- SUBSTITUTED 2-AZABICYCLO[3.1.1]HEPTANE AND 2-AZABICYCLO[3.2.1]OCTANE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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There is provided a compound of formula (I), wherein L1 to L3, R1 to R4, X, A and B have meanings given in the description, and pharmaceutically acceptable salts, solvates and prodrugs thereof, which compounds are useful as antagonists of the orexin-1 and orexin-2 receptors or as selective antagonists of the orexin-1 receptor, and thus, in particular, in the treatment or prevention of inter alia substance dependence, addiction, anxiety disorders, panic disorders, binge eating, compulsive disorders, impulse control disorders, cognitive impairment and Alzheimer's disease.
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Page/Page column 128
(2019/03/17)
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- 2-AZABICYCLO[3.1.1] DERIVATIVES AS ANTAGONISTS OF THE OREXIN-1 AND OREXIN-2 RECEPTORS
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There is provided a compound of formula I, wherein L1, R1, R2, R5, X, A and B have meanings given in the description, and pharmaceutically acceptable salts, solvates and prodrugs thereof, which compounds are useful as antagonists of the orexin-1 and orexin-2 receptors or as selective antagonists of the orexin-1 receptor, and thus, in particular, in the treatment or prevention of inter alia substance dependence, addiction, anxiety disorders, panic disorders, binge eating, compulsive disorders, impulse control disorders, cognitive impairment and Alzheimer's disease.
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Page/Page column 78; 79
(2019/05/15)
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- Novel generation of azomethine imines from α-silylnitrosamines by 1,4- silatropic shift and their cycloaddition
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Novel and facile generation of azomethine imines from α- silylnitrosamines and subsequent cycloaddition with dipolarophiles leading to a variety of pyrazole derivatives have been developed. The key to the reaction is a 1,4-silatropic shift caused by stron
- Washizuka, Ken-Ichi,Nagai, Keiko,Minakata, Satoshi,Ryu, Ilhyong,Komatsu, Mitsuo
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p. 8849 - 8853
(2007/10/03)
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- Action of Diazomethane on Methyl (Z(or E))-2-(Acylamino)cinnamates. A New Route to Methyl (Z)-2-(Acylamino)-3-methylcinnamates
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Diazomethane reacts with methyl (Z(or E))-2-acetamido(or benzamido)cinnamates (1,2) to afford regio- and stereospecifically (Z(or E))-4-phenyl-3-acetamido(or benzamido)-3-carbomethoxy-Δ1-pyrazolines (3,4). 3Z and 4Z undergo pyrolysis to afford
- Cativiela, Carlos,Villegas, Maria D. Diaz de,Mayoral, Jose A.,Melendez, Enrique
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p. 3167 - 3169
(2007/10/02)
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- Studies on Organic Fluorine Compounds. XLII. Synthesis and Reactions of Phenyltrifluoromethylacetylenes
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Phenyltrifluoromethylacetylene (4a) was synthesized by the pyrolysis of triphenylphosphonium α-(trifluoroacetyl)benzylide (3a), which was easily derived from benzyl halide (1a).This method can be used for the synthesis of 4-substituted-phenyltrifluoromethylacetylenes (4).The 1,3-dipolar reaction of 4 with diazomethane and phenyl azide proceeds readily to give trifluoromethylated pyrazoles and triazoles.Keywords - trifluoromethyl; acetylene; 1,3-dipolar reaction; intramolecular Wittig reaction; trifluoroacetylphosphonium ylide; pyrazole; diazomethane; phenyl azide
- Kobayashi, Yoshiro,Yamashita, Toshinori,Takahashi, Katsuhiro,Kuroda, Hisashi,Kumadaki, Itsumaro
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p. 4402 - 4409
(2007/10/02)
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