Nippon Kayaku Kabushiki Kaisha

Osamu Kogawa

Hisao Ekimoto

Keizou Ishikawa

Kenji Iwata

Katsutoshi Takahashi

Tadashi Ishii

Masanobu Suzuki

Takeshi Nakanishi

Toshitaka Murata

Yukio Irie

Kimihiko Takada

Fumiko Kobayashi

Miyoji Hanaoka

The present invention relates to a novel fine cisplatin powder utilized as an anticancer agent. The fine cisplatin powder obtained in the present invention does not cause secondary agglomeration, is excellent in fluidity and easily handleable in the pharmaceutical preparation step. Furthermore, the fine cisplatin powder is reduced in the content of N,N-dimethylformamide as the residual solvent, and can be dissolved rapidly in physiological saline, thus being suitable for cancer therapy particularly by intra-arterial injection. This fine powder can be produced by contriving specified means for crystallizing cisplatin from a solution thereof in N,N-dimethylformamide.

Fine cisplatin powder and process for the production thereof

The present invention relates to benzo�c!phenanthridinium derivative of the general formula A: ##STR1## wherein M and N individually represent a hydroxyl or lower alkoxy group, or M and N simultaneously represent a hydrogen atom or together form a methylenedioxy group, X.sup.- represents an acid residue or a hydrogen acid residue, and R represents a lower alkyl group, and a process for preparing such derivatives. The compounds exhibit both potent antitumor activity and platelet aggregation inhibition activity, and are expected to be useful for the treatment of tumors. The process has good reproducibility and may be effected under moderate conditions, and therefore the process is practically useful. In addition, hydrogen salts of the present compounds have an enhanced stability, which is an advantage in formulating the same into pharmaceutical preparations.

Process for preparing benzo�c!phenanthridinium derivatives, novel

A platinum (II) complex represented by the general formula: ##STR1## [wherein A's are each ammonia or two A's jointly represent 1,2-diaminocyclohexane, 1-amino-1-aminomethylcyclohexane or 1,4-diamino-2-methylbutane; and B's may be same or different and represent ##STR2## (wherein m is 0, 1 or 2; n is 0 or 1; R.sub.1 is a C.sub.3 -C.sub.6 alkyl group substituted with one or two hydroxyl groups) or two B's jointly represent ##STR3## (wherein R.sub.2 is a C.sub.2 -C.sub.5 alkyl group substituted with one hydroxyl group)]. These platinum (II) complexes have high potencies for use as an antitumor agent.

Platinum complexes

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Kashiwa, Japan

Osamu Kogawa