Asahi Kasei Kogyo Kabushiki Kaisha

Toyo Jozo Kabushiki Kaisha

Satoshi Shuto

Hiromichi Itoh

Masatoshi Tsujino

Kiyofumi Fukukawa

Tatsuro Fujiwara

Takumi Obara

Hideo Sakakibara

Daisuke Mochizuki

Masao Yaso

Hiromichi Ito

Takehiro Koshio

Aminoalkylcyclopropane derivatives

Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each C.sub.16-18 long-chain aliphatic acyl and are the same or different; and pharmacologically acceptable salts thereof are disclosed. These novel compounds are effective against 5-FU-resistant tumor cells, have low toxicity, and are not inactivated by nucleoside phosphorylase in vivo.

5'-trifluoromethyl-2'-deoxy-uridine phospholipid compounds

A compound of the formula ##STR1## wherein A is adenine-9-yl and X is halogen, Preferably iodine, or a pharmaceutically acceptable salt thereof. It is a novel derivative of neplanocin A and has almost the same level of cytotoxic activity. However, it is not inactivated by the action of adenosine deaminase. It is produced by replacing a hydroxyl at position-6' in neplanocin A or 2', 3'-O-protected neplanocin A with halogen by use of a halogenating agent, and when hydroxyl at position-2' or -3' is protected, removing the protective group thereof.

6'-deoxy-6'-halo-neplanocin A and its production

Novel nucleoside-phospholipid conjugates of the formula ##STR1## wherein R.sub.1 is C.sub.14-24 long chain aliphatic acyl or C.sub.1-24 aliphatic alkyl, R.sub.2 is C.sub.2-10 aliphatic acyl or C.sub.1-24 aliphatic alkyl and N.sub.s is a nucleoside residue; and pharmacologically acceptable salts thereof are prepared in a one-step reaction by reacting the corresponding nucleoside and glycerophospholipid derivative in the presence of phospholipase D-P.

Novel nucleoside-phospholipid conjugate

Novel nucleoside-phospholipid conjugates of the formula ##STR1## wherein R.sub.1 is C.sub.14-24 long chain aliphatic acyl or C.sub.1-24 aliphatic alkyl and N.sub.s is a nucleoside residue; and pharmacologically acceptable salts thereof are prepared in a one-step reaction by reacting the corresponding nucleoside and glycerophospholipid derivative in the presence of phospholipase D-P.

Nucleoside-phospholipid conjugate

A compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are long-chain fatty acid residue, and Ns is nucleoside residue selected from the group consisting of 5-fluorouridine-5'-yl, 5-fluoro-2'-deoxyuridine-5'-yl-, bredinin-5'-yl, tubercidine-5'-yl-, neplanocin A-6'-yl-, 5-fluorocytidine-5'-yl-, arabinosylcytosine-5'-yl, arabinocyl-5-fluorocytosine-5'-yl-, arabinosyladenine-5'-yl- and arabinosylthymine-5 '-yl-, and pharmacologically acceptable salts thereof, having antitumor activity.

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Shizuoka, Japan

Satoshi Shuto