Abstract: The present invention is related to 8-hydroxy-quinoline derivatives having multidrug-resistance reversing activity with improved selectivity and increased cytotoxicity towards multidrug-resistant cancer cells, preparation thereof and use of the same in the treatment of cancer, especially multidrug-resistant variants thereof.

Abstract: The present invention is related to 8-hydroxy-quinoline derivatives having multidrug-resistance reversing activity with improved selectivity and increased cytotoxicity towards multidrug-resistant cancer cells, preparation thereof and use of the same in the treatment of cancer, especially multidrug-resistant variants thereof.

Abstract: Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.

Abstract: Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.

Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxylamine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.

Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxylamine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.

Abstract: Compounds inhibiting phosphatidylinositol 3-kinase (PI 3-K) activities and methods of preparing and using thereof in treating diseases are disclosed. Compounds inhibiting PI 3-K activity and methods of using PI 3-K inhibitory compounds to inhibit cancer cell grwoth or to treat disorders of immunity and inflammation, in which PI 3-K plays a role in leukocyte function are also provided.

Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxylamine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.

Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxylamine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.

Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II).

Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively; an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxyl amine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.

Abstract: The invention relates to a method of treating or preventing illnesses resulting from damaged endothelial cells, wherein the method comprises administering to a patient a product comprising hydroxylamine derivatives of the general formulae (I) ##STR1## with the proviso that in the compounds of general formula (I) when X comprises a --NR.sup.3 R.sup.

Abstract: The invention relates to novel interfuranylene-prostacyclin derivatives of the general formula (I) ##STR1## wherein R.sup.1 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group, an inorganic cation or for the protonated form of a base containing an amino group;R.sup.2 stands for hydrogen, a C.sub.1-4 alkanoyl or benzoyl group, a monosubstituted benzoyl, trialkylsilyl or an alkoxyalkyl group;R.sup.3 stands for a straight or branched chain C.sub.1-6 alkyl group, a phenyl group optionally substituted by halogen or by a C.sub.1-4 alkyl group, a heteroaryl group optionally substituted by halogen or by a C.sub.1-4 alkyl group or a cycloalkyl group;A stands for an ethylene or for a cis- or trans-vinylene or --C.tbd.C-- group;B means a chemical bond, a --CHR.sup.5 --, --CHR.sup.5 --CH.sub.2 -- or a --CH.sub.2 --O-- group: andR.sup.5 means hydrogen or a C.sub.1-4 alkyl group.

Abstract: The invention relates to new 7-oxo-PGI.sub.2 -ephedrine salt analogues of the Formula I ##STR1## wherein A stands for --(CH.sub.2).sub.2 --, cis or trans --CH.dbd.CH-- or --C.tbd.C--;R.sup.1 is lower alkyl or hydrogen;B represents a chemical bond, --CH.sub.2 -- or --CR.sup.2 R.sup.3 ;R.sup.2 stands for lower alkyl or hydrogen;R.sup.3 represents lower alkyl or hydrogen;X is a chemical bond, --O-- or --CH.sub.2 --;R.sup.4 stands for C.sub.1-6 alkyl, C.sub.4-7 cycloalkyl, C.sub.1-6 fluoroalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, phenyl, substituted phenyl or heteroaryl.The salts of the Formula I show the same pharmacological profile as the sodium salt of PGI.sub.2, they inhibit blood aggregation and the secretion of gastric acid, are useful in the prevention of anginal attacks.

Abstract: Compounds of the formula ##STR1## are disclosed wherein R.sup.1 stands for hydrogen, C.sub.1-4 straight or branched alkyl or pharmacologically acceptable cation,R.sup.2 stands for hydrogen, C.sub.1-4 alkanoyl, benzoyl, or benzoyl substituted by C.sub.1-4 alkyl or halogen, and R.sup.2 can further represent tetrahydropyranyl, trialkylsilyl or alkoxyalkyl,A stands for ethylene, cis or trans-vinylene or --C.dbd.C--,n may represent 2, 3 or 4. The compounds are highly effective in the inhibition of thrombocyte aggregation while at the same time exert only a very small hypotensive effect.