Abstract: Novel acitretinamide compounds which are soluble and stable in water and useful in aqueous delivery systems, particularly to treat cancer, are provided. The novel acitretinamide compounds, 1-(D-glucopyranosyl)acitretinamide, 1-(D-glucopyranuronosyl)acitretinamide and the metal salts thereof, are hereinafter collectively referred to as the "acitretinamide compounds". The invention also relates to novel methods of making the acitretinamide compounds.

Abstract: The invention relates to a process for converting Taxol A, B and C to Taxol primary amine which can then be easily and efficiently converted to Taxol A or docetaxel, thereby significantly increasing the yield of these products from biomass. The method includes the removal of the amide from the side-chain with Schwartz's reagent to form an imine, followed by the hydrolysis of the imine to the primary amine. The primary amine can then be converted to Taxol A or docetaxel. New Taxol imine compounds and primary amine salts have been formed by this process.

Abstract: There are provided methods to control mono-cotyledenous weed species in the presence of crops and particularly in the presence of cereal crops. Also provided are 4-(2,6-disubstituted-phenoxy)coumarin derivatives useful as herbicidal agents and methods to prepare same.

Abstract: A method is provided for oxidizing an olefin to an epoxide by treating the olefin with hydrogen peroxide and a carbodiimide in the presence of an acid or base in a solvent system comprising a protic solvent. More specifically, a method is provided for oxidizing an olefin to an epoxide by contacting the olefin with aqueous hydrogen peroxide and a carbodiimide in the presence of a mild acid or mild base in a solvent system comprising a protic solvent.

Abstract: Preparation of 4-hydroxy substituted butyrolactones is described. A process for the preparation of 3-hydroxybutyrolactone, 1,2,4-trihydroxybutane and 3,4-dihydroxy acid methyl ester from malic acid is particularly described. The preparation of 4-hydroxymethyl-4-hydroxybutyric acid -1-methyl ester and 4-hydroxymethyl butyrolactone is particularly described. The compounds are intermediates to various pharmaceutical and agricultural products.

Abstract: An intermediate for the production of (3-oxo-2-oxobicyclo?3,1,0!hexan-1-yl) methanol represented by formula (II): ##STR1## selected from the group of compounds (9)-(11) as shown below, wherein R.sup.1 represents a lower alkyl group, R.sup.3 and R.sup.

Abstract: Novel taxoids are provided having enhanced water solubility and/or improved pharmacological properties as compared to paclitaxel. The subject taxoids comprise a functional group attached to a paclitaxel at the C-2' and/or C-7 position by a linking group. Functional groups present in the subject taxoids may be hydrophilic chains, groups capable of in vivo conversion to hydrophilic chains, targeting moieties capable of specifically binding with cellular receptors and water soluble polymers of at least 5 kD. The subject taxoids find use in the treatment of hosts suffering from a cellular proliferative disease.

Abstract: The amide derivative of the present invention is one represented by the following general formula (I) and the dermatologic preparation of the present invention is one containing said amide derivative. ##STR1## wherein R.sup.1 represents a straight-chain or branched, saturated or unsaturated hydrocarbon group carrying 10 to 40 carbon atoms; R.sup.2 represents a straight-chain or branched, saturated or unsaturated hydrocarbon group carrying 3 to 39 carbon atoms; R.sup.3 represents a group containing at least one group represented by the formula: ##STR2## wherein R.sup.4 and R.sup.5 each represents a hydrogen atom or a straight-chain or branched or cyclic, saturated or unsaturated hydrocarbon group, or R.sup.4 and R.sup.

Abstract: A group of 2-amino-3-aroyl-benzo?.beta.!thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the .alpha.-hydroxy thioamide, and subsequently acylating the benzo?.beta.!thiophene to yield the 2-amino-3-aryl derivative. These compounds may be treated with suitable phenyl Grignard reagents, and after deprotection, yield 6-hydroxy-2-(4-hydroxyphenyl)-3-?4-(2-peperidinoethoxy)benzoyl!benzo?.beta .!thiophene.

Abstract: This invention provides novel physiologically active substances PF1092A, PF1092B and PF1092C, which can inhibit binding of progesterone to progesterone receptor. These substances were obtained by culturing a fungal microorganism belonging to the genus Penicillium using a medium containing ordinary nutrients for microorganisms and isolating the physiologically active substances PF1092A, PF1092B and PF1092C from the resulting culture mixture by means of solvent extraction, silica gel column chromatography, and the like. Molecular formulae of the novel physiologically active substances PF1092A, PF1092B and PF1092C are C.sub.17 H.sub.20 O.sub.5, C.sub.17 H.sub.20 O.sub.5 and C.sub.15 H.sub.18 O.sub.4, respectively.

Abstract: Viral and bacterial contaminants present in biological solutions are inactivated by mixing one of a novel class of photosensitizer with said solution and irradiating the mixture.

Abstract: Halichondrin derivatives, isolatable from a marine sponge of the Lissodendoryx Sp., have cytotoxic preparations and are of the formula: ##STR1## wherein R.sup.1 and R.sup.

Abstract: Process for the synthesis of a-substituted acrylic acids and their application.Process for the synthesis of a-substituted acrylic acids of general formula (I) and their application to the synthesis of N- (mercaptoacyl) aminoacid derivatives of formula (II).

Abstract: A method for esterifying C13 deoxy taxoid intermediates employs three steps, i.e., oxygenation of the C13 deoxy taxoid intermediate to produce a C13 enone taxoid intermediate; reduction of the C13 enone to produce an alcohol; followed by esterification of the C13 alcohol. Key intermediates include C13 deoxy taxoids; C13 enone substituted taxoids; and C1-C2 cyclo carbonate esters of taxoids.

Abstract: Titanostannosilicalites molecular sieves as new compositions of matter have been found to be very selective, active catalysts in the epoxidation of olefins by peroxides. Dilute hydrogen peroxide suffices to afford high yields of the epoxide with good selectivity. The sieves described within have a unit empirical formula, on an anhydrous basis of (Ti.sub.x Sn.sub.y Si.sub.z)O.sub.2, where 0.0005<x<0.03, 0.0001<y<0.

Abstract: Direct oxidation of propylene to propylene oxide is accomplished using alkaline earth metal compound-supported silver catalysts containing an inorganic chloride promoter and a potassium promoter derived from a potassium salt containing a nitrogen oxyanion or precursor thereof.

Abstract: Olefins are selectively converted to epoxides using hydrogen peroxide as oxidant in a single liquid phase reaction system characterized by a liquid phase comprised predominantly of an organic solvent. The reaction is catalyzed by a compound comprised of a phosphate-stabilized peroxotungstate species having a W:P atomic ratio of 2:1.

Abstract: A cyclopropane derivative represented by formula (I): ##STR1## wherein B represents a group of a purine derivative. Another aspect of the invention provides (3-oxa-2-oxobicyclo?3,1,0!hexan-1-yl)methanol and a method of preparing a cyclopropane derivative of formula (I) from this compound by replacing the hydroxyl group of the compound with a leaving group followed by reaction with a purine derivative.

Abstract: This invention relates to taxoids of the formula (I): a method for preparing these taxoids, and pharmaceutical compositions containing them. In formula (I), R is alkyl radical (1-6 carbon atoms), alkenyl (2-6 carbon atoms), alkynyl (2-6 carbon atoms), cycloalkyl (3-6 carbon atoms), cycloalkenyl (4-6 carbon atoms), phenyl, unsaturated heterocyclyl containing from 5 to 6 links, Z is a hydrogen atom or a radical of formula (II): ##STR1## wherein R.sub.1 is an optionally substituted benzoyl radical, thenoyl radical, furoyl radical, or a radical R.sub.2 --O--CO-- in which R.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl, and R.sub.3 is an alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, naphthyl or aromatic heterocyclic radical. The taxoids of formula (I) in which Z is a radical of formula (II) have remarkable antitumoral and antileukemic properties.

Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of ##STR2## which are the same or different, is an aryl group or a heteroaromatic ring group; A is a C.sub.3-8 linear saturated or unsaturated aliphatic hydrocarbon group which may have substituent(s) selected from the group consisting of a lower alkyl group, a hydroxyl group, a lower alkoxy group, a carboxyl group, an aryl group and an aralkyl group; Q is a single bond or a group of the formula --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --OCH.sub.2 --, --SCH.sub.2 --, --CH.sub.2 O-- or --CH.sub.2 S--; each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which are the same or different, is a hydrogen atom, a halogen atom, a lower alkyl group, a hydroxyl group, a lower alkoxy group, or an aryl or heteroaromatic ring group which may have substituent(s) selected from the group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; each of R.sup.5, R.sup.6 and R.sup.