Abstract: The semisynthesis of paclitaxel and its analogs using new intermediates which are derivatives of 10-deacetyl-baccatin III, as well as to a method for preparing these derivatives. These novel derivatives have alkyl carbonate or alkyl carbonyl substituents in the 7 position.

Abstract: Process for preparing N-pyruvyl-L-proline by reaction of L-proline with methyl pyruvate dimethyl ketal in the presence of an alkali metal alkoxide, subsequent acid hydrolysis and extraction of 1-pyruvyl-L-proline.

Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.

Abstract: The salt of a sulfonated succinic acid is cyclized, then converted to novel sulfonated hydroxamic acids by reaction with hydroxylamine (which is added or formed in situ), and the novel hydroxamic acid is then cyclized to the sulfo-N-hydroxysuccinimide salt. This synthetic procedure is simple, direct, and more rapid than present procedures for synthesis of the succinimide. Novel sulfo-hydroxamic acid intermediates are formed during this procedure.

Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.

Abstract: The present invention involves a rapid synthesis of .sup.18 F-FMISO and analogs thereof. New precursors such as 1-(2'-nitro-1'-imidazolyl)-2-0-acetyl-3-0-tosylpropanol, glycerol-1,3-ditosylate-2-0-acetylate, 1-(2'-nitro-1'-imidazolyl)-2,3-0-diacetyl-4-0-tosylbutanol and threitol 1,4-di-tosylate-2,3-0-diacetylate, are also important aspects of the invention.A further aspect of the invention is the development of a hydrophilic PET ligand to image tumor hypoxia. Erythrotosyl analogue of 2-nitroimidazone (Ts-ETNIM) was prepared from a mixture of 2-nitromidazole, ditosylthreitol and cesium carbonate at 60.degree. C. for 1 hr. Ts-ETNIM was isolated at 70% yield. ?.sup.18 F!fluoroerythronitroimidazole (FETNIM) was then prepared from Ts-ETNIM and K.sup.18 F/kryptofix.RTM.. The yield for ?.sup.18 F!FETNIM was 26-30% (60 min, decay corrected). Results of biodistribution and PET studies indicate that ?.sup.18 F!FETNIM has the potential to detect tumor hypoxia and is indicated to be less neurotoxic.

Abstract: A process is provided for the preparation of .alpha.-tocopherol. According to the process, a condensation reaction between trimethylhydroquinone and a specific phytol derivative or isophytol is conducted in the presence of any one of the following solvents:(i) a carbonate ester,(ii) a lower fatty acid ester represented by the following formula:R.sup.1 COOR.sup.2wherein R.sup.1 means a lower alkyl group having 1-4 carbon atoms and R.sup.2 means a lowe alkyl group having 1-5 carbon atoms with the proviso that methyl acetate and ethyl acetate are excluded;(iii) a mixed solvent of a nonpolar solvent and a lower alcohol having 1-5 carbon atoms; and(iv) a mixed solvent of the nonpolar solvent and the lower fatty acid ester.

Abstract: Methods and compounds for inhibiting aldehyde dehydrogenase are disclosed. The compounds are useful as pharmaceutical compositions in methods for therapeutically treating alcohol consumption in a human.

Abstract: The present invention relates to polycyclic iminooxadiazinediones A corresponding to formula I ##STR1## The present invention also relates to mixtures of these polycyclic iminooxadiazinediones with other isocyanate derivatives and to their use for the production of optionally foamed polyurethane plastics, for the production of paints and coatings and for the production or formulation of active ingredients, pharmaceutical products, etc.

Abstract: The invention relates to a process for the preparation of substituted 3-amninobenzonitriles, which comprises reacting the appropriate substituted 3-aminochlorobenzene with a cyano-donating reagent, and to the compounds thereby produced. The compounds are intermediates, which after further reaction, produce 1,2,3-benzothiadiazole-derivatives having plant immunizing properties.

Abstract: Diketopyrrolopyrroles of formula I ##STR1## are prepared by reacting a diketopyrrolopyrrole of formula II ##STR2## with a) formic acid or b) a compound of formula IIIX'--H (III)or with an alkali metal formate or alkaline earth metal formate together with carbon monoxide in the presence of a catalyst, wherein, in formulae I, II and III, A is a direct bond or a group ##STR3## wherein phenylene is bound to the pyrrolopyrrole, R.sub.1, R.sub.2 and R.sub.3 are each independently of one another hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.6 alkylmercapto, --CF.sub.3, --CN or --NO.sub.2, X is X' or OH, X' is --OR.sub.4 or --N(R.sub.5)(R.sub.6), wherein R.sub.4 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.6 cycloalkyl; phenyl or naphthyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, --CN or --NO.sub.2, R.sub.5 and R.sub.

Abstract: Unprotected adenine, 6-chloropurine, 2,6-diaminopurine, and 2-amino-6-chloropurine have been directly coupled with 2-(diethoxyphosphonomethoxy)ethanol under a disclosed method to provide acyclic phosphonate nucleotide analogues which are intermediates for antiviral agents such as 9-?2-(phosphonomethoxy)ethyl!adenine (PMEA) and its analogues having a structure of formula I: ##STR1## wherein Z represents N or CH; R.sub.1 represents hydrogen, alkyl, aryl, or arylalkyl; R.sub.2 and R.sub.3 are independently selected from H, OH, halo, NH.sub.2, C.sub.6 H.sub.5 CH.sub.2 O, or R.sub.4 R.sub.5 N wherein R.sub.4 and R.sub.5 are independently selected from alkyl, aryl, or arylalkyl.

Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.

Abstract: Novel derivatives of benzofuran and dihydrobenzofuran are provided which are useful as melatonergic agents.

Abstract: 1. WF16616 substance represented by the following structural formula (1) or its pharmaceutically acceptable salt. ##STR1## WF16616 substance exhibits an antimicrobial activity, especially an excellent antifungal activity.

Abstract: The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.

Abstract: The present invention provides novel thiadiazole derivatives represented by formula I: ##STR1## or pharmaceutical acceptable salts thereof wherein the compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, predominantly stromelysins, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthritis, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis (invasion and growth), periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, and other diseases related to connective tissue degradation.

Abstract: An article of manufacture illustrated in the form of an impeller having a rotor extending in radial directions from a central axis to an outer periphery and a plurality of vanes unitary with the rotor and extending from the rotor in axial directions essentially parallel to the central axis, each vane having a length along an axial direction, is constructed of a structural composite including a plurality of layers of reinforcing fibers in a matrix of synthetic polymeric material, each layer extending essentially parallel to the radial directions, the layers being juxtaposed with one another along the axial direction, the reinforcing fibers of each layer being woven in a pattern essentially perpendicular to the central axis, and further reinforcing fibers extending in the axial directions and stitched through the juxtaposed layers, the further reinforcing fibers extending within each vane, along the length of each vane, essentially parallel to the length of the vanes.

Abstract: Novel anti-microbial sesquiterpene compounds isolated from the fruit bodies of Roseofomes subflexibilis (Hounen-take) having the general formula ##STR1##

Abstract: Disclosed are catalyst systems comprising one or more transition metals selected from the Group VIII metals and rhenium and one or more fluorophosphite compounds having the general formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrocarbyl radicals. Also disclosed are catalyst solutions comprising one or more the above fluorophosphite compounds, rhodium and a hydroformylation solvent, and hydroformylation processes wherein olefins are contacted with carbon monoxide, hydrogen and the catalyst solution to produce aldehydes.