US6072038A
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Conjugates of texaphyrins
Assignee: Pharmacyclics LLC
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Filing: 1998-06-25
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Granted: 2000-06-06
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Expires: 2018-06-25
Abstract
Abstract The invention relates to the field of radiation sensitizers and the use of texaphyrins for radiation sensitization and other conditions for which X-ray radiation has proven to be therapeutic.
Inventors
- 👤 Jonathan L. Sessler
- 👤 Tarak D. Mody
- 👤 Gregory W. Hemmi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 15:00
CPC Classifications
A; A61; A61K; A61K41/00; A61K41/0038; A61K41/0057; A61K41/0076; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/545; A61K47/546; A61K49/00; A61K49/001; A61K49/0013; A61K49/0017; A61K49/0019; A61K49/0021; A61K49/005; A61K49/0054; A61K49/0058; A61K49/06; A61K49/08; A61K49/085; A61K49/10; A61K49/101; A61K49/106; A61K49/12; A61K49/126; A61K51/00; A61K51/02; A61K51/04; A61K51/0474; A61K51/0485; A61L; A61L2/00; A61L2/02; B; B01; B01J; B01J31/00; B01J31/16; B01J31/165; B01J31/1658; B01J31/18; B01J31/1805; B01J31/181; B01J31/1815; C; C07; C07D; C07D487/00; C07D487/22; C07H; C07H21/00; A61L2103/00; A61L2103/05; B01J2531/00; B01J2531/02; B01J2531/0238; B01J2531/0241; B01J2531/025; B01J2531/20; B01J2531/23; B01J2531/26; B01J2531/27; B01J2531/28; B01J2531/30; B01J2531/36; B01J2531/37; B01J2531/38; B01J2531/70; B01J2531/72; B01J2531/80; B01J2531/84; B01J2531/842; B01J2531/845; B01J2531/847; B01J2531/90; B01J2531/96; B01J31/02; B01J31/06; B01J31/061
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
8 words
A texaphyrin-biomolecule conjugate, wherein the texaphyrin is hydroxylated.
Claim 2
Dependent Claim
8 words
A texaphyrin-biomolecule conjugate, wherein the texaphyrin is hydroxylated.
Claim 3
Dependent Claim
8 words
A texaphyrin-biomolecule conjugate, wherein the texaphyrin is water-soluble.
Claim 4
Dependent Claim
8 words
A texaphyrin-biomolecule conjugate, wherein the texaphyrin is water-soluble.
Claim 5
Dependent Claim
139 words
A texaphyrin-biomolecule conjugate wherein the texaphyrin is represented by the following structure: ##STR7## where, M is a divalent metal cation or a trivalent metal cation; R 1 -R 4 , R 7 and R 8 are independently hydrogen, hydroxyl, alkyl, aryl, hydroxyalkyl, oxyalkyl, oxyhydroxyalkyl, saccharide, carboxyalkyl, carboxyamidealkyl, a biomolecule, or a couple to a biomolecule; where at least one of R 1 , R 7 and R 8 is oxyhydroxyalkyl, saccharide, oxyalkyl, carboxyalkyl, carboxyamidealkyl, or hydroxyalkyl having at least one hydroxy substituent, and provided that R 7 is the same as R 8 ; R 5 , R 6 , R 9 and R 10 are hydrogen; and N is zero, 1 or 2; provided that, at least one of R 1 -R 4 , R 7 and R 8 is a biomolecule or a couple to a biomolecule.
Claim 6
Dependent Claim
139 words
A texaphyrin-biomolecule conjugate wherein the texaphyrin is represented by the following structure: ##STR7## where, M is a divalent metal cation or a trivalent metal cation; R 1 -R 4 , R 7 and R 8 are independently hydrogen, hydroxyl, alkyl, aryl, hydroxyalkyl, oxyalkyl, oxyhydroxyalkyl, saccharide, carboxyalkyl, carboxyamidealkyl, a biomolecule, or a couple to a biomolecule; where at least one of R 1 , R 7 and R 8 is oxyhydroxyalkyl, saccharide, oxyalkyl, carboxyalkyl, carboxyamidealkyl, or hydroxyalkyl having at least one hydroxy substituent, and provided that R 7 is the same as R 8 ; R 5 , R 6 , R 9 and R 10 are hydrogen; and N is zero, 1 or 2; provided that, at least one of R 1 -R 4 , R 7 and R 8 is a biomolecule or a couple to a biomolecule.
Claim 7
Dependent Claim
66 words
The conjugate of claim 3 where the metal cation is a divalent metal cation selected from the group consisting of Ca(II), Mn(II), Co(II), Ni(II), Zn(II), Cd(II), Hg(II), Fe(II), Sm(II) and UO 2 (II), or a trivalent metal cation selected from the group consisting of Mn(III), Co(III), Ni(III), Fe(III), Ho(III), Ce(III), Y(III), In(III), Pr(III), Nd)III), Sm(III), Eu(III), Gd(III), Tb(III), Dy(III), Er(III), Tm(III), Yb(III), Lu(III), La(III), and U(III).
Claim 8
Dependent Claim
11 words
The conjugate of claim 1 where the biomolecule is an antibody.
Claim 9
Dependent Claim
11 words
The conjugate of claim 2 where the biomolecule is an antibody.
Claim 10
Dependent Claim
11 words
The conjugate of claim 3 where the biomolecule is an antibody.
Claim 11
Dependent Claim
25 words
The conjugate of claim 3 where R 1 is alkyl or hydroxyalkyl, and each of R 2 , R 3 and R 4 is alkyl.
Claim 12
Dependent Claim
41 words
The conjugate of claim 3 where R 1 is CH 2 CH 3 or CH 2 CH 2 CH 2 OH, each of R 2 and R 3 is CH 2 CH 3 , and R 4 is CH 3 .
Claim 13
Dependent Claim
14 words
The conjugate of claim 3 where R 7 and R 8 are the same.
Claim 14
Dependent Claim
28 words
The conjugate of claim 3 where R 7 is OCH 2 CH 2 CH 2 OH and R 8 is a biomolecule or a couple to a biomolecule.
Claim 15
Dependent Claim
33 words
The conjugate of claim 3 where R 7 is O(CH 2 CH 2 O) 2 CH 2 CH 2 OCH 3 and R 8 is a biomolecule or a couple to a biomolecule.
Claim 16
Dependent Claim
12 words
The conjugate of claim 3 where M is a lanthanide metal cation.
Claim 17
Dependent Claim
102 words
The conjugate of claim 3 where R 1 is CH 2 CH 3 or CH 2 CH 2 CH 2 OH; each of R 2 and R 3 is CH 2 CH 3 ; R 4 is CH 3 ; each of R 5 , R 6 , R 9 and R 10 is H; R 7 is H, CH 3 , OCH 3 , O(CH 2 ) n COOH, OCH 2 CH 2 CH 2 OH or O(CH 2 CH 2 O) n CH 3 where n is 1-7; and R 8 is a biomolecule or a couple to a biomolecule.
Claim 18
Dependent Claim
108 words
The conjugate of claim 3 where M is a lanthanide metal cation; R 1 is CH 2 CH 3 or CH 2 CH 2 CH 2 OH; each of R 2 and R 3 is CH 2 CH 3 ; R 4 is CH 3 ; each of R 5 , R 6 , R 9 and R 10 is H; R 7 is H, CH 3 , OCH 3 , O(CH 2 ) n COOH, OCH 2 CH 2 CH 2 OH or O(CH 2 CH 2 O) n CH 3 where n is 1-7; and R 8 is a biomolecule or a couple to a biomolecule.
Claim 19
Dependent Claim
79 words
The conjugate of claim 3 where M is a lanthanide metal cation; R 1 is CH 2 CH 3 or CH 2 CH 2 CH 2 OH; each of R 2 and R 3 is CH 2 CH 3 ; R 4 is CH 3 ; each of R 5 , R 6 , R 9 and R 10 is H; R 7 is OCH 2 COOH; and R 8 is a biomolecule or a couple to a biomolecule.
Claim 20
Dependent Claim
85 words
The conjugate of claim 3 where M is a lanthanide metal cation; R 1 is CH 2 CH 3 or CH 2 CH 2 CH 2 OH; each of R 2 and R 3 is CH 2 CH 3 ; R 4 is CH 3 ; each of R 5 , R 6 , R 9 and R 10 is H; R 7 is O(CH 2 CH 2 O) 3 CH 3 ; and R 8 is a biomolecule or a couple to a biomolecule.
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