US5556982A
Expired / Lapsed
US
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Metal radionuclide labeled proteins for diagnosis and therapy
Assignee: Poniard Pharmaceuticals Inc
•
Filing: 1993-07-12
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Granted: 1996-09-17
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Expires: 2013-07-12
Abstract
Abstract Protein, ligand and anti-ligand conjugated chelated metal radionuclides are provided for use in vivo. Intermediates are provided for preparing the compositions efficiently.
Inventors
- 👤 Alan R. Fritzberg
- 👤 Sudhakar Kasina
- 👤 Linda M. Gustavson
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 09:13
CPC Classifications
C; C07; C07D; C07D285/00; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/68; A61K47/6891; A61K47/6897; A61K47/6898; A61K51/00; A61K51/02; A61K51/04; A61K51/0474; A61K51/0478; A61K51/0495; A61K51/0497; A61K51/08; A61K51/10; A61K51/1045; A61K51/1048; A61K51/1066; A61K51/1093; A61K51/12; B; B82; B82Y; B82Y5/00; C07B; C07B59/00; C07B59/004; C07B59/008; C07C; C07C227/00; C07C227/04; C07C227/06; C07C227/08; C07C271/00; C07C271/06; C07C271/08; C07C271/10; C07C271/22; C07C323/00; C07C323/50; C07C323/51; C07C323/60; C07D495/00; C07D495/02; C07D495/04; C07F; C07F13/00; C07F13/005; C07K; C07K14/00; C07K14/195; C07K14/36; C07K14/435; C07K14/46; C07K14/465; A61K2123/00
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
144 words
A compound of the formula: ##STR40## wherein: one of Z 1 , Z 2 , Z 3 , or Z 4 , is (CH 2 ) m --X'--{CO--NH--(CH 2 ) m ,} n --CWY and the others are H 2 or ═O, wherein in (CH 2 ) m and (CH 2 ) m , m ranges from 1 to 6 and m' ranges from 1 to 3 and m+m' ranges from 1 to 6; W is H 2 or ═NH or ═O; n is 0 or 1; T is a removable sulfur protective group, hydrogen, or an alkali metal ion; Y is biotin, avidin, or strept-avidin; X is a bond, methylene or CHZ 4 ; X' is a bond, oxygen or sulfur; and the A's are the same or different and are hydrogen or a lower alkyl of from 1 to 3 carbon atoms.
Claim 2
Dependent Claim
144 words
A compound of the formula: ##STR40## wherein: one of Z 1 , Z 2 , Z 3 , or Z 4 , is (CH 2 ) m --X'--{CO--NH--(CH 2 ) m ,} n --CWY and the others are H 2 or ═O, wherein in (CH 2 ) m and (CH 2 ) m , m ranges from 1 to 6 and m' ranges from 1 to 3 and m+m' ranges from 1 to 6; W is H 2 or ═NH or ═O; n is 0 or 1; T is a removable sulfur protective group, hydrogen, or an alkali metal ion; Y is biotin, avidin, or strept-avidin; X is a bond, methylene or CHZ 4 ; X' is a bond, oxygen or sulfur; and the A's are the same or different and are hydrogen or a lower alkyl of from 1 to 3 carbon atoms.
Claim 3
Dependent Claim
11 words
A compound according to claim 1 wherein X is a bond.
Claim 4
Dependent Claim
10 words
A compound according to claim 1 wherein Y comprises biotin.
Claim 5
Dependent Claim
38 words
A compound according to claim 1 wherein X is a bond, Z 3 is ═O, and one of Z 1 or Z 2 is --(CH 2 ) 2 --CO--Y and the other is ═O or H 2 .
Claim 6
Dependent Claim
13 words
A compound of claim 1 wherein X' is oxygen and Y is biotin.
Claim 7
Dependent Claim
78 words
A compound of claim 1 of the formula: ##STR41## wherein: each T, when taken together with the sulfur atom to be protected, defines a hemithioacetal sulfur protective group of the formula: ##STR42## wherein R 3 represents a lower alkyl group of from two to five carbon atoms, R 4 represents a lower alkyl group of from one to three carbon atoms, and R 5 represents hydrogen or a lower alkyl group of from one to three carbon atoms.
Claim 8
Dependent Claim
155 words
A compound of the formula: ##STR43## wherein: one of Z 1 , Z 2 , Z 3 , or Z 4 , is (CH 2 ) n --CWY, wherein n ranges from 1 to 6, and the others are H 2 or ═O; W is H 2 or ═NH or ═O; Y is biotin, avidin or strept-avidin; X is a bond, methylene or CHZ 4 ; the A's are the same or different and are hydrogen or lower alkyl of from 1 to 3 carbon atoms; and each T, when taken together with the sulfur atom to be protected, defines a hemithioacetal sulfur protective group of the formula: ##STR44## wherein R 3 represents a lower alkyl group of from two to five carbon atoms, R 4 represents a lower alkyl group of from one to three carbon atoms, and R 5 represents hydrogen or a lower alkyl group of from one to three carbon atoms.
Claim 9
Dependent Claim
155 words
A compound of the formula: ##STR43## wherein: one of Z 1 , Z 2 , Z 3 , or Z 4 , is (CH 2 ) n --CWY, wherein n ranges from 1 to 6, and the others are H 2 or ═O; W is H 2 or ═NH or ═O; Y is biotin, avidin or strept-avidin; X is a bond, methylene or CHZ 4 ; the A's are the same or different and are hydrogen or lower alkyl of from 1 to 3 carbon atoms; and each T, when taken together with the sulfur atom to be protected, defines a hemithioacetal sulfur protective group of the formula: ##STR44## wherein R 3 represents a lower alkyl group of from two to five carbon atoms, R 4 represents a lower alkyl group of from one to three carbon atoms, and R 5 represents hydrogen or a lower alkyl group of from one to three carbon atoms.
Claim 10
Dependent Claim
15 words
A compound of claim 7 wherein said hemithioacetal sulfur protective group is an ethoxyethyl group.
Claim 11
Dependent Claim
9 words
A compound of claim 6 wherein Y is biotin.
Claim 12
Dependent Claim
15 words
A compound of claim 9 wherein said hemithioacetal sulfur protective group is an ethoxyethyl group.
Claim 13
Dependent Claim
153 words
A compound of the formula: ##STR45## wherein: one of Z 1 , Z 2 , Z 3 , or Z 4 , is (CH 2 ) n --CWY, wherein n ranges from 1 to 3, and the others are H 2 or ═O; W is ═NH or ═O; Y is biotin, avidin or streptavidin; X is a bond, methylene or CHZ 4 ; the A's are the same or different and are hydrogen or noncyclic lower alkyl of from 1 to 3 carbon atoms; and each T, when taken together with the sulfur atom to be protected, defines a hemithioacetal sulfur protective group of the formula: ##STR46## wherein R 3 represents a lower alkyl group of from two to five carbon atoms, R 4 represents a lower alkyl group of from one to three carbon atoms, and R 5 represents hydrogen or a lower alkyl group of from one to three carbon atoms.
Claim 14
Dependent Claim
153 words
A compound of the formula: ##STR45## wherein: one of Z 1 , Z 2 , Z 3 , or Z 4 , is (CH 2 ) n --CWY, wherein n ranges from 1 to 3, and the others are H 2 or ═O; W is ═NH or ═O; Y is biotin, avidin or streptavidin; X is a bond, methylene or CHZ 4 ; the A's are the same or different and are hydrogen or noncyclic lower alkyl of from 1 to 3 carbon atoms; and each T, when taken together with the sulfur atom to be protected, defines a hemithioacetal sulfur protective group of the formula: ##STR46## wherein R 3 represents a lower alkyl group of from two to five carbon atoms, R 4 represents a lower alkyl group of from one to three carbon atoms, and R 5 represents hydrogen or a lower alkyl group of from one to three carbon atoms.
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