Compositions and methods for cellular imaging and therapy
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-051/00
A61B-005/055
출원번호
US-0737694
(2007-04-19)
등록번호
US-8758723
(2014-06-24)
발명자
/ 주소
Yang, David J.
Oh, Chang-Sok
Yu, Dong-Fang
Azhdarinia, Ali
Kohanim, Saady
출원인 / 주소
The Board of Regents of the University of Texas System
대리인 / 주소
Parker Highlander PLLC
인용정보
피인용 횟수 :
2인용 특허 :
100
초록
The present invention relates generally to the fields of chemistry and radionuclide imaging. More particularly, it concerns compositions, kits and methods for imaging and therapy involving N4 compounds and derivatives.
대표청구항▼
1. A compound of formula (I): wherein A1, A2, A3, and A4 are each independently —(CH2)x —, wherein x=2-4; andR1, R2, R3, R4 are each independently H, alkyl, substituted alkyl, -alkyl-COOH, a protecting group, a targeting ligand that targets an amino acid transporter, or a linker-targeting ligand tha
1. A compound of formula (I): wherein A1, A2, A3, and A4 are each independently —(CH2)x —, wherein x=2-4; andR1, R2, R3, R4 are each independently H, alkyl, substituted alkyl, -alkyl-COOH, a protecting group, a targeting ligand that targets an amino acid transporter, or a linker-targeting ligand that targets an amino acid transporter, provided that R1, R2, R3, and R4 are not all H, not all the same alkyl radical, or not all —CH2COOH; wherein if A1=—(CH2)2— and A3=—(CH2)2—, and either A2 and A4=—(CH2)2—, or A2 and A4=—(CH2)3—, then at least one of R1, R2, R3, and R4 is a targeting ligand that targets an amino acid transporter further wherein the targeting ligand is an amino acid or an amino acid derivative. 2. The compound of claim 1, wherein R1, R2, R3 and/or R4 is a linker-targeting ligand. 3. The compound of claim 2, wherein the linker is selected from the group consisting of a peptide, glutamic acid, aspartic acid, bromo ethylacetate, ethylene diamine, lysine and any combination of one or more of these groups. 4. The compound of claim 1, wherein at least one of R1, R2, R3, and R4 is a targeting ligand. 5. The compound of claim 4, wherein A1=—(CH2)2—, A2=—(CH2)3—, A3=—(CH2)2—, and A4=—(CH2)3—, and at least one of R1, R2, R3, and R4 is a targeting ligand. 6. The compound of claim 4, wherein A1=—(CH2)2—, A2=—(CH2)2—, A3=—(CH2)2—, and A4=—(CH2)2—, and at least one of R1, R2, R3, and R4 is a targeting ligand. 7. The compound of claim 1, wherein A1=—(CH2)2—, A3=—(CH2)2—, A2=—(CH2)3—, and A4=—(CH2)3—, and at least one of R1, R2, R3, and R4 is a protecting group. 8. The compound of claim 7, wherein the protecting group is ethyl trifluoroacetate. 9. The compound of claim 1, wherein A1=—(CH2)2—, A2=—(CH2)2—, A3=—(CH2)2—, and A4=—(CH2)2—, and at least one of R1, R2, R3, and R4 is a protecting group. 10. The compound of claim 9, wherein the protecting group is ethyl trifluoroacetate. 11. The compound of claim 1, wherein A1=—(CH2)3—, A2=—(CH2)2—, A3=—(CH2)2—, and A4=—(CH2)2—. 12. The compound of claim 1, wherein A1=—(CH2)2—, A2=—(CH2)3—, A3=—(CH2)2—, and A4=—(CH2)3—. 13. The compound of claim 1, wherein A1=—(CH2)2—, A2=—(CH2)3—, A3=—(CH2)3—, and A4=—(CH2)3—. 14. The compound of claim 1, wherein A1=—(CH2)3—, A2=—(CH2)3—, A3=—(CH2)3—, and A4=—(CH2)3—. 15. The compound of claim 1, wherein A1=—(CH2)4—, A2=—(CH2)3—, A3=—(CH2)3—, and A4=—(CH2)3—. 16. The compound of claim 1, wherein A1=—(CH2)4—, A2=—(CH2)4—, A3=—(CH2)3—, and A4=—(CH2)3—. 17. The compound of claim 1, wherein A1=—(CH2)3—, A2=—(CH2)4—, A3=—(CH2)3—, and A4=—(CH2)4—. 18. The compound of claim 1, wherein A1=—(CH2)3—, A2=—(CH2)4—, A3=—(CH2)4—, and A4—(CH2)4—. 19. The compound of claim 1, wherein A1=—(CH2)4—, A2=—(CH2)4—, A3=—(CH2)4—, and A4=—(CH2)4—. 20. The compound of claim 1, wherein if A1=—(CH2)2—, A2=—(CH2)3—, and A3=—(CH2)2—, then A4 is not —(CH2)3—. 21. The compound of claim 1, wherein if A1=—(CH2)2—, A2=—(CH2)2—, and A3=—(CH2)2—, then A4 is not —(CH2)2. 22. The compound of claim 1, further defined as having the formula: wherein A1, A2, A3, and A4, are each independently —(CH2)x—, wherein x=2-4; and R1, R2, and R3 are each independently hydrogen, and R4 is chosen from the group consisting of: 23. The compound of claim 1, wherein the compound is chelated to a metal ion. 24. The compound of claim 23, wherein the metal ion is selected from the group consisting of a technetium ion, a copper ion, an indium ion, a thallium ion, a gallium ion, an arsenic ion, a rhenium ion, a holmium ion, a yttrium ion, a samarium ion, a selenium ion, a strontium ion, a gadolinium ion, a bismuth ion, an iron ion, a manganese ion, a lutecium ion, a cobalt ion, a platinum ion, a calcium ion and a rhodium ion. 25. The compound of claim 23, wherein the metal ion is selected from the group consisting of Tc-99m, Cu-60, Cu-61, Cu-62, Cu-64, Cu-67, In-111, Tl-201, Ga-67, Ga-68, As-72,Re-186, Re-187, Re-188, Ho-166, Y-90, Sm-153, Sr-89, Gd-157, Gd-183, Bi-212, Bi-213, Fe-56, Fe-59, Ac-225, At-211, Ti-45, Mn-55, Lu-177, an iron ion, a manganese ion, a cobalt ion, a platinum ion and a rhodium ion. 26. The compound of claim 23, wherein the metal ion is Re-187. 27. The compound of claim 23, wherein the metal ion is a radionuclide. 28. The compound of claim 27, wherein the radionuclide is selected from the group consisting of 99mTc, 188Re, 186Re, 153Sm, 166Ho, 90Y, 89Sr, 67Ga, 68Ga, 111In, 183Gd, 59Fe, 225Ac, 212Bi, 211At, 45Ti, 60Cu, 61Cu, 67Cu, and 64Cu. 29. The compound of claim 28, wherein the radionuclide is 99mTc. 30. The compound of claim 28, wherein the radionuclide is 188Re. 31. The compound of claim 23, wherein the metal ion is not radioactive. 32. A composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier. 33. The composition of claim 32, wherein the composition further comprises a metal ion chelated to the compound of claim 1. 34. The compound of claim 1, wherein the amino acid or amino acid derivative is serine, tryptophan, tyrosine or a tyrosine derivative. 35. The compound of claim 34, wherein the tyrosine derivative is α-β-tyrosine, tyrosine or α-methyltyrosine.
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이 특허에 인용된 특허 (100)
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