Abstract: A non-steroidal compound suitable for use as an inhibitor of oestrone sulphatase. The compound has a polycyclic ring structure comprising two or more rings wherein at least two of the rings mimic the A and B rings of oestrone. The compound can have the general formula A wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R1-R6 is a sulphamate group; and wherein X is any one of O, S, NH, a substituted N, CH2 or a substituted C.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.

Abstract: The invention relates to a process of preparing a chiral compound of the formula: wherein R1 is selected from the group consisting of hydrogen and lower alkyl, and R2 and R2′ are the same, and R2 and R2′ are selected from a group consisting of hydrogen and primary alkyl, or R2 and R2′ taken together form a C3 to C6 cycloalkyl, comprising the steps of chirally reducing a &bgr;-keto ester to afford a &bgr;-hydroxy ester, activating the &bgr;-hydroxy ester by treatment with a sulfonic acid or a derivative thereof to provide an activated compound having sulfonate leaving group, displacing the sulfonate leaving group with an azido moiety, or treating the activated compound with an alkylamine, deprotecting and cyclizing to afford a pyrrolidinone, and reducing the pyrrolidinone to afford a stereoisomerically preferred 3-aminopyrrolidine derivative.

Abstract: There is disclosed a method of producing acetals, which comprises reacting a compound of formula (I), at least one compound selected from a group consisting of a compound of formula (II), paraformaldehyde, and trioxane; and a compound of formula (III), to synthesize an acetal of formula (IV), wherein the reaction is carried out in the presence of an oxidizing agent and an acid:  wherein R1 is an alkyl group etc., R2 is an alkyl or aryl group, R3 and R4 each independently are a hydrogen atom, an alkyl group or an aryl group, X1 and X2 each are a group of nonmetal atoms necessary to form a 5- or 6-membered N-containing heteroring, and M is a hydrogen atom or a cation. This method can give acetal compounds with good efficiency and a high yield.

Abstract: Epoxides of formula having a cyclanic (1R) configuration, the group in position 2 being in a trans configuration and the epoxy group being in a cis configuration with respect to that in position 1 of the ring, and in which R represents a lower alkyl group and R1 represents a saturated or unsaturated, linear or branched hydrocarbon group having from 1 to 8 carbon atoms, are useful molecules for the preparation of very prized perfuming ingredients. A process for the preparation of the epoxides (I) is also described.

Abstract: The invention relates to a novel process for producing thereof hydroxyarenes of the general formula (I) in which n represents the numbers 1, 2, 3 or 4, R represents cyano, carboxyl, formyl, nitro, halogen or represents alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylcarbonyl or alkoxycarbonyl, each of which is optionally substituted, and Z represents hydrogen, cyano, nitro, halogen, alkyl, halogenoalkyl, or represents monocyclic or bicyclic, saturated or unsaturated heterocyclyl, heterocyclylamino or heterocyclylimino, each of which is optionally substituted, characterized in that halogenoarenes of the general formula (II) in which n, R and Z are each as defined above and X represents halogen are reacted with 3-hydroxy-propionitrile of the formula (III), HO—CH2CH2—CN  (III), if appropriate in the presence of a reaction auxiliary and if appropriate in the presence of a diluent, at temperatures between 0° C. and 100° C.

Abstract: wherein R1, R2, R3 and R4 are selected independently from each other from —NR5R6, —NR5R6R7+, hydrogen, aryl or heteroaryl with up to 7 ring members, C1-C20-alkyl, C1-C20-alkenyl and C1-C20-alkinyl, wherein the alkyl, alkenyl and alkinyl residues can be branched, unbranched or cyclized and optionally substituted with halogen, aryl or heteroaryl with up to 7 ring members, with the proviso that at least one of the residues R1, R2, R3 and R4 are represented by —NR5R6 or —NR5R6R7; and R5, R6 and R7 are selected independently from each other from hydrogen, aryl or heteroaryl with up to 7 ring members, C1-C20-alkyl, C1-C20-alkenyl, C1-C20-alkinyl, wherein the alkyl, alkenyl and alkinyl residues can be branched, unbranched or cyclized and optionally substituted with halogen, aryl or heteroaryl with up to 7 ring members, or R5 and R6, together with the nitrogen atom, form a heterocyclic group with up to 7 ring members; for the regulation of the activity of already activ

Abstract: Compounds having Formula I ##STR1## are useful for modulating the glucocorticoid receptor in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of treating immune, autoimmune, inflammatory, adrenal imbalance, cognitive and behavioral diseases in a mammal.

Abstract: A process of manufacturing acrylonitrile or methacrylonitrile by the catalytic reaction in the vapor phase of a paraffin selected from propane and isobutane with molecular oxygen and ammonia by catalytic contact of the reactants in a reaction zone with a catalyst, the feed composition having a mole ratio of the paraffin to ammonia in the range of from about 2.5 to 16 and a mole ratio of paraffin to oxygen in the range of from about 1.0 to 10, wherein said catalyst has the elements in the proportions indicated by the empirical formula:VSb.sub.m A.sub.a D.sub.b Q.sub.q R.sub.r O.sub.xwhereA is one or more of Ti, Sn, Fe, Cr and Ga;D is one or more of Li, Mg, Ca, Sr, Ba, Co, Ni, Zn, Ge, Zr, Cu, Ta, Bi, Ce, In, B and Mn;Q is one or more of Mo, W, and Nb;R is one or more of As, Te, and Se;m equals 0.8 to 4;a equals 0.01 to 2;d is 0 to 2;0.ltoreq.q<0.01; preferably 0<q<0.01, especially 0<q<0.005q+r are greater than 0;x is determined by the oxidation state of the cations present.

Abstract: The present invention provides an improved process and intermediate compounds for the preparation of difluorovinylsilane insecticide and acaricidal agents of the formula I ##STR1## wherein Ar is phenyl, 1- or 2-napthyl or a 5- or 6-membered heteroaromatic ring, each of which may be optionally substituted by any combination of from one to three halogen,C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, haloalkoxy, C(O)R.sub.2 or S(O).sub.n R.sub.3 groups,R and R.sub.1 are each independently C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.5 cycloalkyl;Ar.sub.1 is phenoxyphenyl, phenyl, biphenyl, phenoxypyridyl, benzylpyridyl, benzylphenyl,1- or 2-napthyl or a 5- or 6-membered heteroaromatic ring, each of which may be optionally substituted by any combination of from one to five halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy or C(O)R.sub.4 groups,n is an integer of 0, 1 or 2;R.sub.2 and R.sub.4 are each independently C.sub.

Abstract: 1,3,6-Trihydro-6-Aza-3-Oxapentalen-2-One Derivatives of Formula I are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasia: ##STR1## Wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, lower alkyl, and benzyl,R.sub.3 and R.sub.4 are selected from the group consisting of substituted or unsubstituted phenyl, and the like,R.sub.5 is selected from the group consisting of hydrogen, lower alkyl, and the like,Y is selected from the group consisting of CH.sub.2, C.dbd.O, CH--OH; m is an integer from 0-3; X is selected from the group consisting of CH.sub.2, C.dbd.O, CH--OH, and SO.sub.2 ; and n is an integer from 0-2.

Abstract: An oxonol compound is represented by the following formula (I): ##STR1## in which Z is an atomic group that forms a cyclic amide ring; each of W.sup.1 and W.sup.2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.

Abstract: An efficient and scalable method is reported for the isolation of costatolide (2), an HIV-1-specific nonnucleoside reverse transcriptase inhibitor (NNRTI), from the latex of Calophyllum plants such as C. teysmannii var. inophylloide. An overall yield of 10.6% of costatolide, with a purity of 96%, was obtained by repetitive recrystallization of the latex from a single organic solvent after the oily material was removed by treatment with hexane. A second major component of the latex, soulattrolide (3), another HIV-1 NNRTI, was also isolated. Both compounds were characterized by spectroscopic and chromatographic analyses and their in vitro anti-HIV activities were also confirmed. The results suggest that sufficient supplies of costatolide can be obtained in a relatively low-cost manner from natural sources.

Abstract: Compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.

Abstract: A process for the preparation of a 5,5'-bi-1H-tetrazole diammonium salt by dropwisely adding the aqueous hydrogen peroxide to which a small amount of weakly acidic substance has been added, to a starting aqueous solution containing hydrogen cyanide or sodium cyanide or potassium cyanide, sodium azide and a catalytic amount of copper sulfate preferably at a low temperature to maintain the pH of the reaction solution over a range of from 5 to 6, heating the reaction solution to effect the oxidation and cyclization reaction, reacting the reaction product with ammonium chloride or an aqueous solution thereof, and recovering the formed ammonium salt in the form of sparingly soluble crystals. The desired product is obtained in a high yield and in a high purity from the starting materials which are cheaply available and are easy to handle through a decreased number of steps, i.e., through a one-pot reaction without requiring cumbersome after-treatment.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof.The compounds of formula I are useful in the treatment of a variety of cancers. In addition, the formula I compounds may also be useful in the treatment of diseases other than cancer.

Abstract: The present invention relates to mixtures of cyclic oligocarbonates, to their production by way of mixtures of bischloroformates, and to their use for the production of linear polycarbonates and for the modification of other linear polycarbonates.

Abstract: The present invention relates to a Raney catalyst comprising iron, cobalt, a third metal wherein the third metal is selected from the group consisting of nickel, rhodium, ruthenium, palladium, platinum, osmium, iridium and mixtures of any of the metals of this group.

Abstract: Manufacture of a molecule which is of important olfactory interest for perfumers. This molecule belongs to the group of macrocyclic lactones with a musk odor. The manufacturing process consists in preparing cis-16-hydroxy-9-hexadecenoic acid or an ester of this acid, which is a precursor of cis-isoambrettolide, the latter being obtained by macrolactonization in a very high degree of purity. Use as a fragrance material.

Abstract: The invention relates to compounds of formula (I) ##STR1## wherein R.sub.1 is an electronegative substituent, preferably nitro, cyano, formyl or carboxy, R.sub.2 is --A--R.sub.4, wherein A is a branched or straight chain C.sub.1-9 alkylene and R.sub.4 is carboxy or 5-tetrazolyl; R.sub.3 is an electronegative substituent, preferably nitro, cyano, halogen, formyl, carboxy, C.sub.1-5 alkyl carbonyl, aryl carbonyl or SO.sub.2 R.sub.6, wherein R.sub.6 is a branched or straight chain C.sub.1-5 alkyl, aryl alkyl, aryl or NR.sub.7 R.sub.8, wherein R.sub.7 and R.sub.8 are independently hydrogen, a branched or straight chain C.sub.1-5 alkyl or together form a C.sub.3-6 ring; or a pharmaceutically acceptable ester or salt thereof. The compounds are peripheral, long acting COMT (catechol-O-methyl transferase) inhibitors and are useful, e.g., in the treatment of Parkinson's disease and hypertension.