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Stereoisomers of fatty acid analogs for diagnostic imagingRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Radionuclide Or Intended Radionuclide Containing; Adjuvant Or Carrier Compositions; Intermediate Or Preparatory CompositionsStereoisomers of fatty acid analogs for diagnostic imaging description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070128110, Stereoisomers of fatty acid analogs for diagnostic imaging. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application is a Continuation of U.S. Utility application Ser. No. 11/274,505, filed Nov. 16, 2005, which is a Continuation of U.S. Utility application Ser. No. 10/429,416, filed May 5, 2003, now U.S. Pat. No. 7,005,119, which is a Continuation of U.S. Utility application Ser. No. 09/077,490, filed May, 29, 1998, now abandoned, filed as a 35 U.S.C. .sctn.371 filing of International Application No. PCT/US96/19024, filed on Nov. 25, 1996, which in turn claims priority to U.S. Provisional Application No. 60/007,863, filed on Dec. 1, 1995. DESCRIPTION [0003] The present invention relates to the field of nuclear medicine. More specifically, the invention relates to diagnostic imaging using substantially pure stereoisomers of radionuclide-containing fatty acid analogs. BACKGROUND OF THE INVENTION [0004] Clinical imaging technology plays a significant role in diagnosis of injuries and disease processes. Virtually any part of an animal's body can now be examined for diagnostic purposes using a variety of imaging techniques. Radiography has long been used to image body parts through which externally generated x-rays are transmitted. Computerized axial tomography (CAT) provides cross-sectional x-ray images of a plane of the body. Specific tissues or organs may be targeted in positron emission tomography (PET), single photon emission computed tomography (SPECT), and scintigraphy. In PET, SPECT, and scintigraphy, radiopharmaceutical agents capable of sequestering to some degree in the target tissue or organ are internally administered to the patient, and images are generated by detecting the radioactive emissions from the sequestered radiopharmaceutical agent. Radiopharmaceutical agents include nuclides such as .sup.201TI, .sup.99m Tc, .sup.133Xe, and the like; chelates of nuclides; nuclide labeled metabolic agents such as .sup.11C-deoxy-D-glucose, .sup.18F-2-fluorodeoxy-D-glucose, [1-.sup.11C]- and [.sup.123I]-.beta.-methyl fatty acid analogs, .sup.13N-ammonia, and the like; infarct avid agents such as .sup.99mTc-tetracycline, .sup.99mTc-pyrophosphate, .sup.203Hg-mercurials, .sup.67Ga-citrate, and the like; and nuclide labeled monoclonal antibodies. Whole cells such as erythrocytes and leukocytes may also be labeled with a radionuclide and function as radiopharmaceutical agents. [0005] The amount and type of clinical information that can be derived from PET, SPECT, and scintigraphic images is related in part to the ability of the radiopharmaceutical agent to sequester in the target tissue or organ. Although many radiopharmaceuticals are available for clinical use, for a given imaging instrument, the agents generally have limitations in the resolution of the image generated. The resolution available for a particular imaging agent is highly dependent on the affinity of the radiopharmaceutical to bind at the site of injury as compared to the affinity of the radiopharmaceutical to bind to healthy tissue surrounding the site of injury. [0006] In spite of their limitations, radiopharmaceuticals are used in a variety of types of studies to obtain different kinds of information. For example, radiopharmaceutical agents used in cardiac blood flow and blood pool studies provide information on murmurs, cyanotic heart disease, and ischemic heart disease. Perfusion scintigraphy agents provide measurements of blood flow useful in detection of coronary artery disease, assessment of pathology after coronary arteriography, pre- and postoperative assessment of coronary artery disease, and detection of acute myocardial infarction. Infarct avid agents are used for "hot spot" infarct imaging. Radiopharmaceuticals which allow binding to specific cardiac receptors, while generally still in the developmental stage, may allow detection of highly specific binding in the cardiovascular system. Radionuclide-containing antibodies directed against the heavy chain of cardiac myosin have been proposed to identify zones of acute myocardial necrosis, and .sup.99m Tc-labeled low density lipoprotein may be useful to detect atheromatous lesions in their early stages after onset of endothelial damage. .sup.99m Tc-HMPO and .sup.123I-iodoamphetamines are used to study changes in brain blood flow with SPECT. Receptor-ligand interactions, glucose utilization, protein synthesis, and other physiological parameters are also studied with other radiopharmaceuticals using PET. [0007] Radiopharmaceutical agents capable of detecting the rate and amount of metabolism are particularly important to the progress of clinical nuclear medicine, since they allow studies of the energy consumption in the various stages of disease processes. For example, cardiac metabolism can now be studied using labeled physiologic tracers and using analogs of "natural" metabolites that are transported in the same manner as the metabolite but go through only a few reactions of the metabolic pathway and are then trapped in the tissue in a chemically known form. The glucose analog [.sup.18F]-2-fluoro-2-deoxy-D-glucose can be used to detect areas of altered glucose metabolism in the heart or other target organs which may be associated with hypoxia and anoxia and thus aid in defining the extent of an ischemic injury or cardiomyopathy. Fatty acids are the main source of energy for the heart, and radiolabeled fatty acids or their close analogs have been used to study heart metabolic integrity. .beta.-methyl-fatty acid analogs are one group of fatty acids used as metabolic tracers. [0008] Racemic mixtures of many .beta.-methyl-fatty acid analogs are disclosed in U.S. Pat. No. 4,524,059. One .beta.-methyl-fatty acid analog, [.sup.123I]-15-(p-iodophenyl)-3-R,S-methylpentadecanoic acid ([.sup.123I]-BMIPP) has been used for myocardial imaging in Japan. However, the racemic nature of [.sup.123I]-BMIPP makes it less than optimal for imaging studies, since uptake and metabolism of the R and S stereoisomers may differ and thus decrease the specificity of the reagent for heart tissue. Although use of stereoisomers of .beta.-methyl-fatty acid analogs has been suggested, obtaining such isomers at a meaningful level of purity has been difficult. [0009] Because an accurate imaging diagnosis of injury or disease depends so heavily on the agent used, a need continues to exist for radiopharmaceuticals with improved tissue and organ specificity. SUMMARY OF THE INVENTION [0010] The present invention provides improved and novel radio-pharmaceutical agents for diagnostic imaging of injuries and disease states. The imaging agents of the invention are radionuclide-containing analogs of fatty acids and are particularly suitable for cardiovascular and brain imaging. The imaging agents of the invention are substantially pure stereoisomers of fatty acid analogs. [0011] In one embodiment, the invention provides an imaging agent comprising a radionuclide in spatial proximity to a stereoisomer of more than 75% isomeric purity of a fatty acid analog having the formula [0012] wherein R.sub.1 is selected from the group consisting of a hydrogen, fluorine, an iodoaryl group, an iodoallyl group, and an iodothiophene group; R.sub.2 is selected from the group consisting of a hydrogen, a primary amine, a secondary amine, a tertiary amine, an alkyl group, a substituted alkyl group, an aryl group, and a substituted aryl group; R.sub.3 is selected from the group consisting of a hydrogen, a methyl, a hydroxyl, a keto ester, a methoxy, a halide, and an amine; and n is greater than 12. [0013] In another embodiment the invention provides an analog of the formula [0014] wherein X* is a radioactive isotope of a halogen and n is an integer between 9 and 17, inclusive. [0015] In another embodiment, the invention provides an imaging agent comprising a radionuclide in spatial proximity to an isomer of a fatty acid analog having the formula [0016] wherein R.sub.1 is selected from the group consisting of a hydrogen, fluorine, an aryl group, a substituted aryl group, an allyl group, a substituted allyl group, a vinyl group, a substituted vinyl group, and an iodothiophene group; R.sub.2 is selected from the group consisting of a hydrogen, a primary amine, a secondary amine, a tertiary amine, an alkyl group, a substituted alkyl group, an aryl group, and a substituted aryl group; A is selected from the group consisting of a methylene group, an ethylene group, an oxygen, a sulfur, and a nitrogen; and n is greater than 10. [0017] In another embodiment, the invention provides an imaging agent comprising a radionuclide in spatial proximity to a stereoisomer of a fatty acid analog having the formula [0018] wherein R.sub.1 is selected from the group consisting of a hydrogen, fluorine, an aryl group, a substituted aryl group, an allyl group, a substituted allyl group, a vinyl group, a substituted vinyl group, and an iodothiophene group; R.sub.2 is selected from the group consisting of a hydrogen, a primary amine, a secondary amine, a tertiary amine, an alkyl group, a substituted alkyl group, an aryl group, and a substituted aryl group; R.sub.3 is selected from the group consisting of a hydrogen, a methyl, a hydroxyl, a keto ester, a methoxy, a halide, and an amine; A is selected from the group consisting of a hydrogen, an alkyl group, and a halide; B is selected from the group consisting of a hydrogen, an alkyl group, and a halide; n is greater than 3; and m is greater than 3. [0019] In another embodiment, the invention provides a method of imaging cardiovascular or brain tissue in a mammal which comprises administering to the mammal an imaging agent comprising a radionuclide in spatial proximity to an isomer of a fatty acid analog, and detecting the spatial distribution of the agent accumulated in the mammal. [0020] In another embodiment, the invention provides a method of detecting a cardiovascular lesion in a mammal which comprises administering to the mammal an imaging agent comprising a radionuclide in spatial proximity to an isomer of a fatty acid analog, and detecting the spatial distribution of the agent accumulated in the mammal's cardiovascular system, wherein a detected accumulation of agent in a region which is different from the detected accumulation of agent in other regions is indicative of a lesion. [0021] In another embodiment, the invention provides a method of detecting a brain lesion in a mammal which comprises administering to the mammal an imaging agent comprising a radionuclide in spatial proximity to an isomer of a fatty acid analog, and detecting the spatial distribution of the agent accumulated in the mammal's brain, wherein a detected accumulation of agent in a region which is different from the detected accumulation of agent in other regions is indicative of a lesion. Continue reading about Stereoisomers of fatty acid analogs for diagnostic imaging... Full patent description for Stereoisomers of fatty acid analogs for diagnostic imaging Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Stereoisomers of fatty acid analogs for diagnostic imaging patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. 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