Hoffmann-la Roche Inc.

Chugai Seiyaku Kabushiki Kaisha

Hitomi Suda

Nobuo Shimma

Takeshi Murata

Nobuhiro Oikawa

Kazuo Hattori

Hideo Ishitsuka

Satoshi Niizuma

Yasunori Kohchi

Masao Tsukazaki

Tohru Ishikawa

Hiroshi Fukuda

This invention relates to novel processes for the preparation of compounds of the formula [1], wherein R1, R2, R3 and R4 are as defined in the claims and description as well as pharmaceutically acceptable salts thereof. The compounds of the formula [1] are hexacyclic compounds having potent anti-tumor activity. 

Process for the preparation of hexacyclic compounds

The present invention relates to hexacyclic compound of the formula [1], wherein Z, Rand Rare as identified therein, and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of cell proliferative disorders.

Hexacyclic compounds and their therapeutic use

Hexacyclic compounds

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;

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Kanagawa, Japan

Hitomi Suda