Asahi Kasei Kogyo Kabushiki Kaisha

Eisai Company, Limited

Tanabe Seiyaku Company, Limited

Japanese Foundation for Cancer Research

Cancer Institute, Japanese Foundation for Cancer Research

Yoshio Sakurai

Minoru Akiyama

Torao Ishida

Shigeru Tsukagoshi

Takashi Tsuruo

Koichi Yoshida

Kageyasu Akashi

Hiroshi Hayashi

Daikichi Nishimura

Fujiko Oh-hashi

Tateshi Kataoka

5-((3,4-dimethoxyphenetyl)methylamino)- 2-(3,4-dimethoxy-phenyl)-2-isopropylvaleronitrile or a pharmaceutically acceptable salt thereof is effective to prevent metastasis of cancer.

Antimetastatic agent

An agent for enhancing antitumor activity of antitumor agents comprising as the active ingredient diltiazem or a pharmaceutically acceptable acid addition salt thereof, an antitumor composition comprising the diltiazem or an acid addition salt thereof and a conventional antitumor agent, and further a method for treating tumors by administering diltiazem or an acid addition salt thereof together with a conventional antitumor agent in oral or parenteral route to patients suffering from various tumors. Said active diltiazem or a salt thereof is effective for enhancing the antitumor activity of antitumor agents because it can enhance sensitivity of tumor cells to antitumor agents regardless the tumor cells have resistance to the antitumor agents or not.

Agent for enhancing antitumor activity of antitumor agent

A N.sup.4 -acylcytosine arabinoside preparation which consists essentially of (a) a liposome of lecithin and (b) a N.sup.4 -acylcytosine arabinoside having a C.sub.6-18 aliphatic acyl group and being encapsulated in the liposome.

N.sup.4 -Acylcytosine arabinoside compositions

Compounds represented by formula (I) ##STR1## wherein one of Z.sub.1 ', Z.sub.2 ', Z.sub.3 ' and Z.sub.4 ' represents R, another one of Z.sub.1 ', Z.sub.2 ', Z.sub.3 ' and Z.sub.4 ' represents Z, and the remaining two moieties of Z.sub.1 ', Z.sub.2 ', Z.sub.3 ' and Z.sub.4 ' represents a hydrogen atom and/or a protective group, one of R and Z represents A.sub.1 and the other represents A.sub.2, A.sub.1 being an acyl group having 14 to 22 carbon atoms which does not contain a carboxylic group and A.sub.2 being an acyl group having 2 to 14 carbon atoms and having one carboxyl group, X represents a hydrogen atom or a halogen atom (hereinafter referred to as Compound Ia); a 2,2'-anhydro product of Compound Ia wherein Z.sub.2 ' represents a hydrogen atom (hereinafter referred to as Compound Ib); an arabinosylation product of Compound Ia (hereinafter referred to as Compound Ic); a deamination product of Compound Ia (hereinafter referred to as Compound Id); a 2'-deoxy product of Compound Id wherein Z.sub.2 ' represents a hydrogen atom (hereinafter referred to as Compound Ie); a salt of Compound Ia, Ib, Ic, or Id or Ie having an A.sub.2 group with a base (hereinafter referred to as Compound If); and a salt of Compound Ia, Ib or Ic wherein Z.sub.1 ' represents a hydrogen atom with an acid (hereinafter referred to as Compound Ih); and processes for preparing the same.

Diacylnucleosides and process for preparing the same

A nucleotide derivative represented by the general formula: ##STR1## wherein R represents an acyl group having 14 - 22 carbon atoms and having an aliphatic acyl moiety; X represents a hydrogen atom, a halogen atom, an alkyl group having 1 - 4 carbon atoms, or a trifluoromethyl group; and at least one, but not all, of Y.sub.1, Y.sub.2, and Y.sub.3 represents a phosphate, a pyrophosphate, a triphosphate, or a salt thereof, the balance of Y.sub.1, Y.sub.2 and Y.sub.3 representing a hydroxyl group; or in case of ribosyl, Y.sub.1 and Y.sub.3, or Y.sub.2 and Y.sub.3 represent, at the same time, the aforesaid phosphate, pyrophosphate, triphosphate or salt thereof and the remaining group of Y.sub.1, Y.sub.2 or Y.sub.3 represents a hydroxyl group; or in case of arabinosyl, Y.sub.1 and Y.sub.2, or Y.sub.2 and Y.sub.3 represent, at the same time, the aforesaid phosphate, pyrophosphate, triphosphate or salt therof and the remaining group of Y.sub.1, Y.sub.2 or Y.sub.3 represents a hydroxyl group. The nontoxic salts of these phosphates are useful as an antileukemialagent for mice which is soluble in water and has high stability.

Cytidine nucleotide derivatives

An N.sup.4 -acyl-1-.beta.-D-arabinofuranosylcytosine having the following formula ##SPC1## Wherein R is an aliphatic acyl group having 3 to 35 carbon atoms. The compounds of this invention are useful as a cancer chemotherapeutic agent for controlling tumors, e.g., in mice, an insecticide, and a fungicidal surface active agent.

Growing community of inventors

Mitaka, Japan

Yoshio Sakurai