EP0023401A2
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EP
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Antitumor protein hybrid and process for the preparation thereof
Assignee: Teijin Ltd
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Filing: 1980-07-11
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Granted: —
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Expires: 2000-07-11
Abstract
Abstract 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 bythe following formula (1):(where Fab indicates a moiety which is substantially the fragment Fab of an antitumor immunogloblin; RA indicates a moiety which is the subunit A of ricin; X indicates a divalent organic radical; S, and S<sub>2</sub> are both sulfur atoms, S<sub>1</sub> indicating a sulfur atom arising from the disulfide bond (-S-S- bond) in an immunoglobulin and S<sub>2</sub> a sulfur atom arising from the disulfide bond in ricin; n stands for 0 or 1 and m stands for an integer of 1 to 5). This antitumor protein hybrid has remarkable and specific cytotoxicity against tumor cells.
Inventors
- 👤 Yasuhiko Masuho
- 👤 Takeshi Hara
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-08 23:48
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/68; A61K47/6801; A61K47/6803; A61K47/6811; A61K47/6817; A61K47/6819; A61K47/6825; A61K47/6827; A61K47/6889; Y; Y10; Y10S; Y10S530/00; Y10S530/866
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
120 words
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): (where Fab indicates a moiety which is substantially the fragment Fab of an antitumor immunoglobulin; RA indicates a moiety which is the subunit A of ricin; X indicates a divalent organic radical; S 1 and S 2 are both sulfur atoms, S 1 indicating a sulfur atom arising from the disulfide bond (-S-S- bond) in an immunoglobulin and S 2 a sulfur atom arising from the disulfide bond in ricin; n stands for 0 or 1 and m stands for an integer of 1 to 5).
Claim 2
Dependent Claim
120 words
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): (where Fab indicates a moiety which is substantially the fragment Fab of an antitumor immunoglobulin; RA indicates a moiety which is the subunit A of ricin; X indicates a divalent organic radical; S 1 and S 2 are both sulfur atoms, S 1 indicating a sulfur atom arising from the disulfide bond (-S-S- bond) in an immunoglobulin and S 2 a sulfur atom arising from the disulfide bond in ricin; n stands for 0 or 1 and m stands for an integer of 1 to 5).
Claim 3
Dependent Claim
43 words
Antitumor protein hybrid according to Claim 1 which is expressed by the following formula (II): (where definitions of Fab, RA, S 1 and S 2 are as same as those given in case of formula (I) and p stands for 1 or 2)..
Claim 4
Dependent Claim
24 words
Antitumor protein hybrid according to Claim 1 or Claim 2, wherein Fab is a moiety derived from the fragment Fab of an antitumor immunoglobulin.
Claim 5
Dependent Claim
24 words
Antitumor protein hybrid according to Claim 1 or Claim 2, wherein Fab is a moiety derived from the fragment Fab' of an antitumor immunoglobulin.
Claim 6
Dependent Claim
34 words
Antitumor protein hybrid according to Claim 1, wherein X is a divalent organic radical arising from a dimaleimide compound which is expressed by the following formula (III): (where Y indicates a divalent organic radical).
Claim 7
Dependent Claim
53 words
Antitumor protein hybrid according to Claim 1, wherein X is a divalent organic radical arising from a bishalocarbonyl compound which is expressed by the following formula (IV): (where Z indicates a divalent organic radical, and X 1 and X 2 are either the same or different from each other expressing bromine or iodine).
Claim 8
Dependent Claim
94 words
A process for preparing an antitumor protein hybrid which is expressed by the following formula (II'), which process comprises making the substantial fragment Fab of an antitumor immunogloblin which has at least one S-sulfo radical (-S-SO 3 - ) or an active disulfide radical expressed by the following formula (V) react with the subunit A of ricin which has at least one thiol radical (-SH) in the fragment: (where Z indicates (where definitions of Fab, RA, S 1 , S 2 and m are as same as those given in case of formula (I)).
Claim 9
Dependent Claim
94 words
A process for preparing an antitumor protein hybrid which is expressed by the following formula (II'), which process comprises making the substantial fragment Fab of an antitumor immunogloblin which has at least one S-sulfo radical (-S-SO 3 - ) or an active disulfide radical expressed by the following formula (V) react with the subunit A of ricin which has at least one thiol radical (-SH) in the fragment: (where Z indicates (where definitions of Fab, RA, S 1 , S 2 and m are as same as those given in case of formula (I)).
Claim 10
Dependent Claim
100 words
A process for preparing an antitumor protein hybrid which is expressed by the following formula (I'), which process comprises binding the substantial fragment Fab of an antitumor immunoglobulin which has at least one thiol radical in the fragment with the subunit A of ricin which has at least one thiol radical in the fragment with the use of a compound (cross-linking agent) which has at least two functional groups capable of reacting with a thiol radical. (where definitions of Fab, RA, X, S 1 , S 2 and m are as same as those given in case of formula (I)).
Claim 11
Dependent Claim
100 words
A process for preparing an antitumor protein hybrid which is expressed by the following formula (I'), which process comprises binding the substantial fragment Fab of an antitumor immunoglobulin which has at least one thiol radical in the fragment with the subunit A of ricin which has at least one thiol radical in the fragment with the use of a compound (cross-linking agent) which has at least two functional groups capable of reacting with a thiol radical. (where definitions of Fab, RA, X, S 1 , S 2 and m are as same as those given in case of formula (I)).
References Cited (Backward Citations)
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