst, the method including the transesterification reaction between two molecules of an ester of lactic acid or a mixture containing the ester of lactic acid with a small amount of lactic acid and oligomer of lactic acid under an inert environment in the presence of a titanium-based catalyst or a catalyst mixture containing the titanium-based catalyst so as to produce lactide while simultaneously removing an alcohol (ROH) generated as a by-product.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The raw material used in most process for the production of cyclic diesters of alpha-hydroxyacids, such as Lactide and Glycolide, is a 10% solution of Hydroxyacid. During the evacuation of the solution and condensation reaction water, the organic molecules may be damaged. The present process is characterized by the use of reactants that bring as little water as possible to the reactor. In particular, for the production of Lactide, the main reactant may be anhydrous Calcium Lactate, that will react at about room temperature, for instance, with Sulfuric Anhydride, to give a solid mixture of Lactide, Calcium Sulfate Dihydrate and Calcium Sulfate Hemihydrate. Partial dehydration of the Dihydrate under mild temperature is followed by distillation of the Lactide out of the remaining powder of Calcium Sulfate Hemihydrate, and desublimation of the Lactide. Purification of the Lactide is done in situ in the desublimator.

Abstract: The present invention is directed to multifluoro-substituted Chalcones and analogs thereof, represented by the general Formula I: wherein Ar and R6-R10 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The present invention provides compounds having a cyclopentabenzofuran core and the use of such compounds in therapy as well as compositions comprising said compounds.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The present invention relates to orthocarbonate pro-fragrances useful for delivery of sustained perfume or fragrance to fabric treated with a laundry detergent composition which comprises the herein described pro-fragrances. The orthocarbonate pro-fragrances are also suitable for use in hard surface cleaning compositions. The orthocarbonate pro-fragrances are further suitable for use in personal care compositions. The present invention also relates to method for delivering a pleasurable scent to fabric which has a lasting freshness quality by contacting the fabric with the fragrance-releasable orthocarbonate pro-fragrances of the present invention.

Abstract: A process is provided for the production and purification of cyclic esters in which the purification includes the introduction of an aqueous solvent into a cyclic ester containing composition and allowing two phases to form. A first phase includes cyclic esters and any organic solvent, and a second phase includes the aqueous solvent and impurities.

Abstract: A process is provided for the production and purification of cyclic esters in which the purification includes the introduction of an aqueous solvent into a cyclic ester containing composition and allowing two phases to form. A first phase includes cyclic esters and any organic solvent, and a second phase includes the aqueous solvent and impurities.

Abstract: Processes are disclosed for the recovery of 1,4-dioxanone by melt crystallization from a feed containing impurities capable of initiating the polymerization of 1,4-dioxanone, e.g., diethylene glycol. The processes of the present invention utilize melt crystallization in a cyclic process involving the steps of (i) crystallizing the 1,4-dioxanone out of the feed at a temperature below its melting point and removing a liquid residue containing a higher concentration of impurities, (ii) partially melting the crystallized 1,4-dioxanone to further remove impurities and (iii) thereafter, melting the remaining crystallized 1,4-dioxanone and recovering the melted product. The crystallization process can be repeated as required to achieve the desired purity. The purity of the product obtained is typically 99.5 wt %, 1,4-dioxanone or higher. The purified 1,4-dioxanone is useful, for example, as a monomer in the production of polydioxanone.

Abstract: Reducing the adherence of polyethercyclicpolyol to metal by exposing the metal to a selected surfactant.

Abstract: This invention relates generally to insolubilizers for use with binders in paper coating compositions. There is provided a process for preparing both an insolubilizer and paper coating composition containing the insolubilizer and a binder which, when applied onto paper products, significantly enhances their wet-rub resistance.The insolubilizer is prepared by:(a) forming a glyoxal-urea adduct by reacting from about 1.0 to about 4.0 moles of glyoxal with about 1.0 mole of urea, at an elevated temperature,(b) cooling the glyoxal-urea adduct to room temperature,(c) adding from about 0.5 to about 2.0 moles of free glyoxal to the glyoxal-urea adduct to form an oligomer, and(d) adjusting the pH of the oligomer to from about 5 to about 7.

Abstract: Disclosed is a novel integrated process for production of cyclic esters which includes recovery of starting materials, such as lactic acid from a dilute aqueous lactic acid-containing solution, by solvent extraction. The starting materials are then formed into cyclic esters by removal of water wherein the concentration of higher molecular weight oligomers is maintained below about 20 wt % of the reaction composition. The process further includes providing a recovery solvent for the reaction composition and separating the cyclic esters from the starting materials and higher molecular weight oligomers by liquid-liquid equilibrium separation. The present invention is further directed toward independent novel unit operations of the overall process. The present invention provides for the efficient production and recovery of cyclic esters due to integration of the various unit operations by use of appropriate solvents and recycle streams.

Abstract: A process for the conversion of glycoside substituted taxanes to taxol and related compounds that can serve as precursors to taxol. The process includes the oxidation of glycoside substituted taxanes to convert the glycoside to the hydroxyl group. The oxidation can occur in the presence of an acid or followed by treatment with acid. Application of the process to 7-xylosyl taxol ("XT") yields taxol; application to other glycoside substituted taxanes forms compounds that can serve as precursors for taxol. The process includes the formation of certain new taxol related intermediate compounds having a hemialdal at the C-7 site on the taxane ring, which hemialdal can then be converted to taxol or taxol precursors. Since glycoside substituted taxanes are isolated with taxol from naturally occurring biomass, their conversion to taxol using the process of the present invention significantly improves the total yield of taxol from natural sources.

Abstract: The invention relates to pharmaceutical compositions comprising an effective cytotoxic amount of: ##STR1## Wherein R represents Ac or H; R' represents: ##STR2## OH; and R" represents: ##STR3## these new compounds demonstrate surprising tubulin binding activity and cytotoxicity.

Abstract: Disclosed is a method for producing cyclic esters by the conversion of hydroxy carboxylic acids and their derivatives to their respective cyclic esters. Such cyclic esters, including lactide or glycolide, are particularly useful for producing polymers which can be used to make biodegradable materials, such as biodegradable packaging material. Various methods of cyclic ester production are disclosed, including liquid phase and vapor phase reactions. Also disclosed are various methods for recovering cyclic esters from product-containing streams.

Abstract: The present invention is directed to a method for making L-lactide from aqueous L-lactic acid. Aqueous lactic acid feed for present purposes comprehends an aqueous mixture of one or more of L.sub.1 A, L.sub.2 A, and L.sub.3 A, optionally with LD being present. L-lactic acid is the preferred feed configuration for making L-lactide, and is to be understood even though the configuration symbol is not used throughout this application. Aqueous lactic acid feed is treated for removal of water therefrom until a degree of polymerization (DP) not substantially above about 2 is reached. The treatment then is ceased to produce a crude LD product. LD then is separated from the crude LD product. A preferred treatment involves heating the feed at elevated temperature to remove water. LD can be separated from the crude LD product by a variety of techniques to produce an LD-depleted product.

Abstract: Non-peptidyl compounds characterized generally as chromonyl/chromonylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.7 are taken together to form a partially saturated or fully saturated heterocyclic ring containing five to eight ring members with one or two ring members being oxygen atoms and the remaining ring members being carbon atoms, and which heterocyclic ring may be optionally substituted with lower alkyl; or a pharmaceutically-acceptable salt thereof.

Abstract: Non-peptidyl compounds characterized generally as benzofuranyl/benzofuranylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.

Abstract: The invention concerns a cyclic ether derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo-(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene, or a 6 membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 and R.sup.2 together form a group of the formula --A.sup.2 --X--A.sup.3 -- wherein each of A.sup.2 and A.sup.3 is (1-6C)alkylene and X is oxy, thio, sulphinyl, sulphonyl or imino; andR.sup.3 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

Abstract: Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from cycloalkyl and cycloalkylalkyl groups, wherein said cycloalkyl group contains three to about eight carbon atoms and the acyclic alkyl portion of said cycloalkylalkyl group contains one to about eight carbon atoms; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl: wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.

Abstract: Non-peptidyl compounds characterized generally as heterocyclic acyl aminodiol .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are compounds of the formula ##STR1## wherein R.sub.1 is selected from aryl and aralkyl groups represented by ##STR2## and wherein R.sub.1 may be further selected from heteroaryl and heteroaralkyl represented by ##STR3## wherein each of T and A is independently selected from N and CH; wherein n is a number selected from zero through five, inclusive; wherein X is selected from oxygen atom, methylamino and NH; wherein each of Y and Z is independently selected from chloro, fluoro, methoxy and dimethylamino; wherein Q is oxygen atom; and wherein each of T and A is independently selected from N and CH; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is selected from methyl and ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; wherein R.

Abstract: Cyclohexenone oxime ethers ##STR1## where R.sup.1 is alkyl;A is substituted or unsubstituted alkylene or alkenylene, where methylene is replaced by an oxygen atom, a sulfur atom, a sulfoxyl group, a sulfonyl group or --NR.sup.a --,Z is phenyl or a 5- or 6-membered heteroaromatic structure;X is substituted or unsubstituted amino, nitro, cyano, halogen, alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbony or phenyl;n is 0 to 3, or 1 to 5 where X is halogen;R.sup.

Abstract: A compound of the formula: ##STR1## wherein the dotted line represents optional unsaturation; R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido or sulfonamido or R.sup.1 and R.sup.2 together are methylenedioxy, ethylenedioxy or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2,3 or 4; X is O or NR.sup.4, in which R.sup.4 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof, are antipsychotic agents.

Abstract: The invention relates to compounds of formula: ##STR1## in which m, n, p and q are equal to 0 or 1, p being different from q and the sum m+n+p+q being equal to 2, A denotes a nonionic chain arrangement chosen from the groups:--C.sub.2 H.sub.4 O--.sub.rand/or--C.sub.3 H.sub.5 (OH)O--.sub.s,in which r denotes a number which can assume all integral values between 0 and 5 or a statistical average value between 0 and 20,s denotes a number which can assume all integral values between 0 and 5 or a statistical average value between 0 and 10,u is equal to 0 or 1, with the restriction that when u=0, s and r are also zero,R denotes(i) a linear or branched hydrocarbon radical which has 1 to 32 carbon atoms and can contain one or more oxygen atoms in the chain or bear one or more OH groups or(ii) a (C.sub.8 -C.sub.18 alkyl)phenyl radical.These compounds can be used for preparing stable chemical compounds, for conveying active substances or for forming vesicles.

Abstract: The invention relates to compounds of formula: ##STR1## in which m, n, p and q are equal to 0 or 1, p being different from q and the sum m+n+p+q being equal to 2, A denotes a nonionic chain arrangement chosen from the groups:--C.sub.2 H.sub.4 O--.sub.rand/or--C.sub.3 H.sub.5 (OH)O--.sub.s,in whichr denotes a number which can assume all integral values between 0 and 5 or a statistical average value between 0 and 20,s denotes a number which can assume all integral values between 0 and 5 or a statistical average value between 0 and 10,u is equal to 0 to 1, with the restriction that when u=0, s and r are also zero,R denotes(i) a linear or branched hydrocarbon radical which has 1 to 32 carbon atoms and can contain one or more oxygen atoms in the chain or bear one or more OH groups or(ii) a (C.sub.8 -C.sub.18 alkyl)phenyl radical.These compounds can be used for preparing stable chemical compounds, for conveying active substances or for forming vesicles.

Abstract: New 1,4-dioxanes of the formula I ##STR1## wherein R.sup.1 and R.sup.2 each signify and alkyl group with 1 - 10 C-atoms, wherein one or two CH.sub.2 groups can also be replaced by O-atoms, F, Cl, Br or CN,R.sup.2 also H,A.sup.1 and A.sup.2 each signify 1,4-phenylene, 1,4-cyclohexylene, 1,3-dioxane-2,5-diyl, 1,4-dioxane-2,5-diyl, peperidine-1,4-diyl, 1,4-bicyclo(2,2,2)-octylene or pyrimidine-2,5-diyl groups, unsubstituted or substituted by 1 - 4 F-atoms,Z.sup.1 and Z.sup.2 each signify --CO--O--, --O--CO--, CH.sub.2 CH.sub.2 --, OCH.sub.2 -- --CH.sub.2 O-- or a single bond,m and n each signify 0, 1, 2 or 3,(m+n), however, are at least 1 and at most 3,whereby for m=2 or 3, the groups A.sup.1 and for n=2 or 3 the groups A.sup.2 can each be the same or different from one another,as well as the acid-addition salts of the basic ones of these compounds,are suitable for use as components of liquid-crystalline dielectrics.

Abstract: Paper coating compositions contain at least one pigment, at least one binder, and, as an insolubilizer for the binder, the product of the reaction of glyoxal and a vicinal polyol.

Abstract: The invention provides novel 1-substituted-5-hydroxymethyl-2-mercapto-imidazoles of the formula ##STR1## wherein R is pyridylmethyl, alkyl of 1 to 4 carbon atoms, or a radical of formula: ##STR2## in which R.sub.1 is hydrogen or halogen and n is 1-3. These compounds are prepared by reacting together dihydroxyacetone dimer, the amine R--NH.sub.2, and potassium thiocyanate. The compounds of formula (I) are useful as starting materials in the preparation of known therapeutically valuable imidazole derivatives, by removing the mercapto group, oxidizing the alcohol group to an aldehyde group and condensing the aldehyde with an appropriate phenyl or phenylalkyl magnesium halide.

Abstract: A smoking tobacco composition having incorporated therein a dioxane compound as a flavorant-release additive which under normal smoking conditions imparts improved flavor to mainstream smoke and improved aroma to side-stream smoke.

Abstract: Paper coating compositions contain at least one pigment, at least one binder, and, as an insolubilizer for the binder, the product of the reaction of glyoxal and a vicinal polyol.

Abstract: A process for preparing glycol aldehyde by reacting formaldehyde, hydrogen and carbon monoxide at elevated temperature and superatmospheric pressure in the presence of rhodium catalyst and conversion thereof to ethylene glycol as the substantially exclusive polyol product.