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US4357273A
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Antitumor protein hybrid and process for the preparation thereof
Assignee: Teijin Ltd
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Filing: 1980-07-21
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Granted: 1982-11-02
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Expires: 2000-07-21
Abstract
Abstract 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): Fab-(S1-(X)n-S2-FA)m(I) (where Fab indicates a moiety which is substantially the fragment Fab of an anti- alpha -fetoprotein antibody; FA indicates a moiety which is substantially the fragment A of diphtheria toxin; X indicates a divalent organic radical; S1 and S2 are both sulfur atoms, S1 indicating a sulfur atom arising from the disulfide bond (-S-S-bond) in an anti- alpha -fetoprotein antibody and S2 a sulfur atom arising from the disulfide bond in a diphtheria toxin; n stands for 0 or 1 and m stands for an integer of 1 to 5). This antitumor protein hybrid has remarkable and specific citotoxicity against tumor cells.
Inventors
- 👤 Yasuhiko Masuho
- 👤 Naoji Umemoto
- 👤 Takeshi Hara
- 👤 Hidematsu Hirai
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 06:14
CPC Classifications
C; C07; C07K; C07K16/00; C07K16/18; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/68; A61K47/6801; A61K47/6803; A61K47/6811; A61K47/6817; A61K47/6829; A61K47/6889; C07K16/28; C07K16/30; C07K16/303; C07K2317/00; C07K2317/50; C07K2317/55; C07K2319/00; C07K2319/55; Y; Y10; Y10S; Y10S530/00; Y10S530/806; Y10S530/82; Y10S530/825; Y10S530/866
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
136 words
Antitumor protein hybrid comprising (1) a moiety which is substantially the fragment Fab of an anti-α-fetoprotein antibody and (2) a moiety which is substantially the fragment A of a diphtheria toxin, which antitumor protein hybrid is expressed by the following formula (I): Fab(S.sub.1 --(X).sub.n --S.sub.2 --FA).sub.m (I) where Fab indicates a moiety which is substantially the fragment Fab of an anti-α-fetoprotein antibody; FA indicates a moiety which is substantially the fragment A of diphtheria toxin; X indicates a pharmacologically inert divalent organic radical; S 1 and S 2 are both sulfur atoms, S 1 indicating a sulfur atom arising from the disulfide bond in the anti-α-fetoprotein antibody and S 2 a sulfur atom arising from the disulfide bond in the diphtheria toxin; n represents 0 or 1 and m represents an integer of 1 to 5.
Claim 2
Dependent Claim
136 words
Antitumor protein hybrid comprising (1) a moiety which is substantially the fragment Fab of an anti-α-fetoprotein antibody and (2) a moiety which is substantially the fragment A of a diphtheria toxin, which antitumor protein hybrid is expressed by the following formula (I): Fab(S.sub.1 --(X).sub.n --S.sub.2 --FA).sub.m (I) where Fab indicates a moiety which is substantially the fragment Fab of an anti-α-fetoprotein antibody; FA indicates a moiety which is substantially the fragment A of diphtheria toxin; X indicates a pharmacologically inert divalent organic radical; S 1 and S 2 are both sulfur atoms, S 1 indicating a sulfur atom arising from the disulfide bond in the anti-α-fetoprotein antibody and S 2 a sulfur atom arising from the disulfide bond in the diphtheria toxin; n represents 0 or 1 and m represents an integer of 1 to 5.
Claim 3
Dependent Claim
47 words
Antitumor protein hybrid according to claim 1, which is expressed by the following formula (II): Fab--S.sub.1 --S.sub.2 --FA).sub.p (II) where the definitions of Fab, FA, S 1 and S 2 are the same as those given in case of formula (I) and p represents 1 or 2.
Claim 4
Dependent Claim
24 words
Antitumor protein hybrid according to claim 1 or claim 2, wherein FA is a moiety derived from the fragment A of a diphtheria toxin.
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 anti-α-fetoprotein antibody.
Claim 6
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 anti-α-fetoprotein antibody.
Claim 7
Dependent Claim
35 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): ##STR4## where Y indicates a divalent organic radical.
Claim 8
Dependent Claim
55 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): ##STR5## where Z indicates a divalent organic radical, and X 1 and X 2 are either the same or different from each other and represent bromine or iodine.
Claim 9
Dependent Claim
52 words
Antitumor protein hybrid according to claim 1, wherein X is a divalent organic radical arising from a dihaloketone compound which is expressed by the following formula (V): X.sub.1 --CH.sub.2 --CO--CH.sub.2 --X.sub.2 (V) where X 1 and X 2 are either the same or different from each other and represent bromine or iodine.
Claim 10
Dependent Claim
43 words
Antitumor protein hybrid according to claim 1, wherein X is a divalent organic radical arising from a halocarbonyl maleimide compound which is expressed by the following formula (VI): ##STR6## where W is a divalent organic radical and X 1 represents bromine or iodine.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-11-01 | 1986-05-03 | 1986-11-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-11-01 | 1990-05-03 | 1990-11-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-11-01 | 1994-05-03 | 1994-11-02 | $7700.00 | Window Closed / Lapsed |