Asahi Kasei Kogyo Kabushiki Kaisha

Takashi Shirai

Torao Ishida

Minoru Akiyama

Mitsuru Shibukawa

Hiroshi Hayashi

Yukiji Shimojima

AI-77 compounds, pharmaceutically acceptable salts thereof, and a process for the preparation thereof are described, said compounds having the formulae ##STR1## wherein: X is NR.sub.6 or O; Y is NHR.sub.5 or combine with Z to provide a link for bonding C and C; Z is H or combines with Y to provide a link for bonding C and C; R.sub.1, R.sub.3 and R.sub.5 are each H, R', --CH.sub.2 R, or --COR; R.sub.6 is H or R; R.sub.7 is H, R or CH.sub.2 R; R is a hydrocarbon group consisting of a saturated or unsaturated straight or branched aliphatic group of C.sub.1 to C.sub.17, an aromatic group of C.sub.6 to C.sub.10, a cage type group of C.sub.7 to C.sub.10, a monocyclic aliphatic group of C.sub.3 to C.sub.8, an aromatic-aliphatic group of C.sub.7 to C.sub.15, a heterocyclic hydrocarbon of C.sub.1 to C.sub.9, wherein the above hydrocarbons can be substituted with one or more groups selected from halogen, oxo, carboxyl, hydroxyl, a saturated or unsaturated straight or branched aliphatic group of C.sub.1 to C.sub.5, an aromatic group of C.sub.6 to C.sub.10, a monocyclic aliphatic group of C.sub.3 to C.sub.8, an aromatic-aliphatic group of C.sub.7 to C.sub.11, alkoxy of C.sub.1 to C.sub.5, thioalkoxyl of C.sub.1 to C.sub.5, carboalkoxyl of C.sub.1 to C.sub.6, acyl of C.sub.1 to C.sub.5, acyloxy of C.sub.2 to C.sub.6 and a heterocyclic group of C.sub.1 to C.sub.9 ; R' is the same as R exclusive of those groups wherein unsaturated carbon or tertiary carbon is directly bonded to O or N; R.sub.2 is H, or combines with T.sub.1 to provide a link for bonding C and O in a lactone ring; T.sub.1 is OH or combines with R.sub.2 to provide a link for bonding C and O in a lactone ring; R.sub.4 is H or combines with T.sub.2 to provide a link for bonding C and O in a lactone ring; and T.sub.2 is OH or combines with R.sub.4 to provide a link for bonding C and O in a lactone ring; and pharmaceutically acceptable salts thereof.

AI-77 Compounds and pharmaceutically acceptable salts thereof

N.sup.4 -Acyl-1-.beta.-D-arabinofuranosylcytosine-5'-esters represented by the formula ##STR1## wherein R.sup.1 represents an acyl group having 3 to 28 carbon atoms and R.sup.2 represents an XCH.sub.2, XCH.sub.2 CH.sub.2 or CH.sub.3 CHX group, wherein X represents a halogen atom, a (CH.sub.3).sub.2 N or (C.sub.2 H.sub.5).sub.2 N group.

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Fuji, Japan

Takashi Shirai