Abstract: Disclosed are 13.alpha.-(3-substituted-2-hydroxypropionyloxy)baccatin compounds represented by the formula: ##STR1## wherein R.sup.1 represents a lower alkanoyl group or a protective group for hydroxy group; R.sup.2 represents a protective group for hydroxy group; R.sup.3 represents a lower alkanoyl group; R.sup.4 represents a substituted or unsubstituted benzoyl group; X represents a substituted or unsubstituted aryl group, a substituted or unsubstituted lower alkenyl group, or a substituted or unsubstituted lower alkynyl group; and A' represents a halogen atom, azido group or amino group,and processes for preparing the same.

Abstract: Disclosed is a compound of formula VII: ##STR1## where Ar represents an optionally substituted phenyl or .alpha.- or .beta.-naphthyl radical; R.sub.3 represents hydrogen, a C.sub.1-4 alkyl radical, a C.sub.2-4 alkenyl radical, an aralkyl radical, or an aryl radical; and R.sub.4 represents hydrogen, a C.sub.1-4 alkyl radical, a C.sub.2-4 alkenyl radical, an aralkyl radical, or an aryl radical; or alternatively R.sub.3 and R.sub.4, together with the carbon atom to which they are linked, form a 4- to 7-membered ring; and R.sub.5 represents an C.sub.1-4 alkyl radical substituted with at least one chlorine atom. The compound of formula VI may be used to manufacture a compound of formula VIII: ##STR2## where Ar, R.sub.3, R.sub.4 and R.sub.5 are defined above; G.sub.1 represents a group protecting the hydroxyl function; and where appropriate, G.sub.2 represents a group protecting the hydroxyl function.

Abstract: An efficient protocol for the synthesis of taxol, taxol analogs and their intermediates is described. The process includes the attachment of the taxol A-ring side chain to baccatin III and for the synthesis of taxol and taxol analogs with variable A-ring side chain structures. A rapid and highly efficient esterification of O-protected isoserine and 3-phenylisoserine acids having N-benzyoloxycarbonyl groups to the C-13 hydroxyl of 7-O-protected baccatin III is followed by a deprotection-acylation sequence to make taxol, celphalomanninne and various analogs, including photoaffinity labeling candidates.

Abstract: Disclosed are a process and intermediates of the formulae ##STR1## wherein X.sup.- is halide, BF.sub.4.sup.-, R.sup.3 SO.sub.3.sup.-, wherein R.sup.3 is C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkylphenyl or phenyl, and Q is a group of the formula ##STR2## wherein R is C.sub.1 -C.sub.6 alkyl; useful for preparing benzazepine intermediates of the formula ##STR3## These benzazepine intermediates are useful for preparing benzazepines having activity as selective D1 receptor antagonists.

Abstract: Compounds of the formula ##STR1## in which: n is 0, 1 or 2, and, if n is 2, the two radicals R.sub.3 are identical or different;R.sub.2 is methyl, fluorine, chlorine or bromine;R.sub.3 is C.sub.1 -C.sub.3 -alkyl, halo-C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo-C.sub.1 -C.sub.3 alkoxy, fluorine, chlorine or bromine:R.sub.5 is hydrogen or C.sub.1 -C.sub.9 alkyl andX is methylene, O, S or C(.dbd.O):can be used as intermediates for agrochemical active ingredients.

Abstract: There is disclosed a process of producing a 2-cyano-4-oxo-4H-benzopyran compound of the general formula (2): ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, hydroxy, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, nitro or a group of the RCONH wherein R is C.sub.1 -C.sub.20 alkyl, phenyl, phenyl-substituted (C.sub.1 -C.sub.20) alkyl, phenyl (C.sub.1 -C.sub.20)alkoxyphenyl or (C.sub.1 -C.sub.20) alkoxyphenyl. This production process is characterized in that a carboxamide of the general formula (1): ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, is reacted with a dehydrating agent in the presence of a pyridine compound of the general formula (4): ##STR3## wherein A.sup.1 and A.sup.2 are independently hydrogen or C.sub.1 -C.sub.5 alkyl.

Abstract: The amide derivative of the present invention is one represented by the following general formula (II) and the dermatologic preparation of the present invention is one containing said amide derivative. ##STR1## wherein R.sup.11 represents a straight-chain or branched hydrocarbon group carrying 10 to 40 carbon atoms; R.sup.12 represents a straight-chain or branched hydrocarbon group carrying 1 to 39 carbon atoms; R.sup.13 represents a hydrogen atom or a hydrocarbon group carrying 1 to 6 carbon atoms; and R.sup.14 represents a hydrogen atom or a hydrocarbon group having a straight-chain, branched or cyclic structure and carrying 1 to 40 carbon atoms which may contain an oxygen atom.

Abstract: A novel process for extraction, isolation and separation of taxanes, particularly paclitaxel, from natural sources such as bark, needles and twigs from Taxus species, tissue cultures, and fungi is described, wherein the taxanes are separated from the crude extracts by partitioning between polar and nonpolar solvents, precipitation in nonpolar solutions, reacting the mixture by halogenation of unsaturated taxane derivatives, followed by chromatographically separating and crystallizing taxanes from a mixture of polar and nonpolar solvents; more particularly, the process of halogenation of unsaturated side chain taxane derivatives, particularly cephalomannine in presence of paclitaxel, is described, wherein bromine is preferably added to the double bond of unsaturated taxanes leaving paclitaxel unchanged, with paclitaxel being easily separated from the mixture including the less polar halogenated taxane derivatives.

Abstract: This invention relates to a process for preparing taxoid derivatives of formulae II and XI: ##STR1## in which Ar represents an aryl radical; R.sub.1 represents a benzoyl radical or a radical R.sub.2 --O--CO-- in which R.sub.2 represents an unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl, or saturated or unsaturated heterocyclic radical; R.sub.3 represents an unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, saturated or unsaturated heterocyclic, or aryl radial, but not a phenyl radical; R.sub.4 represents a hydrogen atom and R.sub.5 represents a hydroxyl-protecting group or R.sub.4 and R.sub.5 together form a heterocyclic group; G.sub.1 represents a hydroxyl-protecting group; and G.sub.

Abstract: Psoralen compound compositions are synthesized which have substitutions on the 4, 4', 5', and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.

Abstract: A chemiluminescent 1,2-dioxetane derivative having a formula (I): ##STR1## wherein R.sup.1 and R.sup.4 each represent, individually, hydrogen, an alkyl group, an alkoxyl group, a hydroxyl group, or --OSi(R.sup.9 R.sup.10 R.sup.11) in which R.sup.9, R.sup.10 and R.sup.11 each represent an alkyl group; R.sup.2, R.sup.3, R.sup.5 and R.sup.6 each represent, individually, hydrogen or an alkyl group, provided that R.sup.2, R.sup.3, R.sup.5 and R.sup.6 each cannot be hydrogen at the same time, and that R.sup.2 and R.sup.3, and R.sup.5 and R.sup.6, each taken together, can form a cycloalkyl group; R.sup.7 represents an alkyl group; R.sup.8 represents hydrogen, an alkoxyl group, a phosphate salt group, or --OSi(R.sup.9 R.sup.10 R.sup.11); intermediates for synthesizing the above 1,2-dioxetane derivative; and methods of producing the intermediates are provided.

Abstract: A process for the preparation of a .gamma.-lactone of the formula ##STR1## which can be used to produce a single enantiomer of aminoazanoradamantane which is coupled to aromatic acid moieties to produce compounds useful as 5-HT agonists or antagonists.

Abstract: In accordance with the present invention, there are provided polymeric drug delivery systems in which the drug is bound to a water-soluble polymer to provide a form of soluble drug delivery especially for those cases in which the drug by itself is water-insoluble. In particular, the drug taxol is covalently bound to water-soluble polyethylene glycols such as linear polyethylene glycols, branched polyethylene glycols, star polyethylene glycols, and branched copolymers of polyethylene glycols with other functional monomers to comprise a form of polymeric drug delivery. Also, crosslinked insoluble gels of these materials are prepared to serve as a form of implantable drug delivery.

Abstract: Benzopyran derivatives represented by formula (I): ##STR1## wherein X represents .dbd.O, .dbd.S, .dbd.N--Z, etc. (Z represents a lower alkyl group, etc.); Y represents a substituted amino group, an alkoxy group, an alkylthio group, etc., and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 each represents a hydrogen atom, a lower alkyl group, etc, are disclosed. The benzopyran derivative exhibit K.sup.+ channel opening activities and are widely applicable as antiasthmatics, antiepileptics, and the like.

Abstract: Compound of formula (I): ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3, which are identical or different, represent hydrogen or halogen or alkyl, nitro, cyano or aminosulfonyl, or alternatively, when two of them are located on adjacent carbons, form, with the carbon atoms to which they are attached, (C.sub.3 -C.sub.7) cycloalkyl ring or substituted or unsubstituted benzene ring,R.sub.4 represents hydrogen, linear or branched (C.sub.1 -C.sub.6) alkyl, substituted or unsubstituted phenyl or a group ##STR2## in which R.sub.6 and R.sub.7, which are identical or different, represent hydrogen or substituted or unsubstituted, linear or branched (C.sub.1 -C.sub.6) alkyl,R.sub.5 represents hydrogen, hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy, phenoxy, mercapto, linear or branched (C.sub.1 -C.sub.6) alkylthio, substituted or unsubstituted, linear or branched (C.sub.1 -C.sub.6) alkyl, substituted or unsubstituted phenyl or substituted or unsubstituted amino, or a group ##STR3## in which R.sub.6 and R.sub.

Abstract: The practicality of known depolymerization reactions in which there is a danger of building up adherent residues on heat transfer surfaces is greatly improved by performing the process under conditions that provide a driving force which assures that none of the feed material and none of any liquid or solid residue produced during the depolymerization of the feed material remains in contact with any heat transfer surface for a time sufficiently long to form any adherent solid residue on the surface. A preferred apparatus for achieving such a driving force includes a horizontal thin film evaporator, a controlled continuous input of liquid feed material, and continuous collection of desired reaction product and any residue that remains condensed throughout its passage through the reaction zone.

Abstract: The present invention concerns antitumor compounds. More particularly, the invention provides novel taxane derivatives, pharmaceutical compositions thereof, and their use as antitumor agents.

Abstract: The invention relates to an environmentally friendly process for the preparation of compounds of the formula below ##STR1## in which R.sup.1 and R.sup.2 are preferably H or alkyl, R.sup.3 and R.sup.4 are preferably alkyl or cycloalkyl, R.sup.5 and R.sup.6 are preferably hydrogen or methyl and R.sup.7 is in particular alkyl. In the process, the additional use of a phase transfer catalyst can be dispensed with without loss in yield.

Abstract: The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.

Abstract: The reaction mixture obtained in the production of 2,3-epoxypropyltrialkylammonium chlorides by treatment of chlorohydroxypropyltrialkylammonium chlorides with alkaline acting materials in aqueous medium containing impurities which create problems in the subsequent use of the 2,3-epoxypropyltrialkylammonium chloride. According to the invention the reaction mixture is freed from these impurities by separating it from undissolved impurities by employing at least about 0.2 mole of 2,3-epoxypropyltrialkylammonium chloride per mole of water.