Houston Pharmaceuticals, Inc.

Other

Priebe, Waldemar

Przewloka, Teresa

Fokt, Izabela

Skibicki, Piotr

Krawczyk, Marta

Perez-soler, Roman

Grynkiewicz, Grzegorz

Piotr Skibicki

Roman Perez-Soler

Waldemar Priebe

Marta Krawczyk

Grzegorz Grynkiewicz

Izabella Fokt

Teresa Przewloka

Izabela Fokt

Waldeman Priebe

Krzysztof Dziewiszek

Teresa Prezewloka

The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3' of the sugar moiety or modified or unmodified alkyl-aromatic ring substitutions at the C-4&#x2032; of the sugar moiety. It also discloses novel methods for the preparation of sugar substrates and methods for the preparation of anthracycline antibiotics. These anthracycline analogs show high cytotoxicity in vitro against several tumor cell lines.

Anthracycline antibiotics and methods of treating cancer using the same

Methods and compositions for the manufacture of C-3' and C-4&#x2032; anthracycline antibiotics

The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3&prime; of the sugar moiety or modified or unmodified alkyl-aromatic ring substitutions at the C-4&prime; of the sugar moiety. It also discloses novel methods for the preparation of sugar substrates and methods for the preparation of anthracycline antibiotics. These anthracycline analogs show high cytotoxicity in vitro against several tumor cell lines.

Methods and compositions for the manufacture of C-3&prime; and C-4&prime; anthracycline antibiotics

The present invention discloses new and novel halogenated anthracyclines linked through the saccharide portions. These congeners show high activity in vitro against several tumor cell lines. In doxorubicin (DOX) sensitive cell lines, they are at least as cytotoxic as DOX and in some cases more so. Many of these 4&prime;- and 6&prime;-fluorinated anthracyclines are more effective against multidrug-resistant tumors than was DOX, and/or have greater effectiveness than DOX against DOX sensitive cells. The compounds of this invention also have anti-amyloidogenic effects and the use of these compounds in the treatment of Alzheimer's disease is contemplated.

Methods and compositions for the manufacture of halogenated anthracyclines with increased antitumor activity, other anthracyclines, halogenated sugars, and glycosyl donors

The present disclosure details novel modified anthracyclines, the synthesis thereof, and their use in treating patients with tumors. Preferred aspects of the disclosure involve modified anthracyclines which have an O-substituted aromatic ring on their sugar moiety. Other preferred aspects of the disclosure involve synthesis steps wherein a hydroxyl group on a sugar moiety to be added is blocked with a halo-substituted alkyl group during the process of adding it to an anthracycline ring compound.

Anthracyclines with unusually high activity against cells resistant to

Growing community of inventors

Warsaw, Poland

Piotr Skibicki