190 results about "Thioamide" patented technology

Prodrugs having a hydrolyzable carbamate moiety, compositions including the prodrugs, methods of preparing the prodrugs and methods of treatment using the prodrugs are disclosed. The prodrug has the formula DC(X)XR, where D is a biologically active agent, X is O, S or NR', and R is a moiety that modifies various properties of the biologically active agent. The biologically active agent either includes a functional group such as an amide, thioamide, imide, thioimide, urea, thiourea, carbamate, thiocarbamate, sulfonamide, or sulfonimide group, or includes a hydroxy, amine, carboxylic acid or thiol group that is modified to include such a group. An NH group from the biologically active agent can be coupled to an activated form the C(X)XR moiety to form the prodrugs described herein. Relative to a conventional carbamate group, the presence of the additional carbonyl or sulfonyl group makes the carbamate group more susceptible to hydrolysis. The prodrugs are more stable in certain environments than the biologically active agent, and can permit the drugs to be administered orally, in those embodiments where the biologically active agent must otherwise be administered by injection or intraveneous administration.

Hydrophilic transportable N-linked glycosyl dopaminergic prodrug compounds according to FORMULA V and methods of their use,wherein,Ring 1 comprises an aryl or heteroaryl ring having 4 to 8 carbon atoms, among which atoms are counted “X” and “Y”;each of X and Y is optional; X, when present is either —C(R1)2— or —C(R1)2—; Y, when present, is either —CH2— or —CH2—CH2—;z, R5 and R5′ are optional, and when present z, R5 and R5′ together form a lower alkyl or a substituted lower alkyl moiety;N is part of either an amine or an amide linkage;E is a saccharide which forms a linkage with N through a single bond from a carbon or oxygen atom thereof;R1 and R4 are selected form the group consisting of hydrogen, hydroxyl, halogen, halo-lower alkyl, alkoxyl, alkoxyl-lower alkyl, halo-alkoxy, thioamido, amidosulfonyl, alkoxylcarbonyl, carboxamide, aminocarbonyl, and alkylamino-carbonyl;R2 and R3 are hydroxyl;R5 and R6, when present, are selected from the group consisting of hydrogen, hydroxyl, alkoxyl, carbonyl, alkoxylcarbonyl, aminocarbonyl, alkylamino-carbonyl and dialkylamino-carbonyl; and,R6 and R6′ are selected from the group consisting of hydrogen, hydroxyl, alkoxyl, carboxyl, alkoxylcarbonyl, aminocarbonyl, alkylamino-carbonyl and dialylamino-carbonyl,with the proviso that Ring 1 is capable of binding to any of:a dopaminergic receptor selected from the group consisting of a D1 receptor and a D5 receptor; a DAT transporter; a VMAT transporter; and,with the proviso that E is capable of binding to a GLUT transporter selected from the group consisting of a GLUT1 receptor and a GLUT3 receptor.

The present invention relates to compounds derived from biphenyl with activity as calpain inhibitors. One compound of the present invention is a 2,2′-disubstituted biphenyl, where the substituents in the 2 and 2′ positions of the biphenyl skeleton are chains containing structures related to amino acids, including fragments of aminocarbonylic compounds where at least one of the substituents in said 2- or 2′-positions is bonded to the biphenyl skeleton via a thiocarbonyl group, forming compounds with thioamide functionality. The present invention also encompasses any of the conformational isomers (atropisomers) of said compound of formula I. The compounds of formula I have application in the preventive or therapeutic treatment of a degenerative disease.