N-OXYCARBONYL SUBSTITUTED 5'-DEOXY-5-FLUOROCYTIDINES

• Main Authors: SHIMMA, NOBUO, MIWA, MASANORI, UMEDA, ISAO, MURASAKI, CHIKAKO, KURUMA, ISAMI, ARASAKI, MOTOHIRO, ISHITSUKA, HIDEO
• Format: Patent
• Language: English
• Published: 16.01.2006
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SUGARS

Jedinjenja predstavljena opštom formulom (I) u kojoj R1 označava n-propil, n-butil, n-pentil, izopentil, neopentil, 3,3-dimetilbutil, n-heksil, 2-etilbutil, feniletil i cikloheksilmetil, a R2 označava atom vodonika ili radikal koji se lako može hidrolizovati pod fiziološkim uslovima, kao i hidrati ili solvati jedinjenja opšte formule (I). Prijava sadrži još 3 nezavisna i 3 zavisna patentna zahteva. Compounds represented by the general formula (I), wherein R is a saturated or unsaturated, straight or branched hydrocarbon radical [wherein the number of carbon atoms in the longest straight chain of this hydrocarbon radical ranges from three to seven], or a radical of the formula -(CH2)n-Y [in which n is an integer from 0 to 4, when Y is a cyclohexyl radical, or n is an integer from 2 to 4, when Y is a lower alkoxy radical having 1 to 4 carbon atom(s) or a phenyl radical], and R is a hydrogen atom or a radical easily hydrolyzable under physiological conditions, as well as hydrates or solvates of the compounds of the general formula (I), can be utilized in the treatment of tumors, They can be prepared by reacting a compound of formula R -OCOCl with a N -unsubstituted 5'-deoxy-5-fluorocytidine of the above formula I, wherein R would stand for protecting groups, and if necessary removing the protecting groups.