Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.

Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.

Disclosed herein are methods of treating conditions, which may be associated with elevated levels of mast cells, basophils, eosinophils, or a combination thereof, with a therapeutically effective amount of dexpramipexole or pharmaceutical acceptable salt thereof.

Disclosed herein are methods of treating conditions, which may be associated with elevated levels of mast cells, basophils, eosinophils, or a combination thereof, with a therapeutically effective amount of dexpramipexole or pharmaceutical acceptable salt thereof.

Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, irritable bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.

Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, irritable bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.

The present invention relates to certain substituted bicyclic compounds that are agonists of RXR and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders.

The present invention relates to certain substituted bicyclic compounds that are agonists of RXR and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders.

Polycyclic aromatic hydrocarbons represented by the following general formula (I) wherein X is one of nitrogen, phosphorus, arsenic, antimony, bismuth, sulphur, selenium, tellurium; R independently represents an aromatic group and/or an aliphatic group; Q is one of a cyclic aliphatic hydrocarbon, a cyclic aromatic hydrocarbon, a polycyclic hydrocarbon, a polycyclic aromatic hydrocarbon, and/or a fused polycyclic aromatic hydrocarbon; wherein the substituents independently comprise one or more of a hydrogen atom, a deuterium atom, a fluorine atom, a chlorine atom, a bromine atom, a carbon atom, an oxygen atom (e.g. an alkylated oxygen atom), a nitrogen atom (e.g. an alkylated nitrogen atom), a cyano group, a nitro group, an alkyl group and/or anaryl group; p is an integer of 1 to 2; q is an integer of 1 to 4; Y.sup.1 and Y.sup.2 independently represent one or more of a hydrogen atom, a deuterium atom, a fluorine atom, a chlorine atom, a bromine atom, a carbon atom, an oxygen atom (e.g. an alkylated oxygen atom), a nitrogen atom (e.g. an alkylated nitrogen 20 atom), a cyano group, a nitro group, an alkyl group and/oranaryl group; and x is an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or more. ##STR00001##

Polycyclic aromatic hydrocarbons represented by the following general formula (I) wherein X is one of nitrogen, phosphorus, arsenic, antimony, bismuth, sulphur, selenium, tellurium; R independently represents an aromatic group and/or an aliphatic group; Q is one of a cyclic aliphatic hydrocarbon, a cyclic aromatic hydrocarbon, a polycyclic hydrocarbon, a polycyclic aromatic hydrocarbon, and/or a fused polycyclic aromatic hydrocarbon; wherein the substituents independently comprise one or more of a hydrogen atom, a deuterium atom, a fluorine atom, a chlorine atom, a bromine atom, a carbon atom, an oxygen atom (e.g. an alkylated oxygen atom), a nitrogen atom (e.g. an alkylated nitrogen atom), a cyano group, a nitro group, an alkyl group and/or anaryl group; p is an integer of 1 to 2; q is an integer of 1 to 4; Y.sup.1 and Y.sup.2 independently represent one or more of a hydrogen atom, a deuterium atom, a fluorine atom, a chlorine atom, a bromine atom, a carbon atom, an oxygen atom (e.g. an alkylated oxygen atom), a nitrogen atom (e.g. an alkylated nitrogen 20 atom), a cyano group, a nitro group, an alkyl group and/oranaryl group; and x is an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or more. ##STR00001##