Abstract: Novel dioxazine- and oxdiazine-substituted arylamides of the formula (I) in which A1, A2, R1, R2, R3, R4 and R5 are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.

Abstract: Since an amide compound represented by the formula (1) is effectiveness for controlling plant diseases, it is useful as an effective ingredient of a composition for controlling plant diseases.

Abstract: Compounds of the formula: wherein Ar1, Ar2, R1 and R2 are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the subject compounds.

Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

Abstract: The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

Abstract: Since an amide compound represented by the formula (1) is effective for controlling plant diseases, it is useful as an effective ingredient of a composition for controlling plant diseases.

Abstract: Compounds of formula (I) wherein R1, R3, R4, R5, R6, R7, and R10 are as defined in the specification, are described. The present invention also relates to pharmaceutical composition comprising said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof. Beside, the invention relates to salts and polymorphic forms of the new compounds as well as the preparation thereof.

Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C?—C—(CH2)2CO2H, meta-C?—C—(CH2)2OH, meta-C?C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C?

Abstract: Disclosed are compounds of the formulae: and method of using the compounds to treat cancer, AIDS, HIV infection, and asthma.

Abstract: This invention relates to novel phenylbenzamides of the formula (I) in which R1 represents trifluoromethyl, chlorine, bromine or iodine and R2 represents hydrogen, methyl or ethyl, to a process for preparing these substances and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.

Abstract: This invention relates to novel phthalamide derivatives of formula (I) wherein R1, R2, R3, R4, and R5 have the meanings given in the disclosure, to processes for their preparation, and to their use as insecticidal agents in agricultural and horticultural field.

Abstract: Colchicine derivatives represented by the formula (I) with a halogen or nitric ester group, or pharmaceutically acceptable salts thereof, are described. Pharmaceutical compositions containing the same as effective components are also described. The colchicine derivatives were found to have anticancer, anti-proliferous and immunosuppressive function. Methods for preparing the colchicines derivatives are also provided.

Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.

Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.

Abstract: The present invention relates to compounds of formula (I) wherein U, Y, V, W, L, X, A1, A2, A3, A4, A5 and A6 are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: The present invention relates to a class of carbocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Abstract: Disclosed are compounds of formula I: 1

Abstract: This invention relates to new compositions comprising predominantly one enantiomer of an N-acetonylbenzamide fungicide, methods of preparing N-acetonylbenzamides, and their use as fungicides.

Abstract: Salicylamide derivatives represented by formulae (1a) and (1b); intermediates in the production thereof; a process for producing the same; and drugs containing the same as the active ingredient. The salicylamide derivatives represented by formulae (1a) and (1b) are useful as anti-inflammatory agents and immunosuppressive agents which exert an effect of inhibiting the activation of NF-&kgr;B with little side effects.

Abstract: Benzenesulfonylureas and -thioureas of the formula I where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto)alk(oxy)yl, E is O or S; Y is —[CR(3)2]n—, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO3 or alk(yl)oxy, are described. The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used an antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.

Abstract: The invention provides compounds of the formula 1 that are active against the HSV primase enzyme: wherein R1 is hydroxy or amino; R2 is hydrogen, halo, (C1-4)alkyl or (C1-4)alkoxy; R3 is hydrogen, halo, (C1-4)alkyl, (C1-4)alkoxy, amino or azido; R4 has the same significance as R2; R5 is hydrogen or (C1-4)alkyl; and R is (C1-7)alkyl, (C3-6)cycloalkyl, {phenyl(C1-7)alkyl}, {phenyl(C1-7)alkoxy}, {{(monocyclic heterocyclo)-{(C1-7)alkoxy}}, CH(W)C(O){O-(C1-4)alkyl} wherein W is hydrogen or (C1-7)alkyl, or  wherein Y is hydrogen or (C1-7)alkyl, and Z is (C1-7)alkyl, (C3-6) cycloalkyl, {(C3-6)cycloalkyl}- {(C1-7)alkyl}, phenyl(C1-7)alkyl or {{(monocyclic heterocyclo)-{(C1-7)alkyl}}, or Y and Z together with the nitrogen atom to which they are attached represent, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or 1-(4-methylpiperazinyl); with the provisos that (1) when R is CH(W

Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: A polymerizable liquid crystal compound is represented by the formula (I):

Abstract: Preparation of antiarrhythmic agents containing novel anilide derivatives represented by the following formula as active ingredient provides a new type of antiarrhythmic agent of highly safe and effective, without effects on cardiac function.

Abstract: Ortho-substituted benzoylguanidines of the formula I in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction and for the treatment of angina pectoris. They also inhibit, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the triggering of ischemically induced cardiac arrhythmias.

Abstract: The invention relates to a process for preparing N-(3-amino-4-fluoro-phenyl)-sulphonamides, N-(3-amino-4-fluoro-phenyl)-carboxamides or N-(3-amino-4-fluoro-phenyl)-carbamates of the general formula (I) in which A represents SO2, CO or CO2 and R represents in each case optionally substituted alkyl or aryl, wherein 1-fluoro-2,4-diamino-benzene of the formula (II) is reacted with sulphonyl chlorides, carbonyl chlorides or chlororformic esters of the general formula (III)  in which A and R are as defined above in the presence of an acid acceptor and in the presence of a diluent at temperatures between −20° C. and +100° C.

Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathsepsin D. The compounds are useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is a heterocycle, amide, sulfonamide or carbamate and Z is an acyl or a functionalized acyl. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid phase support, are also disclosed.

Abstract: Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them.Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction and for the treatment of angina pectoris. They also inhibit, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the triggering of ischemically induced cardiac arrhythmias.

Abstract: A 1,2-di-substituted benzene-carboxamide derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2)n-NR.sup.2 R.sup.3, wherein when A is R.sup.1, B is --(CH.sub.2)n-NR.sup.2 R.sup.3 and when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, B is R.sup.1 ; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.1 is a hydrocarbon group of C.sub.10-30 ; R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, or together represent a heterocyclic ring having 3-7 members; when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.2 may be a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, and R.sup.3 and R.sup.5 together may represent a heterocyclic ring of 6 or 7 members including two nitrogen atoms; when --Z--B is --OCONR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 or --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.

Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(ozy)yl, E is O or S; Y is --[CR(3).sub.2 ].sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z in Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.

Abstract: A phenylenediamine derivative or a salt thereof in accordance with the present invention is expressed by the following formula 1: ##STR1## wherein A represents a group expressed by --CO--, --CH.sub.2 CO--, --CS--, or --SO.sub.2 --; Y represents a carbon atom or nitrogen atom; R.sub.1 represents a lower alkyl group; R.sub.2 represents a hydrogen, lower alkyl, alkenyl, benzyl, or benzoyl group; and each of R.sub.3 and R.sub.4 represents an alkyl group having 1-10 carbon atoms. The phenylenediamine derivative above mentioned, as a radical scavenger, has antioxidant effect and lipid peroxidation inhibitory activity so as to be available for inhibiting brain infarction or brain edema.

Abstract: Benzoylguanidines of formula I ##STR1## with R(1) to R(4) as defined in the specification, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment as well as for the treatment of angina pectoris.They inhibit, in a preventive manner, the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias.

Abstract: Disclosed are A N-[(fluoroalkoxy)phenoxyalkyl]benzamide compound represented by the formula (1): ##STR1## wherein R.sup.1 and R.sup.3 may be the same or different and represent a hydrogen atom, a halogen atom, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group, a C.sub.1-4 haloalkyl group, a C.sub.1-4 haloalkoxy group, a cyano group, a nitro group, or a hydroxy group; R.sup.2 represents a hydrogen atom, a halogen atom, a C.sub.1-4 alkyl group, or a C.sub.1-4 alkoxy group; A represents an oxygen atom, or a sulfur atom; n is an integer of 1 to 6; x is 1 to 4; y is 0 to 6; z is 2 to 9; m is 0 to 2; provided that 2x+1=y+z+m, an intermediate thereof, processes thereof and an agricultural and horticultural chemical for controlling noxious organisms containing the above-mentioned compound as an effective ingredient which is available as a nematocide, an acaricide, a fungicide, etc.

Abstract: The invention provides iodinated bis phenyl compounds, useful as X-ray contrast agents, of formula (I) (wherein each C.sub.6 R.sub.5 moiety may be the same or different; each denotes a hydrogen or iodine atom or a group M, two or three non-adjacent R groups on each C.sub.6 R.sub.5 moiety denoting iodine atoms and one, two or three R groups on each C.sub.6 R.sub.5 moiety denoting M groups; X denotes a group providing a 1, 2 or 3 atom chain linking the two C.sub.6 R.sub.5 groups, preferably where X is or contains in the bridging chain a carbonyloxy group each C.sub.6 R.sub.5 group being a triodophenyl group or a group in which each R is other than hydrogen; and each M is independently a non-ionic hydrophilic moiety, M preferably being a non-ionic hydrophilic moiety comprising a monohydroxy- or polyhydroxy-alkyl group) and isomers, especially stereoisomers and rotamers, thereof.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.

Abstract: A new treatment schedule for administration of N-?2-(dimethylamino)ethyl!acridine-4-carboxamide and other related carboxamide anticancer drugs in which the drug is administered in a divided-dose schedule comprising two or more administrations at frequent intervals, for example every hour. Schedules to produce cyclic peaks/troughs in plasma levels are mentioned. The compounds can be used for circumventing multidrug resistance in cancers and may, for example, be used in combination with other cytotoxic drugs, especially non-topo II inhibitors. Treatment of melanoma and advanced colon cancer is included.

Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.

Abstract: X-ray opaque esters or amides of iodosubstituted benzoic acid according to formula I and polymers and dental materials produced therefrom. ##STR1## R.sup.1 =hydrogen or C.sub.1 to C.sub.3 alkyl, preferably H or CH.sub.3 ; R.sup.2 =straight-chain or branched C.sub.1 to C.sub.6 alkylene, oxyalkylene or arylene, preferably C.sub.2 to C.sub.4 alkylene and particularly preferably --CH.sub.2 --CH.sub.2 -- and --CH.sub.2 CH(--)CH.sub.2 --;X=O or NH, preferably O;R.sup.3 -R.sup.7 =at least 3 iodine substituents, preferably in R.sup.3, R.sup.4 and R.sup.6 or R.sup.3, R.sup.5 and R.sup.7 position, the other groups are hydrogen, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, --Cl, --Br, --OH, --NH.sub.2, --N(C.sub.1 to C.sub.6 alkyl).sub.2 or --NH--CO--(C.sub.1 to C.sub.6 alkyl), preferably R.sup.3, R.sup.4, and R.sup.6 are=I and R.sup.5 and R.sup.7 =H, or R.sup.3, R.sup.5 and R.sup.7 =I and R.sup.4 and R.sup.6 =--NH(COCH.sub.3);n=1, 2 or 3, preferably 1 or 2.

Abstract: Fluorine-containing benzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meanings indicated, and their physiologically acceptable salts, have antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter, for example.

Abstract: The present invention relates to substituted benzoylguanidines, a process for their preparation, their use as medicament or diagnostic agent, and medicament comprising them.

Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.

Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein thyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: ##STR1## wherein R.sup.1 represents farnesyl, geranyl or geranyl-geranyl;Z represents C--R.sup.6 or N;R.sup.2 represents H, CN, the groups COOR.sup.7, SO.sub.3 R.sup.7, CONR.sup.7 R.sup.8 and SO.sub.2 NR.sup.7 R.sup.7, wherein R.sup.7 and R.sup.8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO.sub.3 M, wherein M is a cation;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato;X represents O, S, SO, SO.sub.2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.

Abstract: Disclosed is a preparation for external application to the skin characterized by containing at least one of benzoic acid derivatives represented by formula (I) or pharmacologically acceptable salts thereof as an active ingredient, the preparation having sufficient sebaceous secretion inhibitory activity with no substantial side effect and high safety for human body. ##STR1## wherein R.sup.1 represents --OH, --OR.sup.3 or --NHR.sup.3 ; R.sup.2 represents a hydrogen atom, a lower alkyl group or a lower acyl group; R represents --O--R.sup.4 or ##STR2## R.sup.3 represents an alkyl group, an alkenyl group or a hydroxyalkyl group; R.sup.4 represents a straight-chain or branched, saturated or mono-unsaturated alkyl group or cycloalkylalkyl group having from 4 to 10 carbon atoms; X represents --O-- or --NH--; and n represents 1 or 2.

Abstract: Certain N-acetonylbenzamides exhibit low toxicity to plants are particularly useful for control of fungi, especially Phycomycetes.

Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.

Abstract: Monocarboxamides of formula I ##STR1## wherein R is a radical of formula ##STR2## C.sub.9 -C.sub.19 alkyl, C.sub.9 -C.sub.19 alkenyl or C.sub.9 -C.sub.19 alkdienyl,wherein each R.sup.2 independently of the other is a hydrogen atom or C.sub.1 -C.sub.4 alkyl, each R.sup.3 independently of one another is a hydrogen atom or a hydroxyl group and at least one R.sup.3 is a hydroxyl group, and R.sup.1 is a radical of formula ##STR3## are suitable for curing epoxy resins, in ##STR4## are suitable for curing epoxy resins, in particular for cold curing.

Abstract: The invention concerns a method for treating depression or senile dementia using a compound which acts selectively as an agonist of gamma aminobutyric acid (GABA) at GABA autoreceptors with the proviso that the compound is not fengabine and progabide.

Abstract: This invention relates to a retinoid mpound of formula I ##STR1## in which Y is --CO--NH--, --CR.sup.2 .dbd.CR.sup.3 --, --CO--O--, --O--CO--, --C(.dbd.S)--NH--, --C.tbd.C--, --O--CH.sub.2 --, --CH.sub.2 --O--, or --CH.sub.2 --CH.sub.2 --;A is --(CH.sub.2).sub.t -- or a bond;Q is phenyl optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen, or --CO.sub.2 R.sup.4 ;R.sup.1 is --CO.sub.2 Z, --CONHR.sup.5, C.sub.1-6 alkyl, --CH.sub.2 OH, or --CHO;R.sup.2, R.sup.3, R.sup.4, R.sup.5, and Z are independently hydrogen or C.sub.1-6 alkyl;t is one to six.

Abstract: A compound for controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein R.sup.2 is ethyl, iso-propyl, propyl or allyl; A is N(CH.sub.3).sub.1-n H.sub.n R.sup.5 or OR.sup.6 wherein n is 0 or 1, R.sup.5 is (CH.sub.3).sub.m (CH.sub.3 CH.sub.2).sub.3-m C, 1-methylcyclopentyl, 1-methylcyclohexyl or 2,3-dimethyl-2-butyl wherein m is 0, 1, 2 or 3 and R.sup.6 is independently R.sup.5 or 2,3,3-trimethyl-2-butyl;R.sup.3 is H or independently R.sup.4 ; andR.sup.4 is halo or CH.sub.3 ;with the proviso that when A is N(CH.sub.3).sub.1-n H.sub.n R.sup.5, if R.sup.3 is H and R.sup.5 is 1-methyl-1-cyclohexyl or (CH.sub.3).sub.m (CH.sub.2 CH.sub.3).sub.3-m C, where m is 0 or 3, or if R.sup.3 is halo and R.sup.5 is (CH.sub.3).sub.m (CH.sub.3 CH.sub.2).sub.3-m C, where m is 3, then R.sup.2 cannot be ethyl;and with the proviso that when A is OR.sup.6 then m is equal to or less than 2, and if R.sup.3 is H or halo and R.sup.

Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein methyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: wherein R1represents farnesyl, geranyl or geranyl-geranyl; Z represents C—R6 or N; R2 represents H, CN, the groups COOR7, SO3R7, CONR7R8 and SO2NR7R7, wherein R7 and R8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO3M, wherein M is a cation; R3, R4, R5 and R6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.