The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.

Matyus; Peter

Magyar; Kalman

Pihlavisto; Marjo

Gyires; Klara

Haider; Norbert

Wang; Yinghua

Woda; Patrick

Dunkel; Petra

Toth-Sarudy; Eva

T ros; Gyorgy

Semmelweis Egyetem

Compounds for inhibiting semicarbazide-sensitive amine oxidase (SSAO)/vascular adhesion protein-1 (VAP-1) and uses thereof for treatment and prevention of diseases

Noni juice and a protein-free, alcohol precipitate of Noni juice inhibited angiogenesis in in vitro human angiogenesis models. When growth medium contained Noni juice at least over the range from about 2.5% to about 33% (by volume), angiogenesis was blocked. Moreover, Noni juice and an ethanol precipitate were able to destroy a pre-existing angiogenic response as well as prevent the development of new vessels. Noni juice was effective in inhibiting the growth of angiogenic vessels from breast cancer explants. It will also be effective in treating cancers and non-cancerous diseases whose response includes an increase in angiogenesis, e.g., retinopathy of prematurity, neovascular glaucoma, diabetic retinopathy, and psoriasis. The primary antiangiogenic component is believed to be a carbohydrate with a molecular weight less than about 6000 Daltons. In an initial experiment, oral administration of Noni juice appeared to adversely affect the antioangiogenic component(s) in the juice.

Board of Supervisors of Louisiana State University And Agricultural and Mechanical College

Inhibition of angiogenesis and destruction of angiogenic vessels with extracts of noni juice Morinda citrifolia

Noni juice and a protein-free, alcohol precipitate of Noni juice inhibited angiogenesis in in vitro human angiogenesis models. When growth medium contained Noni juice at least over the range from about 2.5% to about 33% (by volume), angiogenesis was blocked. Moreover, Noni juice and an ethanol precipitate were able to destroy a pre-existing angiogenic response as well as prevent the development of new vessels. Noni juice was effective in inhibiting the growth of angiogenic vessels from breast cancer explants. It will also be effective in treating cancers and non-cancerous diseases whose response includes an increase in angiogenesis, e.g., retinopathy of prematurity, neovascular glaucoma, diabetic retinopathy, and psoriasis. In an initial experiment, Noni juice was effective in treating lesions associated with psoriasis. The primary antiangiogenic component is believed to be a carbohydrate with a molecular weight less than about 6000 Daltons. In an initial experiment, oral administration of Noni juice appeared to adversely affect the antiangiogenic component(s) in the juice.

Inhibition of angiogenesis and destruction of angiogenic vessels with extracts of noni juice (Morinda citrifolia)