Radioimaging applications of and novel formulations of teboroxime
First Claim
Patent Images
1. A method for cardiac imaging, comprising:
- administering to an adult human subject an amount of a 99mTc-containing species having a radioactivity of less than 5 mCi at a time of administration; and
performing a SPECT imaging procedure of a cardiac region of interest (ROI) of the subject, wherein said 99mTc-containing species has the formula 99mTcX(Y)3Z, wherein;
X is an anion;
each Y, which is independently chosen, is a vicinal dioxime having the formula HON═
C(R1)C(R2)═
NOH or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen, halogen, alkyl, aryl, amino or a 5 or 6-membered nitrogen or oxygen containing heterocycle, or together R1 and R2 are —
(CR8CR9)n—
wherein n is 3, 4, 5 or 6 and R8 and R9 are each independently hydrogen or alkyl; and
Z is a boron derivative of the formula B—
R3 wherein R3 is hydroxy, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, carboxyalkyl, carboxyalkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, alkoxyalkenyl, haloalkyl, haloalkenyl, aryl, arylalkyl or (R4R5N)-alkyl and R4 and R5 are each independently hydrogen, alkyl, or arylalkyl, or R4 and R5 when taken together with the nitrogen atom to which they are attached form a 5 or 6-membered nitrogen containing heterocycle.
4 Assignments
0 Petitions
Accused Products
Abstract
A method for cardiac imaging is provided, including administering to an adult human subject an amount of a teboroxime species having a radioactivity of less than 5 mCi at a time of administration, and performing a SPECT imaging procedure of a cardiac region of interest (ROI) of the subject. Other embodiments are also described.
745 Citations
59 Claims
-
1. A method for cardiac imaging, comprising:
-
administering to an adult human subject an amount of a 99mTc-containing species having a radioactivity of less than 5 mCi at a time of administration; and performing a SPECT imaging procedure of a cardiac region of interest (ROI) of the subject, wherein said 99mTc-containing species has the formula 99mTcX(Y)3Z, wherein; X is an anion; each Y, which is independently chosen, is a vicinal dioxime having the formula HON═
C(R1)C(R2)═
NOH or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen, halogen, alkyl, aryl, amino or a 5 or 6-membered nitrogen or oxygen containing heterocycle, or together R1 and R2 are —
(CR8CR9)n—
wherein n is 3, 4, 5 or 6 and R8 and R9 are each independently hydrogen or alkyl; andZ is a boron derivative of the formula B—
R3wherein R3 is hydroxy, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, carboxyalkyl, carboxyalkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, alkoxyalkenyl, haloalkyl, haloalkenyl, aryl, arylalkyl or (R4R5N)-alkyl and R4 and R5 are each independently hydrogen, alkyl, or arylalkyl, or R4 and R5 when taken together with the nitrogen atom to which they are attached form a 5 or 6-membered nitrogen containing heterocycle. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
-
-
16. Apparatus for performing cardiac imaging, comprising an imaging system, which comprises:
-
SPECT imaging functionality; and a control unit configured to drive the imaging functionality to perform a SPECT imaging procedure on a cardiac region of interest (ROI) of an adult human subject after administration to the subject of a 99mTc-containing species having a radioactivity of less than 5 mCi at a time of administration, wherein said 99mTc-containing species has the formula 99mTcX(Y)3Z, wherein; X is an anion; each Y, which is independently chosen, is a vicinal dioxime having the formula HON═
C(R1)(R2)═
NOH or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen, halogen, alkyl, aryl, amino or a 5 or 6-membered, nitrogen or oxygen containing heterocycle, or together R1 and R2 are —
(CR8CR9)n—
wherein n is 3, 4, 5 or 6 and R8 and R9 are each independently hydrogen or alkyl; andZ is a boron derivative of the formula B—
R3wherein R3 is hydroxy, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, carboxyalkyl, carhoxyalkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, alkoxyalkenyl, haloalkyl, haloalkenyl, aryl, arylalkyl or (R4R5N)-alkyl and R4 and R5 are each independently hydrogen, alkyl, or arylalkyl, or R4 and R5 when taken together with the nitrogen atom to which they are attached form a 5 or 6-membered nitrogen containing heterocycle, wherein the SPECT imaging functionality is configured to generate an image having a resolution of at least 7×
7×
7 mm. - View Dependent Claims (17, 18, 19, 20, 21)
-
-
22. Apparatus for cardiac imaging, comprising a portable computer-communicatable non-transitory data carrier, which is configured to contain imaging protocol information for performing SPECT imaging on an adult human subject, the protocol information including an indication to administer a 99mTc-containing species of the formula 99mTcX(Y)3Z, and an indication to perform a SPECT imaging procedure on the subject, which procedure includes an image acquisition period having a duration not exceeding 5 minutes, wherein:
-
X is an anion; each Y, which is independently chosen, is a vicinal dioxime having the formula HON═
C(R1)C(R2)═
NOH or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen, halogen, alkyl, aryl, amino or a 5 or 6-membered nitrogen or oxygen containing heterocycle, or together R1 and R2 are —
(CR8CR9)n—
wherein n is 3, 4, 5 or 6 and R8 and R9 are each independently hydrogen or alkyl; andZ is a boron derivative of the formula B—
R3wherein R3 is hydroxy, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, carboxyalkyl, carboxyalkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, alkoxyalkenyl, haloalkyl, haloalkenyl, aryl, arylalkyl or (R4R5N)-alkyl and R4 and R3 are each independently hydrogen, alkyl, or arylalkyl, or R4 and R5 when taken together with the nitrogen atom to which they are attached form a 5 or 6-membered nitrogen containing heterocycle. - View Dependent Claims (23, 24, 25)
-
-
26. A method for cardiac imaging, comprising:
-
administering to an adult human subject a 99mTc-containing species having a radioactivity of less than 50 mCi at a time of the administering; and performing a SPECT imaging procedure on a cardiac region of interest (ROI) of the subject with a image acquisition period having a duration not exceeding 5 minutes, wherein said 99mTc-containing species has the formula 99mTcX(Y)3Z, wherein; X is an anion; each Y, which is independently chosen, is a vicinal dioxime having the formula HON═
C(R1)C(R2)═
NOH or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen, halogen, alkyl, aryl, amino or a 5 or 6-membered nitrogen or oxygen containing heterocycle, or together R1 and R2 are —
(CR8CR9)n—
wherein n is 3, 4, 5 or 6 and R8 and R9 are each independently hydrogen or alkyl; andZ is a boron derivative of the formula B—
R3wherein R3 is hydroxy, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, carboxyalkyl, carboxyalkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, alkoxyalkenyl, haloalkyl, haloalkenyl, aryl, arylalkyl or (R4R5N)-alkyl and R4 and R5 are each independently hydrogen, alkyl, or arylalkyl, or R4 and R5 when taken together with the nitrogen atom to which they are attached form a 5 or 6-membered nitrogen containing heterocycle. - View Dependent Claims (27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50)
-
-
51. Apparatus for performing cardiac imaging, comprising an imaging system, which comprises:
-
SPECT imaging functionality; and a control unit configured to drive, the imaging functionality to perform a SPECT imaging procedure on a cardiac region of interest (ROD of an adult human subject after administration to the subject of a 99mTc-containing species having a radioactivity of less than 50 mCi at a time of the administration, wherein the imaging procedure has a image acquisition period having a duration not exceeding 5 minutes, and wherein said 99mTc-containing species has the formula 99mTcX(Y)3Z, wherein; X is an anion; each Y, which is independently chosen, is a vicinal dioxime having the formula HON═
C(R1)C(R2)═
NOH or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen, halogen, alkyl, aryl, amino or a 5 or 6-membered nitrogen or oxygen containing heterocycle, or together R1 and R2 are —
(CR8CR9)n—
wherein n is 3, 4, 5 or 6 and R8 and R9 are each independently hydrogen or alkyl; andZ is a boron derivative of the formula B—
R3wherein R3 is hydroxy, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, carboxyalkyl, carboxyalkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, alkoxyalkenyl, haloalkyl, haloalkenyl, aryl, arylalkyl or (R4R5N)-alkyl and R4 and R5 are each independently hydrogen, alkyl, or arylalkyl, or R4 and R5 when taken together with the nitrogen atom to which they are attached form a 5 or 6-membered nitrogen containing heterocycle, wherein the SPECT imaging functionality is configured to generate an image having a resolution of at least 7×
7×
7 mm. - View Dependent Claims (52, 53, 54, 55, 56)
-
-
57. A method for cardiac imaging, comprising:
-
subjecting an adult human subject to stress; during the stress, administering to the subject a 99mTc-containing species having a radioactivity of between 20 and 40 mCi at a time of the administering; and performing a SPECT stress imaging procedure on a cardiac region of interest (ROI) of the subject, with an image acquisition period having a duration not exceeding 5 minutes; and during the stress image acquisition period, acquiring a number of photons greater than or equal to at least one of the following numbers; one in 5000 photons emitted from the ROI during the stress image acquisition period, and 200,000 photons emitted from a portion of the ROI, which portion has a volume of no more than 500 cc, wherein said 99mTc-containing species has the formula 99mTcX(Y)3Z, wherein; X is an anion; each Y, which is independently chosen, is a vicinal dioxime having the formula HON═
C(R1)C(R2)═
NOH or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen, halogen, alkyl, aryl, amino or a 5 or 6-membered nitrogen or oxygen containing heterocycle, or together R1 and R2 are —
(CR8CR9)n—
wherein n is 3, 4, 5 or 6 and R5 and R9 are each independently hydrogen or alkyl; andZ is a boron derivative of the formula B—
R3wherein R3 is hydroxy, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, carboxyalkyl, carboxyalkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, alkoxyalkenyl, haloalkyl, haloalkenyl, aryl, arylalkyl or (R4R5N)-alkyl and R4 and R5 are each independently hydrogen, alkyl, or arylalkyl, or R4 and R5 when taken together with the nitrogen atom to which they are attached form a 5 or 6-membered nitrogen containing heterocycle. - View Dependent Claims (58, 59)
-
Specification