US4933156A
Expired / Lapsed
US
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Amyloidosis and Alzheimer's disease diagnostic assay and reagents therefor
Assignee: Amersham Health Salutar Inc
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Filing: 1988-04-06
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Granted: 1990-06-12
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Expires: 2008-04-06
Abstract
Abstract The presence and location of amyloid deposits in an organ or body area of a patient is effected by intravenous administration of novel radioactive iodine-labeled amyloid binding compounds and preferably 123 I-labeled compounds to the patient and sensing radiation emitted from the organ or body area. Novel non-radioactive iodine substituted amyloid binding compounds and amyloid binding compounds which are readily iodinated are further aspects of the invention.
Inventors
- 👤 Steven C. Quay
- 👤 Scott M. Rocklage
- 👤 Warren K. Miller
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 17:09
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0404; A61K51/0406; A61K51/041; A61K51/044; A61K51/0453; C; C07; C07C; C07C309/00; C07C309/01; C07C309/28; C07C309/45; C07C309/47; C07C309/49; C07C309/50; C07D; C07D277/00; C07D277/60; C07D277/62; C07D277/64; C07D277/66; C09; C09B; C09B29/00; C09B29/0003; C09B29/0011; C09B29/24; C09B29/28; C09B29/30; C09B35/00; C09B35/02; C09B35/039; C09B35/08; C09B35/10; C09B35/16; C09B35/20; C09B43/00; C09B43/40; G; G01; G01N; G01N33/00; G01N33/48; G01N33/50; G01N33/68; G01N33/6893; G01N33/6896; A61K2123/00; G01N2800/00; G01N2800/28; G01N2800/2814; G01N2800/2821
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
464 words
An amyloid binding diazo compound of Formula I, Formula II, Formula III or Formula IV or a water-soluble, non-toxic salt thereof: ##STR13## wherein I* is a non-radioactive or radioactive iodine moiety; R 1 is amino or hydroxy; R 2 , R 3 , R 4 , R 5 and R 6 are hydrogen or sulfo, with the proviso that not more than two of R 2 , R 3 , R 4 , R 5 and R 6 are sulfo and sulfo is not present on adjacent carbons; R 8 , R 9 and R 10 are hydrogen, hydroxy, carboxy or lower alkyl esters thereof, methyl, or methoxy; R 12 and R 14 are each independently hydrogen, methyl, chloro, methoxy, carboxy or a lower alkyl ester thereof, sulfo or nitro; and R 13 and R 15 are each independently hydrogen or sulfo; ##STR14## wherein R 20 , R 24 , R 25 and R 29 each independently are hydrogen, hydroxy or amino, with the proviso that R 24 is not the same as R 20 and R 29 is not the same as R 25 ; R 21 , R 22 , R 23 , R 26 , R 27 and R 28 each independently are hydrogen or sulfo, with the proviso that not more than two of R 21 , R 22 and R 23 is sulfo and not more than two of R 26 , R 27 and R 28 is sulfo, and sulfo is not present on adjacent carbons; R 30 and R 32 are each independently hydrogen, methyl, chloro, methoxy, carboxy or a lower alkyl ester thereof, sulfo or nitro; R 31 and R 33 are each independently hydrogen or sulfo; X 1 , X 2 , X 3 and X 4 are each independently hydrogen or I*, with the proviso that X 1 is hydrogen when R 21 is sulfo, X 2 is hydrogen when R 22 and R 23 is sulfo, X 3 is hydrogen when R 26 is sulfo, and X 4 is hydrogen when R 27 or R 28 is sulfo; ##STR15## wherein R 40 and R 41 are hydroxy or amino, and R 40 and R 41 are not the same group; R 42 , R 43 , R 44 , R 45 , and R 46 are hydrogen or sulfo; one or two of R 42 , R 43 , R 44 , R 45 , and R 46 are sulfo; and sulfo is not present on adjacent carbons; and R 47 is hydrogen, methyl or carboxy; or ##STR16## wherein R 50 is hydrogen or sulfo; R 51 is methyl or carboxy; and R 52 , R 53 and R 54 each are hyrogen, hydroxy, carboxy or lower alkyl esters thereof, methyl, or methoxy.
Claim 2
Dependent Claim
464 words
An amyloid binding diazo compound of Formula I, Formula II, Formula III or Formula IV or a water-soluble, non-toxic salt thereof: ##STR13## wherein I* is a non-radioactive or radioactive iodine moiety; R 1 is amino or hydroxy; R 2 , R 3 , R 4 , R 5 and R 6 are hydrogen or sulfo, with the proviso that not more than two of R 2 , R 3 , R 4 , R 5 and R 6 are sulfo and sulfo is not present on adjacent carbons; R 8 , R 9 and R 10 are hydrogen, hydroxy, carboxy or lower alkyl esters thereof, methyl, or methoxy; R 12 and R 14 are each independently hydrogen, methyl, chloro, methoxy, carboxy or a lower alkyl ester thereof, sulfo or nitro; and R 13 and R 15 are each independently hydrogen or sulfo; ##STR14## wherein R 20 , R 24 , R 25 and R 29 each independently are hydrogen, hydroxy or amino, with the proviso that R 24 is not the same as R 20 and R 29 is not the same as R 25 ; R 21 , R 22 , R 23 , R 26 , R 27 and R 28 each independently are hydrogen or sulfo, with the proviso that not more than two of R 21 , R 22 and R 23 is sulfo and not more than two of R 26 , R 27 and R 28 is sulfo, and sulfo is not present on adjacent carbons; R 30 and R 32 are each independently hydrogen, methyl, chloro, methoxy, carboxy or a lower alkyl ester thereof, sulfo or nitro; R 31 and R 33 are each independently hydrogen or sulfo; X 1 , X 2 , X 3 and X 4 are each independently hydrogen or I*, with the proviso that X 1 is hydrogen when R 21 is sulfo, X 2 is hydrogen when R 22 and R 23 is sulfo, X 3 is hydrogen when R 26 is sulfo, and X 4 is hydrogen when R 27 or R 28 is sulfo; ##STR15## wherein R 40 and R 41 are hydroxy or amino, and R 40 and R 41 are not the same group; R 42 , R 43 , R 44 , R 45 , and R 46 are hydrogen or sulfo; one or two of R 42 , R 43 , R 44 , R 45 , and R 46 are sulfo; and sulfo is not present on adjacent carbons; and R 47 is hydrogen, methyl or carboxy; or ##STR16## wherein R 50 is hydrogen or sulfo; R 51 is methyl or carboxy; and R 52 , R 53 and R 54 each are hyrogen, hydroxy, carboxy or lower alkyl esters thereof, methyl, or methoxy.
Claim 3
Dependent Claim
11 words
As a compound of claim 1, a compound of Formula I.
Claim 4
Dependent Claim
16 words
As a compound of claim 2, 4-amino-3-(4-(1-carboxy-2-hydroxy-3- 123 I-5-phenyldiazo)-biphen-4'-yldiazo)-naphthalene-1-sulfonic acid, or a water-soluble, non-toxic salt thereof.
Claim 5
Dependent Claim
11 words
As a compound of claim 1, a compound of Formula II.
Claim 6
Dependent Claim
16 words
A compound of claim 1, 2, or 4 wherein I* is 123 I or 124 I.
Claim 7
Independent Claim
52 words
A method for determining the presence and location of an amyloid deposit in a body area of a patient comprising intravenous administration of an imaging effective quantity of a compound containing a radioactive iodine group of claims 1, 2,3 or 4, to the patient, and sensing radiation emitted from the body area.
Claim 8
Dependent Claim
29 words
A method of claim 6 wherein the radioactive iodine group is 123 I, and the compound is prepared by exchange of 123 I for non-radioactive iodine in a compound.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-06-11 | 1993-12-11 | 1994-06-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-06-11 | 1997-12-11 | 1998-06-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-06-11 | 2001-12-11 | 2002-06-12 | $7700.00 | Window Closed / Lapsed |