Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: This invention relates to novel fluorinated phenyl thiphenyl (also named diarylsulfide) derivatives and their use in Positron Emission Tomagraphy (PET) imaging of Serotonin Transporters (SERTS). The present invention also provides diagnostic compositions comprising the novel compounds of the present invention, and a pharmaceutically acceptable carrier or diluent. The invention further provides a method of imaging SERTS, comprising introducing into a patient a detectable quantity of a labeled compound of the present invetion, or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: Compounds such as 4-(s'-methoxy)phenyl-?2'-N-2"-pyridinyl)-p-iodobenzamido! ethylpiperazine have affinity and specificity for serotonin 5-HT.sub.1A receptors.

Abstract: Tetralin derivatives, such as 7-hydroxy-2-(N-n-propyl-N-3 '-iodo-2'-propenyl)-amino!tetralin and 8-hydroxy-2-(N-n-propyl-N-3 '-iodo-2'-propenyl)amino-tetralin, are disclosed which have affinity and specificity for dopamine D-3 and/or serotonin 5-HT.sub.1A receptors.

Abstract: Compounds such as 4-(s'-methoxy)phenyl-[2'-N-2"-pyridinyl)-p-iodobenzamido]ethylpiperazine have affinity and specificity for serotonin 5-HT.sub.1A receptors.

Abstract: This invention relates to novel dopamine D-1 and D-2 imaginging agents which are both fluorinated and iodinated and can appropriately labelled for use in both PET and SPECT imaging. Compounds include S-(-)-2-fluoroethoxy-3-methyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-iodoben zamide and R(+)-2,3-dimethoxy-N-[(1-(4'-fluorobenzyl)-2-pyrrolidinyl)methyl]-5-iodobe nzamide.

Abstract: Novel CNS dopamine D-2 receptors, such as the compound 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3-dihydrobenzofur an, are disclosed. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.

Abstract: Novel CNS dopamine D-2 receptors, such as the compound 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3-dihydrobenzofur an, are disclosed. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.

Abstract: Disclosed are novel compounds for CNS neurotransmitter systems, especially for the neurotransmitter serotonin, which have the formula ##STR1## where each of U, V, W, X, Y and Z is independently selected from the group consisting of hydrogen; halogen; C.sub.1 -C.sub.4 alkyl; C.sub.1 -C.sub.4 alkyl substituted with one or more moieties selected from halogen atoms and hydroxy groups; C.sub.1 -C.sub.4 alkoxy; C.sub.1 -C.sub.4 alkoxy substituted with one or more moieties selected from halogen atoms and hydroxy groups; C.sub.1 -C.sub.6 heterocycles; C.sub.1 -C.sub.4 thioalkyl; NR.sub.3 R.sub.4 ; --R.sub.5 --A --R.sub.6 ; and --A--R.sub.7 ; CN; SO.sub.2 R.sub.8 ; --NHCONH.sub.2 ; and C(O)NR.sub.3 R.sub.4 ;each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl;each of R.sub.5 and R.sub.6 is independently a C.sub.1 -C.sub.6 alkyl;R.sub.7 is selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.

Abstract: Compounds of the formula ##STR1## where R.sub.1 and R.sub.2 are independently selected from the group consisting of H, OH, OCH.sub.3, and Halogen or R.sub.1 and R.sub.2 can be taken together to form --O--CH.sub.2 --O--;R.sub.3 and R.sub.4 are independently selected from the group consisting of H, OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 alkenyloxy, --R.sub.7 --CH.dbd.CHI, and ##STR2## n is an integer from 0 to 5; X and Y are independently selected from the group consisting of H, OH, OCH.sub.3, Halogen and --R.sub.7 --CH.dbd.CHI;R.sub.5 and R.sub.6 are independently selected from the group consisting of H, OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 alkenyloxy, --R.sub.7 --CH.dbd.CHI, --CONR.sub.8 R.sub.9 and ##STR3## X' and Y' are independently selected from the group consisting of H, OH, OCH.sub.3, Halogen, and --R.sub.7 --CH.dbd.CHI;R.sub.7 is selected from the group consisting of a chemical bond and C.sub.1 -C.sub.10 alkyl; andR.sub.8 and R.sub.

Abstract: Novel CNS dopamine D-2 receptors, such as the compound 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3-dihydrobenzofur an, are disclosed. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.

Abstract: Novel CNS dopamine D-1 receptors, such as the compound (.+-.)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-(4'-[.sup.125 I]iodophenyl)-1H-3-benzazepine-7-ol, are disclosed. These compounds are useful as imaging agents for D-1 receptors in the human brain and exhibit good brain retention and in vivo stability.

Abstract: Novel CNS dopamine D-2 receptors, such as the compound 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3-dihydrobenzofur an, are disclosed. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.

Abstract: Complexes having the formula: ##STR1## where each of R.sub.1 -R.sub.14 is independently selected from the group consisting of hydrogen, alkyl groups in which one or more carbon atoms is optionally substituted by a heteroatom such as N, O or S, and phenyl optionally mono- or di-substituted with a substituent selected from the group consisting of --SR.sub.15,-- OR.sub.15, and --NR.sub.15 R.sub.16, where R.sub.15 and R.sub.16 are independently selected from H and alkyl groups; or each grouping of R.sub.1 and R.sub.2, R.sub.3 and R.sub.4, R.sub.5 and R.sub.6, R.sub.7 and R.sub.8, R.sub.11 and R.sub.12, and R.sub.13 and R.sub.

Abstract: Novel CNS dopamine D-1 receptors, such as the compound (.+-.)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-(4'-[.sup.125 I]iodophenyl)-1H-3-benzazepine-7-ol, are disclosed. These compounds are useful as imaging agents for D-1 receptors in the human brain and exhibit good brain retention and in vivo stability.

Abstract: A method for radiolabeling organic compounds is disclosed in which said compounds are contacted with carrier-free radioactive halide ion in the presence of an effective amount of peracetic acid.

Abstract: A radiopharmaceutical chemical compound comprising a radioactive isotope, other than an isotope of iodine, in chemical combination with at least one amine group. The compound has a lipophilicity sufficiently high at a pH of 7.6 to permit passage of the compound from the blood of a mammal into a target organ or tissue and sufficiently low at a pH of 6.6 to prevent rapid return of the compound from the target organ or tissue to the blood. The compound has a percent protein binding of less than ninety percent.A method for selectively depositing a radiopharmaceutical compound in at least one target tissue or organ of a mammal, which tissue or organ has a significantly different intracellular pH than the blood of the mammal, by introducing the compound of the invention into the bloodstream of the mammal.

Abstract: The invention is accomplished by the formation at the site of use of the radioactive amine of the invention which is then injected immediately into the mammal for diagnostic purposes. The compounds of the invention are as follows: ##STR1## In the above compound, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently any straight or branched alkyl of between 1 and about 10 carbons; n may be between 1 and about 20.In the invention, the radio labeling of the invention compound is accomplished immediately prior to use of the radio labeled material. The compounds of the invention when boiled for about 15 minutes with iodine-123, a radioactive material, undergo a substitution of radioactive for non-radioactive iodine such that the compound becomes labeled and suitable for use. The compound itself, prior to radio labeling, is storage stable.