Teijin Limited

Other

Hidematsu Hirai

Takeshi Hara

Yasuhiko Masuho

Yoshinori Kato

Naoji Umemoto

Masahiko Saito

Hisashi Fukushima

Yasutaka Kayama

Yumiko Takeda

Sachio Ishimoto

Yoshinobu Hashimoto

Noriaki Endo

Takeo Oba

Kenzo Watanabe

Kazuhiko Itoh

Kazuo Kishida

Yutaka Tsukada

Teruhisa Noguchi

Toshiro Mori

Hitoshi Fujimori

Tamiko Sunami

Process for preparation of antibody conjugates

Cytotoxic antibody conjugates and a process for preparation thereof

Antitumor protein hybrid, composed of a moiety which is substantially the fragment Fab of an antitumor immunoglobulin and a moiety which is substantially the fragment A of a diphtheria toxin, which is expressed by the following formula (I):

Antitumor protein hybrid and process for the preparation thereof

5-fluoro-2'-deoxyuridine derivatives expressed by general formula (1) and their pharmacologically permissible salts ##STR1## wherein A indicates a saturated or unsaturated divalent aliphatic hydrocarbon group having 1 to 30 carbon atoms; the letter n indicates 0 or 1, and when n is 0, it indicates that Y is directly bound to an oxygen atom; Y represents a hydrogen atom, phenyl group, or substituted phenyl group; however, when Y is a hydrogen atom, n is 1; R indicates a hydrogen atom or alcohol-protecting group. These compounds have a very strong antitumor activity.

5-fluoro-2'-deoxyuridine derivatives and a process for the preparation

A conjugate having cytotoxicity prepared by covalently binding a polymer which has cytotoxic substances linked to its side chains and a reactive group at its terminal to an immunoglobulin, or its fragment, which is capable of selectively binding to a particular antigen possessed by cells to be killed.

Conjugate having cytotoxicity and process for the preparation thereof

A conjugate having cytotoxicity prepared by covalently binding a serum albumin having cytotoxic substance linked thereto to an immunoglobulin, or its fragment, which is able to bind selectively with a particular antigen of cells to be killed.

A cytocidal modified immunoglobulin expressed by formula (I) ##STR1## (wherein Ab represents an immunoglobulin or its fragment; R represents a divalent organic group; and n is an integer from 1 to 20).

Cytocidal modified immunoglobulin and process for the preparation thereof

Antitumor protein hybrid, composed of a moiety which is substantially the fragment Fab of an antitumor immunogloblin and a moiety which is the subunit A of ricin, which is expressed by the following formula (I):

Antitumor hybrid and process for the preparation thereof

A reactive polymer having the degree of polymerization in the range of 5 to 3,000, with 60 mole % or more of the whole constituent units comprising the constituent units expressed by formula (I) ##STR1## wherein Z indicates a hydrogen atom or a univalent cation; m is an integer 1 to 4: and has an active group expressed by formula (II) at the carboxyl end of the main chain ##STR2## wherein X indicates a hydrogen atom or a group which can form an active disulfide linkage together with a neighboring sulfur atom; W is a divalent organic group; and R.sub.1 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. Since this reactive polymer can bind to cytotoxic substances, which contain an amino group or imino group in the molecule by way of the carboxyl group of the side chain and it also can bind to, for instance, antitumor immunoglobulins by way of an active group (thiol group or active disulfide group) at the end of the main chain, it can be used as a polymer carrier in the preparation of target seeking antitumor drugs.

Reactive alpha amino acid polymer

Antitumor protein hybrid, having a moiety consisting of the antitumor immunoglobulin and a moiety substantially consisting of the fragment A of a diphtheria toxin, which is expressed by the following formula (I):

A protein hybrid having cytotoxicity obtained by covalently bonding an immunoglobulin or its fragment, which is capable of binding selectively to an antigen possessed by a cell to be destroyed, to a protein, which is obtained from Momordica charantia and has an activity to terminate protein synthesis. This protein hybrid displays remarkable cytotoxicity against targel cells.

Protein hybrid having cytotoxicity and process for the preparation

A cytotoxic protein hybrid obtained by covalently bonding an immunoglobulin or its fragment, which is capable of linking selectively with an antigen possessed by a cell to be destroyed, to a protein, which is obtained from Phytolacca americana and has an activity to terminate protein synthesis. This protein hybrid displays remarkable cytotoxicity against target cells.

Cytotoxic protein hybrid and process for the preparation thereof

Antitumor protein hybrid, composed of a moiety which is substantially the fragment Fab of an anti-.alpha.-fetoprotein antibody and a moiety which is substantially the fragment A of a diphtheria toxin, which is expressed by the following formula (I):

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Hachioji, Japan

Takeshi Hara