Abstract: 13-substituted 5,6-dihydrodibenzo[a,g]quinolizinium salt compounds of the general formula (I): processes for the preparation of said compounds, pharmaceutical compositions containing said compounds and the use of said compounds for the manufacture of medicaments suitable for the treatment of cancerous diseases.

Abstract: The present invention relates to 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the preparation thereof, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.

Abstract: The present invention relates to a method for preparing 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the use of this method, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.

Abstract: 13-substituted 5,6-dihydrodibenzo[a,g]quinolizinium salt compounds of the general formula (I): processes for the preparation of said compounds, pharmaceutical compositions containing said compounds and the use of said compounds for the manufacture of medicaments suitable for the treatment of cancerous diseases.

Abstract: The present invention relates to a method for preparing 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the use of this method, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.

Abstract: A tetralylmethylene-2-oxindole derivative having the following formula (I) ##STR1## wherein one or two of R, R.sub.1, R.sub.2 and R.sub.3 the said two being the same or different, are selected from:a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.4 R.sub.5 or --X--(CH.sub.2).sub.m --NHR.sub.6, in which X is --O--, --S-- or --NH--, m is an integer of 2 to 4, one of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.4 and R.sub.5 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle, and R.sub.6 is C.sub.2 -C.sub.6 alkanoyl or a C-terminally linked peptidyl residue containing from 1 to 3 aminoacids wherein the terminal amino group is either free or protected or in an alkylated form to provide a --NR.sub.4 R.sub.5 group in which R.sub.4 and R.sub.5 are as defined above.

Abstract: Novel and known bicyclic 4-aralkylaminopyrimidine derivatives of formula (I) wherein A is a benzene or imidazole ring; B is a benzene, tetralin, indane or 2-oxindole ring R is (C.sub.1 -C.sub.4)perfluoroalkyl, phenyl, phenyl-(C.sub.1 -C.sub.4)alkyl, hydroxy-(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy-(C.sub.1 -C.sub.4)alkyl, (C.sub.2 -C.sub.4)acyloxy-(C.sub.1 -C.sub.4)alkyl, halobenzoyloxy-(C.sub.1 -C.sub.4)alkyl, carboxy, carbamoyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, cyano, (C.sub.1 -C.sub.4)alkylcarbonyl, carboxy-(C.sub.1 -C.sub.4)alkyl, carbamoyl-(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxycarbonyl-(C.sub.1 -C.sub.4)alkyl, halo-(C.sub.1 -C.sub.4)alkyl, amino-(C.sub.1 -C.sub.4)alkyl, mono- or di-(C.sub.1 -C.sub.4)alkylamino-(C.sub.1 -C.sub.4)alkyl, sulfo-(C.sub.1 -C.sub.4)alkyl or sulfamido-(C.sub.1 -C.sub.4)alkyl; each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen or --NR.sub.5 R.sub.6 in which each of R.sub.

Abstract: Novel bicyclic condensed pyrimidine compounds having general formula (I) ##STR1## wherein X is --CH.sub.2 --, --NH--(CH.sub.2).sub.n --, --O--(CH.sub.2).sub.n -- or --S--(CH.sub.2).sub.n -- in which n is zero or 1; A is a 4,5-fused imidazole ring N-substituted by R.sub.3 which is hydrogen, C.sub.1 -C.sub.4 alkyl or benzyl, or A is a 2,3-fused pyridine ring C-substituted by R.sub.4 which is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen or NR.sub.5 R.sub.6 in which each of R.sub.5 and R.sub.6 independently is H or C.sub.1 -C.sub.4 alkyl; B is a bicyclic ring chosen from tetralin, indane and 2-oxindole; each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.1 -C.sub.4 alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkoxycarbonyl, nitro, cyano or CF.sub.3 ; and the pharmaceutically acceptable salts thereof.

Abstract: Quinolylmethylen-oxindole derivatives having general formula (I), wherein R is H or --(CH.sub.2).sub.n --COR.sub.7 group in which n is an integer of 1 to 4 and R.sub.7 is hydroxy, amino, C.sub.1 -C.sub.6 alkoxy or --NR.sub.5 R.sub.6 in which one of R.sub.5 and R.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.5 and R.sub.6 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle or R.sub.7 is a N-terminally linked peptidyl residue containing from 1 to 3 aminoacids in which the terminal carboxyl group may be present as such, as amide, as alkali metal salt or as a C.sub.1 -C.sub.4 alkyl ester, one or two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are selected from: a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.5 R.sub.6 or --X--(CH.sub.2).sub.m --NHR.sub.8 group; b) --NH--C(.dbd.NH)--NR.sub.5 R.sub.6, --NH--C(.dbd.NH)--NHR.sub.8, --N.dbd.CH--NH.sub.2, --N.dbd.

Abstract: Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; one of R.sup.2 and R.sup.3 independently is hydrogen and the other is a substituent selected from: a C.sub.1 -C.sub.6 alkyl group substituted by 1, 2 or 3 hydroxy groups; --SO.sub.3 R.sup.4 in which R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; --SO.sub.2 NHR.sup.5 in which R.sup.5 is as R.sup.4 defined above or a --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.6 alkyl).sub.2 group in which n is 2 or 3; --COOR.sup.6 in which R.sup.6 is C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; --CONHR.sup.7 in which R.sup.7 is hydrogen, phenyl or C.sub.1 -C.sub.

Abstract: The present invention relates to compound of formula (I) ##STR1## wherein A is benzene, naphthalene, 5,6,7,8,-tetrahydronaphthalene, quinoline, isoquinoline, indole or 7-azaindole;R.sub.1 is --H, --CN, --SO.sub.3 R.sub.4 --, --SO.sub.2 NHR.sub.5, ##STR2## --COOR.sub.6, --CONHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, ##STR3## --NR.sub.7 R.sub.8, --N(CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --NHCONH.sub.2, --NH--C(NH.sub.2).dbd.NH, --NHCO(CHOH).sub.n CH.sub.2 OH, ##STR4## --NHSO.sub.2 R.sub.9, --OR.sub.10, --OCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --OOC(CHOH).sub.n CH.sub.2 OH, --OPO(OH).sub.2, --CH.sub.2 NH.sub.2, --C(NH.sub.2).dbd.NH, --CH.sub.2 NHC(NH.sub.2).dbd.NH, ##STR5## --CH.sub.2 OH, --CH.sub.2 OOC(CHOH).sub.n CH.sub.2 OH, --CH.sub.2 OPO(OH).sub.2 or --PO(OH).sub.2 ;R.sub.2 is C.sub.1 -C.sub.6 alkyl, halogen, or hydroxy;R.sub.3 is --H or C.sub.1 -C.sub.6 alkyl;R.sub.4 is --H, C.sub.1 -C.sub.6 alkyl or --CH.sub.2 (CHOH).sub.n CH.sub.2 OH;R.sub.5 is --H, C.sub.1 -C.sub.6 alkyl, --CH.sub.

Abstract: The present invention relates to compounds useful as tyrosine kinase inhibitors, having the following general formula (I) ##STR1## wherein one of the groups X.sup.1, X.sup.2, X.sup.3, X.sup.4 is N and the others are CH; R is a group of formula (a), (b), (c) or (d) ##STR2## each of R.sup.1 and R.sup.3 independently is hydrogen, amino, carboxy, cyano, --SO.sub.3 R.sup.4, --SO.sub.2 NHR.sup.5, ##STR3## --COOR.sup.6, --CONH(CH.sub.2).sub.o Ph, --CONHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, ##STR4## --N (CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --NHCONH.sub.2, --NHC(NH.sub.2).dbd.NH, --NHCO(CHOH).sub.n CH.sub.2 OH, ##STR5## --NHSO.sub.2 R.sup.7, --OCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --OOC(CHOH).sub.n CH.sub.2 OH, --OPO(OH).sub.2, --OCH.sub.2 SO.sub.2 NH.sub.2, --CH.sub.2 NH.sub.2, --C(NH.sub.2).dbd.NH, --CH.sub.2 NHC(NH.sub.2).dbd.NH, ##STR6## --CH.sub.2 OH, --CH.sub.2 OOC(CHOH).sub.n C.sub.2 OH, --CH.sub.2 OPO(OH).sub.2, --PO(OH).sub.2 ;R.sup.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.

Abstract: Arylidene and heteroarylidene oxindole derivatives of formula (I) ##STR1## wherein, subject to provisos, Y is a bicyclic ring system chosen from naphthalene, tetralin, quinoline and isoquinoline;R is hydrogen or an oxo (.dbd.O) group when Y is tetralin; orR is hydrogen when Y is naphthalene, quinoline or isoquinoline;each of R.sup.1 and R.sup.2 independently is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;m is zero, 1 or 2;n is zero, 1, 2 or 3;each of R.sup.3 and R.sup.4 independently is hydrogen, halogen, cyano, C.sub.1 -C.sub.6 alkyl, carboxy, nitro or --NR.sup.6 R.sup.7 in which each of R.sup.6 and R.sup.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; and their pharmaceutically acceptable salts, which are useful as tyrosine kinase inhibitors.

Abstract: The present invention relates to new compounds of formula ##STR1## wherein A is a bicyclic ring chosen from naphthalene, tetrahydronaphthalene, quinoline, isoquinoline and indole.B is a R.sup.2 substituted benzene ring or an unsubstituted pyridine or thiophene ring;R is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy or a group NR.sup.3 R.sup.4 wherein each of R.sup.3 and R.sup.4 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy or a group NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are as defined above;n is zero or an integer of 1 to 2;x is zero or an integer of 1 to 5;and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful as tyrosine kinase inhibitors.

Abstract: The invention relates to compounds of formula ##STR1## wherein Ar is mono- or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole;Het is ##STR2## R is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is as defined above;R.sub.2 is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar)R.sub.1 R.sub.2 group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.

Abstract: The present invention provides compounds of the formula ##STR1## wherein Y is a naphthyl, tetrahydronaphthyl, pyridyl, quinolyl, isoquinolyl or indolyl ring system, R is a moiety which is an acrylic acid, a CN-substituted acrylic acid, acrylamide, acrylonitrile or thioacrylamide, or a group of formulae (e) to (j): ##STR2## wherein R.sub.3 is OH or NH.sub.2, R.sub.1 is H, alkyl or alkanoyl, R.sub.2 is H, halogen, CN or alkyl; and n is 0, 1, 2 or 3; and the pharmaceutically acceptable salts thereof are useful as tyrosine kinase inhibitors.

Abstract: The invention relates to compounds of formula ##STR1## wherein Ar is mono- or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole;Het is ##STR2## R is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is as defined above;R.sub.2 is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar) R.sub.1 R.sub.2 group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.

Abstract: The new use of a compound of formula (I) ##STR1## wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole;n is zero or an integer of 1 to 3;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; or a pharmaceutically acceptable salt thereof;and wherein when Y is naphthalene then n is zero or an integer of 1 to 3, whereas when Y is tetralin, quinoline, isoquinoline or indole then n is zero, 1 or 2; and wherein when the bicyclic ring Y is naphthalene, quinoline, isoquinoline or indole, then each of the substituents OR.sub.1, R.sub.

Abstract: The present invention relates to a compound of formula (I) ##STR1## wherein (x) and (y) are single or double bonds; A is a ##STR2## R and R.sup.3 are hydrogen or acyl; R.sup.1 is hydrogen or fluorine;and wherein:when (y) is a single bond, R.sup.2 is hydrogen, fluorine methyl, trifluoromethyl;when (y) is a double bond, R.sup.2 is methylene provided that when one of (x) or (y) is a double bond the other is a single bond and at least one of R.sub.1 and R.sub.2 is fluorine or trifluoromethyl or a pharmaceutically acceptable salt thereof. The compounds of formula (I) are useful as aromatase inhibitors.

Abstract: The present invention provides novel aryl- and heteroarylethenylene derivatives which are useful as tyrosine kinase activity inhibitors.