Abstract: The present invention relates to novel metalloproteinase inhibitors having an aryloxybenzenesulfonamide moiety and a carbamoylphosphonic acid moiety, to pharmaceutical compositions comprising them, and to their uses in the prevention and/or treatment of disease or disorder associated with MMP.

Abstract: The present invention relates to novel metalloproteinase inhibitors having an aryloxybenzenesulfonamide moiety and a carbamoylphosphonic acid moiety, to pharmaceutical compositions comprising them, and to their uses in the prevention and/or treatment of disease or disorder associated with MMP.

Abstract: The present invention relates to compositions useful for treating or controlling disease states or conditions associated with zinc containing proteinases, especially metalloproteinases. The active ingredient in these compositions is an alpha-oxo- or alpha-thioxophosphonate of formula (I). Out of the phosphonates of formula (I), some are known and others are new. The novel compounds constitute another aspect of the invention.

Abstract: The present invention provides a compound of the following formula I: R3—NH—C(?X)—P(?O)OR1OR2 including pharmaceutically acceptable salts, solvates, hydrates and polymorphs of the compounds of formula I, as well as geometrical isomers and optically active forms of the compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates and polymorphs of said isomers and forms, wherein R1 and R2 may be the same or different and are each selected from hydrogen, acyloxyalkyl and aryl or R1 and R2 may form together with the oxygen and phosphorus atoms a dioxaphosphacycloalkane ring; X is O or S; and R3 is selected, when X is O, from bicycloalkyl, cycloalkylalkyl and substituted cycloalkyl by at least one of alkyl, amino, amidino and guanidino; and R3 is selected, when X is S, from bicycloalkyl, cycloalkylalkyl and cycloalkyl optionally substituted by at least one of alkyl, amino, amidino and guanidino; with the proviso that: when X is O, R3 is not cyclohexylmethyl, and when X is S, R3 is not cycl

Abstract: The present invention relates to compositions useful for treating or controlling disease states or conditions associated with zinc containing proteinases, especially metalloproteinases. The active ingredient in these compositions is an alpha-oxo- or alpha-thioxophosphonate of formula (I). Out of the phosphonates of formula (I), some are known and others are new. The novel compounds constitute another aspect of the invention.

Abstract: The present invention relates to compositions useful for treating or controlling disease states or conditions associated with zinc containing proteinases, especially metalloproteinases. The active ingredient in these compositions is an alpha-oxo- or alpha-thixophosphpnate of formula (I). Out of the phosphonates of formula (I), some are known and others are new. The novel compounds constitute another aspect of the invention.

Abstract: The present invention provides a compound of the following formula I: R3—NH—C(?X)—P(?O)OR1OR2 including pharmaceutically acceptable salts, solvates, hydrates and polymorphs of the compounds of formula I, as well as geometrical isomers and optically active forms of the compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates and polymorphs of said isomers and forms, wherein R1 and R2 may be the same or different and are each selected from hydrogen, acyloxyalkyl and aryl or R1 and R2 may form together with the oxygen and phosphorus atoms a dioxaphosphacycloalkane ring; X is O or S; and R3 is selected, when X is O, from bicycloalkyl, cycloalkylalkyl and substituted cycloalkyl by at least one of alkyl, amino, amidino and guanidino; and R3 is selected, when X is S, from bicycloalkyl, cycloalkylalkyl and cycloalkyl optionally substituted by at least one of alkyl, amino, amidino and guanidino; with the proviso that: when X is O, R3 is not cyclohexylmethyl, and when X is S, R3 is not c

Abstract: The invention provides novel methods for treating disease based upon the medicinal use of lipids and phospholipids covalently bound to physiologically acceptable monomers or polymers. Phosphatidylethanolamine moieties conjugated to physiologically acceptable monomers and polymers (PE conjugates) manifest an unexpectedly wide range of pharmacological effects, including stabilizing cell membranes; limiting oxidative damage to cell and blood components; limiting cell proliferation, cell extravasation and (tumor) cell migratory behavior; suppressing immune responses; and attenuating physiological reactions to stress, as expressed in elevated chemokine levels.

Abstract: The invention provides novel methods for treating disease based upon the medicinal use of lipids and phospholipids covalently bound to physiologically acceptable monomers or polymers. Phosphatidylethanolamine moieties conjugated to physiologically acceptable monomers and polymers (PE conjugates) manifest an unexpectedly wide range of pharmacological effects, including stabilizing cell membranes; limiting oxidative damage to cell and blood components; limiting cell proliferation, cell extravasation and (tumor) cell migratory behavior; suppressing immune responses; and attenuating physiological reactions to stress, as expressed in elevated chemokine levels.

Abstract: The present invention relates to a method of inhibiting tumor metastasis in an aminal by administering to an animal in need of such treatment an acrylaminoalkylpryridineamides represented by the formula ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided n+m+p is equal to or less than 10; x is thio or sulfinyl; Alk.sub.1 is straight or branched chain lower alkylene of 1 to 6 carbon atoms, R.sub.3 is hydrogen or lower alkyl, Alk.sub.2 is straight or branched chain alkylene of 1 to 4 carbon atoms; R.sub.4 is selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl and lower alkoxy; or a pharmaceutically acceptable salt thereof, in an amount effective to inhibit tumor metastasis.

Abstract: A method of inhibiting tumor metastasis in an animal without treating the tumor cells by administering to said animal a metastasis inhibiting effective amount of a heterocyclic amide represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein q, r and t are independently an integer of from 1 to 8 provided that q+r+t is equal to or less than 10; Y is thio or sulfinyl; alk is straight or branched chain lower alkylene, and R.sub.3 is a heterocyclic amine represented by the formula: ##STR3## wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, phenyl, substituted phenyl, benzyl, or substituted benzyl; p is 0 to 2; or a pharmaceutically acceptable salt thereof.