Abstract: The present invention relates to acrylol substituted distamycin derivatives, to pharmaceutical compositions comprising such derivatives as well as their use in methods of treating humans and animals, particularly as anti-tumor agents.

Abstract: Compounds which are benzoheterocyclic distamycin derivatives of formula (I), wherein n is 2, 3 or 4; A is a heteroatom selected from O and S or is a group NR, wherein R is hydrogen or C1-C4 alkyl; B is CH or N; R1 is hydrogen or C1-C4 alkyl; G is selected from the group consisting of (a, b, c, d, e, f, g, h, i, j), and —C≡N; wherein R5, R6, R7, R8, R9, R10, R11 and R12 are, independently from each other, hydrogen or C1-C4 alkyl; T is a group of formula (II) or (III) as defined above, wherein p is 0 or 1; R2 and R3 are, independently from each other, hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; R4 is C1-C4 alkyl or C1-C3 haloalkyl; X1 and X2 are halogen atoms or pharmaceutically acceptable salts thereof; provided that at least one of R5, R6 and R7 is alkyl; are useful as antitumor agents.

Abstract: A compound which is a distamycin derivative of formula (I), wherein n is 2, 3 or 4; R0is C1-C4 alkyl or C1-C3 haloalkyl; R1 and R2, which may be the same or different, are each hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; X is a halogen atom; B is selected from (A, B, C, D, E, F, G, H, I, J and K); wherein R3, R4, R5, R6, R7, R8, and R9, which may be the same or different, are each hydrogen or C1-C4 alkyl, and m is 0, 1, or 2; or a pharmaceutically acceptable salt thereof. Such compounds are useful as antineoplastic and antiviral agents.

Abstract: A distamycin derivative of formula (I): ##STR1## wherein: n is 2, 3 or 4;R.sub.0 is C.sub.1 -C.sub.4 alkyl or --CH.sub.2 CH.sub.2 --X.sub.2, wherein X.sub.2 is a halogen atom;R.sub.1 and R.sub.2 are selected, each independently, from: hydrogen, C.sub.1 -C.sub.4 alkyl optionally substituted by one or more fluorine atoms, C.sub.1 -C.sub.4 alkoxy, and halogen;X.sub.1 is a halogen atom;B is selected from: ##STR2## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, and R.sub.9 are, each independently, hydrogen or C.sub.1 -C.sub.4 alkyl, and m is 0, 1 or 2; with the proviso that, when R.sub.0 is --CH.sub.2 CH.sub.2 --X.sub.2, B is different from --(CH.sub.2).sub.m --NR.sub.6 R.sub.7 and at least one of R.sub.3, R.sub.4, and R.sub.5 is C.sub.1 -C.sub.4 alkyl;or a pharmaceutically acceptable salt thereof.

Abstract: Benzoheterocyclic distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; A is O, S, or NR, wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl; B is CH or N; R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; T is selected from; (i) formula (II) wherein: p is zero or 1; R.sub.2 and R.sub.3 are selected, each independently, from: hydrogen, C.sub.1 -C.sub.4 alkyl optionally substituted by one or more fluorine atoms, and C.sub.1 -C.sub.4 alkoxy; R.sub.4 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.3 haloalkyl; X.sub.1 is a halogen atom; and (ii) formula (III) wherein X.sub.2 is a halogen atom; and pharmaceutically acceptable salts thereof, are described. Such compounds are useful as antineoplastic and antiviral agents.

Abstract: Imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines of formula (I) ##STR1## wherein Het is ##STR2## A represents a direct linkage, --CH.sub.2 --, CH.sub.2 --CH.sub.2 -- or, when Het is ##STR3## A may also represent --CH.dbd.CH--; R is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy; each of R.sub.3 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group; one of R.sub.1 and R.sub.2 is a group --OR' wherein R' is a C.sub.1 -C.sub.6 alkyl either unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy or cyano, and the other is, independently,a) a group --OR";b) a group ##STR4## or c) a group --OR.sup.IV wherein R.sup.IV is hydrogen or a substituent selected from:(i) --(CH.sub.2).sub.m --CH.dbd.CH--Ph, ##STR5## are useful as Thromboxane A.sub.2 (TxA.sub.2) Synthase inhibitors and as calcium antagonists.

Abstract: Compounds which are useful in anti-tumors therapy having the formula (I) ##STR1## wherein Het imidazole, A represents a direct linkage at the phenyl 4-position: R is hydrogen; one of R.sub.3 and R.sub.4 is C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy, and the other, independently, is:a) C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy; orb) --(CH.sub.2).sub.m --O--(CH.sub.2).sub.n --NR.sub.a R.sub.b wherein each of m and n, which may be the same or different is an integer of 1 to 3, each of R.sub.a and R.sub.b, which may be the same or different, is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by a morpholino;each of R.sub.1 and R.sub.2 is independently a group --OR' wherein R' is C.sub.1 -C.sub.6 alkyl; or a pharmaceutically acceptable salt thereof.

Abstract: Compounds having formula (I) ##STR1## wherein Z is --O-- or --CH.sub.2 --; n is 1-6; R is hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or optionally substituted phenyl-C.sub.1 -C.sub.3 alkyl; R.sub.2 is C.sub.1 -C.sub.8 -alkyl, aryl-C.sub.1 -C.sub.3 alkyl, C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.3 alkyl; each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.4 alkyl, or taken together with the carbon atom to which they are linked form a C.sub.3 -C.sub.6 cycloalkyl ring; Q is --OR' or --NR'R" in which R' and R" are as herein defined, or Q is C.sub.1 -C.sub.8 alkyl, phenyl, phenyl-C.sub.1 -C.sub.3 -alkyl, C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.3 alkyl, in which both the phenyl and cycloalkyl rings or moieties are optionally substituted as herein defined; and the pharmaceutically acceptable salts thereof; are useful in particular as antidislipidaemic and antiatherosclerotic agents.

Abstract: The present invention relates to 2-(imidazol-1-yl)-2 -benzylethylidene-aminoxyalkanoic acid derivatives of formula (I) ##STR1## wherein A is a divalent group of formula ##STR2## in which R is hydrogen, halogen, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylsulfonyl or cyano;R.sub.1 is a) phenyl unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy, CF.sub.3 or C.sub.1 -C.sub.4 alkylsulfonyl; b) cyclohexyl; or c) a straight or branched C.sub.1 -C.sub.6 alkyl group;T is a branched or straight C.sub.3 -C.sub.5 alkylene chain;R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl, and the pharmaceutically acceptable salts thereof, which are useful as selective inhibitors of thromboxane A.sub.2 (TxA.sub.2) synthesis.

Abstract: 1-(Alkoxy-iminoalkyl)imidazole derivatives of formula ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl; A is C.sub.1 -C.sub.4 alkylene optionally substituted by phenyl optionally substituted by halogen or trifluoromethyl; R is (a) hydrogen or a C.sub.1 -C.sub.10 hydrocarbon radical; (b) an aryl or aryl-C.sub.1 -C.sub.4 alkyl group wherein the said aryl is optionally substituted either by halogen, trihalo-methyl, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or C.sub.1 -C.sub.4 alkylsulfonyl or by C.sub.5 -C.sub.8 alkyl, C.sub.4 -C.sub.8 alkenyl, C.sub.5 -C.sub.8 alkoxy, C.sub.5 -C.sub.8 alkylthio or phenyl optionally substituted by halogen, trihalomethyl or C.sub.1 -C.sub.4 alkyl; or (c) a C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl group, wherein the said cycloalkyl is optionally substituted by C.sub.1 -C.sub.4 alkyl; T is a C.sub.1 -C.sub.

Abstract: The invention provides new ureas and thioureas derivatives of general formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are useful as therapeutic agents such as for the prevention of coronary heart disease and as antidyslipidaemic agents.

Abstract: The invention provides new imidazole containing alkoxyimino derivatives of tetrahydronaphthalene and chroman of general formula (I) ##STR1## wherein Z is --CH.sub.2 --or--O--;m is an integer of 1 to 4;n is zero of 1;T is a straight or branched saturated C.sub.1 -C.sub.6 hydrocarbon chain or C.sub.2 -C.sub.5 alkenylene chain;A is a bond or a divalent group consisting of --Si(R'R")--; --O--CH.sub.2 --,--CF.sub.2 --,C(R'R")--,vinylene or isopropenylene, wherein each of R' and R" being the same or different is hydrogen or C.sub.1 -C.sub.4 alkyl;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, being the same, are hydrogen or methyl, or one of R.sub.1 and R.sub.2 is hydrogen and the other isa) a C.sub.1 -C.sub.8 alkyl group;b) a C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl-C.sub.1 C.sub.4 alkyl group, wherein the cycloalkyl group or moiety is unsubstituted or substituted by 1 to 4 C.sub.1 -C.sub.4 alkyl groups; orc) an aryl or aryl-C.sub.1 -C.sub.

Abstract: The invention provides N-imidazolyl derivatives of substituted indole of general formula (I) ##STR1## wherein p is an integer of 1 to 4;A is a straight or branched C.sub.1 -C.sub.4 alkylene chain;B is a direct linkage, a straight or branched, unsaturated or saturated C.sub.1 -C.sub.4 hydrocarbon chain;Q is a straight or branched, saturated or unsaturated C.sub.1 -C.sub.9 hydrocarbon chain, or said chain is interrupted by an oxygen atom;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, halogen or trihalomethyl;each of R.sub.3 and R.sub.5, independently, is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.4 is a --OR.sub.6 or --N(R.sub.6 R.sub.7) group, wherein each of R.sub.6 and R.sub.7 independently is hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of a disease state in which an enhancement of TxA.sub.

Abstract: The invention provides new N-imidazolyl derivatives of substituted tetrahydrocarbazoles and cyclopent[b]indoles of general formula (I) ##STR1## wherein n is 1 or 2;p is an integer of 1 to 4;A is a straight or branched C.sub.1 -C.sub.4 alkylene chain;B is a direct linkage, a straight or branched, unsaturated or saturated C.sub.1 -C.sub.4 alkylene chain;Q is a direct linkage or a straight or branched C.sub.1 -C.sub.4 alkylene chain;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, halogen or trihalomethyl;each of R.sub.3 and R.sub.5, independently is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.4 is --OR.sub.6 or --N(R.sub.6,R.sub.7) group, wherein each of R.sub.6 and R.sub.7 independently is hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of a disease state in which an enhancement of TxA.sub.

Abstract: The present invention relates to new N-imidazolyl and N-imidazolylmethyl derivatives of bicyclic compounds having the general formula (I) ##STR1## Wherein A is a .gtoreq.CR.sub.3 or >CHR.sub.3 group, in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, or a >C.dbd.CR.sub.4 R.sub.5 group, in which each of R.sub.4 and R.sub.5 independently is hydrogen or C.sub.1 -C.sub.5 alkyl;Z is --CH.sub.2 --, --O-- or --S--;n is zero or 1;each of R and R.sub.1 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is --COCH.sub.2 OH, --CH.sub.2 OR', --COOR', --CONR'R" or --CH.dbd.CH--COOR', in which each of R' and R" independently is hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof; and wherein:a) when n is zero, then Z is --CH.sub.2 -- or --O--; whereas when n is one, then Z is --CH.sub.2 --, --O-- or --S--;b) when A is .gtoreq.CR.sub.3 or >CHR.sub.3 in which R.sub.3 is hydrogen, then n is one; andc) when, at the same time, A is >CHR.sub.3 in which R.sub.

Abstract: Compounds having the following formula (I) ##STR1## wherein the symbol represents a single or double bond;Z is --O-- or --CH.sub.2 --;n is zero, 1, 2 or 3;each of R and R.sub.1, independently, is hydrogen or C.sub.1 -C.sub.4 alkyl;each of R.sub.2 and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.8 alkyl; and the pharmaceutically acceptable salts thereof;are useful in therapy in particular as antidislipidaemic and antiatherosclerotic agents.

Abstract: A pharmaceutical compositon having activity against nephropathies comprising, as an active agent, a therapeutically effective amount of a compound of formula (I) ##STR1## wherein (a) ##STR2## wherein Y completes a single bond or is oxygen or a --CH.sub.2 -- group and the symbol ##STR3## represents a single bond or (b) ##STR4## ##STR5## and the symbol ##STR6## represents a double bond; one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is --CH.sub.2 OH, C.sub.2 -C.sub.4 acyl, ##STR7## in which each of R.sub.1, R.sub.8 and R.sub.9 is independently hydrogen or C.sub.1 -C.sub.4 alkyl and the others are independently chosen from hydrogen, hydroxy, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and --COOR, wherein R.sub.7 is as defined above, and one of R.sub.5 and R.sub.6 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier and/or diluent.

Abstract: Alkoxy methyl pyrazine N-oxides having anti lypolytic, hypotriglyceridemic and hypocholesterolaemic properties and utility are disclosed.

Abstract: The compounds of the invention have the following general formula (I) ##STR1## wherein each of the groups R, R.sub.1 and R.sub.2, which may be the same or different, represents a hydrogen atom, a C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl group, and R.sub.3 represents a straight or branched chain, saturated or unsaturated, C.sub.1 -C.sub.8 aliphatic hydrocarbon group. The compounds are useful as antilipolytic agents.

Abstract: Compounds of the formula (I) ##STR1## wherein the symbol represents a single or a double bond;each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different is(a) hydrogen; hydroxy; halogen; cyano; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 alkoxy; a C.sub.2 -C.sub.4 acyl or C.sub.2 -C.sub.4 acylamino group; --SR', --N(R') (R"), --CH.sub.2 OR', --COR or --CH.sub.2 COR, wherein R is OR' or --N(R') (R") and each of R' and R", being the same or different, is hydrogen or C.sub.1 -C.sub.6 alkyl; or(b) one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is 5-tetrazolyl or a group selected from --COCH.sub.2 OR', --CH.dbd.C(R')--COR and --X--C(R')(R")--COR, wherein R, R' and R" are as defined above, and X is --O--, --S--, or --NH--, and the others are as defined above under (a);R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, or a phenyl or 3-pyridyl ring, wherein the phenyl or pyridyl ring is unsubstituted or substituted by one to three substituents chosen from hydroxy and C.sub.