Abstract: It is shown that the potency of anti-cancer drugs, here exemplified by doxorubicin, can be increased by the use of polyunsaturated fatty acid amides and in particular specific combinations of such compounds, forming complexes with doxorubicin. Further, a modified form of doxorubicin is presented.

Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or

Abstract: The present invention provides a novel pyrimidine derivative represented by the general formula (1): (wherein R, R4 and R8 are the same as defined in the specification) or pharmaceutically acceptable salt thereof, which possesses an excellent activity for inhibiting the formation of NO (nitrogen oxide) in vivo.

Abstract: The present invention provides a process for synthesizing a compound or a library of compounds of Formula 1A and 1B:

Abstract: A composition for use in a topical skin formulation such as a shower gel or a bath gel or a cream or lotion, comprises polyalcohol humectant, a mixture of at least two polyquaternary compounds, one of which is a cationic copolymer and one of which is an amphoteric copolymer, the copolymers being present in a weight ratio of cationic copolymer to amphoteric copolymer of 1:1.75 to 1:6, wherein the weight ratio of polyalcohol humectant to the said mixture lies in the range 1:0.06 to 1:0.1. When employed in a topical skin formulation the present combination of humectants provides an improved moisturizing effect.

Abstract: Novel heterocyclyluracils of the formula in which R1, R2 and Het are each as defined in the description, a process for preparing these substances and their use as herbicides.

Abstract: Process for the formation of MeO-Peg-protected dihydroquinine or dihydro quinindine derivatives, new dihydroquinine-or dihyroquinidine derivatives as well as the use thereof. It is known that dihydroquinine or dihydroquinidine derivatives can be successfully used as ligands in the enantioselective dihydroxylation. The new disclosed ligand systems based on dihydroquinine/quinidine, unlike the prior art ligands, can be recycled after enantioselective dihydroxylation by precipitating and filtering the reaction medium, and be reused in the reaction medium. Also disclosed are the ligand systems (I) and (IV), process for preparing the same and their use in the enantioselective dihydroxiation of double bonds.

Abstract: The invention provides pharmaceutically useful thieno[2,3-d]pyrimidinediones, processes for their production, pharmaceutical compositions containing them and methods of treatment involving their use.

Abstract: The present invention relates generally to an asymmetric synthesis of 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones, and intermediates thereof. The target compounds are useful for the treatment of human immunodeficiency virus (HIV) as an inhibitor of reverse transcriptase.

Abstract: 1,3-Dimethylimidazolium 4-carboxylate is prepared by reacting 1-methylimidazole with dimethyl carbonate optionally in the presence of a solvent in accordance with the following reaction scheme:

Abstract: Novel 3-amino-1-cyanophenyl-uracils of the formula in which R1 represents hydrogen or represents in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl, R2 represents hydrogen, cyano or halogen, R3 represents hydrogen, halogen or optionally substituted alkyl, R4 represents optionally substituted alkyl, a process for their preparation and their use as herbicides.

Abstract: A process for advantageously preparing a piperazinesulfonamide derivative represented by the general formula (III): wherein R1 is hydrogen atom, a straight or branched chain alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a halogen atom, hydroxyl group, trifluoromethyl group, nitro group or amino group; R2 is a phenyl group which may have as substituents on its phenyl ring 1 to 3 groups selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a halogen atom, hydroxyl group, trifluoromethyl group, nitro group and amino group, 2-pyridyl group, 3-pyridyl group or 4-pyridyl group; each of R3 and R4 is independently hydrogen atom, a straight or branched chain alkyl group having 1 to 6 carbon atoms, a hydroxyalkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms, or a phenyl group which may be substituted; and Y is an alkylene group having 1 to 12 carbon atoms, and

Abstract: The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.

Abstract: The compound, according to formula (i) wherein X and Y are independently CH, N or N-oxide, provided that X and Y do not both represent CH; Z is CO or CS; R1 is alkyl, optionally substituted with one or more halogens; and R2, R3, R4 and R5 are each various organic groups. Such compounds have therapeutic utility, via inhibition of phosphodiesterase IV.

Abstract: A compound represented by the general formula (I) and a salt thereof: ##STR1## wherein: Rf represents a (C.sub.1 -C.sub.4)haloalkyl group; X.about.Y represents N.dbd.N or CH.dbd.N or the like; A represents a nitrogen atom or CH; Z represents an oxygen or sulfur atom; Rg represents a hydrogen or halogen atom and the like; R1, R2, R3, R4 and R5 are each independently represent a hydrogen or halogen atom or a nitro or cyano group or the like.

Abstract: This invention provides advantageous processes for preparing quinazolinones of Formula I ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.10 alkyl; C.sub.3 -C.sub.10 alkenyl; C.sub.3 -C.sub.10 cycloalkyl; C.sub.3 -C.sub.10 halocycloalkyl; C.sub.4 -C.sub.10 cycloalkylalkyl; C.sub.4 -C.sub.10 halocycloalkylalkyl; or C.sub.3 -C.sub.10 alkynyl;R.sup.2 is C.sub.1 -C.sub.10 alkyl; C.sub.3 -C.sub.10 alkenyl; C.sub.3 -C.sub.10 cycloalkyl; C.sub.3 -C.sub.10 halocycloalkyl; C.sub.4 -C.sub.10 cycloalkylalkyl; C.sub.4 -C.sub.10 halocycloalkylalkyl; C.sub.4 -C.sub.10 cycloalkyl; C.sub.4 -C.sub.10 halocycloalkyl; or C.sub.3 -C.sub.10 alkynyl; andR.sup.3 and R.sup.4 are each independently hydrogen or halogen; from compounds containing the moiety IIg ##STR2## This invention further provides certain compounds of Formula II, IIIa, or IVa ##STR3## where R.sup.7 is C.sub.2 -C.sub.6 alkyl.

Abstract: Triazolo[4,5-d]pyrimidine compounds of the formula ##STR1## where R.sup.1 through R.sup.4 and X are as defined in the specification are provided, together with compositions containing them, a process for their preparation and methods of use. The compounds are useful in the treatment of platelet aggregation disorders and angina.

Abstract: The invention relates to triphendioxazine compounds of the formula (I) ##STR1## where the rings marked with A comprise, independently of one another, rings which are fused linearly in positions 2,3 and 9,10 or angularly in positions 1,2 and 8,9 or 3,4 and 10,11 and have the radical members of the formula (i) --NR.sub.1 (CO).sub.m --NH--, (ii) --CR.sub.1 .dbd.CH--CO--NH--, (iii) --O--CH.sub.2 --CO--NH--, (iv) --CO--CH.dbd.CR.sub.1 --NH--, (v) --CO--NH--CO--NH--, (vi) --CO--NH--CR.sub.2 .dbd.N--, (vii) --CR.sub.2 .dbd.N--CO--NH--, (viii) --NR.sub.1 --(CO).sub.m --O--, (ix) --NH--CR.sub.1 .dbd.N--, (x) --NH--CO--CR.sub.1 .dbd.N--, (xi) --NH--CO--CHR.sub.1 --NH--, (xii) --NR.sub.3 --(CO).sub.m --NR.sub.4 --, (xiii) --NR.sub.5 --(CO).sub.m --NR.sub.6 --, (xiv) --NR.sub.4 --CO--O-- or (xv) --NR.sub.6 --CO--O--,m is 1 or 2,R.sub.1 is hydrogen, C.sub.1-4 alkyl or phenyl, preferably hydrogen, methyl or ethyl,R.sub.2 is hydrogen, C.sub.1-4 alkyl or phenyl, preferably hydrogen, methyl or ethyl,R.sub.3, R.sub.4, R.sub.

Abstract: A bicyclolactam compound of the formula (1) is disclosed, which has an excellent anxiolytic effect, is high in safety, and is useful as an effective component of medicinals which are greatly diminished in side effects such as hypnotic, muscle relaxant and sedative effects ##STR1## A bicyclolactam derivative represented by the following formula (1) is also disclosed, and is useful as an effective component of an anxiolytic agent ##STR2##

Abstract: The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein Alk is C.sub.1-6 alkanediyl or C.sub.3-6 alkenediyl; R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 and R.sup.3 each independently are hydrogen, C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; or R.sup.2 and R.sup.3 may also be taken together with the nitrogen atom to which they are attached, thus forming a pyrrolidine, a piperidine or a perhydro azepine ring; R.sup.