US5117830A
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Method of determining viability of tissue
Assignee: Aderis Pharmaceuticals Inc
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Filing: 1990-11-08
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Granted: 1992-06-02
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Expires: 2010-11-08
Abstract
Abstract A method and composition for determining the viability of tissue in a region of an organism having a vascular circulatory system that supplies blood to said region including the steps of dilating said vascular circulation system by introducing adenosine or an adenosine agonist into said vascular circulation system in order to increase the flow of blood into said region; introducing a blood flow marking medium into said region; alleviating the non-dilating effects of adenosine or said adenosine agonist by introducing an A1 adenosine receptor antagonist into said vascular circulatory system; and determining the amount of marking medium in said region. A composition is disclosed which includes the combination of adenosine or an adenosine agonist in combination with an A1 adenosine receptor which may be: <IMAGE> wherein R1 is hydrogen or R2; R2 is selected from the group consisting of endo-2-norbornyl or cyclopentyl; R3 is selected from the group consisting of hydrogen, halogen, amine, carboxy, alkyl radicals having 1 to 10 carbon atoms, cycloalkyl radicals having from 3 to 8, preferably 5 to 6, ring carbon atoms, thio, sulfonate, sulfonamide, sulfon, sulfoxamide, phenyl, alkyl-substituted amine, and cycloalkyl substituted amine; R4 is selected from the group consisting of benzyl, phenyl, and alkyl groups comprising from 1 to 4 carbon atoms, wherein said alkyl group can be substituted with oxygen, for instance ethers and alcohols; and R5 is selected from the group consisting of hydrogen; hydroxy; sulfonate; halogen; alkoxy and cycloalkoxy groups comprising 1 to 6 carbon atoms.
Inventors
- 👤 Donald A. McAfee
- 👤 Luiz Belardinelli
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-10 01:54
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0491; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/519; A61K31/52; A61K2123/00
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
104 words
A method for determining the viability of tissue in a region of an organism having a vascular circulatory system that supplies blood to said region which comprises the steps of: (a) dilating said vascular circulation system by introducing adenosine or an adenosine agonist into said vascular circulation system in order to increase the flow of blood into said region; (b) introducing a blood flow marking medium into said region; (c) alleviating the non-dilating effects of adenosine or said adenosine agonist by introducing an A 1 adenosine receptor antagonist into said vascular circulatory system; and (d) determining the amount of marking medium in said region.
Claim 2
Independent Claim
104 words
A method for determining the viability of tissue in a region of an organism having a vascular circulatory system that supplies blood to said region which comprises the steps of: (a) dilating said vascular circulation system by introducing adenosine or an adenosine agonist into said vascular circulation system in order to increase the flow of blood into said region; (b) introducing a blood flow marking medium into said region; (c) alleviating the non-dilating effects of adenosine or said adenosine agonist by introducing an A 1 adenosine receptor antagonist into said vascular circulatory system; and (d) determining the amount of marking medium in said region.
Claim 3
Dependent Claim
139 words
The method of claim 1 wherein the A 1 adenosine receptor agonist is ##STR4## wherein R 1 is hydrogen or R 2 ; R 2 is selected from the group consisting of endo-2-norbornyl or cyclopentyl; R 3 is selected from the group consisting of hydrogen, halogen, amine, carboxy, alkyl radicals having 1 to 10 carbon atoms, cycloalkyl radicals having from 3 to 8, preferably 5 to 6, ring carbon atoms, thio, sulfonate, sulfonamide, sulfon, sulfoxamide, phenyl, alkyl-substituted amine, and cycloalkyl substituted amine; is selected from the group consisting of benzyl, phenyl, and alkyl groups comprising from 1 to 4 carbon atoms, wherein said alkyl group can be substituted with oxygen, for instance ethers and alcohols; and R 5 is selected from the group consisting of hydrogen; hydroxy; sulfonate; halogen; alkoxy and cycloalkoxy groups comprising 1 to 6 carbon atoms.
Claim 4
Dependent Claim
19 words
The method of claim 1 wherein the A 1 adenosine receptor agonist is an N 6 -norbornyl substituted adenine.
Claim 5
Dependent Claim
63 words
The method of claim 3 wherein the A 1 adenosine receptor agonist is selected from the group consisting of: N 6 -(endo-2-norbornyl)-9-methyl adenine, N 6 -(endo-2-norbornyl)-2-chloro-9-methyl adenine, N 6 -(endo-2-norbornyl)-8-bromo-9-methyl adenine, N 6 -(endo-2-norbornyl)-8-amino-9-methyl adenine, N 6 -(endo-2-norbornyl)-9-[(2-hydroxyethoxy)methyl]adenine, N 6 -(endo-2-norbornyl)-8-thio-9-methyl adenine, N 6 -(endo-2-norbornyl)-8-chloro-9-methyl adenine, N 6 -(endo-2-norbornyl)-2-oxo-9-methyl adenine, N 6 -(endo-2-norbornyl)-8-cyclopentyl-amine-9-methyl adenine, N 6 -(endo-2-norbornyl)-8-cyclopentyl-9-methyl adenine, and N 6 -(exo-2-norbornyl)-9-methyl adenine.
Claim 6
Independent Claim
35 words
The method of claim wherein the A 1 adenosine receptor agonist is selected from the group consisting of N 6 -3-pentyl-9-methyl adenine, N 6 -cyclopentyl-9-methyl adenine, N 6 -1-(2-thienyl)-2-butyl-9-methyl denine, and N 6 -cyclopentyl-8-cyclopentyl-9-ethyl adenine.
Claim 7
Dependent Claim
19 words
The method of claim 1 wherein said marking medium is selected from the group consisting of thallium-201 and rubidium-82.
Claim 8
Dependent Claim
11 words
The method of claim 6 wherein said marking medium comprises thallium-201.
Claim 9
Dependent Claim
14 words
The method of claim 7 wherein adenosine is introduced into said vascular circulatory system.
Claim 10
Dependent Claim
27 words
The method of claim 8 wherein the amount of marking medium in said region is determined by non-invasive myocardial imaging of the blood flow to said region.
Claim 11
Dependent Claim
17 words
The method of claim 3 wherein said N 6 -norbornyl substituted adenine is N 6 -(endo-norbornyl)-9-methyl adenine.
Claim 12
Independent Claim
109 words
A method for determining the viability of tissue in a region of an organism having a vascular circulatory system that supplies blood to said region which comprises the steps of: (a) dilating said vascular circulation system by introducing adenosine or an adenosine agonist into said vascular circulation system in order to increase the flow of blood into said region; (b) introducing a blood flow marking medium into said region; (c) reducing the amount of adenosine or said adenosine agonist necessary to dilate the vascular circulation system by introducing an A adenosine receptor antagonist into said vascular circulatory system; and (d) determining the amount of marking medium in said region.
Claim 13
Independent Claim
109 words
A method for determining the viability of tissue in a region of an organism having a vascular circulatory system that supplies blood to said region which comprises the steps of: (a) dilating said vascular circulation system by introducing adenosine or an adenosine agonist into said vascular circulation system in order to increase the flow of blood into said region; (b) introducing a blood flow marking medium into said region; (c) reducing the amount of adenosine or said adenosine agonist necessary to dilate the vascular circulation system by introducing an A adenosine receptor antagonist into said vascular circulatory system; and (d) determining the amount of marking medium in said region.
Claim 14
Dependent Claim
141 words
The method of claim 11 wherein the A 1 adenosine receptor agonist is ##STR5## wherein R 1 is hydrogen or R 2 ; R 2 is selected from the group consisting of endo-2-norbornyl or cyclopentyl; R 3 is selected from the group consisting of hydrogen, halogen, amine, carboxy, alkyl radicals having 1 to 10 carbon atoms, cycloalkyl radicals having from 3 to 8, preferably 5 to 6, ring carbon atoms, thio, sulfonate, sulfonamide, sulfon, sulfoxamide, phenyl, alkyl-substituted amine, and cycloalkyl substituted amine; R 4 is selected from the group consisting of benzyl, phenyl, and alkyl groups comprising from 1 to 4 carbon atoms, wherein said alkyl group can be substituted with oxygen, for instance ethers and alcohols; and R 5 is selected from the group consisting of hydrogen; hydroxy; sulfonate; halogen; alkoxy and cycloalkoxy groups comprising 1 to 6 carbon atoms.
Claim 15
Dependent Claim
19 words
The method of claim 11 wherein the A 1 adenosine receptor agonist is an N 6 -norbornyl substituted adenine.
Claim 16
Dependent Claim
63 words
The method of claim 31 wherein the A 1 adenosine receptor agonist is selected from the group consisting of: N 6 -(endo-2-norbornyl)-9-methyl adenine, N 6 -(endo-2-norbornyl)-2-chloro-9-methyl adenine, N 6 -(endo-2-norbornyl)-8-bromo-9-methyl adenine, N 6 -(endo-2-norbornyl)-8-amino-9-methyl adenine, N 6 -(endo-2-norbornyl)-9-[(2-hydroxyethoxy)methyl]adenine, N 6 -(endo-2-norbornyl)-8-thio-9-methyl adenine, N 6 -(endo-2-norbornyl)-8-chloro-9-methyl adenine, N 6 -(endo-2-norbornyl)-2-oxo-9-methyl adenine, N 6 -(endo-2-norbornyl)-8-cyclopentyl-amine-9-methyl adenine, N 6 -(endo-2-norbornyl)-8-cyclopentyl-9-methyl adenine, and N 6 -(exo-2-norbornyl)-9-methyl adenine.
Claim 17
Dependent Claim
36 words
The method of claim 11 wherein the A 1 adenosine receptor agonist is selected from the group consisting of N 6 -3-pentyl-9-methyl adenine, N 6 -cyclopentyl-9-methyl adenine, N 6 -1-(2-thienyl)-2-butyl-methyl adenine, and N 6 -cyclopentyl-8-cyclopentyl-9-methyl adenine.
Claim 18
Dependent Claim
19 words
The method of claim 11 wherein said marking medium is selected from the group consisting of thallium-201 and rubidium-82.
Claim 19
Dependent Claim
11 words
The method of claim 16 wherein said marking medium comprises thallium-201.
Claim 20
Dependent Claim
14 words
The method of claim 17 wherein adenosine is introduced into said vascular circulatory system.
Claim 21
Dependent Claim
27 words
The method of claim 18 wherein the amount of marking medium in said region is determined by non-invasive myocardial imaging of the blood flow to said region.
Claim 22
Dependent Claim
17 words
The method of claim 19 wherein said N 6 -norbornyl substituted adenine is N 6 -(endo-norbornyl)-9-methyl adenine.
Claim 23
Dependent Claim
86 words
In a method for determining the viability of tissue in a region of an organism having a vascular circulatory system that supplies blood to said region the improvement which comprises the steps of; (a) dilating said vascular circulation system by introducing adenosine or an adenosine agonist into said vascular circulation system in order to increase the flow of blood into said region; and, (b) alleviating the non-dilating effects of adenosine or said adenosine agonist by introducing an Al adenosine receptor antagonist into said vascular circulatory system.
Claim 24
Dependent Claim
86 words
In a method for determining the viability of tissue in a region of an organism having a vascular circulatory system that supplies blood to said region the improvement which comprises the steps of; (a) dilating said vascular circulation system by introducing adenosine or an adenosine agonist into said vascular circulation system in order to increase the flow of blood into said region; and, (b) alleviating the non-dilating effects of adenosine or said adenosine agonist by introducing an Al adenosine receptor antagonist into said vascular circulatory system.
References Cited (Backward Citations)
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