Asahi Kasei Kogyo Kabushiki Kaisha

Toyo Jozo Kabushiki Kaisha

Asahi Kasei Kabushiki Kaisha

Hiromichi Itoh

Satoshi Shuto

Tatsuro Fujiwara

Masatoshi Tsujino

Kiyofumi Fukukawa

Takumi Obara

Masao Yaso

Motoshi Shoda

Takehiro Koshio

Biphenyl-5-alkanoic acid derivatives and use thereof

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

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Shizuoka, Japan

Hiromichi Itoh