Nippon Kayaku Kabushiki Kaisha

Keizou Ishikawa

Masayuki Kitagawa

Takeshi Nakanishi

Osamu Kogawa

Katsutoshi Takahashi

Hisao Ekimoto

Keiichirou Yamamoto

Kazutoshi Takashio

Masanobu Suzuki

Kazuhisa Shimizu

Toshitaka Murata

Takeshi Onda

Kenji Iwata

Yukio Irie

Masao Shibata

Fumiko Kobayashi

Miyoji Hanaoka

A medicinal preparation is desired which has no harmful side effects such as hypersensitive reaction, heightens the water solubility of a sparingly water-soluble anticancer agent, maintains a high drug concentration in the blood, accumulates a drug in a tumor tissue at a high concentration, heightens the pharmacological effect of the sparingly water-soluble anticancer agent, and diminishes the side effects of the anticancer agent. Provided are: a novel block copolymer which can be a drug carrier having no harmful side effects such as hypersensitive reaction; a micelle preparation in which micelles are formed and which contains a sparingly water-soluble anticancer agent, especially paclitaxel, incorporated in the micelles in an amount necessary for a disease treatment without bonding it to the block copolymer and which can heighten the solubility of the drug in water; and an anticancer agent which comprises the micelle preparation as a medical ingredient, maintains a high concentration in the blood, has more potent drug activity, and is reduced in toxicity.

Block copolymer, micelle preparation, and anticancer agent containing the same as active ingredient

A novel podophyllotoxin derivative, which is capable of releasing a drug without depending on biological enzymes and can be expected to have an effective therapeutic effect and is soluble in water has been demanded. A polymer having a polyethyleneglycol structural unit and two or more succinic monoamide structural units, particularly a polymer conjugate of a podophyllotoxin in which a carboxylic acid group of polyethyleneglycol/polyaspartic acid copolymer and a hydroxyl group of podophyllotoxin and linked via an ester bond is provided.

High-molecular weight conjugate of podophyllotoxins

[Problems] To provide a novel taxane derivative which can release the medicinal substance in a bioenzyme-independent manner, is expected to have an effective therapeutic efficacy, and has a water-solubility. [Means for Solving Problems] Disclosed is a polymer conjugate of a taxane, which comprises a polymer having a polyethylene glycol moiety and two or more succinic acid monoamide moieties and a taxane, wherein a carboxylate group in the polymer and an alcoholic hydroxyl group in the taxane are bound to each other via an ester bonding.

Polymer conjugate of taxane

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

Growing community of inventors

Kita-ku, Japan

Keizou Ishikawa