Abstract: A process for the preparation of substituted anthraquinones is provided. The anthraquinones can be used to prepare pharmaceutically useful rheins.

Abstract: A process for the preparation of antibiotics of the anthracycline class of formula (A), wherein R.sup.1 is hydrogen, OH, or OCOR.sup.2, wherein R.sup.2 is a C.sub.1 -C.sub.4 -alkyl group; which comprises the epimerization of the 4' hydroxy group of the daunosamine residue by nucleophilic substitution of a triflate group with a carboxylate, which epimerization is carried out on the whole molecule with the hydroxy groups being protected, and subsequent transformation into the final product.

Abstract: N-monosubstituted 4-aminopiperidine is prepared by a process comprising, in a single stage, continuously passing a 4-oxopiperidine and a primary amine over a metal hydrogenation catalyst under a hydrogen partial pressure of 1-500 bar at a LHSV of up to 1 hr.sup.-1.

Abstract: Catalytic reactions are carried out in a reactor which contains a liquid phase in which at least one catalyst is suspended, and which may additionally contain a gas phase, by a process in which the liquid phase and, if present, also the gas phase are fed, at least partly, through an apparatus having orifices or channels in the reactor, the hydraulic diameter of which orifices or channels is from 0.5 to 20 mm, preferably from 1 to 10 mm, particularly preferably from 1 to 3 mm.

Abstract: The invention relates to novel 1-acyl-4-aliphatylaminopiperidine compounds of ##STR1## formula (I), in which R.sub.1 is a benzoyl, naphthoyl or cycloalkanoyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl; R.sub.2 is cycloalkyl or a phenyl or naphthyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen, nitro, cyano and/or trifluoromethyl; R.sub.3 and R.sub.4 together are lower alkylene or aza-, oxa- or thia-lower alkylene; or R.sub.3 is lower alkyl, lower alkoxy-lower alky, di-lower alkylamino-lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); and R.sub.4 is hydrogen, lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); R.sub.

Abstract: Adducts of vinyldioxo compounds comprising a crosslinkable silyl-functional terminal group are disclosed. Such adducts are useful for preparing curable coating compositions.

Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.

Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.

Abstract: The present invention provides illudin analogs of the general formula (I): ##STR1## where R.sub.1 is (CH.sub.2).sub.n --X--Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C.sub.1 -C.sub.8)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.4)alkyl or cyclo(C.sub.3 -C.sub.6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R.sub.2 is absent; or R.sub.1 and R.sub.2 together comprise a 5-7 membered cyclic ring;R.sub.3 is (C.sub.1 -C.sub.4)alkyl or H; R.sub.4 is H, SCH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl, O--(C.sub.5 --C.sub.12)aryl or --S--(C.sub.5 -C.sub.12)aryl; R.sub.5 is H, OH or absent; R.sub.6 is (C.sub.1 -C.sub.4)alkyl or absent; R.sub.7 is OH or OSi((C.sub.1 -C.sub.4)alkyl).sub.3 ; orR.sub.6 and R.sub.7 together are ethylenedioxy;R.sub.8 is optionally substituted (C.sub.1 -C.sub.4)alkyl; andthe bonds represented by -- are individually present or absent.

Abstract: A method for preparing 1,3-dioxane compounds of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2, independently of one another, represent hydrogen or a hydrocarbon radical; and X.sup.1 and X.sup.2, independently of one another, represent an electronegative groups, which method entails reacting a bis(hydroxymethyl) compound of the formula (II): ##STR2## in which X.sup.1 and X.sup.2 each, independently of one another, are as defined above, with an orthocarboxylic acid ester of the formula R.sup.4 --C(OR.sup.5).sub.3 (III), in which R.sup.4 represents hydrogen or a hydrocarbon radical and R.sup.5 represents a hydrocarbon radical, and with an aldehyde or ketone of the formula R.sup.1 --CO--R.sup.2 (IV), in which R and R each, independently of one another, are as defined above.

Abstract: Processes for efficiently producing .alpha.-halo ketones, .alpha.-halohydrins and epoxides on an industrial scale. The prosesses include one for producing an .alpha.-halo ketone of general formula (3) by decarboxylating a product of reaction between a carboxilic acid derivative of general formula (1) and a metal enolate prepared from an .alpha.-haloacetic acid of general formula (2) or an acceptable salt thereof, one for producing an by reducing the .alpha.-halo ketone (3), and one for producing an epoxide (13) by treating the .alpha.-halohydrin (11) with a base to effect ring closure. The above prosesses are particularly suitable for producing optically active .alpha.-halo ketones, .alpha.-halohydrins and epoxides from the corresponding .alpha.-amino acid derivatives.

Abstract: The present invention provides certain 6-hetarylalkyloxy pyrimidine derivatives of formula II ##STR1## wherein R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hetero atom chosen from O, N, or S, or a substituted derivative thereof; or (ii) phenyl or a substituted derivative thereof,R.sup.2 is selected from H, C.sub.1 -C.sub.5 alkyl, halogen or NH.sub.2,R.sup.4 and R.sup.5 which are the same or different are selected fromH, NH.sub.2 or NO.sub.n where n=1 or 2, or R.sup.4 and R.sup.5 together with the pyrimidine ring form a 5-or 6-membered ring structure containing one or more heterocyclic atoms, and pharmaceutically acceptable salts thereof, exhibit the ability to deplete O.sup.6 -alkylguanine-DNA alkyltransferase (ATase) activity.

Abstract: The present invention relates to 2,6-diaminopurine-.beta.-D-ribofuranuronamide derivatives of the following formula (I). These compounds and their salts and solvates are useful as anti-inflammatory agents, particularly in the treatment of patients with inflammatory conditions who are susceptible to leukocyte-induced tissue damage.

Abstract: Compounds of general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkylmethyl or phenyl-(C.sub.1 -C.sub.3)alkyl group optionally substituted on the phenyl ring with one or more atoms or groups chosen from halogens and methyl, trifluoromethyl, methoxy and cyano groups, R.sub.2 represents a hydroxyl or alkoxy group or a group of general formula NR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 each represent a hydrogen atom, an alkyl group, a cycloalkyl group, a cycloalkylmethyl group, a phenyl group, a phenylmethyl group or a pyridyl group, or alternatively R.sub.3 and R.sub.4 form, together with the nitrogen atom, a pyrrolidine or piptzidine ring, and n represents the number 1, 2 or 3.Application in therapy.

Abstract: Biologically active compounds such as pheromones and precursors thereof are produced by catalyzed cross metathesis of dissimilar terminal olefins or of a cyclodiene and a terminal olefin.

Abstract: A process for the preparation of chromanyl derivatives of the formula I ##STR1## where R.sup.1 is hydrogen, C.sub.1 -C.sub.8 -alkyl, aryl, aralkyl, Si(R.sup.4).sub.3, C(.dbd.O)R.sup.4 or C.sub.1 -C.sub.4 -alkoxymethyl,R.sup.2 and R.sup.3 are hydrogen or C.sub.1 -C.sub.3 -alkyl, andR.sup.4 is C.sub.1 -C.sub.8 -alkyl or aryl,which comprises decarboxylating 5-carboxychromanyl derivatives of the formula II ##STR2## where the substituents R.sup.1 to R.sup.3 are as defined above and 5-carboxylchromanyl derivatives of the formula II.

Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and pharmaceutically acceptable solvates of either entity, wherein A is optionally monosaturated C.sub.1 -C.sub.4 alkylene optionaly monounsaturatred with C.sub.1 -C.sub.4 alkyl; B is C.sub.1 -C.sub.3 alkylene optionally substituted with C.sub.1 -C.sub.4 alkyl; R.sup.1 is N-amidino-4-piperidyl or 4-amidinophenyl; R.sup.2 is C.sub.4 -C.sub.12 alkyl; (C.sub.3 -C.sub.8 cycalkyl)C.sub.1 -C.sub.4 alkylene; optionally methylene-bridged C.sub.5 -C.sub.8 cycloalkyl optionally substituted with one to three C.sub.1 -C.sub.4 alkyl groups or with hydroxy; C.sub.5 -C.sub.8 alkenyl; C.sub.5 -C.sub.8 cycloalkenyl optionally subsituted with C.sub.1 -C.sub.4 alkyl; piperidyl N-substituted with C.sub.1 -C.sub.4 alkyl; tetrahydrothiopyranyl or tetrahydropyranyl; and R.sup.3 is H or C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy or with hydroxy; or R.sup.2 and R.sup.

Abstract: A process for preparing piperid-2-one by reacting polymers of delta-valerolactone having a molecular weight of from 200 to 20,000 with ammonia under an inert atmosphere at temperatures of from 250 to 500.degree. C. and pressures of from 30 to 500 bar in valerolactone or in an inert solvent thereby avoiding the use of any special catalyst.

Abstract: A halogenated compound (I) containing one or more >C.dbd.O, olefinic and/or aromatic >C.dbd.C< groups is hydrogenated for producing a halogenated compound (II) having no or a decreased level of >C.dbd.O, olefinic and/or aromatic >C.dbd.C< groups. In the hydrogenation process a liquid feed stream comprising one or more of these compounds (I) is contacted with a hydrogen-rich gaseous stream and a liquid recycle stream comprising one or more of these compounds (II) in the presence of a catalyst.

Abstract: A composition for inactivating a target nucleic acid which comprises an oligonucleoside alkyl or arylphosphonate analogue which is complementary to the sequence of the target nucleic acid and includes a functional group which reacts with the target nucleic acid to render the target nucleic acid inactive or nonfunctional.