Cocaine analogues and their use as cocaine drug therapies and th

Details Cocaine analogues and their use as cocaine drug therapies and th Cocaine analogues and their use as cocaine drug therapies and th

1993-08-24

1996-04-09

Ivy, C. Warren

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546128, 546129, C07D45102

Patent

active

055063594

ABSTRACT:
Disclosed are benztropine and CFT analogs useful for imaging of cocaine receptors and treatment of cocaine abuse. Also disclosed are analogs useful for imaging and treatment of Parkinson's disease.

REFERENCES:
patent: 2799680 (1957-07-01), Fromer
patent: 3452029 (1969-06-01), Childress et al.
patent: 3813404 (1974-05-01), Clarke et al.
patent: 4393069 (1983-07-01), Langbein et al.
patent: 5128118 (1992-07-01), Carroll et al.
Balster et al. "Potent Substituted-3.beta.-phenyltropane Analogs of Cocaine have Cocaine-like Discriminative Stimulus Effects" Drug and Alcohol Dependence, 29:145-151 (1991).
Boja et al. "Isothiocyanate Derivatives of Cocaine: Irreversible Inhibition of Ligand Binding at the Dopamine Transporter" Molecular Pharmacology 39:339-345 (1991).
Boja et al. "New, Potent Cocaine Analogs: Ligand Binding and Transport Studies in Rat Striatum" European J. of Pharmacology, 184:329-332 (1990).
Brownell et al. "Glucose Utilization and N-[C-11]-Methyl-2 Carbomethoxy-3-Phenyl Tropane ([C-11]PT) Studies of the Primate Model of Huntington's Disease" J. Nuclear Med. Abs., 32:981 (1991).
Canfield et al. "Autoradiographic Localization of Cocaine Binding Sites by [.sup.3 H]CFT (.sup.3 H]WIN 35,428) in the Monkey Brain" Synapse, 6:189-195 (1990).
Carroll et al. "Probes for the Cocaine Receptor. Potentially Irreversible Ligands for the Dopamine Transporter" J. Med. Chem., 35:1813-1817 (1992).
Carroll et al. "Cocaine Receptor: Biochemical Characterization and Structure-Activity Relationships of Cocaine Analogues at the Dopamine Transporter" J. Med. Chem., 35:969-981 (1992).
Carroll et al. "Synthesis, Ligand Binding, QSAR, and CoMFA Study of 3.beta.-(p-Substituted phenyl)tropane-2.beta.-carboxylic Acid Methyl Esters" J. Med. Chem., 34:2719-2725 (1991).
Carroll et al. "Synthesis and Ligand Binding of Cocaine Isomers at the Cocaine Receptor" J. Med. Chem., 34:883-886 (1991).
Chen et al. "In Vivo Binding, Internalization, and Dopamine-Releasing Effects of [H-3]-CFT (WIN 35,428): A Potential Brain Imaging Ligand for Dopamine Transporter or Cocaine . . . " Soc. Neuro. Abs., 16:309.5 (1990).
Clarke et al. "(2-exo-3-endo)-2-Aryltropane-3-carboxylic Esters, a New Class of Narcotic Antagonists" J. Med. Chem., 21:1235-1242 (1978).
Clarke et al. "Compounds Affecting the Central Nervous System. 4. 3.beta.-Phenyltropane-2-carboxylic Esters and Analogs" J. Med. Chem., 16:1260-1267 (1973).
Cline et al. "Behavior Effects of Novel Cocaine Analogs: A Comparison with in Vivo Receptor Binding Potency" J. Pharm. & Exp. Therapeutics, 260:1174-1179 (1992).
Daum et al. "Compounds Affecting the Central Nervous System. 3..sup.1 3.beta.-Phenyltropan-2-ols" J. Med. Chem., 16:667-670 (1973).
Elmaleh et al. "N-[C-11]-Methyl-2B-Carbomethoxy-3B-Phenyl Tropane [C-11]PT) and Glucose Utilization in a Primate Model of Huntington's Disease" J. Nuclear Med. Abs., 32:552 (1991).
Elmaleh et al. "Preparation and In Vivo Imaging of N-[C-11]-Methyl-2-Carbomethoxy-3-Phenyl Tropane ([C-11]PT) in Monkey Brain" J. Nuclear Med. Abs., 32:1009 (1991).
Elmaleh et al. "PET Imaging Probes for the Cocaine Receptors: A Validation Study in a Nonhuman Primate Model" J. Nuclear Med. Abs., 33:946 (1992).
Goodman et al. "Radioiodinated 2.beta.-Carbomethoxy-3.beta.-(4-Chlorophenyl)-8-(3E-and 3Z-Iodopropen-2-YL)Nortropanes: Synthesis of Potential Radioligands for Mapping Cocaine Receptor . . . " J. Nuclear Med. Abs., 33:890 (1992).
Hantraye et al. "Dopamine Fiber Detection by [.sup.11 C]-CFT and PET in a Primate Model of Parkinsonism" Clin. Neurosci. and Neuropath., 3:265-268 (1992).
Hillier "WIN-35,428" Drugs of the Future, 5:459-460 (1980).
Horn "Dopamine Uptake: A Review of Progress in the Last Decade" Progress in Neurobiology, 34:387-400 (1990).
Innis et al. "Single Photon Emission Tomography Imaging of Monoamine Reuptake Sites in Primate Brain with [.sup.123 I]CIT" Eur. J. of Pharmacol., 200:369-370 (1991).
Kaufman et al. "Severe Depletion of Cocaine Recognition Sites Associated With the Dopamine Transporter in Parkinson's-Diseased Striatum" Synapse, 9:43-49 (1991).
Kitayama et al. "Dopamine Transporter Site-Directed Mutations Differentially Alter Substrate Transport and Cocaine Binding" Proc. Natl. Acad. Sci., 89:7782-7785 (1992).
Kline, Jr. et al. "Synthesis of 3-Arlecgonine Analogues as Inhibitors of Cocaine Binding and Dopamine Uptake" J. Med. Chem., 33:2024-2027 (1990).
Leete "2-Carbomethoxy-3-tropinone: An Advanced Intermediate in the Biosynthesis of Cocaine" J. Amer. Chem. Soc., 83:6727-6728 (1983).
Madras ".sup.11 C-WIN 35,248 for Detecting Dopamine Depletion in Mild Parkinson's Disease" Annals of Neuro., 35:376-379 (1994).
Madras et al. "Stereoselective [3H]-Cocaine Binding to Membranes of Monkey Caudate-Putamen" Drug Abuse II Abs., A197, Paper No. 135.9.
Madras et al. "N-Modified Fluorophenyltropane Analogs of Cocaine With High Affinity for Cocaine Receptors" Pharmacol. Biochem. & Behav., 35:949-953 (1990).
Madras et al. "[.sup.3 H]CFT: A Novel High Affinity Ligand for Cocaine Receptors" Soc. for Neurosci. Abstracts, 15:803 (1989).
Madras et al. "Cocaine Receptors Labeled by [3H]2.beta.-Carbomethoxy-3.beta.-(4-fluorophenyl)tropane" Molecular Pharmacology, 36:518-524 (1989).
Madras et al. "[3H](-)-Cocaine Binding to Membranes of Monkey Striatum" FASEB J. Abstracts, 2:A1137 (1988).
Meltzer et al. "Substituted 3-Phenyltropane Analogs of Cocaine: Synthesis, Inhibition of Binding at Cocaine Recognition Sites, and Position Emission Tomography Imaging" J. Med. Chem., 36:855-862 (1993).
Milius et al. "Synthesis and Receptor Binding of N-Substituted Tropane Derivatives. High-Affinity Ligands for the Cocaine Receptor" J. Med. Chem., 34:1728-1731 (1991).
Milius et al., "[3H]-CFT, A High-Affinity Probe for the Cocaine Receptor" Amer. Chem. Soc. Abstract, 199:1 (1990).
Neumeyer et al. "[.sup.123 I]-2.beta.-Carbomethoxy-3.beta.-(4-iodophenyl) tropane: High-Affinity SPECT Radiotracer of Monoaminie Reuptake Sites in Brain" J. Med. Chem., 34:3144-3146 (1991).
Patel et al. "A Cocaine Analog and a GBR Analog Label the Same Protein in Rat Striatal Membranes" Brain Res., 576:173-174 (1992).
Reith et al. "Radiolabeling of Dopamine Uptake Sites in Mouse Striatum: Comparison of Binding Sites for Cocaine, Mazindol, and GBR 12935" Arch. of Pharmacol., 345:309-318 (1992).
Ritz et al. "Cocaine Inhibition of Ligand Binding at Dopamine, Norepinephrine and Serotonin Transporters: A Structure-Activity Study" Life Sciences, 46:635-645 (1990).
Rubenstein "III Imaging With Photons" Scientific American, 1/88:1-14 (1988).
Scheffel et al. "In Vivo Labeling of Cocaine Binding Sites on Dopamine Transporters with [.sup.3 H] WIN 35,428" J. Pharmacol. & Exper. Therapeutics, 257:954-958 (1991).
Scheffel et al. "Cocaine Receptors: In Vivo Labeling With .sup.3 H-(-)Cocaine, .sup.3 H-WIN 35,065-2, and .sup.3 H-WIN 35,428"Synapse, 4:390-392 (1989).
Spealman et al. "Self-Administration of the 2.beta.-Carbomethoxy-3.beta.(4-Fluorophenyl)Tropane" Pharmacol. Biochem. & Behavior, 39:1011-1013 (1991).
Zakusov et al. "Pharmacology of New Tropan Derivatives" Pharm. Ther., 32:327-337 (1987).
Cutting W. C. in `The actions and uses of drugs. Handbook of Pharmacology.` Appleton-Century-Crofts N.Y. 1969.
Van der Zee et al., "A comparison of the inhibitory effects of aromatic substituted benzhydryl . . . into synaptosomal preparations of the rat brain", Neuropharmacology, 17(7), 483-90, 1978.

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