Compounds, compositions, and methods for cancer imaging and therapy
First Claim
Patent Images
1. A compound, for use in radioimaging and radiotherapy, of the formula K1 ##STR36## wherein R1 and R2 are H or Me;
- R3 is H, lower alkyl, lower alkylene, cycloalkyenyl, aryl, or arylalkane;
R4 and R5 are independently ##STR37## --CH2 --, or ##STR38## R6 is --(CH2)j --CZ--NR10 --(CH2)m --R9 ;
##STR39## or hydrogen;
R7 is ##STR40## --CH2 --, or ##STR41## R8 is --SH, or ##STR42## R9 and R15 are --N(R10)2 or a 5 to 7 membered heterocyclic ring, containing nitrogen, oxygen, or sulfur, the ring being unsubstituted or optionally substituted wi least one alkyl or arylalkyl substitutent, said heterocyclic ring containing 2-6 ring ca atoms and 1-3 ring heteroatoms;
R10 and R14 are independently lower alkyl or hydrogen;
R11 is hydrogen or methyl;
Z is oxygen or 2 hydrogen atoms;
m is an integer from 0 to 6;
n is an integer from 1 to 6;
and j is an integer from 0 to 6;
whereinif R6 is hydrogen, then R8 is not --SH; and
if R9 is --N(R10)2 or said 5 to 7 membered heterocyclic ring is linked to the --(CH2)m-- moiety by a heteroatom, then m is not 0.
1 Assignment
0 Petitions
Accused Products
Abstract
Disclosed are bisaminothiol and amino compounds with appended pharmacophores, complexes of these compounds with 99m Tc(V)0, Re(V)0, In+3, 67 Ga+3, 90 Y+3, 109 Pd+2 or 105 Rh+3, and pharmaceutical compositions containing the complexes. Also disclosed are methods of diagnosing a mammal for the presence of a mammalian tumor, methods for in vitro detection of a cancer cell in a mammalian tissue sample, and methods of treating a mammal having a tumor.
30 Citations
45 Claims
-
1. A compound, for use in radioimaging and radiotherapy, of the formula K1 ##STR36## wherein R1 and R2 are H or Me;
-
R3 is H, lower alkyl, lower alkylene, cycloalkyenyl, aryl, or arylalkane; R4 and R5 are independently ##STR37## --CH2 --, or ##STR38## R6 is --(CH2)j --CZ--NR10 --(CH2)m --R9 ;
##STR39## or hydrogen;
R7 is ##STR40## --CH2 --, or ##STR41## R8 is --SH, or ##STR42## R9 and R15 are --N(R10)2 or a 5 to 7 membered heterocyclic ring, containing nitrogen, oxygen, or sulfur, the ring being unsubstituted or optionally substituted wi least one alkyl or arylalkyl substitutent, said heterocyclic ring containing 2-6 ring ca atoms and 1-3 ring heteroatoms;R10 and R14 are independently lower alkyl or hydrogen; R11 is hydrogen or methyl; Z is oxygen or 2 hydrogen atoms; m is an integer from 0 to 6; n is an integer from 1 to 6; and j is an integer from 0 to 6; wherein if R6 is hydrogen, then R8 is not --SH; and if R9 is --N(R10)2 or said 5 to 7 membered heterocyclic ring is linked to the --(CH2)m-- moiety by a heteroatom, then m is not 0. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43)
-
-
44. A compound for use in radioimaging and radiotherapy, wherein said compound is:
- ##STR51##
-
45. A compound for use in radioimaging and radiotherapy, wherein said compound is:
Specification