A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/045 (2006.01) A61K 31/403 (2006.01) A61K 31/4164 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2685726
Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are fulvene and/or fulvalene analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, as well as numerous inflammatory, degenerative and vascular diseases, including various ocular diseases. Representative fulvene and/or fulvalene analogs include fulvene and fulvalene analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function, at least, by inhibiting Nox or ROS. In some embodiments, the Nox is one that is selectively expressed in cancer cells over normal cells, or one that is expressed in higher amounts in cancer cells over normal cells. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.
L'invention concerne des composés, des compositions pharmaceutiques contenant ces composés, et des procédés de préparation et d'utilisation de ceux-ci. Ces composés consistent en des analogues de fulvène et/ou fulvalène. Ces composés et ces compositions peuvent être utilisés pour traiter et/ou prévenir une grande variété de cancers, notamment les cancers résistant aux médicaments, ainsi que de nombreuses maladies inflammatoires, dégénératives et vasculaires, de même que diverses maladies oculaires. Les analogues représentatifs de fulvène et/ou fulvalène consistent en des analogues de fulvène et fulvalène de divers colorants, hormones, sucres, peptides, oligonucléotides, acides aminés, nucléotides, nucléosides, et polyols. Ces composés semblent fonctionner, au moins, par inhibition de Nox ou des ROS. Dans certains modes de réalisation, le Nox est celui qui est sélectivement exprimé dans des cellules cancéreuses plutôt que dans les cellules normales, ou celui qui est exprimé en plus grandes quantités dans les cellules cancéreuses que dans les cellules normales. Ainsi, les composés consistent en de nouveaux agents thérapeutiques d'une variété de cancers et d'autres maladies.
Arbiser Jack L.
Emory University
Riches Mckenzie & Herbert Llp
The U.s. Government As Represented By The Department Of Veterans
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