- PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS
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Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
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Page/Page column 12
(2010/03/02)
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- Reactions of dimethoxycarbene with carbon-sulfur double bonds
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Unlike electrophilic carbenes, which react at sulfur to produce thiocarbonyl ylide intermediates, dimethoxycarbene (DMC), generated by thermolysis of an oxadiazoline at 110°C in benzene in a sealed tube, reacts at carbon, possibly to generate a zwitterionic intermediate, or at both carbon and sulfur in a concerted process that generates a thiirane. In case of the strained 2,2,4,4-tetramethylcyclobutane-1,3-dithione (2), an assumed zwitterion undergoes ring expansion. In analogous reactions, unstrained thiones afford thiiranes, possibly by ring closure of the postulated intermediates or by concerted addition. Desulfurization of thiiranes, which occurs spontaneously in some instances, results in the formation of ketene acetals, many of which hydrolyze during workup. O-Alkyl thioesters and xanthates react to afford products via insertion of the DMC into Csp2-O or Csp2-S bonds, respectively. Copyright
- Dawid, Malgorzata,Reid, Darren L.,Warkentin, John,Mloston, Grzegorz
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- Reactions of dimethoxycarbene with thiocarbonyl compounds
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A diverse sample of thiocarbonyl compounds were examined to determine what the ultimate stable products are of their reactions with dimethoxycarbene. Those ultimate products can be significantly different for an oxyphosphinyl dithioformate, methyl dithiobenzoate, O-methyl thiobenzoate, and dimethyl xanthate.
- Dawid, Malgorzata,Mloston, Grzegorz,Reid, Darren L.,Warkentin, John
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p. 1025 - 1028
(2007/10/03)
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- Deprotonative Friedel-Crafts Alkylation of Arylsilanes with α-Chlorosulfides
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Friedel-Crafts alkylation of trimethylphenylsilane with methyl chloro(methylthio)acetate in the presence of tin(IV) chloride gave a mixture of three regioisomers of methyl 2-(trimethylsilylphenyl)-2-(methylthio)acetates in which the meta- and para-isomers
- Ishibashi, Hiroyuki,Salasjota. Jorpsjo,Ikeda, Masazumi
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p. 1953 - 1958
(2007/10/02)
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