Abstract: The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.

Abstract: The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure (I), wherein R1 is C8-C22 alkyl, C8-C22 alkenyl or R12 is O, or R1 and R12 taken together form an optionally substituted aryl or an optionally substituted heteroaryl; R17 is H, alkyl or alkylaryl; R18 is N or CH; R2 and R3 are independently selected from the group consisting of H, NH2, and OH, with the proviso that at least one of R2 and R3 is NH2; R4 is selected from the group consisting of hydroxyl, phosphate, phosphonate methylene phosphonate, &agr;-substituted methylene phosphonate, thiophoasphate and thiophosphonate; and R5 is C8-C22alkenyl.

Abstract: The present invention relates to novel felbamate derivatives and their use to threat neurological diseases such as epilepsy and neuropathic pain, and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.

Abstract: Agonists of A2A adenosine receptors optionally, in combination with a Type IV phosphodiesterase (PDE) inhibitor are effective for the inhibition of an inflammatory response in mammalian tissue, in vivo or in vitro.

Abstract: The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.

Abstract: The invention provides compounds having the following general formula (I): 1

Abstract: The invention relates to the use of certain felbamate derivatives to treat neuropathic pain, obesity, glaucoma, depression, and mood disorders, as well as other conditions.

Abstract: The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.

Abstract: The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.

Abstract: The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.

Abstract: Agonists of A2A adenosine receptors optionally, in combination with a Type IV phosphodiesterase (PDE) inhibitor are effective for the inhibition of an inflammatory response in mammalian tissue, in vivo or in vitro.

Abstract: The application discloses methods of treating mammalian diseases characterized by undesirable angiogenesis by administering compounds including those having the general formulae wherein A is a fused tropone having a general formula: wherein X is selected from the group consisting of hydrogen, hydroxy, carboxy, halogen, nitro, C1 to C12 alkenyl, C1 to C12 alkyl, C1 to C12 alkoxy, SR, NR2, OSO3−, OSO2NR2, HNSO3−, NHSO2NR2, SSO3−, SSO2NR2, wherein R is hydrogen or a C1 to C6 alkyl and the 17-ester and keto derivatives thereof, in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the method of the invention.

Abstract: Azatoxin and derivatives thereof are illustrative of a new class of antitumor drugs that are topoisomerase II (top 2) inhibitors. The pharmacophore inhibits the catalytic activity of the purified enzyme but does not unwind relaxed or supercoiled DNA. It is nonintercalative and has at least two domains: a quasi-planar polycyclic ring system, which may bind between DNA base pairs, and a pendant substituent thought to interact with the enzyme, with the DNA grooves or with both. In SV40 and c-myc DNA, azatoxin induces numerous double-strand breaks according to a cleavage pattern which differs from those of known top 2 inhibitors. Azatoxin also is a potent inhibitor of tubulin polymerization.

Abstract: Azatoxin and derivatives thereof are illustrative of a new class of antitumor drugs that are topoisomerase II (top 2) inhibitors. The pharmacophore inhibits the catalytic activity of the purified enzyme but does not unwind relaxed or supercoiled DNA. It is nonintercalative and has at least two domains: a quasiplanar polycyclic ring system, which may bind between DNA base pairs, and a pendant substituent thought to interact with the enzyme, with the DNA grooves or with both. In SV40 and c-myc DNA, azatoxin induces numerous double-strand breaks according to a cleavage pattern which differs from those of known top 2 inhibitors. Azatoxin also is a potent inhibitor of tubulin polymerization.

Abstract: A method for the treatment of dehydration or nitrogen deficiency-based malnutrition is provided which involves administering to a patient in need thereof an effective amount of a compound selected from oligopeptides formed from the coupling of one or more amino acids with glutamine, the product of coupling glucose with glutamine, the product of coupling glucose and one or more amino acids with glutamine, or the product from acylating glutamine with a carboxylic acid having from 2 to 6 carbon atoms.