US4845200A
Expired / Lapsed
US
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Immunoglobulin conjugates
Assignee: Lilly Industries Ltd
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Filing: 1986-06-23
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Granted: 1989-07-04
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Expires: 2006-06-23
Abstract
Abstract A conjugate comprising a vinca moiety convalently linked at the 4-position via a group of the formula --OCOXCO-- where X represents a single chemical bond or an optionally substituted C 1-10 chain, to an immunoglobulin or an immunoglobulin fragment. The conjugates are useful in the treatment of cancer.
Inventors
- 👤 George J. Cullinan
- 👤 George F. Rowland
- 👤 Robin G. Simmonds
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 18:08
CPC Classifications
A; A61; A61K; A61K39/00; A61K39/395; C; C07; C07D; C07D519/00; C07D519/04; A61K47/00; A61K47/50; A61K47/51; A61K47/68; A61K47/6801; A61K47/6803; A61K47/6805; Y; Y10; Y10S; Y10S530/00; Y10S530/827; Y10S530/828
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
142 words
A cytotoxic conjugate represented by the formula (V--COXCO--) n Ig wherein V is a vinca moiety of the formula ##STR4## and n is 1-20 and in which Ig represents an immunoglobulin with cellular-associated antigen recognizing properties and X is C 1-4 straight chain alkylene, C 2-8 branched alkylene, C 2-4 alkenylene, C 3-4 alkynylene, C 3-6 cycloalkylene, phenylene, hydroxy-substituted C 1-4 alkylene or a direct bond; and in which R 1 is COOCH 3 ; R 2 is H, CH 3 or CHO; and when R 4 and R 5 are taken singly, R 5 is H, and one of R 3 and R 4 is ethyl and the other is H or OH: and when R 4 and R 5 are taken together with the carbons to which they are attached, they form an oxirane ring, and R 3 is ethyl.
Claim 2
Dependent Claim
142 words
A cytotoxic conjugate represented by the formula (V--COXCO--) n Ig wherein V is a vinca moiety of the formula ##STR4## and n is 1-20 and in which Ig represents an immunoglobulin with cellular-associated antigen recognizing properties and X is C 1-4 straight chain alkylene, C 2-8 branched alkylene, C 2-4 alkenylene, C 3-4 alkynylene, C 3-6 cycloalkylene, phenylene, hydroxy-substituted C 1-4 alkylene or a direct bond; and in which R 1 is COOCH 3 ; R 2 is H, CH 3 or CHO; and when R 4 and R 5 are taken singly, R 5 is H, and one of R 3 and R 4 is ethyl and the other is H or OH: and when R 4 and R 5 are taken together with the carbons to which they are attached, they form an oxirane ring, and R 3 is ethyl.
Claim 3
Dependent Claim
22 words
A conjugate according to claim 1 in which the immunoglobulin is derived from an antibody to human or animal tumour associated antigens.
Claim 4
Dependent Claim
13 words
A conjugate according to claim 2 which is derived from a monoclonal antibody.
Claim 5
Dependent Claim
49 words
A conjugate according to claim 1 in which R 1 is COOMe, R 2 is methyl or formyl, R 3 is hydroxy, R 4 is ethyl, R 5 is hydrogen, X is C 1-4 alkylene and Ig is a monoclonal antibody to a human or animal tumor associated antigen.
Claim 6
Dependent Claim
13 words
A conjugate according to claim 4 which comprises 3 to 14 vinca residues.
Claim 7
Dependent Claim
14 words
A conjugate according to claim 1 wherein the vinca moiety is derived from 4-desacetylvinblastine.
Claim 8
Dependent Claim
14 words
A conjugate according to claim 1 wherein the vinca moiety is derived from vindesine.
Claim 9
Dependent Claim
14 words
A conjugate according to claim 1 wherein the vinca moiety is derived from 4-desacetylvincristine.
Claim 10
Dependent Claim
14 words
A conjugate according to claim 1 wherein the vinca moiety is derived from 4'-epideoxy-4-desacetylvinblastine.
Claim 11
Dependent Claim
22 words
A conjugate according to claim 6 wherein X is --CH 2 CH 2 -- or --CH 2 CH 2 CH 2 --.
Claim 12
Dependent Claim
22 words
A conjugate according to claim 7 wherein X is --CH 2 CH 2 -- or --CH 2 CH 2 CH 2 --.
Claim 13
Dependent Claim
22 words
A conjugate according to claim 8 wherein X is --CH 2 CH 2 -- or --CH 2 CH 2 CH 2 --.
Claim 14
Dependent Claim
22 words
A conjugate according to claim 9 wherein X is --CH 2 CH 2 -- or --CH 2 CH 2 CH 2 --.
Claim 15
Dependent Claim
20 words
A conjugate according to claim 10 wherein the immunoglobulin is adapted for recognition of human or animal colorectal carcinoma cells.
Claim 16
Dependent Claim
19 words
A conjugate according to claim 10 wherein the immunoglobulin is adapted for recognition of human or animal osteosarcoma cells.
Claim 17
Dependent Claim
19 words
A conjugate according to claim 10 wherein the immunoglobulin is adapted for recognition of human or animal carcinoembryonic cells.
Claim 18
Dependent Claim
20 words
A conjugate according to claim 10 wherein the immunoglobulin is adapted for recognition of human or animal lung adenocarcinoma cells.
References Cited (Backward Citations)
US4507234A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-07-03 | 1993-01-02 | 1993-07-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-07-03 | 1997-01-02 | 1997-07-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-07-03 | 2001-01-02 | 2001-07-04 | $7700.00 | Window Closed / Lapsed |