Hoffmann-la Roche Inc.

Hideo Ishitsuka

Nobuo Shimma

Isao Umeda

Yasuji Suhara

Nobuhiro Oikawa

Kazuo Hattori

Yasunori Kohchi

Hitomi Suda

Tohru Ishikawa

Masanori Miwa

Morio Fujiu

Arthur M Felix

Johannes A Meienhofer

Kazuteru Yokose

Hiromi Maruyama

Chikako Murasaki

Haruyoshi Shirai

Nobuo Shinma

Kenji Takemoto

Yumiko Miyasaka

Yumiko Ohta

Isami Kuruma

Motohiro Arasaki

Novel 5&prime;-deoxy-cytidine derivatives represented by the general formula (I)

5&prime;-deoxy-cytidine derivative administration to treat solid tumors

Novel 5'-deoxy-cytidine derivatives represented by the general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R.sup.2 is a hydrogen atom, or --CO--OR.sup.4 group [wherein R.sup.4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula --(CH.sub.2).sub.n --Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R.sup.3 is a hydrogen atom, bromo, iodo, cyano, a C.sub.1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C.sub.1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.

5'-deoxy-cytidine derivatives

Compounds of the formula (I) ##STR1## wherein R.sup.1 is each independently hydrogen or a group easily hydrolyzable under physiological conditions;

5'deoxycytidine derivatives

The invention relates to N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives which are useful as an agent for treating tumors, pharmaceutical compositions including the same, a method of treating tumors and a method of preparing N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives for treating tumors. Compounds of formula (I), ##STR1## wherein R.sup.1 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 is a radical of the formula --(CH.sub.2)n--.sup.Y wherein Y is a cyclohexyl radical, a C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical and wherein when Y is a cyclohexyl radical n is an integer from 0 to 4, and when Y is C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical n is an integer from 2 to 4, and R.sup.2 is a hydrogen atom or a radical easily hydrolyzable under physiological conditions, or a hydrate or solvate thereof. Compounds of formula (I) are useful in the treatment of tumors.

N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine compounds,

The novel 5'-deoxy-5-fluorocytidine derivatives of formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen or an easily hydrolyzable radical under physiological conditions, with the proviso that, at least one or R.sup.1, R.sup.2 and R.sup.3 is an easily hydrolyzable radical under physiological conditions, as well as hydrates of solvates of these compounds have antitumor properties. They can be prepared from compounds of formula I, wherein R.sup.1 is hydrogen or an amino-protecting radical and R.sup.2 and R.sup.3 are hydrogen or a hydroxy-protecting radical or taken together are a cyclic hydroxy-protecting radical.

Fluorocytidine derivatives

Antivirally active compounds of the formula ##STR1## wherein R.sup.1 represents hydroxy, acyloxy derived from an aliphatic acid having 2-18 carbon atoms or a heterocyclic carboxylic acid containing nitrogen atom(s), lower alkoxycarbonyloxy, aminoacyloxy or carboxyalkanoyloxy;

Substituted acetophenones and compositions containing them

A pentadecapeptide and salts thereof with immunopotentiating activity is presented. Also presented is a fermentation process for the preparation of the pentadecapeptide by a microorganism of the genus Streptoverticillium and pharmaceutical preparations containing the peptide or its salts.

Pentadecapeptide

Novel hexapeptides corresponding to internal fragments of thymosin .alpha..sub.1 are active as agents which restore and stimulate immune function.

Immunopotentiating peptides

Antiviral compositions containing 3-alkoxyflavone compounds as their active ingredients are disclosed.

3-Alkoxyflavone antiviral agents

Compounds of the formula: ##STR1## wherein R.sub.1 is hydroxy, phosphonooxy, aminoglycosyloxy, acylaminoglycosyloxy, benzyloxycarbonyloxy, arylcarbonyloxy, trialkylammonio-acyloxy or furoyloxy; R.sub.2 and R.sub.3 each are lower alkoxy; and R.sub.4 is benzimidazolyl, furyl which is unsubstituted or substituted with lower alkyl, thienyl which is unsubstituted or substituted with lower alkyl, or phenyl which is substituted with lower alkyl, lower alkoxy, alkoxyalkoxy, alkylthio, alkylenedioxy, or acyloxy, with the proviso that when R.sub.1 is hydroxy, R.sub.4 is benzimidazolyl or phenyl which is substituted by acyloxy or alkoxyalkoxy, or pharmaceutically acceptable salts thereof useful as antiviral agents.

Growing community of inventors

Yokohama, Japan

Hideo Ishitsuka