US4440738A — Stable radiographic imaging agents

Claim 1

Independent Claim 123 words

A composition, useful in the preparation of technetium-99m-based imaging agents, comprising: (a) a pertechnetate reductant; and (b) an effective amount, no more than about 25%, by weight, of a reductate stabilizer selected from the group consisting of compounds and mixtures of compounds having the formula: ##STR12## wherein X is CRR' O, or NR', R' is hydrogen, or lower alkyl, Y is oxygen, sulfur, nitrogen, or CH 2 , R is hydrogen, lower alkyl, alkyl containing from 3 to 8 carbon atoms substituted with one or more hydroxy, halogen, amino, or thiol groups, alkyl containing from 1 to 8 carbon atoms halogen-substituted on the first and/or second carbon atom, lower alkenyl nicotinic acid and nicotinamide complexes thereof and pharmaceutically-acceptable salts, amides, and esters, thereof.

Claim 2

Dependent Claim 123 words

A composition, useful in the preparation of technetium-99m-based imaging agents, comprising: (a) a pertechnetate reductant; and (b) an effective amount, no more than about 25%, by weight, of a reductate stabilizer selected from the group consisting of compounds and mixtures of compounds having the formula: ##STR12## wherein X is CRR' O, or NR', R' is hydrogen, or lower alkyl, Y is oxygen, sulfur, nitrogen, or CH 2 , R is hydrogen, lower alkyl, alkyl containing from 3 to 8 carbon atoms substituted with one or more hydroxy, halogen, amino, or thiol groups, alkyl containing from 1 to 8 carbon atoms halogen-substituted on the first and/or second carbon atom, lower alkenyl nicotinic acid and nicotinamide complexes thereof and pharmaceutically-acceptable salts, amides, and esters, thereof.

Claim 3

Dependent Claim 30 words

A composition, as in claim 1, wherein said reductate stabilizer is selected from the group consisting of 6-bromo-6-deoxyascorbic acid, 6-chloro-6-deoxyascorbic acid, 6-iodo-6-deoxyascorbic acid, and the pharmaceutically-acceptable salts and mixtures thereof.

Claim 4

Dependent Claim 32 words

A composition, as in claim 1, wherein said reductate stabilizer is selected from the group consisting of reductic acid, 4-methylreductic, 5-methlyreductic acid, 4-ethylreductic acid, 5-ethylreductic acid, and pharmaceutically-acceptable salts and mixtures thereof.

Claim 5

Dependent Claim 39 words

A composition as in claim 1, wherein said reductate stabilizer is selected from the group consisting of the nicotinic acid and nicotinamide complexes of 6-bromo-6-deoxyascorbic acid, 6-chloro-6-deoxyascorbic acid, 6-iodo-6-deoxyascorbic acid, reductic acid, 5-methylreductic acid, 5-ethylreductic acid, and mixtures thereof.

Claim 6

Dependent Claim 17 words

A composition, as in claim 1, comprising no more than 10%, by weight, of said reductate stabilizer.

Claim 7

Dependent Claim 24 words

A composition, as in claim 1, wherein said pertechnetate reductant is selected from the group consisting of the soluble stannous, chromous and ferrous salts.

Claim 8

Dependent Claim 24 words

A composition, as in claim 6, wherein said pertechnetate reductant is selected from the group consisting of stannous chloride, chromous chloride and ferrous sulfate.

Claim 9

Dependent Claim 11 words

A composition, as in claim 1, further comprising an organ-specific carrier.

Claim 10

Dependent Claim 14 words

A composition, as in claim 8, wherein the organ specific carrier is an organophosphonate.

Claim 11

Dependent Claim 39 words

A composition, as in claim 9, wherein said organophosphonate is selected from the group consisting of methanediphosphonic acid, methanehydroxydiphosphonic acid, ethane-1-hydroxy-1,1-diphosphonic acid, methaneaminidiphosphonic acid, methane-N-methylaminodiphosphonic acid, methane-N,N-dimethylamniodiphosphonic acid, propane-1-hydroxy-3-amino-1,1-diphosphonic acid, ethane-1-1-hydroxy-2-amino-1,1-diphosphonic acid, and the pharmaceutically-acceptable salts and mixtures thereof.

Claim 12

Dependent Claim 35 words

A composition, as in claim 10, wherein the pertechnetate reductant is stannous chloride, the organ-specific carrier is a sodium salt of methaneaminodiphosphonic acid, and the reductate stabilizer is 6-bromo-6-deoxyascorbic acid or a sodium salt thereof.

Claim 13

Dependent Claim 35 words

A composition, as in claim 10, wherein the pertechnetate reductant is stannous chloride, the organ-specific carrier is a sodium salt of methanediphosphonic acid, and the reductate stabilizer is 6-bromo-6-deoxyascorbic acid or a sodium salt thereof.

Claim 14

Dependent Claim 35 words

A composition, as in claim 10, wherein the pertechnetate reductant is stannous chloride, the organ-specific carrier is a sodium salt of methanehydroxydiphosphonic acid, and the reductate stabilizer is 6-bromo-6-deoxyascorbic acid or a sodium salt thereof.

Claim 15

Dependent Claim 15 words

A composition, as in claim 8, wherein the organ-specific carrier is a water-soluble inorganic phosphate.

Claim 16

Dependent Claim 117 words

A composition, useful in the preparation of technetium-99m-based radiographic imaging agents, comprising: (a) an effective amount of a reductate stabilizer selected from group consisting of compounds and mixtures of compounds having the formula: ##STR13## wherein X is CRR' O, or NR', R' is hydrogen, or lower alkyl, Y is oxygen, sulfur, nitrogen, or CH 2 , R is hydrogen, lower alkyl, alkyl containing from 3 to 8 carbon atoms substituted with one or more hydroxy, halogen, amino, or thiol groups, alkyl containing from 1 to 8 carbon atoms halogen-substituted on the first and/or second carbon atom, lower alkenyl, nicotinic acid, nicotinamide complexes thereof and pharmaceutically-acceptable salts, amides, and esters thereof; dissolved in (b) an oxidized pertechnetate solution.

Claim 17

Dependent Claim 117 words

A composition, useful in the preparation of technetium-99m-based radiographic imaging agents, comprising: (a) an effective amount of a reductate stabilizer selected from group consisting of compounds and mixtures of compounds having the formula: ##STR13## wherein X is CRR' O, or NR', R' is hydrogen, or lower alkyl, Y is oxygen, sulfur, nitrogen, or CH 2 , R is hydrogen, lower alkyl, alkyl containing from 3 to 8 carbon atoms substituted with one or more hydroxy, halogen, amino, or thiol groups, alkyl containing from 1 to 8 carbon atoms halogen-substituted on the first and/or second carbon atom, lower alkenyl, nicotinic acid, nicotinamide complexes thereof and pharmaceutically-acceptable salts, amides, and esters thereof; dissolved in (b) an oxidized pertechnetate solution.

Claim 18

Dependent Claim 25 words

A composition, as in claim 15, comprising said oxidized pertechnetate solution having dissolved therein no more than about 0.1%, by weight, of said reductate stabilizer.

Claim 19

Independent Claim 127 words

A method of preparing a stabilized technetium-99m-based imaging agent, comprising dissolving a reductate stabilizer selected from the group consisting of compounds and mixtures of compounds having the formula: ##STR14## wherein X is CRR' O, or NR', R' is hydrogen, or alkyl containing from 1 to 8 carbon atoms, Y is oxygen, sulfur, nitrogen, or CH 2 , R is hydrogen, lower alkyl, alkyl containing from 3 to 8 carbon atoms substituted with one or more hydroxy, halogen, amino, or thiol groups, alkyl containing from 1 to 8 carbon atoms halogen-substituted on the first and/or second carbon atom, lower alkenyl nicotinic acid and nicotinamide complexes thereof and pharmaceutically-acceptable salts, amides, and esters thereof; in an aqueous solution of radioactive technetium in the +3, +4, or +5 valence state.

Claim 20

Independent Claim 127 words

A method of preparing a stabilized technetium-99m-based imaging agent, comprising dissolving a reductate stabilizer selected from the group consisting of compounds and mixtures of compounds having the formula: ##STR14## wherein X is CRR' O, or NR', R' is hydrogen, or alkyl containing from 1 to 8 carbon atoms, Y is oxygen, sulfur, nitrogen, or CH 2 , R is hydrogen, lower alkyl, alkyl containing from 3 to 8 carbon atoms substituted with one or more hydroxy, halogen, amino, or thiol groups, alkyl containing from 1 to 8 carbon atoms halogen-substituted on the first and/or second carbon atom, lower alkenyl nicotinic acid and nicotinamide complexes thereof and pharmaceutically-acceptable salts, amides, and esters thereof; in an aqueous solution of radioactive technetium in the +3, +4, or +5 valence state.

Claim 21

Dependent Claim 22 words

A method of preparing a stabilized technetium-99m-based imaging agent, as in claim 17, wherein an organ-seeking carrier is included in the solution.

Annuity Stage	Window Opens	Payment Deadline	Surcharge Period Until	Estimated Fee	Status
3.5 Years (Year 4)	1987-04-03	1987-10-03	1988-04-03	$2000.00	Window Closed / Lapsed
7.5 Years (Year 8)	1991-04-03	1991-10-03	1992-04-03	$3760.00	Window Closed / Lapsed
11.5 Years (Year 12)	1995-04-03	1995-10-03	1996-04-03	$7700.00	Window Closed / Lapsed

Stable radiographic imaging agents

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