Bisaminoethanethiol-targeting ligand conjugates and compositions
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-051/00
A61M-036/14
출원번호
US-0563724
(2009-09-21)
등록번호
US-8236279
(2012-08-07)
발명자
/ 주소
Yang, David J.
Liu, Chun W.
Yu, Dong-Fang
Kim, E. Edmund
출원인 / 주소
Board of Regents, The University of Texas System
대리인 / 주소
Fulbright & Jaworski L.L.P.
인용정보
피인용 횟수 :
1인용 특허 :
102
초록▼
The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used
The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.
대표청구항▼
1. A bis-aminoethanethiol (BAT)-targeting ligand conjugate, wherein the targeting ligand is an agent that mimics glucose; a folate receptor targeting ligand; or a tumor hypoxia targeting ligand that is annexin V, colchicine, nitroimidazole, mitomycin, or metronidazole. 2. The conjugate of claim 1, w
1. A bis-aminoethanethiol (BAT)-targeting ligand conjugate, wherein the targeting ligand is an agent that mimics glucose; a folate receptor targeting ligand; or a tumor hypoxia targeting ligand that is annexin V, colchicine, nitroimidazole, mitomycin, or metronidazole. 2. The conjugate of claim 1, wherein the conjugate is further defined as an ethylenedicysteine-targeting ligand conjugate. 3. The conjugate of claim 1, wherein the targeting ligand is an agent that mimics glucose. 4. The conjugate of claim 3, wherein the agent that mimics glucose is glucosamine, deoxyglucose, neomycin, kanamycin, gentamicin, paromycin, amikacin, tobramycin, netilmicin, ribostamycin, sisomicin, micromicin, lividomycin, dibekacin, isepamicin, astromicin, or an aminoglycoside. 5. The conjugate of claim 4, wherein the agent that mimics glucose is glucosamine. 6. The conjugate of claim 5, wherein the conjugate is further defined as EC-glucosamine. 7. The conjugate of claim 4, wherein the agent that mimics glucose is deoxyglucose. 8. The conjugate of claim 7, wherein the conjugate is further defined as EC-deoxyglucose. 9. The conjugate of claim 1, wherein the targeting ligand is a folate receptor targeting ligand. 10. The conjugate of claim 1, wherein the targeting ligand is a tumor hypoxia targeting ligand that is annexin V, colchicine, nitroimidazole, mitomycin, or metronidazole. 11. The conjugate of claim 1, wherein the conjugate further comprises a linker between said BAT and said targeting ligand. 12. The conjugate of claim 11, wherein the linker is a water soluble peptide, glutamic acid, polyglutamic acid, aspartic acid, polyaspartic acid, bromoethylacetate, ethylenediamine or lysine. 13. The conjugate of claim 1, wherein the bis-aminoethanethiol (BAT)-targeting ligand conjugate is labeled with a metal ion. 14. The conjugate of claim 13, wherein the metal ion is a radionuclide. 15. The conjugate of claim 14, wherein the radionuclide is 99mTc, 188Re, 186Re, 183Sm, 166Ho, 90Y, 89Sr, 67Ga, 68Ga, 111In, 153Gd, 59Fe, 255Ac, 212Bi, 211At, 62Cu, or 64Cu. 16. The conjugate of claim 1, wherein the BAT comprises two carboxylic acid moieties. 17. The conjugate of claim 16, wherein a targeting ligand is conjugated to one of the carboxylic acid moieties of the BAT. 18. The conjugate of claim 16, wherein a first targeting ligand is conjugated to one of the carboxylic acid moieties of the BAT and a second targeting ligand is conjugated to another carboxylic acid moiety of the BAT.
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